Ligand source activities (1 row/activity)





Ligands Receptor Assay information Chemical information
Sel. page Common
name
GPCRdb ID #Vendors Reference
ligand
Fold selectivity
(Potency)
# tested GPCRs
(Potency)
Species p-value
(-log)
Type Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI
164617688 187927 0 None 416 2 Human 11.0 pEC50 = 11.0 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 368 7 5 5 2.6 CC(CCc1ccc(O)cc1)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
CHEMBL4847536 187927 0 None 416 2 Human 11.0 pEC50 = 11.0 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 368 7 5 5 2.6 CC(CCc1ccc(O)cc1)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
CHEMBL5028449 187927 0 None 416 2 Human 11.0 pEC50 = 11.0 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 368 7 5 5 2.6 CC(CCc1ccc(O)cc1)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
164622954 187971 0 None 245 2 Human 10.9 pEC50 = 10.9 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 400 7 4 4 3.9 CC(C)(CCc1ccc(Cl)cc1)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
CHEMBL4871708 187971 0 None 245 2 Human 10.9 pEC50 = 10.9 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 400 7 4 4 3.9 CC(C)(CCc1ccc(Cl)cc1)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
CHEMBL5028726 187971 0 None 245 2 Human 10.9 pEC50 = 10.9 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 400 7 4 4 3.9 CC(C)(CCc1ccc(Cl)cc1)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
164625303 187994 0 None 316 2 Human 10.9 pEC50 = 10.9 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 366 7 4 4 3.2 Cc1cccc(CCC(C)NCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1016/j.ejmech.2021.113697
CHEMBL4873082 187994 0 None 316 2 Human 10.9 pEC50 = 10.9 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 366 7 4 4 3.2 Cc1cccc(CCC(C)NCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1016/j.ejmech.2021.113697
CHEMBL5028871 187994 0 None 316 2 Human 10.9 pEC50 = 10.9 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 366 7 4 4 3.2 Cc1cccc(CCC(C)NCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1016/j.ejmech.2021.113697
164617772 187929 0 None 173 2 Human 10.9 pEC50 = 10.9 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 368 7 5 5 2.6 CC(CCc1cccc(O)c1)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
CHEMBL4848793 187929 0 None 173 2 Human 10.9 pEC50 = 10.9 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 368 7 5 5 2.6 CC(CCc1cccc(O)c1)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
CHEMBL5028458 187929 0 None 173 2 Human 10.9 pEC50 = 10.9 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 368 7 5 5 2.6 CC(CCc1cccc(O)c1)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
164615126 187910 0 None 104 2 Human 10.8 pEC50 = 10.8 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 382 8 4 5 2.9 COc1ccccc1CCC(C)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
CHEMBL4854569 187910 0 None 104 2 Human 10.8 pEC50 = 10.8 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 382 8 4 5 2.9 COc1ccccc1CCC(C)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
CHEMBL5028293 187910 0 None 104 2 Human 10.8 pEC50 = 10.8 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 382 8 4 5 2.9 COc1ccccc1CCC(C)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
156010908 177748 0 None 2238 2 Human 10.8 pEC50 = 10.8 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 386 7 5 6 2.5 CC(C)(CCc1cccc(O)c1)NC[C@H](O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmc.2019.115178
CHEMBL4634131 177748 0 None 2238 2 Human 10.8 pEC50 = 10.8 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 386 7 5 6 2.5 CC(C)(CCc1cccc(O)c1)NC[C@H](O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmc.2019.115178
CHEMBL4651173 177748 0 None 2238 2 Human 10.8 pEC50 = 10.8 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 386 7 5 6 2.5 CC(C)(CCc1cccc(O)c1)NC[C@H](O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmc.2019.115178
164623230 187976 0 None 1479 2 Human 10.8 pEC50 = 10.8 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 380 7 4 4 3.6 Cc1ccc(CCC(C)(C)NCC(O)c2ccc(O)c3[nH]c(=O)ccc23)cc1 10.1016/j.ejmech.2021.113697
CHEMBL4865710 187976 0 None 1479 2 Human 10.8 pEC50 = 10.8 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 380 7 4 4 3.6 Cc1ccc(CCC(C)(C)NCC(O)c2ccc(O)c3[nH]c(=O)ccc23)cc1 10.1016/j.ejmech.2021.113697
CHEMBL5028744 187976 0 None 1479 2 Human 10.8 pEC50 = 10.8 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 380 7 4 4 3.6 Cc1ccc(CCC(C)(C)NCC(O)c2ccc(O)c3[nH]c(=O)ccc23)cc1 10.1016/j.ejmech.2021.113697
164618278 187932 0 None 389 2 Human 10.8 pEC50 = 10.8 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 366 7 4 4 3.2 Cc1ccccc1CCC(C)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
CHEMBL4848018 187932 0 None 389 2 Human 10.8 pEC50 = 10.8 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 366 7 4 4 3.2 Cc1ccccc1CCC(C)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
CHEMBL5028489 187932 0 None 389 2 Human 10.8 pEC50 = 10.8 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 366 7 4 4 3.2 Cc1ccccc1CCC(C)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
164615492 187915 0 None 120 2 Human 10.8 pEC50 = 10.8 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 380 7 4 4 3.6 Cc1ccccc1CCC(C)(C)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
CHEMBL4848704 187915 0 None 120 2 Human 10.8 pEC50 = 10.8 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 380 7 4 4 3.6 Cc1ccccc1CCC(C)(C)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
CHEMBL5028319 187915 0 None 120 2 Human 10.8 pEC50 = 10.8 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 380 7 4 4 3.6 Cc1ccccc1CCC(C)(C)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
164623105 187973 0 None 47 2 Human 10.8 pEC50 = 10.8 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 400 7 4 4 3.9 CC(C)(CCc1ccc(Cl)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
CHEMBL4862449 187973 0 None 47 2 Human 10.8 pEC50 = 10.8 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 400 7 4 4 3.9 CC(C)(CCc1ccc(Cl)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
CHEMBL5028738 187973 0 None 47 2 Human 10.8 pEC50 = 10.8 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 400 7 4 4 3.9 CC(C)(CCc1ccc(Cl)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
164611794 187881 0 None 131 2 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 382 7 5 5 3.0 CC(C)(CCc1cccc(O)c1)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
CHEMBL4854261 187881 0 None 131 2 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 382 7 5 5 3.0 CC(C)(CCc1cccc(O)c1)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
CHEMBL5028104 187881 0 None 131 2 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 382 7 5 5 3.0 CC(C)(CCc1cccc(O)c1)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
164612025 187883 0 None 2454 2 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 382 8 4 5 2.9 COc1ccc(CCC(C)NCC(O)c2ccc(O)c3[nH]c(=O)ccc23)cc1 10.1016/j.ejmech.2021.113697
CHEMBL4860454 187883 0 None 2454 2 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 382 8 4 5 2.9 COc1ccc(CCC(C)NCC(O)c2ccc(O)c3[nH]c(=O)ccc23)cc1 10.1016/j.ejmech.2021.113697
CHEMBL5028117 187883 0 None 2454 2 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 382 8 4 5 2.9 COc1ccc(CCC(C)NCC(O)c2ccc(O)c3[nH]c(=O)ccc23)cc1 10.1016/j.ejmech.2021.113697
164618895 187940 0 None 95 2 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 400 7 4 4 3.9 CC(C)(CCc1ccccc1Cl)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
CHEMBL4868938 187940 0 None 95 2 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 400 7 4 4 3.9 CC(C)(CCc1ccccc1Cl)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
CHEMBL5028525 187940 0 None 95 2 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 400 7 4 4 3.9 CC(C)(CCc1ccccc1Cl)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
164610792 187874 0 None 134 2 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 380 7 4 4 3.6 Cc1cccc(CCC(C)(C)NCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1016/j.ejmech.2021.113697
CHEMBL4855974 187874 0 None 134 2 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 380 7 4 4 3.6 Cc1cccc(CCC(C)(C)NCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1016/j.ejmech.2021.113697
CHEMBL5028040 187874 0 None 134 2 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 380 7 4 4 3.6 Cc1cccc(CCC(C)(C)NCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1016/j.ejmech.2021.113697
11504295 2867 40 None 1047 2 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at beta2 adrenoceptor (unknown origin)Agonist activity at beta2 adrenoceptor (unknown origin)
ChEMBL 386 7 4 6 2.4 COc1ccc(cc1)CC(NC[C@@H](c1cc(O)cc2c1OCC(=O)N2)O)(C)C 10.1021/acs.jmedchem.0c01195
4814 2867 40 None 1047 2 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at beta2 adrenoceptor (unknown origin)Agonist activity at beta2 adrenoceptor (unknown origin)
ChEMBL 386 7 4 6 2.4 COc1ccc(cc1)CC(NC[C@@H](c1cc(O)cc2c1OCC(=O)N2)O)(C)C 10.1021/acs.jmedchem.0c01195
7543 2867 40 None 1047 2 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at beta2 adrenoceptor (unknown origin)Agonist activity at beta2 adrenoceptor (unknown origin)
ChEMBL 386 7 4 6 2.4 COc1ccc(cc1)CC(NC[C@@H](c1cc(O)cc2c1OCC(=O)N2)O)(C)C 10.1021/acs.jmedchem.0c01195
CHEMBL605846 2867 40 None 1047 2 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at beta2 adrenoceptor (unknown origin)Agonist activity at beta2 adrenoceptor (unknown origin)
ChEMBL 386 7 4 6 2.4 COc1ccc(cc1)CC(NC[C@@H](c1cc(O)cc2c1OCC(=O)N2)O)(C)C 10.1021/acs.jmedchem.0c01195
DB09080 2867 40 None 1047 2 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at beta2 adrenoceptor (unknown origin)Agonist activity at beta2 adrenoceptor (unknown origin)
ChEMBL 386 7 4 6 2.4 COc1ccc(cc1)CC(NC[C@@H](c1cc(O)cc2c1OCC(=O)N2)O)(C)C 10.1021/acs.jmedchem.0c01195
9957764 88265 0 None - 1 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
ChEMBL 503 11 6 6 3.6 COc1ccccc1CNC(=O)c1cc2cc(C[C@@H](C)NC[C@H](O)c3ccc(O)c(CO)c3)ccc2[nH]1 10.1016/j.bmcl.2007.09.031
CHEMBL236039 88265 0 None - 1 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
ChEMBL 503 11 6 6 3.6 COc1ccccc1CNC(=O)c1cc2cc(C[C@@H](C)NC[C@H](O)c3ccc(O)c(CO)c3)ccc2[nH]1 10.1016/j.bmcl.2007.09.031
11259765 85569 0 None - 1 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human recombinant beta-2 adrenoceptor expressed in CHO cells assessed as elevation of cAMPAgonist activity at human recombinant beta-2 adrenoceptor expressed in CHO cells assessed as elevation of cAMP
ChEMBL 462 11 5 5 3.4 CC(C)(Cc1cccc(CC(=O)NCc2ccccc2)c1)NC[C@H](O)c1ccc(O)c(CO)c1 10.1016/j.bmcl.2007.04.081
CHEMBL230486 85569 0 None - 1 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human recombinant beta-2 adrenoceptor expressed in CHO cells assessed as elevation of cAMPAgonist activity at human recombinant beta-2 adrenoceptor expressed in CHO cells assessed as elevation of cAMP
ChEMBL 462 11 5 5 3.4 CC(C)(Cc1cccc(CC(=O)NCc2ccccc2)c1)NC[C@H](O)c1ccc(O)c(CO)c1 10.1016/j.bmcl.2007.04.081
11621158 16508 0 None - 1 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 575 12 6 7 3.6 CC(C)(Cc1cccc(CC(=O)NCc2ccc(O)cc2Cl)c1)NC[C@H](O)c1ccc(O)c(NS(C)(=O)=O)c1 10.1021/jm1005989
CHEMBL1242943 16508 0 None - 1 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 575 12 6 7 3.6 CC(C)(Cc1cccc(CC(=O)NCc2ccc(O)cc2Cl)c1)NC[C@H](O)c1ccc(O)c(NS(C)(=O)=O)c1 10.1021/jm1005989
155517986 169629 0 None 478630 2 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 366 7 4 4 3.3 CC(C)(CCc1ccccc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.bmc.2018.10.043
CHEMBL4445289 169629 0 None 478630 2 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 366 7 4 4 3.3 CC(C)(CCc1ccccc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.bmc.2018.10.043
155517986 169629 0 None 478630 2 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 366 7 4 4 3.3 CC(C)(CCc1ccccc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.bmc.2018.10.043
CHEMBL4445289 169629 0 None 478630 2 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 366 7 4 4 3.3 CC(C)(CCc1ccccc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.bmc.2018.10.043
164621302 187956 0 None 120 2 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 382 8 4 5 2.9 COc1cccc(CCC(C)NCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1016/j.ejmech.2021.113697
CHEMBL4863282 187956 0 None 120 2 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 382 8 4 5 2.9 COc1cccc(CCC(C)NCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1016/j.ejmech.2021.113697
CHEMBL5028641 187956 0 None 120 2 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 382 8 4 5 2.9 COc1cccc(CCC(C)NCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1016/j.ejmech.2021.113697
164623918 187983 0 None 199 2 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 374 7 4 4 2.8 O=c1ccc2c(C(O)CNCCCc3cc(F)cc(F)c3)ccc(O)c2[nH]1 10.1016/j.ejmech.2021.113697
CHEMBL4872480 187983 0 None 199 2 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 374 7 4 4 2.8 O=c1ccc2c(C(O)CNCCCc3cc(F)cc(F)c3)ccc(O)c2[nH]1 10.1016/j.ejmech.2021.113697
CHEMBL5028793 187983 0 None 199 2 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 374 7 4 4 2.8 O=c1ccc2c(C(O)CNCCCc3cc(F)cc(F)c3)ccc(O)c2[nH]1 10.1016/j.ejmech.2021.113697
44434130 88268 0 None - 1 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
ChEMBL 487 10 5 5 3.9 C[C@H](Cc1ccc2[nH]c(C(=O)N(C)Cc3ccccc3)cc2c1)NC[C@H](O)c1ccc(O)c(CO)c1 10.1016/j.bmcl.2007.09.031
CHEMBL236041 88268 0 None - 1 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
ChEMBL 487 10 5 5 3.9 C[C@H](Cc1ccc2[nH]c(C(=O)N(C)Cc3ccccc3)cc2c1)NC[C@H](O)c1ccc(O)c(CO)c1 10.1016/j.bmcl.2007.09.031
164615222 187912 0 None 91 2 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 396 8 4 5 3.3 COc1ccccc1CCC(C)(C)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
CHEMBL4857267 187912 0 None 91 2 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 396 8 4 5 3.3 COc1ccccc1CCC(C)(C)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
CHEMBL5028301 187912 0 None 91 2 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 396 8 4 5 3.3 COc1ccccc1CCC(C)(C)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
164622827 187969 0 None 26 2 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 400 7 4 4 3.9 CC(C)(CCc1cccc(Cl)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
CHEMBL4868585 187969 0 None 26 2 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 400 7 4 4 3.9 CC(C)(CCc1cccc(Cl)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
CHEMBL5028721 187969 0 None 26 2 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 400 7 4 4 3.9 CC(C)(CCc1cccc(Cl)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
11455274 16530 0 None - 1 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 525 12 5 6 3.3 CC(C)(Cc1cccc(CC(=O)NCc2ccccc2)c1)NC[C@H](O)c1ccc(O)c(NS(C)(=O)=O)c1 10.1021/jm1005989
CHEMBL1243189 16530 0 None - 1 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 525 12 5 6 3.3 CC(C)(Cc1cccc(CC(=O)NCc2ccccc2)c1)NC[C@H](O)c1ccc(O)c(NS(C)(=O)=O)c1 10.1021/jm1005989
164624634 187990 0 None 131 2 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 370 7 4 4 3.0 CC(CCc1cccc(F)c1)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
CHEMBL4868684 187990 0 None 131 2 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 370 7 4 4 3.0 CC(CCc1cccc(F)c1)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
CHEMBL5028836 187990 0 None 131 2 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 370 7 4 4 3.0 CC(CCc1cccc(F)c1)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
156014115 177705 0 None 58 2 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 400 8 4 6 2.8 COc1ccccc1CCC(C)(C)NC[C@H](O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmc.2019.115178
CHEMBL4635163 177705 0 None 58 2 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 400 8 4 6 2.8 COc1ccccc1CCC(C)(C)NC[C@H](O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmc.2019.115178
CHEMBL4650951 177705 0 None 58 2 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 400 8 4 6 2.8 COc1ccccc1CCC(C)(C)NC[C@H](O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmc.2019.115178
11214499 85571 0 None - 1 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 516 11 5 5 4.3 C[C@H](Cc1cccc(CC(=O)NCc2ccc(Cl)c(Cl)c2)c1)NC[C@H](O)c1ccc(O)c(CO)c1 10.1021/jm1005989
CHEMBL230490 85571 0 None - 1 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 516 11 5 5 4.3 C[C@H](Cc1cccc(CC(=O)NCc2ccc(Cl)c(Cl)c2)c1)NC[C@H](O)c1ccc(O)c(CO)c1 10.1021/jm1005989
164608750 187864 0 None 181 2 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 356 7 4 4 2.6 O=c1ccc2c(C(O)CNCCCc3cccc(F)c3)ccc(O)c2[nH]1 10.1016/j.ejmech.2021.113697
CHEMBL4846631 187864 0 None 181 2 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 356 7 4 4 2.6 O=c1ccc2c(C(O)CNCCCc3cccc(F)c3)ccc(O)c2[nH]1 10.1016/j.ejmech.2021.113697
CHEMBL5027923 187864 0 None 181 2 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 356 7 4 4 2.6 O=c1ccc2c(C(O)CNCCCc3cccc(F)c3)ccc(O)c2[nH]1 10.1016/j.ejmech.2021.113697
156015148 177700 0 None 208 2 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 386 7 5 6 2.5 CC(C)(CCc1ccc(O)cc1)NC[C@H](O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmc.2019.115178
CHEMBL4646881 177700 0 None 208 2 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 386 7 5 6 2.5 CC(C)(CCc1ccc(O)cc1)NC[C@H](O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmc.2019.115178
CHEMBL4650929 177700 0 None 208 2 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 386 7 5 6 2.5 CC(C)(CCc1ccc(O)cc1)NC[C@H](O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmc.2019.115178
164620479 187949 0 None 288 2 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 396 8 4 5 3.3 COc1cccc(CCC(C)(C)NCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1016/j.ejmech.2021.113697
CHEMBL4863847 187949 0 None 288 2 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 396 8 4 5 3.3 COc1cccc(CCC(C)(C)NCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1016/j.ejmech.2021.113697
CHEMBL5028596 187949 0 None 288 2 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 396 8 4 5 3.3 COc1cccc(CCC(C)(C)NCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1016/j.ejmech.2021.113697
11249243 16527 0 None - 1 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 511 12 5 6 2.9 C[C@H](Cc1cccc(CC(=O)NCc2ccccc2)c1)NC[C@H](O)c1ccc(O)c(NS(C)(=O)=O)c1 10.1021/jm1005989
CHEMBL1243158 16527 0 None - 1 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 511 12 5 6 2.9 C[C@H](Cc1cccc(CC(=O)NCc2ccccc2)c1)NC[C@H](O)c1ccc(O)c(NS(C)(=O)=O)c1 10.1021/jm1005989
156015482 177667 0 None 204 2 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 400 8 4 6 2.8 COc1cccc(CCC(C)(C)NC[C@H](O)c2cc(O)cc3c2OCC(=O)N3)c1 10.1016/j.bmc.2019.115178
CHEMBL4641262 177667 0 None 204 2 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 400 8 4 6 2.8 COc1cccc(CCC(C)(C)NC[C@H](O)c2cc(O)cc3c2OCC(=O)N3)c1 10.1016/j.bmc.2019.115178
CHEMBL4650664 177667 0 None 204 2 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 400 8 4 6 2.8 COc1cccc(CCC(C)(C)NC[C@H](O)c2cc(O)cc3c2OCC(=O)N3)c1 10.1016/j.bmc.2019.115178
164619360 187943 0 None 371 2 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 370 7 4 4 3.0 CC(CCc1ccc(F)cc1)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
CHEMBL4868763 187943 0 None 371 2 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 370 7 4 4 3.0 CC(CCc1ccc(F)cc1)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
CHEMBL5028547 187943 0 None 371 2 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 370 7 4 4 3.0 CC(CCc1ccc(F)cc1)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
164623544 187979 0 None 2754 2 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 406 7 4 4 3.5 O=c1ccc2c(C(O)CNCCCc3cccc(C(F)(F)F)c3)ccc(O)c2[nH]1 10.1016/j.ejmech.2021.113697
CHEMBL4872653 187979 0 None 2754 2 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 406 7 4 4 3.5 O=c1ccc2c(C(O)CNCCCc3cccc(C(F)(F)F)c3)ccc(O)c2[nH]1 10.1016/j.ejmech.2021.113697
CHEMBL5028764 187979 0 None 2754 2 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 406 7 4 4 3.5 O=c1ccc2c(C(O)CNCCCc3cccc(C(F)(F)F)c3)ccc(O)c2[nH]1 10.1016/j.ejmech.2021.113697
164612078 187884 0 None 64 2 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 382 8 4 5 2.9 COc1ccccc1CC[C@@H](C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
CHEMBL4848617 187884 0 None 64 2 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 382 8 4 5 2.9 COc1ccccc1CC[C@@H](C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
CHEMBL5028119 187884 0 None 64 2 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 382 8 4 5 2.9 COc1ccccc1CC[C@@H](C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
156014817 177719 0 None 134 2 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 400 8 4 6 2.8 COc1ccccc1CCC(C)(C)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmc.2019.115178
CHEMBL4642770 177719 0 None 134 2 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 400 8 4 6 2.8 COc1ccccc1CCC(C)(C)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmc.2019.115178
CHEMBL4650993 177719 0 None 134 2 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 400 8 4 6 2.8 COc1ccccc1CCC(C)(C)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmc.2019.115178
164617235 187924 0 None 251 2 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 396 8 4 5 3.3 COc1ccc(CCC(C)(C)NCC(O)c2ccc(O)c3[nH]c(=O)ccc23)cc1 10.1016/j.ejmech.2021.113697
CHEMBL4848775 187924 0 None 251 2 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 396 8 4 5 3.3 COc1ccc(CCC(C)(C)NCC(O)c2ccc(O)c3[nH]c(=O)ccc23)cc1 10.1016/j.ejmech.2021.113697
CHEMBL5028422 187924 0 None 251 2 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 396 8 4 5 3.3 COc1ccc(CCC(C)(C)NCC(O)c2ccc(O)c3[nH]c(=O)ccc23)cc1 10.1016/j.ejmech.2021.113697
156013777 177763 0 None 134 2 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 386 7 5 6 2.5 CC(C)(CCc1cccc(O)c1)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmc.2019.115178
CHEMBL4636255 177763 0 None 134 2 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 386 7 5 6 2.5 CC(C)(CCc1cccc(O)c1)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmc.2019.115178
CHEMBL4651241 177763 0 None 134 2 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 386 7 5 6 2.5 CC(C)(CCc1cccc(O)c1)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmc.2019.115178
10390417 167191 0 None - 1 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
ChEMBL 480 10 6 7 3.0 C[C@H](Cc1ccc2[nH]c(C(=O)NCc3nccs3)cc2c1)NC[C@H](O)c1ccc(O)c(CO)c1 10.1016/j.bmcl.2007.09.031
CHEMBL430361 167191 0 None - 1 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
ChEMBL 480 10 6 7 3.0 C[C@H](Cc1ccc2[nH]c(C(=O)NCc3nccs3)cc2c1)NC[C@H](O)c1ccc(O)c(CO)c1 10.1016/j.bmcl.2007.09.031
49864395 15446 0 None - 1 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at beta 2 in human A431 cells adrenoceptor assessed as cAMP accumulationAgonist activity at beta 2 in human A431 cells adrenoceptor assessed as cAMP accumulation
ChEMBL 400 7 4 6 3.1 O=c1[nH]c2c(O)ccc([C@@H](O)CN[C@@H]3CCC[C@H]3OCc3ccccc3)c2s1 10.1016/j.bmcl.2010.06.136
CHEMBL1221680 15446 0 None - 1 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at beta 2 in human A431 cells adrenoceptor assessed as cAMP accumulationAgonist activity at beta 2 in human A431 cells adrenoceptor assessed as cAMP accumulation
ChEMBL 400 7 4 6 3.1 O=c1[nH]c2c(O)ccc([C@@H](O)CN[C@@H]3CCC[C@H]3OCc3ccccc3)c2s1 10.1016/j.bmcl.2010.06.136
11477877 16553 0 None - 1 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 517 12 5 6 3.3 C[C@H](Cc1cccc(CC(=O)NCC2CCCCC2)c1)NC[C@H](O)c1ccc(O)c(NS(C)(=O)=O)c1 10.1021/jm1005989
CHEMBL1243348 16553 0 None - 1 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 517 12 5 6 3.3 C[C@H](Cc1cccc(CC(=O)NCC2CCCCC2)c1)NC[C@H](O)c1ccc(O)c(NS(C)(=O)=O)c1 10.1021/jm1005989
13121366 176871 0 None 457 2 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 370 7 4 5 2.8 CC(C)(CCc1ccccc1)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmc.2019.115178
CHEMBL4638864 176871 0 None 457 2 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 370 7 4 5 2.8 CC(C)(CCc1ccccc1)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmc.2019.115178
164612262 187885 0 None 190 2 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 386 7 4 4 3.5 CC(CCc1ccc(Cl)cc1)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
CHEMBL4853372 187885 0 None 190 2 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 386 7 4 4 3.5 CC(CCc1ccc(Cl)cc1)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
CHEMBL5028127 187885 0 None 190 2 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 386 7 4 4 3.5 CC(CCc1ccc(Cl)cc1)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
164614743 187905 0 None 134 2 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 386 7 4 4 3.5 CC(CCc1ccccc1Cl)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
CHEMBL4860764 187905 0 None 134 2 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 386 7 4 4 3.5 CC(CCc1ccccc1Cl)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
CHEMBL5028269 187905 0 None 134 2 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 386 7 4 4 3.5 CC(CCc1ccccc1Cl)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
156014962 177665 0 None 229 2 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 400 8 4 6 2.8 COc1ccc(CCC(C)(C)NC[C@H](O)c2cc(O)cc3c2OCC(=O)N3)cc1 10.1016/j.bmc.2019.115178
CHEMBL4645203 177665 0 None 229 2 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 400 8 4 6 2.8 COc1ccc(CCC(C)(C)NC[C@H](O)c2cc(O)cc3c2OCC(=O)N3)cc1 10.1016/j.bmc.2019.115178
CHEMBL4650644 177665 0 None 229 2 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 400 8 4 6 2.8 COc1ccc(CCC(C)(C)NC[C@H](O)c2cc(O)cc3c2OCC(=O)N3)cc1 10.1016/j.bmc.2019.115178
155536314 171599 0 None 6025 2 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 354 7 5 5 2.2 O=c1ccc2c(C(O)CNCCCc3cccc(O)c3)ccc(O)c2[nH]1 10.1016/j.bmc.2018.10.043
CHEMBL4473515 171599 0 None 6025 2 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 354 7 5 5 2.2 O=c1ccc2c(C(O)CNCCCc3cccc(O)c3)ccc(O)c2[nH]1 10.1016/j.bmc.2018.10.043
155536314 171599 0 None 6025 2 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 354 7 5 5 2.2 O=c1ccc2c(C(O)CNCCCc3cccc(O)c3)ccc(O)c2[nH]1 10.1016/j.bmc.2018.10.043
CHEMBL4473515 171599 0 None 6025 2 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 354 7 5 5 2.2 O=c1ccc2c(C(O)CNCCCc3cccc(O)c3)ccc(O)c2[nH]1 10.1016/j.bmc.2018.10.043
164620585 187950 0 None 616 2 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 382 7 5 5 3.0 CC(C)(CCc1ccc(O)cc1)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
CHEMBL4866766 187950 0 None 616 2 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 382 7 5 5 3.0 CC(C)(CCc1ccc(O)cc1)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
CHEMBL5028602 187950 0 None 616 2 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 382 7 5 5 3.0 CC(C)(CCc1ccc(O)cc1)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
44434126 88267 0 None - 1 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
ChEMBL 519 11 6 6 4.3 CSc1ccccc1CNC(=O)c1cc2cc(C[C@@H](C)NC[C@H](O)c3ccc(O)c(CO)c3)ccc2[nH]1 10.1016/j.bmcl.2007.09.031
CHEMBL236040 88267 0 None - 1 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
ChEMBL 519 11 6 6 4.3 CSc1ccccc1CNC(=O)c1cc2cc(C[C@@H](C)NC[C@H](O)c3ccc(O)c(CO)c3)ccc2[nH]1 10.1016/j.bmcl.2007.09.031
10027868 144347 0 None - 1 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
ChEMBL 474 10 6 6 2.9 C[C@H](Cc1ccc2[nH]c(C(=O)NCc3ccccn3)cc2c1)NC[C@H](O)c1ccc(O)c(CO)c1 10.1016/j.bmcl.2007.09.031
CHEMBL391006 144347 0 None - 1 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
ChEMBL 474 10 6 6 2.9 C[C@H](Cc1ccc2[nH]c(C(=O)NCc3ccccn3)cc2c1)NC[C@H](O)c1ccc(O)c(CO)c1 10.1016/j.bmcl.2007.09.031
164618813 187939 0 None 275 2 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 366 7 4 4 3.2 Cc1ccc(CCC(C)NCC(O)c2ccc(O)c3[nH]c(=O)ccc23)cc1 10.1016/j.ejmech.2021.113697
CHEMBL4865833 187939 0 None 275 2 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 366 7 4 4 3.2 Cc1ccc(CCC(C)NCC(O)c2ccc(O)c3[nH]c(=O)ccc23)cc1 10.1016/j.ejmech.2021.113697
CHEMBL5028523 187939 0 None 275 2 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 366 7 4 4 3.2 Cc1ccc(CCC(C)NCC(O)c2ccc(O)c3[nH]c(=O)ccc23)cc1 10.1016/j.ejmech.2021.113697
164623433 187977 0 None 380 2 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 352 7 4 4 2.8 Cc1cccc(CCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1016/j.ejmech.2021.113697
CHEMBL4870623 187977 0 None 380 2 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 352 7 4 4 2.8 Cc1cccc(CCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1016/j.ejmech.2021.113697
CHEMBL5028756 187977 0 None 380 2 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 352 7 4 4 2.8 Cc1cccc(CCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1016/j.ejmech.2021.113697
156014983 177745 0 None 724 2 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 386 7 5 6 2.5 CC(C)(CCc1ccc(O)cc1)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmc.2019.115178
CHEMBL4644638 177745 0 None 724 2 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 386 7 5 6 2.5 CC(C)(CCc1ccc(O)cc1)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmc.2019.115178
CHEMBL4651152 177745 0 None 724 2 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 386 7 5 6 2.5 CC(C)(CCc1ccc(O)cc1)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmc.2019.115178
11261001 16531 0 None - 1 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 525 13 5 6 2.9 C[C@H](Cc1cccc(CC(=O)NCCc2ccccc2)c1)NC[C@H](O)c1ccc(O)c(NS(C)(=O)=O)c1 10.1021/jm1005989
CHEMBL1243190 16531 0 None - 1 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 525 13 5 6 2.9 C[C@H](Cc1cccc(CC(=O)NCCc2ccccc2)c1)NC[C@H](O)c1ccc(O)c(NS(C)(=O)=O)c1 10.1021/jm1005989
11489605 16538 0 None - 1 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 541 13 5 7 2.9 COc1ccccc1CNC(=O)Cc1cccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)c1 10.1021/jm1005989
CHEMBL1243256 16538 0 None - 1 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 541 13 5 7 2.9 COc1ccccc1CNC(=O)Cc1cccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)c1 10.1021/jm1005989
155533625 171301 0 None - 1 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 366 7 4 4 3.3 CC(C)(CCc1ccccc1)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.bmc.2018.10.043
CHEMBL4469364 171301 0 None - 1 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 366 7 4 4 3.3 CC(C)(CCc1ccccc1)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.bmc.2018.10.043
155564766 174906 0 None 181 2 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 368 8 4 5 2.5 COc1cccc(CCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1016/j.bmc.2018.10.043
CHEMBL4577508 174906 0 None 181 2 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 368 8 4 5 2.5 COc1cccc(CCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1016/j.bmc.2018.10.043
11489574 16535 0 None - 1 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 539 14 5 6 3.3 C[C@H](Cc1cccc(CC(=O)NCCCc2ccccc2)c1)NC[C@H](O)c1ccc(O)c(NS(C)(=O)=O)c1 10.1021/jm1005989
CHEMBL1243222 16535 0 None - 1 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 539 14 5 6 3.3 C[C@H](Cc1cccc(CC(=O)NCCCc2ccccc2)c1)NC[C@H](O)c1ccc(O)c(NS(C)(=O)=O)c1 10.1021/jm1005989
155536813 171630 0 None 263 2 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 368 8 4 5 2.5 COc1ccccc1CCCNCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.bmc.2018.10.043
CHEMBL4473790 171630 0 None 263 2 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 368 8 4 5 2.5 COc1ccccc1CCCNCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.bmc.2018.10.043
164624092 187986 0 None 794 2 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 442 10 4 7 2.9 COc1cc(CCC(C)NCC(O)c2ccc(O)c3[nH]c(=O)ccc23)cc(OC)c1OC 10.1016/j.ejmech.2021.113697
CHEMBL4865514 187986 0 None 794 2 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 442 10 4 7 2.9 COc1cc(CCC(C)NCC(O)c2ccc(O)c3[nH]c(=O)ccc23)cc(OC)c1OC 10.1016/j.ejmech.2021.113697
CHEMBL5028807 187986 0 None 794 2 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 442 10 4 7 2.9 COc1cc(CCC(C)NCC(O)c2ccc(O)c3[nH]c(=O)ccc23)cc(OC)c1OC 10.1016/j.ejmech.2021.113697
2419 3394 80 None 17 6 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmc.2019.115178
5152 3394 80 None 17 6 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmc.2019.115178
559 3394 80 None 17 6 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmc.2019.115178
CHEMBL1263 3394 80 None 17 6 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmc.2019.115178
DB00938 3394 80 None 17 6 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmc.2019.115178
11699773 16522 0 None - 1 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 569 12 6 7 3.6 Cc1cc(O)cc(C)c1CNC(=O)Cc1cccc(CC(C)(C)NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)c1 10.1021/jm1005989
CHEMBL1243101 16522 0 None - 1 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 569 12 6 7 3.6 Cc1cc(O)cc(C)c1CNC(=O)Cc1cccc(CC(C)(C)NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)c1 10.1021/jm1005989
164626310 188000 0 None 346 2 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 356 7 4 4 2.6 O=c1ccc2c(C(O)CNCCCc3ccc(F)cc3)ccc(O)c2[nH]1 10.1016/j.ejmech.2021.113697
CHEMBL4874945 188000 0 None 346 2 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 356 7 4 4 2.6 O=c1ccc2c(C(O)CNCCCc3ccc(F)cc3)ccc(O)c2[nH]1 10.1016/j.ejmech.2021.113697
CHEMBL5028930 188000 0 None 346 2 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 356 7 4 4 2.6 O=c1ccc2c(C(O)CNCCCc3ccc(F)cc3)ccc(O)c2[nH]1 10.1016/j.ejmech.2021.113697
11398811 16541 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 555 14 5 7 3.3 CCOc1ccccc1CNC(=O)Cc1cccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)c1 10.1021/jm1005989
CHEMBL1243285 16541 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 555 14 5 7 3.3 CCOc1ccccc1CNC(=O)Cc1cccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)c1 10.1021/jm1005989
155543358 174191 0 None 102 2 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 354 7 5 5 2.2 O=c1ccc2c(C(O)CNCCCc3ccccc3O)ccc(O)c2[nH]1 10.1016/j.bmc.2018.10.043
CHEMBL4561253 174191 0 None 102 2 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 354 7 5 5 2.2 O=c1ccc2c(C(O)CNCCCc3ccccc3O)ccc(O)c2[nH]1 10.1016/j.bmc.2018.10.043
156015401 177686 0 None 251 2 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 400 8 4 6 2.8 COc1cccc(CCC(C)(C)NCC(O)c2cc(O)cc3c2OCC(=O)N3)c1 10.1016/j.bmc.2019.115178
CHEMBL4645694 177686 0 None 251 2 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 400 8 4 6 2.8 COc1cccc(CCC(C)(C)NCC(O)c2cc(O)cc3c2OCC(=O)N3)c1 10.1016/j.bmc.2019.115178
CHEMBL4650809 177686 0 None 251 2 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 400 8 4 6 2.8 COc1cccc(CCC(C)(C)NCC(O)c2cc(O)cc3c2OCC(=O)N3)c1 10.1016/j.bmc.2019.115178
156015798 177693 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 400 8 4 6 2.8 COc1ccc(CCC(C)(C)NCC(O)c2cc(O)cc3c2OCC(=O)N3)cc1 10.1016/j.bmc.2019.115178
CHEMBL4649233 177693 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 400 8 4 6 2.8 COc1ccc(CCC(C)(C)NCC(O)c2cc(O)cc3c2OCC(=O)N3)cc1 10.1016/j.bmc.2019.115178
CHEMBL4650858 177693 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 400 8 4 6 2.8 COc1ccc(CCC(C)(C)NCC(O)c2cc(O)cc3c2OCC(=O)N3)cc1 10.1016/j.bmc.2019.115178
44434125 145566 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
ChEMBL 473 10 6 5 3.6 C[C@H](Cc1ccc2[nH]c(C(=O)NCc3ccccc3)cc2c1)NC[C@H](O)c1ccc(O)c(CO)c1 10.1016/j.bmcl.2007.09.031
CHEMBL391946 145566 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
ChEMBL 473 10 6 5 3.6 C[C@H](Cc1ccc2[nH]c(C(=O)NCc3ccccc3)cc2c1)NC[C@H](O)c1ccc(O)c(CO)c1 10.1016/j.bmcl.2007.09.031
44237865 57908 0 None - 1 Guinea pig 10.3 pEC50 = 10.3 Functional
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
ChEMBL 500 11 6 5 3.9 O=C(NCCCc1ccccc1)Nc1cccc(CCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1016/j.bmcl.2010.12.096
CHEMBL1682213 57908 0 None - 1 Guinea pig 10.3 pEC50 = 10.3 Functional
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
ChEMBL 500 11 6 5 3.9 O=C(NCCCc1ccccc1)Nc1cccc(CCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1016/j.bmcl.2010.12.096
155557083 173959 0 None 724 2 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 354 7 5 5 2.2 O=c1ccc2c(C(O)CNCCCc3ccc(O)cc3)ccc(O)c2[nH]1 10.1016/j.bmc.2018.10.043
CHEMBL4556022 173959 0 None 724 2 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 354 7 5 5 2.2 O=c1ccc2c(C(O)CNCCCc3ccc(O)cc3)ccc(O)c2[nH]1 10.1016/j.bmc.2018.10.043
10389119 88312 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
ChEMBL 451 10 6 5 3.2 C[C@H](Cc1ccc2[nH]c(C(=O)NCC3CCC3)cc2c1)NC[C@H](O)c1ccc(O)c(CO)c1 10.1016/j.bmcl.2007.09.031
CHEMBL236251 88312 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
ChEMBL 451 10 6 5 3.2 C[C@H](Cc1ccc2[nH]c(C(=O)NCC3CCC3)cc2c1)NC[C@H](O)c1ccc(O)c(CO)c1 10.1016/j.bmcl.2007.09.031
155564340 174841 0 None 263 2 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 493 11 5 5 4.9 CC(CC(=O)Nc1cccc(CCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1)CC(C)(C)C 10.1016/j.bmc.2018.10.043
CHEMBL4576089 174841 0 None 263 2 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 493 11 5 5 4.9 CC(CC(=O)Nc1cccc(CCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1)CC(C)(C)C 10.1016/j.bmc.2018.10.043
44434127 88165 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
ChEMBL 509 10 6 5 3.8 C[C@H](Cc1ccc2[nH]c(C(=O)NCc3c(F)cccc3F)cc2c1)NC[C@H](O)c1ccc(O)c(CO)c1 10.1016/j.bmcl.2007.09.031
CHEMBL235612 88165 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
ChEMBL 509 10 6 5 3.8 C[C@H](Cc1ccc2[nH]c(C(=O)NCc3c(F)cccc3F)cc2c1)NC[C@H](O)c1ccc(O)c(CO)c1 10.1016/j.bmcl.2007.09.031
3466 4063 38 None - 1 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 378 8 4 5 2.4 OC(c1ccc(c(c1)NS(=O)(=O)C)O)CNC(Cc1ccccc1)(C)C 10.1021/jm1005989
37990 4063 38 None - 1 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 378 8 4 5 2.4 OC(c1ccc(c(c1)NS(=O)(=O)C)O)CNC(Cc1ccccc1)(C)C 10.1021/jm1005989
CHEMBL1243407 4063 38 None - 1 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 378 8 4 5 2.4 OC(c1ccc(c(c1)NS(=O)(=O)C)O)CNC(Cc1ccccc1)(C)C 10.1021/jm1005989
1499 2052 43 None -72 36 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2019.115178
3779 2052 43 None -72 36 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2019.115178
536 2052 43 None -72 36 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2019.115178
CHEMBL434 2052 43 None -72 36 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2019.115178
DB01064 2052 43 None -72 36 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2019.115178
11376125 16546 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 539 12 5 6 3.5 Cc1ccc(CNC(=O)Cc2cccc(C[C@@H](C)NC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)c2)cc1C 10.1021/jm1005989
CHEMBL1243317 16546 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 539 12 5 6 3.5 Cc1ccc(CNC(=O)Cc2cccc(C[C@@H](C)NC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)c2)cc1C 10.1021/jm1005989
164614249 187900 0 None 295 2 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 352 7 4 4 2.8 Cc1ccccc1CCCNCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
CHEMBL4859591 187900 0 None 295 2 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 352 7 4 4 2.8 Cc1ccccc1CCCNCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
CHEMBL5028241 187900 0 None 295 2 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 352 7 4 4 2.8 Cc1ccccc1CCCNCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
10324803 89151 0 None - 1 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
ChEMBL 533 12 6 7 3.6 COc1cccc(OC)c1CNC(=O)c1cc2cc(C[C@@H](C)NC[C@H](O)c3ccc(O)c(CO)c3)ccc2[nH]1 10.1016/j.bmcl.2007.09.031
CHEMBL237501 89151 0 None - 1 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
ChEMBL 533 12 6 7 3.6 COc1cccc(OC)c1CNC(=O)c1cc2cc(C[C@@H](C)NC[C@H](O)c3ccc(O)c(CO)c3)ccc2[nH]1 10.1016/j.bmcl.2007.09.031
10390752 145711 0 None - 1 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
ChEMBL 487 10 6 5 4.1 C[C@H](Cc1ccc2[nH]c(C(=O)N[C@H](C)c3ccccc3)cc2c1)NC[C@H](O)c1ccc(O)c(CO)c1 10.1016/j.bmcl.2007.09.031
CHEMBL392056 145711 0 None - 1 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
ChEMBL 487 10 6 5 4.1 C[C@H](Cc1ccc2[nH]c(C(=O)N[C@H](C)c3ccccc3)cc2c1)NC[C@H](O)c1ccc(O)c(CO)c1 10.1016/j.bmcl.2007.09.031
16049087 63737 0 None 125 2 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 448 13 4 7 3.3 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCSCCCOCCc3ccccc3)c2s1 10.1016/j.bmcl.2011.05.097
CHEMBL1807817 63737 0 None 125 2 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 448 13 4 7 3.3 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCSCCCOCCc3ccccc3)c2s1 10.1016/j.bmcl.2011.05.097
9892481 69875 11 None -3 4 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 435 12 6 6 3.0 O=CNc1cc([C@@H](O)CNCCc2ccc(NC[C@H](O)c3ccccc3)cc2)ccc1O 10.1016/j.bmcl.2014.04.095
CHEMBL1940832 69875 11 None -3 4 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 435 12 6 6 3.0 O=CNc1cc([C@@H](O)CNCCc2ccc(NC[C@H](O)c3ccccc3)cc2)ccc1O 10.1016/j.bmcl.2014.04.095
90645347 112008 0 None 7 3 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 578 12 6 7 5.6 CC(C)(N)COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1-c1ccccc1 10.1016/j.bmcl.2014.04.095
CHEMBL3298987 112008 0 None 7 3 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 578 12 6 7 5.6 CC(C)(N)COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1-c1ccccc1 10.1016/j.bmcl.2014.04.095
9892481 69875 11 None -3 4 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 435 12 6 6 3.0 O=CNc1cc([C@@H](O)CNCCc2ccc(NC[C@H](O)c3ccccc3)cc2)ccc1O 10.1016/j.bmcl.2014.04.069
CHEMBL1940832 69875 11 None -3 4 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 435 12 6 6 3.0 O=CNc1cc([C@@H](O)CNCCc2ccc(NC[C@H](O)c3ccccc3)cc2)ccc1O 10.1016/j.bmcl.2014.04.069
9892481 69875 11 None -3 4 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 435 12 6 6 3.0 O=CNc1cc([C@@H](O)CNCCc2ccc(NC[C@H](O)c3ccccc3)cc2)ccc1O 10.1016/j.bmcl.2011.11.072
CHEMBL1940832 69875 11 None -3 4 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 435 12 6 6 3.0 O=CNc1cc([C@@H](O)CNCCc2ccc(NC[C@H](O)c3ccccc3)cc2)ccc1O 10.1016/j.bmcl.2011.11.072
11420492 154649 0 None - 1 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 492 10 5 5 3.8 C[C@H](Cc1cccc(CC(=O)NC23CC4CC(CC(C4)C2)C3)c1)NC[C@H](O)c1ccc(O)c(CO)c1 10.1021/jm1005989
CHEMBL402501 154649 0 None - 1 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 492 10 5 5 3.8 C[C@H](Cc1cccc(CC(=O)NC23CC4CC(CC(C4)C2)C3)c1)NC[C@H](O)c1ccc(O)c(CO)c1 10.1021/jm1005989
155564079 174828 0 None 97 2 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 442 8 4 4 4.9 CC(C)(CC(c1ccccc1)c1ccccc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.bmc.2018.10.043
CHEMBL4575759 174828 0 None 97 2 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 442 8 4 4 4.9 CC(C)(CC(c1ccccc1)c1ccccc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.bmc.2018.10.043
11456127 16552 0 None - 1 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 593 12 5 6 4.6 CC(C)(Cc1cccc(CC(=O)NCc2ccc(Cl)c(Cl)c2)c1)NC[C@H](O)c1ccc(O)c(NS(C)(=O)=O)c1 10.1021/jm1005989
CHEMBL1243347 16552 0 None - 1 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 593 12 5 6 4.6 CC(C)(Cc1cccc(CC(=O)NCc2ccc(Cl)c(Cl)c2)c1)NC[C@H](O)c1ccc(O)c(NS(C)(=O)=O)c1 10.1021/jm1005989
44237667 57905 0 None - 1 Guinea pig 10.2 pEC50 = 10.2 Functional
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
ChEMBL 458 8 6 5 3.7 O=C(Nc1ccccc1)Nc1cccc(CCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1016/j.bmcl.2010.12.096
CHEMBL1682210 57905 0 None - 1 Guinea pig 10.2 pEC50 = 10.2 Functional
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
ChEMBL 458 8 6 5 3.7 O=C(Nc1ccccc1)Nc1cccc(CCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1016/j.bmcl.2010.12.096
2419 3394 80 None 17 6 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2007.09.031
5152 3394 80 None 17 6 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2007.09.031
559 3394 80 None 17 6 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2007.09.031
CHEMBL1263 3394 80 None 17 6 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2007.09.031
DB00938 3394 80 None 17 6 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2007.09.031
2419 3394 80 None 17 6 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human recombinant beta-2 adrenoceptor expressed in CHO cells assessed as elevation of cAMPAgonist activity at human recombinant beta-2 adrenoceptor expressed in CHO cells assessed as elevation of cAMP
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2007.04.081
5152 3394 80 None 17 6 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human recombinant beta-2 adrenoceptor expressed in CHO cells assessed as elevation of cAMPAgonist activity at human recombinant beta-2 adrenoceptor expressed in CHO cells assessed as elevation of cAMP
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2007.04.081
559 3394 80 None 17 6 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human recombinant beta-2 adrenoceptor expressed in CHO cells assessed as elevation of cAMPAgonist activity at human recombinant beta-2 adrenoceptor expressed in CHO cells assessed as elevation of cAMP
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2007.04.081
CHEMBL1263 3394 80 None 17 6 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human recombinant beta-2 adrenoceptor expressed in CHO cells assessed as elevation of cAMPAgonist activity at human recombinant beta-2 adrenoceptor expressed in CHO cells assessed as elevation of cAMP
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2007.04.081
DB00938 3394 80 None 17 6 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human recombinant beta-2 adrenoceptor expressed in CHO cells assessed as elevation of cAMPAgonist activity at human recombinant beta-2 adrenoceptor expressed in CHO cells assessed as elevation of cAMP
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2007.04.081
2419 3394 80 None 17 6 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/jm1005989
5152 3394 80 None 17 6 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/jm1005989
559 3394 80 None 17 6 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/jm1005989
CHEMBL1263 3394 80 None 17 6 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/jm1005989
DB00938 3394 80 None 17 6 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/jm1005989
45269924 193767 0 None - 1 Guinea pig 10.1 pEC50 = 10.1 Functional
Agonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring assessed as bronchorelaxation activity against histamine-induced contractionAgonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring assessed as bronchorelaxation activity against histamine-induced contraction
ChEMBL 283 6 5 6 -0.1 CC(C)(C)NC[C@@H](O)c1ccc(OB(O)O)c(CO)c1 10.1016/j.ejmech.2008.12.016
CHEMBL552398 193767 0 None - 1 Guinea pig 10.1 pEC50 = 10.1 Functional
Agonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring assessed as bronchorelaxation activity against histamine-induced contractionAgonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring assessed as bronchorelaxation activity against histamine-induced contraction
ChEMBL 283 6 5 6 -0.1 CC(C)(C)NC[C@@H](O)c1ccc(OB(O)O)c(CO)c1 10.1016/j.ejmech.2008.12.016
164615474 187914 0 None 61 2 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 386 7 4 4 3.5 CC(CCc1cccc(Cl)c1)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
CHEMBL4847767 187914 0 None 61 2 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 386 7 4 4 3.5 CC(CCc1cccc(Cl)c1)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
CHEMBL5028315 187914 0 None 61 2 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 386 7 4 4 3.5 CC(CCc1cccc(Cl)c1)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
155548071 173167 0 None 131 2 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 338 7 4 4 2.5 O=c1ccc2c(C(O)CNCCCc3ccccc3)ccc(O)c2[nH]1 10.1016/j.bmc.2018.10.043
CHEMBL4536813 173167 0 None 131 2 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 338 7 4 4 2.5 O=c1ccc2c(C(O)CNCCCc3ccccc3)ccc(O)c2[nH]1 10.1016/j.bmc.2018.10.043
155567283 175387 0 None 588 2 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 368 8 4 5 2.5 COc1ccc(CCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)cc1 10.1016/j.bmc.2018.10.043
CHEMBL4588479 175387 0 None 588 2 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 368 8 4 5 2.5 COc1ccc(CCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)cc1 10.1016/j.bmc.2018.10.043
155548668 173201 0 None - 1 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 478 8 4 4 5.1 CC(C)(CC(c1ccc(F)cc1)c1ccc(F)cc1)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.bmc.2018.10.043
CHEMBL4537644 173201 0 None - 1 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 478 8 4 4 5.1 CC(C)(CC(c1ccc(F)cc1)c1ccc(F)cc1)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.bmc.2018.10.043
2419 3394 80 None 17 6 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmc.2018.10.043
5152 3394 80 None 17 6 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmc.2018.10.043
559 3394 80 None 17 6 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmc.2018.10.043
CHEMBL1263 3394 80 None 17 6 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmc.2018.10.043
DB00938 3394 80 None 17 6 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmc.2018.10.043
16049088 63738 0 None 100 2 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 448 13 4 7 3.3 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCCSCCOCCc3ccccc3)c2s1 10.1016/j.bmcl.2011.05.097
CHEMBL1807818 63738 0 None 100 2 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 448 13 4 7 3.3 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCCSCCOCCc3ccccc3)c2s1 10.1016/j.bmcl.2011.05.097
16049028 63739 0 None 50 3 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 462 14 4 7 3.7 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCCSCCCOCCc3ccccc3)c2s1 10.1016/j.bmcl.2011.05.097
CHEMBL1807819 63739 0 None 50 3 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 462 14 4 7 3.7 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCCSCCCOCCc3ccccc3)c2s1 10.1016/j.bmcl.2011.05.097
11592062 111952 0 None 25 3 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 550 11 6 7 5.0 COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1-c1cccc(CN)c1 10.1016/j.bmcl.2014.04.095
CHEMBL3298325 111952 0 None 25 3 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 550 11 6 7 5.0 COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1-c1cccc(CN)c1 10.1016/j.bmcl.2014.04.095
11169365 112007 0 None 22 3 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 502 11 6 7 4.0 CC(C)(N)COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 10.1016/j.bmcl.2014.04.095
CHEMBL3298986 112007 0 None 22 3 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 502 11 6 7 4.0 CC(C)(N)COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 10.1016/j.bmcl.2014.04.095
155513474 169162 0 None 83 2 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 478 8 4 4 5.1 CC(C)(CC(c1ccc(F)cc1)c1ccc(F)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.bmc.2018.10.043
CHEMBL4438531 169162 0 None 83 2 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 478 8 4 4 5.1 CC(C)(CC(c1ccc(F)cc1)c1ccc(F)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.bmc.2018.10.043
164622775 187968 0 None 120226 2 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 428 10 4 7 2.5 COc1cc(CCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)cc(OC)c1OC 10.1016/j.ejmech.2021.113697
CHEMBL4867311 187968 0 None 120226 2 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 428 10 4 7 2.5 COc1cc(CCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)cc(OC)c1OC 10.1016/j.ejmech.2021.113697
CHEMBL5028718 187968 0 None 120226 2 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 428 10 4 7 2.5 COc1cc(CCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)cc(OC)c1OC 10.1016/j.ejmech.2021.113697
11504295 2867 40 None 1047 2 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 386 7 4 6 2.4 COc1ccc(cc1)CC(NC[C@@H](c1cc(O)cc2c1OCC(=O)N2)O)(C)C 10.1016/j.ejmech.2021.113697
4814 2867 40 None 1047 2 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 386 7 4 6 2.4 COc1ccc(cc1)CC(NC[C@@H](c1cc(O)cc2c1OCC(=O)N2)O)(C)C 10.1016/j.ejmech.2021.113697
7543 2867 40 None 1047 2 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 386 7 4 6 2.4 COc1ccc(cc1)CC(NC[C@@H](c1cc(O)cc2c1OCC(=O)N2)O)(C)C 10.1016/j.ejmech.2021.113697
CHEMBL605846 2867 40 None 1047 2 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 386 7 4 6 2.4 COc1ccc(cc1)CC(NC[C@@H](c1cc(O)cc2c1OCC(=O)N2)O)(C)C 10.1016/j.ejmech.2021.113697
DB09080 2867 40 None 1047 2 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 386 7 4 6 2.4 COc1ccc(cc1)CC(NC[C@@H](c1cc(O)cc2c1OCC(=O)N2)O)(C)C 10.1016/j.ejmech.2021.113697
44237615 57907 0 None - 1 Guinea pig 10.1 pEC50 = 10.1 Functional
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
ChEMBL 486 10 6 5 3.5 O=C(NCCc1ccccc1)Nc1cccc(CCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1016/j.bmcl.2010.12.096
CHEMBL1682212 57907 0 None - 1 Guinea pig 10.1 pEC50 = 10.1 Functional
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
ChEMBL 486 10 6 5 3.5 O=C(NCCc1ccccc1)Nc1cccc(CCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1016/j.bmcl.2010.12.096
11707090 16518 0 None - 1 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 609 12 6 7 4.3 CC(C)(Cc1cccc(CC(=O)NCc2cc(Cl)c(O)c(Cl)c2)c1)NC[C@H](O)c1ccc(O)c(NS(C)(=O)=O)c1 10.1021/jm1005989
CHEMBL1243068 16518 0 None - 1 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 609 12 6 7 4.3 CC(C)(Cc1cccc(CC(=O)NCc2cc(Cl)c(O)c(Cl)c2)c1)NC[C@H](O)c1ccc(O)c(NS(C)(=O)=O)c1 10.1021/jm1005989
164623583 187981 0 None 316 2 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 352 7 4 4 2.8 Cc1ccc(CCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)cc1 10.1016/j.ejmech.2021.113697
CHEMBL4873280 187981 0 None 316 2 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 352 7 4 4 2.8 Cc1ccc(CCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)cc1 10.1016/j.ejmech.2021.113697
CHEMBL5028767 187981 0 None 316 2 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 352 7 4 4 2.8 Cc1ccc(CCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)cc1 10.1016/j.ejmech.2021.113697
11247541 85523 0 None - 1 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human recombinant beta-2 adrenoceptor expressed in CHO cells assessed as elevation of cAMPAgonist activity at human recombinant beta-2 adrenoceptor expressed in CHO cells assessed as elevation of cAMP
ChEMBL 434 11 5 5 2.6 O=C(Cc1cccc(CCNC[C@H](O)c2ccc(O)c(CO)c2)c1)NCc1ccccc1 10.1016/j.bmcl.2007.04.081
CHEMBL230203 85523 0 None - 1 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human recombinant beta-2 adrenoceptor expressed in CHO cells assessed as elevation of cAMPAgonist activity at human recombinant beta-2 adrenoceptor expressed in CHO cells assessed as elevation of cAMP
ChEMBL 434 11 5 5 2.6 O=C(Cc1cccc(CCNC[C@H](O)c2ccc(O)c(CO)c2)c1)NCc1ccccc1 10.1016/j.bmcl.2007.04.081
44425580 85570 0 None - 1 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human recombinant beta-2 adrenoceptor expressed in CHO cells assessed as elevation of cAMPAgonist activity at human recombinant beta-2 adrenoceptor expressed in CHO cells assessed as elevation of cAMP
ChEMBL 448 11 5 5 3.0 C[C@H](Cc1cccc(CC(=O)NCc2ccccc2)c1)NC[C@H](O)c1ccc(O)c(CO)c1 10.1016/j.bmcl.2007.04.081
CHEMBL230487 85570 0 None - 1 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human recombinant beta-2 adrenoceptor expressed in CHO cells assessed as elevation of cAMPAgonist activity at human recombinant beta-2 adrenoceptor expressed in CHO cells assessed as elevation of cAMP
ChEMBL 448 11 5 5 3.0 C[C@H](Cc1cccc(CC(=O)NCc2ccccc2)c1)NC[C@H](O)c1ccc(O)c(CO)c1 10.1016/j.bmcl.2007.04.081
57334265 70499 0 None - 1 Guinea pig 10.0 pEC50 = 10 Functional
Agonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contractionAgonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contraction
ChEMBL 538 13 4 8 3.4 COc1ccc(C2=NN(CCCCNC[C@H](O)c3ccc(O)c(NC=O)c3)C(=O)C3CCCCC23)cc1OC 10.1016/j.bmcl.2012.01.013
CHEMBL1951067 70499 0 None - 1 Guinea pig 10.0 pEC50 = 10 Functional
Agonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contractionAgonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contraction
ChEMBL 538 13 4 8 3.4 COc1ccc(C2=NN(CCCCNC[C@H](O)c3ccc(O)c(NC=O)c3)C(=O)C3CCCCC23)cc1OC 10.1016/j.bmcl.2012.01.013
12065 621 21 None 6 2 Human 10.0 pEC50 = 10 Functional
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 370 6 4 5 2.7 Cc1ccccc1CC(C)(C)NCC(c1c2c(c(cc1)O)NC(=O)CO2)O 10.1016/j.bmcl.2009.10.013
45483813 621 21 None 6 2 Human 10.0 pEC50 = 10 Functional
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 370 6 4 5 2.7 Cc1ccccc1CC(C)(C)NCC(c1c2c(c(cc1)O)NC(=O)CO2)O 10.1016/j.bmcl.2009.10.013
CHEMBL579394 621 21 None 6 2 Human 10.0 pEC50 = 10 Functional
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 370 6 4 5 2.7 Cc1ccccc1CC(C)(C)NCC(c1c2c(c(cc1)O)NC(=O)CO2)O 10.1016/j.bmcl.2009.10.013
13345218 195535 0 None 8 2 Human 10.0 pEC50 = 10 Functional
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 372 6 5 6 2.1 CC(C)(Cc1ccc(O)cc1)NCC(O)c1ccc(O)c2c1OCC(=O)N2 10.1016/j.bmcl.2009.10.013
CHEMBL568272 195535 0 None 8 2 Human 10.0 pEC50 = 10 Functional
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 372 6 5 6 2.1 CC(C)(Cc1ccc(O)cc1)NCC(O)c1ccc(O)c2c1OCC(=O)N2 10.1016/j.bmcl.2009.10.013
16049024 63740 0 None 79 3 Human 10.0 pEC50 = 10 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 498 13 4 7 4.5 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCCSCCOCCc3cccc4ccccc34)c2s1 10.1016/j.bmcl.2011.05.097
CHEMBL1807820 63740 0 None 79 3 Human 10.0 pEC50 = 10 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 498 13 4 7 4.5 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCCSCCOCCc3cccc4ccccc34)c2s1 10.1016/j.bmcl.2011.05.097
118737358 118547 0 None - 1 Human 10.0 pEC50 = 10 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 689 13 6 8 5.8 O=C(CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)Nc1cccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1021/jm501915g
CHEMBL3426706 118547 0 None - 1 Human 10.0 pEC50 = 10 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 689 13 6 8 5.8 O=C(CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)Nc1cccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1021/jm501915g
10239722 111953 0 None 11 3 Human 10.0 pEC50 = 10 Functional
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 550 11 6 7 5.0 COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1-c1ccc(CN)cc1 10.1016/j.bmcl.2014.04.095
CHEMBL3298326 111953 0 None 11 3 Human 10.0 pEC50 = 10 Functional
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 550 11 6 7 5.0 COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1-c1ccc(CN)cc1 10.1016/j.bmcl.2014.04.095
66796015 111955 0 None 35 3 Human 10.0 pEC50 = 10 Functional
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 474 11 6 7 3.2 NCCOc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 10.1016/j.bmcl.2014.04.095
CHEMBL3298328 111955 0 None 35 3 Human 10.0 pEC50 = 10 Functional
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 474 11 6 7 3.2 NCCOc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 10.1016/j.bmcl.2014.04.095
10180590 69873 0 None 707 2 Human 10.0 pEC50 = 10 Functional
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 422 11 6 6 2.9 OCc1cc([C@@H](O)CNCCc2ccc(NC[C@H](O)c3ccccc3)cc2)ccc1O 10.1016/j.bmcl.2011.11.072
CHEMBL1940830 69873 0 None 707 2 Human 10.0 pEC50 = 10 Functional
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 422 11 6 6 2.9 OCc1cc([C@@H](O)CNCCc2ccc(NC[C@H](O)c3ccccc3)cc2)ccc1O 10.1016/j.bmcl.2011.11.072
105 3392 84 None -8 3 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1021/acs.jmedchem.1c02006
2083 3392 84 None -8 3 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1021/acs.jmedchem.1c02006
558 3392 84 None -8 3 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1021/acs.jmedchem.1c02006
CHEMBL714 3392 84 None -8 3 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1021/acs.jmedchem.1c02006
DB01001 3392 84 None -8 3 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1021/acs.jmedchem.1c02006
10392857 88217 0 None - 1 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
ChEMBL 552 11 7 7 2.2 C[C@H](Cc1ccc2[nH]c(C(=O)NCc3ccc(S(N)(=O)=O)cc3)cc2c1)NC[C@H](O)c1ccc(O)c(CO)c1 10.1016/j.bmcl.2007.09.031
CHEMBL235818 88217 0 None - 1 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
ChEMBL 552 11 7 7 2.2 C[C@H](Cc1ccc2[nH]c(C(=O)NCc3ccc(S(N)(=O)=O)cc3)cc2c1)NC[C@H](O)c1ccc(O)c(CO)c1 10.1016/j.bmcl.2007.09.031
3083544 462 46 None -1 4 Guinea pig 9.9 pEC50 = 9.9 Functional
Agonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contractionAgonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contraction
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2012.01.013
4943 462 46 None -1 4 Guinea pig 9.9 pEC50 = 9.9 Functional
Agonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contractionAgonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contraction
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2012.01.013
7479 462 46 None -1 4 Guinea pig 9.9 pEC50 = 9.9 Functional
Agonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contractionAgonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contraction
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2012.01.013
CHEMBL1363 462 46 None -1 4 Guinea pig 9.9 pEC50 = 9.9 Functional
Agonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contractionAgonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contraction
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2012.01.013
DB01274 462 46 None -1 4 Guinea pig 9.9 pEC50 = 9.9 Functional
Agonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contractionAgonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contraction
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2012.01.013
16049026 63741 0 None 25 3 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 432 13 4 7 2.6 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCCOCCOCCc3ccccc3)c2s1 10.1016/j.bmcl.2011.05.097
CHEMBL1807821 63741 0 None 25 3 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 432 13 4 7 2.6 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCCOCCOCCc3ccccc3)c2s1 10.1016/j.bmcl.2011.05.097
16049029 63742 0 None 25 2 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 482 13 4 7 3.7 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCCOCCOCCc3cccc4ccccc34)c2s1 10.1016/j.bmcl.2011.05.097
CHEMBL1807822 63742 0 None 25 2 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 482 13 4 7 3.7 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCCOCCOCCc3cccc4ccccc34)c2s1 10.1016/j.bmcl.2011.05.097
10461973 118538 0 None - 1 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 655 15 6 8 4.9 O=C(CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)NCCCCCNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/jm501915g
CHEMBL3426697 118538 0 None - 1 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 655 15 6 8 4.9 O=C(CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)NCCCCCNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/jm501915g
9871386 111766 4 None 8 4 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 521 10 5 6 5.5 COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1-c1ccccc1 10.1016/j.bmcl.2014.04.095
CHEMBL3290999 111766 4 None 8 4 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 521 10 5 6 5.5 COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1-c1ccccc1 10.1016/j.bmcl.2014.04.095
90645344 111951 0 None 7 3 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 550 11 6 7 5.0 COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1-c1ccccc1CN 10.1016/j.bmcl.2014.04.095
CHEMBL3298324 111951 0 None 7 3 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 550 11 6 7 5.0 COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1-c1ccccc1CN 10.1016/j.bmcl.2014.04.095
56943545 111957 0 None 28 3 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 502 13 6 7 4.0 NCCCCOc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 10.1016/j.bmcl.2014.04.095
CHEMBL3298330 111957 0 None 28 3 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 502 13 6 7 4.0 NCCCCOc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 10.1016/j.bmcl.2014.04.095
11180293 112003 0 None 22 3 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 543 12 6 8 3.1 O=c1ccc2c([C@@H](O)CNCCc3ccc(Nc4ccc(OCCN5CCNCC5)cc4)cc3)ccc(O)c2[nH]1 10.1016/j.bmcl.2014.04.095
CHEMBL3298897 112003 0 None 22 3 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 543 12 6 8 3.1 O=c1ccc2c([C@@H](O)CNCCc3ccc(Nc4ccc(OCCN5CCNCC5)cc4)cc3)ccc(O)c2[nH]1 10.1016/j.bmcl.2014.04.095
46832232 14085 0 None 39 3 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 467 16 4 6 4.5 OCc1cc([C@@H](O)CNCCCCCCOCCOCc2cccc3ccccc23)ccc1O 10.1021/jm100326d
CHEMBL1085837 14085 0 None 39 3 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 467 16 4 6 4.5 OCc1cc([C@@H](O)CNCCCCCCOCCOCc2cccc3ccccc23)ccc1O 10.1021/jm100326d
CHEMBL1198923 14085 0 None 39 3 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 467 16 4 6 4.5 OCc1cc([C@@H](O)CNCCCCCCOCCOCc2cccc3ccccc23)ccc1O 10.1021/jm100326d
10217757 111765 0 None 10 4 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 497 12 5 6 5.2 COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c(NC=O)c3)cc2)cc1-c1ccccc1 10.1016/j.bmcl.2014.04.069
CHEMBL3290998 111765 0 None 10 4 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 497 12 5 6 5.2 COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c(NC=O)c3)cc2)cc1-c1ccccc1 10.1016/j.bmcl.2014.04.069
9871386 111766 4 None 8 4 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 521 10 5 6 5.5 COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1-c1ccccc1 10.1016/j.bmcl.2014.04.069
CHEMBL3290999 111766 4 None 8 4 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 521 10 5 6 5.5 COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1-c1ccccc1 10.1016/j.bmcl.2014.04.069
57398384 69876 0 None - 1 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 459 10 6 6 3.2 O=c1ccc2c([C@@H](O)CNCCc3ccc(NC[C@H](O)c4ccccc4)cc3)ccc(O)c2[nH]1 10.1016/j.bmcl.2011.11.072
CHEMBL1940833 69876 0 None - 1 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 459 10 6 6 3.2 O=c1ccc2c([C@@H](O)CNCCc3ccc(NC[C@H](O)c4ccccc4)cc3)ccc(O)c2[nH]1 10.1016/j.bmcl.2011.11.072
156015656 177758 0 None - 1 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 378 7 4 5 2.3 O=C1COc2c(cc(O)cc2C(O)CNCCCc2cc(F)cc(F)c2)N1 10.1016/j.bmc.2019.115178
CHEMBL4639822 177758 0 None - 1 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 378 7 4 5 2.3 O=C1COc2c(cc(O)cc2C(O)CNCCCc2cc(F)cc(F)c2)N1 10.1016/j.bmc.2019.115178
CHEMBL4651230 177758 0 None - 1 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 378 7 4 5 2.3 O=C1COc2c(cc(O)cc2C(O)CNCCCc2cc(F)cc(F)c2)N1 10.1016/j.bmc.2019.115178
53323515 57909 0 None - 1 Guinea pig 9.9 pEC50 = 9.9 Functional
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
ChEMBL 515 10 7 6 2.5 NC(=O)c1cccc(CNC(=O)Nc2cccc(CCNCC(O)c3ccc(O)c4[nH]c(=O)ccc34)c2)c1 10.1016/j.bmcl.2010.12.096
CHEMBL1682214 57909 0 None - 1 Guinea pig 9.9 pEC50 = 9.9 Functional
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
ChEMBL 515 10 7 6 2.5 NC(=O)c1cccc(CNC(=O)Nc2cccc(CCNCC(O)c3ccc(O)c4[nH]c(=O)ccc34)c2)c1 10.1016/j.bmcl.2010.12.096
46938907 16515 0 None - 1 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 609 12 6 7 4.3 CC(C)(Cc1cccc(CC(=O)NCc2cc(Cl)cc(Cl)c2O)c1)NC[C@H](O)c1ccc(O)c(NS(C)(=O)=O)c1 10.1021/jm1005989
CHEMBL1243035 16515 0 None - 1 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 609 12 6 7 4.3 CC(C)(Cc1cccc(CC(=O)NCc2cc(Cl)cc(Cl)c2O)c1)NC[C@H](O)c1ccc(O)c(NS(C)(=O)=O)c1 10.1021/jm1005989
155524038 170314 0 None 120 2 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 414 8 4 4 4.2 O=c1ccc2c(C(O)CNCCCc3ccc(-c4ccccc4)cc3)ccc(O)c2[nH]1 10.1016/j.bmc.2018.10.043
CHEMBL4454489 170314 0 None 120 2 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 414 8 4 4 4.2 O=c1ccc2c(C(O)CNCCCc3ccc(-c4ccccc4)cc3)ccc(O)c2[nH]1 10.1016/j.bmc.2018.10.043
2419 3394 80 None 17 6 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.ejmech.2021.113697
5152 3394 80 None 17 6 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.ejmech.2021.113697
559 3394 80 None 17 6 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.ejmech.2021.113697
CHEMBL1263 3394 80 None 17 6 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.ejmech.2021.113697
DB00938 3394 80 None 17 6 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.ejmech.2021.113697
156020412 177764 0 None - 1 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 446 8 4 5 4.3 CC(C)(CC(c1ccccc1)c1ccccc1)NC[C@H](O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmc.2019.115178
CHEMBL4648525 177764 0 None - 1 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 446 8 4 5 4.3 CC(C)(CC(c1ccccc1)c1ccccc1)NC[C@H](O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmc.2019.115178
CHEMBL4651243 177764 0 None - 1 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 446 8 4 5 4.3 CC(C)(CC(c1ccccc1)c1ccccc1)NC[C@H](O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmc.2019.115178
155550964 173368 0 None 575 2 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 352 8 4 4 2.9 O=c1ccc2c(C(O)CNCCCCc3ccccc3)ccc(O)c2[nH]1 10.1016/j.bmc.2018.10.043
CHEMBL4541263 173368 0 None 575 2 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 352 8 4 4 2.9 O=c1ccc2c(C(O)CNCCCCc3ccccc3)ccc(O)c2[nH]1 10.1016/j.bmc.2018.10.043
1499 2052 43 None -72 36 Human 9.8 pEC50 = 9.8 Functional
Activity against human beta 2 adrenergic receptor (AR), expressed in CHO cellsActivity against human beta 2 adrenergic receptor (AR), expressed in CHO cells
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm0101500
3779 2052 43 None -72 36 Human 9.8 pEC50 = 9.8 Functional
Activity against human beta 2 adrenergic receptor (AR), expressed in CHO cellsActivity against human beta 2 adrenergic receptor (AR), expressed in CHO cells
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm0101500
536 2052 43 None -72 36 Human 9.8 pEC50 = 9.8 Functional
Activity against human beta 2 adrenergic receptor (AR), expressed in CHO cellsActivity against human beta 2 adrenergic receptor (AR), expressed in CHO cells
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm0101500
CHEMBL434 2052 43 None -72 36 Human 9.8 pEC50 = 9.8 Functional
Activity against human beta 2 adrenergic receptor (AR), expressed in CHO cellsActivity against human beta 2 adrenergic receptor (AR), expressed in CHO cells
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm0101500
DB01064 2052 43 None -72 36 Human 9.8 pEC50 = 9.8 Functional
Activity against human beta 2 adrenergic receptor (AR), expressed in CHO cellsActivity against human beta 2 adrenergic receptor (AR), expressed in CHO cells
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm0101500
1499 2052 43 None -72 36 Human 9.8 pEC50 = 9.8 Functional
Activity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm0509445
3779 2052 43 None -72 36 Human 9.8 pEC50 = 9.8 Functional
Activity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm0509445
536 2052 43 None -72 36 Human 9.8 pEC50 = 9.8 Functional
Activity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm0509445
CHEMBL434 2052 43 None -72 36 Human 9.8 pEC50 = 9.8 Functional
Activity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm0509445
DB01064 2052 43 None -72 36 Human 9.8 pEC50 = 9.8 Functional
Activity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm0509445
10394806 118539 0 None - 1 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 681 12 6 8 5.3 O=C(CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)N[C@H]1CC[C@H](CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1021/jm501915g
CHEMBL3426698 118539 0 None - 1 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 681 12 6 8 5.3 O=C(CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)N[C@H]1CC[C@H](CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1021/jm501915g
118737354 118542 0 None - 1 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 703 12 6 8 5.8 Cc1cc(C(=O)NCCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(C)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/jm501915g
CHEMBL3426701 118542 0 None - 1 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 703 12 6 8 5.8 Cc1cc(C(=O)NCCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(C)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/jm501915g
56943518 111956 0 None 25 3 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 488 12 6 7 3.6 NCCCOc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 10.1016/j.bmcl.2014.04.095
CHEMBL3298329 111956 0 None 25 3 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 488 12 6 7 3.6 NCCCOc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 10.1016/j.bmcl.2014.04.095
56943546 111973 0 None 25 3 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 518 14 6 8 3.2 NCCOCCOc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 10.1016/j.bmcl.2014.04.095
CHEMBL3298691 111973 0 None 25 3 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 518 14 6 8 3.2 NCCOCCOc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 10.1016/j.bmcl.2014.04.095
24901144 69971 0 None -1 5 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 481 11 5 6 3.6 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3cccc(CNCCc4ccccc4F)c3)c2s1 10.1016/j.bmcl.2011.10.049
CHEMBL1944691 69971 0 None -1 5 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 481 11 5 6 3.6 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3cccc(CNCCc4ccccc4F)c3)c2s1 10.1016/j.bmcl.2011.10.049
10288976 66232 0 None 10 4 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 487 17 6 6 3.9 Cc1cc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc(NC(N)=O)c1 10.1016/j.bmc.2011.08.043
CHEMBL1835862 66232 0 None 10 4 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 487 17 6 6 3.9 Cc1cc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc(NC(N)=O)c1 10.1016/j.bmc.2011.08.043
CHEMBL1852543 66232 0 None 10 4 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 487 17 6 6 3.9 Cc1cc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc(NC(N)=O)c1 10.1016/j.bmc.2011.08.043
9849126 12318 0 None -3 4 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 507 18 5 7 2.8 NS(=O)(=O)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(NC=O)c2)c1 10.1021/jm801016j
CHEMBL1185969 12318 0 None -3 4 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 507 18 5 7 2.8 NS(=O)(=O)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(NC=O)c2)c1 10.1021/jm801016j
CHEMBL443435 12318 0 None -3 4 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 507 18 5 7 2.8 NS(=O)(=O)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(NC=O)c2)c1 10.1021/jm801016j
9891927 183605 6 None 5 4 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
CHEMBL446840 183605 6 None 5 4 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
CHEMBL483200 183605 6 None 5 4 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
CHEMBL483201 183605 6 None 5 4 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
9891927 183605 6 None 5 4 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm100326d
CHEMBL446840 183605 6 None 5 4 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm100326d
CHEMBL483200 183605 6 None 5 4 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm100326d
CHEMBL483201 183605 6 None 5 4 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm100326d
155551133 173414 0 None 446 2 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 340 7 4 5 1.9 O=c1ccc2c(C(O)CNCCOc3ccccc3)ccc(O)c2[nH]1 10.1016/j.bmc.2018.10.043
CHEMBL4542430 173414 0 None 446 2 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 340 7 4 5 1.9 O=c1ccc2c(C(O)CNCCOc3ccccc3)ccc(O)c2[nH]1 10.1016/j.bmc.2018.10.043
44434128 148595 0 None - 1 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
ChEMBL 489 10 7 6 3.3 C[C@H](Cc1ccc2[nH]c(C(=O)NCc3ccc(O)cc3)cc2c1)NC[C@H](O)c1ccc(O)c(CO)c1 10.1016/j.bmcl.2007.09.031
CHEMBL394339 148595 0 None - 1 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
ChEMBL 489 10 7 6 3.3 C[C@H](Cc1ccc2[nH]c(C(=O)NCc3ccc(O)cc3)cc2c1)NC[C@H](O)c1ccc(O)c(CO)c1 10.1016/j.bmcl.2007.09.031
11534330 16512 0 None - 1 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 575 12 6 7 3.6 CC(C)(Cc1cccc(CC(=O)NCc2cc(Cl)ccc2O)c1)NC[C@H](O)c1ccc(O)c(NS(C)(=O)=O)c1 10.1021/jm1005989
CHEMBL1243000 16512 0 None - 1 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 575 12 6 7 3.6 CC(C)(Cc1cccc(CC(=O)NCc2cc(Cl)ccc2O)c1)NC[C@H](O)c1ccc(O)c(NS(C)(=O)=O)c1 10.1021/jm1005989
156020206 177757 0 None - 1 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 358 7 5 6 1.7 O=C1COc2c(cc(O)cc2C(O)CNCCCc2cccc(O)c2)N1 10.1016/j.bmc.2019.115178
CHEMBL4648663 177757 0 None - 1 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 358 7 5 6 1.7 O=C1COc2c(cc(O)cc2C(O)CNCCCc2cccc(O)c2)N1 10.1016/j.bmc.2019.115178
CHEMBL4651226 177757 0 None - 1 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 358 7 5 6 1.7 O=C1COc2c(cc(O)cc2C(O)CNCCCc2cccc(O)c2)N1 10.1016/j.bmc.2019.115178
156015463 177766 0 None - 1 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 482 8 4 5 4.6 CC(C)(CC(c1ccc(F)cc1)c1ccc(F)cc1)NC[C@H](O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmc.2019.115178
CHEMBL4640925 177766 0 None - 1 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 482 8 4 5 4.6 CC(C)(CC(c1ccc(F)cc1)c1ccc(F)cc1)NC[C@H](O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmc.2019.115178
CHEMBL4651254 177766 0 None - 1 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 482 8 4 5 4.6 CC(C)(CC(c1ccc(F)cc1)c1ccc(F)cc1)NC[C@H](O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmc.2019.115178
1239 1639 46 None -1 5 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2011.01.043
3410 1639 46 None -1 5 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2011.01.043
3465 1639 46 None -1 5 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2011.01.043
CHEMBL1256786 1639 46 None -1 5 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2011.01.043
DB00983 1639 46 None -1 5 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2011.01.043
56658246 64151 0 None 3 4 Guinea pig 9.7 pEC50 = 9.7 Functional
Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contractionAgonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contraction
ChEMBL 525 17 5 8 2.9 O=c1cc[nH]c(=O)n1-c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.05.064
CHEMBL1814277 64151 0 None 3 4 Guinea pig 9.7 pEC50 = 9.7 Functional
Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contractionAgonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contraction
ChEMBL 525 17 5 8 2.9 O=c1cc[nH]c(=O)n1-c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.05.064
CHEMBL1814278 64151 0 None 3 4 Guinea pig 9.7 pEC50 = 9.7 Functional
Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contractionAgonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contraction
ChEMBL 525 17 5 8 2.9 O=c1cc[nH]c(=O)n1-c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.05.064
24901413 69998 0 None 3 4 Guinea pig 9.7 pEC50 = 9.7 Functional
Agonist activity at beta2 adrenoceptor in guinea pig trachea assessed as reduction in methacholine-induced contractionAgonist activity at beta2 adrenoceptor in guinea pig trachea assessed as reduction in methacholine-induced contraction
ChEMBL 516 11 6 6 4.3 Cc1cccc2c(CCNCc3ccc(CCNC[C@H](O)c4ccc(O)c5[nH]c(=O)sc45)cc3)c[nH]c12 10.1016/j.bmcl.2011.10.049
CHEMBL1945032 69998 0 None 3 4 Guinea pig 9.7 pEC50 = 9.7 Functional
Agonist activity at beta2 adrenoceptor in guinea pig trachea assessed as reduction in methacholine-induced contractionAgonist activity at beta2 adrenoceptor in guinea pig trachea assessed as reduction in methacholine-induced contraction
ChEMBL 516 11 6 6 4.3 Cc1cccc2c(CCNCc3ccc(CCNC[C@H](O)c4ccc(O)c5[nH]c(=O)sc45)cc3)c[nH]c12 10.1016/j.bmcl.2011.10.049
15981386 63204 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
ChEMBL 459 12 4 7 2.0 CN(CCNC[C@H](O)c1ccc(O)c2[nH]c(=O)sc12)C(=O)CCOCCc1ccccc1 10.1016/j.bmcl.2011.04.135
CHEMBL1800472 63204 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
ChEMBL 459 12 4 7 2.0 CN(CCNC[C@H](O)c1ccc(O)c2[nH]c(=O)sc12)C(=O)CCOCCc1ccccc1 10.1016/j.bmcl.2011.04.135
56663238 63756 0 None 251 2 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 465 13 5 7 2.8 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCCOCCNCCc3cccc(Cl)c3)c2s1 10.1016/j.bmcl.2011.05.097
CHEMBL1807872 63756 0 None 251 2 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 465 13 5 7 2.8 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCCOCCNCCc3cccc(Cl)c3)c2s1 10.1016/j.bmcl.2011.05.097
11857427 118534 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 689 12 6 8 6.1 Cc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1021/jm501915g
CHEMBL3426693 118534 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 689 12 6 8 6.1 Cc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1021/jm501915g
118737350 118535 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 689 12 6 8 6.1 Cc1cc(NC(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)ccc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/jm501915g
CHEMBL3426694 118535 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 689 12 6 8 6.1 Cc1cc(NC(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)ccc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/jm501915g
1239 1639 46 None -1 5 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.04.095
3410 1639 46 None -1 5 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.04.095
3465 1639 46 None -1 5 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.04.095
CHEMBL1256786 1639 46 None -1 5 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.04.095
DB00983 1639 46 None -1 5 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.04.095
16738927 70000 0 None 31 3 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 464 11 5 7 2.9 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3ccc(CNCCc4ccccn4)cc3)c2s1 10.1016/j.bmcl.2011.10.049
CHEMBL1945034 70000 0 None 31 3 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 464 11 5 7 2.9 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3ccc(CNCCc4ccccn4)cc3)c2s1 10.1016/j.bmcl.2011.10.049
42625823 12555 0 None 251 3 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 576 19 5 7 4.7 O=S(=O)(NC1CCCCC1)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
CHEMBL1187371 12555 0 None 251 3 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 576 19 5 7 4.7 O=S(=O)(NC1CCCCC1)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
CHEMBL500782 12555 0 None 251 3 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 576 19 5 7 4.7 O=S(=O)(NC1CCCCC1)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
1239 1639 46 None -1 5 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.04.069
3410 1639 46 None -1 5 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.04.069
3465 1639 46 None -1 5 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.04.069
CHEMBL1256786 1639 46 None -1 5 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.04.069
DB00983 1639 46 None -1 5 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.04.069
44237612 57906 0 None 4466 2 Guinea pig 9.7 pEC50 = 9.7 Functional
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
ChEMBL 472 9 6 5 3.4 O=C(NCc1ccccc1)Nc1cccc(CCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1016/j.bmcl.2010.12.096
CHEMBL1682211 57906 0 None 4466 2 Guinea pig 9.7 pEC50 = 9.7 Functional
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
ChEMBL 472 9 6 5 3.4 O=C(NCc1ccccc1)Nc1cccc(CCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1016/j.bmcl.2010.12.096
44237613 57910 0 None 2754 2 Guinea pig 9.7 pEC50 = 9.7 Functional
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
ChEMBL 502 10 6 6 3.4 COc1ccccc1CNC(=O)Nc1cccc(CCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1016/j.bmcl.2010.12.096
CHEMBL1682215 57910 0 None 2754 2 Guinea pig 9.7 pEC50 = 9.7 Functional
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
ChEMBL 502 10 6 6 3.4 COc1ccccc1CNC(=O)Nc1cccc(CCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1016/j.bmcl.2010.12.096
44237614 57911 0 None 31622 2 Guinea pig 9.7 pEC50 = 9.7 Functional
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
ChEMBL 490 9 6 5 3.6 O=C(NCc1ccc(F)cc1)Nc1cccc(CCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1016/j.bmcl.2010.12.096
CHEMBL1682216 57911 0 None 31622 2 Guinea pig 9.7 pEC50 = 9.7 Functional
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
ChEMBL 490 9 6 5 3.6 O=C(NCc1ccc(F)cc1)Nc1cccc(CCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1016/j.bmcl.2010.12.096
44237669 57912 0 None 7943 2 Guinea pig 9.7 pEC50 = 9.7 Functional
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
ChEMBL 540 9 6 5 4.7 O=C(NCc1c(Cl)cccc1Cl)Nc1cccc(CCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1016/j.bmcl.2010.12.096
CHEMBL1682217 57912 0 None 7943 2 Guinea pig 9.7 pEC50 = 9.7 Functional
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
ChEMBL 540 9 6 5 4.7 O=C(NCc1c(Cl)cccc1Cl)Nc1cccc(CCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1016/j.bmcl.2010.12.096
44237666 57913 0 None 44668 2 Guinea pig 9.7 pEC50 = 9.7 Functional
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
ChEMBL 548 10 6 5 5.0 O=C(Nc1cccc(CCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1)NC(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2010.12.096
CHEMBL1682218 57913 0 None 44668 2 Guinea pig 9.7 pEC50 = 9.7 Functional
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
ChEMBL 548 10 6 5 5.0 O=C(Nc1cccc(CCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1)NC(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2010.12.096
45483810 195458 0 None 3 2 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 356 6 4 5 2.4 CC(C)(Cc1ccccc1)NCC(O)c1ccc(O)c2c1OCC(=O)N2 10.1016/j.bmcl.2009.10.013
CHEMBL567863 195458 0 None 3 2 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 356 6 4 5 2.4 CC(C)(Cc1ccccc1)NCC(O)c1ccc(O)c2c1OCC(=O)N2 10.1016/j.bmcl.2009.10.013
1499 2052 43 None -72 36 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulationAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2013.11.030
3779 2052 43 None -72 36 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulationAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2013.11.030
536 2052 43 None -72 36 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulationAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2013.11.030
CHEMBL434 2052 43 None -72 36 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulationAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2013.11.030
DB01064 2052 43 None -72 36 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulationAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2013.11.030
11577915 16416 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 591 12 6 7 4.1 CC(C)(Cc1cccc(CC(=O)NCc2ccc3cc(O)ccc3c2)c1)NC[C@H](O)c1ccc(O)c(NS(C)(=O)=O)c1 10.1021/jm1005989
CHEMBL1240965 16416 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 591 12 6 7 4.1 CC(C)(Cc1cccc(CC(=O)NCc2ccc3cc(O)ccc3c2)c1)NC[C@H](O)c1ccc(O)c(NS(C)(=O)=O)c1 10.1021/jm1005989
1499 2052 43 None -72 36 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.ejmech.2021.113697
3779 2052 43 None -72 36 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.ejmech.2021.113697
536 2052 43 None -72 36 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.ejmech.2021.113697
CHEMBL434 2052 43 None -72 36 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.ejmech.2021.113697
DB01064 2052 43 None -72 36 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.ejmech.2021.113697
156014685 177761 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 358 7 5 6 1.7 O=C1COc2c(cc(O)cc2C(O)CNCCCc2ccccc2O)N1 10.1016/j.bmc.2019.115178
CHEMBL4636111 177761 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 358 7 5 6 1.7 O=C1COc2c(cc(O)cc2C(O)CNCCCc2ccccc2O)N1 10.1016/j.bmc.2019.115178
CHEMBL4651237 177761 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 358 7 5 6 1.7 O=C1COc2c(cc(O)cc2C(O)CNCCCc2ccccc2O)N1 10.1016/j.bmc.2019.115178
155536173 171586 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 442 8 4 4 4.9 CC(C)(CC(c1ccccc1)c1ccccc1)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.bmc.2018.10.043
CHEMBL4473349 171586 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 442 8 4 4 4.9 CC(C)(CC(c1ccccc1)c1ccccc1)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.bmc.2018.10.043
155527926 170677 0 None 8709 2 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 451 11 5 5 3.9 CC(C)CCC(=O)Nc1cccc(CCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1016/j.bmc.2018.10.043
CHEMBL4460095 170677 0 None 8709 2 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 451 11 5 5 3.9 CC(C)CCC(=O)Nc1cccc(CCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1016/j.bmc.2018.10.043
11714238 16417 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 617 13 6 7 4.6 CC(C)(Cc1cccc(CC(=O)NCc2ccc(-c3ccc(O)cc3)cc2)c1)NC[C@H](O)c1ccc(O)c(NS(C)(=O)=O)c1 10.1021/jm1005989
CHEMBL1240966 16417 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 617 13 6 7 4.6 CC(C)(Cc1cccc(CC(=O)NCc2ccc(-c3ccc(O)cc3)cc2)c1)NC[C@H](O)c1ccc(O)c(NS(C)(=O)=O)c1 10.1021/jm1005989
11647002 15447 0 None 8 2 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at adrenergic beta2 receptor in human A431 cells assessed as elevation of cAMP levelAgonist activity at adrenergic beta2 receptor in human A431 cells assessed as elevation of cAMP level
ChEMBL 400 7 4 6 3.1 O=c1[nH]c2c(O)ccc([C@@H](O)CN[C@H]3CCC[C@@H]3OCc3ccccc3)c2s1 10.1016/j.bmcl.2014.06.014
CHEMBL1221681 15447 0 None 8 2 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at adrenergic beta2 receptor in human A431 cells assessed as elevation of cAMP levelAgonist activity at adrenergic beta2 receptor in human A431 cells assessed as elevation of cAMP level
ChEMBL 400 7 4 6 3.1 O=c1[nH]c2c(O)ccc([C@@H](O)CN[C@H]3CCC[C@@H]3OCc3ccccc3)c2s1 10.1016/j.bmcl.2014.06.014
164612026 184777 0 None 776 2 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human beta2 adrenoceptor expressed in HEK293 cells assessed as increase in cAMP accumulation measured after 60 mins by HTRF assayAgonist activity at human beta2 adrenoceptor expressed in HEK293 cells assessed as increase in cAMP accumulation measured after 60 mins by HTRF assay
ChEMBL 237 4 3 4 1.3 CC(C)NC(CO)c1cc(F)c(N)c(C#N)c1 10.1021/acs.jmedchem.0c01195
CHEMBL4860455 184777 0 None 776 2 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human beta2 adrenoceptor expressed in HEK293 cells assessed as increase in cAMP accumulation measured after 60 mins by HTRF assayAgonist activity at human beta2 adrenoceptor expressed in HEK293 cells assessed as increase in cAMP accumulation measured after 60 mins by HTRF assay
ChEMBL 237 4 3 4 1.3 CC(C)NC(CO)c1cc(F)c(N)c(C#N)c1 10.1021/acs.jmedchem.0c01195
56672271 66193 0 None -1 4 Guinea pig 9.6 pEC50 = 9.6 Functional
Agonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile responseAgonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response
ChEMBL 530 19 7 7 2.7 NC(=O)CNC(=O)Nc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.08.043
CHEMBL1835859 66193 0 None -1 4 Guinea pig 9.6 pEC50 = 9.6 Functional
Agonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile responseAgonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response
ChEMBL 530 19 7 7 2.7 NC(=O)CNC(=O)Nc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.08.043
CHEMBL1852407 66193 0 None -1 4 Guinea pig 9.6 pEC50 = 9.6 Functional
Agonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile responseAgonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response
ChEMBL 530 19 7 7 2.7 NC(=O)CNC(=O)Nc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.08.043
24901144 69971 0 None 1 5 Guinea pig 9.6 pEC50 = 9.6 Functional
Agonist activity at beta2 adrenoceptor in guinea pig trachea assessed as reduction in methacholine-induced contractionAgonist activity at beta2 adrenoceptor in guinea pig trachea assessed as reduction in methacholine-induced contraction
ChEMBL 481 11 5 6 3.6 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3cccc(CNCCc4ccccc4F)c3)c2s1 10.1016/j.bmcl.2011.10.049
CHEMBL1944691 69971 0 None 1 5 Guinea pig 9.6 pEC50 = 9.6 Functional
Agonist activity at beta2 adrenoceptor in guinea pig trachea assessed as reduction in methacholine-induced contractionAgonist activity at beta2 adrenoceptor in guinea pig trachea assessed as reduction in methacholine-induced contraction
ChEMBL 481 11 5 6 3.6 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3cccc(CNCCc4ccccc4F)c3)c2s1 10.1016/j.bmcl.2011.10.049
57393349 70174 0 None 3 2 Guinea pig 9.6 pEC50 = 9.6 Functional
Agonist activity at beta2 adrenoceptor in guinea pig trachea assessed as reduction in methacholine-induced contractionAgonist activity at beta2 adrenoceptor in guinea pig trachea assessed as reduction in methacholine-induced contraction
ChEMBL 523 11 4 5 6.2 C[C@@H](NCc1ccccc1-c1ccc(CCNCCc2ccc(O)c3[nH]c(=O)sc23)cc1)c1ccccc1 10.1016/j.bmcl.2011.10.049
CHEMBL1947151 70174 0 None 3 2 Guinea pig 9.6 pEC50 = 9.6 Functional
Agonist activity at beta2 adrenoceptor in guinea pig trachea assessed as reduction in methacholine-induced contractionAgonist activity at beta2 adrenoceptor in guinea pig trachea assessed as reduction in methacholine-induced contraction
ChEMBL 523 11 4 5 6.2 C[C@@H](NCc1ccccc1-c1ccc(CCNCCc2ccc(O)c3[nH]c(=O)sc23)cc1)c1ccccc1 10.1016/j.bmcl.2011.10.049
2419 3394 80 None 17 6 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmc.2011.05.064
5152 3394 80 None 17 6 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmc.2011.05.064
559 3394 80 None 17 6 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmc.2011.05.064
CHEMBL1263 3394 80 None 17 6 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmc.2011.05.064
DB00938 3394 80 None 17 6 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmc.2011.05.064
56672116 66018 0 None 316 3 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 570 19 5 8 2.4 NC(=O)CN1C(=O)CN(c2cccc(CCCCOCCCCCCNC[C@H](O)c3ccc(O)c(CO)c3)c2)C1=O 10.1016/j.bmc.2011.05.064
CHEMBL1814276 66018 0 None 316 3 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 570 19 5 8 2.4 NC(=O)CN1C(=O)CN(c2cccc(CCCCOCCCCCCNC[C@H](O)c3ccc(O)c(CO)c3)c2)C1=O 10.1016/j.bmc.2011.05.064
CHEMBL1851624 66018 0 None 316 3 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 570 19 5 8 2.4 NC(=O)CN1C(=O)CN(c2cccc(CCCCOCCCCCCNC[C@H](O)c3ccc(O)c(CO)c3)c2)C1=O 10.1016/j.bmc.2011.05.064
10372836 101912 34 None 6 2 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 739 13 6 9 6.4 COc1cc(NC(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/jm501915g
CHEMBL3039518 101912 34 None 6 2 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 739 13 6 9 6.4 COc1cc(NC(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/jm501915g
10372344 118528 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 675 12 6 8 5.8 O=C(CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)Nc1ccc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1 10.1021/jm501915g
CHEMBL3426687 118528 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 675 12 6 8 5.8 O=C(CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)Nc1ccc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1 10.1021/jm501915g
10327462 118529 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 709 12 6 8 6.4 O=C(CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)Nc1ccc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1Cl 10.1021/jm501915g
CHEMBL3426688 118529 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 709 12 6 8 6.4 O=C(CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)Nc1ccc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1Cl 10.1021/jm501915g
118737348 118532 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 705 13 6 9 5.8 COc1cc(NC(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)ccc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/jm501915g
CHEMBL3426691 118532 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 705 13 6 9 5.8 COc1cc(NC(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)ccc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/jm501915g
118737351 118536 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 719 13 6 9 6.1 COc1c(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc(NC(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1C 10.1021/jm501915g
CHEMBL3426695 118536 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 719 13 6 9 6.1 COc1c(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc(NC(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1C 10.1021/jm501915g
118737355 118543 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 689 12 5 8 5.5 CN(CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)C(=O)c1ccc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1 10.1021/jm501915g
CHEMBL3426702 118543 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 689 12 5 8 5.5 CN(CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)C(=O)c1ccc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1 10.1021/jm501915g
56943515 111939 0 None 7 3 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 478 13 6 7 3.7 CC(C)(N)COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c(NC=O)c3)cc2)cc1 10.1016/j.bmcl.2014.04.095
CHEMBL3298213 111939 0 None 7 3 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 478 13 6 7 3.7 CC(C)(N)COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c(NC=O)c3)cc2)cc1 10.1016/j.bmcl.2014.04.095
10173878 111954 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 459 10 5 6 4.2 CCOc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 10.1016/j.bmcl.2014.04.095
CHEMBL3298327 111954 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 459 10 5 6 4.2 CCOc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 10.1016/j.bmcl.2014.04.095
24901210 69970 0 None 125 4 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 497 11 5 6 4.1 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3cccc(CNCCc4ccccc4Cl)c3)c2s1 10.1016/j.bmcl.2011.10.049
CHEMBL1944690 69970 0 None 125 4 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 497 11 5 6 4.1 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3cccc(CNCCc4ccccc4Cl)c3)c2s1 10.1016/j.bmcl.2011.10.049
24901347 69975 0 None 17 4 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 463 11 5 6 3.5 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3ccc(CNCCc4ccccc4)cc3)c2s1 10.1016/j.bmcl.2011.10.049
CHEMBL1944695 69975 0 None 17 4 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 463 11 5 6 3.5 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3ccc(CNCCc4ccccc4)cc3)c2s1 10.1016/j.bmcl.2011.10.049
24901413 69998 0 None -3 4 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 516 11 6 6 4.3 Cc1cccc2c(CCNCc3ccc(CCNC[C@H](O)c4ccc(O)c5[nH]c(=O)sc45)cc3)c[nH]c12 10.1016/j.bmcl.2011.10.049
CHEMBL1945032 69998 0 None -3 4 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 516 11 6 6 4.3 Cc1cccc2c(CCNCc3ccc(CCNC[C@H](O)c4ccc(O)c5[nH]c(=O)sc45)cc3)c[nH]c12 10.1016/j.bmcl.2011.10.049
2419 3394 80 None 17 6 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/jm401532g
5152 3394 80 None 17 6 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/jm401532g
559 3394 80 None 17 6 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/jm401532g
CHEMBL1263 3394 80 None 17 6 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/jm401532g
DB00938 3394 80 None 17 6 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/jm401532g
156016062 177740 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 356 8 4 5 2.4 O=C1COc2c(cc(O)cc2C(O)CNCCCCc2ccccc2)N1 10.1016/j.bmc.2019.115178
CHEMBL4643148 177740 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 356 8 4 5 2.4 O=C1COc2c(cc(O)cc2C(O)CNCCCCc2ccccc2)N1 10.1016/j.bmc.2019.115178
CHEMBL4651124 177740 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 356 8 4 5 2.4 O=C1COc2c(cc(O)cc2C(O)CNCCCCc2ccccc2)N1 10.1016/j.bmc.2019.115178
2419 3394 80 None 17 6 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmc.2011.08.043
5152 3394 80 None 17 6 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmc.2011.08.043
559 3394 80 None 17 6 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmc.2011.08.043
CHEMBL1263 3394 80 None 17 6 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmc.2011.08.043
DB00938 3394 80 None 17 6 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmc.2011.08.043
56672271 66193 0 None 1 4 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 530 19 7 7 2.7 NC(=O)CNC(=O)Nc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.08.043
CHEMBL1835859 66193 0 None 1 4 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 530 19 7 7 2.7 NC(=O)CNC(=O)Nc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.08.043
CHEMBL1852407 66193 0 None 1 4 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 530 19 7 7 2.7 NC(=O)CNC(=O)Nc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.08.043
2419 3394 80 None 17 6 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/jm801016j
5152 3394 80 None 17 6 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/jm801016j
559 3394 80 None 17 6 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/jm801016j
CHEMBL1263 3394 80 None 17 6 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/jm801016j
DB00938 3394 80 None 17 6 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/jm801016j
2419 3394 80 None 17 6 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/jm100326d
5152 3394 80 None 17 6 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/jm100326d
559 3394 80 None 17 6 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/jm100326d
CHEMBL1263 3394 80 None 17 6 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/jm100326d
DB00938 3394 80 None 17 6 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/jm100326d
46832509 14082 0 None 50 3 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 510 18 5 8 2.7 CS(=O)(=O)Nc1cccc(COCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm100326d
CHEMBL1085399 14082 0 None 50 3 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 510 18 5 8 2.7 CS(=O)(=O)Nc1cccc(COCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm100326d
CHEMBL1198908 14082 0 None 50 3 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 510 18 5 8 2.7 CS(=O)(=O)Nc1cccc(COCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm100326d
10006800 88269 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
ChEMBL 517 12 6 6 3.6 COc1cccc(CCNC(=O)c2cc3cc(C[C@@H](C)NC[C@H](O)c4ccc(O)c(CO)c4)ccc3[nH]2)c1 10.1016/j.bmcl.2007.09.031
CHEMBL236042 88269 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
ChEMBL 517 12 6 6 3.6 COc1cccc(CCNC(=O)c2cc3cc(C[C@@H](C)NC[C@H](O)c4ccc(O)c(CO)c4)ccc3[nH]2)c1 10.1016/j.bmcl.2007.09.031
10256921 144750 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
ChEMBL 547 13 6 7 4.0 CC[C@H](Cc1ccc2[nH]c(C(=O)NCc3c(OC)cccc3OC)cc2c1)NC[C@H](O)c1ccc(O)c(CO)c1 10.1016/j.bmcl.2007.09.031
CHEMBL391308 144750 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
ChEMBL 547 13 6 7 4.0 CC[C@H](Cc1ccc2[nH]c(C(=O)NCc3c(OC)cccc3OC)cc2c1)NC[C@H](O)c1ccc(O)c(CO)c1 10.1016/j.bmcl.2007.09.031
11505444 16418 13 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 617 13 6 7 4.6 CC(C)(Cc1cccc(CC(=O)NCc2cccc(-c3ccc(O)cc3)c2)c1)NC[C@H](O)c1ccc(O)c(NS(C)(=O)=O)c1 10.1021/jm1005989
CHEMBL1240967 16418 13 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 617 13 6 7 4.6 CC(C)(Cc1cccc(CC(=O)NCc2cccc(-c3ccc(O)cc3)c2)c1)NC[C@H](O)c1ccc(O)c(NS(C)(=O)=O)c1 10.1021/jm1005989
11625619 77251 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at beta2-adrenoceptor in human bronchial smooth-muscle cell by cAMP assayAgonist activity at beta2-adrenoceptor in human bronchial smooth-muscle cell by cAMP assay
ChEMBL 406 6 4 4 3.5 CCc1cc2c(cc1CC)CC(C)(NC[C@H](O)c1ccc(O)c3[nH]c(=O)ccc13)C2 10.1016/j.bmcl.2012.07.096
CHEMBL2088201 77251 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at beta2-adrenoceptor in human bronchial smooth-muscle cell by cAMP assayAgonist activity at beta2-adrenoceptor in human bronchial smooth-muscle cell by cAMP assay
ChEMBL 406 6 4 4 3.5 CCc1cc2c(cc1CC)CC(C)(NC[C@H](O)c1ccc(O)c3[nH]c(=O)ccc13)C2 10.1016/j.bmcl.2012.07.096
16735257 85290 0 None 812 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assayAgonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assay
ChEMBL 317 7 4 5 2.4 COc1ccc(C[C@@H](C)NC[C@H](O)c2cc(O)cc(O)c2)cc1 10.1016/j.bmc.2009.11.062
CHEMBL228992 85290 0 None 812 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assayAgonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assay
ChEMBL 317 7 4 5 2.4 COc1ccc(C[C@@H](C)NC[C@H](O)c2cc(O)cc(O)c2)cc1 10.1016/j.bmc.2009.11.062
688468 141788 7 None 346 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assayAgonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assay
ChEMBL 303 6 5 5 2.1 C[C@H](Cc1ccc(O)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2009.11.062
CHEMBL388570 141788 7 None 346 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assayAgonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assay
ChEMBL 303 6 5 5 2.1 C[C@H](Cc1ccc(O)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2009.11.062
16735257 85290 0 None 812 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulationAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulation
ChEMBL 317 7 4 5 2.4 COc1ccc(C[C@@H](C)NC[C@H](O)c2cc(O)cc(O)c2)cc1 10.1016/j.bmc.2013.11.030
CHEMBL228992 85290 0 None 812 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulationAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulation
ChEMBL 317 7 4 5 2.4 COc1ccc(C[C@@H](C)NC[C@H](O)c2cc(O)cc(O)c2)cc1 10.1016/j.bmc.2013.11.030
155543518 174416 0 None 794 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 457 9 5 5 3.7 O=C(Nc1cccc(CCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1)c1ccccc1 10.1016/j.bmc.2018.10.043
CHEMBL4566727 174416 0 None 794 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 457 9 5 5 3.7 O=C(Nc1cccc(CCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1)c1ccccc1 10.1016/j.bmc.2018.10.043
1239 1639 46 None -1 5 Guinea pig 9.5 pEC50 = 9.5 Functional
Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contractionAgonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contraction
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmc.2011.05.064
3410 1639 46 None -1 5 Guinea pig 9.5 pEC50 = 9.5 Functional
Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contractionAgonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contraction
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmc.2011.05.064
3465 1639 46 None -1 5 Guinea pig 9.5 pEC50 = 9.5 Functional
Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contractionAgonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contraction
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmc.2011.05.064
CHEMBL1256786 1639 46 None -1 5 Guinea pig 9.5 pEC50 = 9.5 Functional
Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contractionAgonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contraction
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmc.2011.05.064
DB00983 1639 46 None -1 5 Guinea pig 9.5 pEC50 = 9.5 Functional
Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contractionAgonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contraction
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmc.2011.05.064
3083544 462 46 None -1 4 Guinea pig 9.5 pEC50 = 9.5 Functional
Agonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile responseAgonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O 10.1016/j.bmc.2011.08.043
4943 462 46 None -1 4 Guinea pig 9.5 pEC50 = 9.5 Functional
Agonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile responseAgonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O 10.1016/j.bmc.2011.08.043
7479 462 46 None -1 4 Guinea pig 9.5 pEC50 = 9.5 Functional
Agonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile responseAgonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O 10.1016/j.bmc.2011.08.043
CHEMBL1363 462 46 None -1 4 Guinea pig 9.5 pEC50 = 9.5 Functional
Agonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile responseAgonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O 10.1016/j.bmc.2011.08.043
DB01274 462 46 None -1 4 Guinea pig 9.5 pEC50 = 9.5 Functional
Agonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile responseAgonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O 10.1016/j.bmc.2011.08.043
24900685 69999 0 None 3 5 Guinea pig 9.5 pEC50 = 9.5 Functional
Agonist activity at beta2 adrenoceptor in guinea pig trachea assessed as reduction in methacholine-induced contractionAgonist activity at beta2 adrenoceptor in guinea pig trachea assessed as reduction in methacholine-induced contraction
ChEMBL 464 11 5 7 2.9 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3cccc(CNCCc4ccccn4)c3)c2s1 10.1016/j.bmcl.2011.10.049
CHEMBL1945033 69999 0 None 3 5 Guinea pig 9.5 pEC50 = 9.5 Functional
Agonist activity at beta2 adrenoceptor in guinea pig trachea assessed as reduction in methacholine-induced contractionAgonist activity at beta2 adrenoceptor in guinea pig trachea assessed as reduction in methacholine-induced contraction
ChEMBL 464 11 5 7 2.9 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3cccc(CNCCc4ccccn4)c3)c2s1 10.1016/j.bmcl.2011.10.049
3083544 462 46 None 1 4 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at beta2-adrenergic receptor (unknown origin)Agonist activity at beta2-adrenergic receptor (unknown origin)
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2013.11.028
4943 462 46 None 1 4 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at beta2-adrenergic receptor (unknown origin)Agonist activity at beta2-adrenergic receptor (unknown origin)
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2013.11.028
7479 462 46 None 1 4 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at beta2-adrenergic receptor (unknown origin)Agonist activity at beta2-adrenergic receptor (unknown origin)
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2013.11.028
CHEMBL1363 462 46 None 1 4 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at beta2-adrenergic receptor (unknown origin)Agonist activity at beta2-adrenergic receptor (unknown origin)
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2013.11.028
DB01274 462 46 None 1 4 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at beta2-adrenergic receptor (unknown origin)Agonist activity at beta2-adrenergic receptor (unknown origin)
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2013.11.028
118737352 118537 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 719 13 6 9 6.1 COc1cc(NC(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(C)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/jm501915g
CHEMBL3426696 118537 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 719 13 6 9 6.1 COc1cc(NC(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(C)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/jm501915g
1499 2052 43 None -72 36 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2018.10.043
1499 2052 43 None -72 36 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.ejmech.2018.04.041
3779 2052 43 None -72 36 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2018.10.043
3779 2052 43 None -72 36 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.ejmech.2018.04.041
536 2052 43 None -72 36 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2018.10.043
536 2052 43 None -72 36 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.ejmech.2018.04.041
CHEMBL434 2052 43 None -72 36 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2018.10.043
CHEMBL434 2052 43 None -72 36 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.ejmech.2018.04.041
DB01064 2052 43 None -72 36 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2018.10.043
DB01064 2052 43 None -72 36 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.ejmech.2018.04.041
2419 3394 80 None 17 6 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2014.04.095
5152 3394 80 None 17 6 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2014.04.095
559 3394 80 None 17 6 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2014.04.095
CHEMBL1263 3394 80 None 17 6 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2014.04.095
DB00938 3394 80 None 17 6 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2014.04.095
56943485 111998 0 None 12 3 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 544 12 5 8 3.6 O=c1ccc2c([C@@H](O)CNCCc3ccc(Nc4ccc(OCCN5CCOCC5)cc4)cc3)ccc(O)c2[nH]1 10.1016/j.bmcl.2014.04.095
CHEMBL3298831 111998 0 None 12 3 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 544 12 5 8 3.6 O=c1ccc2c([C@@H](O)CNCCc3ccc(Nc4ccc(OCCN5CCOCC5)cc4)cc3)ccc(O)c2[nH]1 10.1016/j.bmcl.2014.04.095
11592062 111952 0 None 25 3 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 550 11 6 7 5.0 COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1-c1cccc(CN)c1 10.1016/j.bmcl.2014.04.095
CHEMBL3298325 111952 0 None 25 3 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 550 11 6 7 5.0 COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1-c1cccc(CN)c1 10.1016/j.bmcl.2014.04.095
24901348 69969 0 None 70 4 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 531 11 5 6 4.8 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3ccc(CNCCc4c(Cl)cccc4Cl)cc3)c2s1 10.1016/j.bmcl.2011.10.049
CHEMBL1944689 69969 0 None 70 4 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 531 11 5 6 4.8 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3ccc(CNCCc4c(Cl)cccc4Cl)cc3)c2s1 10.1016/j.bmcl.2011.10.049
24901211 69973 0 None 158 3 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 493 12 5 7 3.5 COc1ccccc1CCNCc1cccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)c1 10.1016/j.bmcl.2011.10.049
CHEMBL1944693 69973 0 None 158 3 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 493 12 5 7 3.5 COc1ccccc1CCNCc1cccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)c1 10.1016/j.bmcl.2011.10.049
24901351 69974 0 None 10 4 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 493 12 5 7 3.5 COc1ccccc1CCNCc1ccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)cc1 10.1016/j.bmcl.2011.10.049
CHEMBL1944694 69974 0 None 10 4 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 493 12 5 7 3.5 COc1ccccc1CCNCc1ccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)cc1 10.1016/j.bmcl.2011.10.049
24901209 69997 0 None 177 4 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 516 11 6 6 4.3 Cc1cccc2c(CCNCc3cccc(CCNC[C@H](O)c4ccc(O)c5[nH]c(=O)sc45)c3)c[nH]c12 10.1016/j.bmcl.2011.10.049
CHEMBL1945031 69997 0 None 177 4 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 516 11 6 6 4.3 Cc1cccc2c(CCNCc3cccc(CCNC[C@H](O)c4ccc(O)c5[nH]c(=O)sc45)c3)c[nH]c12 10.1016/j.bmcl.2011.10.049
24901143 70007 0 None 12 4 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 483 10 5 6 4.1 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3cccc(CNCc4ccccc4Cl)c3)c2s1 10.1016/j.bmcl.2011.10.049
CHEMBL1945041 70007 0 None 12 4 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 483 10 5 6 4.1 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3cccc(CNCc4ccccc4Cl)c3)c2s1 10.1016/j.bmcl.2011.10.049
156015043 177679 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 342 7 4 5 2.0 O=C1COc2c(cc(O)cc2C(O)CNCCCc2ccccc2)N1 10.1016/j.bmc.2019.115178
CHEMBL4648975 177679 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 342 7 4 5 2.0 O=C1COc2c(cc(O)cc2C(O)CNCCCc2ccccc2)N1 10.1016/j.bmc.2019.115178
CHEMBL4650763 177679 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 342 7 4 5 2.0 O=C1COc2c(cc(O)cc2C(O)CNCCCc2ccccc2)N1 10.1016/j.bmc.2019.115178
56668796 66254 0 None 31 3 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 598 20 7 7 4.3 O=C(CNC(=O)Nc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1)NC1CCCC1 10.1016/j.bmc.2011.08.043
CHEMBL1835860 66254 0 None 31 3 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 598 20 7 7 4.3 O=C(CNC(=O)Nc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1)NC1CCCC1 10.1016/j.bmc.2011.08.043
CHEMBL1852632 66254 0 None 31 3 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 598 20 7 7 4.3 O=C(CNC(=O)Nc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1)NC1CCCC1 10.1016/j.bmc.2011.08.043
2419 3394 80 None 17 6 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2014.04.069
5152 3394 80 None 17 6 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2014.04.069
559 3394 80 None 17 6 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2014.04.069
CHEMBL1263 3394 80 None 17 6 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2014.04.069
DB00938 3394 80 None 17 6 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2014.04.069
2419 3394 80 None 17 6 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.11.072
5152 3394 80 None 17 6 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.11.072
559 3394 80 None 17 6 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.11.072
CHEMBL1263 3394 80 None 17 6 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.11.072
DB00938 3394 80 None 17 6 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.11.072
9932018 69858 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 422 11 6 6 2.9 OCc1cc(C(O)CNCCc2ccc(NCC(O)c3ccccc3)cc2)ccc1O 10.1016/j.bmcl.2011.11.072
CHEMBL1940815 69858 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 422 11 6 6 2.9 OCc1cc(C(O)CNCCc2ccc(NCC(O)c3ccccc3)cc2)ccc1O 10.1016/j.bmcl.2011.11.072
57403562 69860 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 450 11 6 6 3.7 CC(C)(Cc1ccc(NCC(O)c2ccccc2)cc1)NCC(O)c1ccc(O)c(CO)c1 10.1016/j.bmcl.2011.11.072
CHEMBL1940817 69860 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 450 11 6 6 3.7 CC(C)(Cc1ccc(NCC(O)c2ccccc2)cc1)NCC(O)c1ccc(O)c(CO)c1 10.1016/j.bmcl.2011.11.072
10202462 69874 0 None 223 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 422 11 6 6 2.9 OCc1cc([C@@H](O)CNCCc2ccc(NC[C@@H](O)c3ccccc3)cc2)ccc1O 10.1016/j.bmcl.2011.11.072
CHEMBL1940831 69874 0 None 223 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 422 11 6 6 2.9 OCc1cc([C@@H](O)CNCCc2ccc(NC[C@@H](O)c3ccccc3)cc2)ccc1O 10.1016/j.bmcl.2011.11.072
2419 3394 80 None 17 6 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assayAgonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/jm100068m
5152 3394 80 None 17 6 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assayAgonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/jm100068m
559 3394 80 None 17 6 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assayAgonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/jm100068m
CHEMBL1263 3394 80 None 17 6 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assayAgonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/jm100068m
DB00938 3394 80 None 17 6 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assayAgonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/jm100068m
9986442 58214 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
ChEMBL 626 15 5 7 6.6 O=C(Nc1ccccc1-c1ccccc1)OC1CCN(CCCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1016/j.bmcl.2011.01.043
CHEMBL1683933 58214 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
ChEMBL 626 15 5 7 6.6 O=C(Nc1ccccc1-c1ccccc1)OC1CCN(CCCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1016/j.bmcl.2011.01.043
2419 3394 80 None 17 6 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.01.043
5152 3394 80 None 17 6 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.01.043
559 3394 80 None 17 6 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.01.043
CHEMBL1263 3394 80 None 17 6 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.01.043
DB00938 3394 80 None 17 6 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.01.043
9874175 58215 1 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
ChEMBL 640 16 5 7 7.0 O=C(Nc1ccccc1-c1ccccc1)OC1CCN(CCCCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1016/j.bmcl.2011.01.043
CHEMBL1683934 58215 1 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
ChEMBL 640 16 5 7 7.0 O=C(Nc1ccccc1-c1ccccc1)OC1CCN(CCCCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1016/j.bmcl.2011.01.043
46938906 16510 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 603 13 5 7 4.4 CCN(Cc1ccc(O)cc1Cl)C(=O)Cc1cccc(CC(C)(C)NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)c1 10.1021/jm1005989
CHEMBL1242969 16510 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 603 13 5 7 4.4 CCN(Cc1ccc(O)cc1Cl)C(=O)Cc1cccc(CC(C)(C)NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)c1 10.1021/jm1005989
156019922 177759 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 372 8 4 6 2.0 COc1ccccc1CCCNCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmc.2019.115178
CHEMBL4645720 177759 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 372 8 4 6 2.0 COc1ccccc1CCCNCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmc.2019.115178
CHEMBL4651233 177759 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 372 8 4 6 2.0 COc1ccccc1CCCNCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmc.2019.115178
16049309 63754 0 None 100 3 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 481 13 5 7 3.5 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCCSCCNCCc3ccccc3Cl)c2s1 10.1016/j.bmcl.2011.05.097
CHEMBL1807870 63754 0 None 100 3 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 481 13 5 7 3.5 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCCSCCNCCc3ccccc3Cl)c2s1 10.1016/j.bmcl.2011.05.097
9874175 58215 1 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 640 16 5 7 7.0 O=C(Nc1ccccc1-c1ccccc1)OC1CCN(CCCCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1021/jm501915g
CHEMBL1683934 58215 1 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 640 16 5 7 7.0 O=C(Nc1ccccc1-c1ccccc1)OC1CCN(CCCCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1021/jm501915g
118737349 118533 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 739 13 6 9 6.4 COc1c(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc(NC(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1Cl 10.1021/jm501915g
CHEMBL3426692 118533 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 739 13 6 9 6.4 COc1c(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc(NC(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1Cl 10.1021/jm501915g
9871386 111766 4 None 8 4 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 521 10 5 6 5.5 COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1-c1ccccc1 10.1016/j.bmcl.2014.04.095
CHEMBL3290999 111766 4 None 8 4 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 521 10 5 6 5.5 COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1-c1ccccc1 10.1016/j.bmcl.2014.04.095
24901349 69972 0 None 56 4 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 481 11 5 6 3.6 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3ccc(CNCCc4ccccc4F)cc3)c2s1 10.1016/j.bmcl.2011.10.049
CHEMBL1944692 69972 0 None 56 4 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 481 11 5 6 3.6 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3ccc(CNCCc4ccccc4F)cc3)c2s1 10.1016/j.bmcl.2011.10.049
57398562 70002 0 None 112 4 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 477 11 5 6 4.1 CC(CNCc1ccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)cc1)c1ccccc1 10.1016/j.bmcl.2011.10.049
CHEMBL1945036 70002 0 None 112 4 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 477 11 5 6 4.1 CC(CNCc1ccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)cc1)c1ccccc1 10.1016/j.bmcl.2011.10.049
24900942 70031 0 None 31 4 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 493 12 5 7 3.5 COc1ccccc1CNCCc1cccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)c1 10.1016/j.bmcl.2011.10.049
CHEMBL1945299 70031 0 None 31 4 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 493 12 5 7 3.5 COc1ccccc1CNCCc1cccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)c1 10.1016/j.bmcl.2011.10.049
10184665 3916 48 None 44 3 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1021/jm401532g
4799 3916 48 None 44 3 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1021/jm401532g
7353 3916 48 None 44 3 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1021/jm401532g
CHEMBL1198857 3916 48 None 44 3 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1021/jm401532g
DB09082 3916 48 None 44 3 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1021/jm401532g
10184665 3916 48 None 44 3 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1016/j.bmc.2011.08.043
4799 3916 48 None 44 3 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1016/j.bmc.2011.08.043
7353 3916 48 None 44 3 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1016/j.bmc.2011.08.043
CHEMBL1198857 3916 48 None 44 3 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1016/j.bmc.2011.08.043
DB09082 3916 48 None 44 3 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1016/j.bmc.2011.08.043
9871386 111766 4 None 8 4 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human beta2 receptor in BEAS-2B cells assessed as cAMP accumulation by radioimmunoassayAgonist activity at human beta2 receptor in BEAS-2B cells assessed as cAMP accumulation by radioimmunoassay
ChEMBL 521 10 5 6 5.5 COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1-c1ccccc1 10.1016/j.bmcl.2014.04.069
CHEMBL3290999 111766 4 None 8 4 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human beta2 receptor in BEAS-2B cells assessed as cAMP accumulation by radioimmunoassayAgonist activity at human beta2 receptor in BEAS-2B cells assessed as cAMP accumulation by radioimmunoassay
ChEMBL 521 10 5 6 5.5 COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1-c1ccccc1 10.1016/j.bmcl.2014.04.069
10184665 3916 48 None 44 3 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1021/jm100326d
4799 3916 48 None 44 3 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1021/jm100326d
7353 3916 48 None 44 3 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1021/jm100326d
CHEMBL1198857 3916 48 None 44 3 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1021/jm100326d
DB09082 3916 48 None 44 3 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1021/jm100326d
46832798 14073 0 None 19 3 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 485 16 4 6 4.6 OCc1cc([C@@H](O)CNCCCCCCOCCOCc2cc(Cl)ccc2Cl)ccc1O 10.1021/jm100326d
CHEMBL1084648 14073 0 None 19 3 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 485 16 4 6 4.6 OCc1cc([C@@H](O)CNCCCCCCOCCOCc2cc(Cl)ccc2Cl)ccc1O 10.1021/jm100326d
CHEMBL1198879 14073 0 None 19 3 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 485 16 4 6 4.6 OCc1cc([C@@H](O)CNCCCCCCOCCOCc2cc(Cl)ccc2Cl)ccc1O 10.1021/jm100326d
10225563 14079 0 None 12 3 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 445 16 4 6 3.9 Cc1cc(C)cc(COCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm100326d
CHEMBL1084891 14079 0 None 12 3 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 445 16 4 6 3.9 Cc1cc(C)cc(COCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm100326d
CHEMBL1198889 14079 0 None 12 3 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 445 16 4 6 3.9 Cc1cc(C)cc(COCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm100326d
22712045 69859 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 423 11 5 6 2.9 OCc1cc(C(O)CNCCc2ccc(OCC(O)c3ccccc3)cc2)ccc1O 10.1016/j.bmcl.2011.11.072
CHEMBL1940816 69859 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 423 11 5 6 2.9 OCc1cc(C(O)CNCCc2ccc(OCC(O)c3ccccc3)cc2)ccc1O 10.1016/j.bmcl.2011.11.072
12093446 69877 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 459 10 5 5 4.6 Nc1c(Cl)cc([C@@H](O)CNCCc2ccc(NC[C@H](O)c3ccccc3)cc2)cc1Cl 10.1016/j.bmcl.2011.11.072
CHEMBL1940834 69877 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 459 10 5 5 4.6 Nc1c(Cl)cc([C@@H](O)CNCCc2ccc(NC[C@H](O)c3ccccc3)cc2)cc1Cl 10.1016/j.bmcl.2011.11.072
1239 1639 46 None -1 5 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2009.10.013
3410 1639 46 None -1 5 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2009.10.013
3465 1639 46 None -1 5 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2009.10.013
CHEMBL1256786 1639 46 None -1 5 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2009.10.013
DB00983 1639 46 None -1 5 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2009.10.013
45483816 195450 0 None 12 2 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 370 6 4 5 2.7 Cc1cccc(CC(C)(C)NCC(O)c2ccc(O)c3c2OCC(=O)N3)c1 10.1016/j.bmcl.2009.10.013
CHEMBL567833 195450 0 None 12 2 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 370 6 4 5 2.7 Cc1cccc(CC(C)(C)NCC(O)c2ccc(O)c3c2OCC(=O)N3)c1 10.1016/j.bmcl.2009.10.013
45483864 197221 0 None 9 2 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 424 6 4 5 3.4 CC(C)(Cc1ccc(C(F)(F)F)cc1)NCC(O)c1ccc(O)c2c1OCC(=O)N2 10.1016/j.bmcl.2009.10.013
CHEMBL584498 197221 0 None 9 2 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 424 6 4 5 3.4 CC(C)(Cc1ccc(C(F)(F)F)cc1)NCC(O)c1ccc(O)c2c1OCC(=O)N2 10.1016/j.bmcl.2009.10.013
53379897 63300 0 None 151 2 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assayAgonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assay
ChEMBL 337 6 4 4 3.5 C[C@H](Cc1ccc2ccccc2c1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2009.11.062
CHEMBL1800961 63300 0 None 151 2 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assayAgonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assay
ChEMBL 337 6 4 4 3.5 C[C@H](Cc1ccc2ccccc2c1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2009.11.062
1239 1639 46 None -1 5 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP level
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2009.06.104
3410 1639 46 None -1 5 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP level
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2009.06.104
3465 1639 46 None -1 5 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP level
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2009.06.104
CHEMBL1256786 1639 46 None -1 5 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP level
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2009.06.104
DB00983 1639 46 None -1 5 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP level
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2009.06.104
1239 1639 46 None -1 5 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2009.12.087
3410 1639 46 None -1 5 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2009.12.087
3465 1639 46 None -1 5 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2009.12.087
CHEMBL1256786 1639 46 None -1 5 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2009.12.087
DB00983 1639 46 None -1 5 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2009.12.087
156009486 177678 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 372 8 4 6 2.0 COc1cccc(CCCNCC(O)c2cc(O)cc3c2OCC(=O)N3)c1 10.1016/j.bmc.2019.115178
CHEMBL4632876 177678 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 372 8 4 6 2.0 COc1cccc(CCCNCC(O)c2cc(O)cc3c2OCC(=O)N3)c1 10.1016/j.bmc.2019.115178
CHEMBL4650738 177678 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 372 8 4 6 2.0 COc1cccc(CCCNCC(O)c2cc(O)cc3c2OCC(=O)N3)c1 10.1016/j.bmc.2019.115178
105 3392 84 None 3 3 Guinea pig 9.3 pEC50 = 9.3 Functional
Agonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring assessed as bronchorelaxation activity against histamine-induced contractionAgonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring assessed as bronchorelaxation activity against histamine-induced contraction
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1016/j.ejmech.2008.12.016
2083 3392 84 None 3 3 Guinea pig 9.3 pEC50 = 9.3 Functional
Agonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring assessed as bronchorelaxation activity against histamine-induced contractionAgonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring assessed as bronchorelaxation activity against histamine-induced contraction
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1016/j.ejmech.2008.12.016
558 3392 84 None 3 3 Guinea pig 9.3 pEC50 = 9.3 Functional
Agonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring assessed as bronchorelaxation activity against histamine-induced contractionAgonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring assessed as bronchorelaxation activity against histamine-induced contraction
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1016/j.ejmech.2008.12.016
CHEMBL714 3392 84 None 3 3 Guinea pig 9.3 pEC50 = 9.3 Functional
Agonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring assessed as bronchorelaxation activity against histamine-induced contractionAgonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring assessed as bronchorelaxation activity against histamine-induced contraction
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1016/j.ejmech.2008.12.016
DB01001 3392 84 None 3 3 Guinea pig 9.3 pEC50 = 9.3 Functional
Agonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring assessed as bronchorelaxation activity against histamine-induced contractionAgonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring assessed as bronchorelaxation activity against histamine-induced contraction
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1016/j.ejmech.2008.12.016
45483852 195072 0 None 14 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 392 6 4 5 2.6 CC(C)(Cc1cc(F)cc(F)c1)NCC(O)c1ccc(O)c2c1OCC(=O)N2 10.1016/j.bmcl.2009.10.013
CHEMBL565267 195072 0 None 14 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 392 6 4 5 2.6 CC(C)(Cc1cc(F)cc(F)c1)NCC(O)c1ccc(O)c2c1OCC(=O)N2 10.1016/j.bmcl.2009.10.013
45484568 196663 0 None 10 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP level
ChEMBL 541 13 6 8 1.8 CN(C)CC(=O)NCCCC(=O)Nc1ccc(CC(C)(C)NCC(O)c2ccc(O)c3c2OCC(=O)N3)cc1 10.1016/j.bmcl.2009.06.104
CHEMBL576428 196663 0 None 10 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP level
ChEMBL 541 13 6 8 1.8 CN(C)CC(=O)NCCCC(=O)Nc1ccc(CC(C)(C)NCC(O)c2ccc(O)c3c2OCC(=O)N3)cc1 10.1016/j.bmcl.2009.06.104
57401201 70498 0 None - 1 Guinea pig 9.3 pEC50 = 9.3 Functional
Agonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contractionAgonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contraction
ChEMBL 538 13 4 8 3.4 COc1ccc(C2=NN(CCCCNCC(O)c3ccc(O)c(NC=O)c3)C(=O)C3CCCCC23)cc1OC 10.1016/j.bmcl.2012.01.013
CHEMBL1951066 70498 0 None - 1 Guinea pig 9.3 pEC50 = 9.3 Functional
Agonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contractionAgonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contraction
ChEMBL 538 13 4 8 3.4 COc1ccc(C2=NN(CCCCNCC(O)c3ccc(O)c(NC=O)c3)C(=O)C3CCCCC23)cc1OC 10.1016/j.bmcl.2012.01.013
24900689 70005 0 None 3 5 Guinea pig 9.3 pEC50 = 9.3 Functional
Agonist activity at beta2 adrenoceptor in guinea pig trachea assessed as reduction in methacholine-induced contractionAgonist activity at beta2 adrenoceptor in guinea pig trachea assessed as reduction in methacholine-induced contraction
ChEMBL 479 11 5 7 3.5 COc1ccccc1CNCc1cccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)c1 10.1016/j.bmcl.2011.10.049
CHEMBL1945039 70005 0 None 3 5 Guinea pig 9.3 pEC50 = 9.3 Functional
Agonist activity at beta2 adrenoceptor in guinea pig trachea assessed as reduction in methacholine-induced contractionAgonist activity at beta2 adrenoceptor in guinea pig trachea assessed as reduction in methacholine-induced contraction
ChEMBL 479 11 5 7 3.5 COc1ccccc1CNCc1cccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)c1 10.1016/j.bmcl.2011.10.049
57393350 70175 0 None 63 2 Guinea pig 9.3 pEC50 = 9.3 Functional
Agonist activity at beta2 adrenoceptor in guinea pig trachea assessed as reduction in methacholine-induced contractionAgonist activity at beta2 adrenoceptor in guinea pig trachea assessed as reduction in methacholine-induced contraction
ChEMBL 509 11 4 5 5.6 O=c1[nH]c2c(O)ccc(CCNCCc3cccc(-c4cccc(CNCc5ccccc5)c4)c3)c2s1 10.1016/j.bmcl.2011.10.049
CHEMBL1947152 70175 0 None 63 2 Guinea pig 9.3 pEC50 = 9.3 Functional
Agonist activity at beta2 adrenoceptor in guinea pig trachea assessed as reduction in methacholine-induced contractionAgonist activity at beta2 adrenoceptor in guinea pig trachea assessed as reduction in methacholine-induced contraction
ChEMBL 509 11 4 5 5.6 O=c1[nH]c2c(O)ccc(CCNCCc3cccc(-c4cccc(CNCc5ccccc5)c4)c3)c2s1 10.1016/j.bmcl.2011.10.049
2419 3394 80 None 17 6 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at beta2-adrenoceptor endogenously expressed in human BEAS-2B cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at beta2-adrenoceptor endogenously expressed in human BEAS-2B cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.11.072
5152 3394 80 None 17 6 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at beta2-adrenoceptor endogenously expressed in human BEAS-2B cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at beta2-adrenoceptor endogenously expressed in human BEAS-2B cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.11.072
559 3394 80 None 17 6 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at beta2-adrenoceptor endogenously expressed in human BEAS-2B cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at beta2-adrenoceptor endogenously expressed in human BEAS-2B cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.11.072
CHEMBL1263 3394 80 None 17 6 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at beta2-adrenoceptor endogenously expressed in human BEAS-2B cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at beta2-adrenoceptor endogenously expressed in human BEAS-2B cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.11.072
DB00938 3394 80 None 17 6 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at beta2-adrenoceptor endogenously expressed in human BEAS-2B cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at beta2-adrenoceptor endogenously expressed in human BEAS-2B cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.11.072
9892481 69875 11 None -3 4 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at beta2-adrenoceptor endogenously expressed in human BEAS-2B cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at beta2-adrenoceptor endogenously expressed in human BEAS-2B cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 435 12 6 6 3.0 O=CNc1cc([C@@H](O)CNCCc2ccc(NC[C@H](O)c3ccccc3)cc2)ccc1O 10.1016/j.bmcl.2011.11.072
CHEMBL1940832 69875 11 None -3 4 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at beta2-adrenoceptor endogenously expressed in human BEAS-2B cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at beta2-adrenoceptor endogenously expressed in human BEAS-2B cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 435 12 6 6 3.0 O=CNc1cc([C@@H](O)CNCCc2ccc(NC[C@H](O)c3ccccc3)cc2)ccc1O 10.1016/j.bmcl.2011.11.072
1239 1639 46 None -1 5 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmc.2011.05.064
3410 1639 46 None -1 5 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmc.2011.05.064
3465 1639 46 None -1 5 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmc.2011.05.064
CHEMBL1256786 1639 46 None -1 5 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmc.2011.05.064
DB00983 1639 46 None -1 5 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmc.2011.05.064
1239 1639 46 None -1 5 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2011.04.135
3410 1639 46 None -1 5 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2011.04.135
3465 1639 46 None -1 5 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2011.04.135
CHEMBL1256786 1639 46 None -1 5 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2011.04.135
DB00983 1639 46 None -1 5 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2011.04.135
19082200 109722 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
ChEMBL 443 12 3 7 2.9 CN(CCNCCc1ccc(O)c2nc(O)sc12)C(=O)CCOCCc1ccccc1 10.1016/j.bmcl.2011.04.135
CHEMBL323776 109722 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
ChEMBL 443 12 3 7 2.9 CN(CCNCCc1ccc(O)c2nc(O)sc12)C(=O)CCOCCc1ccccc1 10.1016/j.bmcl.2011.04.135
16049377 63752 0 None 112 3 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 465 13 5 7 2.8 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCOCCCNCCc3cccc(Cl)c3)c2s1 10.1016/j.bmcl.2011.05.097
CHEMBL1807832 63752 0 None 112 3 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 465 13 5 7 2.8 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCOCCCNCCc3cccc(Cl)c3)c2s1 10.1016/j.bmcl.2011.05.097
10484922 118530 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 705 13 6 9 5.8 COc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1021/jm501915g
CHEMBL3426689 118530 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 705 13 6 9 5.8 COc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1021/jm501915g
10327461 118531 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 709 12 6 8 6.4 O=C(CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)Nc1ccc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)c(Cl)c1 10.1021/jm501915g
CHEMBL3426690 118531 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 709 12 6 8 6.4 O=C(CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)Nc1ccc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)c(Cl)c1 10.1021/jm501915g
10439505 118540 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 675 12 6 8 5.2 O=C(Nc1ccccc1-c1ccccc1)OC1CCN(CCNC(=O)c2ccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)CC1 10.1021/jm501915g
CHEMBL3426699 118540 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 675 12 6 8 5.2 O=C(Nc1ccccc1-c1ccccc1)OC1CCN(CCNC(=O)c2ccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)CC1 10.1021/jm501915g
155515718 169385 0 None 2884 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 423 9 5 5 3.1 CC(C)C(=O)Nc1ccc(CCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)cc1 10.1016/j.bmc.2018.10.043
CHEMBL4441752 169385 0 None 2884 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 423 9 5 5 3.1 CC(C)C(=O)Nc1ccc(CCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)cc1 10.1016/j.bmc.2018.10.043
155551006 173363 0 None 44 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 423 9 5 5 3.1 CC(C)C(=O)Nc1cccc(CCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1016/j.bmc.2018.10.043
CHEMBL4541169 173363 0 None 44 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 423 9 5 5 3.1 CC(C)C(=O)Nc1cccc(CCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1016/j.bmc.2018.10.043
90645345 111974 0 None 11 3 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 574 12 6 8 4.7 CC(C)(C)OC(=O)NCCOc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 10.1016/j.bmcl.2014.04.095
CHEMBL3298692 111974 0 None 11 3 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 574 12 6 8 4.7 CC(C)(C)OC(=O)NCCOc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 10.1016/j.bmcl.2014.04.095
90645346 111990 0 None 2 3 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 578 13 6 7 4.7 O=C(NCCOc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1)c1ccccc1 10.1016/j.bmcl.2014.04.095
CHEMBL3298762 111990 0 None 2 3 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 578 13 6 7 4.7 O=C(NCCOc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1)c1ccccc1 10.1016/j.bmcl.2014.04.095
2419 3394 80 None 17 6 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2014.04.095
5152 3394 80 None 17 6 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2014.04.095
559 3394 80 None 17 6 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2014.04.095
CHEMBL1263 3394 80 None 17 6 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2014.04.095
DB00938 3394 80 None 17 6 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2014.04.095
9892481 69875 11 None -3 4 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 435 12 6 6 3.0 O=CNc1cc([C@@H](O)CNCCc2ccc(NC[C@H](O)c3ccccc3)cc2)ccc1O 10.1016/j.bmcl.2014.04.095
CHEMBL1940832 69875 11 None -3 4 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 435 12 6 6 3.0 O=CNc1cc([C@@H](O)CNCCc2ccc(NC[C@H](O)c3ccccc3)cc2)ccc1O 10.1016/j.bmcl.2014.04.095
10239722 111953 0 None 11 3 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 550 11 6 7 5.0 COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1-c1ccc(CN)cc1 10.1016/j.bmcl.2014.04.095
CHEMBL3298326 111953 0 None 11 3 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 550 11 6 7 5.0 COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1-c1ccc(CN)cc1 10.1016/j.bmcl.2014.04.095
66796015 111955 0 None 35 3 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 474 11 6 7 3.2 NCCOc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 10.1016/j.bmcl.2014.04.095
CHEMBL3298328 111955 0 None 35 3 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 474 11 6 7 3.2 NCCOc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 10.1016/j.bmcl.2014.04.095
24900685 69999 0 None -3 5 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 464 11 5 7 2.9 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3cccc(CNCCc4ccccn4)c3)c2s1 10.1016/j.bmcl.2011.10.049
CHEMBL1945033 69999 0 None -3 5 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 464 11 5 7 2.9 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3cccc(CNCCc4ccccn4)c3)c2s1 10.1016/j.bmcl.2011.10.049
24900426 70003 0 None 31 4 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 477 12 5 6 3.9 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3cccc(CNCCCc4ccccc4)c3)c2s1 10.1016/j.bmcl.2011.10.049
CHEMBL1945037 70003 0 None 31 4 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 477 12 5 6 3.9 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3cccc(CNCCCc4ccccc4)c3)c2s1 10.1016/j.bmcl.2011.10.049
24901141 70180 0 None 39 4 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 531 11 5 6 4.8 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3cccc(CNCCc4c(Cl)cccc4Cl)c3)c2s1 10.1016/j.bmcl.2011.10.049
CHEMBL1947157 70180 0 None 39 4 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 531 11 5 6 4.8 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3cccc(CNCCc4c(Cl)cccc4Cl)c3)c2s1 10.1016/j.bmcl.2011.10.049
3083544 462 46 None 1 4 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O 10.1021/jm401532g
4943 462 46 None 1 4 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O 10.1021/jm401532g
7479 462 46 None 1 4 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O 10.1021/jm401532g
CHEMBL1363 462 46 None 1 4 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O 10.1021/jm401532g
DB01274 462 46 None 1 4 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O 10.1021/jm401532g
10482960 105895 0 None 316 3 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 561 18 4 7 5.1 Cc1cc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc(S(=O)(=O)C2CCCC2)c1 10.1021/jm401532g
CHEMBL3126383 105895 0 None 316 3 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 561 18 4 7 5.1 Cc1cc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc(S(=O)(=O)C2CCCC2)c1 10.1021/jm401532g
CHEMBL3139365 105895 0 None 316 3 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 561 18 4 7 5.1 Cc1cc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc(S(=O)(=O)C2CCCC2)c1 10.1021/jm401532g
3083544 462 46 None 1 4 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O 10.1016/j.bmc.2011.08.043
4943 462 46 None 1 4 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O 10.1016/j.bmc.2011.08.043
7479 462 46 None 1 4 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O 10.1016/j.bmc.2011.08.043
CHEMBL1363 462 46 None 1 4 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O 10.1016/j.bmc.2011.08.043
DB01274 462 46 None 1 4 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O 10.1016/j.bmc.2011.08.043
56658405 66240 0 None 25 3 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 501 18 6 6 4.2 CCNC(=O)Nc1ccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc1 10.1016/j.bmc.2011.08.043
CHEMBL1835856 66240 0 None 25 3 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 501 18 6 6 4.2 CCNC(=O)Nc1ccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc1 10.1016/j.bmc.2011.08.043
CHEMBL1852565 66240 0 None 25 3 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 501 18 6 6 4.2 CCNC(=O)Nc1ccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc1 10.1016/j.bmc.2011.08.043
56658407 66290 0 None 15 3 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 487 18 6 6 3.3 NC(=O)NCc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.08.043
CHEMBL1835857 66290 0 None 15 3 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 487 18 6 6 3.3 NC(=O)NCc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.08.043
CHEMBL1852796 66290 0 None 15 3 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 487 18 6 6 3.3 NC(=O)NCc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.08.043
2419 3394 80 None 17 6 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human beta2 receptor in BEAS-2B cells assessed as cAMP accumulation by radioimmunoassayAgonist activity at human beta2 receptor in BEAS-2B cells assessed as cAMP accumulation by radioimmunoassay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2014.04.069
5152 3394 80 None 17 6 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human beta2 receptor in BEAS-2B cells assessed as cAMP accumulation by radioimmunoassayAgonist activity at human beta2 receptor in BEAS-2B cells assessed as cAMP accumulation by radioimmunoassay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2014.04.069
559 3394 80 None 17 6 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human beta2 receptor in BEAS-2B cells assessed as cAMP accumulation by radioimmunoassayAgonist activity at human beta2 receptor in BEAS-2B cells assessed as cAMP accumulation by radioimmunoassay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2014.04.069
CHEMBL1263 3394 80 None 17 6 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human beta2 receptor in BEAS-2B cells assessed as cAMP accumulation by radioimmunoassayAgonist activity at human beta2 receptor in BEAS-2B cells assessed as cAMP accumulation by radioimmunoassay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2014.04.069
DB00938 3394 80 None 17 6 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human beta2 receptor in BEAS-2B cells assessed as cAMP accumulation by radioimmunoassayAgonist activity at human beta2 receptor in BEAS-2B cells assessed as cAMP accumulation by radioimmunoassay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2014.04.069
1239 1639 46 None -1 5 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1021/jm801016j
3410 1639 46 None -1 5 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1021/jm801016j
3465 1639 46 None -1 5 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1021/jm801016j
CHEMBL1256786 1639 46 None -1 5 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1021/jm801016j
DB00983 1639 46 None -1 5 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1021/jm801016j
42625513 12437 0 None 3 4 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1ccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc1 10.1021/jm801016j
CHEMBL1186722 12437 0 None 3 4 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1ccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc1 10.1021/jm801016j
CHEMBL475389 12437 0 None 3 4 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1ccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc1 10.1021/jm801016j
42625517 12597 0 None 19 4 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 536 19 5 7 3.8 CC(C)NS(=O)(=O)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
CHEMBL1187654 12597 0 None 19 4 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 536 19 5 7 3.8 CC(C)NS(=O)(=O)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
CHEMBL514032 12597 0 None 19 4 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 536 19 5 7 3.8 CC(C)NS(=O)(=O)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
3083544 462 46 None 1 4 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O 10.1021/jm100326d
4943 462 46 None 1 4 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O 10.1021/jm100326d
7479 462 46 None 1 4 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O 10.1021/jm100326d
CHEMBL1363 462 46 None 1 4 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O 10.1021/jm100326d
DB01274 462 46 None 1 4 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O 10.1021/jm100326d
10128077 111764 0 None 1 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 484 11 5 6 5.2 COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c(CO)c3)cc2)cc1-c1ccccc1 10.1016/j.bmcl.2014.04.069
CHEMBL3290997 111764 0 None 1 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 484 11 5 6 5.2 COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c(CO)c3)cc2)cc1-c1ccccc1 10.1016/j.bmcl.2014.04.069
45483843 195350 0 None 9 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 384 7 4 5 2.9 CCc1ccc(CC(C)(C)NCC(O)c2ccc(O)c3c2OCC(=O)N3)cc1 10.1016/j.bmcl.2009.10.013
CHEMBL567192 195350 0 None 9 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 384 7 4 5 2.9 CCc1ccc(CC(C)(C)NCC(O)c2ccc(O)c3c2OCC(=O)N3)cc1 10.1016/j.bmcl.2009.10.013
45483868 195536 0 None 6 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 424 6 4 5 3.4 CC(C)(Cc1cccc(C(F)(F)F)c1)NCC(O)c1ccc(O)c2c1OCC(=O)N2 10.1016/j.bmcl.2009.10.013
CHEMBL568273 195536 0 None 6 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 424 6 4 5 3.4 CC(C)(Cc1cccc(C(F)(F)F)c1)NCC(O)c1ccc(O)c2c1OCC(=O)N2 10.1016/j.bmcl.2009.10.013
156010782 177685 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 446 8 4 5 4.3 CC(C)(CC(c1ccccc1)c1ccccc1)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmc.2019.115178
CHEMBL4632435 177685 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 446 8 4 5 4.3 CC(C)(CC(c1ccccc1)c1ccccc1)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmc.2019.115178
CHEMBL4650800 177685 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 446 8 4 5 4.3 CC(C)(CC(c1ccccc1)c1ccccc1)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmc.2019.115178
56678847 66030 0 None 99 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 527 18 5 7 3.2 O=C1CN(Cc2cccc(CCCCOCCCCCCNC[C@H](O)c3ccc(O)c(CO)c3)c2)C(=O)N1 10.1016/j.bmc.2011.05.064
CHEMBL1814274 66030 0 None 99 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 527 18 5 7 3.2 O=C1CN(Cc2cccc(CCCCOCCCCCCNC[C@H](O)c3ccc(O)c(CO)c3)c2)C(=O)N1 10.1016/j.bmc.2011.05.064
CHEMBL1851691 66030 0 None 99 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 527 18 5 7 3.2 O=C1CN(Cc2cccc(CCCCOCCCCCCNC[C@H](O)c3ccc(O)c(CO)c3)c2)C(=O)N1 10.1016/j.bmc.2011.05.064
9871096 66302 0 None 1 4 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 513 17 5 7 3.2 O=C1CNC(=O)N1c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.05.064
CHEMBL1814268 66302 0 None 1 4 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 513 17 5 7 3.2 O=C1CNC(=O)N1c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.05.064
CHEMBL1852860 66302 0 None 1 4 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 513 17 5 7 3.2 O=C1CNC(=O)N1c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.05.064
16049234 63748 0 None 177 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 481 13 5 7 3.5 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCSCCCNCCc3ccccc3Cl)c2s1 10.1016/j.bmcl.2011.05.097
CHEMBL1807828 63748 0 None 177 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 481 13 5 7 3.5 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCSCCCNCCc3ccccc3Cl)c2s1 10.1016/j.bmcl.2011.05.097
56673674 63751 0 None 1258 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 513 13 5 8 2.2 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCS(=O)(=O)CCCNCCc3cccc(Cl)c3)c2s1 10.1016/j.bmcl.2011.05.097
CHEMBL1807831 63751 0 None 1258 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 513 13 5 8 2.2 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCS(=O)(=O)CCCNCCc3cccc(Cl)c3)c2s1 10.1016/j.bmcl.2011.05.097
183812 204015 21 None 15 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 464 13 3 8 2.9 O=S(=O)(CCCOCCc1ccccc1)CCNCCc1ccc(O)c2nc(O)sc12 10.1016/j.bmcl.2011.05.097
CHEMBL82663 204015 21 None 15 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 464 13 3 8 2.9 O=S(=O)(CCCOCCc1ccccc1)CCNCCc1ccc(O)c2nc(O)sc12 10.1016/j.bmcl.2011.05.097
56943517 111999 0 None 3 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 621 13 5 9 2.8 CS(=O)(=O)N1CCN(CCOc2ccc(Nc3ccc(CCNC[C@H](O)c4ccc(O)c5[nH]c(=O)ccc45)cc3)cc2)CC1 10.1016/j.bmcl.2014.04.095
CHEMBL3298832 111999 0 None 3 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 621 13 5 9 2.8 CS(=O)(=O)N1CCN(CCOc2ccc(Nc3ccc(CCNC[C@H](O)c4ccc(O)c5[nH]c(=O)ccc45)cc3)cc2)CC1 10.1016/j.bmcl.2014.04.095
56943518 111956 0 None 25 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 488 12 6 7 3.6 NCCCOc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 10.1016/j.bmcl.2014.04.095
CHEMBL3298329 111956 0 None 25 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 488 12 6 7 3.6 NCCCOc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 10.1016/j.bmcl.2014.04.095
56943545 111957 0 None 28 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 502 13 6 7 4.0 NCCCCOc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 10.1016/j.bmcl.2014.04.095
CHEMBL3298330 111957 0 None 28 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 502 13 6 7 4.0 NCCCCOc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 10.1016/j.bmcl.2014.04.095
56943546 111973 0 None 25 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 518 14 6 8 3.2 NCCOCCOc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 10.1016/j.bmcl.2014.04.095
CHEMBL3298691 111973 0 None 25 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 518 14 6 8 3.2 NCCOCCOc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 10.1016/j.bmcl.2014.04.095
90645347 112008 0 None 7 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 578 12 6 7 5.6 CC(C)(N)COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1-c1ccccc1 10.1016/j.bmcl.2014.04.095
CHEMBL3298987 112008 0 None 7 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 578 12 6 7 5.6 CC(C)(N)COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1-c1ccccc1 10.1016/j.bmcl.2014.04.095
24900689 70005 0 None -3 5 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 479 11 5 7 3.5 COc1ccccc1CNCc1cccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)c1 10.1016/j.bmcl.2011.10.049
CHEMBL1945039 70005 0 None -3 5 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 479 11 5 7 3.5 COc1ccccc1CNCc1cccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)c1 10.1016/j.bmcl.2011.10.049
24900813 70008 0 None 7 4 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 467 10 5 6 3.6 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3cccc(CNCc4ccccc4F)c3)c2s1 10.1016/j.bmcl.2011.10.049
CHEMBL1945042 70008 0 None 7 4 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 467 10 5 6 3.6 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3cccc(CNCc4ccccc4F)c3)c2s1 10.1016/j.bmcl.2011.10.049
24900812 70009 0 None 25 4 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 450 10 5 7 2.8 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3cccc(CNCc4ccccn4)c3)c2s1 10.1016/j.bmcl.2011.10.049
CHEMBL1945043 70009 0 None 25 4 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 450 10 5 7 2.8 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3cccc(CNCc4ccccn4)c3)c2s1 10.1016/j.bmcl.2011.10.049
24900937 70026 0 None 199 4 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 413 8 4 6 2.8 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3cccc(CN4CCCC4)c3)c2s1 10.1016/j.bmcl.2011.10.049
CHEMBL1945294 70026 0 None 199 4 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 413 8 4 6 2.8 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3cccc(CN4CCCC4)c3)c2s1 10.1016/j.bmcl.2011.10.049
24900424 70179 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 525 11 5 6 5.1 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3cccc(-c4cccc(CNCc5ccccc5)c4)c3)c2s1 10.1016/j.bmcl.2011.10.049
CHEMBL1947156 70179 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 525 11 5 6 5.1 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3cccc(-c4cccc(CNCc5ccccc5)c4)c3)c2s1 10.1016/j.bmcl.2011.10.049
183812 204015 21 None 15 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 464 13 3 8 2.9 O=S(=O)(CCCOCCc1ccccc1)CCNCCc1ccc(O)c2nc(O)sc12 10.1016/j.bmcl.2011.10.049
CHEMBL82663 204015 21 None 15 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 464 13 3 8 2.9 O=S(=O)(CCCOCCc1ccccc1)CCNCCc1ccc(O)c2nc(O)sc12 10.1016/j.bmcl.2011.10.049
56672269 66239 0 None 50 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 515 19 6 6 3.9 CCNC(=O)NCc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.08.043
CHEMBL1835858 66239 0 None 50 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 515 19 6 6 3.9 CCNC(=O)NCc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.08.043
CHEMBL1852564 66239 0 None 50 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 515 19 6 6 3.9 CCNC(=O)NCc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.08.043
42625515 12606 0 None 794 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 508 18 5 7 3.0 CNS(=O)(=O)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
CHEMBL1187711 12606 0 None 794 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 508 18 5 7 3.0 CNS(=O)(=O)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
CHEMBL516056 12606 0 None 794 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 508 18 5 7 3.0 CNS(=O)(=O)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
10077662 89793 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
ChEMBL 623 14 5 8 5.1 COc1cccc(OC)c1CNC(=O)c1cc2cc(C[C@@H](C)NC[C@H](O)c3ccc(O)c(CO)c3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2007.09.031
CHEMBL238347 89793 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
ChEMBL 623 14 5 8 5.1 COc1cccc(OC)c1CNC(=O)c1cc2cc(C[C@@H](C)NC[C@H](O)c3ccc(O)c(CO)c3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2007.09.031
156015718 177671 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 356 7 4 5 2.3 Cc1cccc(CCCNCC(O)c2cc(O)cc3c2OCC(=O)N3)c1 10.1016/j.bmc.2019.115178
CHEMBL4648695 177671 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 356 7 4 5 2.3 Cc1cccc(CCCNCC(O)c2cc(O)cc3c2OCC(=O)N3)c1 10.1016/j.bmc.2019.115178
CHEMBL4650694 177671 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 356 7 4 5 2.3 Cc1cccc(CCCNCC(O)c2cc(O)cc3c2OCC(=O)N3)c1 10.1016/j.bmc.2019.115178
44237670 57914 0 None 8128 2 Guinea pig 9.2 pEC50 = 9.2 Functional
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
ChEMBL 534 9 6 5 5.4 O=C(Nc1cccc(CCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1)Nc1ccccc1-c1ccccc1 10.1016/j.bmcl.2010.12.096
CHEMBL1682219 57914 0 None 8128 2 Guinea pig 9.2 pEC50 = 9.2 Functional
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
ChEMBL 534 9 6 5 5.4 O=C(Nc1cccc(CCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1)Nc1ccccc1-c1ccccc1 10.1016/j.bmcl.2010.12.096
45483814 195586 0 None 5 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 440 7 4 6 3.3 CC(C)(Cc1ccc(OC(F)(F)F)cc1)NCC(O)c1ccc(O)c2c1OCC(=O)N2 10.1016/j.bmcl.2009.10.013
CHEMBL568531 195586 0 None 5 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 440 7 4 6 3.3 CC(C)(Cc1ccc(OC(F)(F)F)cc1)NCC(O)c1ccc(O)c2c1OCC(=O)N2 10.1016/j.bmcl.2009.10.013
1499 2052 43 None -72 36 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human beta2-AR expressed in CHOK1 cells co-expressing Galpha15 measured after 21 secs to 120 secs by Calcium-4 dye based FLIPR assayAgonist activity at human beta2-AR expressed in CHOK1 cells co-expressing Galpha15 measured after 21 secs to 120 secs by Calcium-4 dye based FLIPR assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/acs.jnatprod.7b00762
3779 2052 43 None -72 36 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human beta2-AR expressed in CHOK1 cells co-expressing Galpha15 measured after 21 secs to 120 secs by Calcium-4 dye based FLIPR assayAgonist activity at human beta2-AR expressed in CHOK1 cells co-expressing Galpha15 measured after 21 secs to 120 secs by Calcium-4 dye based FLIPR assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/acs.jnatprod.7b00762
536 2052 43 None -72 36 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human beta2-AR expressed in CHOK1 cells co-expressing Galpha15 measured after 21 secs to 120 secs by Calcium-4 dye based FLIPR assayAgonist activity at human beta2-AR expressed in CHOK1 cells co-expressing Galpha15 measured after 21 secs to 120 secs by Calcium-4 dye based FLIPR assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/acs.jnatprod.7b00762
CHEMBL434 2052 43 None -72 36 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human beta2-AR expressed in CHOK1 cells co-expressing Galpha15 measured after 21 secs to 120 secs by Calcium-4 dye based FLIPR assayAgonist activity at human beta2-AR expressed in CHOK1 cells co-expressing Galpha15 measured after 21 secs to 120 secs by Calcium-4 dye based FLIPR assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/acs.jnatprod.7b00762
DB01064 2052 43 None -72 36 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human beta2-AR expressed in CHOK1 cells co-expressing Galpha15 measured after 21 secs to 120 secs by Calcium-4 dye based FLIPR assayAgonist activity at human beta2-AR expressed in CHOK1 cells co-expressing Galpha15 measured after 21 secs to 120 secs by Calcium-4 dye based FLIPR assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/acs.jnatprod.7b00762
46232769 199146 0 None 6 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 370 6 4 5 2.7 Cc1ccccc1CC(C)(C)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmcl.2009.12.087
CHEMBL601036 199146 0 None 6 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 370 6 4 5 2.7 Cc1ccccc1CC(C)(C)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmcl.2009.12.087
44434116 166031 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
ChEMBL 547 12 5 8 3.6 COc1cccc(OC)c1CNC(=O)c1cc2cc(C[C@@H](C)NC[C@H](O)c3ccc(O)c(CO)c3)ccc2n1C 10.1016/j.bmcl.2007.09.031
CHEMBL428027 166031 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
ChEMBL 547 12 5 8 3.6 COc1cccc(OC)c1CNC(=O)c1cc2cc(C[C@@H](C)NC[C@H](O)c3ccc(O)c(CO)c3)ccc2n1C 10.1016/j.bmcl.2007.09.031
2419 3394 80 None 17 6 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technologyAgonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technology
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/acs.jmedchem.0c01195
5152 3394 80 None 17 6 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technologyAgonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technology
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/acs.jmedchem.0c01195
559 3394 80 None 17 6 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technologyAgonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technology
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/acs.jmedchem.0c01195
CHEMBL1263 3394 80 None 17 6 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technologyAgonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technology
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/acs.jmedchem.0c01195
DB00938 3394 80 None 17 6 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technologyAgonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technology
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/acs.jmedchem.0c01195
156014816 177718 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 360 7 4 5 2.1 O=C1COc2c(cc(O)cc2C(O)CNCCCc2ccc(F)cc2)N1 10.1016/j.bmc.2019.115178
CHEMBL4645932 177718 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 360 7 4 5 2.1 O=C1COc2c(cc(O)cc2C(O)CNCCCc2ccc(F)cc2)N1 10.1016/j.bmc.2019.115178
CHEMBL4650992 177718 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 360 7 4 5 2.1 O=C1COc2c(cc(O)cc2C(O)CNCCCc2ccc(F)cc2)N1 10.1016/j.bmc.2019.115178
63952 8487 37 None -2 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assayAgonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assay
ChEMBL 368 7 4 5 2.5 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1 10.1021/jm100068m
86306667 8487 37 None -2 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assayAgonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assay
ChEMBL 368 7 4 5 2.5 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1 10.1021/jm100068m
CHEMBL1094785 8487 37 None -2 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assayAgonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assay
ChEMBL 368 7 4 5 2.5 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1 10.1021/jm100068m
4183 1986 62 None 1 4 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at beta2 adrenoceptor (unknown origin)Agonist activity at beta2 adrenoceptor (unknown origin)
ChEMBL 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O 10.1021/acs.jmedchem.0c01195
6918554 1986 62 None 1 4 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at beta2 adrenoceptor (unknown origin)Agonist activity at beta2 adrenoceptor (unknown origin)
ChEMBL 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O 10.1021/acs.jmedchem.0c01195
7455 1986 62 None 1 4 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at beta2 adrenoceptor (unknown origin)Agonist activity at beta2 adrenoceptor (unknown origin)
ChEMBL 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O 10.1021/acs.jmedchem.0c01195
CHEMBL1095777 1986 62 None 1 4 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at beta2 adrenoceptor (unknown origin)Agonist activity at beta2 adrenoceptor (unknown origin)
ChEMBL 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O 10.1021/acs.jmedchem.0c01195
DB05039 1986 62 None 1 4 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at beta2 adrenoceptor (unknown origin)Agonist activity at beta2 adrenoceptor (unknown origin)
ChEMBL 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O 10.1021/acs.jmedchem.0c01195
9871096 66302 0 None -1 4 Guinea pig 9.1 pEC50 = 9.1 Functional
Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contractionAgonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contraction
ChEMBL 513 17 5 7 3.2 O=C1CNC(=O)N1c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.05.064
CHEMBL1814268 66302 0 None -1 4 Guinea pig 9.1 pEC50 = 9.1 Functional
Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contractionAgonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contraction
ChEMBL 513 17 5 7 3.2 O=C1CNC(=O)N1c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.05.064
CHEMBL1852860 66302 0 None -1 4 Guinea pig 9.1 pEC50 = 9.1 Functional
Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contractionAgonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contraction
ChEMBL 513 17 5 7 3.2 O=C1CNC(=O)N1c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.05.064
56658246 64151 0 None -3 4 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 525 17 5 8 2.9 O=c1cc[nH]c(=O)n1-c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.05.064
CHEMBL1814277 64151 0 None -3 4 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 525 17 5 8 2.9 O=c1cc[nH]c(=O)n1-c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.05.064
CHEMBL1814278 64151 0 None -3 4 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 525 17 5 8 2.9 O=c1cc[nH]c(=O)n1-c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.05.064
53357712 66059 0 None 79 3 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 541 17 5 7 3.9 CC1(C)NC(=O)N(c2cccc(CCCCOCCCCCCNC[C@H](O)c3ccc(O)c(CO)c3)c2)C1=O 10.1016/j.bmc.2011.05.064
CHEMBL1814271 66059 0 None 79 3 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 541 17 5 7 3.9 CC1(C)NC(=O)N(c2cccc(CCCCOCCCCCCNC[C@H](O)c3ccc(O)c(CO)c3)c2)C1=O 10.1016/j.bmc.2011.05.064
CHEMBL1851848 66059 0 None 79 3 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 541 17 5 7 3.9 CC1(C)NC(=O)N(c2cccc(CCCCOCCCCCCNC[C@H](O)c3ccc(O)c(CO)c3)c2)C1=O 10.1016/j.bmc.2011.05.064
56678849 66278 0 None 31 3 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 541 18 5 8 2.7 O=C1NC(=O)N(Cc2cccc(CCCCOCCCCCCNC[C@H](O)c3ccc(O)c(CO)c3)c2)C1=O 10.1016/j.bmc.2011.05.064
CHEMBL1814275 66278 0 None 31 3 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 541 18 5 8 2.7 O=C1NC(=O)N(Cc2cccc(CCCCOCCCCCCNC[C@H](O)c3ccc(O)c(CO)c3)c2)C1=O 10.1016/j.bmc.2011.05.064
CHEMBL1852744 66278 0 None 31 3 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 541 18 5 8 2.7 O=C1NC(=O)N(Cc2cccc(CCCCOCCCCCCNC[C@H](O)c3ccc(O)c(CO)c3)c2)C1=O 10.1016/j.bmc.2011.05.064
2419 3394 80 None 17 6 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.04.135
5152 3394 80 None 17 6 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.04.135
559 3394 80 None 17 6 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.04.135
CHEMBL1263 3394 80 None 17 6 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.04.135
DB00938 3394 80 None 17 6 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.04.135
16049289 63219 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
ChEMBL 501 15 4 7 3.2 CCCCN(CCNC[C@H](O)c1ccc(O)c2[nH]c(=O)sc12)C(=O)CCOCCc1ccccc1 10.1016/j.bmcl.2011.04.135
CHEMBL1800660 63219 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
ChEMBL 501 15 4 7 3.2 CCCCN(CCNC[C@H](O)c1ccc(O)c2[nH]c(=O)sc12)C(=O)CCOCCc1ccccc1 10.1016/j.bmcl.2011.04.135
2419 3394 80 None 17 6 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.05.097
5152 3394 80 None 17 6 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.05.097
559 3394 80 None 17 6 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.05.097
CHEMBL1263 3394 80 None 17 6 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.05.097
DB00938 3394 80 None 17 6 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.05.097
16049090 63743 0 None 316 3 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 447 13 5 7 2.9 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCSCCCNCCc3ccccc3)c2s1 10.1016/j.bmcl.2011.05.097
CHEMBL1807823 63743 0 None 316 3 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 447 13 5 7 2.9 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCSCCCNCCc3ccccc3)c2s1 10.1016/j.bmcl.2011.05.097
56673609 63757 0 None 112 3 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 499 13 5 7 3.5 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCCOCCNCCc3cccc(Cl)c3Cl)c2s1 10.1016/j.bmcl.2011.05.097
CHEMBL1807873 63757 0 None 112 3 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 499 13 5 7 3.5 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCCOCCNCCc3cccc(Cl)c3Cl)c2s1 10.1016/j.bmcl.2011.05.097
319 1292 39 None -2 6 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/jm501915g
321 1292 39 None -2 6 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/jm501915g
444031 1292 39 None -2 6 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/jm501915g
784 1292 39 None -2 6 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/jm501915g
CHEMBL1346 1292 39 None -2 6 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/jm501915g
DB00496 1292 39 None -2 6 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/jm501915g
118737356 118544 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 753 13 5 9 6.5 COc1cc(N(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/jm501915g
CHEMBL3426703 118544 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 753 13 5 9 6.5 COc1cc(N(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/jm501915g
118737360 118549 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 719 14 6 9 5.8 COc1ccc(NC(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)cc1CCNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/jm501915g
CHEMBL3426708 118549 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 719 14 6 9 5.8 COc1ccc(NC(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)cc1CCNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/jm501915g
90645344 111951 0 None 7 3 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 550 11 6 7 5.0 COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1-c1ccccc1CN 10.1016/j.bmcl.2014.04.095
CHEMBL3298324 111951 0 None 7 3 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 550 11 6 7 5.0 COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1-c1ccccc1CN 10.1016/j.bmcl.2014.04.095
2419 3394 80 None 17 6 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.10.049
5152 3394 80 None 17 6 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.10.049
559 3394 80 None 17 6 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.10.049
CHEMBL1263 3394 80 None 17 6 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.10.049
DB00938 3394 80 None 17 6 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.10.049
24900750 70021 0 None 5 4 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 479 11 5 7 3.5 COc1ccc(CNCc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)sc34)c2)cc1 10.1016/j.bmcl.2011.10.049
CHEMBL1945289 70021 0 None 5 4 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 479 11 5 7 3.5 COc1ccc(CNCc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)sc34)c2)cc1 10.1016/j.bmcl.2011.10.049
24901285 70029 0 None 25 4 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 545 11 5 6 5.2 CC(Cc1cccc(CNCCc2c(Cl)cccc2Cl)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)sc12 10.1016/j.bmcl.2011.10.049
CHEMBL1945297 70029 0 None 25 4 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 545 11 5 6 5.2 CC(Cc1cccc(CNCCc2c(Cl)cccc2Cl)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)sc12 10.1016/j.bmcl.2011.10.049
156015629 177668 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 482 8 4 5 4.6 CC(C)(CC(c1ccc(F)cc1)c1ccc(F)cc1)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmc.2019.115178
CHEMBL4648440 177668 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 482 8 4 5 4.6 CC(C)(CC(c1ccc(F)cc1)c1ccc(F)cc1)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmc.2019.115178
CHEMBL4650679 177668 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 482 8 4 5 4.6 CC(C)(CC(c1ccc(F)cc1)c1ccc(F)cc1)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmc.2019.115178
10238776 66128 0 None 3 4 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 473 17 6 6 3.6 NC(=O)Nc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.08.043
CHEMBL1835853 66128 0 None 3 4 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 473 17 6 6 3.6 NC(=O)Nc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.08.043
CHEMBL1852214 66128 0 None 3 4 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 473 17 6 6 3.6 NC(=O)Nc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.08.043
10217757 111765 0 None 10 4 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human beta2 receptor in BEAS-2B cells assessed as cAMP accumulation by radioimmunoassayAgonist activity at human beta2 receptor in BEAS-2B cells assessed as cAMP accumulation by radioimmunoassay
ChEMBL 497 12 5 6 5.2 COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c(NC=O)c3)cc2)cc1-c1ccccc1 10.1016/j.bmcl.2014.04.069
CHEMBL3290998 111765 0 None 10 4 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human beta2 receptor in BEAS-2B cells assessed as cAMP accumulation by radioimmunoassayAgonist activity at human beta2 receptor in BEAS-2B cells assessed as cAMP accumulation by radioimmunoassay
ChEMBL 497 12 5 6 5.2 COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c(NC=O)c3)cc2)cc1-c1ccccc1 10.1016/j.bmcl.2014.04.069
42625511 12613 0 None 3 4 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1ccccc1CCCCOCCCCCCNC[C@H](O)c1ccc(O)c(CO)c1 10.1021/jm801016j
CHEMBL1187778 12613 0 None 3 4 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1ccccc1CCCCOCCCCCCNC[C@H](O)c1ccc(O)c(CO)c1 10.1021/jm801016j
CHEMBL520313 12613 0 None 3 4 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1ccccc1CCCCOCCCCCCNC[C@H](O)c1ccc(O)c(CO)c1 10.1021/jm801016j
10203169 14109 0 None 25 3 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 433 16 5 7 3.0 OCc1cc([C@@H](O)CNCCCCCCOCCOCc2cccc(O)c2)ccc1O 10.1021/jm100326d
CHEMBL1086536 14109 0 None 25 3 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 433 16 5 7 3.0 OCc1cc([C@@H](O)CNCCCCCCOCCOCc2cccc(O)c2)ccc1O 10.1021/jm100326d
CHEMBL1199300 14109 0 None 25 3 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 433 16 5 7 3.0 OCc1cc([C@@H](O)CNCCCCCCOCCOCc2cccc(O)c2)ccc1O 10.1021/jm100326d
319 1292 39 None -2 6 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2011.01.043
321 1292 39 None -2 6 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2011.01.043
444031 1292 39 None -2 6 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2011.01.043
784 1292 39 None -2 6 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2011.01.043
CHEMBL1346 1292 39 None -2 6 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2011.01.043
DB00496 1292 39 None -2 6 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2011.01.043
1499 2052 43 None -72 36 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassayAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmcl.2009.06.083
3779 2052 43 None -72 36 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassayAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmcl.2009.06.083
536 2052 43 None -72 36 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassayAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmcl.2009.06.083
CHEMBL434 2052 43 None -72 36 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassayAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmcl.2009.06.083
DB01064 2052 43 None -72 36 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassayAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmcl.2009.06.083
156014807 177645 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 358 7 5 6 1.7 O=C1COc2c(cc(O)cc2C(O)CNCCCc2ccc(O)cc2)N1 10.1016/j.bmc.2019.115178
CHEMBL4643561 177645 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 358 7 5 6 1.7 O=C1COc2c(cc(O)cc2C(O)CNCCCc2ccc(O)cc2)N1 10.1016/j.bmc.2019.115178
CHEMBL4650530 177645 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 358 7 5 6 1.7 O=C1COc2c(cc(O)cc2C(O)CNCCCc2ccc(O)cc2)N1 10.1016/j.bmc.2019.115178
53316961 57937 0 None - 1 Guinea pig 9.1 pEC50 = 9.1 Functional
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
ChEMBL 528 9 6 5 4.7 CC(C)(C)c1ccc(CNC(=O)Nc2cccc(CCNCC(O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1 10.1016/j.bmcl.2010.12.096
CHEMBL1682302 57937 0 None - 1 Guinea pig 9.1 pEC50 = 9.1 Functional
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
ChEMBL 528 9 6 5 4.7 CC(C)(C)c1ccc(CNC(=O)Nc2cccc(CCNCC(O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1 10.1016/j.bmcl.2010.12.096
45484536 195528 0 None 5 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP level
ChEMBL 527 13 7 8 1.6 CC(C)(Cc1ccc(NC(=O)CCCNC(=O)CCN)cc1)NCC(O)c1ccc(O)c2c1OCC(=O)N2 10.1016/j.bmcl.2009.06.104
CHEMBL568239 195528 0 None 5 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP level
ChEMBL 527 13 7 8 1.6 CC(C)(Cc1ccc(NC(=O)CCCNC(=O)CCN)cc1)NCC(O)c1ccc(O)c2c1OCC(=O)N2 10.1016/j.bmcl.2009.06.104
53326837 58222 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
ChEMBL 722 17 5 10 5.3 C[N+]1(CCCCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)[C@@H]2C[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)C[C@@H]1[C@H]1O[C@H]12 10.1016/j.bmcl.2011.01.043
CHEMBL1683942 58222 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
ChEMBL 722 17 5 10 5.3 C[N+]1(CCCCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)[C@@H]2C[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)C[C@@H]1[C@H]1O[C@H]12 10.1016/j.bmcl.2011.01.043
155541614 172456 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 437 10 5 5 3.5 CC(C)CC(=O)Nc1cccc(CCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1016/j.bmc.2018.10.043
CHEMBL4518961 172456 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 437 10 5 5 3.5 CC(C)CC(=O)Nc1cccc(CCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1016/j.bmc.2018.10.043
156010796 177716 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 372 8 4 6 2.0 COc1ccc(CCCNCC(O)c2cc(O)cc3c2OCC(=O)N3)cc1 10.1016/j.bmc.2019.115178
CHEMBL4632700 177716 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 372 8 4 6 2.0 COc1ccc(CCCNCC(O)c2cc(O)cc3c2OCC(=O)N3)cc1 10.1016/j.bmc.2019.115178
CHEMBL4650979 177716 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 372 8 4 6 2.0 COc1ccc(CCCNCC(O)c2cc(O)cc3c2OCC(=O)N3)cc1 10.1016/j.bmc.2019.115178
11091850 46952 0 None 25 3 Human 9.0 pEC50 = 9 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-2 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-2 AR expressed as the negative logarithm of the molar drug concentration
ChEMBL 465 11 4 4 4.6 Cc1ccc(CNC(=O)Cc2ccc(NC[C@@H](C)NC[C@H](O)c3cccc(Cl)c3)cc2)cc1 10.1021/jm0101500
CHEMBL154370 46952 0 None 25 3 Human 9.0 pEC50 = 9 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-2 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-2 AR expressed as the negative logarithm of the molar drug concentration
ChEMBL 465 11 4 4 4.6 Cc1ccc(CNC(=O)Cc2ccc(NC[C@@H](C)NC[C@H](O)c3cccc(Cl)c3)cc2)cc1 10.1021/jm0101500
53357711 64152 0 None -1 4 Guinea pig 9.0 pEC50 = 9 Functional
Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contractionAgonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contraction
ChEMBL 531 19 7 7 3.3 O=C(O)CNC(=O)Nc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.05.064
CHEMBL1814279 64152 0 None -1 4 Guinea pig 9.0 pEC50 = 9 Functional
Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contractionAgonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contraction
ChEMBL 531 19 7 7 3.3 O=C(O)CNC(=O)Nc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.05.064
CHEMBL1814280 64152 0 None -1 4 Guinea pig 9.0 pEC50 = 9 Functional
Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contractionAgonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contraction
ChEMBL 531 19 7 7 3.3 O=C(O)CNC(=O)Nc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.05.064
319 1292 39 None 2 6 Guinea pig 9.0 pEC50 = 9 Functional
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2010.12.096
321 1292 39 None 2 6 Guinea pig 9.0 pEC50 = 9 Functional
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2010.12.096
444031 1292 39 None 2 6 Guinea pig 9.0 pEC50 = 9 Functional
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2010.12.096
784 1292 39 None 2 6 Guinea pig 9.0 pEC50 = 9 Functional
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2010.12.096
CHEMBL1346 1292 39 None 2 6 Guinea pig 9.0 pEC50 = 9 Functional
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2010.12.096
DB00496 1292 39 None 2 6 Guinea pig 9.0 pEC50 = 9 Functional
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2010.12.096
44237766 57916 0 None 10000 2 Guinea pig 9.0 pEC50 = 9 Functional
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
ChEMBL 550 10 6 6 5.5 O=C(Nc1cccc(CCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1)Nc1cccc(Oc2ccccc2)c1 10.1016/j.bmcl.2010.12.096
CHEMBL1682221 57916 0 None 10000 2 Guinea pig 9.0 pEC50 = 9 Functional
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
ChEMBL 550 10 6 6 5.5 O=C(Nc1cccc(CCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1)Nc1cccc(Oc2ccccc2)c1 10.1016/j.bmcl.2010.12.096
53357711 64152 0 None 1 4 Human 9.0 pEC50 = 9 Functional
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 531 19 7 7 3.3 O=C(O)CNC(=O)Nc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.05.064
CHEMBL1814279 64152 0 None 1 4 Human 9.0 pEC50 = 9 Functional
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 531 19 7 7 3.3 O=C(O)CNC(=O)Nc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.05.064
CHEMBL1814280 64152 0 None 1 4 Human 9.0 pEC50 = 9 Functional
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 531 19 7 7 3.3 O=C(O)CNC(=O)Nc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.05.064
56673241 63214 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
ChEMBL 457 13 3 6 2.9 CCN(CCNCCc1ccc(O)c2[nH]c(=O)sc12)C(=O)CCOCCc1ccccc1 10.1016/j.bmcl.2011.04.135
CHEMBL1800656 63214 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
ChEMBL 457 13 3 6 2.9 CCN(CCNCCc1ccc(O)c2[nH]c(=O)sc12)C(=O)CCOCCc1ccccc1 10.1016/j.bmcl.2011.04.135
1239 1639 46 None -1 5 Human 9.0 pEC50 = 9 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2011.05.097
3410 1639 46 None -1 5 Human 9.0 pEC50 = 9 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2011.05.097
3465 1639 46 None -1 5 Human 9.0 pEC50 = 9 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2011.05.097
CHEMBL1256786 1639 46 None -1 5 Human 9.0 pEC50 = 9 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2011.05.097
DB00983 1639 46 None -1 5 Human 9.0 pEC50 = 9 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2011.05.097
16049450 63747 0 None 125 2 Human 9.0 pEC50 = 9 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 481 13 5 7 3.5 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCSCCCNCCc3cccc(Cl)c3)c2s1 10.1016/j.bmcl.2011.05.097
CHEMBL1807827 63747 0 None 125 2 Human 9.0 pEC50 = 9 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 481 13 5 7 3.5 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCSCCCNCCc3cccc(Cl)c3)c2s1 10.1016/j.bmcl.2011.05.097
11169365 112007 0 None 22 3 Human 9.0 pEC50 = 9 Functional
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 502 11 6 7 4.0 CC(C)(N)COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 10.1016/j.bmcl.2014.04.095
CHEMBL3298986 112007 0 None 22 3 Human 9.0 pEC50 = 9 Functional
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 502 11 6 7 4.0 CC(C)(N)COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 10.1016/j.bmcl.2014.04.095
45484585 13969 0 None 3 2 Human 9.0 pEC50 = 9 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP level
ChEMBL 556 13 6 7 1.9 CC(C)(Cc1ccc(NC(=O)CCCNC(=O)C[N+](C)(C)C)cc1)NCC(O)c1ccc(O)c2c1OCC(=O)N2 10.1016/j.bmcl.2009.06.104
CHEMBL1197807 13969 0 None 3 2 Human 9.0 pEC50 = 9 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP level
ChEMBL 556 13 6 7 1.9 CC(C)(Cc1ccc(NC(=O)CCCNC(=O)C[N+](C)(C)C)cc1)NCC(O)c1ccc(O)c2c1OCC(=O)N2 10.1016/j.bmcl.2009.06.104
CHEMBL587197 13969 0 None 3 2 Human 9.0 pEC50 = 9 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP level
ChEMBL 556 13 6 7 1.9 CC(C)(Cc1ccc(NC(=O)CCCNC(=O)C[N+](C)(C)C)cc1)NCC(O)c1ccc(O)c2c1OCC(=O)N2 10.1016/j.bmcl.2009.06.104
45101519 196836 0 None 1 2 Human 9.0 pEC50 = 9 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP level
ChEMBL 498 11 8 7 1.6 CC(C)(Cc1ccc(NC(=O)CCCNC(=N)N)cc1)NCC(O)c1ccc(O)c2c1OCC(=O)N2 10.1016/j.bmcl.2009.06.104
CHEMBL577917 196836 0 None 1 2 Human 9.0 pEC50 = 9 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP level
ChEMBL 498 11 8 7 1.6 CC(C)(Cc1ccc(NC(=O)CCCNC(=N)N)cc1)NCC(O)c1ccc(O)c2c1OCC(=O)N2 10.1016/j.bmcl.2009.06.104
1239 1639 46 None -1 5 Human 9.0 pEC50 = 9 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2011.10.049
3410 1639 46 None -1 5 Human 9.0 pEC50 = 9 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2011.10.049
3465 1639 46 None -1 5 Human 9.0 pEC50 = 9 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2011.10.049
CHEMBL1256786 1639 46 None -1 5 Human 9.0 pEC50 = 9 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2011.10.049
DB00983 1639 46 None -1 5 Human 9.0 pEC50 = 9 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2011.10.049
24900872 70004 0 None 89 3 Human 9.0 pEC50 = 9 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 478 12 5 7 3.3 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3cccc(CNCCCc4ccccn4)c3)c2s1 10.1016/j.bmcl.2011.10.049
CHEMBL1945038 70004 0 None 89 3 Human 9.0 pEC50 = 9 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 478 12 5 7 3.3 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3cccc(CNCCCc4ccccn4)c3)c2s1 10.1016/j.bmcl.2011.10.049
57391554 70010 0 None 25 4 Human 9.0 pEC50 = 9 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 479 11 5 7 3.5 COc1cccc(CNCc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)sc34)c2)c1 10.1016/j.bmcl.2011.10.049
CHEMBL1945044 70010 0 None 25 4 Human 9.0 pEC50 = 9 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 479 11 5 7 3.5 COc1cccc(CNCc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)sc34)c2)c1 10.1016/j.bmcl.2011.10.049
24901140 70176 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 503 9 4 6 4.5 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3cccc(CN4CCC(c5ccccc5)CC4)c3)c2s1 10.1016/j.bmcl.2011.10.049
CHEMBL1947153 70176 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 503 9 4 6 4.5 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3cccc(CN4CCC(c5ccccc5)CC4)c3)c2s1 10.1016/j.bmcl.2011.10.049
10053159 105787 0 None 398 3 Human 9.0 pEC50 = 9 Functional
Agonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 545 18 4 7 4.6 O=S(=O)(c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1)C1CC=CC1 10.1021/jm401532g
CHEMBL3124955 105787 0 None 398 3 Human 9.0 pEC50 = 9 Functional
Agonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 545 18 4 7 4.6 O=S(=O)(c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1)C1CC=CC1 10.1021/jm401532g
CHEMBL3139033 105787 0 None 398 3 Human 9.0 pEC50 = 9 Functional
Agonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 545 18 4 7 4.6 O=S(=O)(c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1)C1CC=CC1 10.1021/jm401532g
56665368 66111 0 None 1 4 Human 9.0 pEC50 = 9 Functional
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 501 18 6 6 4.2 CCNC(=O)Nc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.08.043
CHEMBL1835854 66111 0 None 1 4 Human 9.0 pEC50 = 9 Functional
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 501 18 6 6 4.2 CCNC(=O)Nc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.08.043
CHEMBL1852119 66111 0 None 1 4 Human 9.0 pEC50 = 9 Functional
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 501 18 6 6 4.2 CCNC(=O)Nc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.08.043
56678973 66231 0 None 2 3 Human 9.0 pEC50 = 9 Functional
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 555 18 6 6 5.6 O=C(Nc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1)NC1CCCCC1 10.1016/j.bmc.2011.08.043
CHEMBL1835855 66231 0 None 2 3 Human 9.0 pEC50 = 9 Functional
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 555 18 6 6 5.6 O=C(Nc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1)NC1CCCCC1 10.1016/j.bmc.2011.08.043
CHEMBL1852541 66231 0 None 2 3 Human 9.0 pEC50 = 9 Functional
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 555 18 6 6 5.6 O=C(Nc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1)NC1CCCCC1 10.1016/j.bmc.2011.08.043
56675663 66241 0 None 25 3 Human 9.0 pEC50 = 9 Functional
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 541 17 6 6 4.6 NC(=O)Nc1cc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc(C(F)(F)F)c1 10.1016/j.bmc.2011.08.043
CHEMBL1835861 66241 0 None 25 3 Human 9.0 pEC50 = 9 Functional
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 541 17 6 6 4.6 NC(=O)Nc1cc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc(C(F)(F)F)c1 10.1016/j.bmc.2011.08.043
CHEMBL1852575 66241 0 None 25 3 Human 9.0 pEC50 = 9 Functional
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 541 17 6 6 4.6 NC(=O)Nc1cc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc(C(F)(F)F)c1 10.1016/j.bmc.2011.08.043
42625821 12422 0 None 630 3 Human 9.0 pEC50 = 9 Functional
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 522 18 4 7 3.4 CN(C)S(=O)(=O)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
CHEMBL1186678 12422 0 None 630 3 Human 9.0 pEC50 = 9 Functional
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 522 18 4 7 3.4 CN(C)S(=O)(=O)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
CHEMBL474393 12422 0 None 630 3 Human 9.0 pEC50 = 9 Functional
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 522 18 4 7 3.4 CN(C)S(=O)(=O)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
42625587 12576 0 None 125 3 Human 9.0 pEC50 = 9 Functional
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 562 18 4 7 4.3 O=S(=O)(c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1)N1CCCCC1 10.1021/jm801016j
CHEMBL1187520 12576 0 None 125 3 Human 9.0 pEC50 = 9 Functional
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 562 18 4 7 4.3 O=S(=O)(c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1)N1CCCCC1 10.1021/jm801016j
CHEMBL506518 12576 0 None 125 3 Human 9.0 pEC50 = 9 Functional
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 562 18 4 7 4.3 O=S(=O)(c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1)N1CCCCC1 10.1021/jm801016j
9958539 102618 0 None 5 3 Human 9.0 pEC50 = 9 Functional
Percent adenylyl cyclase activation at 10000 nM of compound concentrationPercent adenylyl cyclase activation at 10000 nM of compound concentration
ChEMBL 527 3 2 5 3.4 COc1c(I)cc(CC2NCCc3nc(N)sc32)cc1I 10.1016/s0960-894x(00)00459-5
CHEMBL307647 102618 0 None 5 3 Human 9.0 pEC50 = 9 Functional
Percent adenylyl cyclase activation at 10000 nM of compound concentrationPercent adenylyl cyclase activation at 10000 nM of compound concentration
ChEMBL 527 3 2 5 3.4 COc1c(I)cc(CC2NCCc3nc(N)sc32)cc1I 10.1016/s0960-894x(00)00459-5
87142783 118545 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 719 13 5 9 5.8 COc1cc(N(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)ccc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3426704 118545 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 719 13 5 9 5.8 COc1cc(N(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)ccc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548101 123867 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 878 18 6 9 7.1 C[C@H](Cc1ccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3639442 123867 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 878 18 6 9 7.1 C[C@H](Cc1ccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548063 124668 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 788 16 6 9 6.3 Cc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)CCCN(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645274 124668 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 788 16 6 9 6.3 Cc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)CCCN(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
59548134 124669 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 804 17 6 10 6.0 COc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)CCCN(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645275 124669 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 804 17 6 10 6.0 COc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)CCCN(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
66791483 124671 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 802 16 6 9 6.6 Cc1cc(NC(=O)CCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(C)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645277 124671 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 802 16 6 9 6.6 Cc1cc(NC(=O)CCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(C)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548074 124672 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 838 17 6 10 6.7 COc1cc(NC(=O)CCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645278 124672 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 838 17 6 10 6.7 COc1cc(NC(=O)CCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548094 124674 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 802 17 6 9 6.4 CC(Cc1cccc(NC(=O)CCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645280 124674 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 802 17 6 9 6.4 CC(Cc1cccc(NC(=O)CCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548099 124675 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 816 18 6 9 5.8 CC(Cc1cccc(CC(=O)NCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645281 124675 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 816 18 6 9 5.8 CC(Cc1cccc(CC(=O)NCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
68057677 124676 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 816 18 6 9 5.8 C[C@H](Cc1cccc(CC(=O)NCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645282 124676 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 816 18 6 9 5.8 C[C@H](Cc1cccc(CC(=O)NCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548122 124677 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 802 17 6 9 6.7 Cc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)CCCCN(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645283 124677 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 802 17 6 9 6.7 Cc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)CCCCN(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
59548079 124678 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 818 18 6 10 6.4 COc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)CCCCN(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645284 124678 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 818 18 6 10 6.4 COc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)CCCCN(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
59548056 124679 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 818 18 6 10 6.4 COc1cc(NC(=O)CCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)ccc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645285 124679 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 818 18 6 10 6.4 COc1cc(NC(=O)CCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)ccc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548067 124680 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 852 18 6 10 7.1 COc1cc(NC(=O)CCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645286 124680 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 852 18 6 10 7.1 COc1cc(NC(=O)CCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548141 124681 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 802 18 6 9 6.4 CN(CCCCC(=O)Nc1cccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)c1)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645287 124681 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 802 18 6 9 6.4 CN(CCCCC(=O)Nc1cccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)c1)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
59548102 124682 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 802 18 6 9 6.4 CN(CCCCC(=O)Nc1ccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645288 124682 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 802 18 6 9 6.4 CN(CCCCC(=O)Nc1ccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
68057804 124683 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 830 19 6 9 6.2 CC(Cc1cccc(CC(=O)NCCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645289 124683 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 830 19 6 9 6.2 CC(Cc1cccc(CC(=O)NCCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548054 124684 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 830 19 6 9 6.2 C[C@H](Cc1cccc(CC(=O)NCCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645290 124684 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 830 19 6 9 6.2 C[C@H](Cc1cccc(CC(=O)NCCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548125 124685 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 830 19 6 9 6.2 C[C@@H](Cc1cccc(CC(=O)NCCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645291 124685 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 830 19 6 9 6.2 C[C@@H](Cc1cccc(CC(=O)NCCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548051 124686 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 822 14 6 9 7.4 Cc1ccc(C(=O)Nc2ccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645292 124686 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 822 14 6 9 7.4 Cc1ccc(C(=O)Nc2ccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
59548107 124687 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 822 14 6 9 7.4 Cc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)c1cccc(N(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1 nan
CHEMBL3645293 124687 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 822 14 6 9 7.4 Cc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)c1cccc(N(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1 nan
59548124 124688 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 836 14 6 9 7.7 Cc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)c1ccc(C)c(N(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1 nan
CHEMBL3645294 124688 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 836 14 6 9 7.7 Cc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)c1ccc(C)c(N(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1 nan
59548081 124689 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 838 15 6 10 7.1 COc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)c1cccc(N(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1 nan
CHEMBL3645295 124689 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 838 15 6 10 7.1 COc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)c1cccc(N(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1 nan
59548120 124690 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 836 14 6 9 7.7 Cc1cc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c(C)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645296 124690 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 836 14 6 9 7.7 Cc1cc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c(C)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548093 124692 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 822 15 6 9 7.1 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1cccc(C(=O)Nc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)c1 nan
CHEMBL3645298 124692 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 822 15 6 9 7.1 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1cccc(C(=O)Nc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)c1 nan
59548119 124693 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 836 15 6 9 7.4 Cc1ccc(C(=O)Nc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645299 124693 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 836 15 6 9 7.4 Cc1ccc(C(=O)Nc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
59548129 124696 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 836 15 6 9 7.5 CC(Cc1cccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645301 124696 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 836 15 6 9 7.5 CC(Cc1cccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
70843902 124697 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 850 15 6 9 7.8 Cc1ccc(C(=O)Nc2cccc(CC(C)NC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645302 124697 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 850 15 6 9 7.8 Cc1ccc(C(=O)Nc2cccc(CC(C)NC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
59548098 124698 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 836 15 6 9 7.5 C[C@H](Cc1cccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645303 124698 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 836 15 6 9 7.5 C[C@H](Cc1cccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548123 124699 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 836 15 6 9 7.5 C[C@@H](Cc1cccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645304 124699 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 836 15 6 9 7.5 C[C@@H](Cc1cccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548138 124700 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 836 15 6 9 7.5 CC(Cc1ccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645305 124700 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 836 15 6 9 7.5 CC(Cc1ccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548095 124702 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 836 15 6 9 7.5 C[C@H](Cc1ccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645307 124702 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 836 15 6 9 7.5 C[C@H](Cc1ccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548130 124703 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 836 15 6 9 7.5 C[C@@H](Cc1ccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645308 124703 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 836 15 6 9 7.5 C[C@@H](Cc1ccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548100 124704 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 850 16 6 9 7.2 CC(Cc1cccc(CNC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645309 124704 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 850 16 6 9 7.2 CC(Cc1cccc(CNC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548136 124705 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 864 16 6 9 7.5 Cc1ccc(C(=O)NCc2cccc(CC(C)NC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645310 124705 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 864 16 6 9 7.5 Cc1ccc(C(=O)NCc2cccc(CC(C)NC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
66791606 124706 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 850 16 6 9 7.2 CC(Cc1ccc(CNC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645311 124706 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 850 16 6 9 7.2 CC(Cc1ccc(CNC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
70843738 124708 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 850 16 6 9 7.2 C[C@H](Cc1ccc(CNC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645313 124708 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 850 16 6 9 7.2 C[C@H](Cc1ccc(CNC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
70843742 124709 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 850 16 6 9 7.2 C[C@@H](Cc1ccc(CNC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645314 124709 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 850 16 6 9 7.2 C[C@@H](Cc1ccc(CNC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
70843734 124711 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 850 16 6 9 7.2 C[C@@H](Cc1cccc(CNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645316 124711 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 850 16 6 9 7.2 C[C@@H](Cc1cccc(CNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548091 124712 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 850 16 6 9 7.4 CC(Cc1cccc(CC(=O)Nc2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645317 124712 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 850 16 6 9 7.4 CC(Cc1cccc(CC(=O)Nc2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548132 124716 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 864 17 6 9 7.2 C[C@H](Cc1cccc(CCNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645320 124716 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 864 17 6 9 7.2 C[C@H](Cc1cccc(CCNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548118 124717 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 864 17 6 9 7.2 C[C@@H](Cc1cccc(CCNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645321 124717 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 864 17 6 9 7.2 C[C@@H](Cc1cccc(CCNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548139 124719 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 864 17 6 9 7.2 C[C@@H](Cc1ccc(CCNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645323 124719 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 864 17 6 9 7.2 C[C@@H](Cc1ccc(CCNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548061 124722 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 886 16 6 10 7.6 COc1cc(NC(=O)Cc2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645326 124722 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 886 16 6 10 7.6 COc1cc(NC(=O)Cc2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548066 124723 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 836 16 6 9 7.0 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1cccc(CC(=O)Nc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)c1 nan
CHEMBL3645327 124723 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 836 16 6 9 7.0 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1cccc(CC(=O)Nc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)c1 nan
59548076 124724 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 836 16 6 9 7.0 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1cccc(CC(=O)Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)c1 nan
CHEMBL3645328 124724 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 836 16 6 9 7.0 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1cccc(CC(=O)Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)c1 nan
59548128 124725 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 850 17 6 9 6.7 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CC(=O)NCc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 nan
CHEMBL3645329 124725 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 850 17 6 9 6.7 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CC(=O)NCc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 nan
59548117 124726 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 850 17 6 9 6.7 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CC(=O)NCc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1 nan
CHEMBL3645330 124726 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 850 17 6 9 6.7 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CC(=O)NCc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1 nan
59548058 124727 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 864 17 6 9 7.1 CC(Cc1ccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645331 124727 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 864 17 6 9 7.1 CC(Cc1ccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548121 124728 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 864 17 6 9 7.1 C[C@H](Cc1cccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645332 124728 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 864 17 6 9 7.1 C[C@H](Cc1cccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548110 124729 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 864 17 6 9 7.1 C[C@@H](Cc1cccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645333 124729 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 864 17 6 9 7.1 C[C@@H](Cc1cccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548080 124730 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 878 17 6 9 7.4 Cc1ccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1CC(C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645334 124730 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 878 17 6 9 7.4 Cc1ccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1CC(C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548135 124731 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 878 17 6 9 7.4 Cc1c(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cccc1CC(C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645335 124731 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 878 17 6 9 7.4 Cc1c(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cccc1CC(C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548052 124733 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 882 17 6 9 7.2 CC(Cc1cc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)ccc1F)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645337 124733 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 882 17 6 9 7.2 CC(Cc1cc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)ccc1F)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548059 124737 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 850 17 6 9 6.7 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CNC(=O)Cc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1 nan
CHEMBL3645340 124737 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 850 17 6 9 6.7 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CNC(=O)Cc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1 nan
59548142 124738 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 864 17 6 9 7.1 CC(Cc1cccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645341 124738 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 864 17 6 9 7.1 CC(Cc1cccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548084 124739 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 864 17 6 9 7.1 C[C@H](Cc1cccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645342 124739 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 864 17 6 9 7.1 C[C@H](Cc1cccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548083 124740 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 864 17 6 9 7.1 C[C@@H](Cc1cccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645343 124740 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 864 17 6 9 7.1 C[C@@H](Cc1cccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548114 124741 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 864 17 6 9 7.1 CC(Cc1ccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645344 124741 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 864 17 6 9 7.1 CC(Cc1ccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548140 124742 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 894 18 6 10 7.1 COc1ccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1CC(C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645345 124742 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 894 18 6 10 7.1 COc1ccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1CC(C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548050 124743 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 894 18 6 10 7.1 COc1ccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1C[C@@H](C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645346 124743 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 894 18 6 10 7.1 COc1ccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1C[C@@H](C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548069 124745 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 882 17 6 9 7.2 CC(Cc1cc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)ccc1F)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645348 124745 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 882 17 6 9 7.2 CC(Cc1cc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)ccc1F)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548085 124746 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 878 18 6 9 7.1 CC(Cc1cccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645349 124746 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 878 18 6 9 7.1 CC(Cc1cccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548115 124747 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 878 18 6 9 7.1 C[C@@H](Cc1cccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645350 124747 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 878 18 6 9 7.1 C[C@@H](Cc1cccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548103 124748 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 878 18 6 9 7.1 CC(Cc1ccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645351 124748 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 878 18 6 9 7.1 CC(Cc1ccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548057 124749 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 878 18 6 9 7.1 C[C@@H](Cc1ccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645352 124749 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 878 18 6 9 7.1 C[C@@H](Cc1ccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548078 124750 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 878 18 6 9 7.5 CC(Cc1cccc(CCC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645353 124750 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 878 18 6 9 7.5 CC(Cc1cccc(CCC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548082 124751 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 878 18 6 9 7.5 C[C@H](Cc1cccc(CCC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645354 124751 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 878 18 6 9 7.5 C[C@H](Cc1cccc(CCC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548090 124753 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 894 18 6 10 7.1 COc1ccc(CC(C)NC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1CC(=O)NCc1ccc(N(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)cc1 nan
CHEMBL3645356 124753 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 894 18 6 10 7.1 COc1ccc(CC(C)NC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1CC(=O)NCc1ccc(N(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)cc1 nan
59548137 124754 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 882 17 6 9 7.2 CC(Cc1ccc(F)c(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645357 124754 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 882 17 6 9 7.2 CC(Cc1ccc(F)c(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548068 124756 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 788 17 6 9 6.0 CN(CCCC(=O)Nc1ccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645359 124756 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 788 17 6 9 6.0 CN(CCCC(=O)Nc1ccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
59548105 124758 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 836 15 6 9 7.4 Cc1ccc(C(=O)Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645361 124758 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 836 15 6 9 7.4 Cc1ccc(C(=O)Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
56953428 124760 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 788 17 6 9 6.4 CN(CCCCC(=O)Nc1ccc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645363 124760 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 788 17 6 9 6.4 CN(CCCCC(=O)Nc1ccc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
49785227 124762 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 878 18 6 9 7.1 C[C@H](Cc1cccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645365 124762 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 878 18 6 9 7.1 C[C@H](Cc1cccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
49785225 127932 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 816 17 6 9 7.0 Cc1cc(NC(=O)CCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(C)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3666068 127932 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 816 17 6 9 7.0 Cc1cc(NC(=O)CCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(C)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
49785142 142728 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 816 18 6 9 5.8 C[C@@H](Cc1cccc(CC(=O)NCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3896828 142728 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 816 18 6 9 5.8 C[C@@H](Cc1cccc(CC(=O)NCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
118405092 149708 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 848 15 5 8 8.9 Cc1ccc(C(=O)Nc2ccc(CC(C)NC[C@H](C)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3952427 149708 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 848 15 5 8 8.9 Cc1ccc(C(=O)Nc2ccc(CC(C)NC[C@H](C)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
118405970 151261 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 848 17 5 8 7.6 CC(Cc1ccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NCCc1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3965175 151261 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 848 17 5 8 7.6 CC(Cc1ccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NCCc1ccc(O)c2[nH]c(=O)ccc12 nan
118405900 153122 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 852 15 6 10 7.4 COc1cc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c(C)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3981221 153122 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 852 15 6 10 7.4 COc1cc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c(C)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
118405964 160220 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 850 16 6 9 7.3 C[C@@H](NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12)c1cccc(CCNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1 nan
CHEMBL4114219 160220 0 None - 1 Human 9.0 pEC50 = 9 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 850 16 6 9 7.3 C[C@@H](NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12)c1cccc(CCNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1 nan
11214499 85571 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as stimulation of intracellular cAMP production after 30 mins of washing by wash-off assayAgonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as stimulation of intracellular cAMP production after 30 mins of washing by wash-off assay
ChEMBL 516 11 5 5 4.3 C[C@H](Cc1cccc(CC(=O)NCc2ccc(Cl)c(Cl)c2)c1)NC[C@H](O)c1ccc(O)c(CO)c1 10.1016/j.bmcl.2010.10.132
CHEMBL230490 85571 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as stimulation of intracellular cAMP production after 30 mins of washing by wash-off assayAgonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as stimulation of intracellular cAMP production after 30 mins of washing by wash-off assay
ChEMBL 516 11 5 5 4.3 C[C@H](Cc1cccc(CC(=O)NCc2ccc(Cl)c(Cl)c2)c1)NC[C@H](O)c1ccc(O)c(CO)c1 10.1016/j.bmcl.2010.10.132
45484583 196805 0 None 3 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP level
ChEMBL 456 10 6 7 2.0 CC(C)(Cc1ccc(NC(=O)CCCN)cc1)NCC(O)c1ccc(O)c2c1OCC(=O)N2 10.1016/j.bmcl.2009.06.104
CHEMBL577702 196805 0 None 3 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP level
ChEMBL 456 10 6 7 2.0 CC(C)(Cc1ccc(NC(=O)CCCN)cc1)NCC(O)c1ccc(O)c2c1OCC(=O)N2 10.1016/j.bmcl.2009.06.104
10438748 58213 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
ChEMBL 612 14 5 7 6.2 O=C(Nc1ccccc1-c1ccccc1)OC1CCN(CCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1016/j.bmcl.2011.01.043
CHEMBL1683932 58213 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
ChEMBL 612 14 5 7 6.2 O=C(Nc1ccccc1-c1ccccc1)OC1CCN(CCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1016/j.bmcl.2011.01.043
10326800 58218 1 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
ChEMBL 640 16 5 7 7.0 O=C(Nc1ccccc1-c1ccccc1)OC1CCN(CCCCCCCCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1016/j.bmcl.2011.01.043
CHEMBL1683938 58218 1 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
ChEMBL 640 16 5 7 7.0 O=C(Nc1ccccc1-c1ccccc1)OC1CCN(CCCCCCCCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1016/j.bmcl.2011.01.043
1499 2052 43 None -72 36 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human beta2 adrenergic receptor expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium influx by measuring fluorescence intensity by FLIPR assayAgonist activity at human beta2 adrenergic receptor expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium influx by measuring fluorescence intensity by FLIPR assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/acs.jnatprod.9b00418
3779 2052 43 None -72 36 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human beta2 adrenergic receptor expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium influx by measuring fluorescence intensity by FLIPR assayAgonist activity at human beta2 adrenergic receptor expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium influx by measuring fluorescence intensity by FLIPR assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/acs.jnatprod.9b00418
536 2052 43 None -72 36 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human beta2 adrenergic receptor expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium influx by measuring fluorescence intensity by FLIPR assayAgonist activity at human beta2 adrenergic receptor expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium influx by measuring fluorescence intensity by FLIPR assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/acs.jnatprod.9b00418
CHEMBL434 2052 43 None -72 36 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human beta2 adrenergic receptor expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium influx by measuring fluorescence intensity by FLIPR assayAgonist activity at human beta2 adrenergic receptor expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium influx by measuring fluorescence intensity by FLIPR assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/acs.jnatprod.9b00418
DB01064 2052 43 None -72 36 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human beta2 adrenergic receptor expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium influx by measuring fluorescence intensity by FLIPR assayAgonist activity at human beta2 adrenergic receptor expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium influx by measuring fluorescence intensity by FLIPR assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/acs.jnatprod.9b00418
45484569 195947 0 None 4 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP level
ChEMBL 596 13 6 9 1.5 CN1CCN(CC(=O)NCCCC(=O)Nc2ccc(CC(C)(C)NCC(O)c3ccc(O)c4c3OCC(=O)N4)cc2)CC1 10.1016/j.bmcl.2009.06.104
CHEMBL570834 195947 0 None 4 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP level
ChEMBL 596 13 6 9 1.5 CN1CCN(CC(=O)NCCCC(=O)Nc2ccc(CC(C)(C)NCC(O)c3ccc(O)c4c3OCC(=O)N4)cc2)CC1 10.1016/j.bmcl.2009.06.104
45101520 197096 0 None 3 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP level
ChEMBL 513 12 7 8 1.2 CC(C)(Cc1ccc(NC(=O)CCCNC(=O)CN)cc1)NCC(O)c1ccc(O)c2c1OCC(=O)N2 10.1016/j.bmcl.2009.06.104
CHEMBL583235 197096 0 None 3 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP level
ChEMBL 513 12 7 8 1.2 CC(C)(Cc1ccc(NC(=O)CCCNC(=O)CN)cc1)NCC(O)c1ccc(O)c2c1OCC(=O)N2 10.1016/j.bmcl.2009.06.104
44396736 66519 0 None -11 3 Human 8.9 pEC50 = 8.9 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptor
ChEMBL 617 12 4 9 5.1 C[C@H](Cc1c[nH]c2c(OS(=O)(=O)c3cccs3)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2004.10.035
CHEMBL186271 66519 0 None -11 3 Human 8.9 pEC50 = 8.9 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptor
ChEMBL 617 12 4 9 5.1 C[C@H](Cc1c[nH]c2c(OS(=O)(=O)c3cccs3)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2004.10.035
56665368 66111 0 None -1 4 Guinea pig 8.9 pEC50 = 8.9 Functional
Agonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile responseAgonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response
ChEMBL 501 18 6 6 4.2 CCNC(=O)Nc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.08.043
CHEMBL1835854 66111 0 None -1 4 Guinea pig 8.9 pEC50 = 8.9 Functional
Agonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile responseAgonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response
ChEMBL 501 18 6 6 4.2 CCNC(=O)Nc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.08.043
CHEMBL1852119 66111 0 None -1 4 Guinea pig 8.9 pEC50 = 8.9 Functional
Agonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile responseAgonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response
ChEMBL 501 18 6 6 4.2 CCNC(=O)Nc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.08.043
10180590 69873 0 None 707 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at beta2-adrenoceptor endogenously expressed in human BEAS-2B cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at beta2-adrenoceptor endogenously expressed in human BEAS-2B cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 422 11 6 6 2.9 OCc1cc([C@@H](O)CNCCc2ccc(NC[C@H](O)c3ccccc3)cc2)ccc1O 10.1016/j.bmcl.2011.11.072
CHEMBL1940830 69873 0 None 707 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at beta2-adrenoceptor endogenously expressed in human BEAS-2B cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at beta2-adrenoceptor endogenously expressed in human BEAS-2B cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 422 11 6 6 2.9 OCc1cc([C@@H](O)CNCCc2ccc(NC[C@H](O)c3ccccc3)cc2)ccc1O 10.1016/j.bmcl.2011.11.072
57398384 69876 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at beta2-adrenoceptor endogenously expressed in human BEAS-2B cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at beta2-adrenoceptor endogenously expressed in human BEAS-2B cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 459 10 6 6 3.2 O=c1ccc2c([C@@H](O)CNCCc3ccc(NC[C@H](O)c4ccccc4)cc3)ccc(O)c2[nH]1 10.1016/j.bmcl.2011.11.072
CHEMBL1940833 69876 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at beta2-adrenoceptor endogenously expressed in human BEAS-2B cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at beta2-adrenoceptor endogenously expressed in human BEAS-2B cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 459 10 6 6 3.2 O=c1ccc2c([C@@H](O)CNCCc3ccc(NC[C@H](O)c4ccccc4)cc3)ccc(O)c2[nH]1 10.1016/j.bmcl.2011.11.072
9893058 66035 0 None 39 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 525 17 5 8 2.9 O=c1ccn(-c2cccc(CCCCOCCCCCCNC[C@H](O)c3ccc(O)c(CO)c3)c2)c(=O)[nH]1 10.1016/j.bmc.2011.05.064
CHEMBL1814267 66035 0 None 39 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 525 17 5 8 2.9 O=c1ccn(-c2cccc(CCCCOCCCCCCNC[C@H](O)c3ccc(O)c(CO)c3)c2)c(=O)[nH]1 10.1016/j.bmc.2011.05.064
CHEMBL1851721 66035 0 None 39 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 525 17 5 8 2.9 O=c1ccn(-c2cccc(CCCCOCCCCCCNC[C@H](O)c3ccc(O)c(CO)c3)c2)c(=O)[nH]1 10.1016/j.bmc.2011.05.064
56675511 66061 0 None 31 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 527 18 5 7 3.2 O=C1CNC(=O)N1Cc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.05.064
CHEMBL1814273 66061 0 None 31 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 527 18 5 7 3.2 O=C1CNC(=O)N1Cc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.05.064
CHEMBL1851850 66061 0 None 31 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 527 18 5 7 3.2 O=C1CNC(=O)N1Cc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.05.064
16049374 63753 0 None 89 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 481 13 5 7 3.5 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCCSCCNCCc3cccc(Cl)c3)c2s1 10.1016/j.bmcl.2011.05.097
CHEMBL1807869 63753 0 None 89 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 481 13 5 7 3.5 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCCSCCNCCc3cccc(Cl)c3)c2s1 10.1016/j.bmcl.2011.05.097
118737359 118548 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 719 14 6 9 5.8 COc1ccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1NC(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1021/jm501915g
CHEMBL3426707 118548 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 719 14 6 9 5.8 COc1ccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1NC(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1021/jm501915g
24901284 70028 0 None 2 4 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 545 12 5 6 5.2 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCCc3cccc(CNCCc4c(Cl)cccc4Cl)c3)c2s1 10.1016/j.bmcl.2011.10.049
CHEMBL1945296 70028 0 None 2 4 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 545 12 5 6 5.2 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCCc3cccc(CNCCc4c(Cl)cccc4Cl)c3)c2s1 10.1016/j.bmcl.2011.10.049
42625897 12355 0 None 501 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 564 18 4 8 3.1 O=S(=O)(c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1)N1CCOCC1 10.1021/jm801016j
CHEMBL1186265 12355 0 None 501 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 564 18 4 8 3.1 O=S(=O)(c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1)N1CCOCC1 10.1021/jm801016j
CHEMBL456485 12355 0 None 501 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 564 18 4 8 3.1 O=S(=O)(c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1)N1CCOCC1 10.1021/jm801016j
10311070 111755 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 484 11 5 6 5.2 COc1ccc(Nc2ccc(CCNCC(O)c3ccc(O)c(CO)c3)cc2)cc1-c1ccccc1 10.1016/j.bmcl.2014.04.069
CHEMBL3290989 111755 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 484 11 5 6 5.2 COc1ccc(Nc2ccc(CCNCC(O)c3ccc(O)c(CO)c3)cc2)cc1-c1ccccc1 10.1016/j.bmcl.2014.04.069
10310047 111758 0 None 158 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 422 11 5 6 3.9 CCOc1ccc(Nc2ccc(CCNCC(O)c3ccc(O)c(CO)c3)cc2)cc1 10.1016/j.bmcl.2014.04.069
CHEMBL3290991 111758 0 None 158 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 422 11 5 6 3.9 CCOc1ccc(Nc2ccc(CCNCC(O)c3ccc(O)c(CO)c3)cc2)cc1 10.1016/j.bmcl.2014.04.069
145989945 166225 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 340 6 5 5 1.8 O=c1ccc2c([C@@H](CO)NCCc3ccc(O)cc3)ccc(O)c2[nH]1 10.1016/j.ejmech.2018.04.041
CHEMBL4284146 166225 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 340 6 5 5 1.8 O=c1ccc2c([C@@H](CO)NCCc3ccc(O)cc3)ccc(O)c2[nH]1 10.1016/j.ejmech.2018.04.041
1239 1639 46 None -1 5 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assayAgonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1021/jm100068m
3410 1639 46 None -1 5 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assayAgonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1021/jm100068m
3465 1639 46 None -1 5 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assayAgonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1021/jm100068m
CHEMBL1256786 1639 46 None -1 5 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assayAgonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1021/jm100068m
DB00983 1639 46 None -1 5 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assayAgonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1021/jm100068m
53318455 58212 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
ChEMBL 556 10 5 7 4.6 O=C(Nc1ccccc1-c1ccccc1)OC1CCN(CCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1016/j.bmcl.2011.01.043
CHEMBL1683931 58212 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
ChEMBL 556 10 5 7 4.6 O=C(Nc1ccccc1-c1ccccc1)OC1CCN(CCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1016/j.bmcl.2011.01.043
11703823 199460 0 None 131 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 390 6 4 5 3.0 CC(C)(Cc1ccc(Cl)cc1)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmcl.2009.12.087
CHEMBL603274 199460 0 None 131 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 390 6 4 5 3.0 CC(C)(Cc1ccc(Cl)cc1)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmcl.2009.12.087
44396715 67097 0 None -20 3 Human 8.9 pEC50 = 8.9 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptor
ChEMBL 612 12 4 9 4.4 C[C@H](Cc1c[nH]c2c(OS(=O)(=O)c3cccnc3)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2004.10.035
CHEMBL189081 67097 0 None -20 3 Human 8.9 pEC50 = 8.9 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptor
ChEMBL 612 12 4 9 4.4 C[C@H](Cc1c[nH]c2c(OS(=O)(=O)c3cccnc3)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2004.10.035
156015726 177691 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 410 7 4 5 3.0 O=C1COc2c(cc(O)cc2C(O)CNCCCc2cccc(C(F)(F)F)c2)N1 10.1016/j.bmc.2019.115178
CHEMBL4647449 177691 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 410 7 4 5 3.0 O=C1COc2c(cc(O)cc2C(O)CNCCCc2cccc(C(F)(F)F)c2)N1 10.1016/j.bmc.2019.115178
CHEMBL4650846 177691 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 410 7 4 5 3.0 O=C1COc2c(cc(O)cc2C(O)CNCCCc2cccc(C(F)(F)F)c2)N1 10.1016/j.bmc.2019.115178
46232973 199094 0 None 19 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 424 6 4 5 3.4 CC(C)(Cc1ccccc1C(F)(F)F)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmcl.2009.12.087
CHEMBL600617 199094 0 None 19 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 424 6 4 5 3.4 CC(C)(Cc1ccccc1C(F)(F)F)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmcl.2009.12.087
9800339 199458 6 None 251 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 386 7 4 6 2.4 COc1ccc(CC(C)(C)NCC(O)c2cc(O)cc3c2OCC(=O)N3)cc1 10.1016/j.bmcl.2009.12.087
CHEMBL603271 199458 6 None 251 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 386 7 4 6 2.4 COc1ccc(CC(C)(C)NCC(O)c2cc(O)cc3c2OCC(=O)N3)cc1 10.1016/j.bmcl.2009.12.087
4183 1986 62 None 1 4 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at adrenergic beta2 receptor in human A431 cells assessed as elevation of cAMP levelAgonist activity at adrenergic beta2 receptor in human A431 cells assessed as elevation of cAMP level
ChEMBL 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O 10.1016/j.bmcl.2014.06.014
6918554 1986 62 None 1 4 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at adrenergic beta2 receptor in human A431 cells assessed as elevation of cAMP levelAgonist activity at adrenergic beta2 receptor in human A431 cells assessed as elevation of cAMP level
ChEMBL 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O 10.1016/j.bmcl.2014.06.014
7455 1986 62 None 1 4 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at adrenergic beta2 receptor in human A431 cells assessed as elevation of cAMP levelAgonist activity at adrenergic beta2 receptor in human A431 cells assessed as elevation of cAMP level
ChEMBL 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O 10.1016/j.bmcl.2014.06.014
CHEMBL1095777 1986 62 None 1 4 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at adrenergic beta2 receptor in human A431 cells assessed as elevation of cAMP levelAgonist activity at adrenergic beta2 receptor in human A431 cells assessed as elevation of cAMP level
ChEMBL 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O 10.1016/j.bmcl.2014.06.014
DB05039 1986 62 None 1 4 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at adrenergic beta2 receptor in human A431 cells assessed as elevation of cAMP levelAgonist activity at adrenergic beta2 receptor in human A431 cells assessed as elevation of cAMP level
ChEMBL 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O 10.1016/j.bmcl.2014.06.014
45483844 196709 0 None 4 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 398 7 4 5 3.5 CC(C)c1ccc(CC(C)(C)NCC(O)c2ccc(O)c3c2OCC(=O)N3)cc1 10.1016/j.bmcl.2009.10.013
CHEMBL576848 196709 0 None 4 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 398 7 4 5 3.5 CC(C)c1ccc(CC(C)(C)NCC(O)c2ccc(O)c3c2OCC(=O)N3)cc1 10.1016/j.bmcl.2009.10.013
44392566 64482 0 None 11 2 Human 8.8 pEC50 = 8.8 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-2 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-2 adrenergic receptor
ChEMBL 457 11 4 6 3.7 C=C(C)CNc1cccc([C@@H](O)CN[C@H](C)Cc2c[nH]c3c(OS(C)(=O)=O)cccc23)c1 10.1016/j.bmcl.2004.12.033
CHEMBL181964 64482 0 None 11 2 Human 8.8 pEC50 = 8.8 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-2 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-2 adrenergic receptor
ChEMBL 457 11 4 6 3.7 C=C(C)CNc1cccc([C@@H](O)CN[C@H](C)Cc2c[nH]c3c(OS(C)(=O)=O)cccc23)c1 10.1016/j.bmcl.2004.12.033
2233849 33118 8 None - 1 Human 8.8 pEC50 = 8.8 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory)
ChEMBL 446 10 1 7 4.1 C=CCn1c(CCNC(=O)c2cccs2)nnc1SCC(=O)c1ccc(Cl)cc1 nan
CHEMBL1419122 33118 8 None - 1 Human 8.8 pEC50 = 8.8 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory)
ChEMBL 446 10 1 7 4.1 C=CCn1c(CCNC(=O)c2cccs2)nnc1SCC(=O)c1ccc(Cl)cc1 nan
10288976 66232 0 None -10 4 Guinea pig 8.8 pEC50 = 8.8 Functional
Agonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile responseAgonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response
ChEMBL 487 17 6 6 3.9 Cc1cc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc(NC(N)=O)c1 10.1016/j.bmc.2011.08.043
CHEMBL1835862 66232 0 None -10 4 Guinea pig 8.8 pEC50 = 8.8 Functional
Agonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile responseAgonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response
ChEMBL 487 17 6 6 3.9 Cc1cc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc(NC(N)=O)c1 10.1016/j.bmc.2011.08.043
CHEMBL1852543 66232 0 None -10 4 Guinea pig 8.8 pEC50 = 8.8 Functional
Agonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile responseAgonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response
ChEMBL 487 17 6 6 3.9 Cc1cc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc(NC(N)=O)c1 10.1016/j.bmc.2011.08.043
44339091 9341 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
ChEMBL 429 12 4 7 2.6 O=C(CCOCCc1ccccc1)NCCNCCc1ccc(O)c2nc(O)sc12 10.1016/j.bmcl.2011.04.135
CHEMBL111775 9341 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
ChEMBL 429 12 4 7 2.6 O=C(CCOCCc1ccccc1)NCCNCCc1ccc(O)c2nc(O)sc12 10.1016/j.bmcl.2011.04.135
53307432 63217 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
ChEMBL 485 15 3 6 3.7 CCCCN(CCNCCc1ccc(O)c2[nH]c(=O)sc12)C(=O)CCOCCc1ccccc1 10.1016/j.bmcl.2011.04.135
CHEMBL1800659 63217 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
ChEMBL 485 15 3 6 3.7 CCCCN(CCNCCc1ccc(O)c2[nH]c(=O)sc12)C(=O)CCOCCc1ccccc1 10.1016/j.bmcl.2011.04.135
16049448 63749 0 None 56 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 515 13 5 7 4.2 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCSCCCNCCc3cccc(Cl)c3Cl)c2s1 10.1016/j.bmcl.2011.05.097
CHEMBL1807829 63749 0 None 56 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 515 13 5 7 4.2 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCSCCCNCCc3cccc(Cl)c3Cl)c2s1 10.1016/j.bmcl.2011.05.097
16049376 63755 0 None 44 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 515 13 5 7 4.2 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCCSCCNCCc3cccc(Cl)c3Cl)c2s1 10.1016/j.bmcl.2011.05.097
CHEMBL1807871 63755 0 None 44 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 515 13 5 7 4.2 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCCSCCNCCc3cccc(Cl)c3Cl)c2s1 10.1016/j.bmcl.2011.05.097
53307432 63217 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assayAgonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assay
ChEMBL 485 15 3 6 3.7 CCCCN(CCNCCc1ccc(O)c2[nH]c(=O)sc12)C(=O)CCOCCc1ccccc1 10.1021/ml4005232
CHEMBL1800659 63217 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assayAgonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assay
ChEMBL 485 15 3 6 3.7 CCCCN(CCNCCc1ccc(O)c2[nH]c(=O)sc12)C(=O)CCOCCc1ccccc1 10.1021/ml4005232
118737353 118541 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 705 13 6 9 5.2 COc1cc(C(=O)NCCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)ccc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/jm501915g
CHEMBL3426700 118541 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 705 13 6 9 5.2 COc1cc(C(=O)NCCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)ccc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/jm501915g
145989075 166528 0 None 524 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 324 6 4 4 2.1 O=c1ccc2c(C(CO)NCCc3ccccc3)ccc(O)c2[nH]1 10.1016/j.ejmech.2018.04.041
CHEMBL4289813 166528 0 None 524 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 324 6 4 4 2.1 O=c1ccc2c(C(CO)NCCc3ccccc3)ccc(O)c2[nH]1 10.1016/j.ejmech.2018.04.041
90645346 111990 0 None 2 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 578 13 6 7 4.7 O=C(NCCOc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1)c1ccccc1 10.1016/j.bmcl.2014.04.095
CHEMBL3298762 111990 0 None 2 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 578 13 6 7 4.7 O=C(NCCOc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1)c1ccccc1 10.1016/j.bmcl.2014.04.095
11180293 112003 0 None 22 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 543 12 6 8 3.1 O=c1ccc2c([C@@H](O)CNCCc3ccc(Nc4ccc(OCCN5CCNCC5)cc4)cc3)ccc(O)c2[nH]1 10.1016/j.bmcl.2014.04.095
CHEMBL3298897 112003 0 None 22 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 543 12 6 8 3.1 O=c1ccc2c([C@@H](O)CNCCc3ccc(Nc4ccc(OCCN5CCNCC5)cc4)cc3)ccc(O)c2[nH]1 10.1016/j.bmcl.2014.04.095
24901416 70001 0 None -2 4 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 481 11 5 6 3.6 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3ccccc3CNCCc3ccccc3F)c2s1 10.1016/j.bmcl.2011.10.049
CHEMBL1945035 70001 0 None -2 4 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 481 11 5 6 3.6 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3ccccc3CNCCc3ccccc3F)c2s1 10.1016/j.bmcl.2011.10.049
10370605 105939 0 None 158 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 561 18 4 7 5.2 O=S(=O)(c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1)C1CCCCC1 10.1021/jm401532g
CHEMBL3126385 105939 0 None 158 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 561 18 4 7 5.2 O=S(=O)(c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1)C1CCCCC1 10.1021/jm401532g
CHEMBL3139615 105939 0 None 158 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 561 18 4 7 5.2 O=S(=O)(c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1)C1CCCCC1 10.1021/jm401532g
42625588 179835 0 None 630 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 508 18 5 7 2.9 NS(=O)(=O)Cc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
CHEMBL475237 179835 0 None 630 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 508 18 5 7 2.9 NS(=O)(=O)Cc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
46833102 14076 0 None 31 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 496 17 5 8 1.9 NS(=O)(=O)c1cccc(COCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm100326d
CHEMBL1084656 14076 0 None 31 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 496 17 5 8 1.9 NS(=O)(=O)c1cccc(COCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm100326d
CHEMBL1198882 14076 0 None 31 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 496 17 5 8 1.9 NS(=O)(=O)c1cccc(COCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm100326d
46832507 14084 0 None 12 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 475 17 6 7 2.8 NC(=O)Nc1cccc(COCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm100326d
CHEMBL1085638 14084 0 None 12 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 475 17 6 7 2.8 NC(=O)Nc1cccc(COCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm100326d
CHEMBL1198915 14084 0 None 12 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 475 17 6 7 2.8 NC(=O)Nc1cccc(COCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm100326d
57400045 69863 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 456 11 6 6 3.5 OCc1cc(C(O)CNCCc2ccc(NCC(O)c3ccc(Cl)cc3)cc2)ccc1O 10.1016/j.bmcl.2011.11.072
CHEMBL1940820 69863 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 456 11 6 6 3.5 OCc1cc(C(O)CNCCc2ccc(NCC(O)c3ccc(Cl)cc3)cc2)ccc1O 10.1016/j.bmcl.2011.11.072
149373618 177664 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 358 7 4 6 1.6 COc1ccc(CCNCC(O)c2cc(O)cc3c2OCC(=O)N3)cc1 10.1016/j.bmc.2019.115178
CHEMBL4642893 177664 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 358 7 4 6 1.6 COc1ccc(CCNCC(O)c2cc(O)cc3c2OCC(=O)N3)cc1 10.1016/j.bmc.2019.115178
CHEMBL4650643 177664 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 358 7 4 6 1.6 COc1ccc(CCNCC(O)c2cc(O)cc3c2OCC(=O)N3)cc1 10.1016/j.bmc.2019.115178
73056754 103786 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulationAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulation
ChEMBL 331 8 4 5 2.8 CC[C@H](Cc1ccc(OC)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2013.11.030
CHEMBL3099659 103786 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulationAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulation
ChEMBL 331 8 4 5 2.8 CC[C@H](Cc1ccc(OC)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2013.11.030
45483847 195127 0 None 2 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 432 7 4 5 4.0 CC(C)(Cc1ccc(-c2ccccc2)cc1)NCC(O)c1ccc(O)c2c1OCC(=O)N2 10.1016/j.bmcl.2009.10.013
CHEMBL565686 195127 0 None 2 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 432 7 4 5 4.0 CC(C)(Cc1ccc(-c2ccccc2)cc1)NCC(O)c1ccc(O)c2c1OCC(=O)N2 10.1016/j.bmcl.2009.10.013
45101522 197329 0 None 5 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP level
ChEMBL 578 15 7 9 2.0 CC(C)(Cc1ccc(NC(=O)CCCNCCCS(=O)(=O)O)cc1)NCC(O)c1ccc(O)c2c1OCC(=O)N2 10.1016/j.bmcl.2009.06.104
CHEMBL585751 197329 0 None 5 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP level
ChEMBL 578 15 7 9 2.0 CC(C)(Cc1ccc(NC(=O)CCCNCCCS(=O)(=O)O)cc1)NCC(O)c1ccc(O)c2c1OCC(=O)N2 10.1016/j.bmcl.2009.06.104
11962616 219 7 None 40 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at beta2 adrenoceptor human bronchi assessed as induction of maximum relaxationAgonist activity at beta2 adrenoceptor human bronchi assessed as induction of maximum relaxation
ChEMBL 460 13 4 5 4.2 O=c1ccc2c([nH]1)c(O)ccc2[C@H](CNCCCCCCOCC(c1ccccc1)(F)F)O 10.1021/acs.jmedchem.0c01195
9326 219 7 None 40 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at beta2 adrenoceptor human bronchi assessed as induction of maximum relaxationAgonist activity at beta2 adrenoceptor human bronchi assessed as induction of maximum relaxation
ChEMBL 460 13 4 5 4.2 O=c1ccc2c([nH]1)c(O)ccc2[C@H](CNCCCCCCOCC(c1ccccc1)(F)F)O 10.1021/acs.jmedchem.0c01195
CHEMBL3039530 219 7 None 40 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at beta2 adrenoceptor human bronchi assessed as induction of maximum relaxationAgonist activity at beta2 adrenoceptor human bronchi assessed as induction of maximum relaxation
ChEMBL 460 13 4 5 4.2 O=c1ccc2c([nH]1)c(O)ccc2[C@H](CNCCCCCCOCC(c1ccccc1)(F)F)O 10.1021/acs.jmedchem.0c01195
DB12100 219 7 None 40 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at beta2 adrenoceptor human bronchi assessed as induction of maximum relaxationAgonist activity at beta2 adrenoceptor human bronchi assessed as induction of maximum relaxation
ChEMBL 460 13 4 5 4.2 O=c1ccc2c([nH]1)c(O)ccc2[C@H](CNCCCCCCOCC(c1ccccc1)(F)F)O 10.1021/acs.jmedchem.0c01195
56678845 66058 0 None 15 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 513 17 5 7 3.2 O=C1CNC(=O)N1c1ccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc1 10.1016/j.bmc.2011.05.064
CHEMBL1814269 66058 0 None 15 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 513 17 5 7 3.2 O=C1CNC(=O)N1c1ccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc1 10.1016/j.bmc.2011.05.064
CHEMBL1851839 66058 0 None 15 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 513 17 5 7 3.2 O=C1CNC(=O)N1c1ccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc1 10.1016/j.bmc.2011.05.064
145981405 165934 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 358 6 4 4 2.8 O=c1ccc2c(C(CO)NCCc3ccccc3Cl)ccc(O)c2[nH]1 10.1016/j.ejmech.2018.04.041
CHEMBL4278577 165934 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 358 6 4 4 2.8 O=c1ccc2c(C(CO)NCCc3ccccc3Cl)ccc(O)c2[nH]1 10.1016/j.ejmech.2018.04.041
145987168 166651 0 None 316 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 354 7 4 5 2.1 COc1cccc(CCNC(CO)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1016/j.ejmech.2018.04.041
CHEMBL4291941 166651 0 None 316 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 354 7 4 5 2.1 COc1cccc(CCNC(CO)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1016/j.ejmech.2018.04.041
10173878 111954 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 459 10 5 6 4.2 CCOc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 10.1016/j.bmcl.2014.04.095
CHEMBL3298327 111954 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 459 10 5 6 4.2 CCOc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 10.1016/j.bmcl.2014.04.095
24901283 70024 0 None -2 5 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 417 11 5 7 1.9 COCCNCc1cccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)c1 10.1016/j.bmcl.2011.10.049
CHEMBL1945292 70024 0 None -2 5 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 417 11 5 7 1.9 COCCNCc1cccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)c1 10.1016/j.bmcl.2011.10.049
10076176 105941 0 None 50 5 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 547 18 4 7 4.8 O=S(=O)(c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1)C1CCCC1 10.1021/jm401532g
CHEMBL3126382 105941 0 None 50 5 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 547 18 4 7 4.8 O=S(=O)(c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1)C1CCCC1 10.1021/jm401532g
CHEMBL3139683 105941 0 None 50 5 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 547 18 4 7 4.8 O=S(=O)(c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1)C1CCCC1 10.1021/jm401532g
46832804 6893 0 None 50 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 496 17 5 8 1.9 NS(=O)(=O)c1ccc(COCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc1 10.1021/jm100326d
CHEMBL1084655 6893 0 None 50 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 496 17 5 8 1.9 NS(=O)(=O)c1ccc(COCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc1 10.1021/jm100326d
10310564 111754 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 454 10 5 5 5.2 OCc1cc(C(O)CNCCc2ccc(Nc3cccc(-c4ccccc4)c3)cc2)ccc1O 10.1016/j.bmcl.2014.04.069
CHEMBL3290988 111754 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 454 10 5 5 5.2 OCc1cc(C(O)CNCCc2ccc(Nc3cccc(-c4ccccc4)c3)cc2)ccc1O 10.1016/j.bmcl.2014.04.069
57396615 69861 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 436 11 5 6 2.9 CN(CC(O)c1ccccc1)c1ccc(CCNCC(O)c2ccc(O)c(CO)c2)cc1 10.1016/j.bmcl.2011.11.072
CHEMBL1940818 69861 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 436 11 5 6 2.9 CN(CC(O)c1ccccc1)c1ccc(CCNCC(O)c2ccc(O)c(CO)c2)cc1 10.1016/j.bmcl.2011.11.072
57391344 69864 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 440 11 6 6 3.0 OCc1cc(C(O)CNCCc2ccc(NCC(O)c3ccc(F)cc3)cc2)ccc1O 10.1016/j.bmcl.2011.11.072
CHEMBL1940821 69864 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 440 11 6 6 3.0 OCc1cc(C(O)CNCCc2ccc(NCC(O)c3ccc(F)cc3)cc2)ccc1O 10.1016/j.bmcl.2011.11.072
10902809 47798 0 None -1 3 Human 8.0 pEC50 = 8 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-2 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-2 AR expressed as the negative logarithm of the molar drug concentration
ChEMBL 304 7 3 3 3.5 C[C@H](CNc1ccccc1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0101500
CHEMBL155072 47798 0 None -1 3 Human 8.0 pEC50 = 8 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-2 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-2 AR expressed as the negative logarithm of the molar drug concentration
ChEMBL 304 7 3 3 3.5 C[C@H](CNc1ccccc1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0101500
11005613 119281 0 None 1 3 Human 8.0 pEC50 = 8 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-2 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-2 AR expressed as the negative logarithm of the molar drug concentration
ChEMBL 501 12 4 5 4.3 Cc1ccc(S(=O)(=O)NCCc2ccc(NC[C@@H](C)NC[C@H](O)c3cccc(Cl)c3)cc2)cc1 10.1021/jm0101500
CHEMBL348269 119281 0 None 1 3 Human 8.0 pEC50 = 8 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-2 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-2 AR expressed as the negative logarithm of the molar drug concentration
ChEMBL 501 12 4 5 4.3 Cc1ccc(S(=O)(=O)NCCc2ccc(NC[C@@H](C)NC[C@H](O)c3cccc(Cl)c3)cc2)cc1 10.1021/jm0101500
90655867 110763 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assayAgonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assay
ChEMBL 562 17 3 7 3.9 CCN(C)CCCN(CCNCCc1ccc(O)c2[nH]c(=O)sc12)C(=O)CCOCCc1cccc(Cl)c1 10.1021/ml4005232
CHEMBL3265164 110763 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assayAgonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assay
ChEMBL 562 17 3 7 3.9 CCN(C)CCCN(CCNCCc1ccc(O)c2[nH]c(=O)sc12)C(=O)CCOCCc1cccc(Cl)c1 10.1021/ml4005232
16036676 110766 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assayAgonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assay
ChEMBL 578 17 3 7 4.4 CCN(CC)CCN(CCNCCc1ccc(O)c2[nH]c(=O)sc12)C(=O)CCOCCc1ccc2ccccc2c1 10.1021/ml4005232
CHEMBL3265168 110766 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assayAgonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assay
ChEMBL 578 17 3 7 4.4 CCN(CC)CCN(CCNCCc1ccc(O)c2[nH]c(=O)sc12)C(=O)CCOCCc1ccc2ccccc2c1 10.1021/ml4005232
54586985 61469 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as stimulation of intracellular cAMP production after 30 mins of washing by wash-off assayAgonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as stimulation of intracellular cAMP production after 30 mins of washing by wash-off assay
ChEMBL 583 15 5 7 5.0 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCNC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)ccc1O)C(C)C 10.1016/j.bmcl.2010.10.132
CHEMBL1773262 61469 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as stimulation of intracellular cAMP production after 30 mins of washing by wash-off assayAgonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as stimulation of intracellular cAMP production after 30 mins of washing by wash-off assay
ChEMBL 583 15 5 7 5.0 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCNC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)ccc1O)C(C)C 10.1016/j.bmcl.2010.10.132
145981007 166029 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 340 6 5 5 1.8 O=c1ccc2c(C(CO)NCCc3ccccc3O)ccc(O)c2[nH]1 10.1016/j.ejmech.2018.04.041
CHEMBL4280227 166029 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 340 6 5 5 1.8 O=c1ccc2c(C(CO)NCCc3ccccc3O)ccc(O)c2[nH]1 10.1016/j.ejmech.2018.04.041
145994130 166816 0 None 83 2 Human 8.0 pEC50 = 8 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 338 7 4 4 2.5 O=c1ccc2c(C(CO)NCCCc3ccccc3)ccc(O)c2[nH]1 10.1016/j.ejmech.2018.04.041
CHEMBL4294937 166816 0 None 83 2 Human 8.0 pEC50 = 8 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 338 7 4 4 2.5 O=c1ccc2c(C(CO)NCCCc3ccccc3)ccc(O)c2[nH]1 10.1016/j.ejmech.2018.04.041
24900423 70177 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 537 9 4 6 5.3 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3ccc(-c4cccc(CN5Cc6ccccc6C5)c4)cc3)c2s1 10.1016/j.bmcl.2011.10.049
CHEMBL1947154 70177 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 537 9 4 6 5.3 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3ccc(-c4cccc(CN5Cc6ccccc6C5)c4)cc3)c2s1 10.1016/j.bmcl.2011.10.049
45271518 193404 0 None 6 3 Human 8.0 pEC50 = 8 Functional
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 479 11 4 6 3.9 COC(=O)c1ccc(NC(=S)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)cc1 10.1016/j.bmc.2009.06.031
CHEMBL1203999 193404 0 None 6 3 Human 8.0 pEC50 = 8 Functional
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 479 11 4 6 3.9 COC(=O)c1ccc(NC(=S)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)cc1 10.1016/j.bmc.2009.06.031
CHEMBL549689 193404 0 None 6 3 Human 8.0 pEC50 = 8 Functional
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 479 11 4 6 3.9 COC(=O)c1ccc(NC(=S)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)cc1 10.1016/j.bmc.2009.06.031
45272431 193429 0 None 6 3 Human 8.0 pEC50 = 8 Functional
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 547 10 4 4 4.7 O[C@@H](CNCCc1ccc(NC(=S)Nc2ccc(I)cc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL1204002 193429 0 None 6 3 Human 8.0 pEC50 = 8 Functional
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 547 10 4 4 4.7 O[C@@H](CNCCc1ccc(NC(=S)Nc2ccc(I)cc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL549960 193429 0 None 6 3 Human 8.0 pEC50 = 8 Functional
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 547 10 4 4 4.7 O[C@@H](CNCCc1ccc(NC(=S)Nc2ccc(I)cc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
45271523 193448 0 None 10 3 Human 8.0 pEC50 = 8 Functional
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 435 10 4 4 4.4 Cc1ccc(NC(=S)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)cc1 10.1016/j.bmc.2009.06.031
CHEMBL1204000 193448 0 None 10 3 Human 8.0 pEC50 = 8 Functional
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 435 10 4 4 4.4 Cc1ccc(NC(=S)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)cc1 10.1016/j.bmc.2009.06.031
CHEMBL550096 193448 0 None 10 3 Human 8.0 pEC50 = 8 Functional
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 435 10 4 4 4.4 Cc1ccc(NC(=S)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)cc1 10.1016/j.bmc.2009.06.031
45270697 193490 0 None 20 3 Human 8.0 pEC50 = 8 Functional
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 451 11 4 5 4.1 COc1ccccc1NC(=S)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.06.031
CHEMBL1203995 193490 0 None 20 3 Human 8.0 pEC50 = 8 Functional
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 451 11 4 5 4.1 COc1ccccc1NC(=S)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.06.031
CHEMBL550444 193490 0 None 20 3 Human 8.0 pEC50 = 8 Functional
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 451 11 4 5 4.1 COc1ccccc1NC(=S)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.06.031
45272430 193763 0 None 8 3 Human 8.0 pEC50 = 8 Functional
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 439 10 4 4 4.2 O[C@@H](CNCCc1ccc(NC(=S)Nc2ccc(F)cc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL1204001 193763 0 None 8 3 Human 8.0 pEC50 = 8 Functional
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 439 10 4 4 4.2 O[C@@H](CNCCc1ccc(NC(=S)Nc2ccc(F)cc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL552374 193763 0 None 8 3 Human 8.0 pEC50 = 8 Functional
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 439 10 4 4 4.2 O[C@@H](CNCCc1ccc(NC(=S)Nc2ccc(F)cc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
45269025 194463 0 None 3 3 Human 8.0 pEC50 = 8 Functional
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 500 11 5 6 2.7 NS(=O)(=O)c1ccc(NC(=S)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)cc1 10.1016/j.bmc.2009.06.031
CHEMBL1203991 194463 0 None 3 3 Human 8.0 pEC50 = 8 Functional
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 500 11 5 6 2.7 NS(=O)(=O)c1ccc(NC(=S)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)cc1 10.1016/j.bmc.2009.06.031
CHEMBL561173 194463 0 None 3 3 Human 8.0 pEC50 = 8 Functional
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 500 11 5 6 2.7 NS(=O)(=O)c1ccc(NC(=S)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)cc1 10.1016/j.bmc.2009.06.031
45267257 194997 0 None 3 3 Human 8.0 pEC50 = 8 Functional
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 449 12 4 4 3.8 O[C@@H](CNCCc1ccc(NC(=S)NCCc2ccccc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL1203987 194997 0 None 3 3 Human 8.0 pEC50 = 8 Functional
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 449 12 4 4 3.8 O[C@@H](CNCCc1ccc(NC(=S)NCCc2ccccc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL564648 194997 0 None 3 3 Human 8.0 pEC50 = 8 Functional
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 449 12 4 4 3.8 O[C@@H](CNCCc1ccc(NC(=S)NCCc2ccccc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
11605652 12433 0 None 501 3 Human 8.0 pEC50 = 8 Functional
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1cccc(CCCCOCCCCCCNC[C@@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
CHEMBL1186715 12433 0 None 501 3 Human 8.0 pEC50 = 8 Functional
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1cccc(CCCCOCCCCCCNC[C@@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
CHEMBL475236 12433 0 None 501 3 Human 8.0 pEC50 = 8 Functional
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1cccc(CCCCOCCCCCCNC[C@@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
59119455 111757 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 408 10 5 6 3.5 COc1cccc(Nc2ccc(CCNCC(O)c3ccc(O)c(CO)c3)cc2)c1 10.1016/j.bmcl.2014.04.069
CHEMBL3290990 111757 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 408 10 5 6 3.5 COc1cccc(Nc2ccc(CCNCC(O)c3ccc(O)c(CO)c3)cc2)c1 10.1016/j.bmcl.2014.04.069
44392457 165393 0 None -34 3 Human 8.0 pEC50 = 8 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-2 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-2 adrenergic receptor
ChEMBL 457 11 4 6 3.7 C/C=C/CNc1cccc([C@@H](O)CN[C@H](C)Cc2c[nH]c3c(OS(C)(=O)=O)cccc23)c1 10.1016/j.bmcl.2004.12.033
CHEMBL425161 165393 0 None -34 3 Human 8.0 pEC50 = 8 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-2 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-2 adrenergic receptor
ChEMBL 457 11 4 6 3.7 C/C=C/CNc1cccc([C@@H](O)CN[C@H](C)Cc2c[nH]c3c(OS(C)(=O)=O)cccc23)c1 10.1016/j.bmcl.2004.12.033
10121328 4357 0 None 4 3 Human 8.0 pEC50 = 8 Functional
Beta-2 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-2-adrenoceptorBeta-2 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-2-adrenoceptor
ChEMBL 593 11 5 10 1.4 CS(=O)(=O)Nc1cc([C@@H](O)CNCC2CCN(S(=O)(=O)c3ccc(-n4cc(C(=O)O)cn4)cc3)CC2)ccc1O 10.1016/s0960-894x(02)00608-x
CHEMBL101606 4357 0 None 4 3 Human 8.0 pEC50 = 8 Functional
Beta-2 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-2-adrenoceptorBeta-2 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-2-adrenoceptor
ChEMBL 593 11 5 10 1.4 CS(=O)(=O)Nc1cc([C@@H](O)CNCC2CCN(S(=O)(=O)c3ccc(-n4cc(C(=O)O)cn4)cc3)CC2)ccc1O 10.1016/s0960-894x(02)00608-x
73056757 103784 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulationAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulation
ChEMBL 303 7 4 5 2.0 COc1ccc(CCNC[C@H](O)c2cc(O)cc(O)c2)cc1 10.1016/j.bmc.2013.11.030
CHEMBL3099657 103784 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulationAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulation
ChEMBL 303 7 4 5 2.0 COc1ccc(CCNC[C@H](O)c2cc(O)cc(O)c2)cc1 10.1016/j.bmc.2013.11.030
11539348 199093 0 None 9 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 434 6 4 5 3.1 CC(C)(Cc1ccc(Br)cc1)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmcl.2009.12.087
CHEMBL600616 199093 0 None 9 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 434 6 4 5 3.1 CC(C)(Cc1ccc(Br)cc1)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmcl.2009.12.087
6852397 59902 1 None - 1 Human 8.0 pEC50 = 8.0 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 330 8 4 5 2.4 COc1ccc([C@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 nan
CHEMBL1735137 59902 1 None - 1 Human 8.0 pEC50 = 8.0 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 330 8 4 5 2.4 COc1ccc([C@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 nan
CHEMBL1740818 59902 1 None - 1 Human 8.0 pEC50 = 8.0 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 330 8 4 5 2.4 COc1ccc([C@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 nan
44441226 93222 0 None -7 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 415 9 4 6 3.8 C[C@H](CNc1ccc(-c2nc(C(=O)O)co2)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2007.05.069
CHEMBL246908 93222 0 None -7 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 415 9 4 6 3.8 C[C@H](CNc1ccc(-c2nc(C(=O)O)co2)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2007.05.069
44441231 147510 0 None -50 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 431 9 4 6 4.3 C[C@H](CNc1cccc(-c2csc(C(=O)O)n2)c1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2007.05.069
CHEMBL393470 147510 0 None -50 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 431 9 4 6 4.3 C[C@H](CNc1cccc(-c2csc(C(=O)O)n2)c1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2007.05.069
57397010 70137 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 515 11 4 5 5.3 O=c1[nH]c2c(O)ccc(CCNCCc3ccc(CNCCc4c(Cl)cccc4Cl)cc3)c2s1 10.1016/j.bmcl.2011.10.049
CHEMBL1946761 70137 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 515 11 4 5 5.3 O=c1[nH]c2c(O)ccc(CCNCCc3ccc(CNCCc4c(Cl)cccc4Cl)cc3)c2s1 10.1016/j.bmcl.2011.10.049
11124502 119190 0 None -630 2 Human 6.0 pEC50 = 6 Functional
Activity against human beta 2 adrenergic receptor (AR), expressed in CHO cellsActivity against human beta 2 adrenergic receptor (AR), expressed in CHO cells
ChEMBL 551 13 4 7 3.3 C[C@H](CNc1cccc(CCS(=O)(=O)NS(=O)(=O)c2ccccc2)c1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0101500
CHEMBL347400 119190 0 None -630 2 Human 6.0 pEC50 = 6 Functional
Activity against human beta 2 adrenergic receptor (AR), expressed in CHO cellsActivity against human beta 2 adrenergic receptor (AR), expressed in CHO cells
ChEMBL 551 13 4 7 3.3 C[C@H](CNc1cccc(CCS(=O)(=O)NS(=O)(=O)c2ccccc2)c1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0101500
11647543 137695 0 None -3981 3 Human 6.0 pEC50 = 6 Functional
Activity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 424 9 4 4 4.8 C[C@H](CNc1cccc(-c2ccccc2C(=O)O)c1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0509445
CHEMBL377028 137695 0 None -3981 3 Human 6.0 pEC50 = 6 Functional
Activity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 424 9 4 4 4.8 C[C@H](CNc1cccc(-c2ccccc2C(=O)O)c1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0509445
44428083 92115 0 None 4 2 Guinea pig 6.0 pEC50 = 6 Functional
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contractionAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction
ChEMBL 444 10 5 9 0.7 CC(Cc1ccc(OCc2no[n+]([O-])c2C(N)=O)cc1)NCC(O)c1cc(O)cc(O)c1 10.1021/jm0704595
CHEMBL243266 92115 0 None 4 2 Guinea pig 6.0 pEC50 = 6 Functional
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contractionAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction
ChEMBL 444 10 5 9 0.7 CC(Cc1ccc(OCc2no[n+]([O-])c2C(N)=O)cc1)NCC(O)c1cc(O)cc(O)c1 10.1021/jm0704595
127045854 139021 0 None -3 2 Human 6.0 pEC50 = 6 Functional
Agonist activity at human beta2 receptor expressed in HEK293 cells cotransfected with Gqs5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositolAgonist activity at human beta2 receptor expressed in HEK293 cells cotransfected with Gqs5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositol
ChEMBL 492 12 4 7 3.6 COc1cc(CCNC[C@@H](O)c2ccc(O)c3c2OCC(=O)N3)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
CHEMBL3797205 139021 0 None -3 2 Human 6.0 pEC50 = 6 Functional
Agonist activity at human beta2 receptor expressed in HEK293 cells cotransfected with Gqs5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositolAgonist activity at human beta2 receptor expressed in HEK293 cells cotransfected with Gqs5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositol
ChEMBL 492 12 4 7 3.6 COc1cc(CCNC[C@@H](O)c2ccc(O)c3c2OCC(=O)N3)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
1499 2052 43 None -72 36 Human 6.0 pEC50 = 6 Functional
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2009.06.031
3779 2052 43 None -72 36 Human 6.0 pEC50 = 6 Functional
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2009.06.031
536 2052 43 None -72 36 Human 6.0 pEC50 = 6 Functional
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2009.06.031
CHEMBL434 2052 43 None -72 36 Human 6.0 pEC50 = 6 Functional
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2009.06.031
DB01064 2052 43 None -72 36 Human 6.0 pEC50 = 6 Functional
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2009.06.031
90644152 111747 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 503 11 5 6 3.1 O=C(Cc1ccccc1)NC1CCN(c2ccc(CCNCC(O)c3ccc(O)c(CO)c3)cc2)CC1 10.1016/j.bmcl.2014.04.069
CHEMBL3290981 111747 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 503 11 5 6 3.1 O=C(Cc1ccccc1)NC1CCN(c2ccc(CCNCC(O)c3ccc(O)c(CO)c3)cc2)CC1 10.1016/j.bmcl.2014.04.069
44331425 4364 0 None -100 3 Human 6.0 pEC50 = 6 Functional
Beta-2 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-2-adrenoceptorBeta-2 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-2-adrenoceptor
ChEMBL 576 13 6 8 2.5 CC(C)C[C@H](NC(=O)c1ccc(N2CCC(CNC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)CC2)cc1)C(=O)O 10.1016/s0960-894x(02)00608-x
CHEMBL101630 4364 0 None -100 3 Human 6.0 pEC50 = 6 Functional
Beta-2 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-2-adrenoceptorBeta-2 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-2-adrenoceptor
ChEMBL 576 13 6 8 2.5 CC(C)C[C@H](NC(=O)c1ccc(N2CCC(CNC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)CC2)cc1)C(=O)O 10.1016/s0960-894x(02)00608-x
11718543 165268 0 None -251 3 Human 5.0 pEC50 = 5 Functional
Activity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 411 9 4 5 3.8 O=C(O)c1cccc(-c2cccc(NCCNC[C@H](O)c3cccc(Cl)c3)c2)n1 10.1021/jm0509445
CHEMBL424866 165268 0 None -251 3 Human 5.0 pEC50 = 5 Functional
Activity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 411 9 4 5 3.8 O=C(O)c1cccc(-c2cccc(NCCNC[C@H](O)c3cccc(Cl)c3)c2)n1 10.1021/jm0509445
168277791 192231 0 None - 1 Human 5.0 pEC50 = 5 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 368 6 3 4 3.0 COc1ccc(CNC(CO)c2cc(F)c(N)c(Br)c2)cc1 10.1021/acs.jmedchem.1c02006
CHEMBL5176681 192231 0 None - 1 Human 5.0 pEC50 = 5 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 368 6 3 4 3.0 COc1ccc(CNC(CO)c2cc(F)c(N)c(Br)c2)cc1 10.1021/acs.jmedchem.1c02006
CHEMBL5221722 192231 0 None - 1 Human 5.0 pEC50 = 5 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 368 6 3 4 3.0 COc1ccc(CNC(CO)c2cc(F)c(N)c(Br)c2)cc1 10.1021/acs.jmedchem.1c02006
168294241 192392 0 None - 1 Human 5.0 pEC50 = 5 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 338 5 3 3 3.0 Nc1c(F)cc(C(CO)NCc2ccccc2)cc1Br 10.1021/acs.jmedchem.1c02006
CHEMBL5205567 192392 0 None - 1 Human 5.0 pEC50 = 5 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 338 5 3 3 3.0 Nc1c(F)cc(C(CO)NCc2ccccc2)cc1Br 10.1021/acs.jmedchem.1c02006
CHEMBL5222734 192392 0 None - 1 Human 5.0 pEC50 = 5 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 338 5 3 3 3.0 Nc1c(F)cc(C(CO)NCc2ccccc2)cc1Br 10.1021/acs.jmedchem.1c02006
2685 875 15 None - 1 Human 5.0 pEC50 = 5 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 494 11 4 8 2.3 OC(COc1ccc(cc1)c1nc(cn1C)C(F)(F)F)CNCCOc1ccc(c(c1)C(=O)N)O 10.1021/jm400348g
541 875 15 None - 1 Human 5.0 pEC50 = 5 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 494 11 4 8 2.3 OC(COc1ccc(cc1)c1nc(cn1C)C(F)(F)F)CNCCOc1ccc(c(c1)C(=O)N)O 10.1021/jm400348g
CHEMBL280822 875 15 None - 1 Human 5.0 pEC50 = 5 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 494 11 4 8 2.3 OC(COc1ccc(cc1)c1nc(cn1C)C(F)(F)F)CNCCOc1ccc(c(c1)C(=O)N)O 10.1021/jm400348g
12578 921 55 None -1348 3 Human 5.0 pEC50 = 5 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 219 4 3 4 1.2 CC(C)NCC(C1=CC(=C(C=C1)N)C#N)O 10.1021/jm400348g
2755 921 55 None -1348 3 Human 5.0 pEC50 = 5 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 219 4 3 4 1.2 CC(C)NCC(C1=CC(=C(C=C1)N)C#N)O 10.1021/jm400348g
CHEMBL1374751 921 55 None -1348 3 Human 5.0 pEC50 = 5 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 219 4 3 4 1.2 CC(C)NCC(C1=CC(=C(C=C1)N)C#N)O 10.1021/jm400348g
5311116 2293 6 None -4365 3 Human 5.0 pEC50 = 5 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 484 15 5 8 2.2 N#Cc1cc(OCCOCC2CC2)ccc1OCC(CNCCNC(=O)Nc1ccc(cc1)O)O 10.1021/jm400348g
544 2293 6 None -4365 3 Human 5.0 pEC50 = 5 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 484 15 5 8 2.2 N#Cc1cc(OCCOCC2CC2)ccc1OCC(CNCCNC(=O)Nc1ccc(cc1)O)O 10.1021/jm400348g
CHEMBL207802 2293 6 None -4365 3 Human 5.0 pEC50 = 5 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 484 15 5 8 2.2 N#Cc1cc(OCCOCC2CC2)ccc1OCC(CNCCNC(=O)Nc1ccc(cc1)O)O 10.1021/jm400348g
66653268 87809 0 None -3311 3 Human 5.0 pEC50 = 5 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 491 14 4 6 3.8 O=C(NCCNCC(O)COc1ccc(OCCOC2CCCC2)cc1)Nc1cccc(Cl)c1 10.1021/jm400348g
CHEMBL2348201 87809 0 None -3311 3 Human 5.0 pEC50 = 5 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 491 14 4 6 3.8 O=C(NCCNCC(O)COc1ccc(OCCOC2CCCC2)cc1)Nc1cccc(Cl)c1 10.1021/jm400348g
56598967 87819 0 None -2238 3 Human 5.0 pEC50 = 5 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 457 14 4 6 3.2 O=C(NCCNCC(O)COc1ccc(OCCOC2CCCC2)cc1)Nc1ccccc1 10.1021/jm400348g
CHEMBL2348211 87819 0 None -2238 3 Human 5.0 pEC50 = 5 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 457 14 4 6 3.2 O=C(NCCNCC(O)COc1ccc(OCCOC2CCCC2)cc1)Nc1ccccc1 10.1021/jm400348g
56598833 87825 0 None -436 3 Human 5.0 pEC50 = 5 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 433 14 5 7 2.0 CCOCCOc1ccc(OCC(O)CNCCNC(=O)Nc2ccc(O)cc2)cc1 10.1021/jm400348g
CHEMBL2348217 87825 0 None -436 3 Human 5.0 pEC50 = 5 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 433 14 5 7 2.0 CCOCCOc1ccc(OCC(O)CNCCNC(=O)Nc2ccc(O)cc2)cc1 10.1021/jm400348g
56598832 87826 0 None -4365 3 Human 5.0 pEC50 = 5 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 527 16 5 7 3.3 O=C(NCCNCC(O)COc1ccc(OCCOCCc2ccc(F)cc2)cc1)Nc1ccc(O)cc1 10.1021/jm400348g
CHEMBL2348218 87826 0 None -4365 3 Human 5.0 pEC50 = 5 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 527 16 5 7 3.3 O=C(NCCNCC(O)COc1ccc(OCCOCCc2ccc(F)cc2)cc1)Nc1ccc(O)cc1 10.1021/jm400348g
56597179 87827 0 None -2754 3 Human 5.0 pEC50 = 5 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 473 14 5 7 2.9 O=C(NCCNCC(O)COc1ccc(OCCOC2CCCC2)cc1)Nc1ccc(O)cc1 10.1021/jm400348g
CHEMBL2348219 87827 0 None -2754 3 Human 5.0 pEC50 = 5 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 473 14 5 7 2.9 O=C(NCCNCC(O)COc1ccc(OCCOC2CCCC2)cc1)Nc1ccc(O)cc1 10.1021/jm400348g
56598831 88699 0 None -1023 3 Human 5.0 pEC50 = 5 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 459 15 5 7 2.3 O=C(NCCNCC(O)COc1ccc(OCCOCC2CC2)cc1)Nc1ccc(O)cc1 10.1021/jm400348g
CHEMBL2348220 88699 0 None -1023 3 Human 5.0 pEC50 = 5 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 459 15 5 7 2.3 O=C(NCCNCC(O)COc1ccc(OCCOCC2CC2)cc1)Nc1ccc(O)cc1 10.1021/jm400348g
CHEMBL2365796 88699 0 None -1023 3 Human 5.0 pEC50 = 5 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 459 15 5 7 2.3 O=C(NCCNCC(O)COc1ccc(OCCOCC2CC2)cc1)Nc1ccc(O)cc1 10.1021/jm400348g
90644151 111746 0 None - 1 Human 5.0 pEC50 = 5 Functional
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 413 8 4 6 1.4 CC(=O)N1CCN(c2ccc(CCNCC(O)c3ccc(O)c(CO)c3)cc2)CC1 10.1016/j.bmcl.2014.04.069
CHEMBL3290980 111746 0 None - 1 Human 5.0 pEC50 = 5 Functional
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 413 8 4 6 1.4 CC(=O)N1CCN(c2ccc(CCNCC(O)c3ccc(O)c(CO)c3)cc2)CC1 10.1016/j.bmcl.2014.04.069
73056758 103787 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulationAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulation
ChEMBL 331 8 4 5 2.8 CC[C@@H](Cc1ccc(OC)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2013.11.030
CHEMBL3099660 103787 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulationAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulation
ChEMBL 331 8 4 5 2.8 CC[C@@H](Cc1ccc(OC)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2013.11.030
90666108 108837 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP productionAgonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP production
ChEMBL 718 18 6 9 6.5 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3cc(F)cc(F)c3O)CC2)ccc1O 10.1039/C1MD00140J
CHEMBL3219038 108837 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP productionAgonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP production
ChEMBL 718 18 6 9 6.5 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3cc(F)cc(F)c3O)CC2)ccc1O 10.1039/C1MD00140J
89108753 192267 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 310 6 3 3 3.4 CCCCNC(CO)c1cc(Cl)c(N)c(C(F)(F)F)c1 10.1021/acs.jmedchem.1c02006
CHEMBL5186069 192267 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 310 6 3 3 3.4 CCCCNC(CO)c1cc(Cl)c(N)c(C(F)(F)F)c1 10.1021/acs.jmedchem.1c02006
CHEMBL5221958 192267 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 310 6 3 3 3.4 CCCCNC(CO)c1cc(Cl)c(N)c(C(F)(F)F)c1 10.1021/acs.jmedchem.1c02006
16735272 85371 0 None -57 2 Rat 7.0 pEC50 = 7.0 Functional
Agonist activity beta2-adrenergic receptor in rat ventricular myocytes assessed as cell contraction following electrical stimulation by optical edge tracking method using photodiode arrayAgonist activity beta2-adrenergic receptor in rat ventricular myocytes assessed as cell contraction following electrical stimulation by optical edge tracking method using photodiode array
ChEMBL 337 6 4 4 3.5 C[C@@H](Cc1cccc2ccccc12)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2009.11.062
CHEMBL229614 85371 0 None -57 2 Rat 7.0 pEC50 = 7.0 Functional
Agonist activity beta2-adrenergic receptor in rat ventricular myocytes assessed as cell contraction following electrical stimulation by optical edge tracking method using photodiode arrayAgonist activity beta2-adrenergic receptor in rat ventricular myocytes assessed as cell contraction following electrical stimulation by optical edge tracking method using photodiode array
ChEMBL 337 6 4 4 3.5 C[C@@H](Cc1cccc2ccccc12)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2009.11.062
2952103 29087 12 None - 1 Human 6.0 pEC50 = 6.0 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 376 3 0 5 3.9 CCOC(=O)N1CCN(c2nnc(-c3ccc(C)cc3)c3ccccc23)CC1 nan
CHEMBL1383120 29087 12 None - 1 Human 6.0 pEC50 = 6.0 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 376 3 0 5 3.9 CCOC(=O)N1CCN(c2nnc(-c3ccc(C)cc3)c3ccccc23)CC1 nan
2945777 31517 14 None - 1 Human 6.0 pEC50 = 6.0 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 454 8 1 9 4.0 COc1cc(OC)nc(NC(=O)CSc2nnc(-c3ccccc3)n2C2CCCCC2)n1 nan
CHEMBL1405897 31517 14 None - 1 Human 6.0 pEC50 = 6.0 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 454 8 1 9 4.0 COc1cc(OC)nc(NC(=O)CSc2nnc(-c3ccccc3)n2C2CCCCC2)n1 nan
10745501 110047 0 None -288 2 Human 5.0 pEC50 = 5.0 Functional
Increased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 2 adrenergic receptorsIncreased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 2 adrenergic receptors
ChEMBL 562 13 5 8 2.4 CCCCN(CC(=O)O)C(=O)c1ccc(N2CCC(NC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)CC2)cc1 10.1021/jm000544b
CHEMBL32521 110047 0 None -288 2 Human 5.0 pEC50 = 5.0 Functional
Increased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 2 adrenergic receptorsIncreased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 2 adrenergic receptors
ChEMBL 562 13 5 8 2.4 CCCCN(CC(=O)O)C(=O)c1ccc(N2CCC(NC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)CC2)cc1 10.1021/jm000544b
659759 46992 10 None 14 2 Human 7.0 pEC50 = 7.0 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 359 4 1 4 3.0 CC(=O)Nc1ccc(S(=O)(=O)N2CCCCC2c2cccnc2)cc1 nan
CHEMBL1543973 46992 10 None 14 2 Human 7.0 pEC50 = 7.0 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 359 4 1 4 3.0 CC(=O)Nc1ccc(S(=O)(=O)N2CCCCC2c2cccnc2)cc1 nan
18559738 35067 8 None - 1 Human 6.0 pEC50 = 6.0 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 426 5 0 6 4.3 COc1cc2ncc(S(=O)(=O)c3ccccc3)c(N3CCCC(C)C3)c2cc1OC nan
CHEMBL1436649 35067 8 None - 1 Human 6.0 pEC50 = 6.0 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 426 5 0 6 4.3 COc1cc2ncc(S(=O)(=O)c3ccccc3)c(N3CCCC(C)C3)c2cc1OC nan
664890 40141 9 None 9 3 Human 6.0 pEC50 = 6.0 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 431 8 1 7 5.0 Cc1ccc(OCc2nnc(SCc3nc4ccccc4[nH]3)n2Cc2ccco2)cc1 nan
CHEMBL1482007 40141 9 None 9 3 Human 6.0 pEC50 = 6.0 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 431 8 1 7 5.0 Cc1ccc(OCc2nnc(SCc3nc4ccccc4[nH]3)n2Cc2ccco2)cc1 nan
25023951 176369 0 None - 1 Golden hamster 6.0 pEC50 = 6.0 Functional
Agonist activity at adrenergic beta2 receptor in Syrian hamster DDT1 MF2 cells assessed as stimulation of cAMP accumulation by radioimmunoassay in presence of 1 uM DPCPXAgonist activity at adrenergic beta2 receptor in Syrian hamster DDT1 MF2 cells assessed as stimulation of cAMP accumulation by radioimmunoassay in presence of 1 uM DPCPX
ChEMBL 489 11 8 13 -0.8 Nc1cc(C(O)CNCCCCNc2ncnc3c2ncn3[C@@H]2O[C@H](CO)[C@@H](O)[C@H]2O)ccc1O 10.1021/jm800613s
CHEMBL462274 176369 0 None - 1 Golden hamster 6.0 pEC50 = 6.0 Functional
Agonist activity at adrenergic beta2 receptor in Syrian hamster DDT1 MF2 cells assessed as stimulation of cAMP accumulation by radioimmunoassay in presence of 1 uM DPCPXAgonist activity at adrenergic beta2 receptor in Syrian hamster DDT1 MF2 cells assessed as stimulation of cAMP accumulation by radioimmunoassay in presence of 1 uM DPCPX
ChEMBL 489 11 8 13 -0.8 Nc1cc(C(O)CNCCCCNc2ncnc3c2ncn3[C@@H]2O[C@H](CO)[C@@H](O)[C@H]2O)ccc1O 10.1021/jm800613s
3759952 22268 7 None - 1 Human 6.0 pEC50 = 6.0 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 368 5 3 6 2.8 CCOC(=O)C1(C)C=C(Nc2ccc(O)cc2)C(=O)N1c1ccc(O)cc1 nan
4017821 22268 7 None - 1 Human 6.0 pEC50 = 6.0 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 368 5 3 6 2.8 CCOC(=O)C1(C)C=C(Nc2ccc(O)cc2)C(=O)N1c1ccc(O)cc1 nan
CHEMBL1325241 22268 7 None - 1 Human 6.0 pEC50 = 6.0 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 368 5 3 6 2.8 CCOC(=O)C1(C)C=C(Nc2ccc(O)cc2)C(=O)N1c1ccc(O)cc1 nan
4183 1986 62 None 1 4 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assayAgonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assay
ChEMBL 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O 10.1021/jm100068m
6918554 1986 62 None 1 4 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assayAgonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assay
ChEMBL 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O 10.1021/jm100068m
7455 1986 62 None 1 4 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assayAgonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assay
ChEMBL 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O 10.1021/jm100068m
CHEMBL1095777 1986 62 None 1 4 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assayAgonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assay
ChEMBL 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O 10.1021/jm100068m
DB05039 1986 62 None 1 4 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assayAgonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assay
ChEMBL 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O 10.1021/jm100068m
44392480 64233 0 None -1 2 Human 8.0 pEC50 = 8.0 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-2 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-2 adrenergic receptor
ChEMBL 471 12 4 6 4.1 CC/C=C/CNc1cccc([C@@H](O)CN[C@H](C)Cc2c[nH]c3c(OS(C)(=O)=O)cccc23)c1 10.1016/j.bmcl.2004.12.033
CHEMBL181603 64233 0 None -1 2 Human 8.0 pEC50 = 8.0 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-2 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-2 adrenergic receptor
ChEMBL 471 12 4 6 4.1 CC/C=C/CNc1cccc([C@@H](O)CN[C@H](C)Cc2c[nH]c3c(OS(C)(=O)=O)cccc23)c1 10.1016/j.bmcl.2004.12.033
59548053 124752 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 878 18 6 9 7.5 C[C@@H](Cc1cccc(CCC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645355 124752 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 878 18 6 9 7.5 C[C@@H](Cc1cccc(CCC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
45484538 13968 0 None 2 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP level
ChEMBL 556 13 6 7 1.9 CC(C)(Cc1ccc(NC(=O)CCCNC(=O)C[N+](C)(C)C)cc1)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmcl.2009.06.104
CHEMBL1197779 13968 0 None 2 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP level
ChEMBL 556 13 6 7 1.9 CC(C)(Cc1ccc(NC(=O)CCCNC(=O)C[N+](C)(C)C)cc1)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmcl.2009.06.104
CHEMBL585382 13968 0 None 2 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP level
ChEMBL 556 13 6 7 1.9 CC(C)(Cc1ccc(NC(=O)CCCNC(=O)C[N+](C)(C)C)cc1)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmcl.2009.06.104
1287365 37568 9 None - 1 Human 7.9 pEC50 = 7.9 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 373 5 2 3 5.3 Cc1ccc(SCC(=O)Nc2ccc(-c3nc4ccccc4[nH]3)cc2)cc1 nan
CHEMBL1458579 37568 9 None - 1 Human 7.9 pEC50 = 7.9 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 373 5 2 3 5.3 Cc1ccc(SCC(=O)Nc2ccc(-c3nc4ccccc4[nH]3)cc2)cc1 nan
46232857 199064 0 None 19 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 440 7 4 6 3.3 CC(C)(Cc1ccc(OC(F)(F)F)cc1)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmcl.2009.12.087
CHEMBL600400 199064 0 None 19 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 440 7 4 6 3.3 CC(C)(Cc1ccc(OC(F)(F)F)cc1)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmcl.2009.12.087
44428083 92115 0 None 4 2 Guinea pig 7.0 pEC50 = 7.0 Functional
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contractionAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction
ChEMBL 444 10 5 9 0.7 CC(Cc1ccc(OCc2no[n+]([O-])c2C(N)=O)cc1)NCC(O)c1cc(O)cc(O)c1 10.1021/jm0704595
CHEMBL243266 92115 0 None 4 2 Guinea pig 7.0 pEC50 = 7.0 Functional
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contractionAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction
ChEMBL 444 10 5 9 0.7 CC(Cc1ccc(OCc2no[n+]([O-])c2C(N)=O)cc1)NCC(O)c1cc(O)cc(O)c1 10.1021/jm0704595
44428085 92816 0 None - 1 Guinea pig 7.0 pEC50 = 7.0 Functional
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contractionAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction
ChEMBL 399 9 4 8 2.6 Cc1nonc1COc1ccc(CC(C)NCC(O)c2cc(O)cc(O)c2)cc1 10.1021/jm0704595
CHEMBL244906 92816 0 None - 1 Guinea pig 7.0 pEC50 = 7.0 Functional
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contractionAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction
ChEMBL 399 9 4 8 2.6 Cc1nonc1COc1ccc(CC(C)NCC(O)c2cc(O)cc(O)c2)cc1 10.1021/jm0704595
1155 1592 45 None 2 3 Human 7.0 pEC50 = 7.0 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O nan
3343 1592 45 None 2 3 Human 7.0 pEC50 = 7.0 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O nan
557 1592 45 None 2 3 Human 7.0 pEC50 = 7.0 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O nan
CHEMBL32800 1592 45 None 2 3 Human 7.0 pEC50 = 7.0 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O nan
DB01288 1592 45 None 2 3 Human 7.0 pEC50 = 7.0 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O nan
44428083 92115 0 None 4 2 Guinea pig 6.0 pEC50 = 6.0 Functional
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-oneAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-one
ChEMBL 444 10 5 9 0.7 CC(Cc1ccc(OCc2no[n+]([O-])c2C(N)=O)cc1)NCC(O)c1cc(O)cc(O)c1 10.1021/jm0704595
CHEMBL243266 92115 0 None 4 2 Guinea pig 6.0 pEC50 = 6.0 Functional
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-oneAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-one
ChEMBL 444 10 5 9 0.7 CC(Cc1ccc(OCc2no[n+]([O-])c2C(N)=O)cc1)NCC(O)c1cc(O)cc(O)c1 10.1021/jm0704595
24895263 192943 0 None -31622 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 475 10 4 6 4.6 Nc1ccc([C@@H](O)CNCCc2ccc(-c3ccc(C(=O)O)c(OC4CCCCC4)c3)cc2)cn1 10.1021/jm8000345
CHEMBL529659 192943 0 None -31622 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 475 10 4 6 4.6 Nc1ccc([C@@H](O)CNCCc2ccc(-c3ccc(C(=O)O)c(OC4CCCCC4)c3)cc2)cn1 10.1021/jm8000345
44591508 178407 0 None -31622 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 475 10 4 6 4.6 Nc1ccncc1[C@@H](O)CNCCc1ccc(-c2ccc(C(=O)O)c(OC3CCCCC3)c2)cc1 10.1021/jm9000709
CHEMBL470857 178407 0 None -31622 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 475 10 4 6 4.6 Nc1ccncc1[C@@H](O)CNCCc1ccc(-c2ccc(C(=O)O)c(OC3CCCCC3)c2)cc1 10.1021/jm9000709
1542103 22269 24 None -3 3 Human 5.9 pEC50 = 5.9 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory)
ChEMBL 418 4 0 6 4.2 Cc1ccccc1N1CCN(c2ncnc3c2cnn3Cc2ccc(Cl)cc2)CC1 nan
CHEMBL1325250 22269 24 None -3 3 Human 5.9 pEC50 = 5.9 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory)
ChEMBL 418 4 0 6 4.2 Cc1ccccc1N1CCN(c2ncnc3c2cnn3Cc2ccc(Cl)cc2)CC1 nan
46221604 8457 0 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assayAgonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assay
ChEMBL 392 6 4 4 3.1 CCc1ccc(CC)c2c1CC(NC[C@H](O)c1ccc(O)c3[nH]c(=O)ccc13)C2 10.1021/jm100068m
CHEMBL1094487 8457 0 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assayAgonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assay
ChEMBL 392 6 4 4 3.1 CCc1ccc(CC)c2c1CC(NC[C@H](O)c1ccc(O)c3[nH]c(=O)ccc13)C2 10.1021/jm100068m
44589133 175261 0 None -1 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at adrenergic beta-2 receptorAgonist activity at adrenergic beta-2 receptor
ChEMBL 354 8 2 4 3.4 CC(C)NCC(O)COc1ccc2c(c1)CCCN2Cc1ccccc1 10.1016/j.bmc.2008.11.030
CHEMBL458541 175261 0 None -1 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at adrenergic beta-2 receptorAgonist activity at adrenergic beta-2 receptor
ChEMBL 354 8 2 4 3.4 CC(C)NCC(O)COc1ccc2c(c1)CCCN2Cc1ccccc1 10.1016/j.bmc.2008.11.030
54586986 61470 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as stimulation of intracellular cAMP production after 30 mins of washing by wash-off assayAgonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as stimulation of intracellular cAMP production after 30 mins of washing by wash-off assay
ChEMBL 780 27 6 8 8.0 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCCNC(=O)CCCCCCCCCCNC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)ccc1O)C(C)C 10.1016/j.bmcl.2010.10.132
CHEMBL1773263 61470 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as stimulation of intracellular cAMP production after 30 mins of washing by wash-off assayAgonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as stimulation of intracellular cAMP production after 30 mins of washing by wash-off assay
ChEMBL 780 27 6 8 8.0 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCCNC(=O)CCCCCCCCCCNC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)ccc1O)C(C)C 10.1016/j.bmcl.2010.10.132
44610361 123457 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as stumulation of intracellular cAMP productionAgonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as stumulation of intracellular cAMP production
ChEMBL 698 14 5 9 4.9 O=c1ccc2c([C@@H](O)CNCCc3ccc(CCN4CCC(Cn5cnc(C(O)(c6ccccc6)c6ccccc6)n5)CC4)cc3)ccc(O)c2[nH]1 10.1016/j.bmcl.2015.10.008
CHEMBL3629357 123457 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as stumulation of intracellular cAMP productionAgonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as stumulation of intracellular cAMP production
ChEMBL 698 14 5 9 4.9 O=c1ccc2c([C@@H](O)CNCCc3ccc(CCN4CCC(Cn5cnc(C(O)(c6ccccc6)c6ccccc6)n5)CC4)cc3)ccc(O)c2[nH]1 10.1016/j.bmcl.2015.10.008
2488220 28601 3 None - 1 Human 6.9 pEC50 = 6.9 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 409 5 0 6 1.1 CN(CC(=O)N1CCN(c2ncccn2)CC1)S(=O)(=O)c1ccc(Cl)cc1 nan
CHEMBL1379002 28601 3 None - 1 Human 6.9 pEC50 = 6.9 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 409 5 0 6 1.1 CN(CC(=O)N1CCN(c2ncccn2)CC1)S(=O)(=O)c1ccc(Cl)cc1 nan
145986105 164807 0 None -83 3 Human 6.9 pEC50 = 6.9 Functional
Antagonist activity at human beta2 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta2 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 429 10 4 4 4.0 O=C(Nc1ccc(CCNC[C@H](O)COc2cccc3[nH]ccc23)cc1)c1ccccc1 10.1016/j.ejmech.2018.03.032
CHEMBL4237453 164807 0 None -83 3 Human 6.9 pEC50 = 6.9 Functional
Antagonist activity at human beta2 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta2 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 429 10 4 4 4.0 O=C(Nc1ccc(CCNC[C@H](O)COc2cccc3[nH]ccc23)cc1)c1ccccc1 10.1016/j.ejmech.2018.03.032
168289963 192350 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 334 8 3 4 2.2 CCOCCCNC(CO)c1cc(F)c(N)c(Br)c1 10.1021/acs.jmedchem.1c02006
CHEMBL5195910 192350 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 334 8 3 4 2.2 CCOCCCNC(CO)c1cc(F)c(N)c(Br)c1 10.1021/acs.jmedchem.1c02006
CHEMBL5222469 192350 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 334 8 3 4 2.2 CCOCCCNC(CO)c1cc(F)c(N)c(Br)c1 10.1021/acs.jmedchem.1c02006
2560512 23840 6 None - 1 Human 5.9 pEC50 = 5.9 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 335 4 2 9 1.7 Nc1cc(N)nc(SCc2cc([N+](=O)[O-])cc3c2OCOC3)n1 nan
CHEMBL1338286 23840 6 None - 1 Human 5.9 pEC50 = 5.9 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 335 4 2 9 1.7 Nc1cc(N)nc(SCc2cc([N+](=O)[O-])cc3c2OCOC3)n1 nan
1267856 45671 11 None 31 2 Human 5.9 pEC50 = 5.9 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 351 6 1 7 2.2 CCOC(=O)c1ccc(NC(=O)Cn2nnc(-c3ccccc3)n2)cc1 nan
CHEMBL1532219 45671 11 None 31 2 Human 5.9 pEC50 = 5.9 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 351 6 1 7 2.2 CCOC(=O)c1ccc(NC(=O)Cn2nnc(-c3ccccc3)n2)cc1 nan
5182299 24714 9 None - 1 Human 6.9 pEC50 = 6.9 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory)
ChEMBL 457 5 1 4 4.5 O=C(Nc1ccc(S(=O)(=O)N2CCCCC2c2cccnc2)cc1)c1c(F)cccc1F nan
CHEMBL1345891 24714 9 None - 1 Human 6.9 pEC50 = 6.9 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory)
ChEMBL 457 5 1 4 4.5 O=C(Nc1ccc(S(=O)(=O)N2CCCCC2c2cccnc2)cc1)c1c(F)cccc1F nan
9871800 56179 0 None -120 3 Human 5.9 pEC50 = 5.9 Functional
Agonistic activity was assessed by measurement of cAMP accumulation levels in CHO cells expressing human beta-2-adrenergic receptorAgonistic activity was assessed by measurement of cAMP accumulation levels in CHO cells expressing human beta-2-adrenergic receptor
ChEMBL 534 9 5 9 2.0 CS(=O)(=O)Nc1cc([C@@H](O)CNC2CCN(c3ccc(CC4SC(=O)NC4=O)cc3)CC2)ccc1O 10.1016/s0960-894x(01)00063-4
CHEMBL163262 56179 0 None -120 3 Human 5.9 pEC50 = 5.9 Functional
Agonistic activity was assessed by measurement of cAMP accumulation levels in CHO cells expressing human beta-2-adrenergic receptorAgonistic activity was assessed by measurement of cAMP accumulation levels in CHO cells expressing human beta-2-adrenergic receptor
ChEMBL 534 9 5 9 2.0 CS(=O)(=O)Nc1cc([C@@H](O)CNC2CCN(c3ccc(CC4SC(=O)NC4=O)cc3)CC2)ccc1O 10.1016/s0960-894x(01)00063-4
44396509 66947 0 None -6 2 Human 7.9 pEC50 = 7.9 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptor
ChEMBL 513 11 4 6 5.1 CC(C)Oc1cccc2c(C[C@@H](C)NC[C@H](O)c3cccc(NS(=O)(=O)c4cccs4)c3)c[nH]c12 10.1016/j.bmcl.2004.10.035
CHEMBL188315 66947 0 None -6 2 Human 7.9 pEC50 = 7.9 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptor
ChEMBL 513 11 4 6 5.1 CC(C)Oc1cccc2c(C[C@@H](C)NC[C@H](O)c3cccc(NS(=O)(=O)c4cccs4)c3)c[nH]c12 10.1016/j.bmcl.2004.10.035
44331444 4190 0 None 2 3 Human 7.9 pEC50 = 7.9 Functional
Beta-2 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-2-adrenoceptorBeta-2 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-2-adrenoceptor
ChEMBL 709 13 5 8 4.2 CC(C)N(Cc1cc(F)ccc1F)C(=O)Nc1ccc(S(=O)(=O)N2CCC(CNC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)CC2)cc1 10.1016/s0960-894x(02)00608-x
CHEMBL100589 4190 0 None 2 3 Human 7.9 pEC50 = 7.9 Functional
Beta-2 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-2-adrenoceptorBeta-2 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-2-adrenoceptor
ChEMBL 709 13 5 8 4.2 CC(C)N(Cc1cc(F)ccc1F)C(=O)Nc1ccc(S(=O)(=O)N2CCC(CNC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)CC2)cc1 10.1016/s0960-894x(02)00608-x
10221081 123568 1 None -10 3 Rat 7.9 pEC50 = 7.9 Functional
Vasodilating activity against phenylephrine-induced contractions in rat thoracic aortaVasodilating activity against phenylephrine-induced contractions in rat thoracic aorta
ChEMBL 270 4 0 6 0.5 CCOc1no[n+]([O-])c1S(=O)(=O)c1ccccc1 10.1021/jm0704595
CHEMBL363325 123568 1 None -10 3 Rat 7.9 pEC50 = 7.9 Functional
Vasodilating activity against phenylephrine-induced contractions in rat thoracic aortaVasodilating activity against phenylephrine-induced contractions in rat thoracic aorta
ChEMBL 270 4 0 6 0.5 CCOc1no[n+]([O-])c1S(=O)(=O)c1ccccc1 10.1021/jm0704595
16222317 199187 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 392 6 4 5 2.6 CC(C)(Cc1cc(F)cc(F)c1)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmcl.2009.12.087
CHEMBL601429 199187 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 392 6 4 5 2.6 CC(C)(Cc1cc(F)cc(F)c1)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmcl.2009.12.087
11189433 199189 0 None 57 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 424 6 4 5 3.4 CC(C)(Cc1ccc(C(F)(F)F)cc1)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmcl.2009.12.087
CHEMBL601430 199189 0 None 57 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 424 6 4 5 3.4 CC(C)(Cc1ccc(C(F)(F)F)cc1)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmcl.2009.12.087
16735495 85345 0 None 3 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assayAgonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assay
ChEMBL 337 6 4 4 3.5 C[C@H](Cc1cccc2ccccc12)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2009.11.062
CHEMBL229401 85345 0 None 3 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assayAgonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assay
ChEMBL 337 6 4 4 3.5 C[C@H](Cc1cccc2ccccc12)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2009.11.062
16049160 63745 0 None 10 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 491 15 5 8 3.3 CCOc1ccc(CCNCCCSCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)cc1 10.1016/j.bmcl.2011.05.097
CHEMBL1807825 63745 0 None 10 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 491 15 5 8 3.3 CCOc1ccc(CCNCCCSCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)cc1 10.1016/j.bmcl.2011.05.097
90655869 110765 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assayAgonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assay
ChEMBL 574 15 3 7 4.0 O=C(CCOCCc1cccc(Cl)c1)N(CCNCCc1ccc(O)c2[nH]c(=O)sc12)CCN1CCCCC1 10.1021/ml4005232
CHEMBL3265166 110765 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assayAgonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assay
ChEMBL 574 15 3 7 4.0 O=C(CCOCCc1cccc(Cl)c1)N(CCNCCc1ccc(O)c2[nH]c(=O)sc12)CCN1CCCCC1 10.1021/ml4005232
145992462 166377 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 352 8 4 4 2.9 O=c1ccc2c(C(CO)NCCCCc3ccccc3)ccc(O)c2[nH]1 10.1016/j.ejmech.2018.04.041
CHEMBL4287029 166377 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 352 8 4 4 2.9 O=c1ccc2c(C(CO)NCCCCc3ccccc3)ccc(O)c2[nH]1 10.1016/j.ejmech.2018.04.041
76315639 84879 0 None -1 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at Homo sapiens (human) beta2 adrenoreceptorAgonist activity at Homo sapiens (human) beta2 adrenoreceptor
ChEMBL 507 10 4 6 4.0 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1ccc(C(=O)Nc2ccccc2)cc1 10.1007/s00044-009-9257-x
CHEMBL2260987 84879 0 None -1 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at Homo sapiens (human) beta2 adrenoreceptorAgonist activity at Homo sapiens (human) beta2 adrenoreceptor
ChEMBL 507 10 4 6 4.0 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1ccc(C(=O)Nc2ccccc2)cc1 10.1007/s00044-009-9257-x
127045855 139121 0 None -2 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human beta2 receptor expressed in HEK293 cells cotransfected with Gqs5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositolAgonist activity at human beta2 receptor expressed in HEK293 cells cotransfected with Gqs5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositol
ChEMBL 319 8 4 6 1.8 COc1ccccc1OCCNC[C@H](O)c1ccc(O)c(O)c1 10.1016/j.bmc.2016.04.028
CHEMBL3797876 139121 0 None -2 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human beta2 receptor expressed in HEK293 cells cotransfected with Gqs5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositolAgonist activity at human beta2 receptor expressed in HEK293 cells cotransfected with Gqs5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositol
ChEMBL 319 8 4 6 1.8 COc1ccccc1OCCNC[C@H](O)c1ccc(O)c(O)c1 10.1016/j.bmc.2016.04.028
44428086 149535 0 None 7 2 Guinea pig 5.9 pEC50 = 5.9 Functional
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-oneAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-one
ChEMBL 415 9 4 8 1.9 Cc1c(COc2ccc(CC(C)NCC(O)c3cc(O)cc(O)c3)cc2)no[n+]1[O-] 10.1021/jm0704595
CHEMBL395082 149535 0 None 7 2 Guinea pig 5.9 pEC50 = 5.9 Functional
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-oneAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-one
ChEMBL 415 9 4 8 1.9 Cc1c(COc2ccc(CC(C)NCC(O)c3cc(O)cc(O)c3)cc2)no[n+]1[O-] 10.1021/jm0704595
44565932 186418 0 None -15135 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 528 11 4 8 3.4 CC(C)Sc1cc(-c2ccc(CCNC[C@H](O)c3cnccc3N)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
CHEMBL490733 186418 0 None -15135 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 528 11 4 8 3.4 CC(C)Sc1cc(-c2ccc(CCNC[C@H](O)c3cnccc3N)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
10221081 123568 1 None -10 3 Rat 5.9 pEC50 = 5.9 Functional
Vasodilating activity against phenylephrine-induced contraction in rat thoracic aorta in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-oneVasodilating activity against phenylephrine-induced contraction in rat thoracic aorta in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-one
ChEMBL 270 4 0 6 0.5 CCOc1no[n+]([O-])c1S(=O)(=O)c1ccccc1 10.1021/jm0704595
CHEMBL363325 123568 1 None -10 3 Rat 5.9 pEC50 = 5.9 Functional
Vasodilating activity against phenylephrine-induced contraction in rat thoracic aorta in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-oneVasodilating activity against phenylephrine-induced contraction in rat thoracic aorta in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-one
ChEMBL 270 4 0 6 0.5 CCOc1no[n+]([O-])c1S(=O)(=O)c1ccccc1 10.1021/jm0704595
44428083 92115 0 None -4 2 Rat 5.9 pEC50 = 5.9 Functional
Vasodilating activity against phenylephrine-induced contractions in rat thoracic aortaVasodilating activity against phenylephrine-induced contractions in rat thoracic aorta
ChEMBL 444 10 5 9 0.7 CC(Cc1ccc(OCc2no[n+]([O-])c2C(N)=O)cc1)NCC(O)c1cc(O)cc(O)c1 10.1021/jm0704595
CHEMBL243266 92115 0 None -4 2 Rat 5.9 pEC50 = 5.9 Functional
Vasodilating activity against phenylephrine-induced contractions in rat thoracic aortaVasodilating activity against phenylephrine-induced contractions in rat thoracic aorta
ChEMBL 444 10 5 9 0.7 CC(Cc1ccc(OCc2no[n+]([O-])c2C(N)=O)cc1)NCC(O)c1cc(O)cc(O)c1 10.1021/jm0704595
162386697 184157 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Antagonist activity at ADRB2 (unknown origin)Antagonist activity at ADRB2 (unknown origin)
ChEMBL 390 3 0 6 2.3 O=C(Cc1ccc(Cl)c(Cl)c1)N1CCN(c2ccc3nncn3n2)CC1 10.1021/acs.jmedchem.1c01136
CHEMBL4850904 184157 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Antagonist activity at ADRB2 (unknown origin)Antagonist activity at ADRB2 (unknown origin)
ChEMBL 390 3 0 6 2.3 O=C(Cc1ccc(Cl)c(Cl)c1)N1CCN(c2ccc3nncn3n2)CC1 10.1021/acs.jmedchem.1c01136
580005 44062 10 None - 1 Human 5.9 pEC50 = 5.9 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 319 4 0 6 3.5 c1ccc(CSc2nnnn2-c2cccc3ccccc23)nc1 nan
CHEMBL1517798 44062 10 None - 1 Human 5.9 pEC50 = 5.9 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 319 4 0 6 3.5 c1ccc(CSc2nnnn2-c2cccc3ccccc23)nc1 nan
651592 45628 5 None - 1 Human 5.9 pEC50 = 5.9 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 446 5 0 6 4.0 CN(C)c1ccc(-c2noc(C3CCN(S(=O)(=O)c4cccc(Cl)c4)CC3)n2)cc1 nan
CHEMBL1531826 45628 5 None - 1 Human 5.9 pEC50 = 5.9 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 446 5 0 6 4.0 CN(C)c1ccc(-c2noc(C3CCN(S(=O)(=O)c4cccc(Cl)c4)CC3)n2)cc1 nan
57399439 70500 0 None - 1 Guinea pig 6.9 pEC50 = 6.9 Functional
Agonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contractionAgonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contraction
ChEMBL 538 13 4 8 3.4 COc1ccc(C2=NN(CCCCNC[C@@H](O)c3ccc(O)c(NC=O)c3)C(=O)C3CCCCC23)cc1OC 10.1016/j.bmcl.2012.01.013
CHEMBL1951068 70500 0 None - 1 Guinea pig 6.9 pEC50 = 6.9 Functional
Agonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contractionAgonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contraction
ChEMBL 538 13 4 8 3.4 COc1ccc(C2=NN(CCCCNC[C@@H](O)c3ccc(O)c(NC=O)c3)C(=O)C3CCCCC23)cc1OC 10.1016/j.bmcl.2012.01.013
53307431 63206 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
ChEMBL 499 15 2 6 4.0 CCCCN(CCN(C)CCc1ccc(O)c2[nH]c(=O)sc12)C(=O)CCOCCc1ccccc1 10.1016/j.bmcl.2011.04.135
CHEMBL1800475 63206 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
ChEMBL 499 15 2 6 4.0 CCCCN(CCN(C)CCc1ccc(O)c2[nH]c(=O)sc12)C(=O)CCOCCc1ccccc1 10.1016/j.bmcl.2011.04.135
9888047 92936 0 None -501 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 414 9 4 5 4.4 C[C@H](CNc1cccc(-c2occc2C(=O)O)c1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2007.05.069
CHEMBL245673 92936 0 None -501 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 414 9 4 5 4.4 C[C@H](CNc1cccc(-c2occc2C(=O)O)c1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2007.05.069
44441227 147505 0 None -7 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 415 9 4 6 3.8 C[C@H](CNc1cccc(-c2nc(C(=O)O)co2)c1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2007.05.069
CHEMBL393469 147505 0 None -7 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 415 9 4 6 3.8 C[C@H](CNc1cccc(-c2nc(C(=O)O)co2)c1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2007.05.069
929341 26810 8 None - 1 Human 5.9 pEC50 = 5.9 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 307 3 0 4 4.5 N#Cc1cc(-c2ccccc2)nc(Oc2ccc(Cl)cc2)n1 nan
CHEMBL1364979 26810 8 None - 1 Human 5.9 pEC50 = 5.9 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 307 3 0 4 4.5 N#Cc1cc(-c2ccccc2)nc(Oc2ccc(Cl)cc2)n1 nan
1025603 28216 11 None - 1 Human 5.9 pEC50 = 5.9 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 430 8 1 4 3.4 CN(Cc1ccccc1)S(=O)(=O)c1ccc(NS(=O)(=O)Cc2ccccc2)cc1 nan
CHEMBL1375364 28216 11 None - 1 Human 5.9 pEC50 = 5.9 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 430 8 1 4 3.4 CN(Cc1ccccc1)S(=O)(=O)c1ccc(NS(=O)(=O)Cc2ccccc2)cc1 nan
9512 3566 35 None -316 3 Human 5.9 pEC50 = 5.9 Functional
Activity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 410 9 4 4 4.4 Clc1cccc(c1)[C@H](CNCCNc1cccc(c1)c1cccc(c1)C(=O)O)O 10.1021/jm0509445
9887812 3566 35 None -316 3 Human 5.9 pEC50 = 5.9 Functional
Activity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 410 9 4 4 4.4 Clc1cccc(c1)[C@H](CNCCNc1cccc(c1)c1cccc(c1)C(=O)O)O 10.1021/jm0509445
CHEMBL208427 3566 35 None -316 3 Human 5.9 pEC50 = 5.9 Functional
Activity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 410 9 4 4 4.4 Clc1cccc(c1)[C@H](CNCCNc1cccc(c1)c1cccc(c1)C(=O)O)O 10.1021/jm0509445
DB06190 3566 35 None -316 3 Human 5.9 pEC50 = 5.9 Functional
Activity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 410 9 4 4 4.4 Clc1cccc(c1)[C@H](CNCCNc1cccc(c1)c1cccc(c1)C(=O)O)O 10.1021/jm0509445
90644148 111742 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 474 10 4 6 3.9 O=C(c1ccccc1)C1CCN(c2ccc(CCNCC(O)c3ccc(O)c(CO)c3)cc2)CC1 10.1016/j.bmcl.2014.04.069
CHEMBL3290977 111742 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 474 10 4 6 3.9 O=C(c1ccccc1)C1CCN(c2ccc(CCNCC(O)c3ccc(O)c(CO)c3)cc2)CC1 10.1016/j.bmcl.2014.04.069
16013947 21470 6 None - 1 Human 6.9 pEC50 = 6.9 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 442 6 1 8 1.9 CC(=O)Nc1ccc(S(=O)(=O)N2CCC(Oc3ccc(-n4cnnn4)cc3)CC2)cc1 nan
CHEMBL1318405 21470 6 None - 1 Human 6.9 pEC50 = 6.9 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 442 6 1 8 1.9 CC(=O)Nc1ccc(S(=O)(=O)N2CCC(Oc3ccc(-n4cnnn4)cc3)CC2)cc1 nan
2475524 23307 7 None - 1 Human 5.9 pEC50 = 5.9 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 332 4 0 5 4.4 CN(Cc1cccs1)c1nc(-c2cccnc2)nc2ccccc12 nan
CHEMBL1333885 23307 7 None - 1 Human 5.9 pEC50 = 5.9 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 332 4 0 5 4.4 CN(Cc1cccs1)c1nc(-c2cccnc2)nc2ccccc12 nan
1499 2052 43 None -72 36 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human beta2 adrenoceptor expressed in DU145 cells assessed as increase in cAMP accumulationAgonist activity at recombinant human beta2 adrenoceptor expressed in DU145 cells assessed as increase in cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2011.11.054
3779 2052 43 None -72 36 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human beta2 adrenoceptor expressed in DU145 cells assessed as increase in cAMP accumulationAgonist activity at recombinant human beta2 adrenoceptor expressed in DU145 cells assessed as increase in cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2011.11.054
536 2052 43 None -72 36 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human beta2 adrenoceptor expressed in DU145 cells assessed as increase in cAMP accumulationAgonist activity at recombinant human beta2 adrenoceptor expressed in DU145 cells assessed as increase in cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2011.11.054
CHEMBL434 2052 43 None -72 36 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human beta2 adrenoceptor expressed in DU145 cells assessed as increase in cAMP accumulationAgonist activity at recombinant human beta2 adrenoceptor expressed in DU145 cells assessed as increase in cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2011.11.054
DB01064 2052 43 None -72 36 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human beta2 adrenoceptor expressed in DU145 cells assessed as increase in cAMP accumulationAgonist activity at recombinant human beta2 adrenoceptor expressed in DU145 cells assessed as increase in cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2011.11.054
90666103 108833 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP productionAgonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP production
ChEMBL 682 18 6 9 6.2 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3cccc(O)c3)CC2)ccc1O 10.1039/C1MD00140J
CHEMBL3219033 108833 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP productionAgonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP production
ChEMBL 682 18 6 9 6.2 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3cccc(O)c3)CC2)ccc1O 10.1039/C1MD00140J
24876564 61437 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as stimulation of intracellular cAMP production after 30 mins of washing by wash-off assayAgonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as stimulation of intracellular cAMP production after 30 mins of washing by wash-off assay
ChEMBL 668 20 5 7 7.5 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCCCOc2ccc(CCNC[C@H](O)c3ccc(O)c(CO)c3)cc2)ccc1O)C(C)C 10.1016/j.bmcl.2010.10.132
CHEMBL1773074 61437 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as stimulation of intracellular cAMP production after 30 mins of washing by wash-off assayAgonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as stimulation of intracellular cAMP production after 30 mins of washing by wash-off assay
ChEMBL 668 20 5 7 7.5 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCCCOc2ccc(CCNC[C@H](O)c3ccc(O)c(CO)c3)cc2)ccc1O)C(C)C 10.1016/j.bmcl.2010.10.132
24791478 30363 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 420 8 1 7 2.7 COCCc1ncc(CN2CCC(C(=O)Nc3ccc(-n4cccn4)cc3)CC2)cn1 nan
CHEMBL1393806 30363 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 420 8 1 7 2.7 COCCc1ncc(CN2CCC(C(=O)Nc3ccc(-n4cccn4)cc3)CC2)cn1 nan
76315638 84878 0 None -23 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at Homo sapiens (human) beta2 adrenoreceptorAgonist activity at Homo sapiens (human) beta2 adrenoreceptor
ChEMBL 543 11 4 7 3.6 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1ccc(S(=O)(=O)Nc2ccccc2)cc1 10.1007/s00044-009-9257-x
CHEMBL2260986 84878 0 None -23 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at Homo sapiens (human) beta2 adrenoreceptorAgonist activity at Homo sapiens (human) beta2 adrenoreceptor
ChEMBL 543 11 4 7 3.6 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1ccc(S(=O)(=O)Nc2ccccc2)cc1 10.1007/s00044-009-9257-x
6916441 98855 1 None -158 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at Homo sapiens (human) beta2 adrenoreceptorAgonist activity at Homo sapiens (human) beta2 adrenoreceptor
ChEMBL 402 9 4 4 3.5 CC(Cc1c[nH]c2c(OCC(=O)O)cccc12)NC[C@H](O)c1cccc(Cl)c1 10.1007/s00044-009-9257-x
CHEMBL282190 98855 1 None -158 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at Homo sapiens (human) beta2 adrenoreceptorAgonist activity at Homo sapiens (human) beta2 adrenoreceptor
ChEMBL 402 9 4 4 3.5 CC(Cc1c[nH]c2c(OCC(=O)O)cccc12)NC[C@H](O)c1cccc(Cl)c1 10.1007/s00044-009-9257-x
12582 935 40 None 9 4 Guinea pig 7.9 pEC50 = 7.9 Functional
Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as relaxation of carbachol-induced tissue contractionAgonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as relaxation of carbachol-induced tissue contraction
ChEMBL 276 3 3 3 3.0 CC(C)(C)NCC(C1=CC(=C(C(=C1)Cl)N)Cl)O 10.1021/jm801211c
2783 935 40 None 9 4 Guinea pig 7.9 pEC50 = 7.9 Functional
Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as relaxation of carbachol-induced tissue contractionAgonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as relaxation of carbachol-induced tissue contraction
ChEMBL 276 3 3 3 3.0 CC(C)(C)NCC(C1=CC(=C(C(=C1)Cl)N)Cl)O 10.1021/jm801211c
CHEMBL49080 935 40 None 9 4 Guinea pig 7.9 pEC50 = 7.9 Functional
Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as relaxation of carbachol-induced tissue contractionAgonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as relaxation of carbachol-induced tissue contraction
ChEMBL 276 3 3 3 3.0 CC(C)(C)NCC(C1=CC(=C(C(=C1)Cl)N)Cl)O 10.1021/jm801211c
DB01407 935 40 None 9 4 Guinea pig 7.9 pEC50 = 7.9 Functional
Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as relaxation of carbachol-induced tissue contractionAgonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as relaxation of carbachol-induced tissue contraction
ChEMBL 276 3 3 3 3.0 CC(C)(C)NCC(C1=CC(=C(C(=C1)Cl)N)Cl)O 10.1021/jm801211c
9874175 58215 1 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP productionAgonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP production
ChEMBL 640 16 5 7 7.0 O=C(Nc1ccccc1-c1ccccc1)OC1CCN(CCCCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1039/C1MD00140J
CHEMBL1683934 58215 1 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP productionAgonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP production
ChEMBL 640 16 5 7 7.0 O=C(Nc1ccccc1-c1ccccc1)OC1CCN(CCCCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1039/C1MD00140J
90666123 108856 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP productionAgonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP production
ChEMBL 752 16 6 10 6.1 CS(=O)(=O)Nc1cc([C@@H](O)CNCCc2ccc(OCCCN3CCC(OC(=O)Nc4ccccc4-c4ccc(O)c(Cl)c4)CC3)cc2)ccc1O 10.1039/C1MD00140J
CHEMBL3219056 108856 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP productionAgonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP production
ChEMBL 752 16 6 10 6.1 CS(=O)(=O)Nc1cc([C@@H](O)CNCCc2ccc(OCCCN3CCC(OC(=O)Nc4ccccc4-c4ccc(O)c(Cl)c4)CC3)cc2)ccc1O 10.1039/C1MD00140J
54583100 61471 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as stimulation of intracellular cAMP production after 30 mins of washing by wash-off assayAgonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as stimulation of intracellular cAMP production after 30 mins of washing by wash-off assay
ChEMBL 731 21 5 8 7.4 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCCCOc2ccc(CCNC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)cc2)ccc1O)C(C)C 10.1016/j.bmcl.2010.10.132
CHEMBL1773264 61471 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as stimulation of intracellular cAMP production after 30 mins of washing by wash-off assayAgonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as stimulation of intracellular cAMP production after 30 mins of washing by wash-off assay
ChEMBL 731 21 5 8 7.4 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCCCOc2ccc(CCNC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)cc2)ccc1O)C(C)C 10.1016/j.bmcl.2010.10.132
44554514 123456 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as stumulation of intracellular cAMP productionAgonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as stumulation of intracellular cAMP production
ChEMBL 692 18 5 9 5.9 O=c1ccc2c([C@@H](O)CNCCCCCCCCCN3CCC(Cn4cnc(C(O)(c5ccccc5)c5ccccc5)n4)CC3)ccc(O)c2[nH]1 10.1016/j.bmcl.2015.10.008
CHEMBL3629356 123456 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as stumulation of intracellular cAMP productionAgonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as stumulation of intracellular cAMP production
ChEMBL 692 18 5 9 5.9 O=c1ccc2c([C@@H](O)CNCCCCCCCCCN3CCC(Cn4cnc(C(O)(c5ccccc5)c5ccccc5)n4)CC3)ccc(O)c2[nH]1 10.1016/j.bmcl.2015.10.008
5493324 98432 18 None -416 3 Human 7.9 pEC50 = 7.9 Functional
Agonistic activity against human Beta-2 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonistic activity against human Beta-2 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 402 9 4 4 3.5 C[C@H](Cc1c[nH]c2c(OCC(=O)O)cccc12)NC[C@H](O)c1cccc(Cl)c1 10.1016/s0960-894x(03)00073-8
CHEMBL279260 98432 18 None -416 3 Human 7.9 pEC50 = 7.9 Functional
Agonistic activity against human Beta-2 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonistic activity against human Beta-2 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 402 9 4 4 3.5 C[C@H](Cc1c[nH]c2c(OCC(=O)O)cccc12)NC[C@H](O)c1cccc(Cl)c1 10.1016/s0960-894x(03)00073-8
11785699 64494 0 None -12 2 Human 7.9 pEC50 = 7.9 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-2 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-2 adrenergic receptor
ChEMBL 519 12 4 6 4.9 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(NC/C=C/c2ccccc2)c1 10.1016/j.bmcl.2004.12.033
CHEMBL182018 64494 0 None -12 2 Human 7.9 pEC50 = 7.9 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-2 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-2 adrenergic receptor
ChEMBL 519 12 4 6 4.9 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(NC/C=C/c2ccccc2)c1 10.1016/j.bmcl.2004.12.033
44396798 168815 0 None -27 3 Human 7.9 pEC50 = 7.9 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptor
ChEMBL 542 10 5 7 3.2 C[C@H](Cc1c[nH]c2c(S(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccc(N)c2)c1 10.1016/j.bmcl.2004.09.054
CHEMBL442225 168815 0 None -27 3 Human 7.9 pEC50 = 7.9 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptor
ChEMBL 542 10 5 7 3.2 C[C@H](Cc1c[nH]c2c(S(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccc(N)c2)c1 10.1016/j.bmcl.2004.09.054
1608445 23933 10 None - 1 Human 7.9 pEC50 = 7.9 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 396 4 2 8 3.8 CC1(C)Cc2c(c(-c3ccco3)nc3sc4c(NCCO)ncnc4c23)CO1 nan
CHEMBL1339094 23933 10 None - 1 Human 7.9 pEC50 = 7.9 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 396 4 2 8 3.8 CC1(C)Cc2c(c(-c3ccco3)nc3sc4c(NCCO)ncnc4c23)CO1 nan
45483846 195126 0 None 1 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 412 6 4 5 3.7 CC(C)(Cc1ccc(C(C)(C)C)cc1)NCC(O)c1ccc(O)c2c1OCC(=O)N2 10.1016/j.bmcl.2009.10.013
CHEMBL565685 195126 0 None 1 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 412 6 4 5 3.7 CC(C)(Cc1ccc(C(C)(C)C)cc1)NCC(O)c1ccc(O)c2c1OCC(=O)N2 10.1016/j.bmcl.2009.10.013
44428083 92115 0 None 4 2 Guinea pig 6.9 pEC50 = 6.9 Functional
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-oneAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-one
ChEMBL 444 10 5 9 0.7 CC(Cc1ccc(OCc2no[n+]([O-])c2C(N)=O)cc1)NCC(O)c1cc(O)cc(O)c1 10.1021/jm0704595
CHEMBL243266 92115 0 None 4 2 Guinea pig 6.9 pEC50 = 6.9 Functional
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-oneAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-one
ChEMBL 444 10 5 9 0.7 CC(Cc1ccc(OCc2no[n+]([O-])c2C(N)=O)cc1)NCC(O)c1cc(O)cc(O)c1 10.1021/jm0704595
559926 96546 5 None -27 2 Guinea pig 6.9 pEC50 = 6.9 Functional
Agonistic activity (beta2- adrenergic) for the percent maximal relaxation of isolated guinea pig tracheaAgonistic activity (beta2- adrenergic) for the percent maximal relaxation of isolated guinea pig trachea
ChEMBL 255 5 4 5 1.2 CC(C)(C)NCC(O)COc1ccc(O)c(O)c1 10.1021/jm00107a027
CHEMBL266619 96546 5 None -27 2 Guinea pig 6.9 pEC50 = 6.9 Functional
Agonistic activity (beta2- adrenergic) for the percent maximal relaxation of isolated guinea pig tracheaAgonistic activity (beta2- adrenergic) for the percent maximal relaxation of isolated guinea pig trachea
ChEMBL 255 5 4 5 1.2 CC(C)(C)NCC(O)COc1ccc(O)c(O)c1 10.1021/jm00107a027
44428086 149535 0 None 7 2 Guinea pig 5.9 pEC50 = 5.9 Functional
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contractionAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction
ChEMBL 415 9 4 8 1.9 Cc1c(COc2ccc(CC(C)NCC(O)c3cc(O)cc(O)c3)cc2)no[n+]1[O-] 10.1021/jm0704595
CHEMBL395082 149535 0 None 7 2 Guinea pig 5.9 pEC50 = 5.9 Functional
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contractionAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction
ChEMBL 415 9 4 8 1.9 Cc1c(COc2ccc(CC(C)NCC(O)c3cc(O)cc(O)c3)cc2)no[n+]1[O-] 10.1021/jm0704595
102335359 121021 0 None - 1 Rat 5.9 pEC50 = 5.9 Functional
Agonist activity at beta2 adrenergic receptor in rat L6 cell lysate assessed as increase in intracellular 2-deoxyglucose uptake preincubated for 4 hrs followed by 2-deoxyglucose addition measured after 20 mins by fluorescence-based enzymatic assay relative to controlAgonist activity at beta2 adrenergic receptor in rat L6 cell lysate assessed as increase in intracellular 2-deoxyglucose uptake preincubated for 4 hrs followed by 2-deoxyglucose addition measured after 20 mins by fluorescence-based enzymatic assay relative to control
ChEMBL 433 5 7 9 -0.3 OC[C@H]1O[C@@H](Oc2ccc(C[C@@H]3NCCc4cc(O)c(O)cc43)cc2)[C@H](O)[C@@H](O)[C@@H]1O 10.1016/j.bmc.2017.10.011
CHEMBL3585932 121021 0 None - 1 Rat 5.9 pEC50 = 5.9 Functional
Agonist activity at beta2 adrenergic receptor in rat L6 cell lysate assessed as increase in intracellular 2-deoxyglucose uptake preincubated for 4 hrs followed by 2-deoxyglucose addition measured after 20 mins by fluorescence-based enzymatic assay relative to controlAgonist activity at beta2 adrenergic receptor in rat L6 cell lysate assessed as increase in intracellular 2-deoxyglucose uptake preincubated for 4 hrs followed by 2-deoxyglucose addition measured after 20 mins by fluorescence-based enzymatic assay relative to control
ChEMBL 433 5 7 9 -0.3 OC[C@H]1O[C@@H](Oc2ccc(C[C@@H]3NCCc4cc(O)c(O)cc43)cc2)[C@H](O)[C@@H](O)[C@@H]1O 10.1016/j.bmc.2017.10.011
9896817 102399 0 None -44 3 Human 5.9 pEC50 = 5.9 Functional
Compound was evaluated for its inhibitory activity against human beta-2 adrenergic receptor (AR)Compound was evaluated for its inhibitory activity against human beta-2 adrenergic receptor (AR)
ChEMBL 628 12 6 6 6.7 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2cccc(-c3ccc(CC4NCCc5cc(O)c(O)cc54)cc3)c2)cc1 10.1016/s0960-894x(00)00459-5
CHEMBL305891 102399 0 None -44 3 Human 5.9 pEC50 = 5.9 Functional
Compound was evaluated for its inhibitory activity against human beta-2 adrenergic receptor (AR)Compound was evaluated for its inhibitory activity against human beta-2 adrenergic receptor (AR)
ChEMBL 628 12 6 6 6.7 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2cccc(-c3ccc(CC4NCCc5cc(O)c(O)cc54)cc3)c2)cc1 10.1016/s0960-894x(00)00459-5
24180436 92772 0 None 1 2 Rat 5.9 pEC50 = 5.9 Functional
Vasodilating activity against phenylephrine-induced contraction in rat thoracic aorta in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-oneVasodilating activity against phenylephrine-induced contraction in rat thoracic aorta in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-one
ChEMBL 527 10 4 10 2.6 CC(Cc1ccc(Oc2no[n+]([O-])c2S(=O)(=O)c2ccccc2)cc1)NCC(O)c1cc(O)cc(O)c1 10.1021/jm0704595
CHEMBL244687 92772 0 None 1 2 Rat 5.9 pEC50 = 5.9 Functional
Vasodilating activity against phenylephrine-induced contraction in rat thoracic aorta in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-oneVasodilating activity against phenylephrine-induced contraction in rat thoracic aorta in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-one
ChEMBL 527 10 4 10 2.6 CC(Cc1ccc(Oc2no[n+]([O-])c2S(=O)(=O)c2ccccc2)cc1)NCC(O)c1cc(O)cc(O)c1 10.1021/jm0704595
45483838 195247 0 None 14 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 383 7 4 4 3.5 CC(C)(Cc1cccc(C(F)(F)F)c1)NCC(O)c1ccc(O)c(CO)c1 10.1016/j.bmcl.2009.10.013
CHEMBL566352 195247 0 None 14 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 383 7 4 4 3.5 CC(C)(Cc1cccc(C(F)(F)F)c1)NCC(O)c1ccc(O)c(CO)c1 10.1016/j.bmcl.2009.10.013
659802 26932 10 None - 1 Human 5.9 pEC50 = 5.9 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 425 8 2 7 2.4 CCCCCCN1C(=O)NC(=O)/C(=C\Nc2c(C)n(C)n(-c3ccccc3)c2=O)C1=O nan
CHEMBL1365995 26932 10 None - 1 Human 5.9 pEC50 = 5.9 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 425 8 2 7 2.4 CCCCCCN1C(=O)NC(=O)/C(=C\Nc2c(C)n(C)n(-c3ccccc3)c2=O)C1=O nan
1267856 45671 11 None 31 2 Human 5.9 pEC50 = 5.9 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset2. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset2. (Class of assay: confirmatory)
ChEMBL 351 6 1 7 2.2 CCOC(=O)c1ccc(NC(=O)Cn2nnc(-c3ccccc3)n2)cc1 nan
CHEMBL1532219 45671 11 None 31 2 Human 5.9 pEC50 = 5.9 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset2. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset2. (Class of assay: confirmatory)
ChEMBL 351 6 1 7 2.2 CCOC(=O)c1ccc(NC(=O)Cn2nnc(-c3ccccc3)n2)cc1 nan
645398 50636 9 None - 1 Human 6.9 pEC50 = 6.9 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 336 4 3 4 3.8 Cc1ccc(O)c(NC(=O)c2cccc(NC(=O)c3ccco3)c2)c1 nan
CHEMBL1577767 50636 9 None - 1 Human 6.9 pEC50 = 6.9 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 336 4 3 4 3.8 Cc1ccc(O)c(NC(=O)c2cccc(NC(=O)c3ccco3)c2)c1 nan
24891819 55148 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 481 9 1 6 6.9 COc1ccc(CSc2ccc(-c3nc4ccccn4c3NCc3ccccc3)cc2OC)cc1 nan
CHEMBL1406272 55148 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 481 9 1 6 6.9 COc1ccc(CSc2ccc(-c3nc4ccccn4c3NCc3ccccc3)cc2OC)cc1 nan
CHEMBL1619809 55148 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 481 9 1 6 6.9 COc1ccc(CSc2ccc(-c3nc4ccccn4c3NCc3ccccc3)cc2OC)cc1 nan
53379897 63300 0 None -151 2 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity beta2-adrenergic receptor in rat ventricular myocytes assessed as cell contraction following electrical stimulation by optical edge tracking method using photodiode arrayAgonist activity beta2-adrenergic receptor in rat ventricular myocytes assessed as cell contraction following electrical stimulation by optical edge tracking method using photodiode array
ChEMBL 337 6 4 4 3.5 C[C@H](Cc1ccc2ccccc2c1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2009.11.062
CHEMBL1800961 63300 0 None -151 2 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity beta2-adrenergic receptor in rat ventricular myocytes assessed as cell contraction following electrical stimulation by optical edge tracking method using photodiode arrayAgonist activity beta2-adrenergic receptor in rat ventricular myocytes assessed as cell contraction following electrical stimulation by optical edge tracking method using photodiode array
ChEMBL 337 6 4 4 3.5 C[C@H](Cc1ccc2ccccc2c1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2009.11.062
2231941 33969 8 None - 1 Human 6.9 pEC50 = 6.9 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 457 11 1 9 3.4 C=CCn1c(CCNC(=O)c2cccs2)nnc1SCC(=O)c1cccc([N+](=O)[O-])c1 nan
CHEMBL1426242 33969 8 None - 1 Human 6.9 pEC50 = 6.9 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 457 11 1 9 3.4 C=CCn1c(CCNC(=O)c2cccs2)nnc1SCC(=O)c1cccc([N+](=O)[O-])c1 nan
1084214 45263 9 None - 1 Human 5.9 pEC50 = 5.9 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset2. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset2. (Class of assay: confirmatory)
ChEMBL 432 8 1 6 2.7 CCOC(=O)c1ccc(NC(=O)COc2ccc(S(=O)(=O)N3CCCC3)cc2)cc1 nan
CHEMBL1528594 45263 9 None - 1 Human 5.9 pEC50 = 5.9 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset2. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset2. (Class of assay: confirmatory)
ChEMBL 432 8 1 6 2.7 CCOC(=O)c1ccc(NC(=O)COc2ccc(S(=O)(=O)N3CCCC3)cc2)cc1 nan
70684522 76409 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation countingAgonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting
ChEMBL 343 4 3 4 1.4 CC(C)(C)NC[C@H](O)c1ccc2c(c1)C[OH+][B-](O)(c1ccccc1)O2 10.1016/j.bmc.2011.11.054
CHEMBL2068577 76409 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation countingAgonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting
ChEMBL 343 4 3 4 1.4 CC(C)(C)NC[C@H](O)c1ccc2c(c1)C[OH+][B-](O)(c1ccccc1)O2 10.1016/j.bmc.2011.11.054
70684522 76409 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation countingAgonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting
ChEMBL 343 4 3 4 1.4 CC(C)(C)NC[C@H](O)c1ccc2c(c1)C[OH+][B-](O)(c1ccccc1)O2 10.1016/j.bmc.2011.11.054
CHEMBL2068577 76409 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation countingAgonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting
ChEMBL 343 4 3 4 1.4 CC(C)(C)NC[C@H](O)c1ccc2c(c1)C[OH+][B-](O)(c1ccccc1)O2 10.1016/j.bmc.2011.11.054
1028 287 69 None -15 16 Human 5.9 pEC50 = 5.9 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O nan
139148732 287 69 None -15 16 Human 5.9 pEC50 = 5.9 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O nan
479 287 69 None -15 16 Human 5.9 pEC50 = 5.9 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O nan
5816 287 69 None -15 16 Human 5.9 pEC50 = 5.9 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O nan
CHEMBL679 287 69 None -15 16 Human 5.9 pEC50 = 5.9 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O nan
DB00668 287 69 None -15 16 Human 5.9 pEC50 = 5.9 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O nan
24794116 66740 1 None - 1 Human 5.9 pEC50 = 5.9 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 410 6 0 4 4.7 CSc1ccc(CN2CCC(Oc3ccc(C(=O)N4CCCC4)cc3)CC2)cc1 nan
CHEMBL1873201 66740 1 None - 1 Human 5.9 pEC50 = 5.9 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 410 6 0 4 4.7 CSc1ccc(CN2CCC(Oc3ccc(C(=O)N4CCCC4)cc3)CC2)cc1 nan
54757772 65644 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP productionAgonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP production
ChEMBL 675 16 5 9 6.0 O=c1ccc2c([C@@H](O)CNCCCCCCCCCN3CCC(Oc4nn(-c5c(O)cccc5F)c5c4CCCC5)CC3)ccc(O)c2[nH]1 10.1021/jm2007535
CHEMBL1836647 65644 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP productionAgonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP production
ChEMBL 675 16 5 9 6.0 O=c1ccc2c([C@@H](O)CNCCCCCCCCCN3CCC(Oc4nn(-c5c(O)cccc5F)c5c4CCCC5)CC3)ccc(O)c2[nH]1 10.1021/jm2007535
90666112 108843 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP productionAgonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP production
ChEMBL 730 18 6 9 7.2 Cc1ccc(-c2ccc(O)c(Cl)c2)c(NC(=O)OC2CCN(CCCCCCCCCNC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)CC2)c1 10.1039/C1MD00140J
CHEMBL3219044 108843 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP productionAgonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP production
ChEMBL 730 18 6 9 7.2 Cc1ccc(-c2ccc(O)c(Cl)c2)c(NC(=O)OC2CCN(CCCCCCCCCNC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)CC2)c1 10.1039/C1MD00140J
46221397 8600 0 None 1 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assayAgonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assay
ChEMBL 420 8 4 4 3.9 CCCc1cc2c(cc1CCC)CC(NC[C@H](O)c1ccc(O)c3[nH]c(=O)ccc13)C2 10.1021/jm100068m
CHEMBL1095778 8600 0 None 1 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assayAgonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assay
ChEMBL 420 8 4 4 3.9 CCCc1cc2c(cc1CCC)CC(NC[C@H](O)c1ccc(O)c3[nH]c(=O)ccc13)C2 10.1021/jm100068m
44609903 123459 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as stumulation of intracellular cAMP productionAgonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as stumulation of intracellular cAMP production
ChEMBL 698 18 5 9 6.4 O=c1ccc2c([C@@H](O)CNCCCCCCCCCN3CCC(Cn4cnc([C@](O)(c5ccccc5)C5CCCCC5)n4)CC3)ccc(O)c2[nH]1 10.1016/j.bmcl.2015.10.008
CHEMBL3629359 123459 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as stumulation of intracellular cAMP productionAgonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as stumulation of intracellular cAMP production
ChEMBL 698 18 5 9 6.4 O=c1ccc2c([C@@H](O)CNCCCCCCCCCN3CCC(Cn4cnc([C@](O)(c5ccccc5)C5CCCCC5)n4)CC3)ccc(O)c2[nH]1 10.1016/j.bmcl.2015.10.008
10054373 58217 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
ChEMBL 603 17 5 7 6.6 O=C(Nc1ccccc1-c1ccccc1)OC1CCN(CCCCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)CC1 10.1016/j.bmcl.2011.01.043
CHEMBL1683936 58217 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
ChEMBL 603 17 5 7 6.6 O=C(Nc1ccccc1-c1ccccc1)OC1CCN(CCCCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)CC1 10.1016/j.bmcl.2011.01.043
24180436 92772 0 None 1 2 Rat 7.9 pEC50 = 7.9 Functional
Vasodilating activity against phenylephrine-induced contractions in rat thoracic aortaVasodilating activity against phenylephrine-induced contractions in rat thoracic aorta
ChEMBL 527 10 4 10 2.6 CC(Cc1ccc(Oc2no[n+]([O-])c2S(=O)(=O)c2ccccc2)cc1)NCC(O)c1cc(O)cc(O)c1 10.1021/jm0704595
CHEMBL244687 92772 0 None 1 2 Rat 7.9 pEC50 = 7.9 Functional
Vasodilating activity against phenylephrine-induced contractions in rat thoracic aortaVasodilating activity against phenylephrine-induced contractions in rat thoracic aorta
ChEMBL 527 10 4 10 2.6 CC(Cc1ccc(Oc2no[n+]([O-])c2S(=O)(=O)c2ccccc2)cc1)NCC(O)c1cc(O)cc(O)c1 10.1021/jm0704595
46233013 199609 0 None 19 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 386 7 4 6 2.4 COc1cccc(CC(C)(C)NCC(O)c2cc(O)cc3c2OCC(=O)N3)c1 10.1016/j.bmcl.2009.12.087
CHEMBL604125 199609 0 None 19 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 386 7 4 6 2.4 COc1cccc(CC(C)(C)NCC(O)c2cc(O)cc3c2OCC(=O)N3)c1 10.1016/j.bmcl.2009.12.087
3145649 39219 9 None 177 2 Human 7.8 pEC50 = 7.8 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory)
ChEMBL 395 4 0 4 4.7 CC(Sc1nc(-c2ccccc2)cc(C(F)(F)F)n1)C(=O)N1CCCCC1 nan
CHEMBL1472233 39219 9 None 177 2 Human 7.8 pEC50 = 7.8 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory)
ChEMBL 395 4 0 4 4.7 CC(Sc1nc(-c2ccccc2)cc(C(F)(F)F)n1)C(=O)N1CCCCC1 nan
3145570 46721 5 None 1 2 Human 7.8 pEC50 = 7.8 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory)
ChEMBL 397 4 0 5 3.5 CC(Sc1nc(-c2ccccc2)cc(C(F)(F)F)n1)C(=O)N1CCOCC1 nan
CHEMBL1541608 46721 5 None 1 2 Human 7.8 pEC50 = 7.8 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory)
ChEMBL 397 4 0 5 3.5 CC(Sc1nc(-c2ccccc2)cc(C(F)(F)F)n1)C(=O)N1CCOCC1 nan
127047221 139387 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human beta2 receptor expressed in HEK293 cells cotransfected with Gqs5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositolAgonist activity at human beta2 receptor expressed in HEK293 cells cotransfected with Gqs5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositol
ChEMBL 319 8 4 6 1.8 COc1ccccc1OCCNC[C@@H](O)c1ccc(O)c(O)c1 10.1016/j.bmc.2016.04.028
CHEMBL3799593 139387 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human beta2 receptor expressed in HEK293 cells cotransfected with Gqs5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositolAgonist activity at human beta2 receptor expressed in HEK293 cells cotransfected with Gqs5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositol
ChEMBL 319 8 4 6 1.8 COc1ccccc1OCCNC[C@@H](O)c1ccc(O)c(O)c1 10.1016/j.bmc.2016.04.028
10722793 112835 0 None -114 3 Human 5.9 pEC50 = 5.9 Functional
In vitro functional efficacy in stimulating increase in cAMP in chinese hamster ovary (CHO) cells expressing the cloned human beta-2 receptor.In vitro functional efficacy in stimulating increase in cAMP in chinese hamster ovary (CHO) cells expressing the cloned human beta-2 receptor.
ChEMBL 640 12 3 8 6.4 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3ccc(OC(F)(F)F)cc3)cs2)cc1 10.1021/jm000286i
CHEMBL331744 112835 0 None -114 3 Human 5.9 pEC50 = 5.9 Functional
In vitro functional efficacy in stimulating increase in cAMP in chinese hamster ovary (CHO) cells expressing the cloned human beta-2 receptor.In vitro functional efficacy in stimulating increase in cAMP in chinese hamster ovary (CHO) cells expressing the cloned human beta-2 receptor.
ChEMBL 640 12 3 8 6.4 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3ccc(OC(F)(F)F)cc3)cs2)cc1 10.1021/jm000286i
2382050 36626 7 None - 1 Human 5.9 pEC50 = 5.9 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 487 9 1 7 3.3 O=C(CCc1ccc(S(=O)(=O)N2CCOCC2)cc1)Nc1nc(COc2ccccc2)cs1 nan
CHEMBL1450612 36626 7 None - 1 Human 5.9 pEC50 = 5.9 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 487 9 1 7 3.3 O=C(CCc1ccc(S(=O)(=O)N2CCOCC2)cc1)Nc1nc(COc2ccccc2)cs1 nan
24789191 39431 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 453 11 3 6 2.4 NC(=O)CC(NC(=O)c1ccccc1)c1ccc(NCCCN2CCCC2=O)c([N+](=O)[O-])c1 nan
CHEMBL1475105 39431 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 453 11 3 6 2.4 NC(=O)CC(NC(=O)c1ccccc1)c1ccc(NCCCN2CCCC2=O)c([N+](=O)[O-])c1 nan
44428083 92115 0 None -4 2 Rat 4.9 pEC50 = 4.9 Functional
Vasodilating activity against phenylephrine-induced contraction in rat thoracic aorta in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-oneVasodilating activity against phenylephrine-induced contraction in rat thoracic aorta in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-one
ChEMBL 444 10 5 9 0.7 CC(Cc1ccc(OCc2no[n+]([O-])c2C(N)=O)cc1)NCC(O)c1cc(O)cc(O)c1 10.1021/jm0704595
CHEMBL243266 92115 0 None -4 2 Rat 4.9 pEC50 = 4.9 Functional
Vasodilating activity against phenylephrine-induced contraction in rat thoracic aorta in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-oneVasodilating activity against phenylephrine-induced contraction in rat thoracic aorta in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-one
ChEMBL 444 10 5 9 0.7 CC(Cc1ccc(OCc2no[n+]([O-])c2C(N)=O)cc1)NCC(O)c1cc(O)cc(O)c1 10.1021/jm0704595
2340194 34407 6 None - 1 Human 5.9 pEC50 = 5.9 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 461 7 2 7 4.8 Cc1ccc(C(=O)OCC(=O)Nc2nc(-c3ccccc3)cs2)cc1NC(=O)c1ccco1 nan
CHEMBL1429919 34407 6 None - 1 Human 5.9 pEC50 = 5.9 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 461 7 2 7 4.8 Cc1ccc(C(=O)OCC(=O)Nc2nc(-c3ccccc3)cs2)cc1NC(=O)c1ccco1 nan
145984324 165275 0 None -25 3 Human 5.9 pEC50 = 5.9 Functional
Antagonist activity at human beta2 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta2 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 449 11 4 4 4.6 CCc1ccccc1OC[C@@H](O)CNCCc1ccc(NC(=S)Nc2ccccc2)cc1 10.1016/j.ejmech.2018.03.032
CHEMBL4248727 165275 0 None -25 3 Human 5.9 pEC50 = 5.9 Functional
Antagonist activity at human beta2 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta2 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 449 11 4 4 4.6 CCc1ccccc1OC[C@@H](O)CNCCc1ccc(NC(=S)Nc2ccccc2)cc1 10.1016/j.ejmech.2018.03.032
21977086 192354 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 323 4 3 4 2.5 N#Cc1cc(C(CO)NC2CCCC2)cc(Br)c1N 10.1021/acs.jmedchem.1c02006
CHEMBL5200823 192354 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 323 4 3 4 2.5 N#Cc1cc(C(CO)NC2CCCC2)cc(Br)c1N 10.1021/acs.jmedchem.1c02006
CHEMBL5222486 192354 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 323 4 3 4 2.5 N#Cc1cc(C(CO)NC2CCCC2)cc(Br)c1N 10.1021/acs.jmedchem.1c02006
655617 30174 3 None - 1 Human 6.8 pEC50 = 6.8 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 415 5 0 7 3.4 CC(=O)c1cccc(S(=O)(=O)N2CCCC(c3nc(-c4ccc(C)o4)no3)C2)c1 nan
CHEMBL1392252 30174 3 None - 1 Human 6.8 pEC50 = 6.8 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 415 5 0 7 3.4 CC(=O)c1cccc(S(=O)(=O)N2CCCC(c3nc(-c4ccc(C)o4)no3)C2)c1 nan
168282645 192276 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 386 6 3 3 4.6 CC(C)(Cc1ccccc1)NC(CO)c1cc(Cl)c(N)c(C(F)(F)F)c1 10.1021/acs.jmedchem.1c02006
CHEMBL5186002 192276 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 386 6 3 3 4.6 CC(C)(Cc1ccccc1)NC(CO)c1cc(Cl)c(N)c(C(F)(F)F)c1 10.1021/acs.jmedchem.1c02006
CHEMBL5222019 192276 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 386 6 3 3 4.6 CC(C)(Cc1ccccc1)NC(CO)c1cc(Cl)c(N)c(C(F)(F)F)c1 10.1021/acs.jmedchem.1c02006
123600 2275 0 None 1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation countingAgonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)[C@H](CNC(C)(C)C)O 10.1016/j.bmc.2011.11.054
1575 2275 0 None 1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation countingAgonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)[C@H](CNC(C)(C)C)O 10.1016/j.bmc.2011.11.054
9816 2275 0 None 1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation countingAgonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)[C@H](CNC(C)(C)C)O 10.1016/j.bmc.2011.11.054
CHEMBL1002 2275 0 None 1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation countingAgonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)[C@H](CNC(C)(C)C)O 10.1016/j.bmc.2011.11.054
DB13139 2275 0 None 1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation countingAgonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)[C@H](CNC(C)(C)C)O 10.1016/j.bmc.2011.11.054
123600 2275 0 None 1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation countingAgonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)[C@H](CNC(C)(C)C)O 10.1016/j.bmc.2011.11.054
1575 2275 0 None 1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation countingAgonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)[C@H](CNC(C)(C)C)O 10.1016/j.bmc.2011.11.054
9816 2275 0 None 1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation countingAgonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)[C@H](CNC(C)(C)C)O 10.1016/j.bmc.2011.11.054
CHEMBL1002 2275 0 None 1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation countingAgonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)[C@H](CNC(C)(C)C)O 10.1016/j.bmc.2011.11.054
DB13139 2275 0 None 1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation countingAgonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)[C@H](CNC(C)(C)C)O 10.1016/j.bmc.2011.11.054
4184788 24993 6 None - 1 Human 5.8 pEC50 = 5.8 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 452 3 0 4 4.5 Cc1c(C(=O)N2CCc3ccccc3C2)oc2ccc(S(=O)(=O)N3CCCCCC3)cc12 nan
CHEMBL1348147 24993 6 None - 1 Human 5.8 pEC50 = 5.8 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 452 3 0 4 4.5 Cc1c(C(=O)N2CCc3ccccc3C2)oc2ccc(S(=O)(=O)N3CCCCCC3)cc12 nan
54583092 61452 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as stimulation of intracellular cAMP production after 30 mins of washing by wash-off assayAgonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as stimulation of intracellular cAMP production after 30 mins of washing by wash-off assay
ChEMBL 695 19 6 7 7.0 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCCNC(=O)Cc2cccc(C[C@@H](C)NC[C@H](O)c3cc(O)cc(O)c3)c2)ccc1O)C(C)C 10.1016/j.bmcl.2010.10.132
CHEMBL1773198 61452 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as stimulation of intracellular cAMP production after 30 mins of washing by wash-off assayAgonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as stimulation of intracellular cAMP production after 30 mins of washing by wash-off assay
ChEMBL 695 19 6 7 7.0 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCCNC(=O)Cc2cccc(C[C@@H](C)NC[C@H](O)c3cc(O)cc(O)c3)c2)ccc1O)C(C)C 10.1016/j.bmcl.2010.10.132
1028 287 69 None -2 16 Guinea pig 7.8 pEC50 = 7.8 Functional
Effective dose for relaxation of guinea pig trachea.Effective dose for relaxation of guinea pig trachea.
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00019a001
139148732 287 69 None -2 16 Guinea pig 7.8 pEC50 = 7.8 Functional
Effective dose for relaxation of guinea pig trachea.Effective dose for relaxation of guinea pig trachea.
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00019a001
479 287 69 None -2 16 Guinea pig 7.8 pEC50 = 7.8 Functional
Effective dose for relaxation of guinea pig trachea.Effective dose for relaxation of guinea pig trachea.
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00019a001
5816 287 69 None -2 16 Guinea pig 7.8 pEC50 = 7.8 Functional
Effective dose for relaxation of guinea pig trachea.Effective dose for relaxation of guinea pig trachea.
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00019a001
CHEMBL679 287 69 None -2 16 Guinea pig 7.8 pEC50 = 7.8 Functional
Effective dose for relaxation of guinea pig trachea.Effective dose for relaxation of guinea pig trachea.
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00019a001
DB00668 287 69 None -2 16 Guinea pig 7.8 pEC50 = 7.8 Functional
Effective dose for relaxation of guinea pig trachea.Effective dose for relaxation of guinea pig trachea.
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00019a001
11625493 199018 0 None 12 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 400 8 4 6 2.8 CCOc1ccc(CC(C)(C)NCC(O)c2cc(O)cc3c2OCC(=O)N3)cc1 10.1016/j.bmcl.2009.12.087
CHEMBL600007 199018 0 None 12 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 400 8 4 6 2.8 CCOc1ccc(CC(C)(C)NCC(O)c2cc(O)cc3c2OCC(=O)N3)cc1 10.1016/j.bmcl.2009.12.087
1094286 50549 15 None - 1 Human 7.8 pEC50 = 7.8 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory)
ChEMBL 359 5 1 5 4.2 Cc1ccc(OCC(=O)Nc2ccc(-c3nc4ncccc4o3)cc2)cc1 nan
CHEMBL1577023 50549 15 None - 1 Human 7.8 pEC50 = 7.8 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory)
ChEMBL 359 5 1 5 4.2 Cc1ccc(OCC(=O)Nc2ccc(-c3nc4ncccc4o3)cc2)cc1 nan
319 1292 39 None -2 6 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2011.05.097
321 1292 39 None -2 6 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2011.05.097
444031 1292 39 None -2 6 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2011.05.097
784 1292 39 None -2 6 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2011.05.097
CHEMBL1346 1292 39 None -2 6 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2011.05.097
DB00496 1292 39 None -2 6 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2011.05.097
90655865 110761 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assayAgonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assay
ChEMBL 514 16 3 7 2.9 CN(C)CCCN(CCNCCc1ccc(O)c2[nH]c(=O)sc12)C(=O)CCOCCc1ccccc1 10.1021/ml4005232
CHEMBL3265162 110761 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assayAgonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assay
ChEMBL 514 16 3 7 2.9 CN(C)CCCN(CCNCCc1ccc(O)c2[nH]c(=O)sc12)C(=O)CCOCCc1ccccc1 10.1021/ml4005232
4183 1986 62 None 1 4 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O 10.1016/j.bmcl.2011.10.049
6918554 1986 62 None 1 4 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O 10.1016/j.bmcl.2011.10.049
7455 1986 62 None 1 4 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O 10.1016/j.bmcl.2011.10.049
CHEMBL1095777 1986 62 None 1 4 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O 10.1016/j.bmcl.2011.10.049
DB05039 1986 62 None 1 4 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O 10.1016/j.bmcl.2011.10.049
24900874 70025 0 None 8 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 417 11 5 7 1.9 COCCNCc1ccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)cc1 10.1016/j.bmcl.2011.10.049
CHEMBL1945293 70025 0 None 8 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 417 11 5 7 1.9 COCCNCc1ccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)cc1 10.1016/j.bmcl.2011.10.049
44312924 164263 0 None -39 3 Human 5.8 pEC50 = 5.8 Functional
Compound was evaluated for its inhibitory activity against human beta-2 adrenergic receptor (AR)Compound was evaluated for its inhibitory activity against human beta-2 adrenergic receptor (AR)
ChEMBL 421 6 3 6 4.2 COc1cc(-c2ccc(CC3NCCc4cc(O)c(O)cc43)cc2)cc(OC)c1OC 10.1016/s0960-894x(00)00459-5
CHEMBL421871 164263 0 None -39 3 Human 5.8 pEC50 = 5.8 Functional
Compound was evaluated for its inhibitory activity against human beta-2 adrenergic receptor (AR)Compound was evaluated for its inhibitory activity against human beta-2 adrenergic receptor (AR)
ChEMBL 421 6 3 6 4.2 COc1cc(-c2ccc(CC3NCCc4cc(O)c(O)cc43)cc2)cc(OC)c1OC 10.1016/s0960-894x(00)00459-5
10651147 110181 0 None -380 3 Human 5.8 pEC50 = 5.8 Functional
Increased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 2 adrenergic receptorsIncreased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 2 adrenergic receptors
ChEMBL 596 12 6 8 2.5 CS(=O)(=O)Nc1cc([C@@H](O)CNC2CCN(c3ccc(C(=O)N[C@@H](Cc4ccccc4)C(=O)O)cc3)CC2)ccc1O 10.1021/jm000544b
CHEMBL32599 110181 0 None -380 3 Human 5.8 pEC50 = 5.8 Functional
Increased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 2 adrenergic receptorsIncreased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 2 adrenergic receptors
ChEMBL 596 12 6 8 2.5 CS(=O)(=O)Nc1cc([C@@H](O)CNC2CCN(c3ccc(C(=O)N[C@@H](Cc4ccccc4)C(=O)O)cc3)CC2)ccc1O 10.1021/jm000544b
3986625 42924 4 None - 1 Human 5.8 pEC50 = 5.8 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory)
ChEMBL 344 4 1 3 3.7 Cc1ccc(NC(=O)C(c2ccc(Cl)cc2)N2CCOCC2)cc1 nan
CHEMBL1505690 42924 4 None - 1 Human 5.8 pEC50 = 5.8 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory)
ChEMBL 344 4 1 3 3.7 Cc1ccc(NC(=O)C(c2ccc(Cl)cc2)N2CCOCC2)cc1 nan
5307895 49843 7 None 9 2 Human 5.8 pEC50 = 5.8 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory)
ChEMBL 441 8 1 8 2.9 COc1ccc(OC)c(CCNC(=O)C2CCN(c3nnc(-n4cccc4)s3)CC2)c1 nan
CHEMBL1570251 49843 7 None 9 2 Human 5.8 pEC50 = 5.8 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory)
ChEMBL 441 8 1 8 2.9 COc1ccc(OC)c(CCNC(=O)C2CCN(c3nnc(-n4cccc4)s3)CC2)c1 nan
168273723 192195 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 304 6 3 3 2.6 CCCCNC(CO)c1cc(F)c(N)c(Br)c1 10.1021/acs.jmedchem.1c02006
CHEMBL5178340 192195 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 304 6 3 3 2.6 CCCCNC(CO)c1cc(F)c(N)c(Br)c1 10.1021/acs.jmedchem.1c02006
CHEMBL5221450 192195 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 304 6 3 3 2.6 CCCCNC(CO)c1cc(F)c(N)c(Br)c1 10.1021/acs.jmedchem.1c02006
1104203 44603 12 None - 1 Human 6.8 pEC50 = 6.8 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory)
ChEMBL 350 4 1 7 3.6 O=C(Nc1ccc(-c2nc3ncccc3o2)cc1)c1ccc([N+](=O)[O-])o1 nan
CHEMBL1522618 44603 12 None - 1 Human 6.8 pEC50 = 6.8 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory)
ChEMBL 350 4 1 7 3.6 O=C(Nc1ccc(-c2nc3ncccc3o2)cc1)c1ccc([N+](=O)[O-])o1 nan
1266768 33785 11 None - 1 Human 6.8 pEC50 = 6.8 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 365 6 1 7 2.5 CCOC(=O)c1ccc(NC(=O)Cn2nnc(-c3ccc(C)cc3)n2)cc1 nan
CHEMBL1424678 33785 11 None - 1 Human 6.8 pEC50 = 6.8 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 365 6 1 7 2.5 CCOC(=O)c1ccc(NC(=O)Cn2nnc(-c3ccc(C)cc3)n2)cc1 nan
3301343 59415 10 None - 1 Human 6.8 pEC50 = 6.8 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 414 4 2 9 2.3 CC1(C)Cc2c(c(N3CCOCC3)nc3sc4c(NCCN)ncnc4c23)CO1 nan
CHEMBL1724644 59415 10 None - 1 Human 6.8 pEC50 = 6.8 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 414 4 2 9 2.3 CC1(C)Cc2c(c(N3CCOCC3)nc3sc4c(NCCN)ncnc4c23)CO1 nan
44441229 93303 0 None -199 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 431 9 4 6 4.3 C[C@H](CNc1cccc(-c2nc(C(=O)O)cs2)c1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2007.05.069
CHEMBL247315 93303 0 None -199 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 431 9 4 6 4.3 C[C@H](CNc1cccc(-c2nc(C(=O)O)cs2)c1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2007.05.069
57395241 70139 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 448 11 4 6 3.4 O=c1[nH]c2c(O)ccc(CCNCCc3ccc(CNCCc4ccccn4)cc3)c2s1 10.1016/j.bmcl.2011.10.049
CHEMBL1946763 70139 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 448 11 4 6 3.4 O=c1[nH]c2c(O)ccc(CCNCCc3ccc(CNCCc4ccccn4)cc3)c2s1 10.1016/j.bmcl.2011.10.049
57391792 70140 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 523 10 3 6 5.0 O=c1[nH]c2c(O)ccc(CCNCCc3ccc(CN4CC[C@@H](Oc5ccc(Cl)cc5)C4)cc3)c2s1 10.1016/j.bmcl.2011.10.049
CHEMBL1946764 70140 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 523 10 3 6 5.0 O=c1[nH]c2c(O)ccc(CCNCCc3ccc(CN4CC[C@@H](Oc5ccc(Cl)cc5)C4)cc3)c2s1 10.1016/j.bmcl.2011.10.049
90644144 111738 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 442 10 5 5 4.5 OCc1cc(C(O)CNCCc2ccc(NCc3ccc4ccccc4c3)cc2)ccc1O 10.1016/j.bmcl.2014.04.069
CHEMBL3290973 111738 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 442 10 5 5 4.5 OCc1cc(C(O)CNCCc2ccc(NCc3ccc4ccccc4c3)cc2)ccc1O 10.1016/j.bmcl.2014.04.069
11495581 76954 0 None -50 3 Human 5.8 pEC50 = 5.8 Functional
Activity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 425 9 4 5 4.2 C[C@H](CNc1cccc(-c2ncccc2C(=O)O)c1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0509445
CHEMBL208328 76954 0 None -50 3 Human 5.8 pEC50 = 5.8 Functional
Activity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 425 9 4 5 4.2 C[C@H](CNc1cccc(-c2ncccc2C(=O)O)c1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0509445
11546349 140789 0 None -50 3 Human 5.8 pEC50 = 5.8 Functional
Activity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 424 9 4 4 4.8 C[C@H](CNc1cccc(-c2ccc(C(=O)O)cc2)c1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0509445
CHEMBL383511 140789 0 None -50 3 Human 5.8 pEC50 = 5.8 Functional
Activity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 424 9 4 4 4.8 C[C@H](CNc1cccc(-c2ccc(C(=O)O)cc2)c1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0509445
90644143 111737 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 460 10 5 5 4.7 OCc1cc(C(O)CNCCc2ccc(NCc3ccc(Cl)c(Cl)c3)cc2)ccc1O 10.1016/j.bmcl.2014.04.069
CHEMBL3290972 111737 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 460 10 5 5 4.7 OCc1cc(C(O)CNCCc2ccc(NCc3ccc(Cl)c(Cl)c3)cc2)ccc1O 10.1016/j.bmcl.2014.04.069
90644147 111741 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 488 12 4 5 5.0 OCc1cc(C(O)CNCCc2ccc(N3CCC(CCCc4ccccc4)CC3)cc2)ccc1O 10.1016/j.bmcl.2014.04.069
CHEMBL3290976 111741 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 488 12 4 5 5.0 OCc1cc(C(O)CNCCc2ccc(N3CCC(CCCc4ccccc4)CC3)cc2)ccc1O 10.1016/j.bmcl.2014.04.069
145984042 165112 0 None -3467 3 Human 4.8 pEC50 = 4.8 Functional
Antagonist activity at human beta2 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta2 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 475 13 4 5 3.1 CC(=O)NCc1cccc(OC[C@@H](O)CNCCc2ccc(NC(=O)Cc3ccccc3)cc2)c1 10.1016/j.ejmech.2018.03.032
CHEMBL4244929 165112 0 None -3467 3 Human 4.8 pEC50 = 4.8 Functional
Antagonist activity at human beta2 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta2 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 475 13 4 5 3.1 CC(=O)NCc1cccc(OC[C@@H](O)CNCCc2ccc(NC(=O)Cc3ccccc3)cc2)c1 10.1016/j.ejmech.2018.03.032
53380558 63302 2 None -4 2 Rat 7.8 pEC50 = 7.8 Functional
Agonist activity beta2-adrenergic receptor in rat ventricular myocytes assessed as cell contraction following electrical stimulation by optical edge tracking method using photodiode arrayAgonist activity beta2-adrenergic receptor in rat ventricular myocytes assessed as cell contraction following electrical stimulation by optical edge tracking method using photodiode array
ChEMBL 367 7 4 5 3.5 COc1ccc(C[C@@H](C)NC[C@H](O)c2cc(O)cc(O)c2)c2ccccc12 10.1016/j.bmc.2009.11.062
CHEMBL1800963 63302 2 None -4 2 Rat 7.8 pEC50 = 7.8 Functional
Agonist activity beta2-adrenergic receptor in rat ventricular myocytes assessed as cell contraction following electrical stimulation by optical edge tracking method using photodiode arrayAgonist activity beta2-adrenergic receptor in rat ventricular myocytes assessed as cell contraction following electrical stimulation by optical edge tracking method using photodiode array
ChEMBL 367 7 4 5 3.5 COc1ccc(C[C@@H](C)NC[C@H](O)c2cc(O)cc(O)c2)c2ccccc12 10.1016/j.bmc.2009.11.062
44392519 123262 0 None -1 2 Human 7.8 pEC50 = 7.8 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-2 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-2 adrenergic receptor
ChEMBL 493 11 4 6 4.4 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(NCc2ccccc2)c1 10.1016/j.bmcl.2004.12.033
CHEMBL362293 123262 0 None -1 2 Human 7.8 pEC50 = 7.8 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-2 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-2 adrenergic receptor
ChEMBL 493 11 4 6 4.4 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(NCc2ccccc2)c1 10.1016/j.bmcl.2004.12.033
56663519 63299 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assayAgonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assay
ChEMBL 317 7 5 5 2.4 CC[C@@H](Cc1ccc(O)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2009.11.062
CHEMBL1800960 63299 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assayAgonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assay
ChEMBL 317 7 5 5 2.4 CC[C@@H](Cc1ccc(O)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2009.11.062
44392558 64909 0 None -2 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at Homo sapiens (human) beta2 adrenoreceptorAgonist activity at Homo sapiens (human) beta2 adrenoreceptor
ChEMBL 471 11 4 6 4.1 CC(C)=CCNc1cccc([C@@H](O)CN[C@H](C)Cc2c[nH]c3c(OS(C)(=O)=O)cccc23)c1 10.1007/s00044-009-9257-x
CHEMBL182770 64909 0 None -2 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at Homo sapiens (human) beta2 adrenoreceptorAgonist activity at Homo sapiens (human) beta2 adrenoreceptor
ChEMBL 471 11 4 6 4.1 CC(C)=CCNc1cccc([C@@H](O)CN[C@H](C)Cc2c[nH]c3c(OS(C)(=O)=O)cccc23)c1 10.1007/s00044-009-9257-x
24817062 28550 7 None - 1 Human 5.8 pEC50 = 5.8 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 382 5 0 3 4.1 O=C(c1ccc(OC2CCN(Cc3ccc(F)cc3)CC2)cc1)N1CCCC1 nan
CHEMBL1378531 28550 7 None - 1 Human 5.8 pEC50 = 5.8 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 382 5 0 3 4.1 O=C(c1ccc(OC2CCN(Cc3ccc(F)cc3)CC2)cc1)N1CCCC1 nan
2307884 67025 7 None - 1 Human 5.8 pEC50 = 5.8 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 347 3 0 2 4.7 O=C(COc1ccccc1F)N1c2ccccc2CCc2ccccc21 nan
CHEMBL1886907 67025 7 None - 1 Human 5.8 pEC50 = 5.8 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 347 3 0 2 4.7 O=C(COc1ccccc1F)N1c2ccccc2CCc2ccccc21 nan
44428083 92115 0 None -4 2 Rat 4.8 pEC50 = 4.8 Functional
Vasodilating activity against phenylephrine-induced contraction in rat thoracic aorta in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-oneVasodilating activity against phenylephrine-induced contraction in rat thoracic aorta in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-one
ChEMBL 444 10 5 9 0.7 CC(Cc1ccc(OCc2no[n+]([O-])c2C(N)=O)cc1)NCC(O)c1cc(O)cc(O)c1 10.1021/jm0704595
CHEMBL243266 92115 0 None -4 2 Rat 4.8 pEC50 = 4.8 Functional
Vasodilating activity against phenylephrine-induced contraction in rat thoracic aorta in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-oneVasodilating activity against phenylephrine-induced contraction in rat thoracic aorta in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-one
ChEMBL 444 10 5 9 0.7 CC(Cc1ccc(OCc2no[n+]([O-])c2C(N)=O)cc1)NCC(O)c1cc(O)cc(O)c1 10.1021/jm0704595
1292336 32044 11 None 9 2 Human 6.8 pEC50 = 6.8 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 403 8 1 6 5.1 CCCc1ccc(OCc2nc(-c3ccc(NC(=O)c4ccco4)cc3)no2)cc1 nan
CHEMBL1410048 32044 11 None 9 2 Human 6.8 pEC50 = 6.8 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 403 8 1 6 5.1 CCCc1ccc(OCc2nc(-c3ccc(NC(=O)c4ccco4)cc3)no2)cc1 nan
1084214 45263 9 None - 1 Human 6.8 pEC50 = 6.8 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 432 8 1 6 2.7 CCOC(=O)c1ccc(NC(=O)COc2ccc(S(=O)(=O)N3CCCC3)cc2)cc1 nan
CHEMBL1528594 45263 9 None - 1 Human 6.8 pEC50 = 6.8 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 432 8 1 6 2.7 CCOC(=O)c1ccc(NC(=O)COc2ccc(S(=O)(=O)N3CCCC3)cc2)cc1 nan
16832456 51020 11 None - 1 Human 6.8 pEC50 = 6.8 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 402 7 2 6 2.7 CC(=O)Nc1ccc(S(=O)(=O)NCCc2csc(-c3cccnc3)n2)cc1 nan
CHEMBL1581044 51020 11 None - 1 Human 6.8 pEC50 = 6.8 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 402 7 2 6 2.7 CC(=O)Nc1ccc(S(=O)(=O)NCCc2csc(-c3cccnc3)n2)cc1 nan
168276741 192220 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 330 4 3 3 3.1 Nc1c(F)cc(C(CO)NC2CCCCC2)cc1Br 10.1021/acs.jmedchem.1c02006
CHEMBL5180409 192220 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 330 4 3 3 3.1 Nc1c(F)cc(C(CO)NC2CCCCC2)cc1Br 10.1021/acs.jmedchem.1c02006
CHEMBL5221644 192220 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 330 4 3 3 3.1 Nc1c(F)cc(C(CO)NC2CCCCC2)cc1Br 10.1021/acs.jmedchem.1c02006
70686652 76408 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation countingAgonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting
ChEMBL 283 3 4 5 -0.1 CC(C)(C)NC[C@H](O)c1ccc2c(c1)C[OH+][B-](O)(O)O2 10.1016/j.bmc.2011.11.054
CHEMBL2068576 76408 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation countingAgonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting
ChEMBL 283 3 4 5 -0.1 CC(C)(C)NC[C@H](O)c1ccc2c(c1)C[OH+][B-](O)(O)O2 10.1016/j.bmc.2011.11.054
70686652 76408 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation countingAgonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting
ChEMBL 283 3 4 5 -0.1 CC(C)(C)NC[C@H](O)c1ccc2c(c1)C[OH+][B-](O)(O)O2 10.1016/j.bmc.2011.11.054
CHEMBL2068576 76408 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation countingAgonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting
ChEMBL 283 3 4 5 -0.1 CC(C)(C)NC[C@H](O)c1ccc2c(c1)C[OH+][B-](O)(O)O2 10.1016/j.bmc.2011.11.054
6407382 44907 4 None - 1 Human 5.8 pEC50 = 5.8 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 527 4 1 6 5.8 Cc1cccc(Nc2nnc(-c3ccc(C(=O)N4C[C@H]5C[C@H](C4)c4cccc(=O)n4C5)cc3)c3ccccc23)c1 nan
CHEMBL1525540 44907 4 None - 1 Human 5.8 pEC50 = 5.8 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 527 4 1 6 5.8 Cc1cccc(Nc2nnc(-c3ccc(C(=O)N4C[C@H]5C[C@H](C4)c4cccc(=O)n4C5)cc3)c3ccccc23)c1 nan
2953239 31012 5 None - 1 Human 6.8 pEC50 = 6.8 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 388 5 0 5 1.4 Cc1ccc(S(=O)(=O)N(C)CC(=O)N2CCN(c3ccccn3)CC2)cc1 nan
CHEMBL1401186 31012 5 None - 1 Human 6.8 pEC50 = 6.8 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 388 5 0 5 1.4 Cc1ccc(S(=O)(=O)N(C)CC(=O)N2CCN(c3ccccn3)CC2)cc1 nan
2233849 33118 8 None - 1 Human 6.8 pEC50 = 6.8 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 446 10 1 7 4.1 C=CCn1c(CCNC(=O)c2cccs2)nnc1SCC(=O)c1ccc(Cl)cc1 nan
CHEMBL1419122 33118 8 None - 1 Human 6.8 pEC50 = 6.8 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 446 10 1 7 4.1 C=CCn1c(CCNC(=O)c2cccs2)nnc1SCC(=O)c1ccc(Cl)cc1 nan
24180436 92772 0 None -1 2 Guinea pig 7.8 pEC50 = 7.8 Functional
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-oneAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-one
ChEMBL 527 10 4 10 2.6 CC(Cc1ccc(Oc2no[n+]([O-])c2S(=O)(=O)c2ccccc2)cc1)NCC(O)c1cc(O)cc(O)c1 10.1021/jm0704595
CHEMBL244687 92772 0 None -1 2 Guinea pig 7.8 pEC50 = 7.8 Functional
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-oneAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-one
ChEMBL 527 10 4 10 2.6 CC(Cc1ccc(Oc2no[n+]([O-])c2S(=O)(=O)c2ccccc2)cc1)NCC(O)c1cc(O)cc(O)c1 10.1021/jm0704595
90666119 108852 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP productionAgonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP production
ChEMBL 728 19 6 9 6.7 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2C[C@H]3C[C@@]3(COC(=O)Nc3ccccc3-c3ccc(O)c(Cl)c3)C2)ccc1O 10.1039/C1MD00140J
CHEMBL3219052 108852 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP productionAgonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP production
ChEMBL 728 19 6 9 6.7 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2C[C@H]3C[C@@]3(COC(=O)Nc3ccccc3-c3ccc(O)c(Cl)c3)C2)ccc1O 10.1039/C1MD00140J
54580128 61450 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as stimulation of intracellular cAMP production after 30 mins of washing by wash-off assayAgonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as stimulation of intracellular cAMP production after 30 mins of washing by wash-off assay
ChEMBL 723 20 6 7 7.2 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCCNC(=O)Cc2cccc(CC(C)(C)NC[C@H](O)c3ccc(O)c(CO)c3)c2)ccc1O)C(C)C 10.1016/j.bmcl.2010.10.132
CHEMBL1773196 61450 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as stimulation of intracellular cAMP production after 30 mins of washing by wash-off assayAgonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as stimulation of intracellular cAMP production after 30 mins of washing by wash-off assay
ChEMBL 723 20 6 7 7.2 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCCNC(=O)Cc2cccc(CC(C)(C)NC[C@H](O)c3ccc(O)c(CO)c3)c2)ccc1O)C(C)C 10.1016/j.bmcl.2010.10.132
44392457 165393 0 None -34 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at Homo sapiens (human) beta2 adrenoreceptorAgonist activity at Homo sapiens (human) beta2 adrenoreceptor
ChEMBL 457 11 4 6 3.7 C/C=C/CNc1cccc([C@@H](O)CN[C@H](C)Cc2c[nH]c3c(OS(C)(=O)=O)cccc23)c1 10.1007/s00044-009-9257-x
CHEMBL425161 165393 0 None -34 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at Homo sapiens (human) beta2 adrenoreceptorAgonist activity at Homo sapiens (human) beta2 adrenoreceptor
ChEMBL 457 11 4 6 3.7 C/C=C/CNc1cccc([C@@H](O)CN[C@H](C)Cc2c[nH]c3c(OS(C)(=O)=O)cccc23)c1 10.1007/s00044-009-9257-x
44428081 92688 0 None - 1 Guinea pig 6.8 pEC50 = 6.8 Functional
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contractionAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction
ChEMBL 428 10 5 9 1.4 CC(Cc1ccc(OCc2nonc2C(N)=O)cc1)NCC(O)c1cc(O)cc(O)c1 10.1021/jm0704595
CHEMBL244321 92688 0 None - 1 Guinea pig 6.8 pEC50 = 6.8 Functional
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contractionAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction
ChEMBL 428 10 5 9 1.4 CC(Cc1ccc(OCc2nonc2C(N)=O)cc1)NCC(O)c1cc(O)cc(O)c1 10.1021/jm0704595
45483831 195329 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 343 8 4 4 3.1 CCc1ccc(CC(C)(C)NCC(O)c2ccc(O)c(CO)c2)cc1 10.1016/j.bmcl.2009.10.013
CHEMBL566992 195329 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 343 8 4 4 3.1 CCc1ccc(CC(C)(C)NCC(O)c2ccc(O)c(CO)c2)cc1 10.1016/j.bmcl.2009.10.013
5808 176196 20 None -4 5 Guinea pig 5.8 pEC50 = 5.8 Functional
Activity for Beta-2 adrenergic receptor was assessed from effect on relaxation of guinea pig trachea.Activity for Beta-2 adrenergic receptor was assessed from effect on relaxation of guinea pig trachea.
ChEMBL 211 4 4 4 1.1 CC(C)NC[C@@H](O)c1ccc(O)c(O)c1 10.1021/jm00019a001
CHEMBL1257092 176196 20 None -4 5 Guinea pig 5.8 pEC50 = 5.8 Functional
Activity for Beta-2 adrenergic receptor was assessed from effect on relaxation of guinea pig trachea.Activity for Beta-2 adrenergic receptor was assessed from effect on relaxation of guinea pig trachea.
ChEMBL 211 4 4 4 1.1 CC(C)NC[C@@H](O)c1ccc(O)c(O)c1 10.1021/jm00019a001
CHEMBL460574 176196 20 None -4 5 Guinea pig 5.8 pEC50 = 5.8 Functional
Activity for Beta-2 adrenergic receptor was assessed from effect on relaxation of guinea pig trachea.Activity for Beta-2 adrenergic receptor was assessed from effect on relaxation of guinea pig trachea.
ChEMBL 211 4 4 4 1.1 CC(C)NC[C@@H](O)c1ccc(O)c(O)c1 10.1021/jm00019a001
1271047 44090 13 None - 1 Human 5.8 pEC50 = 5.8 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 301 5 1 1 4.7 O=C(Nc1ccccc1)c1ccccc1CCc1ccccc1 nan
CHEMBL1518070 44090 13 None - 1 Human 5.8 pEC50 = 5.8 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 301 5 1 1 4.7 O=C(Nc1ccccc1)c1ccccc1CCc1ccccc1 nan
664105 29551 8 None - 1 Human 5.8 pEC50 = 5.8 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory)
ChEMBL 468 4 1 9 2.8 CC1(C)Cc2c(c(N3CCCC3)nc3sc4c(N5CCN(CCO)CC5)ncnc4c23)CO1 nan
CHEMBL1387056 29551 8 None - 1 Human 5.8 pEC50 = 5.8 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory)
ChEMBL 468 4 1 9 2.8 CC1(C)Cc2c(c(N3CCCC3)nc3sc4c(N5CCN(CCO)CC5)ncnc4c23)CO1 nan
54580133 61472 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as stimulation of intracellular cAMP production after 30 mins of washing by wash-off assayAgonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as stimulation of intracellular cAMP production after 30 mins of washing by wash-off assay
ChEMBL 654 19 5 7 7.7 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCCCOc2ccc(CCNC[C@H](O)c3ccc(O)c(O)c3)cc2)ccc1O)C(C)C 10.1016/j.bmcl.2010.10.132
CHEMBL1773265 61472 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as stimulation of intracellular cAMP production after 30 mins of washing by wash-off assayAgonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as stimulation of intracellular cAMP production after 30 mins of washing by wash-off assay
ChEMBL 654 19 5 7 7.7 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCCCOc2ccc(CCNC[C@H](O)c3ccc(O)c(O)c3)cc2)ccc1O)C(C)C 10.1016/j.bmcl.2010.10.132
6404528 44526 24 None - 1 Human 6.8 pEC50 = 6.8 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 307 3 0 4 4.5 N#Cc1cc(-c2ccccc2)nnc1Oc1ccccc1Cl nan
CHEMBL1521880 44526 24 None - 1 Human 6.8 pEC50 = 6.8 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 307 3 0 4 4.5 N#Cc1cc(-c2ccccc2)nnc1Oc1ccccc1Cl nan
1231538 27296 23 None 1 3 Human 5.8 pEC50 = 5.8 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 523 6 1 6 6.0 O=C(Nc1ccc2nc(SCc3ccc(Cl)cc3)sc2c1)c1ccccc1C(=O)N1CCOCC1 nan
CHEMBL1368962 27296 23 None 1 3 Human 5.8 pEC50 = 5.8 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 523 6 1 6 6.0 O=C(Nc1ccc2nc(SCc3ccc(Cl)cc3)sc2c1)c1ccccc1C(=O)N1CCOCC1 nan
135799875 185828 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at beta2 adrenoceptor in HEK293 cells co-expressing V2 receptor assessed as increase in cAMP accumulation measured after 30 mins by HTRF assayAgonist activity at beta2 adrenoceptor in HEK293 cells co-expressing V2 receptor assessed as increase in cAMP accumulation measured after 30 mins by HTRF assay
ChEMBL 276 3 4 4 1.7 CC(C)(C)NC(CO)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/acs.jmedchem.0c01195
CHEMBL4876155 185828 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at beta2 adrenoceptor in HEK293 cells co-expressing V2 receptor assessed as increase in cAMP accumulation measured after 30 mins by HTRF assayAgonist activity at beta2 adrenoceptor in HEK293 cells co-expressing V2 receptor assessed as increase in cAMP accumulation measured after 30 mins by HTRF assay
ChEMBL 276 3 4 4 1.7 CC(C)(C)NC(CO)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/acs.jmedchem.0c01195
24791840 59481 5 None - 1 Human 5.8 pEC50 = 5.8 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 406 6 0 3 4.9 CCc1ccc(CN2CCC(Oc3ccc(C(=O)N4CCCCC4)cc3)CC2)cc1 nan
CHEMBL1727257 59481 5 None - 1 Human 5.8 pEC50 = 5.8 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 406 6 0 3 4.9 CCc1ccc(CN2CCC(Oc3ccc(C(=O)N4CCCCC4)cc3)CC2)cc1 nan
25023953 186790 0 None - 1 Golden hamster 6.8 pEC50 = 6.8 Functional
Agonist activity at adrenergic beta2 receptor in Syrian hamster DDT1 MF2 cells assessed as stimulation of cAMP accumulation by radioimmunoassay in presence of 1 uM DPCPXAgonist activity at adrenergic beta2 receptor in Syrian hamster DDT1 MF2 cells assessed as stimulation of cAMP accumulation by radioimmunoassay in presence of 1 uM DPCPX
ChEMBL 577 17 8 15 -1.5 O=CNc1cc(C(O)CNCCOCCOCCNc2ncnc3c2ncn3[C@@H]2O[C@H](CO)[C@@H](O)[C@H]2O)ccc1O 10.1021/jm800613s
CHEMBL493489 186790 0 None - 1 Golden hamster 6.8 pEC50 = 6.8 Functional
Agonist activity at adrenergic beta2 receptor in Syrian hamster DDT1 MF2 cells assessed as stimulation of cAMP accumulation by radioimmunoassay in presence of 1 uM DPCPXAgonist activity at adrenergic beta2 receptor in Syrian hamster DDT1 MF2 cells assessed as stimulation of cAMP accumulation by radioimmunoassay in presence of 1 uM DPCPX
ChEMBL 577 17 8 15 -1.5 O=CNc1cc(C(O)CNCCOCCOCCNc2ncnc3c2ncn3[C@@H]2O[C@H](CO)[C@@H](O)[C@H]2O)ccc1O 10.1021/jm800613s
1155 1592 45 None -2 3 Guinea pig 7.8 pEC50 = 7.8 Functional
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contractionAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction
ChEMBL 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 10.1021/jm0704595
3343 1592 45 None -2 3 Guinea pig 7.8 pEC50 = 7.8 Functional
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contractionAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction
ChEMBL 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 10.1021/jm0704595
557 1592 45 None -2 3 Guinea pig 7.8 pEC50 = 7.8 Functional
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contractionAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction
ChEMBL 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 10.1021/jm0704595
CHEMBL32800 1592 45 None -2 3 Guinea pig 7.8 pEC50 = 7.8 Functional
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contractionAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction
ChEMBL 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 10.1021/jm0704595
DB01288 1592 45 None -2 3 Guinea pig 7.8 pEC50 = 7.8 Functional
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contractionAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction
ChEMBL 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 10.1021/jm0704595
24180436 92772 0 None -1 2 Guinea pig 7.8 pEC50 = 7.8 Functional
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contractionAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction
ChEMBL 527 10 4 10 2.6 CC(Cc1ccc(Oc2no[n+]([O-])c2S(=O)(=O)c2ccccc2)cc1)NCC(O)c1cc(O)cc(O)c1 10.1021/jm0704595
CHEMBL244687 92772 0 None -1 2 Guinea pig 7.8 pEC50 = 7.8 Functional
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contractionAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction
ChEMBL 527 10 4 10 2.6 CC(Cc1ccc(Oc2no[n+]([O-])c2S(=O)(=O)c2ccccc2)cc1)NCC(O)c1cc(O)cc(O)c1 10.1021/jm0704595
46221603 8456 0 None -7 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assayAgonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assay
ChEMBL 396 6 4 6 2.0 COc1cc2c(cc1OC)CC(NC[C@H](O)c1ccc(O)c3[nH]c(=O)ccc13)C2 10.1021/jm100068m
CHEMBL1094486 8456 0 None -7 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assayAgonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assay
ChEMBL 396 6 4 6 2.0 COc1cc2c(cc1OC)CC(NC[C@H](O)c1ccc(O)c3[nH]c(=O)ccc13)C2 10.1021/jm100068m
44392577 122014 0 None -2 2 Human 7.8 pEC50 = 7.8 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-2 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-2 adrenergic receptor
ChEMBL 455 10 4 6 3.2 CC#CCNc1cccc([C@@H](O)CN[C@H](C)Cc2c[nH]c3c(OS(C)(=O)=O)cccc23)c1 10.1016/j.bmcl.2004.12.033
CHEMBL360133 122014 0 None -2 2 Human 7.8 pEC50 = 7.8 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-2 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-2 adrenergic receptor
ChEMBL 455 10 4 6 3.2 CC#CCNc1cccc([C@@H](O)CN[C@H](C)Cc2c[nH]c3c(OS(C)(=O)=O)cccc23)c1 10.1016/j.bmcl.2004.12.033
11432806 65851 0 None -134 3 Human 7.8 pEC50 = 7.8 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptor
ChEMBL 549 11 4 8 3.6 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2004.09.054
11432806 65851 0 None -134 3 Human 7.8 pEC50 = 7.8 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptor
ChEMBL 549 11 4 8 3.6 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2004.10.035
CHEMBL184407 65851 0 None -134 3 Human 7.8 pEC50 = 7.8 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptor
ChEMBL 549 11 4 8 3.6 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2004.09.054
CHEMBL184407 65851 0 None -134 3 Human 7.8 pEC50 = 7.8 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptor
ChEMBL 549 11 4 8 3.6 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2004.10.035
44396568 66934 0 None -34 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at Homo sapiens (human) beta2 adrenoreceptorAgonist activity at Homo sapiens (human) beta2 adrenoreceptor
ChEMBL 529 12 5 7 3.7 C[C@H](Cc1c[nH]c2c(OCC(=O)O)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1007/s00044-009-9257-x
CHEMBL188196 66934 0 None -34 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at Homo sapiens (human) beta2 adrenoreceptorAgonist activity at Homo sapiens (human) beta2 adrenoreceptor
ChEMBL 529 12 5 7 3.7 C[C@H](Cc1c[nH]c2c(OCC(=O)O)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1007/s00044-009-9257-x
9873257 84507 12 None -47 3 Human 5.8 pEC50 = 5.8 Functional
Agonistic activity against the cloned human Beta-2 adrenergic receptor was measured by its by its ability to stimulate adenylyl cyclaseAgonistic activity against the cloned human Beta-2 adrenergic receptor was measured by its by its ability to stimulate adenylyl cyclase
ChEMBL 591 14 3 10 3.5 O=c1n(CCCC2CCCC2)nnn1-c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(99)00182-1
CHEMBL22375 84507 12 None -47 3 Human 5.8 pEC50 = 5.8 Functional
Agonistic activity against the cloned human Beta-2 adrenergic receptor was measured by its by its ability to stimulate adenylyl cyclaseAgonistic activity against the cloned human Beta-2 adrenergic receptor was measured by its by its ability to stimulate adenylyl cyclase
ChEMBL 591 14 3 10 3.5 O=c1n(CCCC2CCCC2)nnn1-c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(99)00182-1
11758172 100454 0 None -147 3 Human 5.8 pEC50 = 5.8 Functional
In vitro functional efficacy in stimulating increase in cAMP in chinese hamster ovary (CHO) cells expressing the cloned human beta-2 receptor.In vitro functional efficacy in stimulating increase in cAMP in chinese hamster ovary (CHO) cells expressing the cloned human beta-2 receptor.
ChEMBL 592 11 3 7 5.8 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3ccc(F)c(F)c3)cs2)cc1 10.1021/jm000286i
CHEMBL293994 100454 0 None -147 3 Human 5.8 pEC50 = 5.8 Functional
In vitro functional efficacy in stimulating increase in cAMP in chinese hamster ovary (CHO) cells expressing the cloned human beta-2 receptor.In vitro functional efficacy in stimulating increase in cAMP in chinese hamster ovary (CHO) cells expressing the cloned human beta-2 receptor.
ChEMBL 592 11 3 7 5.8 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3ccc(F)c(F)c3)cs2)cc1 10.1021/jm000286i
44428086 149535 0 None -7 2 Rat 4.8 pEC50 = 4.8 Functional
Vasodilating activity against phenylephrine-induced contractions in rat thoracic aortaVasodilating activity against phenylephrine-induced contractions in rat thoracic aorta
ChEMBL 415 9 4 8 1.9 Cc1c(COc2ccc(CC(C)NCC(O)c3cc(O)cc(O)c3)cc2)no[n+]1[O-] 10.1021/jm0704595
CHEMBL395082 149535 0 None -7 2 Rat 4.8 pEC50 = 4.8 Functional
Vasodilating activity against phenylephrine-induced contractions in rat thoracic aortaVasodilating activity against phenylephrine-induced contractions in rat thoracic aorta
ChEMBL 415 9 4 8 1.9 Cc1c(COc2ccc(CC(C)NCC(O)c3cc(O)cc(O)c3)cc2)no[n+]1[O-] 10.1021/jm0704595
2005835 22354 8 None 6 2 Human 5.7 pEC50 = 5.7 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory)
ChEMBL 459 5 1 9 5.2 CSc1nc(SCCO)c2sc3nc(-c4ccco4)c4c(c3c2n1)CC(C)(C)OC4 nan
CHEMBL1326167 22354 8 None 6 2 Human 5.7 pEC50 = 5.7 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory)
ChEMBL 459 5 1 9 5.2 CSc1nc(SCCO)c2sc3nc(-c4ccco4)c4c(c3c2n1)CC(C)(C)OC4 nan
24791840 59481 5 None - 1 Human 5.7 pEC50 = 5.7 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory)
ChEMBL 406 6 0 3 4.9 CCc1ccc(CN2CCC(Oc3ccc(C(=O)N4CCCCC4)cc3)CC2)cc1 nan
CHEMBL1727257 59481 5 None - 1 Human 5.7 pEC50 = 5.7 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory)
ChEMBL 406 6 0 3 4.9 CCc1ccc(CN2CCC(Oc3ccc(C(=O)N4CCCCC4)cc3)CC2)cc1 nan
12988999 192192 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 354 3 3 3 3.5 CC(C)(C)NC(CO)c1cc(Br)c(N)c(C(F)(F)F)c1 10.1021/acs.jmedchem.1c02006
CHEMBL5176025 192192 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 354 3 3 3 3.5 CC(C)(C)NC(CO)c1cc(Br)c(N)c(C(F)(F)F)c1 10.1021/acs.jmedchem.1c02006
CHEMBL5221441 192192 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 354 3 3 3 3.5 CC(C)(C)NC(CO)c1cc(Br)c(N)c(C(F)(F)F)c1 10.1021/acs.jmedchem.1c02006
16735257 85290 0 None -812 2 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity beta2-adrenergic receptor in rat ventricular myocytes assessed as cell contraction following electrical stimulation by optical edge tracking method using photodiode arrayAgonist activity beta2-adrenergic receptor in rat ventricular myocytes assessed as cell contraction following electrical stimulation by optical edge tracking method using photodiode array
ChEMBL 317 7 4 5 2.4 COc1ccc(C[C@@H](C)NC[C@H](O)c2cc(O)cc(O)c2)cc1 10.1016/j.bmc.2009.11.062
CHEMBL228992 85290 0 None -812 2 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity beta2-adrenergic receptor in rat ventricular myocytes assessed as cell contraction following electrical stimulation by optical edge tracking method using photodiode arrayAgonist activity beta2-adrenergic receptor in rat ventricular myocytes assessed as cell contraction following electrical stimulation by optical edge tracking method using photodiode array
ChEMBL 317 7 4 5 2.4 COc1ccc(C[C@@H](C)NC[C@H](O)c2cc(O)cc(O)c2)cc1 10.1016/j.bmc.2009.11.062
76319327 84888 0 None -14 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at Homo sapiens (human) beta2 adrenoreceptorAgonist activity at Homo sapiens (human) beta2 adrenoreceptor
ChEMBL 584 14 4 7 4.5 CCN(CC)C(=O)COc1cccc2c(C[C@@H](C)NC[C@H](O)c3cccc(NS(=O)(=O)c4cccs4)c3)c[nH]c12 10.1007/s00044-009-9257-x
CHEMBL2261203 84888 0 None -14 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at Homo sapiens (human) beta2 adrenoreceptorAgonist activity at Homo sapiens (human) beta2 adrenoreceptor
ChEMBL 584 14 4 7 4.5 CCN(CC)C(=O)COc1cccc2c(C[C@@H](C)NC[C@H](O)c3cccc(NS(=O)(=O)c4cccs4)c3)c[nH]c12 10.1007/s00044-009-9257-x
1155 1592 45 None -2 3 Guinea pig 7.7 pEC50 = 7.7 Functional
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-oneAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-one
ChEMBL 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 10.1021/jm0704595
3343 1592 45 None -2 3 Guinea pig 7.7 pEC50 = 7.7 Functional
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-oneAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-one
ChEMBL 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 10.1021/jm0704595
557 1592 45 None -2 3 Guinea pig 7.7 pEC50 = 7.7 Functional
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-oneAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-one
ChEMBL 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 10.1021/jm0704595
CHEMBL32800 1592 45 None -2 3 Guinea pig 7.7 pEC50 = 7.7 Functional
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-oneAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-one
ChEMBL 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 10.1021/jm0704595
DB01288 1592 45 None -2 3 Guinea pig 7.7 pEC50 = 7.7 Functional
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-oneAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-one
ChEMBL 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 10.1021/jm0704595
25218684 178376 4 None 891 2 Guinea pig 7.7 pEC50 = 7.7 Functional
Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as relaxation of carbachol-induced tissue contractionAgonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as relaxation of carbachol-induced tissue contraction
ChEMBL 261 2 3 4 1.1 CC(C)N[C@H]1CCn2c(=O)[nH]c3cccc(c32)[C@@H]1O 10.1021/jm801211c
CHEMBL470584 178376 4 None 891 2 Guinea pig 7.7 pEC50 = 7.7 Functional
Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as relaxation of carbachol-induced tissue contractionAgonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as relaxation of carbachol-induced tissue contraction
ChEMBL 261 2 3 4 1.1 CC(C)N[C@H]1CCn2c(=O)[nH]c3cccc(c32)[C@@H]1O 10.1021/jm801211c
CHEMBL470585 178376 4 None 891 2 Guinea pig 7.7 pEC50 = 7.7 Functional
Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as relaxation of carbachol-induced tissue contractionAgonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as relaxation of carbachol-induced tissue contraction
ChEMBL 261 2 3 4 1.1 CC(C)N[C@H]1CCn2c(=O)[nH]c3cccc(c32)[C@@H]1O 10.1021/jm801211c
44396568 66934 0 None -34 3 Human 7.7 pEC50 = 7.7 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptor
ChEMBL 529 12 5 7 3.7 C[C@H](Cc1c[nH]c2c(OCC(=O)O)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2004.10.035
CHEMBL188196 66934 0 None -34 3 Human 7.7 pEC50 = 7.7 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptor
ChEMBL 529 12 5 7 3.7 C[C@H](Cc1c[nH]c2c(OCC(=O)O)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2004.10.035
44392552 64180 0 None -35 3 Human 7.7 pEC50 = 7.7 Functional
Effective concentration against human beta-2 adrenergic receptorEffective concentration against human beta-2 adrenergic receptor
ChEMBL 543 11 4 7 3.6 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2ccccc2)c1 10.1016/j.bmcl.2004.12.033
CHEMBL181440 64180 0 None -35 3 Human 7.7 pEC50 = 7.7 Functional
Effective concentration against human beta-2 adrenergic receptorEffective concentration against human beta-2 adrenergic receptor
ChEMBL 543 11 4 7 3.6 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2ccccc2)c1 10.1016/j.bmcl.2004.12.033
2977891 21588 8 None - 1 Human 7.7 pEC50 = 7.7 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory)
ChEMBL 452 5 0 5 1.8 CN(CC(=O)N1CCN(c2ccccn2)CC1)S(=O)(=O)c1ccc(Br)cc1 nan
CHEMBL1319376 21588 8 None - 1 Human 7.7 pEC50 = 7.7 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory)
ChEMBL 452 5 0 5 1.8 CN(CC(=O)N1CCN(c2ccccn2)CC1)S(=O)(=O)c1ccc(Br)cc1 nan
168278795 192241 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 304 3 3 3 2.6 CC(C)(C)NC(CO)c1cc(F)c(N)c(Br)c1 10.1021/acs.jmedchem.1c02006
CHEMBL5183062 192241 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 304 3 3 3 2.6 CC(C)(C)NC(CO)c1cc(F)c(N)c(Br)c1 10.1021/acs.jmedchem.1c02006
CHEMBL5221779 192241 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 304 3 3 3 2.6 CC(C)(C)NC(CO)c1cc(F)c(N)c(Br)c1 10.1021/acs.jmedchem.1c02006
10863093 50041 0 None -3 3 Human 7.7 pEC50 = 7.7 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-2 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-2 AR expressed as the negative logarithm of the molar drug concentration
ChEMBL 439 10 4 6 2.1 C[C@H](CNc1ccc(CC(=O)NS(C)(=O)=O)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0101500
CHEMBL157210 50041 0 None -3 3 Human 7.7 pEC50 = 7.7 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-2 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-2 AR expressed as the negative logarithm of the molar drug concentration
ChEMBL 439 10 4 6 2.1 C[C@H](CNc1ccc(CC(=O)NS(C)(=O)=O)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0101500
57401200 70497 0 None - 1 Guinea pig 7.7 pEC50 = 7.7 Functional
Agonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contractionAgonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contraction
ChEMBL 510 11 4 8 2.7 COc1ccc(C2=NN(CCNCC(O)c3ccc(O)c(NC=O)c3)C(=O)C3CCCCC23)cc1OC 10.1016/j.bmcl.2012.01.013
CHEMBL1951065 70497 0 None - 1 Guinea pig 7.7 pEC50 = 7.7 Functional
Agonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contractionAgonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contraction
ChEMBL 510 11 4 8 2.7 COc1ccc(C2=NN(CCNCC(O)c3ccc(O)c(NC=O)c3)C(=O)C3CCCCC23)cc1OC 10.1016/j.bmcl.2012.01.013
57401202 70501 0 None - 1 Guinea pig 7.7 pEC50 = 7.7 Functional
Agonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contractionAgonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contraction
ChEMBL 552 14 4 8 3.8 COc1ccc(C2=NN(CCCCCNCC(O)c3ccc(O)c(NC=O)c3)C(=O)C3CCCCC23)cc1OC 10.1016/j.bmcl.2012.01.013
CHEMBL1951069 70501 0 None - 1 Guinea pig 7.7 pEC50 = 7.7 Functional
Agonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contractionAgonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contraction
ChEMBL 552 14 4 8 3.8 COc1ccc(C2=NN(CCCCCNCC(O)c3ccc(O)c(NC=O)c3)C(=O)C3CCCCC23)cc1OC 10.1016/j.bmcl.2012.01.013
145987938 166496 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 354 7 4 5 2.1 COc1ccc(CCNC(CO)c2ccc(O)c3[nH]c(=O)ccc23)cc1 10.1016/j.ejmech.2018.04.041
CHEMBL4289233 166496 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 354 7 4 5 2.1 COc1ccc(CCNC(CO)c2ccc(O)c3[nH]c(=O)ccc23)cc1 10.1016/j.ejmech.2018.04.041
76329060 105942 0 None 199 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 493 17 4 7 3.5 CS(=O)(=O)c1ccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc1 10.1021/jm401532g
CHEMBL3126381 105942 0 None 199 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 493 17 4 7 3.5 CS(=O)(=O)c1ccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc1 10.1021/jm401532g
CHEMBL3139685 105942 0 None 199 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 493 17 4 7 3.5 CS(=O)(=O)c1ccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc1 10.1021/jm401532g
90644153 111748 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 470 11 5 6 5.3 OCc1cc(C(O)CNCCc2ccc(Nc3ccc(Oc4ccccc4)cc3)cc2)ccc1O 10.1016/j.bmcl.2014.04.069
CHEMBL3290982 111748 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 470 11 5 6 5.3 OCc1cc(C(O)CNCCc2ccc(Nc3ccc(Oc4ccccc4)cc3)cc2)ccc1O 10.1016/j.bmcl.2014.04.069
1369799 44199 8 None - 1 Human 7.7 pEC50 = 7.7 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory)
ChEMBL 401 5 1 5 5.2 CC(C)(C)c1ccc(OCC(=O)Nc2ccc(-c3nc4cccnc4o3)cc2)cc1 nan
CHEMBL1519042 44199 8 None - 1 Human 7.7 pEC50 = 7.7 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory)
ChEMBL 401 5 1 5 5.2 CC(C)(C)c1ccc(OCC(=O)Nc2ccc(-c3nc4cccnc4o3)cc2)cc1 nan
135799865 185998 0 None - 1 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at beta2 adrenoceptor in HEK293 cells co-expressing V2 receptor assessed as increase in cAMP accumulation measured after 30 mins by HTRF assayAgonist activity at beta2 adrenoceptor in HEK293 cells co-expressing V2 receptor assessed as increase in cAMP accumulation measured after 30 mins by HTRF assay
ChEMBL 262 4 4 4 1.3 CC(C)NC(CO)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/acs.jmedchem.0c01195
CHEMBL4878555 185998 0 None - 1 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at beta2 adrenoceptor in HEK293 cells co-expressing V2 receptor assessed as increase in cAMP accumulation measured after 30 mins by HTRF assayAgonist activity at beta2 adrenoceptor in HEK293 cells co-expressing V2 receptor assessed as increase in cAMP accumulation measured after 30 mins by HTRF assay
ChEMBL 262 4 4 4 1.3 CC(C)NC(CO)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/acs.jmedchem.0c01195
24819471 30049 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 408 9 0 6 3.9 CC(=O)c1ccc(OCc2cc(C(=O)N(C)CCOc3ccc(C)cc3)no2)cc1 nan
CHEMBL1391134 30049 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 408 9 0 6 3.9 CC(=O)c1ccc(OCc2cc(C(=O)N(C)CCOc3ccc(C)cc3)no2)cc1 nan
90666117 108850 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP productionAgonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP production
ChEMBL 744 20 6 9 7.6 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3ccc(O)c(Cl)c3)CC2)ccc1O 10.1039/C1MD00140J
CHEMBL3219050 108850 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP productionAgonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP production
ChEMBL 744 20 6 9 7.6 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3ccc(O)c(Cl)c3)CC2)ccc1O 10.1039/C1MD00140J
24817788 33251 1 None - 1 Human 6.7 pEC50 = 6.7 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 407 7 1 7 3.2 Cc1ccc(OCc2cc(C(=O)NCc3cnn(-c4cccc(F)c4)c3)no2)cn1 nan
CHEMBL1420188 33251 1 None - 1 Human 6.7 pEC50 = 6.7 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 407 7 1 7 3.2 Cc1ccc(OCc2cc(C(=O)NCc3cnn(-c4cccc(F)c4)c3)no2)cn1 nan
1073012 33485 18 None - 1 Human 5.7 pEC50 = 5.7 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 403 5 0 5 1.3 CCOC(=O)N1CCN(C(=O)CN(C)S(=O)(=O)c2ccc(Cl)cc2)CC1 nan
CHEMBL1422244 33485 18 None - 1 Human 5.7 pEC50 = 5.7 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 403 5 0 5 1.3 CCOC(=O)N1CCN(C(=O)CN(C)S(=O)(=O)c2ccc(Cl)cc2)CC1 nan
105 3392 84 None -8 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1016/j.bmcl.2011.04.135
2083 3392 84 None -8 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1016/j.bmcl.2011.04.135
558 3392 84 None -8 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1016/j.bmcl.2011.04.135
CHEMBL714 3392 84 None -8 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1016/j.bmcl.2011.04.135
DB01001 3392 84 None -8 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1016/j.bmcl.2011.04.135
90644149 111743 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 447 9 4 6 3.1 OCc1cc(C(O)CNCCc2ccc(N3CCN(c4ccccc4)CC3)cc2)ccc1O 10.1016/j.bmcl.2014.04.069
CHEMBL3290978 111743 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 447 9 4 6 3.1 OCc1cc(C(O)CNCCc2ccc(N3CCN(c4ccccc4)CC3)cc2)ccc1O 10.1016/j.bmcl.2014.04.069
90644154 111751 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 428 9 5 5 4.6 OCc1cc(C(O)CNCCc2ccc(Nc3cccc4ccccc34)cc2)ccc1O 10.1016/j.bmcl.2014.04.069
CHEMBL3290985 111751 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 428 9 5 5 4.6 OCc1cc(C(O)CNCCc2ccc(Nc3cccc4ccccc34)cc2)ccc1O 10.1016/j.bmcl.2014.04.069
90644140 111761 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 394 9 6 6 3.2 OCc1cc(C(O)CNCCc2ccc(Nc3ccc(O)cc3)cc2)ccc1O 10.1016/j.bmcl.2014.04.069
CHEMBL3290994 111761 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 394 9 6 6 3.2 OCc1cc(C(O)CNCCc2ccc(Nc3ccc(O)cc3)cc2)ccc1O 10.1016/j.bmcl.2014.04.069
1499 2052 43 None -72 36 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm800222k
3779 2052 43 None -72 36 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm800222k
536 2052 43 None -72 36 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm800222k
CHEMBL434 2052 43 None -72 36 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm800222k
DB01064 2052 43 None -72 36 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm800222k
16736091 85291 0 None 251 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assayAgonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assay
ChEMBL 317 7 4 5 2.4 COc1ccc(C[C@H](C)NC[C@H](O)c2cc(O)cc(O)c2)cc1 10.1016/j.bmc.2009.11.062
CHEMBL228996 85291 0 None 251 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assayAgonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assay
ChEMBL 317 7 4 5 2.4 COc1ccc(C[C@H](C)NC[C@H](O)c2cc(O)cc(O)c2)cc1 10.1016/j.bmc.2009.11.062
16736091 85291 0 None 251 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulationAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulation
ChEMBL 317 7 4 5 2.4 COc1ccc(C[C@H](C)NC[C@H](O)c2cc(O)cc(O)c2)cc1 10.1016/j.bmc.2013.11.030
CHEMBL228996 85291 0 None 251 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulationAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulation
ChEMBL 317 7 4 5 2.4 COc1ccc(C[C@H](C)NC[C@H](O)c2cc(O)cc(O)c2)cc1 10.1016/j.bmc.2013.11.030
1499 2052 43 None -72 36 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm8000345
3779 2052 43 None -72 36 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm8000345
536 2052 43 None -72 36 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm8000345
CHEMBL434 2052 43 None -72 36 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm8000345
DB01064 2052 43 None -72 36 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm8000345
1499 2052 43 None -72 36 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm9000709
3779 2052 43 None -72 36 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm9000709
536 2052 43 None -72 36 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm9000709
CHEMBL434 2052 43 None -72 36 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm9000709
DB01064 2052 43 None -72 36 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm9000709
1499 2052 43 None -72 36 Human 8.7 pEC50 = 8.7 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-2 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-2 adrenergic receptor
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmcl.2004.11.001
3779 2052 43 None -72 36 Human 8.7 pEC50 = 8.7 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-2 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-2 adrenergic receptor
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmcl.2004.11.001
536 2052 43 None -72 36 Human 8.7 pEC50 = 8.7 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-2 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-2 adrenergic receptor
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmcl.2004.11.001
CHEMBL434 2052 43 None -72 36 Human 8.7 pEC50 = 8.7 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-2 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-2 adrenergic receptor
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmcl.2004.11.001
DB01064 2052 43 None -72 36 Human 8.7 pEC50 = 8.7 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-2 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-2 adrenergic receptor
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmcl.2004.11.001
2953239 31012 5 None - 1 Human 8.7 pEC50 = 8.7 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory)
ChEMBL 388 5 0 5 1.4 Cc1ccc(S(=O)(=O)N(C)CC(=O)N2CCN(c3ccccn3)CC2)cc1 nan
CHEMBL1401186 31012 5 None - 1 Human 8.7 pEC50 = 8.7 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory)
ChEMBL 388 5 0 5 1.4 Cc1ccc(S(=O)(=O)N(C)CC(=O)N2CCN(c3ccccn3)CC2)cc1 nan
68057795 124670 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 804 17 6 10 6.0 COc1cc(NC(=O)CCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)ccc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645276 124670 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 804 17 6 10 6.0 COc1cc(NC(=O)CCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)ccc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548077 124714 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 880 17 6 10 7.4 COc1ccc(CC(=O)Nc2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1CC(C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645319 124714 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 880 17 6 10 7.4 COc1ccc(CC(=O)Nc2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1CC(C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548088 124734 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 836 16 6 9 6.6 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CNC(=O)Cc2cccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1 nan
CHEMBL3645338 124734 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 836 16 6 9 6.6 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CNC(=O)Cc2cccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1 nan
59548072 124735 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 836 16 6 9 6.6 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CNC(=O)Cc2ccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 nan
CHEMBL3645339 124735 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 836 16 6 9 6.6 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CNC(=O)Cc2ccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 nan
59548116 124744 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 894 18 6 10 7.1 COc1ccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1C[C@H](C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645347 124744 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 894 18 6 10 7.1 COc1ccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1C[C@H](C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548085 124746 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 878 18 6 9 7.1 CC(Cc1cccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645349 124746 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 878 18 6 9 7.1 CC(Cc1cccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
319 1292 39 None -2 6 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at beta2-adrenoceptor in human bronchial smooth-muscle cell by cAMP assayAgonist activity at beta2-adrenoceptor in human bronchial smooth-muscle cell by cAMP assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2012.07.096
321 1292 39 None -2 6 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at beta2-adrenoceptor in human bronchial smooth-muscle cell by cAMP assayAgonist activity at beta2-adrenoceptor in human bronchial smooth-muscle cell by cAMP assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2012.07.096
444031 1292 39 None -2 6 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at beta2-adrenoceptor in human bronchial smooth-muscle cell by cAMP assayAgonist activity at beta2-adrenoceptor in human bronchial smooth-muscle cell by cAMP assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2012.07.096
784 1292 39 None -2 6 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at beta2-adrenoceptor in human bronchial smooth-muscle cell by cAMP assayAgonist activity at beta2-adrenoceptor in human bronchial smooth-muscle cell by cAMP assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2012.07.096
CHEMBL1346 1292 39 None -2 6 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at beta2-adrenoceptor in human bronchial smooth-muscle cell by cAMP assayAgonist activity at beta2-adrenoceptor in human bronchial smooth-muscle cell by cAMP assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2012.07.096
DB00496 1292 39 None -2 6 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at beta2-adrenoceptor in human bronchial smooth-muscle cell by cAMP assayAgonist activity at beta2-adrenoceptor in human bronchial smooth-muscle cell by cAMP assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2012.07.096
45269924 193767 0 None - 1 Guinea pig 8.7 pEC50 = 8.7 Functional
Agonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring assessed as bronchorelaxation activity against carbachol-induced contractionAgonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring assessed as bronchorelaxation activity against carbachol-induced contraction
ChEMBL 283 6 5 6 -0.1 CC(C)(C)NC[C@@H](O)c1ccc(OB(O)O)c(CO)c1 10.1016/j.ejmech.2008.12.016
CHEMBL552398 193767 0 None - 1 Guinea pig 8.7 pEC50 = 8.7 Functional
Agonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring assessed as bronchorelaxation activity against carbachol-induced contractionAgonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring assessed as bronchorelaxation activity against carbachol-induced contraction
ChEMBL 283 6 5 6 -0.1 CC(C)(C)NC[C@@H](O)c1ccc(OB(O)O)c(CO)c1 10.1016/j.ejmech.2008.12.016
54580129 61451 0 None 3 2 Guinea pig 8.7 pEC50 = 8.7 Functional
Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as bronchorelaxation activity against histamine-induced contractionAgonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as bronchorelaxation activity against histamine-induced contraction
ChEMBL 786 21 6 8 7.0 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCCNC(=O)Cc2cccc(CC(C)(C)NC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)c2)ccc1O)C(C)C 10.1016/j.bmcl.2010.10.132
CHEMBL1773197 61451 0 None 3 2 Guinea pig 8.7 pEC50 = 8.7 Functional
Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as bronchorelaxation activity against histamine-induced contractionAgonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as bronchorelaxation activity against histamine-induced contraction
ChEMBL 786 21 6 8 7.0 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCCNC(=O)Cc2cccc(CC(C)(C)NC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)c2)ccc1O)C(C)C 10.1016/j.bmcl.2010.10.132
44392534 64892 0 None 1 2 Human 8.7 pEC50 = 8.7 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-2 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-2 adrenergic receptor
ChEMBL 443 11 4 6 3.4 C=CCNc1cccc([C@@H](O)CN[C@H](C)Cc2c[nH]c3c(OS(C)(=O)=O)cccc23)c1 10.1016/j.bmcl.2004.12.033
CHEMBL182689 64892 0 None 1 2 Human 8.7 pEC50 = 8.7 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-2 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-2 adrenergic receptor
ChEMBL 443 11 4 6 3.4 C=CCNc1cccc([C@@H](O)CN[C@H](C)Cc2c[nH]c3c(OS(C)(=O)=O)cccc23)c1 10.1016/j.bmcl.2004.12.033
156014385 177765 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 356 7 4 5 2.3 Cc1ccc(CCCNCC(O)c2cc(O)cc3c2OCC(=O)N3)cc1 10.1016/j.bmc.2019.115178
CHEMBL4636080 177765 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 356 7 4 5 2.3 Cc1ccc(CCCNCC(O)c2cc(O)cc3c2OCC(=O)N3)cc1 10.1016/j.bmc.2019.115178
CHEMBL4651252 177765 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 356 7 4 5 2.3 Cc1ccc(CCCNCC(O)c2cc(O)cc3c2OCC(=O)N3)cc1 10.1016/j.bmc.2019.115178
156015552 177709 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 328 6 4 5 1.6 O=C1COc2c(cc(O)cc2C(O)CNCCc2ccccc2)N1 10.1016/j.bmc.2019.115178
CHEMBL4641339 177709 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 328 6 4 5 1.6 O=C1COc2c(cc(O)cc2C(O)CNCCc2ccccc2)N1 10.1016/j.bmc.2019.115178
CHEMBL4650961 177709 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 328 6 4 5 1.6 O=C1COc2c(cc(O)cc2C(O)CNCCc2ccccc2)N1 10.1016/j.bmc.2019.115178
44419254 82717 0 None 4 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP levelsAgonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP levels
ChEMBL 587 14 4 8 4.5 CC(C)(Cc1ccc(Oc2ccc(C(N)=O)cn2)cc1)NC[C@H](O)COc1cccc2[nH]c(=O)n(CCC3CCCC3)c12 10.1016/j.bmcl.2006.08.010
CHEMBL218210 82717 0 None 4 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP levelsAgonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP levels
ChEMBL 587 14 4 8 4.5 CC(C)(Cc1ccc(Oc2ccc(C(N)=O)cn2)cc1)NC[C@H](O)COc1cccc2[nH]c(=O)n(CCC3CCCC3)c12 10.1016/j.bmcl.2006.08.010
53239456 61474 0 None 1 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as stimulation of intracellular cAMP production after 30 mins of washing by wash-off assayAgonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as stimulation of intracellular cAMP production after 30 mins of washing by wash-off assay
ChEMBL 705 19 5 7 7.8 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCCCOc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)ccc1O)C(C)C 10.1016/j.bmcl.2010.10.132
CHEMBL1773267 61474 0 None 1 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as stimulation of intracellular cAMP production after 30 mins of washing by wash-off assayAgonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as stimulation of intracellular cAMP production after 30 mins of washing by wash-off assay
ChEMBL 705 19 5 7 7.8 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCCCOc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)ccc1O)C(C)C 10.1016/j.bmcl.2010.10.132
53239456 61474 0 None 1 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as stumulation of intracellular cAMP productionAgonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as stumulation of intracellular cAMP production
ChEMBL 705 19 5 7 7.8 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCCCOc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)ccc1O)C(C)C 10.1016/j.bmcl.2015.10.008
CHEMBL1773267 61474 0 None 1 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as stumulation of intracellular cAMP productionAgonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as stumulation of intracellular cAMP production
ChEMBL 705 19 5 7 7.8 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCCCOc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)ccc1O)C(C)C 10.1016/j.bmcl.2015.10.008
46232768 197943 0 None 14 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 356 6 4 5 2.4 CC(C)(Cc1ccccc1)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmcl.2009.12.087
CHEMBL592879 197943 0 None 14 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 356 6 4 5 2.4 CC(C)(Cc1ccccc1)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmcl.2009.12.087
56658244 66060 0 None -1 4 Guinea pig 8.6 pEC50 = 8.6 Functional
Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contractionAgonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contraction
ChEMBL 513 17 5 7 3.2 O=C1CN(c2cccc(CCCCOCCCCCCNC[C@H](O)c3ccc(O)c(CO)c3)c2)C(=O)N1 10.1016/j.bmc.2011.05.064
CHEMBL1814272 66060 0 None -1 4 Guinea pig 8.6 pEC50 = 8.6 Functional
Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contractionAgonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contraction
ChEMBL 513 17 5 7 3.2 O=C1CN(c2cccc(CCCCOCCCCCCNC[C@H](O)c3ccc(O)c(CO)c3)c2)C(=O)N1 10.1016/j.bmc.2011.05.064
CHEMBL1851849 66060 0 None -1 4 Guinea pig 8.6 pEC50 = 8.6 Functional
Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contractionAgonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contraction
ChEMBL 513 17 5 7 3.2 O=C1CN(c2cccc(CCCCOCCCCCCNC[C@H](O)c3ccc(O)c(CO)c3)c2)C(=O)N1 10.1016/j.bmc.2011.05.064
10238776 66128 0 None -3 4 Guinea pig 8.6 pEC50 = 8.6 Functional
Agonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile responseAgonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response
ChEMBL 473 17 6 6 3.6 NC(=O)Nc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.08.043
CHEMBL1835853 66128 0 None -3 4 Guinea pig 8.6 pEC50 = 8.6 Functional
Agonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile responseAgonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response
ChEMBL 473 17 6 6 3.6 NC(=O)Nc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.08.043
CHEMBL1852214 66128 0 None -3 4 Guinea pig 8.6 pEC50 = 8.6 Functional
Agonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile responseAgonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response
ChEMBL 473 17 6 6 3.6 NC(=O)Nc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.08.043
56675509 64150 0 None 79 3 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 513 17 5 7 3.2 O=C1CNC(=O)N1c1ccccc1CCCCOCCCCCCNC[C@H](O)c1ccc(O)c(CO)c1 10.1016/j.bmc.2011.05.064
CHEMBL1814270 64150 0 None 79 3 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 513 17 5 7 3.2 O=C1CNC(=O)N1c1ccccc1CCCCOCCCCCCNC[C@H](O)c1ccc(O)c(CO)c1 10.1016/j.bmc.2011.05.064
56658244 66060 0 None 1 4 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 513 17 5 7 3.2 O=C1CN(c2cccc(CCCCOCCCCCCNC[C@H](O)c3ccc(O)c(CO)c3)c2)C(=O)N1 10.1016/j.bmc.2011.05.064
CHEMBL1814272 66060 0 None 1 4 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 513 17 5 7 3.2 O=C1CN(c2cccc(CCCCOCCCCCCNC[C@H](O)c3ccc(O)c(CO)c3)c2)C(=O)N1 10.1016/j.bmc.2011.05.064
CHEMBL1851849 66060 0 None 1 4 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 513 17 5 7 3.2 O=C1CN(c2cccc(CCCCOCCCCCCNC[C@H](O)c3ccc(O)c(CO)c3)c2)C(=O)N1 10.1016/j.bmc.2011.05.064
56670092 63758 0 None 112 3 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 445 13 4 7 2.5 CN(CCOCCCNC[C@H](O)c1ccc(O)c2[nH]c(=O)sc12)CCc1ccccc1 10.1016/j.bmcl.2011.05.097
CHEMBL1807874 63758 0 None 112 3 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 445 13 4 7 2.5 CN(CCOCCCNC[C@H](O)c1ccc(O)c2[nH]c(=O)sc12)CCc1ccccc1 10.1016/j.bmcl.2011.05.097
1239 1639 46 None -1 5 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assayAgonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1021/ml4005232
3410 1639 46 None -1 5 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assayAgonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1021/ml4005232
3465 1639 46 None -1 5 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assayAgonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1021/ml4005232
CHEMBL1256786 1639 46 None -1 5 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assayAgonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1021/ml4005232
DB00983 1639 46 None -1 5 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assayAgonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1021/ml4005232
145987415 166684 0 None 1258 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 358 6 4 4 2.8 O=c1ccc2c(C(CO)NCCc3cccc(Cl)c3)ccc(O)c2[nH]1 10.1016/j.ejmech.2018.04.041
CHEMBL4292648 166684 0 None 1258 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 358 6 4 4 2.8 O=c1ccc2c(C(CO)NCCc3cccc(Cl)c3)ccc(O)c2[nH]1 10.1016/j.ejmech.2018.04.041
155540608 172359 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 493 11 5 5 4.9 CC(CC(=O)Nc1ccc(CCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)cc1)CC(C)(C)C 10.1016/j.bmc.2018.10.043
CHEMBL4516838 172359 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 493 11 5 5 4.9 CC(CC(=O)Nc1ccc(CCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)cc1)CC(C)(C)C 10.1016/j.bmc.2018.10.043
1239 1639 46 None -1 5 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.04.095
3410 1639 46 None -1 5 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.04.095
3465 1639 46 None -1 5 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.04.095
CHEMBL1256786 1639 46 None -1 5 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.04.095
DB00983 1639 46 None -1 5 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.04.095
90645345 111974 0 None 11 3 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 574 12 6 8 4.7 CC(C)(C)OC(=O)NCCOc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 10.1016/j.bmcl.2014.04.095
CHEMBL3298692 111974 0 None 11 3 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 574 12 6 8 4.7 CC(C)(C)OC(=O)NCCOc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 10.1016/j.bmcl.2014.04.095
57400229 70030 0 None 5 4 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 497 12 5 7 3.5 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCOc3cccc(CNCCc4ccccc4F)c3)c2s1 10.1016/j.bmcl.2011.10.049
CHEMBL1945298 70030 0 None 5 4 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 497 12 5 7 3.5 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCOc3cccc(CNCCc4ccccc4F)c3)c2s1 10.1016/j.bmcl.2011.10.049
57401435 70042 0 None 31 3 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 458 11 5 6 2.8 O=c1ccc2c([C@@H](O)CNCCc3cccc(CNCCc4ccccn4)c3)ccc(O)c2[nH]1 10.1016/j.bmcl.2011.10.049
CHEMBL1945503 70042 0 None 31 3 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 458 11 5 6 2.8 O=c1ccc2c([C@@H](O)CNCCc3cccc(CNCCc4ccccn4)c3)ccc(O)c2[nH]1 10.1016/j.bmcl.2011.10.049
1239 1639 46 None -1 5 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human beta2 receptor in BEAS-2B cells assessed as cAMP accumulation by radioimmunoassayAgonist activity at human beta2 receptor in BEAS-2B cells assessed as cAMP accumulation by radioimmunoassay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.04.069
3410 1639 46 None -1 5 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human beta2 receptor in BEAS-2B cells assessed as cAMP accumulation by radioimmunoassayAgonist activity at human beta2 receptor in BEAS-2B cells assessed as cAMP accumulation by radioimmunoassay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.04.069
3465 1639 46 None -1 5 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human beta2 receptor in BEAS-2B cells assessed as cAMP accumulation by radioimmunoassayAgonist activity at human beta2 receptor in BEAS-2B cells assessed as cAMP accumulation by radioimmunoassay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.04.069
CHEMBL1256786 1639 46 None -1 5 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human beta2 receptor in BEAS-2B cells assessed as cAMP accumulation by radioimmunoassayAgonist activity at human beta2 receptor in BEAS-2B cells assessed as cAMP accumulation by radioimmunoassay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.04.069
DB00983 1639 46 None -1 5 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human beta2 receptor in BEAS-2B cells assessed as cAMP accumulation by radioimmunoassayAgonist activity at human beta2 receptor in BEAS-2B cells assessed as cAMP accumulation by radioimmunoassay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.04.069
42625898 184663 0 None 125 3 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 591 17 7 9 1.5 NS(=O)(=O)O.NS(=O)(=O)c1cccc(CCCOCCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
CHEMBL485847 184663 0 None 125 3 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 591 17 7 9 1.5 NS(=O)(=O)O.NS(=O)(=O)c1cccc(CCCOCCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
46832801 14074 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 431 16 4 6 3.6 Cc1ccc(COCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc1 10.1021/jm100326d
CHEMBL1084649 14074 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 431 16 4 6 3.6 Cc1ccc(COCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc1 10.1021/jm100326d
CHEMBL1198880 14074 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 431 16 4 6 3.6 Cc1ccc(COCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc1 10.1021/jm100326d
46832803 14075 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 451 16 4 6 4.0 OCc1cc([C@@H](O)CNCCCCCCOCCOCc2ccc(Cl)cc2)ccc1O 10.1021/jm100326d
CHEMBL1084654 14075 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 451 16 4 6 4.0 OCc1cc([C@@H](O)CNCCCCCCOCCOCc2ccc(Cl)cc2)ccc1O 10.1021/jm100326d
CHEMBL1198881 14075 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 451 16 4 6 4.0 OCc1cc([C@@H](O)CNCCCCCCOCCOCc2ccc(Cl)cc2)ccc1O 10.1021/jm100326d
46832505 14105 0 None 12 3 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 417 16 4 6 3.3 OCc1cc([C@@H](O)CNCCCCCCOCCOCc2ccccc2)ccc1O 10.1021/jm100326d
CHEMBL1085395 14105 0 None 12 3 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 417 16 4 6 3.3 OCc1cc([C@@H](O)CNCCCCCCOCCOCc2ccccc2)ccc1O 10.1021/jm100326d
CHEMBL1199261 14105 0 None 12 3 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 417 16 4 6 3.3 OCc1cc([C@@H](O)CNCCCCCCOCCOCc2ccccc2)ccc1O 10.1021/jm100326d
59119467 111749 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 428 9 5 5 4.6 OCc1cc(C(O)CNCCc2ccc(Nc3ccc4ccccc4c3)cc2)ccc1O 10.1016/j.bmcl.2014.04.069
CHEMBL3290983 111749 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 428 9 5 5 4.6 OCc1cc(C(O)CNCCc2ccc(Nc3ccc4ccccc4c3)cc2)ccc1O 10.1016/j.bmcl.2014.04.069
90644139 111759 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 424 10 5 6 4.2 CSc1ccc(Nc2ccc(CCNCC(O)c3ccc(O)c(CO)c3)cc2)cc1 10.1016/j.bmcl.2014.04.069
CHEMBL3290992 111759 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 424 10 5 6 4.2 CSc1ccc(Nc2ccc(CCNCC(O)c3ccc(O)c(CO)c3)cc2)cc1 10.1016/j.bmcl.2014.04.069
59119410 111760 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 436 11 5 6 4.3 CC(C)Oc1ccc(Nc2ccc(CCNCC(O)c3ccc(O)c(CO)c3)cc2)cc1 10.1016/j.bmcl.2014.04.069
CHEMBL3290993 111760 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 436 11 5 6 4.3 CC(C)Oc1ccc(Nc2ccc(CCNCC(O)c3ccc(O)c(CO)c3)cc2)cc1 10.1016/j.bmcl.2014.04.069
57391347 69868 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 436 11 6 6 3.2 Cc1ccc(C(O)CNc2ccc(CCNCC(O)c3ccc(O)c(CO)c3)cc2)cc1 10.1016/j.bmcl.2011.11.072
CHEMBL1940825 69868 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 436 11 6 6 3.2 Cc1ccc(C(O)CNc2ccc(CCNCC(O)c3ccc(O)c(CO)c3)cc2)cc1 10.1016/j.bmcl.2011.11.072
44434117 89305 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
ChEMBL 561 13 5 8 4.1 CCn1c(C(=O)NCc2c(OC)cccc2OC)cc2cc(C[C@@H](C)NC[C@H](O)c3ccc(O)c(CO)c3)ccc21 10.1016/j.bmcl.2007.09.031
CHEMBL237709 89305 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
ChEMBL 561 13 5 8 4.1 CCn1c(C(=O)NCc2c(OC)cccc2OC)cc2cc(C[C@@H](C)NC[C@H](O)c3ccc(O)c(CO)c3)ccc21 10.1016/j.bmcl.2007.09.031
10348864 58216 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
ChEMBL 616 18 5 7 6.7 O=CNc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)ccc1O 10.1016/j.bmcl.2011.01.043
CHEMBL1683935 58216 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
ChEMBL 616 18 5 7 6.7 O=CNc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)ccc1O 10.1016/j.bmcl.2011.01.043
3083544 462 46 None 1 4 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technologyAgonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technology
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O 10.1021/acs.jmedchem.0c01195
4943 462 46 None 1 4 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technologyAgonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technology
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O 10.1021/acs.jmedchem.0c01195
7479 462 46 None 1 4 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technologyAgonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technology
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O 10.1021/acs.jmedchem.0c01195
CHEMBL1363 462 46 None 1 4 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technologyAgonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technology
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O 10.1021/acs.jmedchem.0c01195
DB01274 462 46 None 1 4 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technologyAgonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technology
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O 10.1021/acs.jmedchem.0c01195
16735272 85371 0 None 57 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assayAgonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assay
ChEMBL 337 6 4 4 3.5 C[C@@H](Cc1cccc2ccccc12)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2009.11.062
CHEMBL229614 85371 0 None 57 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assayAgonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assay
ChEMBL 337 6 4 4 3.5 C[C@@H](Cc1cccc2ccccc12)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2009.11.062
45483815 196755 0 None 11 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 400 7 5 6 2.1 CC(C)(Cc1ccc(C(=O)O)cc1)NCC(O)c1ccc(O)c2c1OCC(=O)N2 10.1016/j.bmcl.2009.10.013
CHEMBL577289 196755 0 None 11 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 400 7 5 6 2.1 CC(C)(Cc1ccc(C(=O)O)cc1)NCC(O)c1ccc(O)c2c1OCC(=O)N2 10.1016/j.bmcl.2009.10.013
53380559 63295 0 None 4265 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assayAgonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assay
ChEMBL 317 7 5 5 2.4 CC[C@H](Cc1ccc(O)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2009.11.062
CHEMBL1800936 63295 0 None 4265 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assayAgonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assay
ChEMBL 317 7 5 5 2.4 CC[C@H](Cc1ccc(O)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2009.11.062
45375919 195326 0 None 87 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 400 7 5 6 2.1 CC(C)(Cc1cccc(C(=O)O)c1)NCC(O)c1ccc(O)c2c1OCC(=O)N2 10.1016/j.bmcl.2009.10.013
CHEMBL566973 195326 0 None 87 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 400 7 5 6 2.1 CC(C)(Cc1cccc(C(=O)O)c1)NCC(O)c1ccc(O)c2c1OCC(=O)N2 10.1016/j.bmcl.2009.10.013
164615990 184710 0 None 831 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as increase in cAMP level incubated for 30 mins by immunoassayAgonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as increase in cAMP level incubated for 30 mins by immunoassay
ChEMBL 427 9 5 6 1.6 CN(C)C(=O)CNc1ccc2c(c1)C[C@@H](NC[C@H](O)c1ccc(O)c(CCO)c1)CC2 10.1021/acs.jmedchem.0c01195
CHEMBL4859326 184710 0 None 831 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as increase in cAMP level incubated for 30 mins by immunoassayAgonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as increase in cAMP level incubated for 30 mins by immunoassay
ChEMBL 427 9 5 6 1.6 CN(C)C(=O)CNc1ccc2c(c1)C[C@@H](NC[C@H](O)c1ccc(O)c(CCO)c1)CC2 10.1021/acs.jmedchem.0c01195
45375919 195326 0 None 87 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 400 7 5 6 2.1 CC(C)(Cc1cccc(C(=O)O)c1)NCC(O)c1ccc(O)c2c1OCC(=O)N2 10.1016/j.bmcl.2009.12.087
CHEMBL566973 195326 0 None 87 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 400 7 5 6 2.1 CC(C)(Cc1cccc(C(=O)O)c1)NCC(O)c1ccc(O)c2c1OCC(=O)N2 10.1016/j.bmcl.2009.12.087
44396531 66486 0 None -38 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at Homo sapiens (human) beta2 adrenoreceptorAgonist activity at Homo sapiens (human) beta2 adrenoreceptor
ChEMBL 647 18 4 8 6.4 CCCCCCCCS(=O)(=O)Oc1cccc2c(C[C@@H](C)NC[C@H](O)c3cccc(NS(=O)(=O)c4cccs4)c3)c[nH]c12 10.1007/s00044-009-9257-x
CHEMBL186135 66486 0 None -38 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at Homo sapiens (human) beta2 adrenoreceptorAgonist activity at Homo sapiens (human) beta2 adrenoreceptor
ChEMBL 647 18 4 8 6.4 CCCCCCCCS(=O)(=O)Oc1cccc2c(C[C@@H](C)NC[C@H](O)c3cccc(NS(=O)(=O)c4cccs4)c3)c[nH]c12 10.1007/s00044-009-9257-x
443372 10123 23 None -9 8 Golden hamster 7.7 pEC50 = 7.7 Functional
Agonist activity at adrenergic beta2 receptor in Syrian hamster DDT1 MF2 cells assessed as stimulation of cAMP accumulation by radioimmunoassay in presence of 1 uM DPCPXAgonist activity at adrenergic beta2 receptor in Syrian hamster DDT1 MF2 cells assessed as stimulation of cAMP accumulation by radioimmunoassay in presence of 1 uM DPCPX
ChEMBL 211 4 4 4 1.1 CC(C)NC[C@H](O)c1ccc(O)c(O)c1 10.1021/jm800613s
CHEMBL1160723 10123 23 None -9 8 Golden hamster 7.7 pEC50 = 7.7 Functional
Agonist activity at adrenergic beta2 receptor in Syrian hamster DDT1 MF2 cells assessed as stimulation of cAMP accumulation by radioimmunoassay in presence of 1 uM DPCPXAgonist activity at adrenergic beta2 receptor in Syrian hamster DDT1 MF2 cells assessed as stimulation of cAMP accumulation by radioimmunoassay in presence of 1 uM DPCPX
ChEMBL 211 4 4 4 1.1 CC(C)NC[C@H](O)c1ccc(O)c(O)c1 10.1021/jm800613s
CHEMBL2062275 10123 23 None -9 8 Golden hamster 7.7 pEC50 = 7.7 Functional
Agonist activity at adrenergic beta2 receptor in Syrian hamster DDT1 MF2 cells assessed as stimulation of cAMP accumulation by radioimmunoassay in presence of 1 uM DPCPXAgonist activity at adrenergic beta2 receptor in Syrian hamster DDT1 MF2 cells assessed as stimulation of cAMP accumulation by radioimmunoassay in presence of 1 uM DPCPX
ChEMBL 211 4 4 4 1.1 CC(C)NC[C@H](O)c1ccc(O)c(O)c1 10.1021/jm800613s
45483830 195310 0 None 14 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 329 7 4 4 2.8 Cc1ccccc1CC(C)(C)NCC(O)c1ccc(O)c(CO)c1 10.1016/j.bmcl.2009.10.013
CHEMBL566777 195310 0 None 14 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 329 7 4 4 2.8 Cc1ccccc1CC(C)(C)NCC(O)c1ccc(O)c(CO)c1 10.1016/j.bmcl.2009.10.013
90666115 108847 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP productionAgonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP production
ChEMBL 702 17 6 9 6.5 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3ccc(O)c(Cl)c3)CC2)ccc1O 10.1039/C1MD00140J
CHEMBL3219048 108847 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP productionAgonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP production
ChEMBL 702 17 6 9 6.5 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3ccc(O)c(Cl)c3)CC2)ccc1O 10.1039/C1MD00140J
9933039 162483 0 None 1 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 442 11 4 6 2.8 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1)c1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL417613 162483 0 None 1 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 442 11 4 6 2.8 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1)c1ccccc1 10.1016/j.bmc.2009.06.031
45271517 193371 0 None 3 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 499 10 4 4 4.8 O[C@@H](CNCCc1ccc(NC(=S)Nc2ccc(Br)cc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL1203998 193371 0 None 3 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 499 10 4 4 4.8 O[C@@H](CNCCc1ccc(NC(=S)Nc2ccc(Br)cc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL549487 193371 0 None 3 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 499 10 4 4 4.8 O[C@@H](CNCCc1ccc(NC(=S)Nc2ccc(Br)cc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
45270690 193441 0 None 3 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 466 11 4 6 4.0 O=[N+]([O-])c1ccccc1NC(=S)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.06.031
CHEMBL1203994 193441 0 None 3 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 466 11 4 6 4.0 O=[N+]([O-])c1ccccc1NC(=S)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.06.031
CHEMBL550037 193441 0 None 3 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 466 11 4 6 4.0 O=[N+]([O-])c1ccccc1NC(=S)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.06.031
44517694 193491 0 None 3 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 451 11 4 5 4.1 COc1cccc(NC(=S)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)c1 10.1016/j.bmc.2009.06.031
CHEMBL1203996 193491 0 None 3 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 451 11 4 5 4.1 COc1cccc(NC(=S)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)c1 10.1016/j.bmc.2009.06.031
CHEMBL550445 193491 0 None 3 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 451 11 4 5 4.1 COc1cccc(NC(=S)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)c1 10.1016/j.bmc.2009.06.031
44517696 194088 0 None 3 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 451 11 4 5 4.1 COc1ccc(NC(=S)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)cc1 10.1016/j.bmc.2009.06.031
CHEMBL1204007 194088 0 None 3 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 451 11 4 5 4.1 COc1ccc(NC(=S)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)cc1 10.1016/j.bmc.2009.06.031
CHEMBL557705 194088 0 None 3 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 451 11 4 5 4.1 COc1ccc(NC(=S)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)cc1 10.1016/j.bmc.2009.06.031
44517692 194984 0 None 4 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 466 11 4 6 4.0 O=[N+]([O-])c1ccc(NC(=S)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)cc1 10.1016/j.bmc.2009.06.031
CHEMBL1203990 194984 0 None 4 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 466 11 4 6 4.0 O=[N+]([O-])c1ccc(NC(=S)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)cc1 10.1016/j.bmc.2009.06.031
CHEMBL564516 194984 0 None 4 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 466 11 4 6 4.0 O=[N+]([O-])c1ccc(NC(=S)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)cc1 10.1016/j.bmc.2009.06.031
44331443 4368 0 None 1 3 Human 7.7 pEC50 = 7.7 Functional
Beta-2 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-2-adrenoceptorBeta-2 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-2-adrenoceptor
ChEMBL 689 14 7 9 2.3 CS(=O)(=O)Nc1cc([C@@H](O)CNCC2CCN(S(=O)(=O)c3ccc(NC(=O)N[C@@H](Cc4ccccc4)C(=O)O)cc3)CC2)ccc1O 10.1016/s0960-894x(02)00608-x
CHEMBL101674 4368 0 None 1 3 Human 7.7 pEC50 = 7.7 Functional
Beta-2 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-2-adrenoceptorBeta-2 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-2-adrenoceptor
ChEMBL 689 14 7 9 2.3 CS(=O)(=O)Nc1cc([C@@H](O)CNCC2CCN(S(=O)(=O)c3ccc(NC(=O)N[C@@H](Cc4ccccc4)C(=O)O)cc3)CC2)ccc1O 10.1016/s0960-894x(02)00608-x
3931 2208 42 None -691 4 Human 7.7 pEC50 = 7.7 Functional
Increased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 2 adrenergic receptorsIncreased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 2 adrenergic receptors
ChEMBL 584 17 6 7 4.5 CCCCCCNC(=O)Nc1ccc(cc1)S(=O)(=O)Nc1ccc(cc1)CCNC[C@@H](COc1ccc(cc1)O)O 10.1021/jm000544b
9829836 2208 42 None -691 4 Human 7.7 pEC50 = 7.7 Functional
Increased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 2 adrenergic receptorsIncreased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 2 adrenergic receptors
ChEMBL 584 17 6 7 4.5 CCCCCCNC(=O)Nc1ccc(cc1)S(=O)(=O)Nc1ccc(cc1)CCNC[C@@H](COc1ccc(cc1)O)O 10.1021/jm000544b
CHEMBL12998 2208 42 None -691 4 Human 7.7 pEC50 = 7.7 Functional
Increased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 2 adrenergic receptorsIncreased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 2 adrenergic receptors
ChEMBL 584 17 6 7 4.5 CCCCCCNC(=O)Nc1ccc(cc1)S(=O)(=O)Nc1ccc(cc1)CCNC[C@@H](COc1ccc(cc1)O)O 10.1021/jm000544b
10697841 162307 0 None 4 2 Human 7.7 pEC50 = 7.7 Functional
Increased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 2 adrenergic receptorsIncreased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 2 adrenergic receptors
ChEMBL 546 9 5 8 1.7 CS(=O)(=O)Nc1cc([C@@H](O)CNC2CCN(c3ccc(C(=O)N4CCC[C@H]4C(=O)O)cc3)CC2)ccc1O 10.1021/jm000544b
CHEMBL417325 162307 0 None 4 2 Human 7.7 pEC50 = 7.7 Functional
Increased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 2 adrenergic receptorsIncreased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 2 adrenergic receptors
ChEMBL 546 9 5 8 1.7 CS(=O)(=O)Nc1cc([C@@H](O)CNC2CCN(c3ccc(C(=O)N4CCC[C@H]4C(=O)O)cc3)CC2)ccc1O 10.1021/jm000544b
2297789 40456 7 None - 1 Human 7.7 pEC50 = 7.7 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 469 11 2 6 4.8 CCCCN(CCCC)c1nc2ccccc2nc1NS(=O)(=O)c1ccc(NC(C)=O)cc1 nan
CHEMBL1484690 40456 7 None - 1 Human 7.7 pEC50 = 7.7 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 469 11 2 6 4.8 CCCCN(CCCC)c1nc2ccccc2nc1NS(=O)(=O)c1ccc(NC(C)=O)cc1 nan
1913590 19567 7 None - 1 Human 7.7 pEC50 = 7.7 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 410 5 2 8 4.1 CC1(C)Cc2c(c(-c3ccco3)nc3sc4c(NCCCO)ncnc4c23)CO1 nan
CHEMBL1301481 19567 7 None - 1 Human 7.7 pEC50 = 7.7 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 410 5 2 8 4.1 CC1(C)Cc2c(c(-c3ccco3)nc3sc4c(NCCCO)ncnc4c23)CO1 nan
44610056 123460 0 None -1 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as stumulation of intracellular cAMP productionAgonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as stumulation of intracellular cAMP production
ChEMBL 704 14 5 9 5.5 O=c1ccc2c([C@@H](O)CNCCc3ccc(CCN4CCC(Cn5cnc([C@](O)(c6ccccc6)C6CCCCC6)n5)CC4)cc3)ccc(O)c2[nH]1 10.1016/j.bmcl.2015.10.008
CHEMBL3629360 123460 0 None -1 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as stumulation of intracellular cAMP productionAgonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as stumulation of intracellular cAMP production
ChEMBL 704 14 5 9 5.5 O=c1ccc2c([C@@H](O)CNCCc3ccc(CCN4CCC(Cn5cnc([C@](O)(c6ccccc6)C6CCCCC6)n5)CC4)cc3)ccc(O)c2[nH]1 10.1016/j.bmcl.2015.10.008
44331351 206390 0 None -645 3 Human 4.7 pEC50 = 4.7 Functional
Beta-2 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-2-adrenoceptorBeta-2 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-2-adrenoceptor
ChEMBL 610 13 6 8 2.7 CS(=O)(=O)Nc1cc([C@@H](O)CNCC2CCN(c3ccc(C(=O)N[C@@H](Cc4ccccc4)C(=O)O)cc3)CC2)ccc1O 10.1016/s0960-894x(02)00608-x
CHEMBL98088 206390 0 None -645 3 Human 4.7 pEC50 = 4.7 Functional
Beta-2 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-2-adrenoceptorBeta-2 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-2-adrenoceptor
ChEMBL 610 13 6 8 2.7 CS(=O)(=O)Nc1cc([C@@H](O)CNCC2CCN(c3ccc(C(=O)N[C@@H](Cc4ccccc4)C(=O)O)cc3)CC2)ccc1O 10.1016/s0960-894x(02)00608-x
44428086 149535 0 None -7 2 Rat 4.7 pEC50 = 4.7 Functional
Vasodilating activity against phenylephrine-induced contractions in rat thoracic aortaVasodilating activity against phenylephrine-induced contractions in rat thoracic aorta
ChEMBL 415 9 4 8 1.9 Cc1c(COc2ccc(CC(C)NCC(O)c3cc(O)cc(O)c3)cc2)no[n+]1[O-] 10.1021/jm0704595
CHEMBL395082 149535 0 None -7 2 Rat 4.7 pEC50 = 4.7 Functional
Vasodilating activity against phenylephrine-induced contractions in rat thoracic aortaVasodilating activity against phenylephrine-induced contractions in rat thoracic aorta
ChEMBL 415 9 4 8 1.9 Cc1c(COc2ccc(CC(C)NCC(O)c3cc(O)cc(O)c3)cc2)no[n+]1[O-] 10.1021/jm0704595
2952777 192988 7 None - 1 Human 6.7 pEC50 = 6.7 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory)
ChEMBL 443 6 1 6 6.0 CC(Oc1ccc(Cl)cc1Cl)c1nc(-c2ccc(NC(=O)c3ccco3)cc2)no1 nan
CHEMBL531401 192988 7 None - 1 Human 6.7 pEC50 = 6.7 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory)
ChEMBL 443 6 1 6 6.0 CC(Oc1ccc(Cl)cc1Cl)c1nc(-c2ccc(NC(=O)c3ccco3)cc2)no1 nan
666902 24765 9 None 213 2 Human 6.7 pEC50 = 6.7 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 451 8 1 7 5.3 Clc1ccc(OCc2nnc(SCc3nc4ccccc4[nH]3)n2Cc2ccco2)cc1 nan
CHEMBL1346316 24765 9 None 213 2 Human 6.7 pEC50 = 6.7 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 451 8 1 7 5.3 Clc1ccc(OCc2nnc(SCc3nc4ccccc4[nH]3)n2Cc2ccco2)cc1 nan
893042 51642 11 None - 1 Human 5.7 pEC50 = 5.7 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 331 5 1 6 2.3 CCn1c(SCC(=O)N2CCCC2)nnc1-c1ccc(N)cc1 nan
CHEMBL1586182 51642 11 None - 1 Human 5.7 pEC50 = 5.7 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 331 5 1 6 2.3 CCn1c(SCC(=O)N2CCCC2)nnc1-c1ccc(N)cc1 nan
90666116 108848 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP productionAgonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP production
ChEMBL 730 19 6 9 7.2 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3ccc(O)c(Cl)c3)CC2)ccc1O 10.1039/C1MD00140J
CHEMBL3219049 108848 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP productionAgonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP production
ChEMBL 730 19 6 9 7.2 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3ccc(O)c(Cl)c3)CC2)ccc1O 10.1039/C1MD00140J
59145957 123458 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as stumulation of intracellular cAMP productionAgonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as stumulation of intracellular cAMP production
ChEMBL 698 18 5 9 6.4 O=c1ccc2c([C@@H](O)CNCCCCCCCCCN3CCC(Cn4cnc(C(O)(c5ccccc5)C5CCCCC5)n4)CC3)ccc(O)c2[nH]1 10.1016/j.bmcl.2015.10.008
CHEMBL3629358 123458 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as stumulation of intracellular cAMP productionAgonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as stumulation of intracellular cAMP production
ChEMBL 698 18 5 9 6.4 O=c1ccc2c([C@@H](O)CNCCCCCCCCCN3CCC(Cn4cnc(C(O)(c5ccccc5)C5CCCCC5)n4)CC3)ccc(O)c2[nH]1 10.1016/j.bmcl.2015.10.008
44396532 66408 0 None -42 3 Human 7.7 pEC50 = 7.7 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptor
ChEMBL 455 9 4 5 4.3 C[C@H](Cc1c[nH]c2ccccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2004.10.035
CHEMBL185836 66408 0 None -42 3 Human 7.7 pEC50 = 7.7 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptor
ChEMBL 455 9 4 5 4.3 C[C@H](Cc1c[nH]c2ccccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2004.10.035
9997789 185709 0 None 107 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at beta2 adrenoceptor (unknown origin)Agonist activity at beta2 adrenoceptor (unknown origin)
ChEMBL 310 3 3 3 3.4 CC(C)(C)NC(CO)c1cc(Cl)c(N)c(C(F)(F)F)c1 10.1021/acs.jmedchem.0c01195
CHEMBL4874511 185709 0 None 107 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at beta2 adrenoceptor (unknown origin)Agonist activity at beta2 adrenoceptor (unknown origin)
ChEMBL 310 3 3 3 3.4 CC(C)(C)NC(CO)c1cc(Cl)c(N)c(C(F)(F)F)c1 10.1021/acs.jmedchem.0c01195
CHEMBL5192245 185709 0 None 107 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at beta2 adrenoceptor (unknown origin)Agonist activity at beta2 adrenoceptor (unknown origin)
ChEMBL 310 3 3 3 3.4 CC(C)(C)NC(CO)c1cc(Cl)c(N)c(C(F)(F)F)c1 10.1021/acs.jmedchem.0c01195
73057083 103785 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulationAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulation
ChEMBL 303 7 4 5 2.0 COc1ccc(CCNC[C@@H](O)c2cc(O)cc(O)c2)cc1 10.1016/j.bmc.2013.11.030
CHEMBL3099658 103785 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulationAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulation
ChEMBL 303 7 4 5 2.0 COc1ccc(CCNC[C@@H](O)c2cc(O)cc(O)c2)cc1 10.1016/j.bmc.2013.11.030
665098 19601 9 None - 1 Human 5.7 pEC50 = 5.7 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 384 7 0 6 4.7 CCn1c(COc2ccc(Cl)cc2)nnc1SCc1ccc(C#N)cc1 nan
CHEMBL1301877 19601 9 None - 1 Human 5.7 pEC50 = 5.7 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 384 7 0 6 4.7 CCn1c(COc2ccc(Cl)cc2)nnc1SCc1ccc(C#N)cc1 nan
6407382 44907 4 None - 1 Human 5.7 pEC50 = 5.7 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 527 4 1 6 5.8 Cc1cccc(Nc2nnc(-c3ccc(C(=O)N4C[C@H]5C[C@H](C4)c4cccc(=O)n4C5)cc3)c3ccccc23)c1 nan
CHEMBL1525540 44907 4 None - 1 Human 5.7 pEC50 = 5.7 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 527 4 1 6 5.8 Cc1cccc(Nc2nnc(-c3ccc(C(=O)N4C[C@H]5C[C@H](C4)c4cccc(=O)n4C5)cc3)c3ccccc23)c1 nan
1960 2805 64 None -436 13 Guinea pig 6.7 pEC50 = 6.7 Functional
Activity for Beta-2 adrenergic receptor was assessed from effect on relaxation of guinea pig trachea.Activity for Beta-2 adrenergic receptor was assessed from effect on relaxation of guinea pig trachea.
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00019a001
439260 2805 64 None -436 13 Guinea pig 6.7 pEC50 = 6.7 Functional
Activity for Beta-2 adrenergic receptor was assessed from effect on relaxation of guinea pig trachea.Activity for Beta-2 adrenergic receptor was assessed from effect on relaxation of guinea pig trachea.
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00019a001
505 2805 64 None -436 13 Guinea pig 6.7 pEC50 = 6.7 Functional
Activity for Beta-2 adrenergic receptor was assessed from effect on relaxation of guinea pig trachea.Activity for Beta-2 adrenergic receptor was assessed from effect on relaxation of guinea pig trachea.
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00019a001
CHEMBL1437 2805 64 None -436 13 Guinea pig 6.7 pEC50 = 6.7 Functional
Activity for Beta-2 adrenergic receptor was assessed from effect on relaxation of guinea pig trachea.Activity for Beta-2 adrenergic receptor was assessed from effect on relaxation of guinea pig trachea.
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00019a001
DB00368 2805 64 None -436 13 Guinea pig 6.7 pEC50 = 6.7 Functional
Activity for Beta-2 adrenergic receptor was assessed from effect on relaxation of guinea pig trachea.Activity for Beta-2 adrenergic receptor was assessed from effect on relaxation of guinea pig trachea.
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00019a001
16746244 48630 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 552 8 2 7 3.4 NC(=O)CC(NC(=O)c1ccc(Br)cc1)c1ccc(N2CCN(c3ccccn3)CC2)c([N+](=O)[O-])c1 nan
CHEMBL1559831 48630 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 552 8 2 7 3.4 NC(=O)CC(NC(=O)c1ccc(Br)cc1)c1ccc(N2CCN(c3ccccn3)CC2)c([N+](=O)[O-])c1 nan
2212788 27931 9 None - 1 Human 6.7 pEC50 = 6.7 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 490 10 1 7 4.2 C=CCn1c(CCNC(=O)c2cccs2)nnc1SCC(=O)c1ccc(Br)cc1 nan
CHEMBL1373386 27931 9 None - 1 Human 6.7 pEC50 = 6.7 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 490 10 1 7 4.2 C=CCn1c(CCNC(=O)c2cccs2)nnc1SCC(=O)c1ccc(Br)cc1 nan
3145649 39219 9 None 177 2 Human 6.7 pEC50 = 6.7 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 395 4 0 4 4.7 CC(Sc1nc(-c2ccccc2)cc(C(F)(F)F)n1)C(=O)N1CCCCC1 nan
CHEMBL1472233 39219 9 None 177 2 Human 6.7 pEC50 = 6.7 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 395 4 0 4 4.7 CC(Sc1nc(-c2ccccc2)cc(C(F)(F)F)n1)C(=O)N1CCCCC1 nan
3986625 42924 4 None - 1 Human 5.7 pEC50 = 5.7 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 344 4 1 3 3.7 Cc1ccc(NC(=O)C(c2ccc(Cl)cc2)N2CCOCC2)cc1 nan
CHEMBL1505690 42924 4 None - 1 Human 5.7 pEC50 = 5.7 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 344 4 1 3 3.7 Cc1ccc(NC(=O)C(c2ccc(Cl)cc2)N2CCOCC2)cc1 nan
44396715 67097 0 None -20 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at Homo sapiens (human) beta2 adrenoreceptorAgonist activity at Homo sapiens (human) beta2 adrenoreceptor
ChEMBL 612 12 4 9 4.4 C[C@H](Cc1c[nH]c2c(OS(=O)(=O)c3cccnc3)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1007/s00044-009-9257-x
CHEMBL189081 67097 0 None -20 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at Homo sapiens (human) beta2 adrenoreceptorAgonist activity at Homo sapiens (human) beta2 adrenoreceptor
ChEMBL 612 12 4 9 4.4 C[C@H](Cc1c[nH]c2c(OS(=O)(=O)c3cccnc3)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1007/s00044-009-9257-x
90666110 108840 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP productionAgonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP production
ChEMBL 718 18 6 9 6.5 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3cc(F)c(O)cc3F)CC2)ccc1O 10.1039/C1MD00140J
CHEMBL3219041 108840 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP productionAgonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP production
ChEMBL 718 18 6 9 6.5 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3cc(F)c(O)cc3F)CC2)ccc1O 10.1039/C1MD00140J
44428086 149535 0 None 7 2 Guinea pig 6.7 pEC50 = 6.7 Functional
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contractionAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction
ChEMBL 415 9 4 8 1.9 Cc1c(COc2ccc(CC(C)NCC(O)c3cc(O)cc(O)c3)cc2)no[n+]1[O-] 10.1021/jm0704595
CHEMBL395082 149535 0 None 7 2 Guinea pig 6.7 pEC50 = 6.7 Functional
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contractionAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction
ChEMBL 415 9 4 8 1.9 Cc1c(COc2ccc(CC(C)NCC(O)c3cc(O)cc(O)c3)cc2)no[n+]1[O-] 10.1021/jm0704595
1165076 39694 4 None - 1 Human 6.7 pEC50 = 6.7 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 466 5 1 7 4.8 Cc1ccc(Cn2ccc(NC(=O)c3cc4nc(-c5ccco5)cc(C(F)(F)F)n4n3)n2)cc1 nan
CHEMBL1478198 39694 4 None - 1 Human 6.7 pEC50 = 6.7 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 466 5 1 7 4.8 Cc1ccc(Cn2ccc(NC(=O)c3cc4nc(-c5ccco5)cc(C(F)(F)F)n4n3)n2)cc1 nan
44428085 92816 0 None - 1 Guinea pig 5.7 pEC50 = 5.7 Functional
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contractionAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction
ChEMBL 399 9 4 8 2.6 Cc1nonc1COc1ccc(CC(C)NCC(O)c2cc(O)cc(O)c2)cc1 10.1021/jm0704595
CHEMBL244906 92816 0 None - 1 Guinea pig 5.7 pEC50 = 5.7 Functional
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contractionAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction
ChEMBL 399 9 4 8 2.6 Cc1nonc1COc1ccc(CC(C)NCC(O)c2cc(O)cc(O)c2)cc1 10.1021/jm0704595
10221081 123568 1 None -186 3 Guinea pig 5.7 pEC50 = 5.7 Functional
Agonist activity at adrenergic beta2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of propranololAgonist activity at adrenergic beta2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of propranolol
ChEMBL 270 4 0 6 0.5 CCOc1no[n+]([O-])c1S(=O)(=O)c1ccccc1 10.1021/jm0704595
CHEMBL363325 123568 1 None -186 3 Guinea pig 5.7 pEC50 = 5.7 Functional
Agonist activity at adrenergic beta2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of propranololAgonist activity at adrenergic beta2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of propranolol
ChEMBL 270 4 0 6 0.5 CCOc1no[n+]([O-])c1S(=O)(=O)c1ccccc1 10.1021/jm0704595
24789160 35116 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 501 12 3 6 2.9 NC(=O)CC(NC(=O)Cc1ccc(Cl)cc1)c1ccc(NCCCN2CCCC2=O)c([N+](=O)[O-])c1 nan
CHEMBL1437255 35116 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 501 12 3 6 2.9 NC(=O)CC(NC(=O)Cc1ccc(Cl)cc1)c1ccc(NCCCN2CCCC2=O)c([N+](=O)[O-])c1 nan
44428083 92115 0 None 4 2 Guinea pig 4.7 pEC50 = 4.7 Functional
Agonist activity at adrenergic beta2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of propranololAgonist activity at adrenergic beta2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of propranolol
ChEMBL 444 10 5 9 0.7 CC(Cc1ccc(OCc2no[n+]([O-])c2C(N)=O)cc1)NCC(O)c1cc(O)cc(O)c1 10.1021/jm0704595
CHEMBL243266 92115 0 None 4 2 Guinea pig 4.7 pEC50 = 4.7 Functional
Agonist activity at adrenergic beta2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of propranololAgonist activity at adrenergic beta2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of propranolol
ChEMBL 444 10 5 9 0.7 CC(Cc1ccc(OCc2no[n+]([O-])c2C(N)=O)cc1)NCC(O)c1cc(O)cc(O)c1 10.1021/jm0704595
3119289 47214 4 None - 1 Human 6.7 pEC50 = 6.7 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 378 8 2 4 5.0 CCCCOc1cccc(C(=O)Nc2ccc(NC(=O)c3ccco3)cc2)c1 nan
CHEMBL1545591 47214 4 None - 1 Human 6.7 pEC50 = 6.7 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 378 8 2 4 5.0 CCCCOc1cccc(C(=O)Nc2ccc(NC(=O)c3ccco3)cc2)c1 nan
24789183 32636 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 552 8 2 7 3.4 NC(=O)CC(NC(=O)c1cccc(Br)c1)c1ccc(N2CCN(c3ccccn3)CC2)c([N+](=O)[O-])c1 nan
CHEMBL1414874 32636 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 552 8 2 7 3.4 NC(=O)CC(NC(=O)c1cccc(Br)c1)c1ccc(N2CCN(c3ccccn3)CC2)c([N+](=O)[O-])c1 nan
2234461 43512 9 None - 1 Human 6.7 pEC50 = 6.7 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory)
ChEMBL 432 7 1 6 2.7 COC(=O)c1ccc(NC(=O)COc2ccc(S(=O)(=O)N3CCCCC3)cc2)cc1 nan
CHEMBL1510834 43512 9 None - 1 Human 6.7 pEC50 = 6.7 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory)
ChEMBL 432 7 1 6 2.7 COC(=O)c1ccc(NC(=O)COc2ccc(S(=O)(=O)N3CCCCC3)cc2)cc1 nan
16279412 59044 5 None - 1 Human 6.6 pEC50 = 6.6 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 467 10 2 7 3.5 CCOc1ccccc1C(=O)NCC(=O)OCc1csc(CC(=O)Nc2ccc(C)cc2)n1 nan
CHEMBL1708092 59044 5 None - 1 Human 6.6 pEC50 = 6.6 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 467 10 2 7 3.5 CCOc1ccccc1C(=O)NCC(=O)OCc1csc(CC(=O)Nc2ccc(C)cc2)n1 nan
59707188 108845 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP productionAgonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP production
ChEMBL 734 18 6 9 7.0 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccc(F)cc3-c3ccc(O)c(Cl)c3)CC2)ccc1O 10.1039/C1MD00140J
CHEMBL3219046 108845 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP productionAgonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP production
ChEMBL 734 18 6 9 7.0 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccc(F)cc3-c3ccc(O)c(Cl)c3)CC2)ccc1O 10.1039/C1MD00140J
90666121 108854 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP productionAgonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP production
ChEMBL 742 18 6 9 7.4 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2C3CCC2CC(OC(=O)Nc2ccccc2-c2ccc(O)c(Cl)c2)C3)ccc1O 10.1039/C1MD00140J
CHEMBL3219054 108854 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP productionAgonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP production
ChEMBL 742 18 6 9 7.4 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2C3CCC2CC(OC(=O)Nc2ccccc2-c2ccc(O)c(Cl)c2)C3)ccc1O 10.1039/C1MD00140J
11324939 94014 0 None -6 2 Human 7.6 pEC50 = 7.6 Functional
Agonistic activity against human Beta-2 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonistic activity against human Beta-2 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 328 6 3 2 4.1 CC(Cc1c[nH]c2ccccc12)NCC(O)c1cccc(Cl)c1 10.1016/s0960-894x(03)00073-8
CHEMBL25133 94014 0 None -6 2 Human 7.6 pEC50 = 7.6 Functional
Agonistic activity against human Beta-2 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonistic activity against human Beta-2 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 328 6 3 2 4.1 CC(Cc1c[nH]c2ccccc12)NCC(O)c1cccc(Cl)c1 10.1016/s0960-894x(03)00073-8
659759 46992 10 None 14 2 Human 7.6 pEC50 = 7.6 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory)
ChEMBL 359 4 1 4 3.0 CC(=O)Nc1ccc(S(=O)(=O)N2CCCCC2c2cccnc2)cc1 nan
CHEMBL1543973 46992 10 None 14 2 Human 7.6 pEC50 = 7.6 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory)
ChEMBL 359 4 1 4 3.0 CC(=O)Nc1ccc(S(=O)(=O)N2CCCCC2c2cccnc2)cc1 nan
1854978 37465 8 None - 1 Human 7.6 pEC50 = 7.6 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory)
ChEMBL 422 5 1 7 5.5 CC(C)Cc1nc2sc3c(NCc4ccco4)ncnc3c2c2c1COC(C)(C)C2 nan
CHEMBL1457704 37465 8 None - 1 Human 7.6 pEC50 = 7.6 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory)
ChEMBL 422 5 1 7 5.5 CC(C)Cc1nc2sc3c(NCc4ccco4)ncnc3c2c2c1COC(C)(C)C2 nan
44428086 149535 0 None 7 2 Guinea pig 6.6 pEC50 = 6.6 Functional
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-oneAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-one
ChEMBL 415 9 4 8 1.9 Cc1c(COc2ccc(CC(C)NCC(O)c3cc(O)cc(O)c3)cc2)no[n+]1[O-] 10.1021/jm0704595
CHEMBL395082 149535 0 None 7 2 Guinea pig 6.6 pEC50 = 6.6 Functional
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-oneAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-one
ChEMBL 415 9 4 8 1.9 Cc1c(COc2ccc(CC(C)NCC(O)c3cc(O)cc(O)c3)cc2)no[n+]1[O-] 10.1021/jm0704595
10221081 123568 1 None -186 3 Guinea pig 5.6 pEC50 = 5.6 Functional
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contractionAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction
ChEMBL 270 4 0 6 0.5 CCOc1no[n+]([O-])c1S(=O)(=O)c1ccccc1 10.1021/jm0704595
CHEMBL363325 123568 1 None -186 3 Guinea pig 5.6 pEC50 = 5.6 Functional
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contractionAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction
ChEMBL 270 4 0 6 0.5 CCOc1no[n+]([O-])c1S(=O)(=O)c1ccccc1 10.1021/jm0704595
10028830 2206 33 None -1949 3 Human 4.6 pEC50 = 4.6 Functional
Antagonist activity at human beta2 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta2 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 497 13 4 6 2.7 O[C@H](COc1cccc(c1)CNC(=O)C)CNCCc1ccc(cc1)NS(=O)(=O)c1ccccc1 10.1016/j.ejmech.2018.03.032
3932 2206 33 None -1949 3 Human 4.6 pEC50 = 4.6 Functional
Antagonist activity at human beta2 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta2 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 497 13 4 6 2.7 O[C@H](COc1cccc(c1)CNC(=O)C)CNCCc1ccc(cc1)NS(=O)(=O)c1ccccc1 10.1016/j.ejmech.2018.03.032
CHEMBL4238084 2206 33 None -1949 3 Human 4.6 pEC50 = 4.6 Functional
Antagonist activity at human beta2 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta2 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 497 13 4 6 2.7 O[C@H](COc1cccc(c1)CNC(=O)C)CNCCc1ccc(cc1)NS(=O)(=O)c1ccccc1 10.1016/j.ejmech.2018.03.032
141286040 192390 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 290 4 3 3 2.2 CC(C)NC(CO)c1cc(F)c(N)c(Br)c1 10.1021/acs.jmedchem.1c02006
CHEMBL5203966 192390 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 290 4 3 3 2.2 CC(C)NC(CO)c1cc(F)c(N)c(Br)c1 10.1021/acs.jmedchem.1c02006
CHEMBL5222714 192390 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 290 4 3 3 2.2 CC(C)NC(CO)c1cc(F)c(N)c(Br)c1 10.1021/acs.jmedchem.1c02006
102139105 185739 0 None - 1 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at beta2 adrenoceptor in human A431 cells measured for 24 hrsAgonist activity at beta2 adrenoceptor in human A431 cells measured for 24 hrs
ChEMBL 392 10 5 7 2.5 COc1cc(CCC(O)CC(O)CCc2cc(O)c(O)c(OC)c2)ccc1O 10.1021/acs.jmedchem.0c01195
CHEMBL4874899 185739 0 None - 1 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at beta2 adrenoceptor in human A431 cells measured for 24 hrsAgonist activity at beta2 adrenoceptor in human A431 cells measured for 24 hrs
ChEMBL 392 10 5 7 2.5 COc1cc(CCC(O)CC(O)CCc2cc(O)c(O)c(OC)c2)ccc1O 10.1021/acs.jmedchem.0c01195
1499 2052 43 None -72 36 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation countingAgonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2011.11.054
3779 2052 43 None -72 36 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation countingAgonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2011.11.054
536 2052 43 None -72 36 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation countingAgonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2011.11.054
CHEMBL434 2052 43 None -72 36 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation countingAgonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2011.11.054
DB01064 2052 43 None -72 36 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation countingAgonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2011.11.054
90666118 108851 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP productionAgonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP production
ChEMBL 702 18 6 9 6.5 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CC[C@@H](OC(=O)Nc3ccccc3-c3ccc(O)c(Cl)c3)C2)ccc1O 10.1039/C1MD00140J
CHEMBL3219051 108851 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP productionAgonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP production
ChEMBL 702 18 6 9 6.5 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CC[C@@H](OC(=O)Nc3ccccc3-c3ccc(O)c(Cl)c3)C2)ccc1O 10.1039/C1MD00140J
1499 2052 43 None -72 36 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation countingAgonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2011.11.054
3779 2052 43 None -72 36 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation countingAgonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2011.11.054
536 2052 43 None -72 36 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation countingAgonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2011.11.054
CHEMBL434 2052 43 None -72 36 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation countingAgonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2011.11.054
DB01064 2052 43 None -72 36 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation countingAgonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2011.11.054
3038500 9235 8 None -575 6 Human 5.6 pEC50 = 5.6 Functional
In vitro functional efficacy in stimulating increase in cAMP in chinese hamster ovary (CHO) cells expressing the cloned human beta-2 receptor.In vitro functional efficacy in stimulating increase in cAMP in chinese hamster ovary (CHO) cells expressing the cloned human beta-2 receptor.
ChEMBL 624 11 3 7 6.6 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/jm000286i
CHEMBL111201 9235 8 None -575 6 Human 5.6 pEC50 = 5.6 Functional
In vitro functional efficacy in stimulating increase in cAMP in chinese hamster ovary (CHO) cells expressing the cloned human beta-2 receptor.In vitro functional efficacy in stimulating increase in cAMP in chinese hamster ovary (CHO) cells expressing the cloned human beta-2 receptor.
ChEMBL 624 11 3 7 6.6 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/jm000286i
44428083 92115 0 None 4 2 Guinea pig 4.6 pEC50 = 4.6 Functional
Agonist activity at adrenergic beta2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of propranololAgonist activity at adrenergic beta2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of propranolol
ChEMBL 444 10 5 9 0.7 CC(Cc1ccc(OCc2no[n+]([O-])c2C(N)=O)cc1)NCC(O)c1cc(O)cc(O)c1 10.1021/jm0704595
CHEMBL243266 92115 0 None 4 2 Guinea pig 4.6 pEC50 = 4.6 Functional
Agonist activity at adrenergic beta2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of propranololAgonist activity at adrenergic beta2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of propranolol
ChEMBL 444 10 5 9 0.7 CC(Cc1ccc(OCc2no[n+]([O-])c2C(N)=O)cc1)NCC(O)c1cc(O)cc(O)c1 10.1021/jm0704595
3145657 36437 13 None - 1 Human 6.6 pEC50 = 6.6 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 381 4 0 4 4.3 CC(Sc1nc(-c2ccccc2)cc(C(F)(F)F)n1)C(=O)N1CCCC1 nan
CHEMBL1449091 36437 13 None - 1 Human 6.6 pEC50 = 6.6 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 381 4 0 4 4.3 CC(Sc1nc(-c2ccccc2)cc(C(F)(F)F)n1)C(=O)N1CCCC1 nan
652434 53802 5 None - 1 Human 5.6 pEC50 = 5.6 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 399 6 1 8 3.7 CCOc1ccc2nc(NC(=O)CSc3nc4cccnc4n3C)sc2c1 nan
CHEMBL1606638 53802 5 None - 1 Human 5.6 pEC50 = 5.6 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 399 6 1 8 3.7 CCOc1ccc2nc(NC(=O)CSc3nc4cccnc4n3C)sc2c1 nan
44142358 21453 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 311 0 1 3 3.9 Nc1cccc(C#Cc2ccc3c(=O)c4ccccc4oc3c2)c1 nan
CHEMBL1318214 21453 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 311 0 1 3 3.9 Nc1cccc(C#Cc2ccc3c(=O)c4ccccc4oc3c2)c1 nan
5182299 24714 9 None - 1 Human 5.6 pEC50 = 5.6 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 457 5 1 4 4.5 O=C(Nc1ccc(S(=O)(=O)N2CCCCC2c2cccnc2)cc1)c1c(F)cccc1F nan
CHEMBL1345891 24714 9 None - 1 Human 5.6 pEC50 = 5.6 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 457 5 1 4 4.5 O=C(Nc1ccc(S(=O)(=O)N2CCCCC2c2cccnc2)cc1)c1c(F)cccc1F nan
20959170 28555 5 None - 1 Human 5.6 pEC50 = 5.6 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 382 5 0 4 4.7 Cc1ccc(N(C)S(=O)(=O)c2cc(-c3cnc(C4CC4)o3)ccc2C)cc1 nan
CHEMBL1378598 28555 5 None - 1 Human 5.6 pEC50 = 5.6 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 382 5 0 4 4.7 Cc1ccc(N(C)S(=O)(=O)c2cc(-c3cnc(C4CC4)o3)ccc2C)cc1 nan
9927453 96226 0 None -18 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at Homo sapiens (human) beta2 adrenoreceptorAgonist activity at Homo sapiens (human) beta2 adrenoreceptor
ChEMBL 328 6 3 2 4.1 C[C@H](Cc1c[nH]c2ccccc12)NC[C@H](O)c1cccc(Cl)c1 10.1007/s00044-009-9257-x
CHEMBL26393 96226 0 None -18 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at Homo sapiens (human) beta2 adrenoreceptorAgonist activity at Homo sapiens (human) beta2 adrenoreceptor
ChEMBL 328 6 3 2 4.1 C[C@H](Cc1c[nH]c2ccccc12)NC[C@H](O)c1cccc(Cl)c1 10.1007/s00044-009-9257-x
46221398 8601 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assayAgonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assay
ChEMBL 448 10 4 4 4.7 CCCCc1cc2c(cc1CCCC)CC(NC[C@H](O)c1ccc(O)c3[nH]c(=O)ccc13)C2 10.1021/jm100068m
CHEMBL1095779 8601 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assayAgonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assay
ChEMBL 448 10 4 4 4.7 CCCCc1cc2c(cc1CCCC)CC(NC[C@H](O)c1ccc(O)c3[nH]c(=O)ccc13)C2 10.1021/jm100068m
9927453 96226 0 None -18 3 Human 7.6 pEC50 = 7.6 Functional
Agonistic activity against human Beta-2 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonistic activity against human Beta-2 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 328 6 3 2 4.1 C[C@H](Cc1c[nH]c2ccccc12)NC[C@H](O)c1cccc(Cl)c1 10.1016/s0960-894x(03)00073-8
CHEMBL26393 96226 0 None -18 3 Human 7.6 pEC50 = 7.6 Functional
Agonistic activity against human Beta-2 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonistic activity against human Beta-2 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 328 6 3 2 4.1 C[C@H](Cc1c[nH]c2ccccc12)NC[C@H](O)c1cccc(Cl)c1 10.1016/s0960-894x(03)00073-8
90644142 111736 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 365 7 4 4 2.5 OCc1cc(C(O)CNCCc2ccc(Br)cc2)ccc1O 10.1016/j.bmcl.2014.04.069
CHEMBL3290971 111736 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 365 7 4 4 2.5 OCc1cc(C(O)CNCCc2ccc(Br)cc2)ccc1O 10.1016/j.bmcl.2014.04.069
105 3392 84 None -8 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1016/j.bmcl.2011.11.072
2083 3392 84 None -8 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1016/j.bmcl.2011.11.072
558 3392 84 None -8 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1016/j.bmcl.2011.11.072
CHEMBL714 3392 84 None -8 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1016/j.bmcl.2011.11.072
DB01001 3392 84 None -8 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1016/j.bmcl.2011.11.072
3366873 24121 6 None - 1 Human 7.6 pEC50 = 7.6 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 410 10 3 6 4.2 COc1ccc(CNC(=O)CCCCCNc2nc(S)nc3ccccc23)cc1 nan
CHEMBL1340869 24121 6 None - 1 Human 7.6 pEC50 = 7.6 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 410 10 3 6 4.2 COc1ccc(CNC(=O)CCCCCNc2nc(S)nc3ccccc23)cc1 nan
24180436 92772 0 None -1 2 Guinea pig 6.6 pEC50 = 6.6 Functional
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contractionAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction
ChEMBL 527 10 4 10 2.6 CC(Cc1ccc(Oc2no[n+]([O-])c2S(=O)(=O)c2ccccc2)cc1)NCC(O)c1cc(O)cc(O)c1 10.1021/jm0704595
CHEMBL244687 92772 0 None -1 2 Guinea pig 6.6 pEC50 = 6.6 Functional
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contractionAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction
ChEMBL 527 10 4 10 2.6 CC(Cc1ccc(Oc2no[n+]([O-])c2S(=O)(=O)c2ccccc2)cc1)NCC(O)c1cc(O)cc(O)c1 10.1021/jm0704595
105 3392 84 None -8 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technologyAgonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technology
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1021/acs.jmedchem.0c01195
2083 3392 84 None -8 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technologyAgonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technology
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1021/acs.jmedchem.0c01195
558 3392 84 None -8 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technologyAgonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technology
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1021/acs.jmedchem.0c01195
CHEMBL714 3392 84 None -8 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technologyAgonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technology
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1021/acs.jmedchem.0c01195
DB01001 3392 84 None -8 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technologyAgonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technology
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1021/acs.jmedchem.0c01195
145989107 166565 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 424 13 4 5 3.7 O=c1ccc2c(C(CO)NCCCCOCCCCc3ccccc3)ccc(O)c2[nH]1 10.1016/j.ejmech.2018.04.041
CHEMBL4290441 166565 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 424 13 4 5 3.7 O=c1ccc2c(C(CO)NCCCCOCCCCc3ccccc3)ccc(O)c2[nH]1 10.1016/j.ejmech.2018.04.041
11038599 47589 0 None -15 3 Human 6.6 pEC50 = 6.6 Functional
Concentration that causes 50% inhibition of human beta 2 adrenergic receptor (AR), expressed in CHO cells.Concentration that causes 50% inhibition of human beta 2 adrenergic receptor (AR), expressed in CHO cells.
ChEMBL 516 11 5 6 3.7 C[C@H](CNc1cccc(CNC(=O)NS(=O)(=O)c2ccccc2)c1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0101500
CHEMBL154906 47589 0 None -15 3 Human 6.6 pEC50 = 6.6 Functional
Concentration that causes 50% inhibition of human beta 2 adrenergic receptor (AR), expressed in CHO cells.Concentration that causes 50% inhibition of human beta 2 adrenergic receptor (AR), expressed in CHO cells.
ChEMBL 516 11 5 6 3.7 C[C@H](CNc1cccc(CNC(=O)NS(=O)(=O)c2ccccc2)c1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0101500
9801145 92976 0 None -316 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 400 9 4 5 4.0 O=C(O)c1ccoc1-c1cccc(NCCNC[C@H](O)c2cccc(Cl)c2)c1 10.1016/j.bmcl.2007.05.069
CHEMBL245874 92976 0 None -316 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 400 9 4 5 4.0 O=C(O)c1ccoc1-c1cccc(NCCNC[C@H](O)c2cccc(Cl)c2)c1 10.1016/j.bmcl.2007.05.069
46832227 14067 1 None 5 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 327 13 5 6 1.1 OCCOCCCCCCNC[C@H](O)c1ccc(O)c(CO)c1 10.1021/jm100326d
CHEMBL1083884 14067 1 None 5 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 327 13 5 6 1.1 OCCOCCCCCCNC[C@H](O)c1ccc(O)c(CO)c1 10.1021/jm100326d
CHEMBL1198851 14067 1 None 5 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 327 13 5 6 1.1 OCCOCCCCCCNC[C@H](O)c1ccc(O)c(CO)c1 10.1021/jm100326d
42625743 12478 0 None -12 3 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1cccc(CCCCCCOCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
CHEMBL1186943 12478 0 None -12 3 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1cccc(CCCCCCOCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
CHEMBL483407 12478 0 None -12 3 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1cccc(CCCCCCOCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
2816345 29093 5 None - 1 Human 6.6 pEC50 = 6.6 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 415 4 1 7 5.2 Cc1cc(C)c2c(N)c(-c3nnc(SCc4ccc(Cl)cc4)n3C)sc2n1 nan
CHEMBL1383213 29093 5 None - 1 Human 6.6 pEC50 = 6.6 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 415 4 1 7 5.2 Cc1cc(C)c2c(N)c(-c3nnc(SCc4ccc(Cl)cc4)n3C)sc2n1 nan
4384568 162541 8 None - 1 Human 5.6 pEC50 = 5.6 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 438 6 0 4 3.4 O=C1C2CCCCN2C(=O)N1CCCCN1CCN(c2cccc(C(F)(F)F)c2)CC1 nan
CHEMBL417709 162541 8 None - 1 Human 5.6 pEC50 = 5.6 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 438 6 0 4 3.4 O=C1C2CCCCN2C(=O)N1CCCCN1CCN(c2cccc(C(F)(F)F)c2)CC1 nan
1481480 24049 12 None - 1 Human 5.6 pEC50 = 5.6 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 484 8 0 7 4.9 CN(CCOc1ccc(-c2ccn(S(=O)(=O)c3cccc4ccccc34)n2)cc1)c1ccccn1 nan
CHEMBL1340208 24049 12 None - 1 Human 5.6 pEC50 = 5.6 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 484 8 0 7 4.9 CN(CCOc1ccc(-c2ccn(S(=O)(=O)c3cccc4ccccc34)n2)cc1)c1ccccn1 nan
8441531 45177 6 None - 1 Human 6.6 pEC50 = 6.6 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 394 8 2 4 5.4 CCCCOc1cccc(C(=O)Nc2ccc(NC(=O)c3cccs3)cc2)c1 nan
CHEMBL1527861 45177 6 None - 1 Human 6.6 pEC50 = 6.6 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 394 8 2 4 5.4 CCCCOc1cccc(C(=O)Nc2ccc(NC(=O)c3cccs3)cc2)c1 nan
24794188 33483 1 None - 1 Human 5.6 pEC50 = 5.6 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 446 5 0 3 5.4 O=C(c1ccc(OC2CCN(Cc3ccc(C(F)(F)F)cc3)CC2)cc1)N1CCCCC1 nan
CHEMBL1422222 33483 1 None - 1 Human 5.6 pEC50 = 5.6 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 446 5 0 3 5.4 O=C(c1ccc(OC2CCN(Cc3ccc(C(F)(F)F)cc3)CC2)cc1)N1CCCCC1 nan
44396530 66738 0 None -23 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at Homo sapiens (human) beta2 adrenoreceptorAgonist activity at Homo sapiens (human) beta2 adrenoreceptor
ChEMBL 591 14 4 8 4.8 CCCCS(=O)(=O)Oc1cccc2c(C[C@@H](C)NC[C@H](O)c3cccc(NS(=O)(=O)c4cccs4)c3)c[nH]c12 10.1007/s00044-009-9257-x
CHEMBL187317 66738 0 None -23 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at Homo sapiens (human) beta2 adrenoreceptorAgonist activity at Homo sapiens (human) beta2 adrenoreceptor
ChEMBL 591 14 4 8 4.8 CCCCS(=O)(=O)Oc1cccc2c(C[C@@H](C)NC[C@H](O)c3cccc(NS(=O)(=O)c4cccs4)c3)c[nH]c12 10.1007/s00044-009-9257-x
76333795 84877 0 None -56 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at Homo sapiens (human) beta2 adrenoreceptorAgonist activity at Homo sapiens (human) beta2 adrenoreceptor
ChEMBL 558 11 5 8 3.1 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccc(N)c2)c1 10.1007/s00044-009-9257-x
CHEMBL2260985 84877 0 None -56 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at Homo sapiens (human) beta2 adrenoreceptorAgonist activity at Homo sapiens (human) beta2 adrenoreceptor
ChEMBL 558 11 5 8 3.1 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccc(N)c2)c1 10.1007/s00044-009-9257-x
90666102 108832 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP productionAgonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP production
ChEMBL 682 18 6 9 6.2 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3ccc(O)cc3)CC2)ccc1O 10.1039/C1MD00140J
CHEMBL3219032 108832 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP productionAgonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP production
ChEMBL 682 18 6 9 6.2 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3ccc(O)cc3)CC2)ccc1O 10.1039/C1MD00140J
59707195 108839 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP productionAgonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP production
ChEMBL 700 18 6 9 6.3 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3ccc(O)c(F)c3)CC2)ccc1O 10.1039/C1MD00140J
CHEMBL3219040 108839 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP productionAgonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP production
ChEMBL 700 18 6 9 6.3 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3ccc(O)c(F)c3)CC2)ccc1O 10.1039/C1MD00140J
1362375 22770 14 None - 1 Human 6.6 pEC50 = 6.6 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory)
ChEMBL 388 6 2 5 4.8 CCc1ccc(OCC(=O)Nc2ccc(-c3nc4ccccc4o3)c(O)c2)cc1 nan
CHEMBL1329712 22770 14 None - 1 Human 6.6 pEC50 = 6.6 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory)
ChEMBL 388 6 2 5 4.8 CCc1ccc(OCC(=O)Nc2ccc(-c3nc4ccccc4o3)c(O)c2)cc1 nan
127046951 139359 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human beta2 receptor expressed in HEK293 cells cotransfected with Gqs5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositolAgonist activity at human beta2 receptor expressed in HEK293 cells cotransfected with Gqs5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositol
ChEMBL 437 12 4 6 4.0 COc1cc(CCNC[C@@H](O)c2ccc(O)c(O)c2)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
CHEMBL3799427 139359 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human beta2 receptor expressed in HEK293 cells cotransfected with Gqs5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositolAgonist activity at human beta2 receptor expressed in HEK293 cells cotransfected with Gqs5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositol
ChEMBL 437 12 4 6 4.0 COc1cc(CCNC[C@@H](O)c2ccc(O)c(O)c2)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
659759 46992 10 None 14 2 Human 6.6 pEC50 = 6.6 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 359 4 1 4 3.0 CC(=O)Nc1ccc(S(=O)(=O)N2CCCCC2c2cccnc2)cc1 nan
CHEMBL1543973 46992 10 None 14 2 Human 6.6 pEC50 = 6.6 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 359 4 1 4 3.0 CC(=O)Nc1ccc(S(=O)(=O)N2CCCCC2c2cccnc2)cc1 nan
4508 3078 91 None 1 2 Human 5.6 pEC50 = 5.6 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 183 3 4 4 0.4 CNCC(c1ccc(c(c1)O)O)O nan
4866774 3078 91 None 1 2 Human 5.6 pEC50 = 5.6 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 183 3 4 4 0.4 CNCC(c1ccc(c(c1)O)O)O nan
509 3078 91 None 1 2 Human 5.6 pEC50 = 5.6 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 183 3 4 4 0.4 CNCC(c1ccc(c(c1)O)O)O nan
838 3078 91 None 1 2 Human 5.6 pEC50 = 5.6 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 183 3 4 4 0.4 CNCC(c1ccc(c(c1)O)O)O nan
CHEMBL1740 3078 91 None 1 2 Human 5.6 pEC50 = 5.6 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 183 3 4 4 0.4 CNCC(c1ccc(c(c1)O)O)O nan
73056755 103788 0 None - 1 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulationAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulation
ChEMBL 345 8 4 5 3.0 COc1ccc(C[C@H](NC[C@H](O)c2cc(O)cc(O)c2)C(C)C)cc1 10.1016/j.bmc.2013.11.030
CHEMBL3099661 103788 0 None - 1 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulationAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulation
ChEMBL 345 8 4 5 3.0 COc1ccc(C[C@H](NC[C@H](O)c2cc(O)cc(O)c2)C(C)C)cc1 10.1016/j.bmc.2013.11.030
2803618 58963 6 None - 1 Human 5.6 pEC50 = 5.6 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 324 5 0 3 4.8 COc1ccc(C(C)=O)cc1COc1ccc(Cl)cc1Cl nan
CHEMBL1704973 58963 6 None - 1 Human 5.6 pEC50 = 5.6 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 324 5 0 3 4.8 COc1ccc(C(C)=O)cc1COc1ccc(Cl)cc1Cl nan
105 3392 84 None 3 3 Guinea pig 6.6 pEC50 = 6.6 Functional
Agonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring assessed as bronchorelaxation activity against carbachol-induced contractionAgonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring assessed as bronchorelaxation activity against carbachol-induced contraction
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1016/j.ejmech.2008.12.016
2083 3392 84 None 3 3 Guinea pig 6.6 pEC50 = 6.6 Functional
Agonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring assessed as bronchorelaxation activity against carbachol-induced contractionAgonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring assessed as bronchorelaxation activity against carbachol-induced contraction
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1016/j.ejmech.2008.12.016
558 3392 84 None 3 3 Guinea pig 6.6 pEC50 = 6.6 Functional
Agonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring assessed as bronchorelaxation activity against carbachol-induced contractionAgonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring assessed as bronchorelaxation activity against carbachol-induced contraction
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1016/j.ejmech.2008.12.016
CHEMBL714 3392 84 None 3 3 Guinea pig 6.6 pEC50 = 6.6 Functional
Agonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring assessed as bronchorelaxation activity against carbachol-induced contractionAgonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring assessed as bronchorelaxation activity against carbachol-induced contraction
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1016/j.ejmech.2008.12.016
DB01001 3392 84 None 3 3 Guinea pig 6.6 pEC50 = 6.6 Functional
Agonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring assessed as bronchorelaxation activity against carbachol-induced contractionAgonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring assessed as bronchorelaxation activity against carbachol-induced contraction
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1016/j.ejmech.2008.12.016
49837874 54654 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at beta2 adrenoceptor (unknown origin)Agonist activity at beta2 adrenoceptor (unknown origin)
ChEMBL 370 6 4 5 2.7 Cc1ccccc1CC(C)(C)NC[C@H](O)c1ccc(O)c2c1OCC(=O)N2 10.1021/acs.jmedchem.0c01195
CHEMBL1615159 54654 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at beta2 adrenoceptor (unknown origin)Agonist activity at beta2 adrenoceptor (unknown origin)
ChEMBL 370 6 4 5 2.7 Cc1ccccc1CC(C)(C)NC[C@H](O)c1ccc(O)c2c1OCC(=O)N2 10.1021/acs.jmedchem.0c01195
44219641 177854 0 None 3 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 498 13 3 6 4.1 CC(Cc1ccc(NC(=O)Cc2nccn2Cc2ccccc2)cc1)NC[C@H](O)COc1ccccc1 10.1016/j.bmc.2009.03.044
CHEMBL466088 177854 0 None 3 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 498 13 3 6 4.1 CC(Cc1ccc(NC(=O)Cc2nccn2Cc2ccccc2)cc1)NC[C@H](O)COc1ccccc1 10.1016/j.bmc.2009.03.044
22422248 21955 1 None - 1 Human 7.6 pEC50 = 7.6 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 452 5 0 4 3.6 CCC(=O)N1CCc2cc(Br)cc(S(=O)(=O)N(C)c3ccc(OC)cc3)c21 nan
CHEMBL1322514 21955 1 None - 1 Human 7.6 pEC50 = 7.6 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 452 5 0 4 3.6 CCC(=O)N1CCc2cc(Br)cc(S(=O)(=O)N(C)c3ccc(OC)cc3)c21 nan
10575455 99503 0 None -13 3 Human 6.6 pEC50 = 6.6 Functional
Increased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 2 adrenergic receptorsIncreased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 2 adrenergic receptors
ChEMBL 448 8 5 7 1.2 CS(=O)(=O)Nc1cc([C@@H](O)CNC2CCN(c3ccc(C(N)=O)cc3)CC2)ccc1O 10.1021/jm000544b
CHEMBL286574 99503 0 None -13 3 Human 6.6 pEC50 = 6.6 Functional
Increased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 2 adrenergic receptorsIncreased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 2 adrenergic receptors
ChEMBL 448 8 5 7 1.2 CS(=O)(=O)Nc1cc([C@@H](O)CNC2CCN(c3ccc(C(N)=O)cc3)CC2)ccc1O 10.1021/jm000544b
44313150 103288 0 None -3 3 Human 5.6 pEC50 = 5.6 Functional
Compound was evaluated for its inhibitory activity against human beta-2 adrenergic receptor (AR)Compound was evaluated for its inhibitory activity against human beta-2 adrenergic receptor (AR)
ChEMBL 628 12 6 6 6.7 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2cccc(-c3cccc(CC4NCCc5cc(O)c(O)cc54)c3)c2)cc1 10.1016/s0960-894x(00)00459-5
CHEMBL308868 103288 0 None -3 3 Human 5.6 pEC50 = 5.6 Functional
Compound was evaluated for its inhibitory activity against human beta-2 adrenergic receptor (AR)Compound was evaluated for its inhibitory activity against human beta-2 adrenergic receptor (AR)
ChEMBL 628 12 6 6 6.7 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2cccc(-c3cccc(CC4NCCc5cc(O)c(O)cc54)c3)c2)cc1 10.1016/s0960-894x(00)00459-5
2964893 49794 8 None - 1 Human 6.6 pEC50 = 6.6 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 374 5 0 5 1.1 CN(CC(=O)N1CCN(c2ccccn2)CC1)S(=O)(=O)c1ccccc1 nan
CHEMBL1569866 49794 8 None - 1 Human 6.6 pEC50 = 6.6 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 374 5 0 5 1.1 CN(CC(=O)N1CCN(c2ccccn2)CC1)S(=O)(=O)c1ccccc1 nan
123600 2275 0 None 1 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting in presence of 100 uM boric acidAgonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting in presence of 100 uM boric acid
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)[C@H](CNC(C)(C)C)O 10.1016/j.bmc.2011.11.054
1575 2275 0 None 1 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting in presence of 100 uM boric acidAgonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting in presence of 100 uM boric acid
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)[C@H](CNC(C)(C)C)O 10.1016/j.bmc.2011.11.054
9816 2275 0 None 1 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting in presence of 100 uM boric acidAgonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting in presence of 100 uM boric acid
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)[C@H](CNC(C)(C)C)O 10.1016/j.bmc.2011.11.054
CHEMBL1002 2275 0 None 1 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting in presence of 100 uM boric acidAgonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting in presence of 100 uM boric acid
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)[C@H](CNC(C)(C)C)O 10.1016/j.bmc.2011.11.054
DB13139 2275 0 None 1 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting in presence of 100 uM boric acidAgonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting in presence of 100 uM boric acid
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)[C@H](CNC(C)(C)C)O 10.1016/j.bmc.2011.11.054
123600 2275 0 None 1 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting in presence of 100 uM boric acidAgonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting in presence of 100 uM boric acid
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)[C@H](CNC(C)(C)C)O 10.1016/j.bmc.2011.11.054
1575 2275 0 None 1 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting in presence of 100 uM boric acidAgonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting in presence of 100 uM boric acid
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)[C@H](CNC(C)(C)C)O 10.1016/j.bmc.2011.11.054
9816 2275 0 None 1 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting in presence of 100 uM boric acidAgonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting in presence of 100 uM boric acid
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)[C@H](CNC(C)(C)C)O 10.1016/j.bmc.2011.11.054
CHEMBL1002 2275 0 None 1 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting in presence of 100 uM boric acidAgonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting in presence of 100 uM boric acid
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)[C@H](CNC(C)(C)C)O 10.1016/j.bmc.2011.11.054
DB13139 2275 0 None 1 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting in presence of 100 uM boric acidAgonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting in presence of 100 uM boric acid
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)[C@H](CNC(C)(C)C)O 10.1016/j.bmc.2011.11.054
3104427 16906 8 None - 1 Human 5.6 pEC50 = 5.6 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 436 7 2 3 4.4 O=C(C[n+]1cccc(NC(=O)c2ccccc2)c1)c1ccc(NC(=O)c2ccccc2)cc1 nan
CHEMBL125497 16906 8 None - 1 Human 5.6 pEC50 = 5.6 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 436 7 2 3 4.4 O=C(C[n+]1cccc(NC(=O)c2ccccc2)c1)c1ccc(NC(=O)c2ccccc2)cc1 nan
CHEMBL1461759 16906 8 None - 1 Human 5.6 pEC50 = 5.6 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 436 7 2 3 4.4 O=C(C[n+]1cccc(NC(=O)c2ccccc2)c1)c1ccc(NC(=O)c2ccccc2)cc1 nan
160510 100645 36 None - 1 Human 5.6 pEC50 = 5.6 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 184 0 1 1 2.5 CC1=NCCc2c1[nH]c1ccccc21 nan
CHEMBL1506260 100645 36 None - 1 Human 5.6 pEC50 = 5.6 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 184 0 1 1 2.5 CC1=NCCc2c1[nH]c1ccccc21 nan
CHEMBL295234 100645 36 None - 1 Human 5.6 pEC50 = 5.6 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 184 0 1 1 2.5 CC1=NCCc2c1[nH]c1ccccc21 nan
2234461 43512 9 None - 1 Human 6.6 pEC50 = 6.6 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 432 7 1 6 2.7 COC(=O)c1ccc(NC(=O)COc2ccc(S(=O)(=O)N3CCCCC3)cc2)cc1 nan
CHEMBL1510834 43512 9 None - 1 Human 6.6 pEC50 = 6.6 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 432 7 1 6 2.7 COC(=O)c1ccc(NC(=O)COc2ccc(S(=O)(=O)N3CCCCC3)cc2)cc1 nan
145982607 165156 0 None -32 3 Human 6.6 pEC50 = 6.6 Functional
Antagonist activity at human beta2 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta2 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 432 12 3 4 4.0 CCc1ccccc1OC[C@@H](O)CNCCc1ccc(NC(=O)Cc2ccccc2)cc1 10.1016/j.ejmech.2018.03.032
CHEMBL4245968 165156 0 None -32 3 Human 6.6 pEC50 = 6.6 Functional
Antagonist activity at human beta2 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta2 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 432 12 3 4 4.0 CCc1ccccc1OC[C@@H](O)CNCCc1ccc(NC(=O)Cc2ccccc2)cc1 10.1016/j.ejmech.2018.03.032
5307895 49843 7 None 9 2 Human 5.5 pEC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 441 8 1 8 2.9 COc1ccc(OC)c(CCNC(=O)C2CCN(c3nnc(-n4cccc4)s3)CC2)c1 nan
CHEMBL1570251 49843 7 None 9 2 Human 5.5 pEC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 441 8 1 8 2.9 COc1ccc(OC)c(CCNC(=O)C2CCN(c3nnc(-n4cccc4)s3)CC2)c1 nan
44396596 122771 0 None -25 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at Homo sapiens (human) beta2 adrenoreceptorAgonist activity at Homo sapiens (human) beta2 adrenoreceptor
ChEMBL 485 10 4 6 4.3 COc1cccc2c(C[C@@H](C)NC[C@H](O)c3cccc(NS(=O)(=O)c4cccs4)c3)c[nH]c12 10.1007/s00044-009-9257-x
CHEMBL361505 122771 0 None -25 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at Homo sapiens (human) beta2 adrenoreceptorAgonist activity at Homo sapiens (human) beta2 adrenoreceptor
ChEMBL 485 10 4 6 4.3 COc1cccc2c(C[C@@H](C)NC[C@H](O)c3cccc(NS(=O)(=O)c4cccs4)c3)c[nH]c12 10.1007/s00044-009-9257-x
44428081 92688 0 None - 1 Guinea pig 7.5 pEC50 = 7.5 Functional
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contractionAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction
ChEMBL 428 10 5 9 1.4 CC(Cc1ccc(OCc2nonc2C(N)=O)cc1)NCC(O)c1cc(O)cc(O)c1 10.1021/jm0704595
CHEMBL244321 92688 0 None - 1 Guinea pig 7.5 pEC50 = 7.5 Functional
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contractionAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction
ChEMBL 428 10 5 9 1.4 CC(Cc1ccc(OCc2nonc2C(N)=O)cc1)NCC(O)c1cc(O)cc(O)c1 10.1021/jm0704595
2816338 46290 5 None - 1 Human 7.5 pEC50 = 7.5 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 425 6 1 7 5.4 C=CCn1c(SCc2ccc(F)cc2)nnc1-c1sc2nc(C)cc(C)c2c1N nan
CHEMBL1538061 46290 5 None - 1 Human 7.5 pEC50 = 7.5 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 425 6 1 7 5.4 C=CCn1c(SCc2ccc(F)cc2)nnc1-c1sc2nc(C)cc(C)c2c1N nan
567 715 10 None -83 7 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at Homo sapiens (human) beta2 adrenoreceptorAgonist activity at Homo sapiens (human) beta2 adrenoreceptor
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1007/s00044-009-9257-x
9841972 715 10 None -83 7 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at Homo sapiens (human) beta2 adrenoreceptorAgonist activity at Homo sapiens (human) beta2 adrenoreceptor
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1007/s00044-009-9257-x
CHEMBL284782 715 10 None -83 7 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at Homo sapiens (human) beta2 adrenoreceptorAgonist activity at Homo sapiens (human) beta2 adrenoreceptor
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1007/s00044-009-9257-x
44565931 12324 0 None -9549 4 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 552 11 4 8 3.6 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3cnccc3N)cc2)cc1OC1CCCCC1 10.1021/jm9000709
CHEMBL1186040 12324 0 None -9549 4 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 552 11 4 8 3.6 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3cnccc3N)cc2)cc1OC1CCCCC1 10.1021/jm9000709
CHEMBL446806 12324 0 None -9549 4 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 552 11 4 8 3.6 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3cnccc3N)cc2)cc1OC1CCCCC1 10.1021/jm9000709
567 715 10 None -83 7 Human 6.5 pEC50 = 6.5 Functional
Agonistic activity against human Beta-2 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonistic activity against human Beta-2 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1016/s0960-894x(03)00073-8
9841972 715 10 None -83 7 Human 6.5 pEC50 = 6.5 Functional
Agonistic activity against human Beta-2 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonistic activity against human Beta-2 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1016/s0960-894x(03)00073-8
CHEMBL284782 715 10 None -83 7 Human 6.5 pEC50 = 6.5 Functional
Agonistic activity against human Beta-2 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonistic activity against human Beta-2 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1016/s0960-894x(03)00073-8
24180436 92772 0 None -1 2 Guinea pig 5.5 pEC50 = 5.5 Functional
Agonist activity at adrenergic beta2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of propranololAgonist activity at adrenergic beta2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of propranolol
ChEMBL 527 10 4 10 2.6 CC(Cc1ccc(Oc2no[n+]([O-])c2S(=O)(=O)c2ccccc2)cc1)NCC(O)c1cc(O)cc(O)c1 10.1021/jm0704595
CHEMBL244687 92772 0 None -1 2 Guinea pig 5.5 pEC50 = 5.5 Functional
Agonist activity at adrenergic beta2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of propranololAgonist activity at adrenergic beta2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of propranolol
ChEMBL 527 10 4 10 2.6 CC(Cc1ccc(Oc2no[n+]([O-])c2S(=O)(=O)c2ccccc2)cc1)NCC(O)c1cc(O)cc(O)c1 10.1021/jm0704595
145982668 165350 0 None -38 3 Human 6.5 pEC50 = 6.5 Functional
Antagonist activity at human beta2 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta2 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 418 11 3 4 4.1 CCc1ccccc1OC[C@@H](O)CNCCc1ccc(NC(=O)c2ccccc2)cc1 10.1016/j.ejmech.2018.03.032
CHEMBL4250215 165350 0 None -38 3 Human 6.5 pEC50 = 6.5 Functional
Antagonist activity at human beta2 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta2 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 418 11 3 4 4.1 CCc1ccccc1OC[C@@H](O)CNCCc1ccc(NC(=O)c2ccccc2)cc1 10.1016/j.ejmech.2018.03.032
168286800 192318 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 380 4 3 3 4.0 Nc1c(Br)cc(C(CO)NC2CCCCC2)cc1C(F)(F)F 10.1021/acs.jmedchem.1c02006
CHEMBL5197382 192318 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 380 4 3 3 4.0 Nc1c(Br)cc(C(CO)NC2CCCCC2)cc1C(F)(F)F 10.1021/acs.jmedchem.1c02006
CHEMBL5222266 192318 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 380 4 3 3 4.0 Nc1c(Br)cc(C(CO)NC2CCCCC2)cc1C(F)(F)F 10.1021/acs.jmedchem.1c02006
3904428 20236 8 None 4 2 Human 5.5 pEC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 342 4 1 2 4.8 Cc1ccc(NC(=O)C(c2ccc(Cl)cc2)N2CCCCC2)cc1 nan
CHEMBL1306990 20236 8 None 4 2 Human 5.5 pEC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 342 4 1 2 4.8 Cc1ccc(NC(=O)C(c2ccc(Cl)cc2)N2CCCCC2)cc1 nan
443372 10123 23 None -1 8 Guinea pig 8.5 pEC50 = 8.5 Functional
Activity for Beta-2 adrenergic receptor was assessed from effect on relaxation of guinea pig trachea.Activity for Beta-2 adrenergic receptor was assessed from effect on relaxation of guinea pig trachea.
ChEMBL 211 4 4 4 1.1 CC(C)NC[C@H](O)c1ccc(O)c(O)c1 10.1021/jm00019a001
CHEMBL1160723 10123 23 None -1 8 Guinea pig 8.5 pEC50 = 8.5 Functional
Activity for Beta-2 adrenergic receptor was assessed from effect on relaxation of guinea pig trachea.Activity for Beta-2 adrenergic receptor was assessed from effect on relaxation of guinea pig trachea.
ChEMBL 211 4 4 4 1.1 CC(C)NC[C@H](O)c1ccc(O)c(O)c1 10.1021/jm00019a001
CHEMBL2062275 10123 23 None -1 8 Guinea pig 8.5 pEC50 = 8.5 Functional
Activity for Beta-2 adrenergic receptor was assessed from effect on relaxation of guinea pig trachea.Activity for Beta-2 adrenergic receptor was assessed from effect on relaxation of guinea pig trachea.
ChEMBL 211 4 4 4 1.1 CC(C)NC[C@H](O)c1ccc(O)c(O)c1 10.1021/jm00019a001
1499 2052 43 None -72 36 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2009.03.044
3779 2052 43 None -72 36 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2009.03.044
536 2052 43 None -72 36 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2009.03.044
CHEMBL434 2052 43 None -72 36 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2009.03.044
DB01064 2052 43 None -72 36 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2009.03.044
1499 2052 43 None -72 36 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2009.06.031
3779 2052 43 None -72 36 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2009.06.031
536 2052 43 None -72 36 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2009.06.031
CHEMBL434 2052 43 None -72 36 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2009.06.031
DB01064 2052 43 None -72 36 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2009.06.031
1499 2052 43 None -72 36 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.ejmech.2009.01.022
3779 2052 43 None -72 36 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.ejmech.2009.01.022
536 2052 43 None -72 36 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.ejmech.2009.01.022
CHEMBL434 2052 43 None -72 36 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.ejmech.2009.01.022
DB01064 2052 43 None -72 36 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.ejmech.2009.01.022
70843740 124707 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 864 16 6 9 7.5 Cc1ccc(C(=O)NCc2ccc(CC(C)NC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645312 124707 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 864 16 6 9 7.5 Cc1ccc(C(=O)NCc2ccc(CC(C)NC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
59548073 124720 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 822 15 6 9 7.0 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1cccc(CC(=O)Nc2ccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)c1 nan
CHEMBL3645324 124720 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 822 15 6 9 7.0 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1cccc(CC(=O)Nc2ccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)c1 nan
59548112 124721 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 850 15 6 9 7.6 Cc1cc(NC(=O)Cc2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c(C)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645325 124721 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 850 15 6 9 7.6 Cc1cc(NC(=O)Cc2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c(C)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548133 124755 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 850 17 6 9 7.0 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CNC(=O)CCc2cccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1 nan
CHEMBL3645358 124755 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 850 17 6 9 7.0 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CNC(=O)CCc2cccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1 nan
59548071 124759 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 774 16 6 9 6.0 CN(CCCC(=O)Nc1ccc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645362 124759 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 774 16 6 9 6.0 CN(CCCC(=O)Nc1ccc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
44396779 66711 0 None -17 3 Human 8.5 pEC50 = 8.5 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptor
ChEMBL 611 12 4 8 5.1 C[C@H](Cc1c[nH]c2c(OS(=O)(=O)c3ccccc3)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2004.10.035
CHEMBL187209 66711 0 None -17 3 Human 8.5 pEC50 = 8.5 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptor
ChEMBL 611 12 4 8 5.1 C[C@H](Cc1c[nH]c2c(OS(=O)(=O)c3ccccc3)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2004.10.035
11810896 118964 0 None 2 3 Human 8.5 pEC50 = 8.5 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-2 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-2 AR expressed as the negative logarithm of the molar drug concentration
ChEMBL 375 9 4 4 3.1 CC(=O)NCc1ccc(NC[C@@H](C)NC[C@H](O)c2cccc(Cl)c2)cc1 10.1021/jm0101500
CHEMBL345304 118964 0 None 2 3 Human 8.5 pEC50 = 8.5 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-2 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-2 AR expressed as the negative logarithm of the molar drug concentration
ChEMBL 375 9 4 4 3.1 CC(=O)NCc1ccc(NC[C@@H](C)NC[C@H](O)c2cccc(Cl)c2)cc1 10.1021/jm0101500
24901283 70024 0 None 2 5 Guinea pig 8.5 pEC50 = 8.5 Functional
Agonist activity at beta2 adrenoceptor in guinea pig trachea assessed as reduction in methacholine-induced contractionAgonist activity at beta2 adrenoceptor in guinea pig trachea assessed as reduction in methacholine-induced contraction
ChEMBL 417 11 5 7 1.9 COCCNCc1cccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)c1 10.1016/j.bmcl.2011.10.049
CHEMBL1945292 70024 0 None 2 5 Guinea pig 8.5 pEC50 = 8.5 Functional
Agonist activity at beta2 adrenoceptor in guinea pig trachea assessed as reduction in methacholine-induced contractionAgonist activity at beta2 adrenoceptor in guinea pig trachea assessed as reduction in methacholine-induced contraction
ChEMBL 417 11 5 7 1.9 COCCNCc1cccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)c1 10.1016/j.bmcl.2011.10.049
16049162 63746 0 None 31 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 515 13 5 7 3.9 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCSCCCNCCc3cccc(C(F)(F)F)c3)c2s1 10.1016/j.bmcl.2011.05.097
CHEMBL1807826 63746 0 None 31 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 515 13 5 7 3.9 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCSCCCNCCc3cccc(C(F)(F)F)c3)c2s1 10.1016/j.bmcl.2011.05.097
145991661 166197 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 340 6 5 5 1.8 O=c1ccc2c(C(CO)NCCc3ccc(O)cc3)ccc(O)c2[nH]1 10.1016/j.ejmech.2018.04.041
CHEMBL4283676 166197 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 340 6 5 5 1.8 O=c1ccc2c(C(CO)NCCc3ccc(O)cc3)ccc(O)c2[nH]1 10.1016/j.ejmech.2018.04.041
56943515 111939 0 None 7 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 478 13 6 7 3.7 CC(C)(N)COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c(NC=O)c3)cc2)cc1 10.1016/j.bmcl.2014.04.095
CHEMBL3298213 111939 0 None 7 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 478 13 6 7 3.7 CC(C)(N)COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c(NC=O)c3)cc2)cc1 10.1016/j.bmcl.2014.04.095
56943485 111998 0 None 12 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 544 12 5 8 3.6 O=c1ccc2c([C@@H](O)CNCCc3ccc(Nc4ccc(OCCN5CCOCC5)cc4)cc3)ccc(O)c2[nH]1 10.1016/j.bmcl.2014.04.095
CHEMBL3298831 111998 0 None 12 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 544 12 5 8 3.6 O=c1ccc2c([C@@H](O)CNCCc3ccc(Nc4ccc(OCCN5CCOCC5)cc4)cc3)ccc(O)c2[nH]1 10.1016/j.bmcl.2014.04.095
24900811 70006 0 None 5 4 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 479 11 5 7 3.5 COc1ccccc1CNCc1ccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)cc1 10.1016/j.bmcl.2011.10.049
CHEMBL1945040 70006 0 None 5 4 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 479 11 5 7 3.5 COc1ccccc1CNCc1ccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)cc1 10.1016/j.bmcl.2011.10.049
24900751 70022 0 None 3 4 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 493 12 5 7 3.8 CCOc1ccccc1CNCc1cccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)c1 10.1016/j.bmcl.2011.10.049
CHEMBL1945290 70022 0 None 3 4 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 493 12 5 7 3.8 CCOc1ccccc1CNCc1cccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)c1 10.1016/j.bmcl.2011.10.049
24900749 70023 0 None 22 4 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 493 11 4 7 3.8 COc1ccccc1CN(C)Cc1cccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)c1 10.1016/j.bmcl.2011.10.049
CHEMBL1945291 70023 0 None 22 4 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 493 11 4 7 3.8 COc1ccccc1CN(C)Cc1cccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)c1 10.1016/j.bmcl.2011.10.049
44237720 57915 0 None 91 2 Guinea pig 8.5 pEC50 = 8.5 Functional
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
ChEMBL 530 9 6 5 4.4 O=C(NCC12CC3CC(CC(C3)C1)C2)Nc1cccc(CCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1016/j.bmcl.2010.12.096
CHEMBL1682220 57915 0 None 91 2 Guinea pig 8.5 pEC50 = 8.5 Functional
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
ChEMBL 530 9 6 5 4.4 O=C(NCC12CC3CC(CC(C3)C1)C2)Nc1cccc(CCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1016/j.bmcl.2010.12.096
53319788 58219 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
ChEMBL 624 17 5 6 5.4 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(CCCCCCCCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)C1 10.1016/j.bmcl.2011.01.043
CHEMBL1683939 58219 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
ChEMBL 624 17 5 6 5.4 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(CCCCCCCCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)C1 10.1016/j.bmcl.2011.01.043
11567751 199065 0 None 29 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 374 6 4 5 2.5 CC(C)(Cc1ccc(F)cc1)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmcl.2009.12.087
CHEMBL600401 199065 0 None 29 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 374 6 4 5 2.5 CC(C)(Cc1ccc(F)cc1)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmcl.2009.12.087
46232856 199648 0 None 128 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 424 6 4 5 3.4 CC(C)(Cc1cccc(C(F)(F)F)c1)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmcl.2009.12.087
CHEMBL604333 199648 0 None 128 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 424 6 4 5 3.4 CC(C)(Cc1cccc(C(F)(F)F)c1)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmcl.2009.12.087
5581 101175 10 None -2 6 Human 8.5 pEC50 = 8.5 Functional
Compound was evaluated for its inhibitory activity against human beta-2 adrenergic receptor (AR)Compound was evaluated for its inhibitory activity against human beta-2 adrenergic receptor (AR)
ChEMBL 345 5 3 6 2.6 COc1cc(CC2NCCc3cc(O)c(O)cc32)cc(OC)c1OC 10.1016/s0960-894x(00)00459-5
CHEMBL299175 101175 10 None -2 6 Human 8.5 pEC50 = 8.5 Functional
Compound was evaluated for its inhibitory activity against human beta-2 adrenergic receptor (AR)Compound was evaluated for its inhibitory activity against human beta-2 adrenergic receptor (AR)
ChEMBL 345 5 3 6 2.6 COc1cc(CC2NCCc3cc(O)c(O)cc32)cc(OC)c1OC 10.1016/s0960-894x(00)00459-5
24764458 108841 2 None 1 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP productionAgonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP production
ChEMBL 716 18 6 9 6.9 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3ccc(O)c(Cl)c3)CC2)ccc1O 10.1039/C1MD00140J
CHEMBL3219042 108841 2 None 1 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP productionAgonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP production
ChEMBL 716 18 6 9 6.9 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3ccc(O)c(Cl)c3)CC2)ccc1O 10.1039/C1MD00140J
122194235 123453 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as stumulation of intracellular cAMP productionAgonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as stumulation of intracellular cAMP production
ChEMBL 690 16 6 8 7.3 O=C(Nc1ccccc1-c1ccc(O)c(Cl)c1)OC1CCN(CCCCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1016/j.bmcl.2015.10.008
CHEMBL3629353 123453 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as stumulation of intracellular cAMP productionAgonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as stumulation of intracellular cAMP production
ChEMBL 690 16 6 8 7.3 O=C(Nc1ccccc1-c1ccc(O)c(Cl)c1)OC1CCN(CCCCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1016/j.bmcl.2015.10.008
53380558 63302 2 None 4 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assayAgonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assay
ChEMBL 367 7 4 5 3.5 COc1ccc(C[C@@H](C)NC[C@H](O)c2cc(O)cc(O)c2)c2ccccc12 10.1016/j.bmc.2009.11.062
CHEMBL1800963 63302 2 None 4 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assayAgonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assay
ChEMBL 367 7 4 5 3.5 COc1ccc(C[C@@H](C)NC[C@H](O)c2cc(O)cc(O)c2)c2ccccc12 10.1016/j.bmc.2009.11.062
10202462 69874 0 None 223 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at beta2-adrenoceptor endogenously expressed in human BEAS-2B cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at beta2-adrenoceptor endogenously expressed in human BEAS-2B cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 422 11 6 6 2.9 OCc1cc([C@@H](O)CNCCc2ccc(NC[C@@H](O)c3ccccc3)cc2)ccc1O 10.1016/j.bmcl.2011.11.072
CHEMBL1940831 69874 0 None 223 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at beta2-adrenoceptor endogenously expressed in human BEAS-2B cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at beta2-adrenoceptor endogenously expressed in human BEAS-2B cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 422 11 6 6 2.9 OCc1cc([C@@H](O)CNCCc2ccc(NC[C@@H](O)c3ccccc3)cc2)ccc1O 10.1016/j.bmcl.2011.11.072
16049158 63744 0 None 12 3 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 475 14 5 7 3.4 CCc1ccc(CCNCCCSCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)cc1 10.1016/j.bmcl.2011.05.097
CHEMBL1807824 63744 0 None 12 3 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 475 14 5 7 3.4 CCc1ccc(CCNCCCSCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)cc1 10.1016/j.bmcl.2011.05.097
16049361 110757 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assayAgonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assay
ChEMBL 544 17 4 8 2.7 CCN(CC)CCN(CCNC[C@H](O)c1ccc(O)c2[nH]c(=O)sc12)C(=O)CCOCCc1ccccc1 10.1021/ml4005232
CHEMBL3265158 110757 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assayAgonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assay
ChEMBL 544 17 4 8 2.7 CCN(CC)CCN(CCNC[C@H](O)c1ccc(O)c2[nH]c(=O)sc12)C(=O)CCOCCc1ccccc1 10.1021/ml4005232
16049363 110758 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assayAgonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assay
ChEMBL 578 17 4 8 3.4 CCN(CC)CCN(CCNC[C@H](O)c1ccc(O)c2[nH]c(=O)sc12)C(=O)CCOCCc1cccc(Cl)c1 10.1021/ml4005232
CHEMBL3265159 110758 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assayAgonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assay
ChEMBL 578 17 4 8 3.4 CCN(CC)CCN(CCNC[C@H](O)c1ccc(O)c2[nH]c(=O)sc12)C(=O)CCOCCc1cccc(Cl)c1 10.1021/ml4005232
118737357 118546 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 703 12 5 8 6.1 Cc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1021/jm501915g
CHEMBL3426705 118546 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 703 12 5 8 6.1 Cc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1021/jm501915g
145990793 166235 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 457 9 5 5 3.3 O=C(Cc1ccccc1)Nc1ccc(CCNC(CO)c2ccc(O)c3[nH]c(=O)ccc23)cc1 10.1016/j.ejmech.2018.04.041
CHEMBL4284345 166235 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 457 9 5 5 3.3 O=C(Cc1ccccc1)Nc1ccc(CCNC(CO)c2ccc(O)c3[nH]c(=O)ccc23)cc1 10.1016/j.ejmech.2018.04.041
57398768 70141 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 459 10 4 5 4.3 O=c1[nH]c2c(O)ccc(CCNCCc3cccc(CN[C@H]4C[C@@H]4c4ccccc4)c3)c2s1 10.1016/j.bmcl.2011.10.049
CHEMBL1946765 70141 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 459 10 4 5 4.3 O=c1[nH]c2c(O)ccc(CCNCCc3cccc(CN[C@H]4C[C@@H]4c4ccccc4)c3)c2s1 10.1016/j.bmcl.2011.10.049
57403815 70178 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 539 11 5 6 5.7 C[C@@H](NCc1ccccc1-c1ccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)cc1)c1ccccc1 10.1016/j.bmcl.2011.10.049
CHEMBL1947155 70178 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 539 11 5 6 5.7 C[C@@H](NCc1ccccc1-c1ccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)cc1)c1ccccc1 10.1016/j.bmcl.2011.10.049
10128077 111764 0 None 1 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human beta2 receptor in BEAS-2B cells assessed as cAMP accumulation by radioimmunoassayAgonist activity at human beta2 receptor in BEAS-2B cells assessed as cAMP accumulation by radioimmunoassay
ChEMBL 484 11 5 6 5.2 COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c(CO)c3)cc2)cc1-c1ccccc1 10.1016/j.bmcl.2014.04.069
CHEMBL3290997 111764 0 None 1 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human beta2 receptor in BEAS-2B cells assessed as cAMP accumulation by radioimmunoassayAgonist activity at human beta2 receptor in BEAS-2B cells assessed as cAMP accumulation by radioimmunoassay
ChEMBL 484 11 5 6 5.2 COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c(CO)c3)cc2)cc1-c1ccccc1 10.1016/j.bmcl.2014.04.069
10287658 111750 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 408 10 5 6 3.5 COc1ccc(Nc2ccc(CCNCC(O)c3ccc(O)c(CO)c3)cc2)cc1 10.1016/j.bmcl.2014.04.069
CHEMBL3290984 111750 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 408 10 5 6 3.5 COc1ccc(Nc2ccc(CCNCC(O)c3ccc(O)c(CO)c3)cc2)cc1 10.1016/j.bmcl.2014.04.069
45269866 193614 0 None -1 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 455 10 4 4 4.7 O[C@@H](CNCCc1ccc(NC(=S)Nc2ccc(Cl)cc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL2448072 193614 0 None -1 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 455 10 4 4 4.7 O[C@@H](CNCCc1ccc(NC(=S)Nc2ccc(Cl)cc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL551389 193614 0 None -1 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 455 10 4 4 4.7 O[C@@H](CNCCc1ccc(NC(=S)Nc2ccc(Cl)cc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
45273276 194001 0 None 2 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 429 10 4 5 3.6 N#C/N=C(\Nc1ccccc1)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.06.031
CHEMBL1204005 194001 0 None 2 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 429 10 4 5 3.6 N#C/N=C(\Nc1ccccc1)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.06.031
CHEMBL556689 194001 0 None 2 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 429 10 4 5 3.6 N#C/N=C(\Nc1ccccc1)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.06.031
45273280 194036 0 None 1 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 435 11 4 4 3.7 O[C@@H](CNCCc1ccc(NC(=S)NCc2ccccc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL1204006 194036 0 None 1 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 435 11 4 4 3.7 O[C@@H](CNCCc1ccc(NC(=S)NCc2ccccc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL557095 194036 0 None 1 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 435 11 4 4 3.7 O[C@@H](CNCCc1ccc(NC(=S)NCc2ccccc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
45268128 194638 0 None 1 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 427 10 4 4 3.9 O[C@@H](CNCCc1ccc(NC(=S)NC2CCCCC2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL1203988 194638 0 None 1 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 427 10 4 4 3.9 O[C@@H](CNCCc1ccc(NC(=S)NC2CCCCC2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL562315 194638 0 None 1 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 427 10 4 4 3.9 O[C@@H](CNCCc1ccc(NC(=S)NC2CCCCC2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
45268136 194701 0 None 2 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 466 11 4 6 4.0 O=[N+]([O-])c1cccc(NC(=S)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)c1 10.1016/j.bmc.2009.06.031
CHEMBL1203989 194701 0 None 2 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 466 11 4 6 4.0 O=[N+]([O-])c1cccc(NC(=S)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)c1 10.1016/j.bmc.2009.06.031
CHEMBL562669 194701 0 None 2 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 466 11 4 6 4.0 O=[N+]([O-])c1cccc(NC(=S)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)c1 10.1016/j.bmc.2009.06.031
10283146 106776 0 None -2 3 Human 7.5 pEC50 = 7.5 Functional
Beta-2 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-2-adrenoceptorBeta-2 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-2-adrenoceptor
ChEMBL 656 12 5 9 3.1 CS(=O)(=O)Nc1cc([C@@H](O)CNCC2CCN(S(=O)(=O)c3ccc(-n4cc(CC(=O)O)c5ccccc54)cc3)CC2)ccc1O 10.1016/s0960-894x(02)00608-x
CHEMBL317003 106776 0 None -2 3 Human 7.5 pEC50 = 7.5 Functional
Beta-2 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-2-adrenoceptorBeta-2 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-2-adrenoceptor
ChEMBL 656 12 5 9 3.1 CS(=O)(=O)Nc1cc([C@@H](O)CNCC2CCN(S(=O)(=O)c3ccc(-n4cc(CC(=O)O)c5ccccc54)cc3)CC2)ccc1O 10.1016/s0960-894x(02)00608-x
44331346 206638 0 None -5 3 Human 7.5 pEC50 = 7.5 Functional
Beta-2 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-2-adrenoceptorBeta-2 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-2-adrenoceptor
ChEMBL 638 17 5 8 4.2 CCCCCCCCC(=O)Nc1ccc(S(=O)(=O)N2CCC(CNC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)CC2)cc1 10.1016/s0960-894x(02)00608-x
CHEMBL99599 206638 0 None -5 3 Human 7.5 pEC50 = 7.5 Functional
Beta-2 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-2-adrenoceptorBeta-2 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-2-adrenoceptor
ChEMBL 638 17 5 8 4.2 CCCCCCCCC(=O)Nc1ccc(S(=O)(=O)N2CCC(CNC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)CC2)cc1 10.1016/s0960-894x(02)00608-x
44331302 206577 0 None -6 3 Human 7.5 pEC50 = 7.5 Functional
Beta-2 adrenergic receptor agonist activity was determined by a measurement of increased cAMP levels in CHO cells expressing human Beta-2 adrenergic receptorBeta-2 adrenergic receptor agonist activity was determined by a measurement of increased cAMP levels in CHO cells expressing human Beta-2 adrenergic receptor
ChEMBL 667 12 6 8 3.1 CS(=O)(=O)Nc1cc([C@@H](O)CNCC2CCN(S(=O)(=O)c3ccc(NC(=O)NCc4cc(F)ccc4F)cc3)CC2)ccc1O 10.1016/s0960-894x(02)00608-x
CHEMBL99219 206577 0 None -6 3 Human 7.5 pEC50 = 7.5 Functional
Beta-2 adrenergic receptor agonist activity was determined by a measurement of increased cAMP levels in CHO cells expressing human Beta-2 adrenergic receptorBeta-2 adrenergic receptor agonist activity was determined by a measurement of increased cAMP levels in CHO cells expressing human Beta-2 adrenergic receptor
ChEMBL 667 12 6 8 3.1 CS(=O)(=O)Nc1cc([C@@H](O)CNCC2CCN(S(=O)(=O)c3ccc(NC(=O)NCc4cc(F)ccc4F)cc3)CC2)ccc1O 10.1016/s0960-894x(02)00608-x
44268267 18239 0 None 199 2 Human 7.5 pEC50 = 7.5 Functional
Compound was tested for agonist activity against cloned human beta-2 adrenergic receptorCompound was tested for agonist activity against cloned human beta-2 adrenergic receptor
ChEMBL 345 10 3 5 2.8 COc1ccc(CC[C@@H](C)NC[C@@H](O)COc2ccc(O)cc2)cc1 10.1016/s0960-894x(98)00169-3
CHEMBL12719 18239 0 None 199 2 Human 7.5 pEC50 = 7.5 Functional
Compound was tested for agonist activity against cloned human beta-2 adrenergic receptorCompound was tested for agonist activity against cloned human beta-2 adrenergic receptor
ChEMBL 345 10 3 5 2.8 COc1ccc(CC[C@@H](C)NC[C@@H](O)COc2ccc(O)cc2)cc1 10.1016/s0960-894x(98)00169-3
1960 2805 64 None -436 13 Guinea pig 4.5 pEC50 = 4.5 Functional
Activity for Beta-2 adrenergic receptor was assessed from effect on relaxation of guinea pig trachea.Activity for Beta-2 adrenergic receptor was assessed from effect on relaxation of guinea pig trachea.
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00019a001
439260 2805 64 None -436 13 Guinea pig 4.5 pEC50 = 4.5 Functional
Activity for Beta-2 adrenergic receptor was assessed from effect on relaxation of guinea pig trachea.Activity for Beta-2 adrenergic receptor was assessed from effect on relaxation of guinea pig trachea.
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00019a001
505 2805 64 None -436 13 Guinea pig 4.5 pEC50 = 4.5 Functional
Activity for Beta-2 adrenergic receptor was assessed from effect on relaxation of guinea pig trachea.Activity for Beta-2 adrenergic receptor was assessed from effect on relaxation of guinea pig trachea.
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00019a001
CHEMBL1437 2805 64 None -436 13 Guinea pig 4.5 pEC50 = 4.5 Functional
Activity for Beta-2 adrenergic receptor was assessed from effect on relaxation of guinea pig trachea.Activity for Beta-2 adrenergic receptor was assessed from effect on relaxation of guinea pig trachea.
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00019a001
DB00368 2805 64 None -436 13 Guinea pig 4.5 pEC50 = 4.5 Functional
Activity for Beta-2 adrenergic receptor was assessed from effect on relaxation of guinea pig trachea.Activity for Beta-2 adrenergic receptor was assessed from effect on relaxation of guinea pig trachea.
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00019a001
22554040 20105 4 None - 1 Human 5.5 pEC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 441 4 1 5 3.7 CC1=C(C(=O)Nc2ccc(C(=O)N3CCN(c4ccccc4F)CC3)cc2)SCCO1 nan
CHEMBL1305925 20105 4 None - 1 Human 5.5 pEC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 441 4 1 5 3.7 CC1=C(C(=O)Nc2ccc(C(=O)N3CCN(c4ccccc4F)CC3)cc2)SCCO1 nan
24790337 22543 5 None - 1 Human 6.5 pEC50 = 6.5 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 417 7 0 7 3.7 Cc1ccc(OCc2cc(C(=O)N(C)Cc3cnn(-c4ccccc4C)c3)no2)cn1 nan
CHEMBL1327806 22543 5 None - 1 Human 6.5 pEC50 = 6.5 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 417 7 0 7 3.7 Cc1ccc(OCc2cc(C(=O)N(C)Cc3cnn(-c4ccccc4C)c3)no2)cn1 nan
1094286 50549 15 None - 1 Human 7.5 pEC50 = 7.5 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 359 5 1 5 4.2 Cc1ccc(OCC(=O)Nc2ccc(-c3nc4ncccc4o3)cc2)cc1 nan
CHEMBL1577023 50549 15 None - 1 Human 7.5 pEC50 = 7.5 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 359 5 1 5 4.2 Cc1ccc(OCC(=O)Nc2ccc(-c3nc4ncccc4o3)cc2)cc1 nan
11060184 119212 0 None -39 3 Human 7.5 pEC50 = 7.5 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-2 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-2 AR expressed as the negative logarithm of the molar drug concentration
ChEMBL 501 11 4 6 3.5 C[C@H](CNc1ccc(CC(=O)NS(=O)(=O)c2ccccc2)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0101500
CHEMBL347616 119212 0 None -39 3 Human 7.5 pEC50 = 7.5 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-2 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-2 AR expressed as the negative logarithm of the molar drug concentration
ChEMBL 501 11 4 6 3.5 C[C@H](CNc1ccc(CC(=O)NS(=O)(=O)c2ccccc2)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0101500
1499 2052 43 None -165 36 Guinea pig 7.5 pEC50 = 7.5 Functional
Agonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contractionAgonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contraction
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmcl.2012.01.013
3779 2052 43 None -165 36 Guinea pig 7.5 pEC50 = 7.5 Functional
Agonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contractionAgonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contraction
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmcl.2012.01.013
536 2052 43 None -165 36 Guinea pig 7.5 pEC50 = 7.5 Functional
Agonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contractionAgonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contraction
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmcl.2012.01.013
CHEMBL434 2052 43 None -165 36 Guinea pig 7.5 pEC50 = 7.5 Functional
Agonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contractionAgonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contraction
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmcl.2012.01.013
DB01064 2052 43 None -165 36 Guinea pig 7.5 pEC50 = 7.5 Functional
Agonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contractionAgonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contraction
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmcl.2012.01.013
57395043 70033 0 None 3 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 420 12 5 5 3.1 OCc1cc([C@@H](O)CNCCc2ccc(CNCCc3ccccc3)cc2)ccc1O 10.1016/j.bmcl.2011.10.049
CHEMBL1945300 70033 0 None 3 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 420 12 5 5 3.1 OCc1cc([C@@H](O)CNCCc2ccc(CNCCc3ccccc3)cc2)ccc1O 10.1016/j.bmcl.2011.10.049
10347461 105786 0 None 12 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 547 18 4 7 4.8 O=S(=O)(c1ccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc1)C1CCCC1 10.1021/jm401532g
CHEMBL3126384 105786 0 None 12 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 547 18 4 7 4.8 O=S(=O)(c1ccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc1)C1CCCC1 10.1021/jm401532g
CHEMBL3139025 105786 0 None 12 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 547 18 4 7 4.8 O=S(=O)(c1ccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc1)C1CCCC1 10.1021/jm401532g
90644141 111762 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 396 9 5 5 3.6 OCc1cc(C(O)CNCCc2ccc(Nc3ccc(F)cc3)cc2)ccc1O 10.1016/j.bmcl.2014.04.069
CHEMBL3290995 111762 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 396 9 5 5 3.6 OCc1cc(C(O)CNCCc2ccc(Nc3ccc(F)cc3)cc2)ccc1O 10.1016/j.bmcl.2014.04.069
168290228 192355 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 253 4 3 5 1.6 CC(C)(C)NC(CO)c1ccc(N)c([N+](=O)[O-])c1 10.1021/acs.jmedchem.1c02006
CHEMBL5201031 192355 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 253 4 3 5 1.6 CC(C)(C)NC(CO)c1ccc(N)c([N+](=O)[O-])c1 10.1021/acs.jmedchem.1c02006
CHEMBL5222490 192355 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 253 4 3 5 1.6 CC(C)(C)NC(CO)c1ccc(N)c([N+](=O)[O-])c1 10.1021/acs.jmedchem.1c02006
653846 38314 10 None - 1 Human 5.5 pEC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 301 3 1 6 2.8 CCC(=O)Nc1ccc(-c2nn3c(C)nnc3s2)cc1C nan
CHEMBL1464795 38314 10 None - 1 Human 5.5 pEC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 301 3 1 6 2.8 CCC(=O)Nc1ccc(-c2nn3c(C)nnc3s2)cc1C nan
1371669 37341 10 None 64 2 Human 6.5 pEC50 = 6.5 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 373 5 1 5 4.5 Cc1ccc(OCC(=O)Nc2ccc(-c3nc4ncccc4o3)cc2)c(C)c1 nan
CHEMBL1456621 37341 10 None 64 2 Human 6.5 pEC50 = 6.5 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 373 5 1 5 4.5 Cc1ccc(OCC(=O)Nc2ccc(-c3nc4ncccc4o3)cc2)c(C)c1 nan
44441233 147512 0 None -79 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 415 9 4 6 3.8 C[C@H](CNc1cccc(-c2ocnc2C(=O)O)c1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2007.05.069
CHEMBL393471 147512 0 None -79 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 415 9 4 6 3.8 C[C@H](CNc1cccc(-c2ocnc2C(=O)O)c1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2007.05.069
90655864 110760 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assayAgonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assay
ChEMBL 486 15 4 7 2.3 NCCCN(CCNCCc1ccc(O)c2[nH]c(=O)sc12)C(=O)CCOCCc1ccccc1 10.1021/ml4005232
CHEMBL3265161 110760 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assayAgonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assay
ChEMBL 486 15 4 7 2.3 NCCCN(CCNCCc1ccc(O)c2[nH]c(=O)sc12)C(=O)CCOCCc1ccccc1 10.1021/ml4005232
145985170 165835 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 423 10 5 5 3.2 CCCCC(=O)Nc1ccc(CCNC(CO)c2ccc(O)c3[nH]c(=O)ccc23)cc1 10.1016/j.ejmech.2018.04.041
CHEMBL4276877 165835 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 423 10 5 5 3.2 CCCCC(=O)Nc1ccc(CCNC(CO)c2ccc(O)c3[nH]c(=O)ccc23)cc1 10.1016/j.ejmech.2018.04.041
122680878 165985 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 392 6 4 4 3.1 CCc1cc2c(cc1CC)CC(NC(CO)c1ccc(O)c3[nH]c(=O)ccc13)C2 10.1016/j.ejmech.2018.04.041
CHEMBL4279466 165985 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 392 6 4 4 3.1 CCc1cc2c(cc1CC)CC(NC(CO)c1ccc(O)c3[nH]c(=O)ccc13)C2 10.1016/j.ejmech.2018.04.041
141465530 166003 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 363 6 5 4 2.6 O=c1ccc2c(C(CO)NCCc3c[nH]c4ccccc34)ccc(O)c2[nH]1 10.1016/j.ejmech.2018.04.041
CHEMBL4279788 166003 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 363 6 5 4 2.6 O=c1ccc2c(C(CO)NCCc3c[nH]c4ccccc34)ccc(O)c2[nH]1 10.1016/j.ejmech.2018.04.041
57393524 70142 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 538 12 3 6 5.8 CCN(Cc1ccncc1)Cc1cccc(-c2ccc(CCNCCc3ccc(O)c4[nH]c(=O)sc34)cc2)c1 10.1016/j.bmcl.2011.10.049
CHEMBL1946766 70142 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 538 12 3 6 5.8 CCN(Cc1ccncc1)Cc1cccc(-c2ccc(CCNCCc3ccc(O)c4[nH]c(=O)sc34)cc2)c1 10.1016/j.bmcl.2011.10.049
10940242 164635 0 None -31 3 Human 6.5 pEC50 = 6.5 Functional
Concentration that causes 50% inhibition of human beta 2 adrenergic receptor (AR), expressed in CHO cells.Concentration that causes 50% inhibition of human beta 2 adrenergic receptor (AR), expressed in CHO cells.
ChEMBL 515 12 4 6 3.8 C[C@H](CNc1ccc(CCS(=O)(=O)NC(=O)c2ccccc2)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0101500
CHEMBL422876 164635 0 None -31 3 Human 6.5 pEC50 = 6.5 Functional
Concentration that causes 50% inhibition of human beta 2 adrenergic receptor (AR), expressed in CHO cells.Concentration that causes 50% inhibition of human beta 2 adrenergic receptor (AR), expressed in CHO cells.
ChEMBL 515 12 4 6 3.8 C[C@H](CNc1ccc(CCS(=O)(=O)NC(=O)c2ccccc2)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0101500
11002571 47820 0 None -5 3 Human 5.5 pEC50 = 5.5 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-2 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-2 AR expressed as the negative logarithm of the molar drug concentration
ChEMBL 348 8 4 4 3.2 C[C@H](CNc1ccc(C(=O)O)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0101500
CHEMBL155092 47820 0 None -5 3 Human 5.5 pEC50 = 5.5 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-2 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-2 AR expressed as the negative logarithm of the molar drug concentration
ChEMBL 348 8 4 4 3.2 C[C@H](CNc1ccc(C(=O)O)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0101500
2598 3707 52 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
ChEMBL 225 3 4 4 1.5 OC(c1cc(O)cc(c1)O)CNC(C)(C)C 10.1016/j.bmcl.2011.04.135
5403 3707 52 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
ChEMBL 225 3 4 4 1.5 OC(c1cc(O)cc(c1)O)CNC(C)(C)C 10.1016/j.bmcl.2011.04.135
560 3707 52 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
ChEMBL 225 3 4 4 1.5 OC(c1cc(O)cc(c1)O)CNC(C)(C)C 10.1016/j.bmcl.2011.04.135
CHEMBL1760 3707 52 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
ChEMBL 225 3 4 4 1.5 OC(c1cc(O)cc(c1)O)CNC(C)(C)C 10.1016/j.bmcl.2011.04.135
DB00871 3707 52 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
ChEMBL 225 3 4 4 1.5 OC(c1cc(O)cc(c1)O)CNC(C)(C)C 10.1016/j.bmcl.2011.04.135
168288640 192332 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 354 6 3 3 3.5 CCCCNC(CO)c1cc(Br)c(N)c(C(F)(F)F)c1 10.1021/acs.jmedchem.1c02006
CHEMBL5190961 192332 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 354 6 3 3 3.5 CCCCNC(CO)c1cc(Br)c(N)c(C(F)(F)F)c1 10.1021/acs.jmedchem.1c02006
CHEMBL5222387 192332 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 354 6 3 3 3.5 CCCCNC(CO)c1cc(Br)c(N)c(C(F)(F)F)c1 10.1021/acs.jmedchem.1c02006
76315640 84880 0 None -7 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at Homo sapiens (human) beta2 adrenoreceptorAgonist activity at Homo sapiens (human) beta2 adrenoreceptor
ChEMBL 575 12 3 7 5.8 COc1cccc2c(C[C@@H](C)NC[C@H](O)c3cccc(NS(=O)(=O)c4cccs4)c3)cn(Cc3ccccc3)c12 10.1007/s00044-009-9257-x
CHEMBL2260988 84880 0 None -7 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at Homo sapiens (human) beta2 adrenoreceptorAgonist activity at Homo sapiens (human) beta2 adrenoreceptor
ChEMBL 575 12 3 7 5.8 COc1cccc2c(C[C@@H](C)NC[C@H](O)c3cccc(NS(=O)(=O)c4cccs4)c3)cn(Cc3ccccc3)c12 10.1007/s00044-009-9257-x
25023950 176368 0 None - 1 Golden hamster 7.5 pEC50 = 7.5 Functional
Agonist activity at adrenergic beta2 receptor in Syrian hamster DDT1 MF2 cells assessed as stimulation of cAMP accumulation by radioimmunoassay in presence of 1 uM DPCPXAgonist activity at adrenergic beta2 receptor in Syrian hamster DDT1 MF2 cells assessed as stimulation of cAMP accumulation by radioimmunoassay in presence of 1 uM DPCPX
ChEMBL 517 13 8 13 -0.8 O=CNc1cc(C(O)CNCCCCNc2ncnc3c2ncn3[C@@H]2O[C@H](CO)[C@@H](O)[C@H]2O)ccc1O 10.1021/jm800613s
CHEMBL462273 176368 0 None - 1 Golden hamster 7.5 pEC50 = 7.5 Functional
Agonist activity at adrenergic beta2 receptor in Syrian hamster DDT1 MF2 cells assessed as stimulation of cAMP accumulation by radioimmunoassay in presence of 1 uM DPCPXAgonist activity at adrenergic beta2 receptor in Syrian hamster DDT1 MF2 cells assessed as stimulation of cAMP accumulation by radioimmunoassay in presence of 1 uM DPCPX
ChEMBL 517 13 8 13 -0.8 O=CNc1cc(C(O)CNCCCCNc2ncnc3c2ncn3[C@@H]2O[C@H](CO)[C@@H](O)[C@H]2O)ccc1O 10.1021/jm800613s
4611324 21556 8 None - 1 Human 7.5 pEC50 = 7.5 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory)
ChEMBL 401 7 1 4 4.1 CCCCC(=O)Nc1ccc(S(=O)(=O)N2CCCCC2c2cccnc2)cc1 nan
CHEMBL1319108 21556 8 None - 1 Human 7.5 pEC50 = 7.5 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory)
ChEMBL 401 7 1 4 4.1 CCCCC(=O)Nc1ccc(S(=O)(=O)N2CCCCC2c2cccnc2)cc1 nan
24180436 92772 0 None -1 2 Guinea pig 5.5 pEC50 = 5.5 Functional
Agonist activity at adrenergic beta2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of propranololAgonist activity at adrenergic beta2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of propranolol
ChEMBL 527 10 4 10 2.6 CC(Cc1ccc(Oc2no[n+]([O-])c2S(=O)(=O)c2ccccc2)cc1)NCC(O)c1cc(O)cc(O)c1 10.1021/jm0704595
CHEMBL244687 92772 0 None -1 2 Guinea pig 5.5 pEC50 = 5.5 Functional
Agonist activity at adrenergic beta2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of propranololAgonist activity at adrenergic beta2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of propranolol
ChEMBL 527 10 4 10 2.6 CC(Cc1ccc(Oc2no[n+]([O-])c2S(=O)(=O)c2ccccc2)cc1)NCC(O)c1cc(O)cc(O)c1 10.1021/jm0704595
139368780 184640 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells co-expressing V2 receptor assessed as induction of beta-arrestin 2 recruitment preincubated for 20 mins followed by beta2 receptor agonist and measured after 6 hrs by Bright-Glo reagent based chemiluminescence assayAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells co-expressing V2 receptor assessed as induction of beta-arrestin 2 recruitment preincubated for 20 mins followed by beta2 receptor agonist and measured after 6 hrs by Bright-Glo reagent based chemiluminescence assay
ChEMBL 611 12 2 6 5.4 COc1ccc(Sc2ccc(S(=O)(=O)N(C)C(C)C)cc2C(=O)N[C@@H](CC(N)=O)Cc2ccc(C(C)(C)C)cc2)cc1 10.1021/acs.jmedchem.0c01195
CHEMBL4858076 184640 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells co-expressing V2 receptor assessed as induction of beta-arrestin 2 recruitment preincubated for 20 mins followed by beta2 receptor agonist and measured after 6 hrs by Bright-Glo reagent based chemiluminescence assayAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells co-expressing V2 receptor assessed as induction of beta-arrestin 2 recruitment preincubated for 20 mins followed by beta2 receptor agonist and measured after 6 hrs by Bright-Glo reagent based chemiluminescence assay
ChEMBL 611 12 2 6 5.4 COc1ccc(Sc2ccc(S(=O)(=O)N(C)C(C)C)cc2C(=O)N[C@@H](CC(N)=O)Cc2ccc(C(C)(C)C)cc2)cc1 10.1021/acs.jmedchem.0c01195
16222940 185882 0 None -47863 4 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 433 10 4 5 4.1 CC(C)Cc1cc(-c2ccc(CCNC[C@H](O)c3ccc(N)nc3)cc2)ccc1C(=O)O 10.1021/jm8000345
CHEMBL487682 185882 0 None -47863 4 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 433 10 4 5 4.1 CC(C)Cc1cc(-c2ccc(CCNC[C@H](O)c3ccc(N)nc3)cc2)ccc1C(=O)O 10.1021/jm8000345
44591507 178769 0 None -47863 4 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 433 10 4 5 4.1 CC(C)Cc1cc(-c2ccc(CCNC[C@H](O)c3cnccc3N)cc2)ccc1C(=O)O 10.1021/jm9000709
CHEMBL473702 178769 0 None -47863 4 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 433 10 4 5 4.1 CC(C)Cc1cc(-c2ccc(CCNC[C@H](O)c3cnccc3N)cc2)ccc1C(=O)O 10.1021/jm9000709
10626150 99551 0 None -208 3 Human 5.5 pEC50 = 5.5 Functional
Increased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 2 adrenergic receptorsIncreased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 2 adrenergic receptors
ChEMBL 534 11 5 9 1.3 CCOC(=O)CNC(=O)c1ccc(N2CCC(NC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)CC2)cc1 10.1021/jm000544b
CHEMBL286868 99551 0 None -208 3 Human 5.5 pEC50 = 5.5 Functional
Increased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 2 adrenergic receptorsIncreased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 2 adrenergic receptors
ChEMBL 534 11 5 9 1.3 CCOC(=O)CNC(=O)c1ccc(N2CCC(NC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)CC2)cc1 10.1021/jm000544b
145990515 166465 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 340 6 5 5 1.8 O=c1ccc2c([C@H](CO)NCCc3ccc(O)cc3)ccc(O)c2[nH]1 10.1016/j.ejmech.2018.04.041
CHEMBL4288610 166465 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 340 6 5 5 1.8 O=c1ccc2c([C@H](CO)NCCc3ccc(O)cc3)ccc(O)c2[nH]1 10.1016/j.ejmech.2018.04.041
16735259 85207 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulationAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulation
ChEMBL 317 7 4 5 2.4 COc1ccc(C[C@H](C)NC[C@@H](O)c2cc(O)cc(O)c2)cc1 10.1016/j.bmc.2013.11.030
CHEMBL228417 85207 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulationAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulation
ChEMBL 317 7 4 5 2.4 COc1ccc(C[C@H](C)NC[C@@H](O)c2cc(O)cc(O)c2)cc1 10.1016/j.bmc.2013.11.030
11270071 98520 0 None -7 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at Homo sapiens (human) beta2 adrenoreceptorAgonist activity at Homo sapiens (human) beta2 adrenoreceptor
ChEMBL 328 6 3 2 4.1 C[C@H](Cc1c[nH]c2ccccc12)NC[C@@H](O)c1cccc(Cl)c1 10.1007/s00044-009-9257-x
CHEMBL279931 98520 0 None -7 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at Homo sapiens (human) beta2 adrenoreceptorAgonist activity at Homo sapiens (human) beta2 adrenoreceptor
ChEMBL 328 6 3 2 4.1 C[C@H](Cc1c[nH]c2ccccc12)NC[C@@H](O)c1cccc(Cl)c1 10.1007/s00044-009-9257-x
11270071 98520 0 None -7 3 Human 6.5 pEC50 = 6.5 Functional
Agonistic activity against human Beta-2 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonistic activity against human Beta-2 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 328 6 3 2 4.1 C[C@H](Cc1c[nH]c2ccccc12)NC[C@@H](O)c1cccc(Cl)c1 10.1016/s0960-894x(03)00073-8
CHEMBL279931 98520 0 None -7 3 Human 6.5 pEC50 = 6.5 Functional
Agonistic activity against human Beta-2 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonistic activity against human Beta-2 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 328 6 3 2 4.1 C[C@H](Cc1c[nH]c2ccccc12)NC[C@@H](O)c1cccc(Cl)c1 10.1016/s0960-894x(03)00073-8
2839830 49775 9 None 9 2 Human 5.5 pEC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 287 4 0 2 3.9 CC(C)=CCC(C)(C)C1OCCN1C(=O)c1ccccc1 nan
CHEMBL1569630 49775 9 None 9 2 Human 5.5 pEC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 287 4 0 2 3.9 CC(C)=CCC(C)(C)C1OCCN1C(=O)c1ccccc1 nan
663855 32670 8 None - 1 Human 5.5 pEC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 440 5 1 9 2.3 c1nc(NCCN2CCOCC2)c2sc3nc(N4CCOCC4)c4c(c3c2n1)CCC4 nan
CHEMBL1415227 32670 8 None - 1 Human 5.5 pEC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 440 5 1 9 2.3 c1nc(NCCN2CCOCC2)c2sc3nc(N4CCOCC4)c4c(c3c2n1)CCC4 nan
12989000 192330 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 340 4 3 3 3.1 CC(C)NC(CO)c1cc(Br)c(N)c(C(F)(F)F)c1 10.1021/acs.jmedchem.1c02006
CHEMBL5192613 192330 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 340 4 3 3 3.1 CC(C)NC(CO)c1cc(Br)c(N)c(C(F)(F)F)c1 10.1021/acs.jmedchem.1c02006
CHEMBL5222371 192330 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 340 4 3 3 3.1 CC(C)NC(CO)c1cc(Br)c(N)c(C(F)(F)F)c1 10.1021/acs.jmedchem.1c02006
24820094 59387 1 None - 1 Human 5.5 pEC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 409 5 1 4 5.1 Cc1ncc(CN2CCCC(C(=O)Nc3ccc(-c4cccc(F)c4)cc3)C2)s1 nan
CHEMBL1723653 59387 1 None - 1 Human 5.5 pEC50 = 5.5 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 409 5 1 4 5.1 Cc1ncc(CN2CCCC(C(=O)Nc3ccc(-c4cccc(F)c4)cc3)C2)s1 nan
4312580 39907 7 None - 1 Human 7.5 pEC50 = 7.5 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 436 5 1 7 2.8 Cc1cc(C)n2nc(C(=O)Nc3cccc(S(=O)(=O)N(C)c4ccccc4)c3)nc2n1 nan
CHEMBL1479957 39907 7 None - 1 Human 7.5 pEC50 = 7.5 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 436 5 1 7 2.8 Cc1cc(C)n2nc(C(=O)Nc3cccc(S(=O)(=O)N(C)c4ccccc4)c3)nc2n1 nan
9853471 203136 0 None -177 3 Human 6.5 pEC50 = 6.5 Functional
Compound was evaluated for its inhibitory activity against human beta-2 adrenergic receptor (AR)Compound was evaluated for its inhibitory activity against human beta-2 adrenergic receptor (AR)
ChEMBL 628 12 6 6 6.7 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(-c3ccc(CC4NCCc5cc(O)c(O)cc54)cc3)cc2)cc1 10.1016/s0960-894x(00)00459-5
CHEMBL75604 203136 0 None -177 3 Human 6.5 pEC50 = 6.5 Functional
Compound was evaluated for its inhibitory activity against human beta-2 adrenergic receptor (AR)Compound was evaluated for its inhibitory activity against human beta-2 adrenergic receptor (AR)
ChEMBL 628 12 6 6 6.7 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(-c3ccc(CC4NCCc5cc(O)c(O)cc54)cc3)cc2)cc1 10.1016/s0960-894x(00)00459-5
3167769 23786 5 None 28 2 Human 6.5 pEC50 = 6.5 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 531 6 0 8 6.6 O=C(CSc1nnc(-c2ccncc2)n1Cc1ccco1)N1c2ccccc2Sc2ccc(Cl)cc21 nan
CHEMBL1337858 23786 5 None 28 2 Human 6.5 pEC50 = 6.5 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 531 6 0 8 6.6 O=C(CSc1nnc(-c2ccncc2)n1Cc1ccco1)N1c2ccccc2Sc2ccc(Cl)cc21 nan
21044607 192328 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 340 8 3 4 3.0 CCOCCCNC(CO)c1cc(Cl)c(N)c(C(F)(F)F)c1 10.1021/acs.jmedchem.1c02006
CHEMBL5191729 192328 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 340 8 3 4 3.0 CCOCCCNC(CO)c1cc(Cl)c(N)c(C(F)(F)F)c1 10.1021/acs.jmedchem.1c02006
CHEMBL5222365 192328 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 340 8 3 4 3.0 CCOCCCNC(CO)c1cc(Cl)c(N)c(C(F)(F)F)c1 10.1021/acs.jmedchem.1c02006
24794116 66740 1 None - 1 Human 6.5 pEC50 = 6.5 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory)
ChEMBL 410 6 0 4 4.7 CSc1ccc(CN2CCC(Oc3ccc(C(=O)N4CCCC4)cc3)CC2)cc1 nan
CHEMBL1873201 66740 1 None - 1 Human 6.5 pEC50 = 6.5 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory)
ChEMBL 410 6 0 4 4.7 CSc1ccc(CN2CCC(Oc3ccc(C(=O)N4CCCC4)cc3)CC2)cc1 nan
44444173 93534 0 None -5 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP levelAgonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP level
ChEMBL 516 11 4 7 3.3 CC(C)(Cc1ccc(Oc2ccc(C(N)=O)cn2)cc1)NC[C@H](O)COc1cccc2c1C1(CC1)C(=O)N2 10.1016/j.bmcl.2007.09.011
CHEMBL248547 93534 0 None -5 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP levelAgonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP level
ChEMBL 516 11 4 7 3.3 CC(C)(Cc1ccc(Oc2ccc(C(N)=O)cn2)cc1)NC[C@H](O)COc1cccc2c1C1(CC1)C(=O)N2 10.1016/j.bmcl.2007.09.011
2977891 21588 8 None - 1 Human 7.5 pEC50 = 7.5 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 452 5 0 5 1.8 CN(CC(=O)N1CCN(c2ccccn2)CC1)S(=O)(=O)c1ccc(Br)cc1 nan
CHEMBL1319376 21588 8 None - 1 Human 7.5 pEC50 = 7.5 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 452 5 0 5 1.8 CN(CC(=O)N1CCN(c2ccccn2)CC1)S(=O)(=O)c1ccc(Br)cc1 nan
1716469 59526 1 None - 1 Human 6.5 pEC50 = 6.5 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 393 8 1 6 3.2 CCOC(=O)c1cn(C2CC2)c2c(F)c(NCCCN(C)C)c(F)cc2c1=O nan
CHEMBL1728955 59526 1 None - 1 Human 6.5 pEC50 = 6.5 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 393 8 1 6 3.2 CCOC(=O)c1cn(C2CC2)c2c(F)c(NCCCN(C)C)c(F)cc2c1=O nan
9804536 165133 0 None -169 3 Human 6.5 pEC50 = 6.5 Functional
Antagonist activity at human beta2 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta2 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 465 11 4 5 3.5 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2cccc3[nH]ccc23)cc1)c1ccccc1 10.1016/j.ejmech.2018.03.032
CHEMBL4245391 165133 0 None -169 3 Human 6.5 pEC50 = 6.5 Functional
Antagonist activity at human beta2 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta2 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 465 11 4 5 3.5 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2cccc3[nH]ccc23)cc1)c1ccccc1 10.1016/j.ejmech.2018.03.032
135799890 185195 0 None - 1 Human 4.5 pEC50 = 4.5 Functional
Agonist activity at beta2 adrenoceptor in HEK293 cells co-expressing V2 receptor assessed as increase in cAMP accumulation measured after 30 mins by HTRF assayAgonist activity at beta2 adrenoceptor in HEK293 cells co-expressing V2 receptor assessed as increase in cAMP accumulation measured after 30 mins by HTRF assay
ChEMBL 304 8 4 4 2.4 CCCCCCNC(CO)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/acs.jmedchem.0c01195
CHEMBL4866730 185195 0 None - 1 Human 4.5 pEC50 = 4.5 Functional
Agonist activity at beta2 adrenoceptor in HEK293 cells co-expressing V2 receptor assessed as increase in cAMP accumulation measured after 30 mins by HTRF assayAgonist activity at beta2 adrenoceptor in HEK293 cells co-expressing V2 receptor assessed as increase in cAMP accumulation measured after 30 mins by HTRF assay
ChEMBL 304 8 4 4 2.4 CCCCCCNC(CO)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/acs.jmedchem.0c01195
3164412 52873 9 None - 1 Human 6.5 pEC50 = 6.5 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset2. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset2. (Class of assay: confirmatory)
ChEMBL 408 5 0 5 1.7 CN(CC(=O)N1CCN(c2ccccn2)CC1)S(=O)(=O)c1ccc(Cl)cc1 nan
CHEMBL1598434 52873 9 None - 1 Human 6.5 pEC50 = 6.5 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset2. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset2. (Class of assay: confirmatory)
ChEMBL 408 5 0 5 1.7 CN(CC(=O)N1CCN(c2ccccn2)CC1)S(=O)(=O)c1ccc(Cl)cc1 nan
90666113 108844 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP productionAgonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP production
ChEMBL 744 18 6 9 7.5 Cc1cc(C)c(NC(=O)OC2CCN(CCCCCCCCCNC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)CC2)c(-c2ccc(O)c(Cl)c2)c1 10.1039/C1MD00140J
CHEMBL3219045 108844 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP productionAgonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP production
ChEMBL 744 18 6 9 7.5 Cc1cc(C)c(NC(=O)OC2CCN(CCCCCCCCCNC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)CC2)c(-c2ccc(O)c(Cl)c2)c1 10.1039/C1MD00140J
44392558 64909 0 None -2 3 Human 7.4 pEC50 = 7.4 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-2 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-2 adrenergic receptor
ChEMBL 471 11 4 6 4.1 CC(C)=CCNc1cccc([C@@H](O)CN[C@H](C)Cc2c[nH]c3c(OS(C)(=O)=O)cccc23)c1 10.1016/j.bmcl.2004.12.033
CHEMBL182770 64909 0 None -2 3 Human 7.4 pEC50 = 7.4 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-2 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-2 adrenergic receptor
ChEMBL 471 11 4 6 4.1 CC(C)=CCNc1cccc([C@@H](O)CN[C@H](C)Cc2c[nH]c3c(OS(C)(=O)=O)cccc23)c1 10.1016/j.bmcl.2004.12.033
9831168 202986 0 None -1 3 Human 7.4 pEC50 = 7.4 Functional
Percent adenylyl cyclase activation at 10000 nM of compound concentrationPercent adenylyl cyclase activation at 10000 nM of compound concentration
ChEMBL 552 11 6 6 5.0 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC3NCCc4cc(O)c(O)cc43)cc2)cc1 10.1016/s0960-894x(00)00459-5
CHEMBL74085 202986 0 None -1 3 Human 7.4 pEC50 = 7.4 Functional
Percent adenylyl cyclase activation at 10000 nM of compound concentrationPercent adenylyl cyclase activation at 10000 nM of compound concentration
ChEMBL 552 11 6 6 5.0 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC3NCCc4cc(O)c(O)cc43)cc2)cc1 10.1016/s0960-894x(00)00459-5
16013947 21470 6 None - 1 Human 7.4 pEC50 = 7.4 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory)
ChEMBL 442 6 1 8 1.9 CC(=O)Nc1ccc(S(=O)(=O)N2CCC(Oc3ccc(-n4cnnn4)cc3)CC2)cc1 nan
CHEMBL1318405 21470 6 None - 1 Human 7.4 pEC50 = 7.4 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory)
ChEMBL 442 6 1 8 1.9 CC(=O)Nc1ccc(S(=O)(=O)N2CCC(Oc3ccc(-n4cnnn4)cc3)CC2)cc1 nan
1236197 24748 10 None - 1 Human 5.4 pEC50 = 5.4 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 352 5 1 5 4.0 CC(=O)Nc1ccc(-c2nnc(SCc3ccc(C)cc3)n2C)cc1 nan
CHEMBL1346173 24748 10 None - 1 Human 5.4 pEC50 = 5.4 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 352 5 1 5 4.0 CC(=O)Nc1ccc(-c2nnc(SCc3ccc(C)cc3)n2C)cc1 nan
9896742 203226 0 None 2 3 Human 7.4 pEC50 = 7.4 Functional
Percent adenylyl cyclase activation at 10000 nM of compound concentrationPercent adenylyl cyclase activation at 10000 nM of compound concentration
ChEMBL 618 12 6 7 6.0 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc3cc(OCC4NCCc5cc(O)c(O)cc54)ccc3c2)cc1 10.1016/s0960-894x(00)00459-5
CHEMBL76403 203226 0 None 2 3 Human 7.4 pEC50 = 7.4 Functional
Percent adenylyl cyclase activation at 10000 nM of compound concentrationPercent adenylyl cyclase activation at 10000 nM of compound concentration
ChEMBL 618 12 6 7 6.0 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc3cc(OCC4NCCc5cc(O)c(O)cc54)ccc3c2)cc1 10.1016/s0960-894x(00)00459-5
244359 39800 19 None - 1 Human 7.4 pEC50 = 7.4 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 357 4 0 3 3.6 O=C(C(c1ccccc1)c1ccccc1)N1CCN(c2ccccn2)CC1 nan
CHEMBL1479163 39800 19 None - 1 Human 7.4 pEC50 = 7.4 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 357 4 0 3 3.6 O=C(C(c1ccccc1)c1ccccc1)N1CCN(c2ccccn2)CC1 nan
21044603 192273 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 384 8 3 4 3.1 CCOCCCNC(CO)c1cc(Br)c(N)c(C(F)(F)F)c1 10.1021/acs.jmedchem.1c02006
CHEMBL5187056 192273 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 384 8 3 4 3.1 CCOCCCNC(CO)c1cc(Br)c(N)c(C(F)(F)F)c1 10.1021/acs.jmedchem.1c02006
CHEMBL5221997 192273 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 384 8 3 4 3.1 CCOCCCNC(CO)c1cc(Br)c(N)c(C(F)(F)F)c1 10.1021/acs.jmedchem.1c02006
1202551 26432 11 None - 1 Human 5.4 pEC50 = 5.4 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 366 3 0 3 5.1 Cc1cccc2nc(COc3ccc4ccccc4c3Br)cn12 nan
CHEMBL1361693 26432 11 None - 1 Human 5.4 pEC50 = 5.4 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 366 3 0 3 5.1 Cc1cccc2nc(COc3ccc4ccccc4c3Br)cn12 nan
559929 4816 10 None -4 2 Guinea pig 7.4 pEC50 = 7.4 Functional
Agonistic activity (beta2- adrenergic) for the percent maximal relaxation of isolated guinea pig tracheaAgonistic activity (beta2- adrenergic) for the percent maximal relaxation of isolated guinea pig trachea
ChEMBL 273 5 4 5 1.4 CC(C)(C)NCC(O)COc1ccc(O)c(O)c1F 10.1021/jm00107a027
CHEMBL10453 4816 10 None -4 2 Guinea pig 7.4 pEC50 = 7.4 Functional
Agonistic activity (beta2- adrenergic) for the percent maximal relaxation of isolated guinea pig tracheaAgonistic activity (beta2- adrenergic) for the percent maximal relaxation of isolated guinea pig trachea
ChEMBL 273 5 4 5 1.4 CC(C)(C)NCC(O)COc1ccc(O)c(O)c1F 10.1021/jm00107a027
24979207 35382 6 None - 1 Human 7.4 pEC50 = 7.4 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 374 6 1 5 2.2 CCN(CC)S(=O)(=O)c1cc(NC(=O)C2=COCCO2)ccc1Cl nan
CHEMBL1439691 35382 6 None - 1 Human 7.4 pEC50 = 7.4 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 374 6 1 5 2.2 CCN(CC)S(=O)(=O)c1cc(NC(=O)C2=COCCO2)ccc1Cl nan
3762 14316 24 None -1 2 Human 5.4 pEC50 = 5.4 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 239 5 4 4 1.9 CCC(NC(C)C)C(O)c1ccc(O)c(O)c1 nan
CHEMBL1201153 14316 24 None -1 2 Human 5.4 pEC50 = 5.4 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 239 5 4 4 1.9 CCC(NC(C)C)C(O)c1ccc(O)c(O)c1 nan
CHEMBL1201213 14316 24 None -1 2 Human 5.4 pEC50 = 5.4 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 239 5 4 4 1.9 CCC(NC(C)C)C(O)c1ccc(O)c(O)c1 nan
44428080 148904 0 None - 1 Guinea pig 7.4 pEC50 = 7.4 Functional
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contractionAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction
ChEMBL 511 10 4 10 3.4 CC(Cc1ccc(Oc2nonc2S(=O)(=O)c2ccccc2)cc1)NCC(O)c1cc(O)cc(O)c1 10.1021/jm0704595
CHEMBL394600 148904 0 None - 1 Guinea pig 7.4 pEC50 = 7.4 Functional
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contractionAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction
ChEMBL 511 10 4 10 3.4 CC(Cc1ccc(Oc2nonc2S(=O)(=O)c2ccccc2)cc1)NCC(O)c1cc(O)cc(O)c1 10.1021/jm0704595
46221396 8455 0 None 1 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assayAgonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assay
ChEMBL 364 4 4 4 2.6 Cc1cc2c(cc1C)CC(NC[C@H](O)c1ccc(O)c3[nH]c(=O)ccc13)C2 10.1021/jm100068m
CHEMBL1094483 8455 0 None 1 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assayAgonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assay
ChEMBL 364 4 4 4 2.6 Cc1cc2c(cc1C)CC(NC[C@H](O)c1ccc(O)c3[nH]c(=O)ccc13)C2 10.1021/jm100068m
11957285 41350 6 None - 1 Human 7.4 pEC50 = 7.4 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 415 8 2 7 2.4 O=C(CCCCCn1c(=O)[nH]c2ccsc2c1=O)NCc1ccc2c(c1)OCO2 nan
CHEMBL1491674 41350 6 None - 1 Human 7.4 pEC50 = 7.4 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 415 8 2 7 2.4 O=C(CCCCCn1c(=O)[nH]c2ccsc2c1=O)NCc1ccc2c(c1)OCO2 nan
3164412 52873 9 None - 1 Human 7.4 pEC50 = 7.4 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 408 5 0 5 1.7 CN(CC(=O)N1CCN(c2ccccn2)CC1)S(=O)(=O)c1ccc(Cl)cc1 nan
CHEMBL1598434 52873 9 None - 1 Human 7.4 pEC50 = 7.4 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 408 5 0 5 1.7 CN(CC(=O)N1CCN(c2ccccn2)CC1)S(=O)(=O)c1ccc(Cl)cc1 nan
1499 2052 43 None -72 36 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2011.05.064
3779 2052 43 None -72 36 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2011.05.064
536 2052 43 None -72 36 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2011.05.064
CHEMBL434 2052 43 None -72 36 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2011.05.064
DB01064 2052 43 None -72 36 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2011.05.064
1499 2052 43 None -72 36 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmcl.2011.04.135
3779 2052 43 None -72 36 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmcl.2011.04.135
536 2052 43 None -72 36 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmcl.2011.04.135
CHEMBL434 2052 43 None -72 36 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmcl.2011.04.135
DB01064 2052 43 None -72 36 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmcl.2011.04.135
145981079 166118 0 None 39 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 358 6 4 4 2.8 O=c1ccc2c(C(CO)NCCc3ccc(Cl)cc3)ccc(O)c2[nH]1 10.1016/j.ejmech.2018.04.041
CHEMBL4282047 166118 0 None 39 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 358 6 4 4 2.8 O=c1ccc2c(C(CO)NCCc3ccc(Cl)cc3)ccc(O)c2[nH]1 10.1016/j.ejmech.2018.04.041
57400228 70027 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 413 8 4 6 2.8 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3ccc(CN4CCCC4)cc3)c2s1 10.1016/j.bmcl.2011.10.049
CHEMBL1945295 70027 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 413 8 4 6 2.8 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3ccc(CN4CCCC4)cc3)c2s1 10.1016/j.bmcl.2011.10.049
443372 10123 23 None -3 8 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 211 4 4 4 1.1 CC(C)NC[C@H](O)c1ccc(O)c(O)c1 10.1021/jm401532g
CHEMBL1160723 10123 23 None -3 8 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 211 4 4 4 1.1 CC(C)NC[C@H](O)c1ccc(O)c(O)c1 10.1021/jm401532g
CHEMBL2062275 10123 23 None -3 8 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 211 4 4 4 1.1 CC(C)NC[C@H](O)c1ccc(O)c(O)c1 10.1021/jm401532g
11318358 105938 0 None 50 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 519 16 4 7 3.8 O=S1(=O)CCCc2ccc(CCCCOCCCCCCNC[C@H](O)c3ccc(O)c(CO)c3)cc21 10.1021/jm401532g
CHEMBL3126387 105938 0 None 50 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 519 16 4 7 3.8 O=S1(=O)CCCc2ccc(CCCCOCCCCCCNC[C@H](O)c3ccc(O)c(CO)c3)cc21 10.1021/jm401532g
CHEMBL3139613 105938 0 None 50 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 519 16 4 7 3.8 O=S1(=O)CCCc2ccc(CCCCOCCCCCCNC[C@H](O)c3ccc(O)c(CO)c3)cc21 10.1021/jm401532g
1499 2052 43 None -72 36 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2011.08.043
3779 2052 43 None -72 36 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2011.08.043
536 2052 43 None -72 36 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2011.08.043
CHEMBL434 2052 43 None -72 36 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2011.08.043
DB01064 2052 43 None -72 36 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2011.08.043
1499 2052 43 None -72 36 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm801016j
3779 2052 43 None -72 36 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm801016j
536 2052 43 None -72 36 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm801016j
CHEMBL434 2052 43 None -72 36 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm801016j
DB01064 2052 43 None -72 36 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm801016j
1499 2052 43 None -72 36 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm100326d
3779 2052 43 None -72 36 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm100326d
536 2052 43 None -72 36 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm100326d
CHEMBL434 2052 43 None -72 36 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm100326d
DB01064 2052 43 None -72 36 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm100326d
57403563 69865 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 482 13 6 8 2.9 COc1ccc(C(O)CNc2ccc(CCNCC(O)c3ccc(O)c(CO)c3)cc2)c(OC)c1 10.1016/j.bmcl.2011.11.072
CHEMBL1940822 69865 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 482 13 6 8 2.9 COc1ccc(C(O)CNc2ccc(CCNCC(O)c3ccc(O)c(CO)c3)cc2)c(OC)c1 10.1016/j.bmcl.2011.11.072
57391348 69871 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 498 12 6 6 4.6 OCc1cc(C(O)CNCCc2ccc(NCC(O)c3ccc(-c4ccccc4)cc3)cc2)ccc1O 10.1016/j.bmcl.2011.11.072
CHEMBL1940828 69871 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 498 12 6 6 4.6 OCc1cc(C(O)CNCCc2ccc(NCC(O)c3ccc(-c4ccccc4)cc3)cc2)ccc1O 10.1016/j.bmcl.2011.11.072
1084214 45263 9 None - 1 Human 6.4 pEC50 = 6.4 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 432 8 1 6 2.7 CCOC(=O)c1ccc(NC(=O)COc2ccc(S(=O)(=O)N3CCCC3)cc2)cc1 nan
CHEMBL1528594 45263 9 None - 1 Human 6.4 pEC50 = 6.4 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 432 8 1 6 2.7 CCOC(=O)c1ccc(NC(=O)COc2ccc(S(=O)(=O)N3CCCC3)cc2)cc1 nan
5808 176196 20 None 1 5 Human 6.4 pEC50 = 6.4 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 211 4 4 4 1.1 CC(C)NC[C@@H](O)c1ccc(O)c(O)c1 nan
CHEMBL1257092 176196 20 None 1 5 Human 6.4 pEC50 = 6.4 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 211 4 4 4 1.1 CC(C)NC[C@@H](O)c1ccc(O)c(O)c1 nan
CHEMBL460574 176196 20 None 1 5 Human 6.4 pEC50 = 6.4 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 211 4 4 4 1.1 CC(C)NC[C@@H](O)c1ccc(O)c(O)c1 nan
11003341 46021 0 None -15 3 Human 6.4 pEC50 = 6.4 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-2 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-2 AR expressed as the negative logarithm of the molar drug concentration
ChEMBL 376 10 4 4 3.5 C[C@H](CNc1ccc(CCC(=O)O)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0101500
CHEMBL153558 46021 0 None -15 3 Human 6.4 pEC50 = 6.4 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-2 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-2 AR expressed as the negative logarithm of the molar drug concentration
ChEMBL 376 10 4 4 3.5 C[C@H](CNc1ccc(CCC(=O)O)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0101500
11003341 46021 0 None -15 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 376 10 4 4 3.5 C[C@H](CNc1ccc(CCC(=O)O)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2007.05.069
CHEMBL153558 46021 0 None -15 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 376 10 4 4 3.5 C[C@H](CNc1ccc(CCC(=O)O)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2007.05.069
44441232 93342 0 None -316 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 415 9 4 6 3.8 C[C@H](CNc1ccc(-c2ocnc2C(=O)O)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2007.05.069
CHEMBL247519 93342 0 None -316 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 415 9 4 6 3.8 C[C@H](CNc1ccc(-c2ocnc2C(=O)O)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2007.05.069
90644145 111739 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 446 9 4 5 4.1 OCc1cc(C(O)CNCCc2ccc(N3CCC(c4ccccc4)CC3)cc2)ccc1O 10.1016/j.bmcl.2014.04.069
CHEMBL3290974 111739 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 446 9 4 5 4.1 OCc1cc(C(O)CNCCc2ccc(N3CCC(c4ccccc4)CC3)cc2)ccc1O 10.1016/j.bmcl.2014.04.069
168290423 192358 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 356 5 3 3 3.1 Nc1c(F)cc(C(CO)NCc2ccc(F)cc2)cc1Br 10.1021/acs.jmedchem.1c02006
CHEMBL5201243 192358 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 356 5 3 3 3.1 Nc1c(F)cc(C(CO)NCc2ccc(F)cc2)cc1Br 10.1021/acs.jmedchem.1c02006
CHEMBL5222511 192358 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 356 5 3 3 3.1 Nc1c(F)cc(C(CO)NCc2ccc(F)cc2)cc1Br 10.1021/acs.jmedchem.1c02006
11661536 75608 0 None -63 3 Human 5.4 pEC50 = 5.4 Functional
Activity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 411 9 4 5 3.8 O=C(O)c1cncc(-c2cccc(NCCNC[C@H](O)c3cccc(Cl)c3)c2)c1 10.1021/jm0509445
CHEMBL205389 75608 0 None -63 3 Human 5.4 pEC50 = 5.4 Functional
Activity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 411 9 4 5 3.8 O=C(O)c1cncc(-c2cccc(NCCNC[C@H](O)c3cccc(Cl)c3)c2)c1 10.1021/jm0509445
53239456 61474 0 None -1 2 Guinea pig 8.4 pEC50 = 8.4 Functional
Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as bronchorelaxation activity against histamine-induced contractionAgonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as bronchorelaxation activity against histamine-induced contraction
ChEMBL 705 19 5 7 7.8 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCCCOc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)ccc1O)C(C)C 10.1016/j.bmcl.2010.10.132
CHEMBL1773267 61474 0 None -1 2 Guinea pig 8.4 pEC50 = 8.4 Functional
Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as bronchorelaxation activity against histamine-induced contractionAgonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as bronchorelaxation activity against histamine-induced contraction
ChEMBL 705 19 5 7 7.8 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCCCOc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)ccc1O)C(C)C 10.1016/j.bmcl.2010.10.132
56677231 63293 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assayAgonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assay
ChEMBL 367 7 4 5 3.5 COc1ccc(C[C@H](C)NC[C@H](O)c2cc(O)cc(O)c2)c2ccccc12 10.1016/j.bmc.2009.11.062
CHEMBL1800934 63293 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assayAgonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assay
ChEMBL 367 7 4 5 3.5 COc1ccc(C[C@H](C)NC[C@H](O)c2cc(O)cc(O)c2)c2ccccc12 10.1016/j.bmc.2009.11.062
59548060 124732 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 894 18 6 10 7.1 COc1ccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1CC(C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645336 124732 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 894 18 6 10 7.1 COc1ccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1CC(C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
45484558 195149 0 None 4 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP level
ChEMBL 498 11 8 7 1.6 CC(C)(Cc1ccc(NC(=O)CCCNC(=N)N)cc1)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmcl.2009.06.104
CHEMBL565770 195149 0 None 4 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP level
ChEMBL 498 11 8 7 1.6 CC(C)(Cc1ccc(NC(=O)CCCNC(=N)N)cc1)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmcl.2009.06.104
22063464 199315 0 None 10 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 370 6 4 5 2.7 Cc1cccc(CC(C)(C)NCC(O)c2cc(O)cc3c2OCC(=O)N3)c1 10.1016/j.bmcl.2009.12.087
CHEMBL602257 199315 0 None 10 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 370 6 4 5 2.7 Cc1cccc(CC(C)(C)NCC(O)c2cc(O)cc3c2OCC(=O)N3)c1 10.1016/j.bmcl.2009.12.087
2419 3394 80 None 17 6 Human 8.4 pEC50 = 8.4 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O nan
5152 3394 80 None 17 6 Human 8.4 pEC50 = 8.4 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O nan
559 3394 80 None 17 6 Human 8.4 pEC50 = 8.4 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O nan
CHEMBL1263 3394 80 None 17 6 Human 8.4 pEC50 = 8.4 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O nan
DB00938 3394 80 None 17 6 Human 8.4 pEC50 = 8.4 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O nan
4907596 48954 9 None - 1 Human 8.3 pEC50 = 8.3 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 451 7 2 6 3.9 CC(=O)Nc1ccc(S(=O)(=O)N(Cc2ccco2)Cc2cc3ccccc3nc2O)cc1 nan
CHEMBL1562838 48954 9 None - 1 Human 8.3 pEC50 = 8.3 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 451 7 2 6 3.9 CC(=O)Nc1ccc(S(=O)(=O)N(Cc2ccco2)Cc2cc3ccccc3nc2O)cc1 nan
688467 85357 2 None 107 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assayAgonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assay
ChEMBL 303 6 5 5 2.1 C[C@@H](Cc1ccc(O)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2009.11.062
CHEMBL229476 85357 2 None 107 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assayAgonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assay
ChEMBL 303 6 5 5 2.1 C[C@@H](Cc1ccc(O)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2009.11.062
156015491 177725 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 346 6 4 5 1.7 O=C1COc2c(cc(O)cc2C(O)CNCCc2ccc(F)cc2)N1 10.1016/j.bmc.2019.115178
CHEMBL4649718 177725 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 346 6 4 5 1.7 O=C1COc2c(cc(O)cc2C(O)CNCCc2ccc(F)cc2)N1 10.1016/j.bmc.2019.115178
CHEMBL4651054 177725 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 346 6 4 5 1.7 O=C1COc2c(cc(O)cc2C(O)CNCCc2ccc(F)cc2)N1 10.1016/j.bmc.2019.115178
44396513 66375 0 None -30 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at Homo sapiens (human) beta2 adrenoreceptorAgonist activity at Homo sapiens (human) beta2 adrenoreceptor
ChEMBL 577 12 4 8 4.4 CC(C)S(=O)(=O)Oc1cccc2c(C[C@@H](C)NC[C@H](O)c3cccc(NS(=O)(=O)c4cccs4)c3)c[nH]c12 10.1007/s00044-009-9257-x
CHEMBL185660 66375 0 None -30 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at Homo sapiens (human) beta2 adrenoreceptorAgonist activity at Homo sapiens (human) beta2 adrenoreceptor
ChEMBL 577 12 4 8 4.4 CC(C)S(=O)(=O)Oc1cccc2c(C[C@@H](C)NC[C@H](O)c3cccc(NS(=O)(=O)c4cccs4)c3)c[nH]c12 10.1007/s00044-009-9257-x
45273281 194055 0 None 1 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 455 10 4 4 4.7 O[C@@H](CNCCc1ccc(NC(=S)Nc2ccccc2Cl)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL2448075 194055 0 None 1 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 455 10 4 4 4.7 O[C@@H](CNCCc1ccc(NC(=S)Nc2ccccc2Cl)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL557295 194055 0 None 1 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 455 10 4 4 4.7 O[C@@H](CNCCc1ccc(NC(=S)Nc2ccccc2Cl)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
10553602 126618 0 None 1 3 Human 7.4 pEC50 = 7.4 Functional
Increased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 2 adrenergic receptorsIncreased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 2 adrenergic receptors
ChEMBL 506 10 6 8 0.9 CS(=O)(=O)Nc1cc([C@@H](O)CNC2CCN(c3ccc(C(=O)NCC(=O)O)cc3)CC2)ccc1O 10.1021/jm000544b
CHEMBL36568 126618 0 None 1 3 Human 7.4 pEC50 = 7.4 Functional
Increased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 2 adrenergic receptorsIncreased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 2 adrenergic receptors
ChEMBL 506 10 6 8 0.9 CS(=O)(=O)Nc1cc([C@@H](O)CNC2CCN(c3ccc(C(=O)NCC(=O)O)cc3)CC2)ccc1O 10.1021/jm000544b
2934084 51043 14 None - 1 Human 6.4 pEC50 = 6.4 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 387 6 1 4 4.7 CC(=O)Nc1cc(C(=O)OC(C(=O)c2ccccc2)c2ccccc2)ccc1C nan
CHEMBL1581214 51043 14 None - 1 Human 6.4 pEC50 = 6.4 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 387 6 1 4 4.7 CC(=O)Nc1cc(C(=O)OC(C(=O)c2ccccc2)c2ccccc2)ccc1C nan
4586131 36747 8 None - 1 Human 5.4 pEC50 = 5.4 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 426 5 1 8 3.7 CN(C)CCNc1ncnc2c1sc1nc(N3CCCC3)c3c(c12)CC(C)(C)OC3 nan
CHEMBL1451649 36747 8 None - 1 Human 5.4 pEC50 = 5.4 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 426 5 1 8 3.7 CN(C)CCNc1ncnc2c1sc1nc(N3CCCC3)c3c(c12)CC(C)(C)OC3 nan
1542103 22269 24 None -3 3 Human 5.4 pEC50 = 5.4 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 418 4 0 6 4.2 Cc1ccccc1N1CCN(c2ncnc3c2cnn3Cc2ccc(Cl)cc2)CC1 nan
CHEMBL1325250 22269 24 None -3 3 Human 5.4 pEC50 = 5.4 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 418 4 0 6 4.2 Cc1ccccc1N1CCN(c2ncnc3c2cnn3Cc2ccc(Cl)cc2)CC1 nan
2044389 48942 8 None - 1 Human 7.4 pEC50 = 7.4 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 424 6 1 8 4.8 COCCCNc1ncnc2c1sc1nc(-c3ccco3)c3c(c12)CC(C)(C)OC3 nan
CHEMBL1562748 48942 8 None - 1 Human 7.4 pEC50 = 7.4 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 424 6 1 8 4.8 COCCCNc1ncnc2c1sc1nc(-c3ccco3)c3c(c12)CC(C)(C)OC3 nan
2999219 45581 3 None - 1 Human 5.4 pEC50 = 5.4 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 486 8 1 6 2.2 O=S(=O)(c1cc(C(F)(F)F)ccc1Cl)N1CCN(CC(O)COCC2CCCO2)CC1 nan
CHEMBL1531486 45581 3 None - 1 Human 5.4 pEC50 = 5.4 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 486 8 1 6 2.2 O=S(=O)(c1cc(C(F)(F)F)ccc1Cl)N1CCN(CC(O)COCC2CCCO2)CC1 nan
90666120 108853 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP productionAgonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP production
ChEMBL 728 19 6 9 6.6 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2C[C@@H]3[C@@H](COC(=O)Nc4ccccc4-c4ccc(O)c(Cl)c4)[C@@H]3C2)ccc1O 10.1039/C1MD00140J
CHEMBL3219053 108853 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP productionAgonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP production
ChEMBL 728 19 6 9 6.6 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2C[C@@H]3[C@@H](COC(=O)Nc4ccccc4-c4ccc(O)c(Cl)c4)[C@@H]3C2)ccc1O 10.1039/C1MD00140J
2964893 49794 8 None - 1 Human 7.4 pEC50 = 7.4 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory)
ChEMBL 374 5 0 5 1.1 CN(CC(=O)N1CCN(c2ccccn2)CC1)S(=O)(=O)c1ccccc1 nan
CHEMBL1569866 49794 8 None - 1 Human 7.4 pEC50 = 7.4 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory)
ChEMBL 374 5 0 5 1.1 CN(CC(=O)N1CCN(c2ccccn2)CC1)S(=O)(=O)c1ccccc1 nan
3145570 46721 5 None 1 2 Human 7.4 pEC50 = 7.4 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 397 4 0 5 3.5 CC(Sc1nc(-c2ccccc2)cc(C(F)(F)F)n1)C(=O)N1CCOCC1 nan
CHEMBL1541608 46721 5 None 1 2 Human 7.4 pEC50 = 7.4 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 397 4 0 5 3.5 CC(Sc1nc(-c2ccccc2)cc(C(F)(F)F)n1)C(=O)N1CCOCC1 nan
9541908 40286 6 None - 1 Human 5.4 pEC50 = 5.4 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 426 5 1 5 4.9 O=S(=O)(Nc1cccc(-c2cn3cccnc3n2)c1)c1ccc(-c2ccccc2)cc1 nan
CHEMBL1483308 40286 6 None - 1 Human 5.4 pEC50 = 5.4 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 426 5 1 5 4.9 O=S(=O)(Nc1cccc(-c2cn3cccnc3n2)c1)c1ccc(-c2ccccc2)cc1 nan
16746367 45625 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 473 7 0 4 5.0 COc1ccc(C2/C=C\CN(Cc3ccc(N(C)C)cc3)CC(=O)N2Cc2ccc(F)cc2)cc1 nan
CHEMBL1531814 45625 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 473 7 0 4 5.0 COc1ccc(C2/C=C\CN(Cc3ccc(N(C)C)cc3)CC(=O)N2Cc2ccc(F)cc2)cc1 nan
1028 287 69 None -2 16 Guinea pig 6.4 pEC50 = 6.4 Functional
Effective dose for relaxation of guinea pig trachea.Effective dose for relaxation of guinea pig trachea.
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00019a001
139148732 287 69 None -2 16 Guinea pig 6.4 pEC50 = 6.4 Functional
Effective dose for relaxation of guinea pig trachea.Effective dose for relaxation of guinea pig trachea.
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00019a001
479 287 69 None -2 16 Guinea pig 6.4 pEC50 = 6.4 Functional
Effective dose for relaxation of guinea pig trachea.Effective dose for relaxation of guinea pig trachea.
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00019a001
5816 287 69 None -2 16 Guinea pig 6.4 pEC50 = 6.4 Functional
Effective dose for relaxation of guinea pig trachea.Effective dose for relaxation of guinea pig trachea.
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00019a001
CHEMBL679 287 69 None -2 16 Guinea pig 6.4 pEC50 = 6.4 Functional
Effective dose for relaxation of guinea pig trachea.Effective dose for relaxation of guinea pig trachea.
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00019a001
DB00668 287 69 None -2 16 Guinea pig 6.4 pEC50 = 6.4 Functional
Effective dose for relaxation of guinea pig trachea.Effective dose for relaxation of guinea pig trachea.
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00019a001
24747616 19762 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 487 7 0 4 5.4 COc1ccc([C@H]2/C=C\CN(Cc3ccc(N(C)C)cc3)[C@@H](C)C(=O)N2Cc2ccc(F)cc2)cc1 nan
CHEMBL1303120 19762 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 487 7 0 4 5.4 COc1ccc([C@H]2/C=C\CN(Cc3ccc(N(C)C)cc3)[C@@H](C)C(=O)N2Cc2ccc(F)cc2)cc1 nan
44392542 65516 0 None -6 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at Homo sapiens (human) beta2 adrenoreceptorAgonist activity at Homo sapiens (human) beta2 adrenoreceptor
ChEMBL 543 11 4 6 5.5 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(NCc2ccc3ccccc3c2)c1 10.1007/s00044-009-9257-x
CHEMBL183552 65516 0 None -6 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at Homo sapiens (human) beta2 adrenoreceptorAgonist activity at Homo sapiens (human) beta2 adrenoreceptor
ChEMBL 543 11 4 6 5.5 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(NCc2ccc3ccccc3c2)c1 10.1007/s00044-009-9257-x
11432806 65851 0 None -134 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at Homo sapiens (human) beta2 adrenoreceptorAgonist activity at Homo sapiens (human) beta2 adrenoreceptor
ChEMBL 549 11 4 8 3.6 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1007/s00044-009-9257-x
CHEMBL184407 65851 0 None -134 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at Homo sapiens (human) beta2 adrenoreceptorAgonist activity at Homo sapiens (human) beta2 adrenoreceptor
ChEMBL 549 11 4 8 3.6 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1007/s00044-009-9257-x
4144800 47497 6 None 28 2 Human 7.4 pEC50 = 7.4 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 372 4 1 7 2.5 O=C(CN1C(=O)CCC1=O)Nc1nc(-c2nc3ccccc3s2)cs1 nan
CHEMBL1548237 47497 6 None 28 2 Human 7.4 pEC50 = 7.4 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 372 4 1 7 2.5 O=C(CN1C(=O)CCC1=O)Nc1nc(-c2nc3ccccc3s2)cs1 nan
24180436 92772 0 None -1 2 Guinea pig 6.4 pEC50 = 6.4 Functional
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-oneAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-one
ChEMBL 527 10 4 10 2.6 CC(Cc1ccc(Oc2no[n+]([O-])c2S(=O)(=O)c2ccccc2)cc1)NCC(O)c1cc(O)cc(O)c1 10.1021/jm0704595
CHEMBL244687 92772 0 None -1 2 Guinea pig 6.4 pEC50 = 6.4 Functional
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-oneAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-one
ChEMBL 527 10 4 10 2.6 CC(Cc1ccc(Oc2no[n+]([O-])c2S(=O)(=O)c2ccccc2)cc1)NCC(O)c1cc(O)cc(O)c1 10.1021/jm0704595
168294773 192412 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 341 8 3 5 2.0 CCOCCCNC(CO)c1cc(Br)c(N)c(C#N)c1 10.1021/acs.jmedchem.1c02006
CHEMBL5208931 192412 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 341 8 3 5 2.0 CCOCCCNC(CO)c1cc(Br)c(N)c(C#N)c1 10.1021/acs.jmedchem.1c02006
CHEMBL5222827 192412 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 341 8 3 5 2.0 CCOCCCNC(CO)c1cc(Br)c(N)c(C#N)c1 10.1021/acs.jmedchem.1c02006
44392575 64026 0 None -2 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at Homo sapiens (human) beta2 adrenoreceptorAgonist activity at Homo sapiens (human) beta2 adrenoreceptor
ChEMBL 441 10 4 6 2.8 C#CCNc1cccc([C@@H](O)CN[C@H](C)Cc2c[nH]c3c(OS(C)(=O)=O)cccc23)c1 10.1007/s00044-009-9257-x
CHEMBL181300 64026 0 None -2 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at Homo sapiens (human) beta2 adrenoreceptorAgonist activity at Homo sapiens (human) beta2 adrenoreceptor
ChEMBL 441 10 4 6 2.8 C#CCNc1cccc([C@@H](O)CN[C@H](C)Cc2c[nH]c3c(OS(C)(=O)=O)cccc23)c1 10.1007/s00044-009-9257-x
983630 43009 10 None - 1 Human 7.4 pEC50 = 7.4 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 357 5 1 4 4.2 COc1ccc(CC(=O)Nc2ccc(-c3cn4ccccc4n3)cc2)cc1 nan
CHEMBL1506379 43009 10 None - 1 Human 7.4 pEC50 = 7.4 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 357 5 1 4 4.2 COc1ccc(CC(=O)Nc2ccc(-c3cn4ccccc4n3)cc2)cc1 nan
3764964 42986 8 None - 1 Human 7.3 pEC50 = 7.3 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 414 6 1 7 4.1 CCN(CCO)c1ncnc2c1sc1nc(CC(C)C)c3c(c12)CC(C)(C)OC3 nan
CHEMBL1506229 42986 8 None - 1 Human 7.3 pEC50 = 7.3 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 414 6 1 7 4.1 CCN(CCO)c1ncnc2c1sc1nc(CC(C)C)c3c(c12)CC(C)(C)OC3 nan
440988 187802 10 None - 1 Rat 5.4 pEC50 = 5.4 Functional
Agonist activity at beta2 adrenergic receptor in rat L6 cell lysate assessed as increase in intracellular 2-deoxyglucose uptake preincubated for 4 hrs followed by 2-deoxyglucose addition measured after 20 mins by fluorescence-based enzymatic assay relative to controlAgonist activity at beta2 adrenergic receptor in rat L6 cell lysate assessed as increase in intracellular 2-deoxyglucose uptake preincubated for 4 hrs followed by 2-deoxyglucose addition measured after 20 mins by fluorescence-based enzymatic assay relative to control
ChEMBL 271 2 4 4 2.2 Oc1ccc(C[C@H]2NCCc3cc(O)c(O)cc32)cc1 10.1016/j.bmc.2017.10.011
CHEMBL501778 187802 10 None - 1 Rat 5.4 pEC50 = 5.4 Functional
Agonist activity at beta2 adrenergic receptor in rat L6 cell lysate assessed as increase in intracellular 2-deoxyglucose uptake preincubated for 4 hrs followed by 2-deoxyglucose addition measured after 20 mins by fluorescence-based enzymatic assay relative to controlAgonist activity at beta2 adrenergic receptor in rat L6 cell lysate assessed as increase in intracellular 2-deoxyglucose uptake preincubated for 4 hrs followed by 2-deoxyglucose addition measured after 20 mins by fluorescence-based enzymatic assay relative to control
ChEMBL 271 2 4 4 2.2 Oc1ccc(C[C@H]2NCCc3cc(O)c(O)cc32)cc1 10.1016/j.bmc.2017.10.011
10283539 167291 0 None -346 3 Human 6.3 pEC50 = 6.3 Functional
In vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-2 adrenergic receptorIn vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-2 adrenergic receptor
ChEMBL 697 14 6 9 2.8 CS(=O)(=O)Nc1cc(OC[C@@H](O)CNCC2CCN(S(=O)(=O)c3ccc(NC(=O)NCc4cc(F)ccc4F)cc3)CC2)ccc1O 10.1016/s0960-894x(02)00607-8
CHEMBL431048 167291 0 None -346 3 Human 6.3 pEC50 = 6.3 Functional
In vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-2 adrenergic receptorIn vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-2 adrenergic receptor
ChEMBL 697 14 6 9 2.8 CS(=O)(=O)Nc1cc(OC[C@@H](O)CNCC2CCN(S(=O)(=O)c3ccc(NC(=O)NCc4cc(F)ccc4F)cc3)CC2)ccc1O 10.1016/s0960-894x(02)00607-8
123600 2275 0 None 1 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting in presence of 100 uM phenylboronic acidAgonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting in presence of 100 uM phenylboronic acid
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)[C@H](CNC(C)(C)C)O 10.1016/j.bmc.2011.11.054
1575 2275 0 None 1 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting in presence of 100 uM phenylboronic acidAgonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting in presence of 100 uM phenylboronic acid
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)[C@H](CNC(C)(C)C)O 10.1016/j.bmc.2011.11.054
9816 2275 0 None 1 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting in presence of 100 uM phenylboronic acidAgonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting in presence of 100 uM phenylboronic acid
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)[C@H](CNC(C)(C)C)O 10.1016/j.bmc.2011.11.054
CHEMBL1002 2275 0 None 1 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting in presence of 100 uM phenylboronic acidAgonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting in presence of 100 uM phenylboronic acid
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)[C@H](CNC(C)(C)C)O 10.1016/j.bmc.2011.11.054
DB13139 2275 0 None 1 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting in presence of 100 uM phenylboronic acidAgonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting in presence of 100 uM phenylboronic acid
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)[C@H](CNC(C)(C)C)O 10.1016/j.bmc.2011.11.054
123600 2275 0 None 1 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting in presence of 100 uM phenylboronic acidAgonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting in presence of 100 uM phenylboronic acid
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)[C@H](CNC(C)(C)C)O 10.1016/j.bmc.2011.11.054
1575 2275 0 None 1 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting in presence of 100 uM phenylboronic acidAgonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting in presence of 100 uM phenylboronic acid
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)[C@H](CNC(C)(C)C)O 10.1016/j.bmc.2011.11.054
9816 2275 0 None 1 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting in presence of 100 uM phenylboronic acidAgonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting in presence of 100 uM phenylboronic acid
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)[C@H](CNC(C)(C)C)O 10.1016/j.bmc.2011.11.054
CHEMBL1002 2275 0 None 1 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting in presence of 100 uM phenylboronic acidAgonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting in presence of 100 uM phenylboronic acid
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)[C@H](CNC(C)(C)C)O 10.1016/j.bmc.2011.11.054
DB13139 2275 0 None 1 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting in presence of 100 uM phenylboronic acidAgonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting in presence of 100 uM phenylboronic acid
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)[C@H](CNC(C)(C)C)O 10.1016/j.bmc.2011.11.054
44392508 64875 0 None -3 2 Human 7.3 pEC50 = 7.3 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-2 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-2 adrenergic receptor
ChEMBL 494 11 3 6 4.3 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(OCc2ccccc2)c1 10.1016/j.bmcl.2004.12.033
CHEMBL182614 64875 0 None -3 2 Human 7.3 pEC50 = 7.3 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-2 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-2 adrenergic receptor
ChEMBL 494 11 3 6 4.3 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(OCc2ccccc2)c1 10.1016/j.bmcl.2004.12.033
73056756 103790 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulationAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulation
ChEMBL 345 9 4 5 3.1 CCC[C@H](Cc1ccc(OC)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2013.11.030
CHEMBL3099663 103790 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulationAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulation
ChEMBL 345 9 4 5 3.1 CCC[C@H](Cc1ccc(OC)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2013.11.030
24817832 66811 3 None - 1 Human 5.3 pEC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 412 6 0 4 4.1 COc1ccc(CN2CCC(Oc3ccc(C(=O)N4CCCC4)cc3)CC2)c(F)c1 nan
CHEMBL1876406 66811 3 None - 1 Human 5.3 pEC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 412 6 0 4 4.1 COc1ccc(CN2CCC(Oc3ccc(C(=O)N4CCCC4)cc3)CC2)c(F)c1 nan
2812 4696 96 None -48 39 Human 5.3 pEC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
CHEMBL104 4696 96 None -48 39 Human 5.3 pEC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
5309628 38042 5 None 134 2 Human 7.3 pEC50 = 7.3 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 397 4 0 4 3.3 CC(=O)N1CCc2cc(C(=O)CN3CCN(c4cccc(Cl)c4)CC3)ccc21 nan
CHEMBL1462616 38042 5 None 134 2 Human 7.3 pEC50 = 7.3 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 397 4 0 4 3.3 CC(=O)N1CCc2cc(C(=O)CN3CCN(c4cccc(Cl)c4)CC3)ccc21 nan
10648298 99245 0 None -120 3 Human 5.3 pEC50 = 5.3 Functional
Increased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 2 adrenergic receptorsIncreased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 2 adrenergic receptors
ChEMBL 477 10 5 7 2.1 CS(=O)(=O)Nc1cc([C@@H](O)CNC2CCN(c3ccc(CCC(=O)O)cc3)CC2)ccc1O 10.1021/jm000544b
CHEMBL284788 99245 0 None -120 3 Human 5.3 pEC50 = 5.3 Functional
Increased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 2 adrenergic receptorsIncreased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 2 adrenergic receptors
ChEMBL 477 10 5 7 2.1 CS(=O)(=O)Nc1cc([C@@H](O)CNC2CCN(c3ccc(CCC(=O)O)cc3)CC2)ccc1O 10.1021/jm000544b
127046952 139558 0 None -87 2 Human 4.3 pEC50 = 4.3 Functional
Agonist activity at human beta2 receptor expressed in HEK293 cells cotransfected with Gqs5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositolAgonist activity at human beta2 receptor expressed in HEK293 cells cotransfected with Gqs5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositol
ChEMBL 421 12 3 5 4.5 COc1cc(CCNCCc2ccc(O)c(O)c2)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
CHEMBL3800636 139558 0 None -87 2 Human 4.3 pEC50 = 4.3 Functional
Agonist activity at human beta2 receptor expressed in HEK293 cells cotransfected with Gqs5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositolAgonist activity at human beta2 receptor expressed in HEK293 cells cotransfected with Gqs5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositol
ChEMBL 421 12 3 5 4.5 COc1cc(CCNCCc2ccc(O)c(O)c2)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
1362375 22770 14 None - 1 Human 6.3 pEC50 = 6.3 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 388 6 2 5 4.8 CCc1ccc(OCC(=O)Nc2ccc(-c3nc4ccccc4o3)c(O)c2)cc1 nan
CHEMBL1329712 22770 14 None - 1 Human 6.3 pEC50 = 6.3 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 388 6 2 5 4.8 CCc1ccc(OCC(=O)Nc2ccc(-c3nc4ccccc4o3)c(O)c2)cc1 nan
20954901 44546 5 None - 1 Human 7.3 pEC50 = 7.3 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 400 6 2 5 3.9 CSc1ccc(CNC(=O)c2ccc(NC(=O)C3=CSCCO3)cc2)cc1 nan
CHEMBL1522050 44546 5 None - 1 Human 7.3 pEC50 = 7.3 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 400 6 2 5 3.9 CSc1ccc(CNC(=O)c2ccc(NC(=O)C3=CSCCO3)cc2)cc1 nan
44144146 59176 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 500 7 1 4 5.5 COC(=O)C1=C(c2cccc(OCc3ccccc3)c2)C[C@@H]2CC[C@H]1N2C(=O)NCc1cccc(F)c1 nan
CHEMBL1714856 59176 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 500 7 1 4 5.5 COC(=O)C1=C(c2cccc(OCc3ccccc3)c2)C[C@@H]2CC[C@H]1N2C(=O)NCc1cccc(F)c1 nan
1484653 50576 12 None - 1 Human 5.3 pEC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 363 4 0 5 4.4 Cc1ccc(Sc2cc(N3CCOCC3)nc(-c3ccccc3)n2)cc1 nan
CHEMBL1577237 50576 12 None - 1 Human 5.3 pEC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 363 4 0 5 4.4 Cc1ccc(Sc2cc(N3CCOCC3)nc(-c3ccccc3)n2)cc1 nan
3317235 46509 5 None 2 2 Human 5.3 pEC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 392 5 0 5 4.8 COc1ccc(C2=NN(C(=O)c3cccs3)C(c3ccc(OC)cc3)C2)cc1 nan
CHEMBL1539906 46509 5 None 2 2 Human 5.3 pEC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 392 5 0 5 4.8 COc1ccc(C2=NN(C(=O)c3cccs3)C(c3ccc(OC)cc3)C2)cc1 nan
44396736 66519 0 None -11 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at Homo sapiens (human) beta2 adrenoreceptorAgonist activity at Homo sapiens (human) beta2 adrenoreceptor
ChEMBL 617 12 4 9 5.1 C[C@H](Cc1c[nH]c2c(OS(=O)(=O)c3cccs3)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1007/s00044-009-9257-x
CHEMBL186271 66519 0 None -11 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at Homo sapiens (human) beta2 adrenoreceptorAgonist activity at Homo sapiens (human) beta2 adrenoreceptor
ChEMBL 617 12 4 9 5.1 C[C@H](Cc1c[nH]c2c(OS(=O)(=O)c3cccs3)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1007/s00044-009-9257-x
2986164 51547 10 None - 1 Human 7.3 pEC50 = 7.3 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 338 7 1 2 4.7 CCCCN(C(=O)c1ccc(NC(=O)C(C)C)cc1)c1ccccc1 nan
CHEMBL1585368 51547 10 None - 1 Human 7.3 pEC50 = 7.3 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 338 7 1 2 4.7 CCCCN(C(=O)c1ccc(NC(=O)C(C)C)cc1)c1ccccc1 nan
1016754 22479 12 None - 1 Human 7.3 pEC50 = 7.3 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 395 5 1 5 5.3 O=C(CSc1ccc(Cl)cc1)Nc1ccc(-c2nc3ncccc3o2)cc1 nan
CHEMBL1327325 22479 12 None - 1 Human 7.3 pEC50 = 7.3 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 395 5 1 5 5.3 O=C(CSc1ccc(Cl)cc1)Nc1ccc(-c2nc3ncccc3o2)cc1 nan
11668125 199316 0 None 4 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 384 7 4 5 2.9 CCc1ccc(CC(C)(C)NCC(O)c2cc(O)cc3c2OCC(=O)N3)cc1 10.1016/j.bmcl.2009.12.087
CHEMBL602258 199316 0 None 4 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 384 7 4 5 2.9 CCc1ccc(CC(C)(C)NCC(O)c2cc(O)cc3c2OCC(=O)N3)cc1 10.1016/j.bmcl.2009.12.087
962697 197408 4 None 51 2 Human 6.3 pEC50 = 6.3 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 332 5 3 6 4.3 Oc1ccccc1Nc1nc(NCc2ccco2)c2ccccc2n1 nan
CHEMBL531322 197408 4 None 51 2 Human 6.3 pEC50 = 6.3 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 332 5 3 6 4.3 Oc1ccccc1Nc1nc(NCc2ccco2)c2ccccc2n1 nan
CHEMBL588751 197408 4 None 51 2 Human 6.3 pEC50 = 6.3 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 332 5 3 6 4.3 Oc1ccccc1Nc1nc(NCc2ccco2)c2ccccc2n1 nan
46221395 8429 0 None -6 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assayAgonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assay
ChEMBL 336 4 4 4 2.0 O=c1ccc2c([C@@H](O)CNC3Cc4ccccc4C3)ccc(O)c2[nH]1 10.1021/jm100068m
CHEMBL1094323 8429 0 None -6 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assayAgonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assay
ChEMBL 336 4 4 4 2.0 O=c1ccc2c([C@@H](O)CNC3Cc4ccccc4C3)ccc(O)c2[nH]1 10.1021/jm100068m
44331426 4342 0 None 1 3 Human 8.3 pEC50 = 8.3 Functional
Beta-2 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-2-adrenoceptorBeta-2 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-2-adrenoceptor
ChEMBL 578 13 7 9 1.0 CS(=O)(=O)Nc1cc([C@@H](O)CNCC2CCN(c3ccc(C(=O)N[C@@H](CC(=O)O)C(=O)O)cc3)CC2)ccc1O 10.1016/s0960-894x(02)00608-x
CHEMBL101521 4342 0 None 1 3 Human 8.3 pEC50 = 8.3 Functional
Beta-2 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-2-adrenoceptorBeta-2 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-2-adrenoceptor
ChEMBL 578 13 7 9 1.0 CS(=O)(=O)Nc1cc([C@@H](O)CNCC2CCN(c3ccc(C(=O)N[C@@H](CC(=O)O)C(=O)O)cc3)CC2)ccc1O 10.1016/s0960-894x(02)00608-x
44268264 97767 0 None 120 2 Human 8.3 pEC50 = 8.3 Functional
Compound was tested for agonist activity against cloned human beta-2 adrenergic receptorCompound was tested for agonist activity against cloned human beta-2 adrenergic receptor
ChEMBL 345 10 3 5 2.8 COc1ccc(CC[C@@H](C)NC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/s0960-894x(98)00169-3
CHEMBL274361 97767 0 None 120 2 Human 8.3 pEC50 = 8.3 Functional
Compound was tested for agonist activity against cloned human beta-2 adrenergic receptorCompound was tested for agonist activity against cloned human beta-2 adrenergic receptor
ChEMBL 345 10 3 5 2.8 COc1ccc(CC[C@@H](C)NC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/s0960-894x(98)00169-3
11026016 46422 0 None -1 3 Human 8.3 pEC50 = 8.3 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-2 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-2 AR expressed as the negative logarithm of the molar drug concentration
ChEMBL 411 10 4 5 2.5 C[C@H](CNc1ccc(CNS(C)(=O)=O)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0101500
CHEMBL153916 46422 0 None -1 3 Human 8.3 pEC50 = 8.3 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-2 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-2 AR expressed as the negative logarithm of the molar drug concentration
ChEMBL 411 10 4 5 2.5 C[C@H](CNc1ccc(CNS(C)(=O)=O)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0101500
2419 3394 80 None -22 6 Guinea pig 8.3 pEC50 = 8.3 Functional
Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contractionAgonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contraction
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmc.2011.05.064
5152 3394 80 None -22 6 Guinea pig 8.3 pEC50 = 8.3 Functional
Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contractionAgonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contraction
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmc.2011.05.064
559 3394 80 None -22 6 Guinea pig 8.3 pEC50 = 8.3 Functional
Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contractionAgonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contraction
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmc.2011.05.064
CHEMBL1263 3394 80 None -22 6 Guinea pig 8.3 pEC50 = 8.3 Functional
Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contractionAgonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contraction
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmc.2011.05.064
DB00938 3394 80 None -22 6 Guinea pig 8.3 pEC50 = 8.3 Functional
Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contractionAgonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contraction
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmc.2011.05.064
2419 3394 80 None -22 6 Guinea pig 8.3 pEC50 = 8.3 Functional
Agonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile responseAgonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmc.2011.08.043
5152 3394 80 None -22 6 Guinea pig 8.3 pEC50 = 8.3 Functional
Agonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile responseAgonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmc.2011.08.043
559 3394 80 None -22 6 Guinea pig 8.3 pEC50 = 8.3 Functional
Agonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile responseAgonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmc.2011.08.043
CHEMBL1263 3394 80 None -22 6 Guinea pig 8.3 pEC50 = 8.3 Functional
Agonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile responseAgonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmc.2011.08.043
DB00938 3394 80 None -22 6 Guinea pig 8.3 pEC50 = 8.3 Functional
Agonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile responseAgonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmc.2011.08.043
56670158 63750 0 None 15 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 497 13 5 7 2.5 O=c1[nH]c2c(O)ccc([C@@H](O)CNCC[S+]([O-])CCCNCCc3cccc(Cl)c3)c2s1 10.1016/j.bmcl.2011.05.097
CHEMBL1807830 63750 0 None 15 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 497 13 5 7 2.5 O=c1[nH]c2c(O)ccc([C@@H](O)CNCC[S+]([O-])CCCNCCc3cccc(Cl)c3)c2s1 10.1016/j.bmcl.2011.05.097
90655866 110762 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assayAgonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assay
ChEMBL 576 17 3 7 4.3 CC(C)N(C)CCCN(CCNCCc1ccc(O)c2[nH]c(=O)sc12)C(=O)CCOCCc1cccc(Cl)c1 10.1021/ml4005232
CHEMBL3265163 110762 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assayAgonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assay
ChEMBL 576 17 3 7 4.3 CC(C)N(C)CCCN(CCNCCc1ccc(O)c2[nH]c(=O)sc12)C(=O)CCOCCc1cccc(Cl)c1 10.1021/ml4005232
145980824 166082 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 354 7 4 5 2.1 COc1ccccc1CCNC(CO)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2018.04.041
CHEMBL4281324 166082 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 354 7 4 5 2.1 COc1ccccc1CCNC(CO)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2018.04.041
145992510 166443 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 452 15 4 5 4.5 O=c1ccc2c(C(CO)NCCCCCCOCCCCc3ccccc3)ccc(O)c2[nH]1 10.1016/j.ejmech.2018.04.041
CHEMBL4288132 166443 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 452 15 4 5 4.5 O=c1ccc2c(C(CO)NCCCCCCOCCCCc3ccccc3)ccc(O)c2[nH]1 10.1016/j.ejmech.2018.04.041
57394848 69862 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 434 9 6 6 2.8 OCc1cc(C(O)CNC2Cc3ccc(NCC(O)c4ccccc4)cc3C2)ccc1O 10.1016/j.bmcl.2011.11.072
CHEMBL1940819 69862 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 434 9 6 6 2.8 OCc1cc(C(O)CNC2Cc3ccc(NCC(O)c4ccccc4)cc3C2)ccc1O 10.1016/j.bmcl.2011.11.072
9906822 161476 0 None -40 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at Homo sapiens (human) beta2 adrenoreceptorAgonist activity at Homo sapiens (human) beta2 adrenoreceptor
ChEMBL 358 7 3 3 4.1 COc1cccc2c(CC(C)NC[C@H](O)c3cccc(Cl)c3)c[nH]c12 10.1007/s00044-009-9257-x
CHEMBL416012 161476 0 None -40 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at Homo sapiens (human) beta2 adrenoreceptorAgonist activity at Homo sapiens (human) beta2 adrenoreceptor
ChEMBL 358 7 3 3 4.1 COc1cccc2c(CC(C)NC[C@H](O)c3cccc(Cl)c3)c[nH]c12 10.1007/s00044-009-9257-x
11268355 95936 0 None -40 3 Human 8.3 pEC50 = 8.3 Functional
Agonistic activity against human Beta-2 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonistic activity against human Beta-2 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 358 7 3 3 4.1 COc1cccc2c(C[C@@H](C)NC[C@H](O)c3cccc(Cl)c3)c[nH]c12 10.1016/s0960-894x(03)00073-8
CHEMBL26183 95936 0 None -40 3 Human 8.3 pEC50 = 8.3 Functional
Agonistic activity against human Beta-2 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonistic activity against human Beta-2 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 358 7 3 3 4.1 COc1cccc2c(C[C@@H](C)NC[C@H](O)c3cccc(Cl)c3)c[nH]c12 10.1016/s0960-894x(03)00073-8
45101521 195142 0 None 4 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP level
ChEMBL 570 15 8 9 1.3 CC(C)(Cc1ccc(NC(=O)CCCNC(=O)C(N)CCCN)cc1)NCC(O)c1ccc(O)c2c1OCC(=O)N2 10.1016/j.bmcl.2009.06.104
CHEMBL565747 195142 0 None 4 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP level
ChEMBL 570 15 8 9 1.3 CC(C)(Cc1ccc(NC(=O)CCCNC(=O)C(N)CCCN)cc1)NCC(O)c1ccc(O)c2c1OCC(=O)N2 10.1016/j.bmcl.2009.06.104
2212788 27931 9 None - 1 Human 8.3 pEC50 = 8.3 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory)
ChEMBL 490 10 1 7 4.2 C=CCn1c(CCNC(=O)c2cccs2)nnc1SCC(=O)c1ccc(Br)cc1 nan
CHEMBL1373386 27931 9 None - 1 Human 8.3 pEC50 = 8.3 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory)
ChEMBL 490 10 1 7 4.2 C=CCn1c(CCNC(=O)c2cccs2)nnc1SCC(=O)c1ccc(Br)cc1 nan
44396531 66486 0 None -38 3 Human 8.3 pEC50 = 8.3 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptor
ChEMBL 647 18 4 8 6.4 CCCCCCCCS(=O)(=O)Oc1cccc2c(C[C@@H](C)NC[C@H](O)c3cccc(NS(=O)(=O)c4cccs4)c3)c[nH]c12 10.1016/j.bmcl.2004.10.035
CHEMBL186135 66486 0 None -38 3 Human 8.3 pEC50 = 8.3 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptor
ChEMBL 647 18 4 8 6.4 CCCCCCCCS(=O)(=O)Oc1cccc2c(C[C@@H](C)NC[C@H](O)c3cccc(NS(=O)(=O)c4cccs4)c3)c[nH]c12 10.1016/j.bmcl.2004.10.035
54582151 61473 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as stimulation of intracellular cAMP production after 30 mins of washing by wash-off assayAgonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as stimulation of intracellular cAMP production after 30 mins of washing by wash-off assay
ChEMBL 711 24 5 8 7.3 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)ccc1O)C(C)C 10.1016/j.bmcl.2010.10.132
CHEMBL1773266 61473 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as stimulation of intracellular cAMP production after 30 mins of washing by wash-off assayAgonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as stimulation of intracellular cAMP production after 30 mins of washing by wash-off assay
ChEMBL 711 24 5 8 7.3 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)ccc1O)C(C)C 10.1016/j.bmcl.2010.10.132
1499 2052 43 None -72 36 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/acs.jmedchem.1c02006
3779 2052 43 None -72 36 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/acs.jmedchem.1c02006
536 2052 43 None -72 36 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/acs.jmedchem.1c02006
CHEMBL434 2052 43 None -72 36 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/acs.jmedchem.1c02006
DB01064 2052 43 None -72 36 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/acs.jmedchem.1c02006
49861320 54666 0 None 6 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 426 11 3 5 3.1 O=S(=O)(Nc1ccccc1)c1ccc(CCNC[C@@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.06.031
CHEMBL1204003 54666 0 None 6 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 426 11 3 5 3.1 O=S(=O)(Nc1ccccc1)c1ccc(CCNC[C@@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.06.031
CHEMBL1615579 54666 0 None 6 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 426 11 3 5 3.1 O=S(=O)(Nc1ccccc1)c1ccc(CCNC[C@@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.06.031
45272417 193760 0 None 1 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 455 10 4 4 4.7 O[C@@H](CNCCc1ccc(NC(=S)Nc2cccc(Cl)c2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL2448074 193760 0 None 1 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 455 10 4 4 4.7 O[C@@H](CNCCc1ccc(NC(=S)Nc2cccc(Cl)c2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL552368 193760 0 None 1 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 455 10 4 4 4.7 O[C@@H](CNCCc1ccc(NC(=S)Nc2cccc(Cl)c2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
567 715 10 None -83 7 Human 7.3 pEC50 = 7.3 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-2 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-2 AR expressed as the negative logarithm of the molar drug concentration
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1021/jm0101500
9841972 715 10 None -83 7 Human 7.3 pEC50 = 7.3 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-2 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-2 AR expressed as the negative logarithm of the molar drug concentration
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1021/jm0101500
CHEMBL284782 715 10 None -83 7 Human 7.3 pEC50 = 7.3 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-2 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-2 AR expressed as the negative logarithm of the molar drug concentration
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1021/jm0101500
44369602 46564 0 None 6 2 Human 7.3 pEC50 = 7.3 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-2 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-2 AR expressed as the negative logarithm of the molar drug concentration
ChEMBL 362 9 4 4 3.1 C[C@H](CNc1cccc(CC(=O)O)c1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0101500
CHEMBL154036 46564 0 None 6 2 Human 7.3 pEC50 = 7.3 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-2 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-2 AR expressed as the negative logarithm of the molar drug concentration
ChEMBL 362 9 4 4 3.1 C[C@H](CNc1cccc(CC(=O)O)c1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0101500
9799092 47027 0 None -12 3 Human 7.3 pEC50 = 7.3 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-2 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-2 AR expressed as the negative logarithm of the molar drug concentration
ChEMBL 362 9 4 4 3.1 C[C@H](CNc1ccc(CC(=O)O)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0101500
CHEMBL154419 47027 0 None -12 3 Human 7.3 pEC50 = 7.3 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-2 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-2 AR expressed as the negative logarithm of the molar drug concentration
ChEMBL 362 9 4 4 3.1 C[C@H](CNc1ccc(CC(=O)O)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0101500
567 715 10 None -83 7 Human 7.3 pEC50 = 7.3 Functional
Activity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1021/jm0509445
9841972 715 10 None -83 7 Human 7.3 pEC50 = 7.3 Functional
Activity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1021/jm0509445
CHEMBL284782 715 10 None -83 7 Human 7.3 pEC50 = 7.3 Functional
Activity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1021/jm0509445
9799092 47027 0 None -12 3 Human 7.3 pEC50 = 7.3 Functional
Activity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 362 9 4 4 3.1 C[C@H](CNc1ccc(CC(=O)O)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0509445
CHEMBL154419 47027 0 None -12 3 Human 7.3 pEC50 = 7.3 Functional
Activity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 362 9 4 4 3.1 C[C@H](CNc1ccc(CC(=O)O)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0509445
9845282 75584 0 None -501 3 Human 7.3 pEC50 = 7.3 Functional
Activity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 424 9 4 4 4.8 C[C@H](CNc1cccc(-c2cccc(C(=O)O)c2)c1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0509445
CHEMBL205224 75584 0 None -501 3 Human 7.3 pEC50 = 7.3 Functional
Activity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 424 9 4 4 4.8 C[C@H](CNc1cccc(-c2cccc(C(=O)O)c2)c1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0509445
57401203 70502 0 None - 1 Guinea pig 7.3 pEC50 = 7.3 Functional
Agonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contractionAgonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contraction
ChEMBL 566 15 4 8 4.2 COc1ccc(C2=NN(CCCCCCNCC(O)c3ccc(O)c(NC=O)c3)C(=O)C3CCCCC23)cc1OC 10.1016/j.bmcl.2012.01.013
CHEMBL1951070 70502 0 None - 1 Guinea pig 7.3 pEC50 = 7.3 Functional
Agonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contractionAgonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contraction
ChEMBL 566 15 4 8 4.2 COc1ccc(C2=NN(CCCCCCNCC(O)c3ccc(O)c(NC=O)c3)C(=O)C3CCCCC23)cc1OC 10.1016/j.bmcl.2012.01.013
9799092 47027 0 None -12 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 362 9 4 4 3.1 C[C@H](CNc1ccc(CC(=O)O)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2007.05.069
CHEMBL154419 47027 0 None -12 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 362 9 4 4 3.1 C[C@H](CNc1ccc(CC(=O)O)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2007.05.069
44441230 93341 0 None -31 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 431 9 4 6 4.3 C[C@H](CNc1ccc(-c2csc(C(=O)O)n2)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2007.05.069
CHEMBL247518 93341 0 None -31 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 431 9 4 6 4.3 C[C@H](CNc1ccc(-c2csc(C(=O)O)n2)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2007.05.069
44441228 167198 0 None -7 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 431 9 4 6 4.3 C[C@H](CNc1ccc(-c2nc(C(=O)O)cs2)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2007.05.069
CHEMBL430390 167198 0 None -7 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 431 9 4 6 4.3 C[C@H](CNc1ccc(-c2nc(C(=O)O)cs2)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2007.05.069
87142783 118545 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 719 13 5 9 5.8 COc1cc(N(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)ccc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/jm501915g
CHEMBL3426704 118545 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 719 13 5 9 5.8 COc1cc(N(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)ccc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/jm501915g
141465526 165876 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 352 6 4 4 2.9 CC(C)(Cc1ccccc1)NC(CO)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2018.04.041
CHEMBL4277527 165876 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 352 6 4 4 2.9 CC(C)(Cc1ccccc1)NC(CO)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2018.04.041
145992971 166475 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 443 8 5 5 3.4 O=C(Nc1ccc(CCNC(CO)c2ccc(O)c3[nH]c(=O)ccc23)cc1)c1ccccc1 10.1016/j.ejmech.2018.04.041
CHEMBL4288842 166475 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 443 8 5 5 3.4 O=C(Nc1ccc(CCNC(CO)c2ccc(O)c3[nH]c(=O)ccc23)cc1)c1ccccc1 10.1016/j.ejmech.2018.04.041
145989180 166663 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 409 8 5 5 2.7 CC(C)C(=O)Nc1ccc(CCNC(CO)c2ccc(O)c3[nH]c(=O)ccc23)cc1 10.1016/j.ejmech.2018.04.041
CHEMBL4292249 166663 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 409 8 5 5 2.7 CC(C)C(=O)Nc1ccc(CCNC(CO)c2ccc(O)c3[nH]c(=O)ccc23)cc1 10.1016/j.ejmech.2018.04.041
57393116 69869 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 478 11 6 6 4.2 CC(C)(C)c1ccc(C(O)CNc2ccc(CCNCC(O)c3ccc(O)c(CO)c3)cc2)cc1 10.1016/j.bmcl.2011.11.072
CHEMBL1940826 69869 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 478 11 6 6 4.2 CC(C)(C)c1ccc(C(O)CNc2ccc(CCNCC(O)c3ccc(O)c(CO)c3)cc2)cc1 10.1016/j.bmcl.2011.11.072
57391349 69872 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 472 11 6 6 4.0 OCc1cc(C(O)CNCCc2ccc(NCC(O)c3ccc4ccccc4c3)cc2)ccc1O 10.1016/j.bmcl.2011.11.072
CHEMBL1940829 69872 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 472 11 6 6 4.0 OCc1cc(C(O)CNCCc2ccc(NCC(O)c3ccc4ccccc4c3)cc2)ccc1O 10.1016/j.bmcl.2011.11.072
10393774 120218 0 None -1258 3 Human 5.3 pEC50 = 5.3 Functional
Increased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 2 adrenergic receptorsIncreased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 2 adrenergic receptors
ChEMBL 598 14 5 9 2.1 CCCCN(c1ccc(N2CCC(NC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)CC2)cc1)S(=O)(=O)CC(=O)O 10.1021/jm000544b
CHEMBL35500 120218 0 None -1258 3 Human 5.3 pEC50 = 5.3 Functional
Increased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 2 adrenergic receptorsIncreased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 2 adrenergic receptors
ChEMBL 598 14 5 9 2.1 CCCCN(c1ccc(N2CCC(NC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)CC2)cc1)S(=O)(=O)CC(=O)O 10.1021/jm000544b
9845280 76959 0 None -3 3 Human 6.3 pEC50 = 6.3 Functional
Activity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 424 9 3 5 4.5 COC(=O)c1cccc(-c2cccc(NCCNC[C@H](O)c3cccc(Cl)c3)c2)c1 10.1021/jm0509445
CHEMBL208352 76959 0 None -3 3 Human 6.3 pEC50 = 6.3 Functional
Activity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 424 9 3 5 4.5 COC(=O)c1cccc(-c2cccc(NCCNC[C@H](O)c3cccc(Cl)c3)c2)c1 10.1021/jm0509445
90644146 111740 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 460 10 4 5 4.2 OCc1cc(C(O)CNCCc2ccc(N3CCC(Cc4ccccc4)CC3)cc2)ccc1O 10.1016/j.bmcl.2014.04.069
CHEMBL3290975 111740 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 460 10 4 5 4.2 OCc1cc(C(O)CNCCc2ccc(N3CCC(Cc4ccccc4)CC3)cc2)ccc1O 10.1016/j.bmcl.2014.04.069
135799875 185828 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHO cells harboring beta2-beta-arr assessed as induction of beta-arrestin 2 recruitment using beta-galactosidase as substrate preincubated for 90 mins followed by substrate addition and measured after 60 mins by luminescence assayAgonist activity at human beta2 adrenoceptor expressed in CHO cells harboring beta2-beta-arr assessed as induction of beta-arrestin 2 recruitment using beta-galactosidase as substrate preincubated for 90 mins followed by substrate addition and measured after 60 mins by luminescence assay
ChEMBL 276 3 4 4 1.7 CC(C)(C)NC(CO)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/acs.jmedchem.0c01195
CHEMBL4876155 185828 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHO cells harboring beta2-beta-arr assessed as induction of beta-arrestin 2 recruitment using beta-galactosidase as substrate preincubated for 90 mins followed by substrate addition and measured after 60 mins by luminescence assayAgonist activity at human beta2 adrenoceptor expressed in CHO cells harboring beta2-beta-arr assessed as induction of beta-arrestin 2 recruitment using beta-galactosidase as substrate preincubated for 90 mins followed by substrate addition and measured after 60 mins by luminescence assay
ChEMBL 276 3 4 4 1.7 CC(C)(C)NC(CO)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/acs.jmedchem.0c01195
44441236 92977 0 None -3981 3 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 416 9 4 5 4.5 O=C(O)c1ccsc1-c1cccc(NCCNC[C@H](O)c2cccc(Cl)c2)c1 10.1016/j.bmcl.2007.05.069
CHEMBL245875 92977 0 None -3981 3 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 416 9 4 5 4.5 O=C(O)c1ccsc1-c1cccc(NCCNC[C@H](O)c2cccc(Cl)c2)c1 10.1016/j.bmcl.2007.05.069
1371669 37341 10 None 64 2 Human 6.3 pEC50 = 6.3 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory)
ChEMBL 373 5 1 5 4.5 Cc1ccc(OCC(=O)Nc2ccc(-c3nc4ncccc4o3)cc2)c(C)c1 nan
CHEMBL1456621 37341 10 None 64 2 Human 6.3 pEC50 = 6.3 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory)
ChEMBL 373 5 1 5 4.5 Cc1ccc(OCC(=O)Nc2ccc(-c3nc4ncccc4o3)cc2)c(C)c1 nan
16736091 85291 0 None -251 2 Rat 6.3 pEC50 = 6.3 Functional
Agonist activity beta2-adrenergic receptor in rat ventricular myocytes assessed as cell contraction following electrical stimulation by optical edge tracking method using photodiode arrayAgonist activity beta2-adrenergic receptor in rat ventricular myocytes assessed as cell contraction following electrical stimulation by optical edge tracking method using photodiode array
ChEMBL 317 7 4 5 2.4 COc1ccc(C[C@H](C)NC[C@H](O)c2cc(O)cc(O)c2)cc1 10.1016/j.bmc.2009.11.062
CHEMBL228996 85291 0 None -251 2 Rat 6.3 pEC50 = 6.3 Functional
Agonist activity beta2-adrenergic receptor in rat ventricular myocytes assessed as cell contraction following electrical stimulation by optical edge tracking method using photodiode arrayAgonist activity beta2-adrenergic receptor in rat ventricular myocytes assessed as cell contraction following electrical stimulation by optical edge tracking method using photodiode array
ChEMBL 317 7 4 5 2.4 COc1ccc(C[C@H](C)NC[C@H](O)c2cc(O)cc(O)c2)cc1 10.1016/j.bmc.2009.11.062
127046950 139502 0 None -2 3 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human beta2 receptor expressed in HEK293 cells cotransfected with Gqs5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositolAgonist activity at human beta2 receptor expressed in HEK293 cells cotransfected with Gqs5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositol
ChEMBL 437 12 4 6 4.0 COc1cc(CCNC[C@H](O)c2ccc(O)c(O)c2)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
CHEMBL3800303 139502 0 None -2 3 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human beta2 receptor expressed in HEK293 cells cotransfected with Gqs5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositolAgonist activity at human beta2 receptor expressed in HEK293 cells cotransfected with Gqs5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositol
ChEMBL 437 12 4 6 4.0 COc1cc(CCNC[C@H](O)c2ccc(O)c(O)c2)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
141486999 166127 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human beta2-AR expressed in CHOK1 cells co-expressing Galpha15 measured after 21 secs to 120 secs by Calcium-4 dye based FLIPR assayAgonist activity at human beta2-AR expressed in CHOK1 cells co-expressing Galpha15 measured after 21 secs to 120 secs by Calcium-4 dye based FLIPR assay
ChEMBL 229 1 2 4 2.1 Oc1cc2c(cc1O)C(c1ccco1)=NCC2 10.1021/acs.jnatprod.7b00762
CHEMBL4282215 166127 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human beta2-AR expressed in CHOK1 cells co-expressing Galpha15 measured after 21 secs to 120 secs by Calcium-4 dye based FLIPR assayAgonist activity at human beta2-AR expressed in CHOK1 cells co-expressing Galpha15 measured after 21 secs to 120 secs by Calcium-4 dye based FLIPR assay
ChEMBL 229 1 2 4 2.1 Oc1cc2c(cc1O)C(c1ccco1)=NCC2 10.1021/acs.jnatprod.7b00762
1631626 27275 14 None - 1 Human 5.3 pEC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 292 7 1 5 2.9 COc1ccccc1OCCCC(=O)Nc1nccs1 nan
CHEMBL1368804 27275 14 None - 1 Human 5.3 pEC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 292 7 1 5 2.9 COc1ccccc1OCCCC(=O)Nc1nccs1 nan
46232815 199986 0 None -5 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 412 6 4 5 3.7 CC(C)(Cc1ccc(C(C)(C)C)cc1)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmcl.2009.12.087
CHEMBL606208 199986 0 None -5 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 412 6 4 5 3.7 CC(C)(Cc1ccc(C(C)(C)C)cc1)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmcl.2009.12.087
145984584 165323 0 None -102 3 Human 7.3 pEC50 = 7.3 Functional
Antagonist activity at human beta2 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta2 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 444 10 5 4 4.4 O=C(Nc1ccccc1)Nc1ccc(CCNC[C@H](O)COc2cccc3[nH]ccc23)cc1 10.1016/j.ejmech.2018.03.032
CHEMBL4249564 165323 0 None -102 3 Human 7.3 pEC50 = 7.3 Functional
Antagonist activity at human beta2 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta2 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 444 10 5 4 4.4 O=C(Nc1ccccc1)Nc1ccc(CCNC[C@H](O)COc2cccc3[nH]ccc23)cc1 10.1016/j.ejmech.2018.03.032
11074 482 5 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in sf9 cells assessed as reversal of norepinephrine inhibition of [3H]DHAP binding to beta2 adrenoceptor by radioligand binding assayAgonist activity at beta2 adrenoceptor (unknown origin) expressed in sf9 cells assessed as reversal of norepinephrine inhibition of [3H]DHAP binding to beta2 adrenoceptor by radioligand binding assay
ChEMBL 314 2 2 4 3.7 Brc1ccc2c(c1)c(N)nc(n2)Nc1ccccc1 10.1021/acs.jmedchem.0c01195
145998261 482 5 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in sf9 cells assessed as reversal of norepinephrine inhibition of [3H]DHAP binding to beta2 adrenoceptor by radioligand binding assayAgonist activity at beta2 adrenoceptor (unknown origin) expressed in sf9 cells assessed as reversal of norepinephrine inhibition of [3H]DHAP binding to beta2 adrenoceptor by radioligand binding assay
ChEMBL 314 2 2 4 3.7 Brc1ccc2c(c1)c(N)nc(n2)Nc1ccccc1 10.1021/acs.jmedchem.0c01195
CHEMBL4869271 482 5 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in sf9 cells assessed as reversal of norepinephrine inhibition of [3H]DHAP binding to beta2 adrenoceptor by radioligand binding assayAgonist activity at beta2 adrenoceptor (unknown origin) expressed in sf9 cells assessed as reversal of norepinephrine inhibition of [3H]DHAP binding to beta2 adrenoceptor by radioligand binding assay
ChEMBL 314 2 2 4 3.7 Brc1ccc2c(c1)c(N)nc(n2)Nc1ccccc1 10.1021/acs.jmedchem.0c01195
20950665 66864 4 None - 1 Human 6.3 pEC50 = 6.3 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 418 6 1 4 2.8 CC1CCC(NC(=O)CCS(=O)(=O)c2ccc3c(c2)CCN3C(=O)C2CC2)CC1 nan
CHEMBL1878737 66864 4 None - 1 Human 6.3 pEC50 = 6.3 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 418 6 1 4 2.8 CC1CCC(NC(=O)CCS(=O)(=O)c2ccc3c(c2)CCN3C(=O)C2CC2)CC1 nan
24817062 28550 7 None - 1 Human 5.3 pEC50 = 5.3 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory)
ChEMBL 382 5 0 3 4.1 O=C(c1ccc(OC2CCN(Cc3ccc(F)cc3)CC2)cc1)N1CCCC1 nan
CHEMBL1378531 28550 7 None - 1 Human 5.3 pEC50 = 5.3 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory)
ChEMBL 382 5 0 3 4.1 O=C(c1ccc(OC2CCN(Cc3ccc(F)cc3)CC2)cc1)N1CCCC1 nan
76322965 84881 0 None -52 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at Homo sapiens (human) beta2 adrenoreceptorAgonist activity at Homo sapiens (human) beta2 adrenoreceptor
ChEMBL 511 9 3 7 4.5 C[C@H](Cc1cn2c3c(cccc13)OCCC2)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1007/s00044-009-9257-x
CHEMBL2260989 84881 0 None -52 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at Homo sapiens (human) beta2 adrenoreceptorAgonist activity at Homo sapiens (human) beta2 adrenoreceptor
ChEMBL 511 9 3 7 4.5 C[C@H](Cc1cn2c3c(cccc13)OCCC2)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1007/s00044-009-9257-x
4625323 199642 8 None 46 2 Human 6.3 pEC50 = 6.3 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 419 8 1 6 5.6 CCCc1ccc(OCc2nc(-c3ccc(NC(=O)c4cccs4)cc3)no2)cc1 nan
CHEMBL604311 199642 8 None 46 2 Human 6.3 pEC50 = 6.3 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 419 8 1 6 5.6 CCCc1ccc(OCc2nc(-c3ccc(NC(=O)c4cccs4)cc3)no2)cc1 nan
44396577 66603 0 None -25 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at Homo sapiens (human) beta2 adrenoreceptorAgonist activity at Homo sapiens (human) beta2 adrenoreceptor
ChEMBL 561 12 4 6 5.9 C[C@H](Cc1c[nH]c2c(OCc3ccccc3)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1007/s00044-009-9257-x
CHEMBL186676 66603 0 None -25 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at Homo sapiens (human) beta2 adrenoreceptorAgonist activity at Homo sapiens (human) beta2 adrenoreceptor
ChEMBL 561 12 4 6 5.9 C[C@H](Cc1c[nH]c2c(OCc3ccccc3)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1007/s00044-009-9257-x
145971070 164437 2 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as increase in isoproterenol-induced cAMP production preincubated for 20 mins followed by isoproterenol stimulation and measured after 5 mins by chemiluminescence-based assayAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as increase in isoproterenol-induced cAMP production preincubated for 20 mins followed by isoproterenol stimulation and measured after 5 mins by chemiluminescence-based assay
ChEMBL 646 12 4 4 4.4 CNC(=O)[C@H](Cc1cccc(Br)c1)NC(=O)[C@H](Cc1ccc(C(N)=O)cc1)NC(=O)C(c1ccccc1)C1CCCCC1 10.1021/acs.jmedchem.0c01195
CHEMBL4225747 164437 2 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as increase in isoproterenol-induced cAMP production preincubated for 20 mins followed by isoproterenol stimulation and measured after 5 mins by chemiluminescence-based assayAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as increase in isoproterenol-induced cAMP production preincubated for 20 mins followed by isoproterenol stimulation and measured after 5 mins by chemiluminescence-based assay
ChEMBL 646 12 4 4 4.4 CNC(=O)[C@H](Cc1cccc(Br)c1)NC(=O)[C@H](Cc1ccc(C(N)=O)cc1)NC(=O)C(c1ccccc1)C1CCCCC1 10.1021/acs.jmedchem.0c01195
44428086 149535 0 None 7 2 Guinea pig 4.3 pEC50 = 4.3 Functional
Agonist activity at adrenergic beta2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of propranololAgonist activity at adrenergic beta2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of propranolol
ChEMBL 415 9 4 8 1.9 Cc1c(COc2ccc(CC(C)NCC(O)c3cc(O)cc(O)c3)cc2)no[n+]1[O-] 10.1021/jm0704595
CHEMBL395082 149535 0 None 7 2 Guinea pig 4.3 pEC50 = 4.3 Functional
Agonist activity at adrenergic beta2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of propranololAgonist activity at adrenergic beta2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of propranolol
ChEMBL 415 9 4 8 1.9 Cc1c(COc2ccc(CC(C)NCC(O)c3cc(O)cc(O)c3)cc2)no[n+]1[O-] 10.1021/jm0704595
24817832 66811 3 None - 1 Human 5.3 pEC50 = 5.3 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory)
ChEMBL 412 6 0 4 4.1 COc1ccc(CN2CCC(Oc3ccc(C(=O)N4CCCC4)cc3)CC2)c(F)c1 nan
CHEMBL1876406 66811 3 None - 1 Human 5.3 pEC50 = 5.3 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory)
ChEMBL 412 6 0 4 4.1 COc1ccc(CN2CCC(Oc3ccc(C(=O)N4CCCC4)cc3)CC2)c(F)c1 nan
24790337 22543 5 None - 1 Human 7.3 pEC50 = 7.3 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory)
ChEMBL 417 7 0 7 3.7 Cc1ccc(OCc2cc(C(=O)N(C)Cc3cnn(-c4ccccc4C)c3)no2)cn1 nan
CHEMBL1327806 22543 5 None - 1 Human 7.3 pEC50 = 7.3 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory)
ChEMBL 417 7 0 7 3.7 Cc1ccc(OCc2cc(C(=O)N(C)Cc3cnn(-c4ccccc4C)c3)no2)cn1 nan
44428086 149535 0 None 7 2 Guinea pig 4.3 pEC50 = 4.3 Functional
Agonist activity at adrenergic beta2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of propranololAgonist activity at adrenergic beta2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of propranolol
ChEMBL 415 9 4 8 1.9 Cc1c(COc2ccc(CC(C)NCC(O)c3cc(O)cc(O)c3)cc2)no[n+]1[O-] 10.1021/jm0704595
CHEMBL395082 149535 0 None 7 2 Guinea pig 4.3 pEC50 = 4.3 Functional
Agonist activity at adrenergic beta2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of propranololAgonist activity at adrenergic beta2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of propranolol
ChEMBL 415 9 4 8 1.9 Cc1c(COc2ccc(CC(C)NCC(O)c3cc(O)cc(O)c3)cc2)no[n+]1[O-] 10.1021/jm0704595
193350 67305 7 None - 1 Human 6.3 pEC50 = 6.3 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 303 6 5 5 2.1 CC(Cc1ccc(O)cc1)NCC(O)c1ccc(O)c(O)c1 nan
CHEMBL1902287 67305 7 None - 1 Human 6.3 pEC50 = 6.3 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 303 6 5 5 2.1 CC(Cc1ccc(O)cc1)NCC(O)c1ccc(O)c(O)c1 nan
CHEMBL1906949 67305 7 None - 1 Human 6.3 pEC50 = 6.3 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 303 6 5 5 2.1 CC(Cc1ccc(O)cc1)NCC(O)c1ccc(O)c(O)c1 nan
4378441 54487 8 None - 1 Human 5.3 pEC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 422 3 1 5 5.7 O=C(Nc1ccc2oc(-c3ccc4ccccc4c3)nc2c1)c1ccc2c(c1)OCCO2 nan
CHEMBL1612392 54487 8 None - 1 Human 5.3 pEC50 = 5.3 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 422 3 1 5 5.7 O=C(Nc1ccc2oc(-c3ccc4ccccc4c3)nc2c1)c1ccc2c(c1)OCCO2 nan
16189131 27540 6 None - 1 Human 6.3 pEC50 = 6.3 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 391 6 0 5 4.7 CSc1ccc(C(=O)C2CCCN(Cc3cccn3-c3cccnc3)C2)cc1 nan
CHEMBL1370616 27540 6 None - 1 Human 6.3 pEC50 = 6.3 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 391 6 0 5 4.7 CSc1ccc(C(=O)C2CCCN(Cc3cccn3-c3cccnc3)C2)cc1 nan
90666114 108846 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP productionAgonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP production
ChEMBL 734 18 6 9 7.0 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3cc(F)ccc3-c3ccc(O)c(Cl)c3)CC2)ccc1O 10.1039/C1MD00140J
CHEMBL3219047 108846 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP productionAgonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP production
ChEMBL 734 18 6 9 7.0 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3cc(F)ccc3-c3ccc(O)c(Cl)c3)CC2)ccc1O 10.1039/C1MD00140J
12005176 48548 5 None - 1 Human 6.2 pEC50 = 6.2 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 458 6 1 7 4.5 CCOC(=O)c1ccc(N2C(=O)c3[nH]nc(-c4ccco4)c3C2c2cccc([N+](=O)[O-])c2)cc1 nan
CHEMBL1559039 48548 5 None - 1 Human 6.2 pEC50 = 6.2 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 458 6 1 7 4.5 CCOC(=O)c1ccc(N2C(=O)c3[nH]nc(-c4ccco4)c3C2c2cccc([N+](=O)[O-])c2)cc1 nan
2957284 37694 10 None - 1 Human 5.2 pEC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 360 7 1 4 3.2 CCCCC(=O)Nc1ccc(C(=O)N2CCCC(C(=O)OCC)C2)cc1 nan
CHEMBL1459608 37694 10 None - 1 Human 5.2 pEC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 360 7 1 4 3.2 CCCCC(=O)Nc1ccc(C(=O)N2CCCC(C(=O)OCC)C2)cc1 nan
688467 85357 2 None -107 2 Rat 6.2 pEC50 = 6.2 Functional
Agonist activity beta2-adrenergic receptor in rat ventricular myocytes assessed as cell contraction following electrical stimulation by optical edge tracking method using photodiode arrayAgonist activity beta2-adrenergic receptor in rat ventricular myocytes assessed as cell contraction following electrical stimulation by optical edge tracking method using photodiode array
ChEMBL 303 6 5 5 2.1 C[C@@H](Cc1ccc(O)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2009.11.062
CHEMBL229476 85357 2 None -107 2 Rat 6.2 pEC50 = 6.2 Functional
Agonist activity beta2-adrenergic receptor in rat ventricular myocytes assessed as cell contraction following electrical stimulation by optical edge tracking method using photodiode arrayAgonist activity beta2-adrenergic receptor in rat ventricular myocytes assessed as cell contraction following electrical stimulation by optical edge tracking method using photodiode array
ChEMBL 303 6 5 5 2.1 C[C@@H](Cc1ccc(O)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2009.11.062
16299699 41237 5 None - 1 Human 6.2 pEC50 = 6.2 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 449 7 2 4 3.7 CN(c1ccccc1)S(=O)(=O)c1cccc(C(=O)Nc2cccc(C(=O)NC3CC3)c2)c1 nan
CHEMBL1490889 41237 5 None - 1 Human 6.2 pEC50 = 6.2 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 449 7 2 4 3.7 CN(c1ccccc1)S(=O)(=O)c1cccc(C(=O)Nc2cccc(C(=O)NC3CC3)c2)c1 nan
76315637 84876 0 None -47 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at Homo sapiens (human) beta2 adrenoreceptorAgonist activity at Homo sapiens (human) beta2 adrenoreceptor
ChEMBL 607 12 4 10 4.2 CCOC(=O)S(=O)(=O)Oc1cccc2c(C[C@@H](C)NC[C@H](O)c3cccc(NS(=O)(=O)c4cccs4)c3)c[nH]c12 10.1007/s00044-009-9257-x
CHEMBL2260984 84876 0 None -47 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at Homo sapiens (human) beta2 adrenoreceptorAgonist activity at Homo sapiens (human) beta2 adrenoreceptor
ChEMBL 607 12 4 10 4.2 CCOC(=O)S(=O)(=O)Oc1cccc2c(C[C@@H](C)NC[C@H](O)c3cccc(NS(=O)(=O)c4cccs4)c3)c[nH]c12 10.1007/s00044-009-9257-x
11632691 199847 0 None 3 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 398 7 4 5 3.5 CC(C)c1ccc(CC(C)(C)NCC(O)c2cc(O)cc3c2OCC(=O)N3)cc1 10.1016/j.bmcl.2009.12.087
CHEMBL605372 199847 0 None 3 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 398 7 4 5 3.5 CC(C)c1ccc(CC(C)(C)NCC(O)c2cc(O)cc3c2OCC(=O)N3)cc1 10.1016/j.bmcl.2009.12.087
1499 2052 43 None -165 36 Guinea pig 7.2 pEC50 = 7.2 Functional
Agonistic activity (beta2- adrenergic) for the percent maximal relaxation of isolated guinea pig tracheaAgonistic activity (beta2- adrenergic) for the percent maximal relaxation of isolated guinea pig trachea
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm00107a027
3779 2052 43 None -165 36 Guinea pig 7.2 pEC50 = 7.2 Functional
Agonistic activity (beta2- adrenergic) for the percent maximal relaxation of isolated guinea pig tracheaAgonistic activity (beta2- adrenergic) for the percent maximal relaxation of isolated guinea pig trachea
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm00107a027
536 2052 43 None -165 36 Guinea pig 7.2 pEC50 = 7.2 Functional
Agonistic activity (beta2- adrenergic) for the percent maximal relaxation of isolated guinea pig tracheaAgonistic activity (beta2- adrenergic) for the percent maximal relaxation of isolated guinea pig trachea
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm00107a027
CHEMBL434 2052 43 None -165 36 Guinea pig 7.2 pEC50 = 7.2 Functional
Agonistic activity (beta2- adrenergic) for the percent maximal relaxation of isolated guinea pig tracheaAgonistic activity (beta2- adrenergic) for the percent maximal relaxation of isolated guinea pig trachea
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm00107a027
DB01064 2052 43 None -165 36 Guinea pig 7.2 pEC50 = 7.2 Functional
Agonistic activity (beta2- adrenergic) for the percent maximal relaxation of isolated guinea pig tracheaAgonistic activity (beta2- adrenergic) for the percent maximal relaxation of isolated guinea pig trachea
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm00107a027
9832011 104989 0 None -19 3 Human 6.2 pEC50 = 6.2 Functional
Compound was evaluated for its inhibitory activity against human beta-2 adrenergic receptor (AR)Compound was evaluated for its inhibitory activity against human beta-2 adrenergic receptor (AR)
ChEMBL 644 13 6 7 6.5 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(-c3ccc(OCC4NCCc5cc(O)c(O)cc54)cc3)cc2)cc1 10.1016/s0960-894x(00)00459-5
CHEMBL312074 104989 0 None -19 3 Human 6.2 pEC50 = 6.2 Functional
Compound was evaluated for its inhibitory activity against human beta-2 adrenergic receptor (AR)Compound was evaluated for its inhibitory activity against human beta-2 adrenergic receptor (AR)
ChEMBL 644 13 6 7 6.5 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(-c3ccc(OCC4NCCc5cc(O)c(O)cc54)cc3)cc2)cc1 10.1016/s0960-894x(00)00459-5
24823464 97156 0 None -2041 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 418 10 4 4 4.7 CC(C)Nc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm9000709
CHEMBL270964 97156 0 None -2041 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 418 10 4 4 4.7 CC(C)Nc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm9000709
12988997 192183 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 322 4 3 3 3.5 Nc1c(Cl)cc(C(CO)NC2CCCC2)cc1C(F)(F)F 10.1021/acs.jmedchem.1c02006
CHEMBL5172759 192183 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 322 4 3 3 3.5 Nc1c(Cl)cc(C(CO)NC2CCCC2)cc1C(F)(F)F 10.1021/acs.jmedchem.1c02006
CHEMBL5221410 192183 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 322 4 3 3 3.5 Nc1c(Cl)cc(C(CO)NC2CCCC2)cc1C(F)(F)F 10.1021/acs.jmedchem.1c02006
5350331 108418 7 None - 1 Human 6.2 pEC50 = 6.2 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 422 12 0 8 3.8 C=CCc1ccc(OCCOc2ccc(/C=N/n3cnnc3)cc2OCC)c(OC)c1 nan
CHEMBL3211107 108418 7 None - 1 Human 6.2 pEC50 = 6.2 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 422 12 0 8 3.8 C=CCc1ccc(OCCOc2ccc(/C=N/n3cnnc3)cc2OCC)c(OC)c1 nan
1329577 53094 6 None - 1 Human 5.2 pEC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 425 4 0 3 3.5 O=C(c1cccc(Cl)c1)N1CCC(C(=O)N2CCN(Cc3ccccc3)CC2)CC1 nan
CHEMBL1600429 53094 6 None - 1 Human 5.2 pEC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 425 4 0 3 3.5 O=C(c1cccc(Cl)c1)N1CCC(C(=O)N2CCN(Cc3ccccc3)CC2)CC1 nan
44589400 192973 0 None -2 3 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at adrenergic beta-2 receptorAgonist activity at adrenergic beta-2 receptor
ChEMBL 446 11 2 5 4.2 COc1ccc(CCNCC(O)COc2ccc3c(c2)CCCN3Cc2ccccc2)cc1 10.1016/j.bmc.2008.11.030
CHEMBL530556 192973 0 None -2 3 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at adrenergic beta-2 receptorAgonist activity at adrenergic beta-2 receptor
ChEMBL 446 11 2 5 4.2 COc1ccc(CCNCC(O)COc2ccc3c(c2)CCCN3Cc2ccccc2)cc1 10.1016/j.bmc.2008.11.030
16735495 85345 0 None -3 2 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity beta2-adrenergic receptor in rat ventricular myocytes assessed as cell contraction following electrical stimulation by optical edge tracking method using photodiode arrayAgonist activity beta2-adrenergic receptor in rat ventricular myocytes assessed as cell contraction following electrical stimulation by optical edge tracking method using photodiode array
ChEMBL 337 6 4 4 3.5 C[C@H](Cc1cccc2ccccc12)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2009.11.062
CHEMBL229401 85345 0 None -3 2 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity beta2-adrenergic receptor in rat ventricular myocytes assessed as cell contraction following electrical stimulation by optical edge tracking method using photodiode arrayAgonist activity beta2-adrenergic receptor in rat ventricular myocytes assessed as cell contraction following electrical stimulation by optical edge tracking method using photodiode array
ChEMBL 337 6 4 4 3.5 C[C@H](Cc1cccc2ccccc12)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2009.11.062
2234461 43512 9 None - 1 Human 6.2 pEC50 = 6.2 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 432 7 1 6 2.7 COC(=O)c1ccc(NC(=O)COc2ccc(S(=O)(=O)N3CCCCC3)cc2)cc1 nan
CHEMBL1510834 43512 9 None - 1 Human 6.2 pEC50 = 6.2 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 432 7 1 6 2.7 COC(=O)c1ccc(NC(=O)COc2ccc(S(=O)(=O)N3CCCCC3)cc2)cc1 nan
24177540 184107 2 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at beta2 adrenoceptor in human A431 cells measured for 24 hrsAgonist activity at beta2 adrenoceptor in human A431 cells measured for 24 hrs
ChEMBL 362 9 5 6 2.5 COc1cc(CCC(O)CC(O)CCc2ccc(O)c(O)c2)ccc1O 10.1021/acs.jmedchem.0c01195
CHEMBL4850211 184107 2 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at beta2 adrenoceptor in human A431 cells measured for 24 hrsAgonist activity at beta2 adrenoceptor in human A431 cells measured for 24 hrs
ChEMBL 362 9 5 6 2.5 COc1cc(CCC(O)CC(O)CCc2ccc(O)c(O)c2)ccc1O 10.1021/acs.jmedchem.0c01195
25023952 192678 0 None - 1 Golden hamster 8.2 pEC50 = 8.2 Functional
Agonist activity at adrenergic beta2 receptor in Syrian hamster DDT1 MF2 cells assessed as stimulation of cAMP accumulation by radioimmunoassay in presence of 1 uM DPCPXAgonist activity at adrenergic beta2 receptor in Syrian hamster DDT1 MF2 cells assessed as stimulation of cAMP accumulation by radioimmunoassay in presence of 1 uM DPCPX
ChEMBL 545 15 8 13 0.0 O=CNc1cc(C(O)CNCCCCCCNc2ncnc3c2ncn3[C@@H]2O[C@H](CO)[C@@H](O)[C@H]2O)ccc1O 10.1021/jm800613s
CHEMBL524037 192678 0 None - 1 Golden hamster 8.2 pEC50 = 8.2 Functional
Agonist activity at adrenergic beta2 receptor in Syrian hamster DDT1 MF2 cells assessed as stimulation of cAMP accumulation by radioimmunoassay in presence of 1 uM DPCPXAgonist activity at adrenergic beta2 receptor in Syrian hamster DDT1 MF2 cells assessed as stimulation of cAMP accumulation by radioimmunoassay in presence of 1 uM DPCPX
ChEMBL 545 15 8 13 0.0 O=CNc1cc(C(O)CNCCCCCCNc2ncnc3c2ncn3[C@@H]2O[C@H](CO)[C@@H](O)[C@H]2O)ccc1O 10.1021/jm800613s
59548089 124673 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 818 18 6 10 6.1 COc1ccc(NC(=O)CCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)cc1CCNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645279 124673 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 818 18 6 10 6.1 COc1ccc(NC(=O)CCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)cc1CCNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
10455 3218 34 None 53 3 Guinea pig 8.2 pEC50 = 8.2 Functional
Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as relaxation of carbachol-induced tissue contractionAgonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as relaxation of carbachol-induced tissue contraction
ChEMBL 301 7 4 4 2.7 CC(NCC(c1ccc(cc1)O)O)CCc1ccc(cc1)O 10.1021/jm801211c
56052 3218 34 None 53 3 Guinea pig 8.2 pEC50 = 8.2 Functional
Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as relaxation of carbachol-induced tissue contractionAgonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as relaxation of carbachol-induced tissue contraction
ChEMBL 301 7 4 4 2.7 CC(NCC(c1ccc(cc1)O)O)CCc1ccc(cc1)O 10.1021/jm801211c
CHEMBL509336 3218 34 None 53 3 Guinea pig 8.2 pEC50 = 8.2 Functional
Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as relaxation of carbachol-induced tissue contractionAgonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as relaxation of carbachol-induced tissue contraction
ChEMBL 301 7 4 4 2.7 CC(NCC(c1ccc(cc1)O)O)CCc1ccc(cc1)O 10.1021/jm801211c
DB11541 3218 34 None 53 3 Guinea pig 8.2 pEC50 = 8.2 Functional
Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as relaxation of carbachol-induced tissue contractionAgonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as relaxation of carbachol-induced tissue contraction
ChEMBL 301 7 4 4 2.7 CC(NCC(c1ccc(cc1)O)O)CCc1ccc(cc1)O 10.1021/jm801211c
102262219 139516 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human beta2 receptor expressed in HEK293 cells cotransfected with Gqs5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositolAgonist activity at human beta2 receptor expressed in HEK293 cells cotransfected with Gqs5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositol
ChEMBL 488 12 4 6 4.1 COc1cc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
CHEMBL3800400 139516 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human beta2 receptor expressed in HEK293 cells cotransfected with Gqs5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositolAgonist activity at human beta2 receptor expressed in HEK293 cells cotransfected with Gqs5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositol
ChEMBL 488 12 4 6 4.1 COc1cc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
44396513 66375 0 None -30 3 Human 8.2 pEC50 = 8.2 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptor
ChEMBL 577 12 4 8 4.4 CC(C)S(=O)(=O)Oc1cccc2c(C[C@@H](C)NC[C@H](O)c3cccc(NS(=O)(=O)c4cccs4)c3)c[nH]c12 10.1016/j.bmcl.2004.10.035
CHEMBL185660 66375 0 None -30 3 Human 8.2 pEC50 = 8.2 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptor
ChEMBL 577 12 4 8 4.4 CC(C)S(=O)(=O)Oc1cccc2c(C[C@@H](C)NC[C@H](O)c3cccc(NS(=O)(=O)c4cccs4)c3)c[nH]c12 10.1016/j.bmcl.2004.10.035
16035377 110759 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assayAgonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assay
ChEMBL 500 15 3 7 2.5 CN(C)CCN(CCNCCc1ccc(O)c2[nH]c(=O)sc12)C(=O)CCOCCc1ccccc1 10.1021/ml4005232
CHEMBL3265160 110759 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assayAgonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assay
ChEMBL 500 15 3 7 2.5 CN(C)CCN(CCNCCc1ccc(O)c2[nH]c(=O)sc12)C(=O)CCOCCc1ccccc1 10.1021/ml4005232
16035379 110770 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assayAgonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assay
ChEMBL 562 17 3 7 3.9 CCN(CC)CCN(CCNCCc1ccc(O)c2[nH]c(=O)sc12)C(=O)CCOCCc1cccc(Cl)c1 10.1021/ml4005232
CHEMBL3265171 110770 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assayAgonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assay
ChEMBL 562 17 3 7 3.9 CCN(CC)CCN(CCNCCc1ccc(O)c2[nH]c(=O)sc12)C(=O)CCOCCc1cccc(Cl)c1 10.1021/ml4005232
16035068 112201 4 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assayAgonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assay
ChEMBL 578 17 3 7 4.4 CCN(CC)CCN(CCNCCc1ccc(O)c2[nH]c(=O)sc12)C(=O)CCOCCc1cccc2ccccc12 10.1021/ml4005232
CHEMBL3265167 112201 4 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assayAgonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assay
ChEMBL 578 17 3 7 4.4 CCN(CC)CCN(CCNCCc1ccc(O)c2[nH]c(=O)sc12)C(=O)CCOCCc1cccc2ccccc12 10.1021/ml4005232
CHEMBL3304488 112201 4 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assayAgonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assay
ChEMBL 578 17 3 7 4.4 CCN(CC)CCN(CCNCCc1ccc(O)c2[nH]c(=O)sc12)C(=O)CCOCCc1cccc2ccccc12 10.1021/ml4005232
56943517 111999 0 None 3 3 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 621 13 5 9 2.8 CS(=O)(=O)N1CCN(CCOc2ccc(Nc3ccc(CCNC[C@H](O)c4ccc(O)c5[nH]c(=O)ccc45)cc3)cc2)CC1 10.1016/j.bmcl.2014.04.095
CHEMBL3298832 111999 0 None 3 3 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 621 13 5 9 2.8 CS(=O)(=O)N1CCN(CCOc2ccc(Nc3ccc(CCNC[C@H](O)c4ccc(O)c5[nH]c(=O)ccc45)cc3)cc2)CC1 10.1016/j.bmcl.2014.04.095
59119466 111763 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 436 10 5 7 3.3 COC(=O)c1ccc(Nc2ccc(CCNCC(O)c3ccc(O)c(CO)c3)cc2)cc1 10.1016/j.bmcl.2014.04.069
CHEMBL3290996 111763 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 436 10 5 7 3.3 COC(=O)c1ccc(Nc2ccc(CCNCC(O)c3ccc(O)c(CO)c3)cc2)cc1 10.1016/j.bmcl.2014.04.069
57391345 69866 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 482 13 6 8 2.9 COc1ccc(OC)c(C(O)CNc2ccc(CCNCC(O)c3ccc(O)c(CO)c3)cc2)c1 10.1016/j.bmcl.2011.11.072
CHEMBL1940823 69866 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 482 13 6 8 2.9 COc1ccc(OC)c(C(O)CNc2ccc(CCNCC(O)c3ccc(O)c(CO)c3)cc2)c1 10.1016/j.bmcl.2011.11.072
1165076 39694 4 None - 1 Human 8.2 pEC50 = 8.2 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory)
ChEMBL 466 5 1 7 4.8 Cc1ccc(Cn2ccc(NC(=O)c3cc4nc(-c5ccco5)cc(C(F)(F)F)n4n3)n2)cc1 nan
CHEMBL1478198 39694 4 None - 1 Human 8.2 pEC50 = 8.2 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory)
ChEMBL 466 5 1 7 4.8 Cc1ccc(Cn2ccc(NC(=O)c3cc4nc(-c5ccco5)cc(C(F)(F)F)n4n3)n2)cc1 nan
44396577 66603 0 None -25 3 Human 8.2 pEC50 = 8.2 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptor
ChEMBL 561 12 4 6 5.9 C[C@H](Cc1c[nH]c2c(OCc3ccccc3)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2004.10.035
CHEMBL186676 66603 0 None -25 3 Human 8.2 pEC50 = 8.2 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptor
ChEMBL 561 12 4 6 5.9 C[C@H](Cc1c[nH]c2c(OCc3ccccc3)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2004.10.035
44396596 122771 0 None -25 3 Human 8.2 pEC50 = 8.2 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptor
ChEMBL 485 10 4 6 4.3 COc1cccc2c(C[C@@H](C)NC[C@H](O)c3cccc(NS(=O)(=O)c4cccs4)c3)c[nH]c12 10.1016/j.bmcl.2004.10.035
CHEMBL361505 122771 0 None -25 3 Human 8.2 pEC50 = 8.2 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptor
ChEMBL 485 10 4 6 4.3 COc1cccc2c(C[C@@H](C)NC[C@H](O)c3cccc(NS(=O)(=O)c4cccs4)c3)c[nH]c12 10.1016/j.bmcl.2004.10.035
44396488 66383 0 None -5 3 Human 8.2 pEC50 = 8.2 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptor
ChEMBL 556 12 4 7 3.8 C[C@H](Cc1c[nH]c2c(OCC(=O)N(C)C)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2004.10.035
CHEMBL185703 66383 0 None -5 3 Human 8.2 pEC50 = 8.2 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptor
ChEMBL 556 12 4 7 3.8 C[C@H](Cc1c[nH]c2c(OCC(=O)N(C)C)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2004.10.035
1287365 37568 9 None - 1 Human 8.2 pEC50 = 8.2 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory)
ChEMBL 373 5 2 3 5.3 Cc1ccc(SCC(=O)Nc2ccc(-c3nc4ccccc4[nH]3)cc2)cc1 nan
CHEMBL1458579 37568 9 None - 1 Human 8.2 pEC50 = 8.2 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory)
ChEMBL 373 5 2 3 5.3 Cc1ccc(SCC(=O)Nc2ccc(-c3nc4ccccc4[nH]3)cc2)cc1 nan
666902 24765 9 None 213 2 Human 8.2 pEC50 = 8.2 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory)
ChEMBL 451 8 1 7 5.3 Clc1ccc(OCc2nnc(SCc3nc4ccccc4[nH]3)n2Cc2ccco2)cc1 nan
CHEMBL1346316 24765 9 None 213 2 Human 8.2 pEC50 = 8.2 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory)
ChEMBL 451 8 1 7 5.3 Clc1ccc(OCc2nnc(SCc3nc4ccccc4[nH]3)n2Cc2ccco2)cc1 nan
44396738 123353 0 None -54 3 Human 7.2 pEC50 = 7.2 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptor
ChEMBL 655 13 5 9 4.8 C[C@H](Cc1c[nH]c2c(OS(=O)(=O)c3ccc(C(=O)O)cc3)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2004.10.035
CHEMBL362763 123353 0 None -54 3 Human 7.2 pEC50 = 7.2 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptor
ChEMBL 655 13 5 9 4.8 C[C@H](Cc1c[nH]c2c(OS(=O)(=O)c3ccc(C(=O)O)cc3)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2004.10.035
10233153 4150 0 None -6 3 Human 7.2 pEC50 = 7.2 Functional
Beta-2 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-2-adrenoceptorBeta-2 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-2-adrenoceptor
ChEMBL 642 11 5 9 3.1 CS(=O)(=O)Nc1cc([C@@H](O)CNCC2CCN(S(=O)(=O)c3ccc(-n4ccc5c(C(=O)O)cccc54)cc3)CC2)ccc1O 10.1016/s0960-894x(02)00608-x
CHEMBL100351 4150 0 None -6 3 Human 7.2 pEC50 = 7.2 Functional
Beta-2 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-2-adrenoceptorBeta-2 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-2-adrenoceptor
ChEMBL 642 11 5 9 3.1 CS(=O)(=O)Nc1cc([C@@H](O)CNCC2CCN(S(=O)(=O)c3ccc(-n4ccc5c(C(=O)O)cccc54)cc3)CC2)ccc1O 10.1016/s0960-894x(02)00608-x
10076548 162701 0 None -6 3 Human 7.2 pEC50 = 7.2 Functional
Increased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 2 adrenergic receptorsIncreased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 2 adrenergic receptors
ChEMBL 562 13 5 8 2.7 CCCCN(C(=O)CC(=O)O)c1ccc(N2CCC(NC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)CC2)cc1 10.1021/jm000544b
CHEMBL418600 162701 0 None -6 3 Human 7.2 pEC50 = 7.2 Functional
Increased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 2 adrenergic receptorsIncreased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 2 adrenergic receptors
ChEMBL 562 13 5 8 2.7 CCCCN(C(=O)CC(=O)O)c1ccc(N2CCC(NC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)CC2)cc1 10.1021/jm000544b
123686 1942 44 None -74 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 354 9 4 5 1.7 C1=CC=C(C=C1)NC(=O)NCCNCC(COC2=CC=CC=C2C#N)O 10.1021/jm400348g
12581 1942 44 None -74 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 354 9 4 5 1.7 C1=CC=C(C=C1)NC(=O)NCCNCC(COC2=CC=CC=C2C#N)O 10.1021/jm400348g
CHEMBL11268 1942 44 None -74 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 354 9 4 5 1.7 C1=CC=C(C=C1)NC(=O)NCCNCC(COC2=CC=CC=C2C#N)O 10.1021/jm400348g
2953239 31012 5 None - 1 Human 7.2 pEC50 = 7.2 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 388 5 0 5 1.4 Cc1ccc(S(=O)(=O)N(C)CC(=O)N2CCN(c3ccccn3)CC2)cc1 nan
CHEMBL1401186 31012 5 None - 1 Human 7.2 pEC50 = 7.2 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 388 5 0 5 1.4 Cc1ccc(S(=O)(=O)N(C)CC(=O)N2CCN(c3ccccn3)CC2)cc1 nan
20954905 22909 5 None - 1 Human 7.2 pEC50 = 7.2 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 398 7 2 5 3.6 CCOc1ccc(CNC(=O)c2ccc(NC(=O)C3=CSCCO3)cc2)cc1 nan
CHEMBL1330871 22909 5 None - 1 Human 7.2 pEC50 = 7.2 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 398 7 2 5 3.6 CCOc1ccc(CNC(=O)c2ccc(NC(=O)C3=CSCCO3)cc2)cc1 nan
1025603 28216 11 None - 1 Human 7.2 pEC50 = 7.2 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory)
ChEMBL 430 8 1 4 3.4 CN(Cc1ccccc1)S(=O)(=O)c1ccc(NS(=O)(=O)Cc2ccccc2)cc1 nan
CHEMBL1375364 28216 11 None - 1 Human 7.2 pEC50 = 7.2 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory)
ChEMBL 430 8 1 4 3.4 CN(Cc1ccccc1)S(=O)(=O)c1ccc(NS(=O)(=O)Cc2ccccc2)cc1 nan
9997789 185709 0 None 107 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 310 3 3 3 3.4 CC(C)(C)NC(CO)c1cc(Cl)c(N)c(C(F)(F)F)c1 10.1021/acs.jmedchem.1c02006
CHEMBL4874511 185709 0 None 107 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 310 3 3 3 3.4 CC(C)(C)NC(CO)c1cc(Cl)c(N)c(C(F)(F)F)c1 10.1021/acs.jmedchem.1c02006
CHEMBL5192245 185709 0 None 107 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 310 3 3 3 3.4 CC(C)(C)NC(CO)c1cc(Cl)c(N)c(C(F)(F)F)c1 10.1021/acs.jmedchem.1c02006
440927 178366 18 None - 1 Rat 6.2 pEC50 = 6.2 Functional
Agonist activity at beta2 adrenergic receptor in rat L6 cell lysate assessed as increase in intracellular 2-deoxyglucose uptake preincubated for 4 hrs followed by 2-deoxyglucose addition measured after 20 mins by fluorescence-based enzymatic assay relative to controlAgonist activity at beta2 adrenergic receptor in rat L6 cell lysate assessed as increase in intracellular 2-deoxyglucose uptake preincubated for 4 hrs followed by 2-deoxyglucose addition measured after 20 mins by fluorescence-based enzymatic assay relative to control
ChEMBL 271 2 4 4 2.2 Oc1ccc(C[C@@H]2NCCc3cc(O)c(O)cc32)cc1 10.1016/j.bmc.2017.10.011
CHEMBL470491 178366 18 None - 1 Rat 6.2 pEC50 = 6.2 Functional
Agonist activity at beta2 adrenergic receptor in rat L6 cell lysate assessed as increase in intracellular 2-deoxyglucose uptake preincubated for 4 hrs followed by 2-deoxyglucose addition measured after 20 mins by fluorescence-based enzymatic assay relative to controlAgonist activity at beta2 adrenergic receptor in rat L6 cell lysate assessed as increase in intracellular 2-deoxyglucose uptake preincubated for 4 hrs followed by 2-deoxyglucose addition measured after 20 mins by fluorescence-based enzymatic assay relative to control
ChEMBL 271 2 4 4 2.2 Oc1ccc(C[C@@H]2NCCc3cc(O)c(O)cc32)cc1 10.1016/j.bmc.2017.10.011
10601234 111502 0 None -91 3 Human 5.2 pEC50 = 5.2 Functional
Increased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 2 adrenergic receptorsIncreased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 2 adrenergic receptors
ChEMBL 493 11 5 8 1.7 CS(=O)(=O)Nc1cc([C@@H](O)CNC2CCN(c3ccc(COCC(=O)O)cc3)CC2)ccc1O 10.1021/jm000544b
CHEMBL32888 111502 0 None -91 3 Human 5.2 pEC50 = 5.2 Functional
Increased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 2 adrenergic receptorsIncreased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 2 adrenergic receptors
ChEMBL 493 11 5 8 1.7 CS(=O)(=O)Nc1cc([C@@H](O)CNC2CCN(c3ccc(COCC(=O)O)cc3)CC2)ccc1O 10.1021/jm000544b
145984792 165165 0 None -776 3 Human 5.2 pEC50 = 5.2 Functional
Antagonist activity at human beta2 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta2 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 461 12 4 5 3.1 CC(=O)NCc1cccc(OC[C@@H](O)CNCCc2ccc(NC(=O)c3ccccc3)cc2)c1 10.1016/j.ejmech.2018.03.032
CHEMBL4246134 165165 0 None -776 3 Human 5.2 pEC50 = 5.2 Functional
Antagonist activity at human beta2 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta2 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 461 12 4 5 3.1 CC(=O)NCc1cccc(OC[C@@H](O)CNCCc2ccc(NC(=O)c3ccccc3)cc2)c1 10.1016/j.ejmech.2018.03.032
2458483 50192 6 None - 1 Human 5.2 pEC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 344 4 0 4 4.5 CN(Cc1ccccc1F)c1nc(-c2cccnc2)nc2ccccc12 nan
CHEMBL1573444 50192 6 None - 1 Human 5.2 pEC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 344 4 0 4 4.5 CN(Cc1ccccc1F)c1nc(-c2cccnc2)nc2ccccc12 nan
1094286 50549 15 None - 1 Human 7.2 pEC50 = 7.2 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 359 5 1 5 4.2 Cc1ccc(OCC(=O)Nc2ccc(-c3nc4ncccc4o3)cc2)cc1 nan
CHEMBL1577023 50549 15 None - 1 Human 7.2 pEC50 = 7.2 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 359 5 1 5 4.2 Cc1ccc(OCC(=O)Nc2ccc(-c3nc4ncccc4o3)cc2)cc1 nan
73056759 103789 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulationAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulation
ChEMBL 345 8 4 5 3.0 COc1ccc(C[C@@H](NC[C@H](O)c2cc(O)cc(O)c2)C(C)C)cc1 10.1016/j.bmc.2013.11.030
CHEMBL3099662 103789 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulationAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulation
ChEMBL 345 8 4 5 3.0 COc1ccc(C[C@@H](NC[C@H](O)c2cc(O)cc(O)c2)C(C)C)cc1 10.1016/j.bmc.2013.11.030
73057082 103791 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulationAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulation
ChEMBL 345 9 4 5 3.1 CCC[C@@H](Cc1ccc(OC)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2013.11.030
CHEMBL3099664 103791 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulationAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulation
ChEMBL 345 9 4 5 3.1 CCC[C@@H](Cc1ccc(OC)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2013.11.030
1854978 37465 8 None - 1 Human 6.2 pEC50 = 6.2 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 422 5 1 7 5.5 CC(C)Cc1nc2sc3c(NCc4ccco4)ncnc3c2c2c1COC(C)(C)C2 nan
CHEMBL1457704 37465 8 None - 1 Human 6.2 pEC50 = 6.2 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 422 5 1 7 5.5 CC(C)Cc1nc2sc3c(NCc4ccco4)ncnc3c2c2c1COC(C)(C)C2 nan
135799890 185195 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHO cells harboring beta2-beta-arr assessed as induction of beta-arrestin 2 recruitment using beta-galactosidase as substrate preincubated for 90 mins followed by substrate addition and measured after 60 mins by luminescence assayAgonist activity at human beta2 adrenoceptor expressed in CHO cells harboring beta2-beta-arr assessed as induction of beta-arrestin 2 recruitment using beta-galactosidase as substrate preincubated for 90 mins followed by substrate addition and measured after 60 mins by luminescence assay
ChEMBL 304 8 4 4 2.4 CCCCCCNC(CO)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/acs.jmedchem.0c01195
CHEMBL4866730 185195 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHO cells harboring beta2-beta-arr assessed as induction of beta-arrestin 2 recruitment using beta-galactosidase as substrate preincubated for 90 mins followed by substrate addition and measured after 60 mins by luminescence assayAgonist activity at human beta2 adrenoceptor expressed in CHO cells harboring beta2-beta-arr assessed as induction of beta-arrestin 2 recruitment using beta-galactosidase as substrate preincubated for 90 mins followed by substrate addition and measured after 60 mins by luminescence assay
ChEMBL 304 8 4 4 2.4 CCCCCCNC(CO)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/acs.jmedchem.0c01195
44377771 164984 0 None -102 3 Human 6.2 pEC50 = 6.2 Functional
Agonistic activity was assessed by measurement of cAMP accumulation levels in CHO cells expressing human beta-2-adrenergic receptorAgonistic activity was assessed by measurement of cAMP accumulation levels in CHO cells expressing human beta-2-adrenergic receptor
ChEMBL 596 10 5 9 3.4 O=C1NC(=O)C(Cc2ccc(N3CCC(NC[C@H](O)c4ccc(O)c(NS(=O)(=O)c5ccccc5)c4)CC3)cc2)S1 10.1016/s0960-894x(01)00063-4
CHEMBL424167 164984 0 None -102 3 Human 6.2 pEC50 = 6.2 Functional
Agonistic activity was assessed by measurement of cAMP accumulation levels in CHO cells expressing human beta-2-adrenergic receptorAgonistic activity was assessed by measurement of cAMP accumulation levels in CHO cells expressing human beta-2-adrenergic receptor
ChEMBL 596 10 5 9 3.4 O=C1NC(=O)C(Cc2ccc(N3CCC(NC[C@H](O)c4ccc(O)c(NS(=O)(=O)c5ccccc5)c4)CC3)cc2)S1 10.1016/s0960-894x(01)00063-4
1090196 53569 15 None - 1 Human 5.2 pEC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 378 5 1 6 3.2 CCN1CCN(c2ccc(NC(=O)c3ccc([N+](=O)[O-])o3)cc2Cl)CC1 nan
CHEMBL1604735 53569 15 None - 1 Human 5.2 pEC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 378 5 1 6 3.2 CCN1CCN(c2ccc(NC(=O)c3ccc([N+](=O)[O-])o3)cc2Cl)CC1 nan
1288829 24917 10 None - 1 Human 6.2 pEC50 = 6.2 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 391 6 1 6 5.0 Cc1ccc(SCC(=O)Nc2ccc(-c3nnc(-c4ccco4)o3)cc2)cc1 nan
CHEMBL1347493 24917 10 None - 1 Human 6.2 pEC50 = 6.2 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 391 6 1 6 5.0 Cc1ccc(SCC(=O)Nc2ccc(-c3nnc(-c4ccco4)o3)cc2)cc1 nan
57396616 69870 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 492 14 6 6 4.5 CC(C)CCc1ccc(C(O)CNc2ccc(CCNCC(O)c3ccc(O)c(CO)c3)cc2)cc1 10.1016/j.bmcl.2011.11.072
CHEMBL1940827 69870 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 492 14 6 6 4.5 CC(C)CCc1ccc(C(O)CNc2ccc(CCNCC(O)c3ccc(O)c(CO)c3)cc2)cc1 10.1016/j.bmcl.2011.11.072
9823696 75408 0 None -398 3 Human 6.2 pEC50 = 6.2 Functional
Activity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 424 9 4 4 4.7 Cc1ccc(C(=O)O)cc1-c1cccc(NCCNC[C@H](O)c2cccc(Cl)c2)c1 10.1021/jm0509445
CHEMBL204827 75408 0 None -398 3 Human 6.2 pEC50 = 6.2 Functional
Activity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 424 9 4 4 4.7 Cc1ccc(C(=O)O)cc1-c1cccc(NCCNC[C@H](O)c2cccc(Cl)c2)c1 10.1021/jm0509445
44441235 150448 0 None -1584 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 430 9 4 5 4.9 C[C@H](CNc1ccc(-c2sccc2C(=O)O)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2007.05.069
CHEMBL395834 150448 0 None -1584 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 430 9 4 5 4.9 C[C@H](CNc1ccc(-c2sccc2C(=O)O)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2007.05.069
145991502 166286 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 400 7 4 4 3.7 O=c1ccc2c(C(CO)NCC(c3ccccc3)c3ccccc3)ccc(O)c2[nH]1 10.1016/j.ejmech.2018.04.041
CHEMBL4285474 166286 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 400 7 4 4 3.7 O=c1ccc2c(C(CO)NCC(c3ccccc3)c3ccccc3)ccc(O)c2[nH]1 10.1016/j.ejmech.2018.04.041
145992059 166408 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 423 9 5 5 3.1 CC(C)CC(=O)Nc1ccc(CCNC(CO)c2ccc(O)c3[nH]c(=O)ccc23)cc1 10.1016/j.ejmech.2018.04.041
CHEMBL4287518 166408 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 423 9 5 5 3.1 CC(C)CC(=O)Nc1ccc(CCNC(CO)c2ccc(O)c3[nH]c(=O)ccc23)cc1 10.1016/j.ejmech.2018.04.041
90644150 111744 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 491 11 4 7 3.1 COc1ccc(CN2CCN(c3ccc(CCNCC(O)c4ccc(O)c(CO)c4)cc3)CC2)cc1 10.1016/j.bmcl.2014.04.069
CHEMBL3290979 111744 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 491 11 4 7 3.1 COc1ccc(CN2CCN(c3ccc(CCNCC(O)c4ccc(O)c(CO)c4)cc3)CC2)cc1 10.1016/j.bmcl.2014.04.069
10103414 76169 13 None -1 3 Rat 5.2 pEC50 = 5.2 Functional
Vasodilating activity against phenylephrine-induced contractions in rat thoracic aortaVasodilating activity against phenylephrine-induced contractions in rat thoracic aorta
ChEMBL 159 2 2 5 -2.1 NC(=O)c1c(CO)no[n+]1[O-] 10.1021/jm0704595
CHEMBL206100 76169 13 None -1 3 Rat 5.2 pEC50 = 5.2 Functional
Vasodilating activity against phenylephrine-induced contractions in rat thoracic aortaVasodilating activity against phenylephrine-induced contractions in rat thoracic aorta
ChEMBL 159 2 2 5 -2.1 NC(=O)c1c(CO)no[n+]1[O-] 10.1021/jm0704595
1104203 44603 12 None - 1 Human 6.2 pEC50 = 6.2 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 350 4 1 7 3.6 O=C(Nc1ccc(-c2nc3ncccc3o2)cc1)c1ccc([N+](=O)[O-])o1 nan
CHEMBL1522618 44603 12 None - 1 Human 6.2 pEC50 = 6.2 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 350 4 1 7 3.6 O=C(Nc1ccc(-c2nc3ncccc3o2)cc1)c1ccc([N+](=O)[O-])o1 nan
9169702 66924 6 None - 1 Human 7.2 pEC50 = 7.2 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 423 8 1 5 2.7 CCC(=O)c1ccc(OCC(=O)N2CCN(CC(=O)Nc3ccc(C)cc3)CC2)cc1 nan
CHEMBL1881705 66924 6 None - 1 Human 7.2 pEC50 = 7.2 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 423 8 1 5 2.7 CCC(=O)c1ccc(OCC(=O)N2CCN(CC(=O)Nc3ccc(C)cc3)CC2)cc1 nan
90666109 108838 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP productionAgonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP production
ChEMBL 700 18 6 9 6.3 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3cc(O)cc(F)c3)CC2)ccc1O 10.1039/C1MD00140J
CHEMBL3219039 108838 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP productionAgonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP production
ChEMBL 700 18 6 9 6.3 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3cc(O)cc(F)c3)CC2)ccc1O 10.1039/C1MD00140J
160510 100645 36 None - 1 Human 5.2 pEC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 184 0 1 1 2.5 CC1=NCCc2c1[nH]c1ccccc21 nan
CHEMBL1506260 100645 36 None - 1 Human 5.2 pEC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 184 0 1 1 2.5 CC1=NCCc2c1[nH]c1ccccc21 nan
CHEMBL295234 100645 36 None - 1 Human 5.2 pEC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 184 0 1 1 2.5 CC1=NCCc2c1[nH]c1ccccc21 nan
6619041 21036 7 None 6 2 Human 5.2 pEC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 502 9 2 8 3.2 CCOc1ccc(NC(=O)CNC(=O)c2nn(-c3ccc(OC)c(OC)c3)c(=O)c3ccccc23)cc1 nan
CHEMBL1313270 21036 7 None 6 2 Human 5.2 pEC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 502 9 2 8 3.2 CCOc1ccc(NC(=O)CNC(=O)c2nn(-c3ccc(OC)c(OC)c3)c(=O)c3ccccc23)cc1 nan
44396532 66408 0 None -42 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at Homo sapiens (human) beta2 adrenoreceptorAgonist activity at Homo sapiens (human) beta2 adrenoreceptor
ChEMBL 455 9 4 5 4.3 C[C@H](Cc1c[nH]c2ccccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1007/s00044-009-9257-x
CHEMBL185836 66408 0 None -42 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at Homo sapiens (human) beta2 adrenoreceptorAgonist activity at Homo sapiens (human) beta2 adrenoreceptor
ChEMBL 455 9 4 5 4.3 C[C@H](Cc1c[nH]c2ccccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1007/s00044-009-9257-x
655791 20381 5 None - 1 Human 6.2 pEC50 = 6.2 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 462 7 1 8 4.2 Cn1c(CNc2nc(-c3ccccc3)cs2)nnc1SCC(=O)N1CCc2ccccc21 nan
CHEMBL1308099 20381 5 None - 1 Human 6.2 pEC50 = 6.2 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 462 7 1 8 4.2 Cn1c(CNc2nc(-c3ccccc3)cs2)nnc1SCC(=O)N1CCc2ccccc21 nan
1369799 44199 8 None - 1 Human 7.2 pEC50 = 7.2 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 401 5 1 5 5.2 CC(C)(C)c1ccc(OCC(=O)Nc2ccc(-c3nc4cccnc4o3)cc2)cc1 nan
CHEMBL1519042 44199 8 None - 1 Human 7.2 pEC50 = 7.2 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 401 5 1 5 5.2 CC(C)(C)c1ccc(OCC(=O)Nc2ccc(-c3nc4cccnc4o3)cc2)cc1 nan
105 3392 84 None -8 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assayAgonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assay
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1021/jm100068m
2083 3392 84 None -8 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assayAgonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assay
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1021/jm100068m
558 3392 84 None -8 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assayAgonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assay
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1021/jm100068m
CHEMBL714 3392 84 None -8 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assayAgonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assay
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1021/jm100068m
DB01001 3392 84 None -8 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assayAgonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assay
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1021/jm100068m
46232816 199259 0 None 3 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 432 7 4 5 4.0 CC(C)(Cc1ccc(-c2ccccc2)cc1)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmcl.2009.12.087
CHEMBL601858 199259 0 None 3 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 432 7 4 5 4.0 CC(C)(Cc1ccc(-c2ccccc2)cc1)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmcl.2009.12.087
10305108 110942 0 None -134 3 Human 6.2 pEC50 = 6.2 Functional
In vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-2 adrenergic receptorIn vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-2 adrenergic receptor
ChEMBL 659 17 6 8 4.2 CCCCCCCCNC(=O)Nc1ccc(S(=O)(=O)N2CCC(CNC[C@H](O)COc3ccc(O)c4c3CCC(=O)N4)CC2)cc1 10.1016/s0960-894x(02)00607-8
CHEMBL327519 110942 0 None -134 3 Human 6.2 pEC50 = 6.2 Functional
In vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-2 adrenergic receptorIn vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-2 adrenergic receptor
ChEMBL 659 17 6 8 4.2 CCCCCCCCNC(=O)Nc1ccc(S(=O)(=O)N2CCC(CNC[C@H](O)COc3ccc(O)c4c3CCC(=O)N4)CC2)cc1 10.1016/s0960-894x(02)00607-8
44392490 64897 0 None 1 3 Human 7.2 pEC50 = 7.2 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-2 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-2 adrenergic receptor
ChEMBL 507 10 4 6 4.0 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(NC(=O)c2ccccc2)c1 10.1016/j.bmcl.2004.12.033
CHEMBL182708 64897 0 None 1 3 Human 7.2 pEC50 = 7.2 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-2 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-2 adrenergic receptor
ChEMBL 507 10 4 6 4.0 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(NC(=O)c2ccccc2)c1 10.1016/j.bmcl.2004.12.033
1253647 36843 9 None - 1 Human 7.2 pEC50 = 7.2 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 448 3 0 8 2.6 O=C(c1cc2c(=O)n3ccccc3nc2s1)N1CCN(Cc2ccc3c(c2)OCO3)CC1 nan
CHEMBL1452334 36843 9 None - 1 Human 7.2 pEC50 = 7.2 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 448 3 0 8 2.6 O=C(c1cc2c(=O)n3ccccc3nc2s1)N1CCN(Cc2ccc3c(c2)OCO3)CC1 nan
3086576 176371 29 None -11 3 Guinea pig 5.2 pEC50 = 5.2 Functional
Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as relaxation of carbachol-induced tissue contractionAgonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as relaxation of carbachol-induced tissue contraction
ChEMBL 261 2 3 4 1.1 CC(C)N[C@@H]1CCn2c(=O)[nH]c3cccc(c32)[C@H]1O 10.1021/jm801211c
CHEMBL462313 176371 29 None -11 3 Guinea pig 5.2 pEC50 = 5.2 Functional
Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as relaxation of carbachol-induced tissue contractionAgonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as relaxation of carbachol-induced tissue contraction
ChEMBL 261 2 3 4 1.1 CC(C)N[C@@H]1CCn2c(=O)[nH]c3cccc(c32)[C@H]1O 10.1021/jm801211c
CHEMBL513390 176371 29 None -11 3 Guinea pig 5.2 pEC50 = 5.2 Functional
Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as relaxation of carbachol-induced tissue contractionAgonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as relaxation of carbachol-induced tissue contraction
ChEMBL 261 2 3 4 1.1 CC(C)N[C@@H]1CCn2c(=O)[nH]c3cccc(c32)[C@H]1O 10.1021/jm801211c
24794013 51113 1 None - 1 Human 6.2 pEC50 = 6.2 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 404 5 1 4 4.4 Cc1ncc(CN2CCCC(C(=O)Nc3ccc(-c4cccc(F)c4)cc3)C2)cn1 nan
CHEMBL1581826 51113 1 None - 1 Human 6.2 pEC50 = 6.2 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 404 5 1 4 4.4 Cc1ncc(CN2CCCC(C(=O)Nc3ccc(-c4cccc(F)c4)cc3)C2)cn1 nan
127045853 139250 0 None 117 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human beta2 receptor expressed in HEK293 cells cotransfected with Gqs5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositolAgonist activity at human beta2 receptor expressed in HEK293 cells cotransfected with Gqs5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositol
ChEMBL 492 12 4 7 3.6 COc1cc(CCNC[C@H](O)c2ccc(O)c3c2OCC(=O)N3)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
CHEMBL3798748 139250 0 None 117 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human beta2 receptor expressed in HEK293 cells cotransfected with Gqs5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositolAgonist activity at human beta2 receptor expressed in HEK293 cells cotransfected with Gqs5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositol
ChEMBL 492 12 4 7 3.6 COc1cc(CCNC[C@H](O)c2ccc(O)c3c2OCC(=O)N3)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
16735261 85292 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assayAgonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assay
ChEMBL 317 7 4 5 2.4 COc1ccc(C[C@@H](C)NC[C@@H](O)c2cc(O)cc(O)c2)cc1 10.1016/j.bmc.2009.11.062
CHEMBL228998 85292 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assayAgonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assay
ChEMBL 317 7 4 5 2.4 COc1ccc(C[C@@H](C)NC[C@@H](O)c2cc(O)cc(O)c2)cc1 10.1016/j.bmc.2009.11.062
16735261 85292 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulationAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulation
ChEMBL 317 7 4 5 2.4 COc1ccc(C[C@@H](C)NC[C@@H](O)c2cc(O)cc(O)c2)cc1 10.1016/j.bmc.2013.11.030
CHEMBL228998 85292 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulationAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulation
ChEMBL 317 7 4 5 2.4 COc1ccc(C[C@@H](C)NC[C@@H](O)c2cc(O)cc(O)c2)cc1 10.1016/j.bmc.2013.11.030
44396737 66509 0 None -6 3 Human 8.1 pEC50 = 8.1 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptor
ChEMBL 683 14 4 10 5.2 CCOC(=O)c1ccc(S(=O)(=O)Oc2cccc3c(C[C@@H](C)NC[C@H](O)c4cccc(NS(=O)(=O)c5cccs5)c4)c[nH]c23)cc1 10.1016/j.bmcl.2004.10.035
CHEMBL186236 66509 0 None -6 3 Human 8.1 pEC50 = 8.1 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptor
ChEMBL 683 14 4 10 5.2 CCOC(=O)c1ccc(S(=O)(=O)Oc2cccc3c(C[C@@H](C)NC[C@H](O)c4cccc(NS(=O)(=O)c5cccs5)c4)c[nH]c23)cc1 10.1016/j.bmcl.2004.10.035
44396530 66738 0 None -23 3 Human 8.1 pEC50 = 8.1 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptor
ChEMBL 591 14 4 8 4.8 CCCCS(=O)(=O)Oc1cccc2c(C[C@@H](C)NC[C@H](O)c3cccc(NS(=O)(=O)c4cccs4)c3)c[nH]c12 10.1016/j.bmcl.2004.10.035
CHEMBL187317 66738 0 None -23 3 Human 8.1 pEC50 = 8.1 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptor
ChEMBL 591 14 4 8 4.8 CCCCS(=O)(=O)Oc1cccc2c(C[C@@H](C)NC[C@H](O)c3cccc(NS(=O)(=O)c4cccs4)c3)c[nH]c12 10.1016/j.bmcl.2004.10.035
658782 49826 10 None - 1 Human 8.1 pEC50 = 8.1 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory)
ChEMBL 465 4 0 9 1.9 Cn1c(N2CCN(c3ccccn3)CC2)nc2c1c(=O)n(Cc1ccc(Cl)cc1)c(=O)n2C nan
CHEMBL1570111 49826 10 None - 1 Human 8.1 pEC50 = 8.1 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory)
ChEMBL 465 4 0 9 1.9 Cn1c(N2CCN(c3ccccn3)CC2)nc2c1c(=O)n(Cc1ccc(Cl)cc1)c(=O)n2C nan
42629372 63301 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assayAgonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assay
ChEMBL 337 6 4 4 3.5 C[C@@H](Cc1ccc2ccccc2c1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2009.11.062
CHEMBL1800962 63301 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assayAgonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assay
ChEMBL 337 6 4 4 3.5 C[C@@H](Cc1ccc2ccccc2c1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2009.11.062
44392542 65516 0 None -6 3 Human 8.1 pEC50 = 8.1 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-2 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-2 adrenergic receptor
ChEMBL 543 11 4 6 5.5 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(NCc2ccc3ccccc3c2)c1 10.1016/j.bmcl.2004.12.033
CHEMBL183552 65516 0 None -6 3 Human 8.1 pEC50 = 8.1 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-2 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-2 adrenergic receptor
ChEMBL 543 11 4 6 5.5 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(NCc2ccc3ccccc3c2)c1 10.1016/j.bmcl.2004.12.033
44396559 66499 0 None -7 2 Human 8.1 pEC50 = 8.1 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptor
ChEMBL 499 11 4 6 4.7 CCOc1cccc2c(C[C@@H](C)NC[C@H](O)c3cccc(NS(=O)(=O)c4cccs4)c3)c[nH]c12 10.1016/j.bmcl.2004.10.035
CHEMBL186196 66499 0 None -7 2 Human 8.1 pEC50 = 8.1 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptor
ChEMBL 499 11 4 6 4.7 CCOc1cccc2c(C[C@@H](C)NC[C@H](O)c3cccc(NS(=O)(=O)c4cccs4)c3)c[nH]c12 10.1016/j.bmcl.2004.10.035
4191632 45299 10 None - 1 Human 8.1 pEC50 = 8.1 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 425 8 2 6 3.7 O=C(CCCCCn1c(=S)[nH]c2ccccc2c1=O)NCc1ccc2c(c1)OCO2 nan
CHEMBL1528906 45299 10 None - 1 Human 8.1 pEC50 = 8.1 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 425 8 2 6 3.7 O=C(CCCCCn1c(=S)[nH]c2ccccc2c1=O)NCc1ccc2c(c1)OCO2 nan
1016754 22479 12 None - 1 Human 8.1 pEC50 = 8.1 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory)
ChEMBL 395 5 1 5 5.3 O=C(CSc1ccc(Cl)cc1)Nc1ccc(-c2nc3ncccc3o2)cc1 nan
CHEMBL1327325 22479 12 None - 1 Human 8.1 pEC50 = 8.1 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory)
ChEMBL 395 5 1 5 5.3 O=C(CSc1ccc(Cl)cc1)Nc1ccc(-c2nc3ncccc3o2)cc1 nan
11134054 46704 0 None -6 3 Human 8.1 pEC50 = 8.1 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-2 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-2 AR expressed as the negative logarithm of the molar drug concentration
ChEMBL 444 10 4 6 4.1 C[C@H](CNc1ccc(CC(=O)Nc2nccs2)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0101500
CHEMBL154150 46704 0 None -6 3 Human 8.1 pEC50 = 8.1 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-2 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-2 AR expressed as the negative logarithm of the molar drug concentration
ChEMBL 444 10 4 6 4.1 C[C@H](CNc1ccc(CC(=O)Nc2nccs2)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0101500
1239 1639 46 None -1 5 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at beta 2 in human A431 cells adrenoceptor assessed as cAMP accumulationAgonist activity at beta 2 in human A431 cells adrenoceptor assessed as cAMP accumulation
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2010.06.136
3410 1639 46 None -1 5 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at beta 2 in human A431 cells adrenoceptor assessed as cAMP accumulationAgonist activity at beta 2 in human A431 cells adrenoceptor assessed as cAMP accumulation
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2010.06.136
3465 1639 46 None -1 5 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at beta 2 in human A431 cells adrenoceptor assessed as cAMP accumulationAgonist activity at beta 2 in human A431 cells adrenoceptor assessed as cAMP accumulation
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2010.06.136
CHEMBL1256786 1639 46 None -1 5 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at beta 2 in human A431 cells adrenoceptor assessed as cAMP accumulationAgonist activity at beta 2 in human A431 cells adrenoceptor assessed as cAMP accumulation
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2010.06.136
DB00983 1639 46 None -1 5 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at beta 2 in human A431 cells adrenoceptor assessed as cAMP accumulationAgonist activity at beta 2 in human A431 cells adrenoceptor assessed as cAMP accumulation
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2010.06.136
56683262 63205 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
ChEMBL 457 12 4 6 3.0 CC(C)(CNCCc1ccc(O)c2[nH]c(=O)sc12)NC(=O)CCOCCc1ccccc1 10.1016/j.bmcl.2011.04.135
CHEMBL1800474 63205 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
ChEMBL 457 12 4 6 3.0 CC(C)(CNCCc1ccc(O)c2[nH]c(=O)sc12)NC(=O)CCOCCc1ccccc1 10.1016/j.bmcl.2011.04.135
56666341 63215 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
ChEMBL 471 14 3 6 3.3 CCCN(CCNCCc1ccc(O)c2[nH]c(=O)sc12)C(=O)CCOCCc1ccccc1 10.1016/j.bmcl.2011.04.135
CHEMBL1800657 63215 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
ChEMBL 471 14 3 6 3.3 CCCN(CCNCCc1ccc(O)c2[nH]c(=O)sc12)C(=O)CCOCCc1ccccc1 10.1016/j.bmcl.2011.04.135
56659408 63216 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
ChEMBL 471 13 3 6 3.3 CC(C)N(CCNCCc1ccc(O)c2[nH]c(=O)sc12)C(=O)CCOCCc1ccccc1 10.1016/j.bmcl.2011.04.135
CHEMBL1800658 63216 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
ChEMBL 471 13 3 6 3.3 CC(C)N(CCNCCc1ccc(O)c2[nH]c(=O)sc12)C(=O)CCOCCc1ccccc1 10.1016/j.bmcl.2011.04.135
16035375 110756 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assayAgonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assay
ChEMBL 528 17 3 7 3.2 CCN(CC)CCN(CCNCCc1ccc(O)c2[nH]c(=O)sc12)C(=O)CCOCCc1ccccc1 10.1021/ml4005232
CHEMBL3265157 110756 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assayAgonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assay
ChEMBL 528 17 3 7 3.2 CCN(CC)CCN(CCNCCc1ccc(O)c2[nH]c(=O)sc12)C(=O)CCOCCc1ccccc1 10.1021/ml4005232
90655868 110764 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assayAgonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assay
ChEMBL 574 17 3 7 4.0 CN(CCCN(CCNCCc1ccc(O)c2[nH]c(=O)sc12)C(=O)CCOCCc1cccc(Cl)c1)C1CC1 10.1021/ml4005232
CHEMBL3265165 110764 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assayAgonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assay
ChEMBL 574 17 3 7 4.0 CN(CCCN(CCNCCc1ccc(O)c2[nH]c(=O)sc12)C(=O)CCOCCc1cccc(Cl)c1)C1CC1 10.1021/ml4005232
16035175 110767 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assayAgonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assay
ChEMBL 546 17 3 7 3.4 CCN(CC)CCN(CCNCCc1ccc(O)c2[nH]c(=O)sc12)C(=O)CCOCCc1cccc(F)c1 10.1021/ml4005232
CHEMBL3265169 110767 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assayAgonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assay
ChEMBL 546 17 3 7 3.4 CCN(CC)CCN(CCNCCc1ccc(O)c2[nH]c(=O)sc12)C(=O)CCOCCc1cccc(F)c1 10.1021/ml4005232
16035281 110769 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assayAgonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assay
ChEMBL 558 18 3 8 3.3 CCN(CC)CCN(CCNCCc1ccc(O)c2[nH]c(=O)sc12)C(=O)CCOCCc1cccc(OC)c1 10.1021/ml4005232
CHEMBL3265170 110769 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assayAgonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assay
ChEMBL 558 18 3 8 3.3 CCN(CC)CCN(CCNCCc1ccc(O)c2[nH]c(=O)sc12)C(=O)CCOCCc1cccc(OC)c1 10.1021/ml4005232
57401436 70043 0 None 1 4 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 479 11 5 7 3.5 COc1ccccc1CNCc1ccc(CCNC[C@@H](O)c2ccc(O)c3[nH]c(=O)sc23)cc1 10.1016/j.bmcl.2011.10.049
CHEMBL1945504 70043 0 None 1 4 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 479 11 5 7 3.5 COc1ccccc1CNCc1ccc(CCNC[C@@H](O)c2ccc(O)c3[nH]c(=O)sc23)cc1 10.1016/j.bmcl.2011.10.049
11318107 105894 0 None 251 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 505 16 4 7 3.4 O=S1(=O)CCc2ccc(CCCCOCCCCCCNC[C@H](O)c3ccc(O)c(CO)c3)cc21 10.1021/jm401532g
CHEMBL3126386 105894 0 None 251 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 505 16 4 7 3.4 O=S1(=O)CCc2ccc(CCCCOCCCCCCNC[C@H](O)c3ccc(O)c(CO)c3)cc21 10.1021/jm401532g
CHEMBL3139364 105894 0 None 251 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 505 16 4 7 3.4 O=S1(=O)CCc2ccc(CCCCOCCCCCCNC[C@H](O)c3ccc(O)c(CO)c3)cc21 10.1021/jm401532g
42625741 12476 0 None 158 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1cccc(CCCCCOCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
CHEMBL1186940 12476 0 None 158 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1cccc(CCCCCOCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
CHEMBL483202 12476 0 None 158 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1cccc(CCCCCOCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
46833103 7317 0 None 7 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 433 16 5 7 3.0 OCc1cc([C@@H](O)CNCCCCCCOCCOCc2ccc(O)cc2)ccc1O 10.1021/jm100326d
CHEMBL1086535 7317 0 None 7 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 433 16 5 7 3.0 OCc1cc([C@@H](O)CNCCCCCCOCCOCc2ccc(O)cc2)ccc1O 10.1021/jm100326d
59119472 111752 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 418 9 5 5 4.0 OCc1cc(C(O)CNCCc2ccc(Nc3ccc4c(c3)CCC4)cc2)ccc1O 10.1016/j.bmcl.2014.04.069
CHEMBL3290986 111752 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 418 9 5 5 4.0 OCc1cc(C(O)CNCCc2ccc(Nc3ccc4c(c3)CCC4)cc2)ccc1O 10.1016/j.bmcl.2014.04.069
59119417 111753 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 454 10 5 5 5.2 OCc1cc(C(O)CNCCc2ccc(Nc3ccc(-c4ccccc4)cc3)cc2)ccc1O 10.1016/j.bmcl.2014.04.069
CHEMBL3290987 111753 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 454 10 5 5 5.2 OCc1cc(C(O)CNCCc2ccc(Nc3ccc(-c4ccccc4)cc3)cc2)ccc1O 10.1016/j.bmcl.2014.04.069
57391346 69867 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 438 11 7 7 2.6 OCc1cc(C(O)CNCCc2ccc(NCC(O)c3ccc(O)cc3)cc2)ccc1O 10.1016/j.bmcl.2011.11.072
CHEMBL1940824 69867 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 438 11 7 7 2.6 OCc1cc(C(O)CNCCc2ccc(NCC(O)c3ccc(O)cc3)cc2)ccc1O 10.1016/j.bmcl.2011.11.072
45483825 195582 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 315 7 4 4 2.5 CC(C)(Cc1ccccc1)NCC(O)c1ccc(O)c(CO)c1 10.1016/j.bmcl.2009.10.013
CHEMBL568511 195582 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 315 7 4 4 2.5 CC(C)(Cc1ccccc1)NCC(O)c1ccc(O)c(CO)c1 10.1016/j.bmcl.2009.10.013
2952777 192988 7 None - 1 Human 5.2 pEC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 443 6 1 6 6.0 CC(Oc1ccc(Cl)cc1Cl)c1nc(-c2ccc(NC(=O)c3ccco3)cc2)no1 nan
CHEMBL531401 192988 7 None - 1 Human 5.2 pEC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 443 6 1 6 6.0 CC(Oc1ccc(Cl)cc1Cl)c1nc(-c2ccc(NC(=O)c3ccco3)cc2)no1 nan
155774 4021 33 None -64 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 339 8 4 6 -0.2 OC(COc1ccc(cc1)O)CNCCNC(=O)N1CCOCC1 10.1021/jm400348g
2848 4021 33 None -64 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 339 8 4 6 -0.2 OC(COc1ccc(cc1)O)CNCCNC(=O)N1CCOCC1 10.1021/jm400348g
538 4021 33 None -64 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 339 8 4 6 -0.2 OC(COc1ccc(cc1)O)CNCCNC(=O)N1CCOCC1 10.1021/jm400348g
CHEMBL75753 4021 33 None -64 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 339 8 4 6 -0.2 OC(COc1ccc(cc1)O)CNCCNC(=O)N1CCOCC1 10.1021/jm400348g
DB13781 4021 33 None -64 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 339 8 4 6 -0.2 OC(COc1ccc(cc1)O)CNCCNC(=O)N1CCOCC1 10.1021/jm400348g
1288829 24917 10 None - 1 Human 6.2 pEC50 = 6.2 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory)
ChEMBL 391 6 1 6 5.0 Cc1ccc(SCC(=O)Nc2ccc(-c3nnc(-c4ccco4)o3)cc2)cc1 nan
CHEMBL1347493 24917 10 None - 1 Human 6.2 pEC50 = 6.2 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory)
ChEMBL 391 6 1 6 5.0 Cc1ccc(SCC(=O)Nc2ccc(-c3nnc(-c4ccco4)o3)cc2)cc1 nan
3105 14318 31 None - 1 Human 5.2 pEC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 351 5 2 6 2.8 CNCC(O)c1ccc(OC(=O)C(C)(C)C)c(OC(=O)C(C)(C)C)c1 nan
CHEMBL1200833 14318 31 None - 1 Human 5.2 pEC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 351 5 2 6 2.8 CNCC(O)c1ccc(OC(=O)C(C)(C)C)c(OC(=O)C(C)(C)C)c1 nan
CHEMBL1201262 14318 31 None - 1 Human 5.2 pEC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 351 5 2 6 2.8 CNCC(O)c1ccc(OC(=O)C(C)(C)C)c(OC(=O)C(C)(C)C)c1 nan
24789167 58966 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 502 8 2 7 3.3 Cc1cc(C)cc(C(=O)NC(CC(N)=O)c2ccc(N3CCN(c4ccccn4)CC3)c([N+](=O)[O-])c2)c1 nan
CHEMBL1705007 58966 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 502 8 2 7 3.3 Cc1cc(C)cc(C(=O)NC(CC(N)=O)c2ccc(N3CCN(c4ccccn4)CC3)c([N+](=O)[O-])c2)c1 nan
44396779 66711 0 None -17 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at Homo sapiens (human) beta2 adrenoreceptorAgonist activity at Homo sapiens (human) beta2 adrenoreceptor
ChEMBL 611 12 4 8 5.1 C[C@H](Cc1c[nH]c2c(OS(=O)(=O)c3ccccc3)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1007/s00044-009-9257-x
CHEMBL187209 66711 0 None -17 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at Homo sapiens (human) beta2 adrenoreceptorAgonist activity at Homo sapiens (human) beta2 adrenoreceptor
ChEMBL 611 12 4 8 5.1 C[C@H](Cc1c[nH]c2c(OS(=O)(=O)c3ccccc3)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1007/s00044-009-9257-x
168292283 192379 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 316 4 3 3 2.7 Nc1c(F)cc(C(CO)NC2CCCC2)cc1Br 10.1021/acs.jmedchem.1c02006
CHEMBL5200165 192379 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 316 4 3 3 2.7 Nc1c(F)cc(C(CO)NC2CCCC2)cc1Br 10.1021/acs.jmedchem.1c02006
CHEMBL5222623 192379 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 316 4 3 3 2.7 Nc1c(F)cc(C(CO)NC2CCCC2)cc1Br 10.1021/acs.jmedchem.1c02006
127047996 139103 0 None -28 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human beta2 receptor expressed in HEK293 cells cotransfected with Gqs5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositolAgonist activity at human beta2 receptor expressed in HEK293 cells cotransfected with Gqs5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositol
ChEMBL 303 8 3 5 2.3 COc1ccccc1OCCNCCc1ccc(O)c(O)c1 10.1016/j.bmc.2016.04.028
CHEMBL3797758 139103 0 None -28 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human beta2 receptor expressed in HEK293 cells cotransfected with Gqs5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositolAgonist activity at human beta2 receptor expressed in HEK293 cells cotransfected with Gqs5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositol
ChEMBL 303 8 3 5 2.3 COc1ccccc1OCCNCCc1ccc(O)c(O)c1 10.1016/j.bmc.2016.04.028
1132508 27913 15 None - 1 Human 6.1 pEC50 = 6.1 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 419 3 1 5 6.3 Cc1ccc(-c2nc3ncccc3o2)cc1NC(=O)c1sc2ccccc2c1Cl nan
CHEMBL1373276 27913 15 None - 1 Human 6.1 pEC50 = 6.1 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 419 3 1 5 6.3 Cc1ccc(-c2nc3ncccc3o2)cc1NC(=O)c1sc2ccccc2c1Cl nan
4117484 48420 2 None - 1 Human 5.1 pEC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 386 5 2 5 3.0 CCc1ccccc1N(C)S(=O)(=O)c1ccc2ncc(C(=O)O)c(O)c2c1 nan
CHEMBL1557985 48420 2 None - 1 Human 5.1 pEC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 386 5 2 5 3.0 CCc1ccccc1N(C)S(=O)(=O)c1ccc2ncc(C(=O)O)c(O)c2c1 nan
168289238 192342 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 304 4 3 5 1.2 CC(C)(C)NC(CO)c1cc(F)c(N)c(S(C)(=O)=O)c1 10.1021/acs.jmedchem.1c02006
CHEMBL5194956 192342 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 304 4 3 5 1.2 CC(C)(C)NC(CO)c1cc(F)c(N)c(S(C)(=O)=O)c1 10.1021/acs.jmedchem.1c02006
CHEMBL5222430 192342 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 304 4 3 5 1.2 CC(C)(C)NC(CO)c1cc(F)c(N)c(S(C)(=O)=O)c1 10.1021/acs.jmedchem.1c02006
688468 141788 7 None -346 2 Rat 7.1 pEC50 = 7.1 Functional
Agonist activity beta2-adrenergic receptor in rat ventricular myocytes assessed as cell contraction following electrical stimulation by optical edge tracking method using photodiode arrayAgonist activity beta2-adrenergic receptor in rat ventricular myocytes assessed as cell contraction following electrical stimulation by optical edge tracking method using photodiode array
ChEMBL 303 6 5 5 2.1 C[C@H](Cc1ccc(O)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2009.11.062
CHEMBL388570 141788 7 None -346 2 Rat 7.1 pEC50 = 7.1 Functional
Agonist activity beta2-adrenergic receptor in rat ventricular myocytes assessed as cell contraction following electrical stimulation by optical edge tracking method using photodiode arrayAgonist activity beta2-adrenergic receptor in rat ventricular myocytes assessed as cell contraction following electrical stimulation by optical edge tracking method using photodiode array
ChEMBL 303 6 5 5 2.1 C[C@H](Cc1ccc(O)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2009.11.062
24820094 59387 1 None - 1 Human 6.1 pEC50 = 6.1 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory)
ChEMBL 409 5 1 4 5.1 Cc1ncc(CN2CCCC(C(=O)Nc3ccc(-c4cccc(F)c4)cc3)C2)s1 nan
CHEMBL1723653 59387 1 None - 1 Human 6.1 pEC50 = 6.1 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory)
ChEMBL 409 5 1 4 5.1 Cc1ncc(CN2CCCC(C(=O)Nc3ccc(-c4cccc(F)c4)cc3)C2)s1 nan
90666101 108831 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP productionAgonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP production
ChEMBL 666 18 5 8 6.5 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)ccc1O 10.1039/C1MD00140J
CHEMBL3219031 108831 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP productionAgonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP production
ChEMBL 666 18 5 8 6.5 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)ccc1O 10.1039/C1MD00140J
878337 44778 4 None - 1 Human 5.1 pEC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 309 4 2 2 4.1 O=C(NC1(Cc2ccc(O)cc2)CCCCC1)c1ccccc1 nan
CHEMBL1524289 44778 4 None - 1 Human 5.1 pEC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 309 4 2 2 4.1 O=C(NC1(Cc2ccc(O)cc2)CCCCC1)c1ccccc1 nan
567055 23189 10 None - 1 Human 5.1 pEC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 323 5 2 2 4.0 O=C(Cc1ccccc1)NC1(Cc2ccc(O)cc2)CCCCC1 nan
CHEMBL1332942 23189 10 None - 1 Human 5.1 pEC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 323 5 2 2 4.0 O=C(Cc1ccccc1)NC1(Cc2ccc(O)cc2)CCCCC1 nan
2816337 46170 5 None - 1 Human 7.1 pEC50 = 7.1 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 441 6 1 7 5.9 C=CCn1c(SCc2ccccc2Cl)nnc1-c1sc2nc(C)cc(C)c2c1N nan
CHEMBL1537056 46170 5 None - 1 Human 7.1 pEC50 = 7.1 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 441 6 1 7 5.9 C=CCn1c(SCc2ccccc2Cl)nnc1-c1sc2nc(C)cc(C)c2c1N nan
2481225 34560 6 None - 1 Human 5.1 pEC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 363 5 1 4 4.3 CCOC(=O)c1ccc(NC(=O)Cc2coc3cc4c(cc23)CCC4)cc1 nan
CHEMBL1431082 34560 6 None - 1 Human 5.1 pEC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 363 5 1 4 4.3 CCOC(=O)c1ccc(NC(=O)Cc2coc3cc4c(cc23)CCC4)cc1 nan
135799865 185998 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHO cells harboring beta2-beta-arr assessed as induction of beta-arrestin 2 recruitment using beta-galactosidase as substrate preincubated for 90 mins followed by substrate addition and measured after 60 mins by luminescence assayAgonist activity at human beta2 adrenoceptor expressed in CHO cells harboring beta2-beta-arr assessed as induction of beta-arrestin 2 recruitment using beta-galactosidase as substrate preincubated for 90 mins followed by substrate addition and measured after 60 mins by luminescence assay
ChEMBL 262 4 4 4 1.3 CC(C)NC(CO)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/acs.jmedchem.0c01195
CHEMBL4878555 185998 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHO cells harboring beta2-beta-arr assessed as induction of beta-arrestin 2 recruitment using beta-galactosidase as substrate preincubated for 90 mins followed by substrate addition and measured after 60 mins by luminescence assayAgonist activity at human beta2 adrenoceptor expressed in CHO cells harboring beta2-beta-arr assessed as induction of beta-arrestin 2 recruitment using beta-galactosidase as substrate preincubated for 90 mins followed by substrate addition and measured after 60 mins by luminescence assay
ChEMBL 262 4 4 4 1.3 CC(C)NC(CO)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/acs.jmedchem.0c01195
9551438 59060 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 389 8 2 5 2.8 O=C(CCCCCn1c(=O)[nH]c2ccsc2c1=O)NCc1ccc(F)cc1 nan
CHEMBL1709014 59060 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 389 8 2 5 2.8 O=C(CCCCCn1c(=O)[nH]c2ccsc2c1=O)NCc1ccc(F)cc1 nan
10346448 119312 0 None -501 3 Human 7.1 pEC50 = 7.1 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-2 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-2 AR expressed as the negative logarithm of the molar drug concentration
ChEMBL 515 11 4 6 3.8 Cc1ccc(S(=O)(=O)NC(=O)Cc2ccc(NC[C@@H](C)NC[C@H](O)c3cccc(Cl)c3)cc2)cc1 10.1021/jm0101500
CHEMBL348501 119312 0 None -501 3 Human 7.1 pEC50 = 7.1 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-2 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-2 AR expressed as the negative logarithm of the molar drug concentration
ChEMBL 515 11 4 6 3.8 Cc1ccc(S(=O)(=O)NC(=O)Cc2ccc(NC[C@@H](C)NC[C@H](O)c3cccc(Cl)c3)cc2)cc1 10.1021/jm0101500
44441234 93343 0 None -251 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 414 9 4 5 4.4 C[C@H](CNc1ccc(-c2occc2C(=O)O)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2007.05.069
CHEMBL247520 93343 0 None -251 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 414 9 4 5 4.4 C[C@H](CNc1ccc(-c2occc2C(=O)O)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2007.05.069
145982386 166066 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 339 6 5 5 1.7 Nc1ccc(CCNC(CO)c2ccc(O)c3[nH]c(=O)ccc23)cc1 10.1016/j.ejmech.2018.04.041
CHEMBL4280939 166066 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 339 6 5 5 1.7 Nc1ccc(CCNC(CO)c2ccc(O)c3[nH]c(=O)ccc23)cc1 10.1016/j.ejmech.2018.04.041
57395240 70138 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 465 11 4 5 4.1 O=c1[nH]c2c(O)ccc(CCNCCc3ccc(CNCCc4ccccc4F)cc3)c2s1 10.1016/j.bmcl.2011.10.049
CHEMBL1946762 70138 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 465 11 4 5 4.1 O=c1[nH]c2c(O)ccc(CCNCCc3ccc(CNCCc4ccccc4F)cc3)c2s1 10.1016/j.bmcl.2011.10.049
4611324 21556 8 None - 1 Human 7.1 pEC50 = 7.1 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 401 7 1 4 4.1 CCCCC(=O)Nc1ccc(S(=O)(=O)N2CCCCC2c2cccnc2)cc1 nan
CHEMBL1319108 21556 8 None - 1 Human 7.1 pEC50 = 7.1 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 401 7 1 4 4.1 CCCCC(=O)Nc1ccc(S(=O)(=O)N2CCCCC2c2cccnc2)cc1 nan
24817704 43038 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 407 7 1 6 3.8 Cc1ccc(OCc2cc(C(=O)NCc3ccc(OC(F)(F)F)cc3)no2)cn1 nan
CHEMBL1506675 43038 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 407 7 1 6 3.8 Cc1ccc(OCc2cc(C(=O)NCc3ccc(OC(F)(F)F)cc3)no2)cn1 nan
23661589 92975 0 None -12589 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 430 9 4 5 4.9 C[C@H](CNc1cccc(-c2sccc2C(=O)O)c1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2007.05.069
CHEMBL245873 92975 0 None -12589 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 430 9 4 5 4.9 C[C@H](CNc1cccc(-c2sccc2C(=O)O)c1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2007.05.069
145987609 166637 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 340 6 5 5 1.8 O=c1ccc2c(C(CO)NCCc3cccc(O)c3)ccc(O)c2[nH]1 10.1016/j.ejmech.2018.04.041
CHEMBL4291538 166637 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 340 6 5 5 1.8 O=c1ccc2c(C(CO)NCCc3cccc(O)c3)ccc(O)c2[nH]1 10.1016/j.ejmech.2018.04.041
54580129 61451 0 None -3 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as stimulation of intracellular cAMP production after 30 mins of washing by wash-off assayAgonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as stimulation of intracellular cAMP production after 30 mins of washing by wash-off assay
ChEMBL 786 21 6 8 7.0 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCCNC(=O)Cc2cccc(CC(C)(C)NC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)c2)ccc1O)C(C)C 10.1016/j.bmcl.2010.10.132
CHEMBL1773197 61451 0 None -3 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as stimulation of intracellular cAMP production after 30 mins of washing by wash-off assayAgonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as stimulation of intracellular cAMP production after 30 mins of washing by wash-off assay
ChEMBL 786 21 6 8 7.0 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCCNC(=O)Cc2cccc(CC(C)(C)NC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)c2)ccc1O)C(C)C 10.1016/j.bmcl.2010.10.132
3224430 35873 6 None - 1 Human 8.1 pEC50 = 8.1 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 425 6 2 6 3.2 O=C(Cn1nc(-c2ccccc2)ccc1=O)Nc1ccc(NC(=O)c2ccccn2)cc1 nan
CHEMBL1444240 35873 6 None - 1 Human 8.1 pEC50 = 8.1 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 425 6 2 6 3.2 O=C(Cn1nc(-c2ccccc2)ccc1=O)Nc1ccc(NC(=O)c2ccccn2)cc1 nan
10484263 58220 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
ChEMBL 639 16 6 6 6.5 O=C(Nc1ccccc1-c1ccccc1)NC1CCN(CCCCCCCCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1016/j.bmcl.2011.01.043
CHEMBL1683940 58220 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
ChEMBL 639 16 6 6 6.5 O=C(Nc1ccccc1-c1ccccc1)NC1CCN(CCCCCCCCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1016/j.bmcl.2011.01.043
667688 85358 4 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assayAgonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assay
ChEMBL 303 6 5 5 2.1 C[C@H](Cc1ccc(O)cc1)NC[C@@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2009.11.062
CHEMBL229477 85358 4 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assayAgonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assay
ChEMBL 303 6 5 5 2.1 C[C@H](Cc1ccc(O)cc1)NC[C@@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2009.11.062
9992825 83937 16 None 125 2 Guinea pig 8.1 pEC50 = 8.1 Functional
Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as relaxation of carbachol-induced tissue contractionAgonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as relaxation of carbachol-induced tissue contraction
ChEMBL 261 2 3 4 1.1 CC(C)NC1CCn2c(=O)[nH]c3cccc(c32)C1O 10.1021/jm801211c
CHEMBL2218907 83937 16 None 125 2 Guinea pig 8.1 pEC50 = 8.1 Functional
Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as relaxation of carbachol-induced tissue contractionAgonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as relaxation of carbachol-induced tissue contraction
ChEMBL 261 2 3 4 1.1 CC(C)NC1CCn2c(=O)[nH]c3cccc(c32)C1O 10.1021/jm801211c
53319789 58221 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
ChEMBL 667 16 5 6 7.1 O=C(Nc1ccccc1-c1ccccc1)O[C@H]1C[N+]2(CCCCCCCCCNCC(O)c3ccc(O)c4[nH]c(=O)ccc34)CCC1CC2 10.1016/j.bmcl.2011.01.043
CHEMBL1683941 58221 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
ChEMBL 667 16 5 6 7.1 O=C(Nc1ccccc1-c1ccccc1)O[C@H]1C[N+]2(CCCCCCCCCNCC(O)c3ccc(O)c4[nH]c(=O)ccc34)CCC1CC2 10.1016/j.bmcl.2011.01.043
10008017 99397 5 None -10 3 Human 7.1 pEC50 = 7.1 Functional
Increased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 2 adrenergic receptorsIncreased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 2 adrenergic receptors
ChEMBL 562 12 6 8 2.3 CC(C)C[C@H](NC(=O)c1ccc(N2CCC(NC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)CC2)cc1)C(=O)O 10.1021/jm000544b
CHEMBL285881 99397 5 None -10 3 Human 7.1 pEC50 = 7.1 Functional
Increased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 2 adrenergic receptorsIncreased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 2 adrenergic receptors
ChEMBL 562 12 6 8 2.3 CC(C)C[C@H](NC(=O)c1ccc(N2CCC(NC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)CC2)cc1)C(=O)O 10.1021/jm000544b
648074 26838 4 None - 1 Human 7.1 pEC50 = 7.1 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 494 7 2 6 3.4 COc1ccc(S(=O)(=O)N2CCCC(C(=O)Nc3ccc(NC(=O)c4ccccn4)cc3)C2)cc1 nan
CHEMBL1365203 26838 4 None - 1 Human 7.1 pEC50 = 7.1 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 494 7 2 6 3.4 COc1ccc(S(=O)(=O)N2CCCC(C(=O)Nc3ccc(NC(=O)c4ccccn4)cc3)C2)cc1 nan
24789201 52153 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 517 12 3 6 3.4 NC(=O)CC(NC(=O)Cc1cccc2ccccc12)c1ccc(NCCCN2CCCC2=O)c([N+](=O)[O-])c1 nan
CHEMBL1590854 52153 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 517 12 3 6 3.4 NC(=O)CC(NC(=O)Cc1cccc2ccccc12)c1ccc(NCCCN2CCCC2=O)c([N+](=O)[O-])c1 nan
4870978 59357 9 None - 1 Human 6.1 pEC50 = 6.1 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 462 7 2 6 3.7 CC(=O)Nc1ccc(S(=O)(=O)N(Cc2cccnc2)Cc2cc3ccccc3nc2O)cc1 nan
CHEMBL1722488 59357 9 None - 1 Human 6.1 pEC50 = 6.1 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 462 7 2 6 3.7 CC(=O)Nc1ccc(S(=O)(=O)N(Cc2cccnc2)Cc2cc3ccccc3nc2O)cc1 nan
998685 33787 14 None -7 3 Human 5.1 pEC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 357 4 1 7 3.3 Cc1ccc(-c2nc(NC(=O)c3nn(C)cc3[N+](=O)[O-])sc2C)cc1 nan
CHEMBL1424697 33787 14 None -7 3 Human 5.1 pEC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 357 4 1 7 3.3 Cc1ccc(-c2nc(NC(=O)c3nn(C)cc3[N+](=O)[O-])sc2C)cc1 nan
667188 40318 11 None 2 2 Human 5.1 pEC50 = 5.1 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory)
ChEMBL 421 6 1 6 5.4 Clc1cccc(-c2nnc(SCc3nc4ccccc4[nH]3)n2Cc2ccco2)c1 nan
CHEMBL1483555 40318 11 None 2 2 Human 5.1 pEC50 = 5.1 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory)
ChEMBL 421 6 1 6 5.4 Clc1cccc(-c2nnc(SCc3nc4ccccc4[nH]3)n2Cc2ccco2)c1 nan
658782 49826 10 None - 1 Human 7.1 pEC50 = 7.1 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 465 4 0 9 1.9 Cn1c(N2CCN(c3ccccn3)CC2)nc2c1c(=O)n(Cc1ccc(Cl)cc1)c(=O)n2C nan
CHEMBL1570111 49826 10 None - 1 Human 7.1 pEC50 = 7.1 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 465 4 0 9 1.9 Cn1c(N2CCN(c3ccccn3)CC2)nc2c1c(=O)n(Cc1ccc(Cl)cc1)c(=O)n2C nan
1480945 50421 13 None - 1 Human 7.1 pEC50 = 7.1 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 345 4 0 5 2.7 Cc1ccc(CS(=O)(=O)c2nc3c(c(N(C)C)n2)CCCC3)cc1 nan
CHEMBL1575889 50421 13 None - 1 Human 7.1 pEC50 = 7.1 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 345 4 0 5 2.7 Cc1ccc(CS(=O)(=O)c2nc3c(c(N(C)C)n2)CCCC3)cc1 nan
2977891 21588 8 None - 1 Human 7.1 pEC50 = 7.1 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 452 5 0 5 1.8 CN(CC(=O)N1CCN(c2ccccn2)CC1)S(=O)(=O)c1ccc(Br)cc1 nan
CHEMBL1319376 21588 8 None - 1 Human 7.1 pEC50 = 7.1 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 452 5 0 5 1.8 CN(CC(=O)N1CCN(c2ccccn2)CC1)S(=O)(=O)c1ccc(Br)cc1 nan
1155 1592 45 None -2 3 Guinea pig 5.1 pEC50 = 5.1 Functional
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contractionAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction
ChEMBL 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 10.1021/jm0704595
3343 1592 45 None -2 3 Guinea pig 5.1 pEC50 = 5.1 Functional
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contractionAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction
ChEMBL 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 10.1021/jm0704595
557 1592 45 None -2 3 Guinea pig 5.1 pEC50 = 5.1 Functional
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contractionAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction
ChEMBL 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 10.1021/jm0704595
CHEMBL32800 1592 45 None -2 3 Guinea pig 5.1 pEC50 = 5.1 Functional
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contractionAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction
ChEMBL 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 10.1021/jm0704595
DB01288 1592 45 None -2 3 Guinea pig 5.1 pEC50 = 5.1 Functional
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contractionAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction
ChEMBL 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 10.1021/jm0704595
1499 2052 43 None -72 36 Human 6.1 pEC50 = 6.1 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C nan
3779 2052 43 None -72 36 Human 6.1 pEC50 = 6.1 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C nan
536 2052 43 None -72 36 Human 6.1 pEC50 = 6.1 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C nan
CHEMBL434 2052 43 None -72 36 Human 6.1 pEC50 = 6.1 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C nan
DB01064 2052 43 None -72 36 Human 6.1 pEC50 = 6.1 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C nan
1499 2052 43 None -72 36 Human 6.1 pEC50 = 6.1 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C nan
3779 2052 43 None -72 36 Human 6.1 pEC50 = 6.1 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C nan
536 2052 43 None -72 36 Human 6.1 pEC50 = 6.1 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C nan
CHEMBL434 2052 43 None -72 36 Human 6.1 pEC50 = 6.1 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C nan
DB01064 2052 43 None -72 36 Human 6.1 pEC50 = 6.1 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C nan
145985242 164982 0 None -75 3 Human 7.1 pEC50 = 7.1 Functional
Antagonist activity at human beta2 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta2 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 443 11 4 4 3.9 O=C(Cc1ccccc1)Nc1ccc(CCNC[C@H](O)COc2cccc3[nH]ccc23)cc1 10.1016/j.ejmech.2018.03.032
CHEMBL4241613 164982 0 None -75 3 Human 7.1 pEC50 = 7.1 Functional
Antagonist activity at human beta2 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta2 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 443 11 4 4 3.9 O=C(Cc1ccccc1)Nc1ccc(CCNC[C@H](O)COc2cccc3[nH]ccc23)cc1 10.1016/j.ejmech.2018.03.032
141286035 192290 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 366 4 3 3 3.6 Nc1c(Br)cc(C(CO)NC2CCCC2)cc1C(F)(F)F 10.1021/acs.jmedchem.1c02006
CHEMBL5190852 192290 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 366 4 3 3 3.6 Nc1c(Br)cc(C(CO)NC2CCCC2)cc1C(F)(F)F 10.1021/acs.jmedchem.1c02006
CHEMBL5222081 192290 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 366 4 3 3 3.6 Nc1c(Br)cc(C(CO)NC2CCCC2)cc1C(F)(F)F 10.1021/acs.jmedchem.1c02006
9266740 30568 8 None - 1 Human 5.1 pEC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 360 3 0 8 3.7 Cn1nnnc1Sc1ncnc2scc(-c3ccc(Cl)cc3)c12 nan
CHEMBL1396351 30568 8 None - 1 Human 5.1 pEC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 360 3 0 8 3.7 Cn1nnnc1Sc1ncnc2scc(-c3ccc(Cl)cc3)c12 nan
1266768 33785 11 None - 1 Human 6.1 pEC50 = 6.1 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 365 6 1 7 2.5 CCOC(=O)c1ccc(NC(=O)Cn2nnc(-c3ccc(C)cc3)n2)cc1 nan
CHEMBL1424678 33785 11 None - 1 Human 6.1 pEC50 = 6.1 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 365 6 1 7 2.5 CCOC(=O)c1ccc(NC(=O)Cn2nnc(-c3ccc(C)cc3)n2)cc1 nan
127046948 139527 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human beta2 receptor expressed in HEK293 cells cotransfected with Gqs5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositolAgonist activity at human beta2 receptor expressed in HEK293 cells cotransfected with Gqs5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositol
ChEMBL 488 12 4 6 4.1 COc1cc(CCNC[C@@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
CHEMBL3800468 139527 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human beta2 receptor expressed in HEK293 cells cotransfected with Gqs5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositolAgonist activity at human beta2 receptor expressed in HEK293 cells cotransfected with Gqs5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositol
ChEMBL 488 12 4 6 4.1 COc1cc(CCNC[C@@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
145983266 164965 0 None -2511 3 Human 5.1 pEC50 = 5.1 Functional
Antagonist activity at human beta2 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta2 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 512 14 5 6 2.7 CC(=O)NCc1cccc(OC[C@@H](O)CNCCc2ccc(NS(=O)(=O)Nc3ccccc3)cc2)c1 10.1016/j.ejmech.2018.03.032
CHEMBL4241176 164965 0 None -2511 3 Human 5.1 pEC50 = 5.1 Functional
Antagonist activity at human beta2 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta2 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 512 14 5 6 2.7 CC(=O)NCc1cccc(OC[C@@H](O)CNCCc2ccc(NS(=O)(=O)Nc3ccccc3)cc2)c1 10.1016/j.ejmech.2018.03.032
31055126 47989 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 404 3 0 8 3.8 Cn1nnnc1Sc1ncnc2scc(-c3ccc(Br)cc3)c12 nan
CHEMBL1553183 47989 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 404 3 0 8 3.8 Cn1nnnc1Sc1ncnc2scc(-c3ccc(Br)cc3)c12 nan
21977117 192320 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 311 3 3 4 2.3 CC(C)(C)NC(CO)c1cc(Br)c(N)c(C#N)c1 10.1021/acs.jmedchem.1c02006
CHEMBL5194651 192320 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 311 3 3 4 2.3 CC(C)(C)NC(CO)c1cc(Br)c(N)c(C#N)c1 10.1021/acs.jmedchem.1c02006
CHEMBL5222287 192320 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 311 3 3 4 2.3 CC(C)(C)NC(CO)c1cc(Br)c(N)c(C#N)c1 10.1021/acs.jmedchem.1c02006
53380559 63295 0 None -4265 2 Rat 5.1 pEC50 = 5.1 Functional
Agonist activity beta2-adrenergic receptor in rat ventricular myocytes assessed as cell contraction following electrical stimulation by optical edge tracking method using photodiode arrayAgonist activity beta2-adrenergic receptor in rat ventricular myocytes assessed as cell contraction following electrical stimulation by optical edge tracking method using photodiode array
ChEMBL 317 7 5 5 2.4 CC[C@H](Cc1ccc(O)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2009.11.062
CHEMBL1800936 63295 0 None -4265 2 Rat 5.1 pEC50 = 5.1 Functional
Agonist activity beta2-adrenergic receptor in rat ventricular myocytes assessed as cell contraction following electrical stimulation by optical edge tracking method using photodiode arrayAgonist activity beta2-adrenergic receptor in rat ventricular myocytes assessed as cell contraction following electrical stimulation by optical edge tracking method using photodiode array
ChEMBL 317 7 5 5 2.4 CC[C@H](Cc1ccc(O)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2009.11.062
24180436 92772 0 None 1 2 Rat 6.1 pEC50 = 6.1 Functional
Vasodilating activity against phenylephrine-induced contraction in rat thoracic aorta in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-oneVasodilating activity against phenylephrine-induced contraction in rat thoracic aorta in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-one
ChEMBL 527 10 4 10 2.6 CC(Cc1ccc(Oc2no[n+]([O-])c2S(=O)(=O)c2ccccc2)cc1)NCC(O)c1cc(O)cc(O)c1 10.1021/jm0704595
CHEMBL244687 92772 0 None 1 2 Rat 6.1 pEC50 = 6.1 Functional
Vasodilating activity against phenylephrine-induced contraction in rat thoracic aorta in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-oneVasodilating activity against phenylephrine-induced contraction in rat thoracic aorta in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-one
ChEMBL 527 10 4 10 2.6 CC(Cc1ccc(Oc2no[n+]([O-])c2S(=O)(=O)c2ccccc2)cc1)NCC(O)c1cc(O)cc(O)c1 10.1021/jm0704595
10103414 76169 13 None -13 3 Guinea pig 4.1 pEC50 = 4.1 Functional
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contractionAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction
ChEMBL 159 2 2 5 -2.1 NC(=O)c1c(CO)no[n+]1[O-] 10.1021/jm0704595
CHEMBL206100 76169 13 None -13 3 Guinea pig 4.1 pEC50 = 4.1 Functional
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contractionAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction
ChEMBL 159 2 2 5 -2.1 NC(=O)c1c(CO)no[n+]1[O-] 10.1021/jm0704595
10103414 76169 13 None -13 3 Guinea pig 4.1 pEC50 = 4.1 Functional
Agonist activity at adrenergic beta2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of propranololAgonist activity at adrenergic beta2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of propranolol
ChEMBL 159 2 2 5 -2.1 NC(=O)c1c(CO)no[n+]1[O-] 10.1021/jm0704595
CHEMBL206100 76169 13 None -13 3 Guinea pig 4.1 pEC50 = 4.1 Functional
Agonist activity at adrenergic beta2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of propranololAgonist activity at adrenergic beta2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of propranolol
ChEMBL 159 2 2 5 -2.1 NC(=O)c1c(CO)no[n+]1[O-] 10.1021/jm0704595
1499 2052 43 None -72 36 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human beta2 receptor expressed in HEK293 cells cotransfected with Gqs5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositolAgonist activity at human beta2 receptor expressed in HEK293 cells cotransfected with Gqs5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositol
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2016.04.028
3779 2052 43 None -72 36 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human beta2 receptor expressed in HEK293 cells cotransfected with Gqs5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositolAgonist activity at human beta2 receptor expressed in HEK293 cells cotransfected with Gqs5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositol
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2016.04.028
536 2052 43 None -72 36 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human beta2 receptor expressed in HEK293 cells cotransfected with Gqs5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositolAgonist activity at human beta2 receptor expressed in HEK293 cells cotransfected with Gqs5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositol
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2016.04.028
CHEMBL434 2052 43 None -72 36 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human beta2 receptor expressed in HEK293 cells cotransfected with Gqs5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositolAgonist activity at human beta2 receptor expressed in HEK293 cells cotransfected with Gqs5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositol
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2016.04.028
DB01064 2052 43 None -72 36 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human beta2 receptor expressed in HEK293 cells cotransfected with Gqs5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositolAgonist activity at human beta2 receptor expressed in HEK293 cells cotransfected with Gqs5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositol
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2016.04.028
141486999 166127 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in CHO-K1 cells harboring Galpha15 assessed as induction of calcium current by FLIPRtetra methodAgonist activity at beta2 adrenoceptor (unknown origin) expressed in CHO-K1 cells harboring Galpha15 assessed as induction of calcium current by FLIPRtetra method
ChEMBL 229 1 2 4 2.1 Oc1cc2c(cc1O)C(c1ccco1)=NCC2 10.1021/acs.jmedchem.0c01195
CHEMBL4282215 166127 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in CHO-K1 cells harboring Galpha15 assessed as induction of calcium current by FLIPRtetra methodAgonist activity at beta2 adrenoceptor (unknown origin) expressed in CHO-K1 cells harboring Galpha15 assessed as induction of calcium current by FLIPRtetra method
ChEMBL 229 1 2 4 2.1 Oc1cc2c(cc1O)C(c1ccco1)=NCC2 10.1021/acs.jmedchem.0c01195
7334649 166693 2 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human beta2-AR expressed in CHOK1 cells co-expressing Galpha15 measured after 21 secs to 120 secs by Calcium-4 dye based FLIPR assayAgonist activity at human beta2-AR expressed in CHOK1 cells co-expressing Galpha15 measured after 21 secs to 120 secs by Calcium-4 dye based FLIPR assay
ChEMBL 255 2 3 3 2.5 Oc1cc2c(cc1O)[C@@H](Cc1ccccc1)NCC2 10.1021/acs.jnatprod.7b00762
CHEMBL4292818 166693 2 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human beta2-AR expressed in CHOK1 cells co-expressing Galpha15 measured after 21 secs to 120 secs by Calcium-4 dye based FLIPR assayAgonist activity at human beta2-AR expressed in CHOK1 cells co-expressing Galpha15 measured after 21 secs to 120 secs by Calcium-4 dye based FLIPR assay
ChEMBL 255 2 3 3 2.5 Oc1cc2c(cc1O)[C@@H](Cc1ccccc1)NCC2 10.1021/acs.jnatprod.7b00762
4968428 24171 7 None - 1 Human 5.1 pEC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 470 9 1 4 4.5 CCN(Cc1ccccc1)S(=O)(=O)c1cc(C(=O)NC(C)C2CC3CCC2C3)ccc1OC nan
CHEMBL1341251 24171 7 None - 1 Human 5.1 pEC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 470 9 1 4 4.5 CCN(Cc1ccccc1)S(=O)(=O)c1cc(C(=O)NC(C)C2CC3CCC2C3)ccc1OC nan
664105 29551 8 None - 1 Human 5.1 pEC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 468 4 1 9 2.8 CC1(C)Cc2c(c(N3CCCC3)nc3sc4c(N5CCN(CCO)CC5)ncnc4c23)CO1 nan
CHEMBL1387056 29551 8 None - 1 Human 5.1 pEC50 = 5.1 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 468 4 1 9 2.8 CC1(C)Cc2c(c(N3CCCC3)nc3sc4c(N5CCN(CCO)CC5)ncnc4c23)CO1 nan
5085262 28352 1 None - 1 Human 7.1 pEC50 = 7.1 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory)
ChEMBL 454 6 1 6 5.8 CC(Oc1ccc(Cl)cc1Cl)c1nc(-c2ccc(NC(=O)c3ccccn3)cc2)no1 nan
CHEMBL1376574 28352 1 None - 1 Human 7.1 pEC50 = 7.1 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory)
ChEMBL 454 6 1 6 5.8 CC(Oc1ccc(Cl)cc1Cl)c1nc(-c2ccc(NC(=O)c3ccccn3)cc2)no1 nan
45484646 195608 0 None 1 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP level
ChEMBL 456 10 6 7 2.0 CC(C)(Cc1ccc(NC(=O)CCCN)cc1)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmcl.2009.06.104
CHEMBL568667 195608 0 None 1 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP level
ChEMBL 456 10 6 7 2.0 CC(C)(Cc1ccc(NC(=O)CCCN)cc1)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmcl.2009.06.104
105 3392 84 None 3 3 Guinea pig 8.0 pEC50 = 8.0 Functional
Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as relaxation of carbachol-induced tissue contractionAgonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as relaxation of carbachol-induced tissue contraction
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1021/jm801211c
2083 3392 84 None 3 3 Guinea pig 8.0 pEC50 = 8.0 Functional
Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as relaxation of carbachol-induced tissue contractionAgonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as relaxation of carbachol-induced tissue contraction
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1021/jm801211c
558 3392 84 None 3 3 Guinea pig 8.0 pEC50 = 8.0 Functional
Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as relaxation of carbachol-induced tissue contractionAgonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as relaxation of carbachol-induced tissue contraction
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1021/jm801211c
CHEMBL714 3392 84 None 3 3 Guinea pig 8.0 pEC50 = 8.0 Functional
Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as relaxation of carbachol-induced tissue contractionAgonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as relaxation of carbachol-induced tissue contraction
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1021/jm801211c
DB01001 3392 84 None 3 3 Guinea pig 8.0 pEC50 = 8.0 Functional
Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as relaxation of carbachol-induced tissue contractionAgonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as relaxation of carbachol-induced tissue contraction
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1021/jm801211c
155550544 173727 0 None 1 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 388 7 4 4 3.6 O=c1ccc2c(C(O)CNCCCc3ccc4ccccc4c3)ccc(O)c2[nH]1 10.1016/j.bmc.2018.10.043
CHEMBL4550290 173727 0 None 1 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 388 7 4 4 3.6 O=c1ccc2c(C(O)CNCCCc3ccc4ccccc4c3)ccc(O)c2[nH]1 10.1016/j.bmc.2018.10.043
44392575 64026 0 None -2 3 Human 8.0 pEC50 = 8.0 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-2 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-2 adrenergic receptor
ChEMBL 441 10 4 6 2.8 C#CCNc1cccc([C@@H](O)CN[C@H](C)Cc2c[nH]c3c(OS(C)(=O)=O)cccc23)c1 10.1016/j.bmcl.2004.12.033
CHEMBL181300 64026 0 None -2 3 Human 8.0 pEC50 = 8.0 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-2 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-2 adrenergic receptor
ChEMBL 441 10 4 6 2.8 C#CCNc1cccc([C@@H](O)CN[C@H](C)Cc2c[nH]c3c(OS(C)(=O)=O)cccc23)c1 10.1016/j.bmcl.2004.12.033
1253647 36843 9 None - 1 Human 8.0 pEC50 = 8.0 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory)
ChEMBL 448 3 0 8 2.6 O=C(c1cc2c(=O)n3ccccc3nc2s1)N1CCN(Cc2ccc3c(c2)OCO3)CC1 nan
CHEMBL1452334 36843 9 None - 1 Human 8.0 pEC50 = 8.0 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory)
ChEMBL 448 3 0 8 2.6 O=C(c1cc2c(=O)n3ccccc3nc2s1)N1CCN(Cc2ccc3c(c2)OCO3)CC1 nan
90666104 108834 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP productionAgonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP production
ChEMBL 682 18 6 9 6.2 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3O)CC2)ccc1O 10.1039/C1MD00140J
CHEMBL3219034 108834 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP productionAgonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP production
ChEMBL 682 18 6 9 6.2 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3O)CC2)ccc1O 10.1039/C1MD00140J
10553603 99224 0 None -8 3 Human 6.1 pEC50 = 6.1 Functional
Increased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 2 adrenergic receptorsIncreased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 2 adrenergic receptors
ChEMBL 506 10 6 8 1.5 CS(=O)(=O)Nc1cc([C@@H](O)CNC2CCN(c3ccc(NC(=O)CC(=O)O)cc3)CC2)ccc1O 10.1021/jm000544b
CHEMBL284612 99224 0 None -8 3 Human 6.1 pEC50 = 6.1 Functional
Increased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 2 adrenergic receptorsIncreased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 2 adrenergic receptors
ChEMBL 506 10 6 8 1.5 CS(=O)(=O)Nc1cc([C@@H](O)CNC2CCN(c3ccc(NC(=O)CC(=O)O)cc3)CC2)ccc1O 10.1021/jm000544b
9889072 164044 0 None - 1 Rat 5.1 pEC50 = 5.1 Functional
Agonist activity at beta2 adrenergic receptor in rat L6 cell lysate assessed as increase in intracellular 2-deoxyglucose uptake preincubated for 4 hrs followed by 2-deoxyglucose addition measured after 20 mins by fluorescence-based enzymatic assay relative to controlAgonist activity at beta2 adrenergic receptor in rat L6 cell lysate assessed as increase in intracellular 2-deoxyglucose uptake preincubated for 4 hrs followed by 2-deoxyglucose addition measured after 20 mins by fluorescence-based enzymatic assay relative to control
ChEMBL 433 5 7 9 -0.3 OC[C@H]1O[C@@H](Oc2ccc(C[C@H]3NCCc4cc(O)c(O)cc43)cc2)[C@H](O)[C@@H](O)[C@@H]1O 10.1016/j.bmc.2017.10.011
CHEMBL4215907 164044 0 None - 1 Rat 5.1 pEC50 = 5.1 Functional
Agonist activity at beta2 adrenergic receptor in rat L6 cell lysate assessed as increase in intracellular 2-deoxyglucose uptake preincubated for 4 hrs followed by 2-deoxyglucose addition measured after 20 mins by fluorescence-based enzymatic assay relative to controlAgonist activity at beta2 adrenergic receptor in rat L6 cell lysate assessed as increase in intracellular 2-deoxyglucose uptake preincubated for 4 hrs followed by 2-deoxyglucose addition measured after 20 mins by fluorescence-based enzymatic assay relative to control
ChEMBL 433 5 7 9 -0.3 OC[C@H]1O[C@@H](Oc2ccc(C[C@H]3NCCc4cc(O)c(O)cc43)cc2)[C@H](O)[C@@H](O)[C@@H]1O 10.1016/j.bmc.2017.10.011
3271684 38908 9 None - 1 Human 7.0 pEC50 = 7.0 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 436 4 1 8 4.9 CC1(C)Cc2c(c(-c3ccco3)nc3sc4c(NCC5CCCO5)ncnc4c23)CO1 nan
CHEMBL1469574 38908 9 None - 1 Human 7.0 pEC50 = 7.0 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 436 4 1 8 4.9 CC1(C)Cc2c(c(-c3ccco3)nc3sc4c(NCC5CCCO5)ncnc4c23)CO1 nan
1371669 37341 10 None 64 2 Human 7.0 pEC50 = 7.0 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 373 5 1 5 4.5 Cc1ccc(OCC(=O)Nc2ccc(-c3nc4ncccc4o3)cc2)c(C)c1 nan
CHEMBL1456621 37341 10 None 64 2 Human 7.0 pEC50 = 7.0 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 373 5 1 5 4.5 Cc1ccc(OCC(=O)Nc2ccc(-c3nc4ncccc4o3)cc2)c(C)c1 nan
44309523 101706 0 None -30 3 Human 6.0 pEC50 = 6.0 Functional
Agonistic activity against cloned human beta1-AR (beta-2-adrenergic receptor) in CHO cellsAgonistic activity against cloned human beta1-AR (beta-2-adrenergic receptor) in CHO cells
ChEMBL 420 10 3 6 2.3 CCCCOc1ccc(S(=O)(=O)N2CC(NC[C@H](O)c3ccc(O)cc3)C2)cc1 10.1016/s0960-894x(03)00387-1
CHEMBL302803 101706 0 None -30 3 Human 6.0 pEC50 = 6.0 Functional
Agonistic activity against cloned human beta1-AR (beta-2-adrenergic receptor) in CHO cellsAgonistic activity against cloned human beta1-AR (beta-2-adrenergic receptor) in CHO cells
ChEMBL 420 10 3 6 2.3 CCCCOc1ccc(S(=O)(=O)N2CC(NC[C@H](O)c3ccc(O)cc3)C2)cc1 10.1016/s0960-894x(03)00387-1
44309272 202171 0 None -181 3 Human 6.0 pEC50 = 6.0 Functional
Agonistic activity against cloned human beta1-AR (beta-2-adrenergic receptor) in CHO cellsAgonistic activity against cloned human beta1-AR (beta-2-adrenergic receptor) in CHO cells
ChEMBL 611 14 6 8 2.9 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)N2CCC(NC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)CC2)cc1 10.1016/s0960-894x(03)00387-1
CHEMBL68766 202171 0 None -181 3 Human 6.0 pEC50 = 6.0 Functional
Agonistic activity against cloned human beta1-AR (beta-2-adrenergic receptor) in CHO cellsAgonistic activity against cloned human beta1-AR (beta-2-adrenergic receptor) in CHO cells
ChEMBL 611 14 6 8 2.9 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)N2CCC(NC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)CC2)cc1 10.1016/s0960-894x(03)00387-1
21977091 192293 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 337 4 3 4 2.9 N#Cc1cc(C(CO)NC2CCCCC2)cc(Br)c1N 10.1021/acs.jmedchem.1c02006
CHEMBL5186459 192293 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 337 4 3 4 2.9 N#Cc1cc(C(CO)NC2CCCCC2)cc(Br)c1N 10.1021/acs.jmedchem.1c02006
CHEMBL5222099 192293 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 337 4 3 4 2.9 N#Cc1cc(C(CO)NC2CCCCC2)cc(Br)c1N 10.1021/acs.jmedchem.1c02006
536369 42383 15 None 1 2 Human 5.0 pEC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 293 1 0 1 4.5 CC(=O)N1c2ccccc2C(C)(c2ccccc2)CC1(C)C nan
CHEMBL1500954 42383 15 None 1 2 Human 5.0 pEC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 293 1 0 1 4.5 CC(=O)N1c2ccccc2C(C)(c2ccccc2)CC1(C)C nan
3238021 45057 7 None 2 2 Human 5.0 pEC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 445 8 1 6 3.3 COc1ccccc1-c1cc(C(F)(F)F)nc(S(=O)(=O)CCCC(=O)NC(C)C)n1 nan
CHEMBL1526751 45057 7 None 2 2 Human 5.0 pEC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 445 8 1 6 3.3 COc1ccccc1-c1cc(C(F)(F)F)nc(S(=O)(=O)CCCC(=O)NC(C)C)n1 nan
24791686 29717 1 None - 1 Human 6.0 pEC50 = 6.0 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 392 6 0 3 4.5 CCc1ccc(CN2CCC(Oc3ccc(C(=O)N4CCCC4)cc3)CC2)cc1 nan
CHEMBL1388401 29717 1 None - 1 Human 6.0 pEC50 = 6.0 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 392 6 0 3 4.5 CCc1ccc(CN2CCC(Oc3ccc(C(=O)N4CCCC4)cc3)CC2)cc1 nan
20954918 23395 5 None - 1 Human 7.0 pEC50 = 7.0 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 382 6 2 4 3.7 CCc1ccc(CNC(=O)c2ccc(NC(=O)C3=CSCCO3)cc2)cc1 nan
CHEMBL1334494 23395 5 None - 1 Human 7.0 pEC50 = 7.0 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 382 6 2 4 3.7 CCc1ccc(CNC(=O)c2ccc(NC(=O)C3=CSCCO3)cc2)cc1 nan
145983355 165237 0 None -85 3 Human 6.0 pEC50 = 6.0 Functional
Antagonist activity at human beta2 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta2 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 454 12 3 5 3.6 CCc1ccccc1OC[C@@H](O)CNCCc1ccc(NS(=O)(=O)c2ccccc2)cc1 10.1016/j.ejmech.2018.03.032
CHEMBL4248093 165237 0 None -85 3 Human 6.0 pEC50 = 6.0 Functional
Antagonist activity at human beta2 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta2 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 454 12 3 5 3.6 CCc1ccccc1OC[C@@H](O)CNCCc1ccc(NS(=O)(=O)c2ccccc2)cc1 10.1016/j.ejmech.2018.03.032
4296505 37565 13 None 1 2 Human 5.0 pEC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 345 5 1 6 2.2 CCCNC(=O)c1nnsc1S(=O)(=O)c1ccc(Cl)cc1 nan
CHEMBL1458548 37565 13 None 1 2 Human 5.0 pEC50 = 5.0 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 345 5 1 6 2.2 CCCNC(=O)c1nnsc1S(=O)(=O)c1ccc(Cl)cc1 nan
46232974 199115 5 None 27 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 386 7 4 6 2.4 COc1ccc(CC(C)(C)NC[C@@H](O)c2cc(O)cc3c2OCC(=O)N3)cc1 10.1016/j.bmcl.2009.12.087
CHEMBL600817 199115 5 None 27 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 386 7 4 6 2.4 COc1ccc(CC(C)(C)NC[C@@H](O)c2cc(O)cc3c2OCC(=O)N3)cc1 10.1016/j.bmcl.2009.12.087
5085262 28352 1 None - 1 Human 6.0 pEC50 = 6.0 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 454 6 1 6 5.8 CC(Oc1ccc(Cl)cc1Cl)c1nc(-c2ccc(NC(=O)c3ccccn3)cc2)no1 nan
CHEMBL1376574 28352 1 None - 1 Human 6.0 pEC50 = 6.0 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 454 6 1 6 5.8 CC(Oc1ccc(Cl)cc1Cl)c1nc(-c2ccc(NC(=O)c3ccccn3)cc2)no1 nan
145983711 164820 0 None -2089 3 Human 5.0 pEC50 = 5.0 Functional
Antagonist activity at human beta2 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta2 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 476 12 5 5 3.5 CC(=O)NCc1cccc(OC[C@@H](O)CNCCc2ccc(NC(=O)Nc3ccccc3)cc2)c1 10.1016/j.ejmech.2018.03.032
CHEMBL4237802 164820 0 None -2089 3 Human 5.0 pEC50 = 5.0 Functional
Antagonist activity at human beta2 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta2 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 476 12 5 5 3.5 CC(=O)NCc1cccc(OC[C@@H](O)CNCCc2ccc(NC(=O)Nc3ccccc3)cc2)c1 10.1016/j.ejmech.2018.03.032
1073012 33485 18 None - 1 Human 6.0 pEC50 = 6.0 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory)
ChEMBL 403 5 0 5 1.3 CCOC(=O)N1CCN(C(=O)CN(C)S(=O)(=O)c2ccc(Cl)cc2)CC1 nan
CHEMBL1422244 33485 18 None - 1 Human 6.0 pEC50 = 6.0 Functional
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory)
ChEMBL 403 5 0 5 1.3 CCOC(=O)N1CCN(C(=O)CN(C)S(=O)(=O)c2ccc(Cl)cc2)CC1 nan
89108754 192297 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 311 6 3 4 2.3 CCCCNC(CO)c1cc(Br)c(N)c(C#N)c1 10.1021/acs.jmedchem.1c02006
CHEMBL5196966 192297 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 311 6 3 4 2.3 CCCCNC(CO)c1cc(Br)c(N)c(C#N)c1 10.1021/acs.jmedchem.1c02006
CHEMBL5222131 192297 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 311 6 3 4 2.3 CCCCNC(CO)c1cc(Br)c(N)c(C#N)c1 10.1021/acs.jmedchem.1c02006
6491897 25343 3 None - 1 Human 6.0 pEC50 = 6 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 444 7 1 5 2.8 O=C(NCCCn1ccnc1)C1CCCN(S(=O)(=O)c2cc(Cl)ccc2Cl)C1 nan
CHEMBL1351178 25343 3 None - 1 Human 6.0 pEC50 = 6 Functional
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 444 7 1 5 2.8 O=C(NCCCn1ccnc1)C1CCCN(S(=O)(=O)c2cc(Cl)ccc2Cl)C1 nan
71093373 191816 0 None - 1 Guinea pig 10.3 pIC50 = 10.3 Functional
Invivo agonist beta2 adrenoceptor activity in Dunkin-Hartley guinea pig trachea assessed as histamine induced contractionInvivo agonist beta2 adrenoceptor activity in Dunkin-Hartley guinea pig trachea assessed as histamine induced contraction
ChEMBL 760 16 5 10 6.0 O=C(NC(c1ccccc1)c1cccc(OCc2ccc(C(=O)OCCCCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
CHEMBL5208201 191816 0 None - 1 Guinea pig 10.3 pIC50 = 10.3 Functional
Invivo agonist beta2 adrenoceptor activity in Dunkin-Hartley guinea pig trachea assessed as histamine induced contractionInvivo agonist beta2 adrenoceptor activity in Dunkin-Hartley guinea pig trachea assessed as histamine induced contraction
ChEMBL 760 16 5 10 6.0 O=C(NC(c1ccccc1)c1cccc(OCc2ccc(C(=O)OCCCCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
12165 896 4 None - 1 Guinea pig 10.1 pIC50 = 10.1 Functional
Invivo agonist beta2 adrenoceptor activity in Dunkin-Hartley guinea pig trachea assessed as histamine induced contractionInvivo agonist beta2 adrenoceptor activity in Dunkin-Hartley guinea pig trachea assessed as histamine induced contraction
ChEMBL 764 16 5 12 4.7 O=C(O[C@@H]1C2CCN(CC2)C1)N[C@@H](c1ccccc1)c1cc(OCc2cc(C(=O)OCCCCNC[C@H](O)c3c4ccc(=O)[nH]c4c(O)cc3)nn2C)ccc1 10.1021/acs.jmedchem.2c00609
90200922 896 4 None - 1 Guinea pig 10.1 pIC50 = 10.1 Functional
Invivo agonist beta2 adrenoceptor activity in Dunkin-Hartley guinea pig trachea assessed as histamine induced contractionInvivo agonist beta2 adrenoceptor activity in Dunkin-Hartley guinea pig trachea assessed as histamine induced contraction
ChEMBL 764 16 5 12 4.7 O=C(O[C@@H]1C2CCN(CC2)C1)N[C@@H](c1ccccc1)c1cc(OCc2cc(C(=O)OCCCCNC[C@H](O)c3c4ccc(=O)[nH]c4c(O)cc3)nn2C)ccc1 10.1021/acs.jmedchem.2c00609
CHEMBL5172865 896 4 None - 1 Guinea pig 10.1 pIC50 = 10.1 Functional
Invivo agonist beta2 adrenoceptor activity in Dunkin-Hartley guinea pig trachea assessed as histamine induced contractionInvivo agonist beta2 adrenoceptor activity in Dunkin-Hartley guinea pig trachea assessed as histamine induced contraction
ChEMBL 764 16 5 12 4.7 O=C(O[C@@H]1C2CCN(CC2)C1)N[C@@H](c1ccccc1)c1cc(OCc2cc(C(=O)OCCCCNC[C@H](O)c3c4ccc(=O)[nH]c4c(O)cc3)nn2C)ccc1 10.1021/acs.jmedchem.2c00609
1499 2052 43 None -85 36 Dog 10.0 pIC50 = 10 Functional
Agonistic activity for Beta-2 adrenergic receptor was assessed by it's inhibitory effect on spontaneous contractions in isolated rat uterusAgonistic activity for Beta-2 adrenergic receptor was assessed by it's inhibitory effect on spontaneous contractions in isolated rat uterus
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm020177z
3779 2052 43 None -85 36 Dog 10.0 pIC50 = 10 Functional
Agonistic activity for Beta-2 adrenergic receptor was assessed by it's inhibitory effect on spontaneous contractions in isolated rat uterusAgonistic activity for Beta-2 adrenergic receptor was assessed by it's inhibitory effect on spontaneous contractions in isolated rat uterus
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm020177z
536 2052 43 None -85 36 Dog 10.0 pIC50 = 10 Functional
Agonistic activity for Beta-2 adrenergic receptor was assessed by it's inhibitory effect on spontaneous contractions in isolated rat uterusAgonistic activity for Beta-2 adrenergic receptor was assessed by it's inhibitory effect on spontaneous contractions in isolated rat uterus
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm020177z
CHEMBL434 2052 43 None -85 36 Dog 10.0 pIC50 = 10 Functional
Agonistic activity for Beta-2 adrenergic receptor was assessed by it's inhibitory effect on spontaneous contractions in isolated rat uterusAgonistic activity for Beta-2 adrenergic receptor was assessed by it's inhibitory effect on spontaneous contractions in isolated rat uterus
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm020177z
DB01064 2052 43 None -85 36 Dog 10.0 pIC50 = 10 Functional
Agonistic activity for Beta-2 adrenergic receptor was assessed by it's inhibitory effect on spontaneous contractions in isolated rat uterusAgonistic activity for Beta-2 adrenergic receptor was assessed by it's inhibitory effect on spontaneous contractions in isolated rat uterus
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm020177z
1499 2052 43 None -85 36 Dog 10.0 pIC50 = 10 Functional
Agonistic activity towards beta-2 adrenoceptor. IC50, the mean concentration required to produce 50% inhibition of uterine contractionAgonistic activity towards beta-2 adrenoceptor. IC50, the mean concentration required to produce 50% inhibition of uterine contraction
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm000455z
3779 2052 43 None -85 36 Dog 10.0 pIC50 = 10 Functional
Agonistic activity towards beta-2 adrenoceptor. IC50, the mean concentration required to produce 50% inhibition of uterine contractionAgonistic activity towards beta-2 adrenoceptor. IC50, the mean concentration required to produce 50% inhibition of uterine contraction
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm000455z
536 2052 43 None -85 36 Dog 10.0 pIC50 = 10 Functional
Agonistic activity towards beta-2 adrenoceptor. IC50, the mean concentration required to produce 50% inhibition of uterine contractionAgonistic activity towards beta-2 adrenoceptor. IC50, the mean concentration required to produce 50% inhibition of uterine contraction
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm000455z
CHEMBL434 2052 43 None -85 36 Dog 10.0 pIC50 = 10 Functional
Agonistic activity towards beta-2 adrenoceptor. IC50, the mean concentration required to produce 50% inhibition of uterine contractionAgonistic activity towards beta-2 adrenoceptor. IC50, the mean concentration required to produce 50% inhibition of uterine contraction
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm000455z
DB01064 2052 43 None -85 36 Dog 10.0 pIC50 = 10 Functional
Agonistic activity towards beta-2 adrenoceptor. IC50, the mean concentration required to produce 50% inhibition of uterine contractionAgonistic activity towards beta-2 adrenoceptor. IC50, the mean concentration required to produce 50% inhibition of uterine contraction
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm000455z
1499 2052 43 None 60 36 Rat 10.0 pIC50 = 10 Functional
Inhibition of spontaneous contractions in isolated rat uterusInhibition of spontaneous contractions in isolated rat uterus
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm020177z
3779 2052 43 None 60 36 Rat 10.0 pIC50 = 10 Functional
Inhibition of spontaneous contractions in isolated rat uterusInhibition of spontaneous contractions in isolated rat uterus
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm020177z
536 2052 43 None 60 36 Rat 10.0 pIC50 = 10 Functional
Inhibition of spontaneous contractions in isolated rat uterusInhibition of spontaneous contractions in isolated rat uterus
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm020177z
CHEMBL434 2052 43 None 60 36 Rat 10.0 pIC50 = 10 Functional
Inhibition of spontaneous contractions in isolated rat uterusInhibition of spontaneous contractions in isolated rat uterus
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm020177z
DB01064 2052 43 None 60 36 Rat 10.0 pIC50 = 10 Functional
Inhibition of spontaneous contractions in isolated rat uterusInhibition of spontaneous contractions in isolated rat uterus
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm020177z
168280960 190244 0 None - 1 Guinea pig 10.0 pIC50 = 10 Functional
Invivo agonist beta2 adrenoceptor activity in Dunkin-Hartley guinea pig trachea assessed as histamine induced contractionInvivo agonist beta2 adrenoceptor activity in Dunkin-Hartley guinea pig trachea assessed as histamine induced contraction
ChEMBL 760 16 5 10 6.0 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2ccc(C(=O)OCCCCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
CHEMBL5184455 190244 0 None - 1 Guinea pig 10.0 pIC50 = 10 Functional
Invivo agonist beta2 adrenoceptor activity in Dunkin-Hartley guinea pig trachea assessed as histamine induced contractionInvivo agonist beta2 adrenoceptor activity in Dunkin-Hartley guinea pig trachea assessed as histamine induced contraction
ChEMBL 760 16 5 10 6.0 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2ccc(C(=O)OCCCCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
90213810 190659 0 None - 1 Guinea pig 9.8 pIC50 = 9.8 Functional
Invivo agonist beta2 adrenoceptor activity in Dunkin-Hartley guinea pig trachea assessed as histamine induced contractionInvivo agonist beta2 adrenoceptor activity in Dunkin-Hartley guinea pig trachea assessed as histamine induced contraction
ChEMBL 750 16 5 11 5.6 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2ccc(C(=O)OCCCCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)o2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
CHEMBL5190387 190659 0 None - 1 Guinea pig 9.8 pIC50 = 9.8 Functional
Invivo agonist beta2 adrenoceptor activity in Dunkin-Hartley guinea pig trachea assessed as histamine induced contractionInvivo agonist beta2 adrenoceptor activity in Dunkin-Hartley guinea pig trachea assessed as histamine induced contraction
ChEMBL 750 16 5 11 5.6 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2ccc(C(=O)OCCCCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)o2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
63952 8487 37 None 2 2 Guinea pig 9.5 pIC50 = 9.5 Functional
Agonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response after 30 minsAgonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response after 30 mins
ChEMBL 368 7 4 5 2.5 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1 10.1021/jm100068m
86306667 8487 37 None 2 2 Guinea pig 9.5 pIC50 = 9.5 Functional
Agonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response after 30 minsAgonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response after 30 mins
ChEMBL 368 7 4 5 2.5 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1 10.1021/jm100068m
CHEMBL1094785 8487 37 None 2 2 Guinea pig 9.5 pIC50 = 9.5 Functional
Agonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response after 30 minsAgonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response after 30 mins
ChEMBL 368 7 4 5 2.5 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1 10.1021/jm100068m
168287036 190900 0 None - 1 Guinea pig 9.4 pIC50 = 9.4 Functional
Invivo agonist beta2 adrenoceptor activity in Dunkin-Hartley guinea pig trachea assessed as histamine induced contractionInvivo agonist beta2 adrenoceptor activity in Dunkin-Hartley guinea pig trachea assessed as histamine induced contraction
ChEMBL 760 16 5 10 6.0 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2cccc(C(=O)OCCCCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
CHEMBL5193853 190900 0 None - 1 Guinea pig 9.4 pIC50 = 9.4 Functional
Invivo agonist beta2 adrenoceptor activity in Dunkin-Hartley guinea pig trachea assessed as histamine induced contractionInvivo agonist beta2 adrenoceptor activity in Dunkin-Hartley guinea pig trachea assessed as histamine induced contraction
ChEMBL 760 16 5 10 6.0 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2cccc(C(=O)OCCCCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
168296356 191877 0 None - 1 Guinea pig 9.4 pIC50 = 9.4 Functional
Invivo agonist beta2 adrenoceptor activity in Dunkin-Hartley guinea pig trachea assessed as histamine induced contractionInvivo agonist beta2 adrenoceptor activity in Dunkin-Hartley guinea pig trachea assessed as histamine induced contraction
ChEMBL 751 16 5 12 5.0 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2nc(C(=O)OCCCCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)co2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
CHEMBL5208957 191877 0 None - 1 Guinea pig 9.4 pIC50 = 9.4 Functional
Invivo agonist beta2 adrenoceptor activity in Dunkin-Hartley guinea pig trachea assessed as histamine induced contractionInvivo agonist beta2 adrenoceptor activity in Dunkin-Hartley guinea pig trachea assessed as histamine induced contraction
ChEMBL 751 16 5 12 5.0 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2nc(C(=O)OCCCCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)co2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
1239 1639 46 None -1 5 Guinea pig 9.4 pIC50 = 9.4 Functional
Agonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response after 30 minsAgonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response after 30 mins
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1021/jm100068m
3410 1639 46 None -1 5 Guinea pig 9.4 pIC50 = 9.4 Functional
Agonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response after 30 minsAgonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response after 30 mins
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1021/jm100068m
3465 1639 46 None -1 5 Guinea pig 9.4 pIC50 = 9.4 Functional
Agonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response after 30 minsAgonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response after 30 mins
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1021/jm100068m
CHEMBL1256786 1639 46 None -1 5 Guinea pig 9.4 pIC50 = 9.4 Functional
Agonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response after 30 minsAgonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response after 30 mins
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1021/jm100068m
DB00983 1639 46 None -1 5 Guinea pig 9.4 pIC50 = 9.4 Functional
Agonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response after 30 minsAgonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response after 30 mins
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1021/jm100068m
165193 3126 60 None 6 13 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at ADRB2 endogenously expressed in HEK293 cells transfected with cAMP FRET biosensor assessed as inhibition of cimaterol-induced response pre-incubated for 45 mins under constant violet light conditions by FRET assayAntagonist activity at ADRB2 endogenously expressed in HEK293 cells transfected with cAMP FRET biosensor assessed as inhibition of cimaterol-induced response pre-incubated for 45 mins under constant violet light conditions by FRET assay
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/acs.jmedchem.0c00831
2303 3126 60 None 6 13 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at ADRB2 endogenously expressed in HEK293 cells transfected with cAMP FRET biosensor assessed as inhibition of cimaterol-induced response pre-incubated for 45 mins under constant violet light conditions by FRET assayAntagonist activity at ADRB2 endogenously expressed in HEK293 cells transfected with cAMP FRET biosensor assessed as inhibition of cimaterol-induced response pre-incubated for 45 mins under constant violet light conditions by FRET assay
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/acs.jmedchem.0c00831
4946 3126 60 None 6 13 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at ADRB2 endogenously expressed in HEK293 cells transfected with cAMP FRET biosensor assessed as inhibition of cimaterol-induced response pre-incubated for 45 mins under constant violet light conditions by FRET assayAntagonist activity at ADRB2 endogenously expressed in HEK293 cells transfected with cAMP FRET biosensor assessed as inhibition of cimaterol-induced response pre-incubated for 45 mins under constant violet light conditions by FRET assay
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/acs.jmedchem.0c00831
564 3126 60 None 6 13 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at ADRB2 endogenously expressed in HEK293 cells transfected with cAMP FRET biosensor assessed as inhibition of cimaterol-induced response pre-incubated for 45 mins under constant violet light conditions by FRET assayAntagonist activity at ADRB2 endogenously expressed in HEK293 cells transfected with cAMP FRET biosensor assessed as inhibition of cimaterol-induced response pre-incubated for 45 mins under constant violet light conditions by FRET assay
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/acs.jmedchem.0c00831
62882 3126 60 None 6 13 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at ADRB2 endogenously expressed in HEK293 cells transfected with cAMP FRET biosensor assessed as inhibition of cimaterol-induced response pre-incubated for 45 mins under constant violet light conditions by FRET assayAntagonist activity at ADRB2 endogenously expressed in HEK293 cells transfected with cAMP FRET biosensor assessed as inhibition of cimaterol-induced response pre-incubated for 45 mins under constant violet light conditions by FRET assay
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/acs.jmedchem.0c00831
63 3126 60 None 6 13 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at ADRB2 endogenously expressed in HEK293 cells transfected with cAMP FRET biosensor assessed as inhibition of cimaterol-induced response pre-incubated for 45 mins under constant violet light conditions by FRET assayAntagonist activity at ADRB2 endogenously expressed in HEK293 cells transfected with cAMP FRET biosensor assessed as inhibition of cimaterol-induced response pre-incubated for 45 mins under constant violet light conditions by FRET assay
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/acs.jmedchem.0c00831
66366 3126 60 None 6 13 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at ADRB2 endogenously expressed in HEK293 cells transfected with cAMP FRET biosensor assessed as inhibition of cimaterol-induced response pre-incubated for 45 mins under constant violet light conditions by FRET assayAntagonist activity at ADRB2 endogenously expressed in HEK293 cells transfected with cAMP FRET biosensor assessed as inhibition of cimaterol-induced response pre-incubated for 45 mins under constant violet light conditions by FRET assay
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/acs.jmedchem.0c00831
91536 3126 60 None 6 13 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at ADRB2 endogenously expressed in HEK293 cells transfected with cAMP FRET biosensor assessed as inhibition of cimaterol-induced response pre-incubated for 45 mins under constant violet light conditions by FRET assayAntagonist activity at ADRB2 endogenously expressed in HEK293 cells transfected with cAMP FRET biosensor assessed as inhibition of cimaterol-induced response pre-incubated for 45 mins under constant violet light conditions by FRET assay
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/acs.jmedchem.0c00831
CHEMBL27 3126 60 None 6 13 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at ADRB2 endogenously expressed in HEK293 cells transfected with cAMP FRET biosensor assessed as inhibition of cimaterol-induced response pre-incubated for 45 mins under constant violet light conditions by FRET assayAntagonist activity at ADRB2 endogenously expressed in HEK293 cells transfected with cAMP FRET biosensor assessed as inhibition of cimaterol-induced response pre-incubated for 45 mins under constant violet light conditions by FRET assay
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/acs.jmedchem.0c00831
CHEMBL452861 3126 60 None 6 13 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at ADRB2 endogenously expressed in HEK293 cells transfected with cAMP FRET biosensor assessed as inhibition of cimaterol-induced response pre-incubated for 45 mins under constant violet light conditions by FRET assayAntagonist activity at ADRB2 endogenously expressed in HEK293 cells transfected with cAMP FRET biosensor assessed as inhibition of cimaterol-induced response pre-incubated for 45 mins under constant violet light conditions by FRET assay
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/acs.jmedchem.0c00831
DB00571 3126 60 None 6 13 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at ADRB2 endogenously expressed in HEK293 cells transfected with cAMP FRET biosensor assessed as inhibition of cimaterol-induced response pre-incubated for 45 mins under constant violet light conditions by FRET assayAntagonist activity at ADRB2 endogenously expressed in HEK293 cells transfected with cAMP FRET biosensor assessed as inhibition of cimaterol-induced response pre-incubated for 45 mins under constant violet light conditions by FRET assay
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/acs.jmedchem.0c00831
168279881 190258 0 None - 1 Guinea pig 9.3 pIC50 = 9.3 Functional
Invivo agonist beta2 adrenoceptor activity in Dunkin-Hartley guinea pig trachea assessed as histamine induced contractionInvivo agonist beta2 adrenoceptor activity in Dunkin-Hartley guinea pig trachea assessed as histamine induced contraction
ChEMBL 760 16 5 10 6.0 O=C(N[C@H](c1ccccc1)c1cccc(OCc2ccc(C(=O)OCCCCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
CHEMBL5184598 190258 0 None - 1 Guinea pig 9.3 pIC50 = 9.3 Functional
Invivo agonist beta2 adrenoceptor activity in Dunkin-Hartley guinea pig trachea assessed as histamine induced contractionInvivo agonist beta2 adrenoceptor activity in Dunkin-Hartley guinea pig trachea assessed as histamine induced contraction
ChEMBL 760 16 5 10 6.0 O=C(N[C@H](c1ccccc1)c1cccc(OCc2ccc(C(=O)OCCCCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
165193 3126 60 None 6 13 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at ADRB2 endogenously expressed in HEK293 cells transfected with cAMP FRET biosensor assessed as inhibition of cimaterol-induced response pre-incubated for 45 mins under dark conditions by FRET assayAntagonist activity at ADRB2 endogenously expressed in HEK293 cells transfected with cAMP FRET biosensor assessed as inhibition of cimaterol-induced response pre-incubated for 45 mins under dark conditions by FRET assay
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/acs.jmedchem.0c00831
2303 3126 60 None 6 13 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at ADRB2 endogenously expressed in HEK293 cells transfected with cAMP FRET biosensor assessed as inhibition of cimaterol-induced response pre-incubated for 45 mins under dark conditions by FRET assayAntagonist activity at ADRB2 endogenously expressed in HEK293 cells transfected with cAMP FRET biosensor assessed as inhibition of cimaterol-induced response pre-incubated for 45 mins under dark conditions by FRET assay
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/acs.jmedchem.0c00831
4946 3126 60 None 6 13 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at ADRB2 endogenously expressed in HEK293 cells transfected with cAMP FRET biosensor assessed as inhibition of cimaterol-induced response pre-incubated for 45 mins under dark conditions by FRET assayAntagonist activity at ADRB2 endogenously expressed in HEK293 cells transfected with cAMP FRET biosensor assessed as inhibition of cimaterol-induced response pre-incubated for 45 mins under dark conditions by FRET assay
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/acs.jmedchem.0c00831
564 3126 60 None 6 13 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at ADRB2 endogenously expressed in HEK293 cells transfected with cAMP FRET biosensor assessed as inhibition of cimaterol-induced response pre-incubated for 45 mins under dark conditions by FRET assayAntagonist activity at ADRB2 endogenously expressed in HEK293 cells transfected with cAMP FRET biosensor assessed as inhibition of cimaterol-induced response pre-incubated for 45 mins under dark conditions by FRET assay
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/acs.jmedchem.0c00831
62882 3126 60 None 6 13 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at ADRB2 endogenously expressed in HEK293 cells transfected with cAMP FRET biosensor assessed as inhibition of cimaterol-induced response pre-incubated for 45 mins under dark conditions by FRET assayAntagonist activity at ADRB2 endogenously expressed in HEK293 cells transfected with cAMP FRET biosensor assessed as inhibition of cimaterol-induced response pre-incubated for 45 mins under dark conditions by FRET assay
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/acs.jmedchem.0c00831
63 3126 60 None 6 13 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at ADRB2 endogenously expressed in HEK293 cells transfected with cAMP FRET biosensor assessed as inhibition of cimaterol-induced response pre-incubated for 45 mins under dark conditions by FRET assayAntagonist activity at ADRB2 endogenously expressed in HEK293 cells transfected with cAMP FRET biosensor assessed as inhibition of cimaterol-induced response pre-incubated for 45 mins under dark conditions by FRET assay
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/acs.jmedchem.0c00831
66366 3126 60 None 6 13 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at ADRB2 endogenously expressed in HEK293 cells transfected with cAMP FRET biosensor assessed as inhibition of cimaterol-induced response pre-incubated for 45 mins under dark conditions by FRET assayAntagonist activity at ADRB2 endogenously expressed in HEK293 cells transfected with cAMP FRET biosensor assessed as inhibition of cimaterol-induced response pre-incubated for 45 mins under dark conditions by FRET assay
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/acs.jmedchem.0c00831
91536 3126 60 None 6 13 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at ADRB2 endogenously expressed in HEK293 cells transfected with cAMP FRET biosensor assessed as inhibition of cimaterol-induced response pre-incubated for 45 mins under dark conditions by FRET assayAntagonist activity at ADRB2 endogenously expressed in HEK293 cells transfected with cAMP FRET biosensor assessed as inhibition of cimaterol-induced response pre-incubated for 45 mins under dark conditions by FRET assay
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/acs.jmedchem.0c00831
CHEMBL27 3126 60 None 6 13 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at ADRB2 endogenously expressed in HEK293 cells transfected with cAMP FRET biosensor assessed as inhibition of cimaterol-induced response pre-incubated for 45 mins under dark conditions by FRET assayAntagonist activity at ADRB2 endogenously expressed in HEK293 cells transfected with cAMP FRET biosensor assessed as inhibition of cimaterol-induced response pre-incubated for 45 mins under dark conditions by FRET assay
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/acs.jmedchem.0c00831
CHEMBL452861 3126 60 None 6 13 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at ADRB2 endogenously expressed in HEK293 cells transfected with cAMP FRET biosensor assessed as inhibition of cimaterol-induced response pre-incubated for 45 mins under dark conditions by FRET assayAntagonist activity at ADRB2 endogenously expressed in HEK293 cells transfected with cAMP FRET biosensor assessed as inhibition of cimaterol-induced response pre-incubated for 45 mins under dark conditions by FRET assay
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/acs.jmedchem.0c00831
DB00571 3126 60 None 6 13 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at ADRB2 endogenously expressed in HEK293 cells transfected with cAMP FRET biosensor assessed as inhibition of cimaterol-induced response pre-incubated for 45 mins under dark conditions by FRET assayAntagonist activity at ADRB2 endogenously expressed in HEK293 cells transfected with cAMP FRET biosensor assessed as inhibition of cimaterol-induced response pre-incubated for 45 mins under dark conditions by FRET assay
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/acs.jmedchem.0c00831
204665 10125 9 None 4 2 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) expressed in HEK293 cell assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 15 minsAntagonist activity at beta2 adrenergic receptor (unknown origin) expressed in HEK293 cell assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 15 mins
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
CHEMBL1160734 10125 9 None 4 2 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) expressed in HEK293 cell assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 15 minsAntagonist activity at beta2 adrenergic receptor (unknown origin) expressed in HEK293 cell assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 15 mins
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
168290830 191348 0 None - 1 Guinea pig 9.1 pIC50 = 9.1 Functional
Invivo agonist beta2 adrenoceptor activity in Dunkin-Hartley guinea pig trachea assessed as histamine induced contractionInvivo agonist beta2 adrenoceptor activity in Dunkin-Hartley guinea pig trachea assessed as histamine induced contraction
ChEMBL 790 17 5 11 6.0 COc1cc(C(=O)OCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1COc1cccc([C@@H](NC(=O)O[C@H]2CN3CCC2CC3)c2ccccc2)c1 10.1021/acs.jmedchem.2c00609
CHEMBL5200887 191348 0 None - 1 Guinea pig 9.1 pIC50 = 9.1 Functional
Invivo agonist beta2 adrenoceptor activity in Dunkin-Hartley guinea pig trachea assessed as histamine induced contractionInvivo agonist beta2 adrenoceptor activity in Dunkin-Hartley guinea pig trachea assessed as histamine induced contraction
ChEMBL 790 17 5 11 6.0 COc1cc(C(=O)OCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1COc1cccc([C@@H](NC(=O)O[C@H]2CN3CCC2CC3)c2ccccc2)c1 10.1021/acs.jmedchem.2c00609
46221395 8429 0 None 6 2 Guinea pig 9.1 pIC50 = 9.1 Functional
Agonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response after 30 minsAgonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response after 30 mins
ChEMBL 336 4 4 4 2.0 O=c1ccc2c([C@@H](O)CNC3Cc4ccccc4C3)ccc(O)c2[nH]1 10.1021/jm100068m
CHEMBL1094323 8429 0 None 6 2 Guinea pig 9.1 pIC50 = 9.1 Functional
Agonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response after 30 minsAgonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response after 30 mins
ChEMBL 336 4 4 4 2.0 O=c1ccc2c([C@@H](O)CNC3Cc4ccccc4C3)ccc(O)c2[nH]1 10.1021/jm100068m
137 367 47 None 1 4 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) expressed in HEK293 cell assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 15 minsAntagonist activity at beta2 adrenergic receptor (unknown origin) expressed in HEK293 cell assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 15 mins
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1021/acs.jmedchem.9b00595
2119 367 47 None 1 4 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) expressed in HEK293 cell assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 15 minsAntagonist activity at beta2 adrenergic receptor (unknown origin) expressed in HEK293 cell assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 15 mins
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1021/acs.jmedchem.9b00595
563 367 47 None 1 4 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) expressed in HEK293 cell assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 15 minsAntagonist activity at beta2 adrenergic receptor (unknown origin) expressed in HEK293 cell assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 15 mins
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1021/acs.jmedchem.9b00595
66368 367 47 None 1 4 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) expressed in HEK293 cell assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 15 minsAntagonist activity at beta2 adrenergic receptor (unknown origin) expressed in HEK293 cell assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 15 mins
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1021/acs.jmedchem.9b00595
CHEMBL266195 367 47 None 1 4 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) expressed in HEK293 cell assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 15 minsAntagonist activity at beta2 adrenergic receptor (unknown origin) expressed in HEK293 cell assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 15 mins
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1021/acs.jmedchem.9b00595
DB00866 367 47 None 1 4 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) expressed in HEK293 cell assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 15 minsAntagonist activity at beta2 adrenergic receptor (unknown origin) expressed in HEK293 cell assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 15 mins
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1021/acs.jmedchem.9b00595
155539613 172268 0 None 2 2 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) expressed in HEK293 cell assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 15 minsAntagonist activity at beta2 adrenergic receptor (unknown origin) expressed in HEK293 cell assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 15 mins
ChEMBL 677 24 5 13 2.9 CC(C)NC[C@H](O)COc1ccccc1CCCn1cc(CNCc2cn(CCCc3ccccc3OC[C@@H](O)CNC(C)C)nn2)nn1 10.1021/acs.jmedchem.9b00595
CHEMBL4514723 172268 0 None 2 2 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) expressed in HEK293 cell assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 15 minsAntagonist activity at beta2 adrenergic receptor (unknown origin) expressed in HEK293 cell assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 15 mins
ChEMBL 677 24 5 13 2.9 CC(C)NC[C@H](O)COc1ccccc1CCCn1cc(CNCc2cn(CCCc3ccccc3OC[C@@H](O)CNC(C)C)nn2)nn1 10.1021/acs.jmedchem.9b00595
155569481 175632 0 None 8 2 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) expressed in HEK293 cell assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 15 minsAntagonist activity at beta2 adrenergic receptor (unknown origin) expressed in HEK293 cell assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 15 mins
ChEMBL 614 23 6 8 2.7 CC(C)NC[C@H](O)COc1ccccc1CCCC(=O)NCCNC(=O)CCCc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
CHEMBL4594173 175632 0 None 8 2 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) expressed in HEK293 cell assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 15 minsAntagonist activity at beta2 adrenergic receptor (unknown origin) expressed in HEK293 cell assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 15 mins
ChEMBL 614 23 6 8 2.7 CC(C)NC[C@H](O)COc1ccccc1CCCC(=O)NCCNC(=O)CCCc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
155518547 169712 0 None 107 2 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) expressed in HEK293 cell assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 15 minsAntagonist activity at beta2 adrenergic receptor (unknown origin) expressed in HEK293 cell assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 15 mins
ChEMBL 558 20 6 7 3.0 CC(C)NC[C@H](O)COc1ccccc1CCCNC(=O)NCCCc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
CHEMBL4446394 169712 0 None 107 2 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) expressed in HEK293 cell assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 15 minsAntagonist activity at beta2 adrenergic receptor (unknown origin) expressed in HEK293 cell assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 15 mins
ChEMBL 558 20 6 7 3.0 CC(C)NC[C@H](O)COc1ccccc1CCCNC(=O)NCCCc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
155559960 174312 0 None 8 2 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assayAntagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assay
ChEMBL 586 22 6 7 3.8 CC(C)NC[C@H](O)COc1ccccc1CCCCNC(=O)NCCCCc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
CHEMBL4564189 174312 0 None 8 2 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assayAntagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assay
ChEMBL 586 22 6 7 3.8 CC(C)NC[C@H](O)COc1ccccc1CCCCNC(=O)NCCCCc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
156010391 176542 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at ADRB2 endogenously expressed in HEK293 cells transfected with cAMP FRET biosensor assessed as inhibition of cimaterol-induced response pre-incubated for 45 mins under dark conditions by FRET assayAntagonist activity at ADRB2 endogenously expressed in HEK293 cells transfected with cAMP FRET biosensor assessed as inhibition of cimaterol-induced response pre-incubated for 45 mins under dark conditions by FRET assay
ChEMBL 370 9 3 6 3.8 CC(=O)Nc1ccc(/N=N/c2ccccc2OC[C@@H](O)CNC(C)C)cc1 10.1021/acs.jmedchem.0c00831
CHEMBL4633760 176542 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at ADRB2 endogenously expressed in HEK293 cells transfected with cAMP FRET biosensor assessed as inhibition of cimaterol-induced response pre-incubated for 45 mins under dark conditions by FRET assayAntagonist activity at ADRB2 endogenously expressed in HEK293 cells transfected with cAMP FRET biosensor assessed as inhibition of cimaterol-induced response pre-incubated for 45 mins under dark conditions by FRET assay
ChEMBL 370 9 3 6 3.8 CC(=O)Nc1ccc(/N=N/c2ccccc2OC[C@@H](O)CNC(C)C)cc1 10.1021/acs.jmedchem.0c00831
155530927 171021 0 None 3 2 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assayAntagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assay
ChEMBL 614 24 6 7 4.6 CC(C)NC[C@H](O)COc1ccccc1CCCCCNC(=O)NCCCCCc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
CHEMBL4465278 171021 0 None 3 2 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assayAntagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assay
ChEMBL 614 24 6 7 4.6 CC(C)NC[C@H](O)COc1ccccc1CCCCCNC(=O)NCCCCCc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
155559960 174312 0 None 8 2 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) expressed in HEK293 cell assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 15 minsAntagonist activity at beta2 adrenergic receptor (unknown origin) expressed in HEK293 cell assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 15 mins
ChEMBL 586 22 6 7 3.8 CC(C)NC[C@H](O)COc1ccccc1CCCCNC(=O)NCCCCc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
CHEMBL4564189 174312 0 None 8 2 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) expressed in HEK293 cell assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 15 minsAntagonist activity at beta2 adrenergic receptor (unknown origin) expressed in HEK293 cell assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 15 mins
ChEMBL 586 22 6 7 3.8 CC(C)NC[C@H](O)COc1ccccc1CCCCNC(=O)NCCCCc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
127034967 135952 0 None 1 3 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human beta2 receptor expressed in CHO-K1 cells assessed as isoproterenol-induced cAMP level by HTRF assayAntagonist activity at human beta2 receptor expressed in CHO-K1 cells assessed as isoproterenol-induced cAMP level by HTRF assay
ChEMBL 260 5 2 4 1.6 CB1C=Cc2c(cccc2OCC(O)CN(C)C)N1 10.1021/acs.jmedchem.5b01088
CHEMBL3736156 135952 0 None 1 3 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human beta2 receptor expressed in CHO-K1 cells assessed as isoproterenol-induced cAMP level by HTRF assayAntagonist activity at human beta2 receptor expressed in CHO-K1 cells assessed as isoproterenol-induced cAMP level by HTRF assay
ChEMBL 260 5 2 4 1.6 CB1C=Cc2c(cccc2OCC(O)CN(C)C)N1 10.1021/acs.jmedchem.5b01088
24936881 17320 0 None -173 3 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as inhibition of isoproterenol-induced cyclic AMP formation by HTRF assayAntagonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as inhibition of isoproterenol-induced cyclic AMP formation by HTRF assay
ChEMBL 476 8 3 8 4.1 Oc1cccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)c1 10.1016/j.bmcl.2010.08.039
CHEMBL1257913 17320 0 None -173 3 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as inhibition of isoproterenol-induced cyclic AMP formation by HTRF assayAntagonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as inhibition of isoproterenol-induced cyclic AMP formation by HTRF assay
ChEMBL 476 8 3 8 4.1 Oc1cccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)c1 10.1016/j.bmcl.2010.08.039
10690668 120075 0 None -478 2 Rat 5.0 pIC50 = 5.0 Functional
Agonistic activity towards beta-2 adrenoceptor. Mean concentration required to produce 50% inhibition of uterine contractionAgonistic activity towards beta-2 adrenoceptor. Mean concentration required to produce 50% inhibition of uterine contraction
ChEMBL 372 9 5 5 2.9 C[C@H](NCCc1ccc(NC(C)(C)C(=O)O)cc1)[C@H](O)c1ccc(O)cc1 10.1021/jm000455z
CHEMBL35459 120075 0 None -478 2 Rat 5.0 pIC50 = 5.0 Functional
Agonistic activity towards beta-2 adrenoceptor. Mean concentration required to produce 50% inhibition of uterine contractionAgonistic activity towards beta-2 adrenoceptor. Mean concentration required to produce 50% inhibition of uterine contraction
ChEMBL 372 9 5 5 2.9 C[C@H](NCCc1ccc(NC(C)(C)C(=O)O)cc1)[C@H](O)c1ccc(O)cc1 10.1021/jm000455z
155535986 171525 0 None 16 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assayAntagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assay
ChEMBL 642 25 6 8 3.5 CC(C)NC[C@H](O)COc1ccccc1CCCC(=O)NCCCCNC(=O)CCCc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
CHEMBL4472564 171525 0 None 16 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assayAntagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assay
ChEMBL 642 25 6 8 3.5 CC(C)NC[C@H](O)COc1ccccc1CCCC(=O)NCCCCNC(=O)CCCc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
155545790 172903 0 None 79 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) expressed in HEK293 cell assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 15 minsAntagonist activity at beta2 adrenergic receptor (unknown origin) expressed in HEK293 cell assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 15 mins
ChEMBL 593 18 5 13 1.6 CC(C)NC[C@H](O)COc1ccccc1-n1cc(CNCc2cn(-c3ccccc3OC[C@@H](O)CNC(C)C)nn2)nn1 10.1021/acs.jmedchem.9b00595
CHEMBL4530266 172903 0 None 79 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) expressed in HEK293 cell assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 15 minsAntagonist activity at beta2 adrenergic receptor (unknown origin) expressed in HEK293 cell assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 15 mins
ChEMBL 593 18 5 13 1.6 CC(C)NC[C@H](O)COc1ccccc1-n1cc(CNCc2cn(-c3ccccc3OC[C@@H](O)CNC(C)C)nn2)nn1 10.1021/acs.jmedchem.9b00595
46889771 6901 0 None -1 3 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human adrenergic beta2 receptor expressed in CHOK1 cells assessed as inhibition of cAMP accumulation by HTRF assayAntagonist activity at human adrenergic beta2 receptor expressed in CHOK1 cells assessed as inhibition of cAMP accumulation by HTRF assay
ChEMBL 549 7 3 6 4.9 O=C1c2cccc3cc(O)cc(c23)C(=O)N1CC1CCN(CC(O)COc2cccc3[nH]c4ccccc4c23)CC1 10.1016/j.bmcl.2010.04.009
CHEMBL1084706 6901 0 None -1 3 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human adrenergic beta2 receptor expressed in CHOK1 cells assessed as inhibition of cAMP accumulation by HTRF assayAntagonist activity at human adrenergic beta2 receptor expressed in CHOK1 cells assessed as inhibition of cAMP accumulation by HTRF assay
ChEMBL 549 7 3 6 4.9 O=C1c2cccc3cc(O)cc(c23)C(=O)N1CC1CCN(CC(O)COc2cccc3[nH]c4ccccc4c23)CC1 10.1016/j.bmcl.2010.04.009
52948056 17322 0 None -18 3 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as inhibition of isoproterenol-induced cyclic AMP formation by HTRF assayAntagonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as inhibition of isoproterenol-induced cyclic AMP formation by HTRF assay
ChEMBL 478 8 2 7 4.5 OC(CNC1CCN(c2ncnc3scc(-c4ccc(F)cc4)c23)CC1)COc1ccccc1 10.1016/j.bmcl.2010.08.039
CHEMBL1257915 17322 0 None -18 3 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as inhibition of isoproterenol-induced cyclic AMP formation by HTRF assayAntagonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as inhibition of isoproterenol-induced cyclic AMP formation by HTRF assay
ChEMBL 478 8 2 7 4.5 OC(CNC1CCN(c2ncnc3scc(-c4ccc(F)cc4)c23)CC1)COc1ccccc1 10.1016/j.bmcl.2010.08.039
52943968 17597 0 None -11 3 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as inhibition of isoproterenol-induced cyclic AMP formation by HTRF assayAntagonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as inhibition of isoproterenol-induced cyclic AMP formation by HTRF assay
ChEMBL 518 9 4 8 3.8 NC(=O)Nc1cccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)c1 10.1016/j.bmcl.2010.08.039
CHEMBL1258824 17597 0 None -11 3 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as inhibition of isoproterenol-induced cyclic AMP formation by HTRF assayAntagonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as inhibition of isoproterenol-induced cyclic AMP formation by HTRF assay
ChEMBL 518 9 4 8 3.8 NC(=O)Nc1cccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)c1 10.1016/j.bmcl.2010.08.039
10573759 99205 0 None -20 2 Rat 5.9 pIC50 = 5.9 Functional
Agonistic activity towards beta-2 adrenoceptor. Mean concentration required to produce 50% inhibition of uterine contractionAgonistic activity towards beta-2 adrenoceptor. Mean concentration required to produce 50% inhibition of uterine contraction
ChEMBL 412 9 5 5 3.5 C[C@H](NCCc1cc(Cl)c(NCC(=O)O)cc1Cl)[C@H](O)c1ccc(O)cc1 10.1021/jm000455z
CHEMBL284520 99205 0 None -20 2 Rat 5.9 pIC50 = 5.9 Functional
Agonistic activity towards beta-2 adrenoceptor. Mean concentration required to produce 50% inhibition of uterine contractionAgonistic activity towards beta-2 adrenoceptor. Mean concentration required to produce 50% inhibition of uterine contraction
ChEMBL 412 9 5 5 3.5 C[C@H](NCCc1cc(Cl)c(NCC(=O)O)cc1Cl)[C@H](O)c1ccc(O)cc1 10.1021/jm000455z
155510718 168937 0 None 1 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) expressed in HEK293 cell assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 15 minsAntagonist activity at beta2 adrenergic receptor (unknown origin) expressed in HEK293 cell assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 15 mins
ChEMBL 556 23 4 6 6.1 CC(C)NC[C@H](O)COc1ccccc1CCCCCCCCCCc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
CHEMBL4434772 168937 0 None 1 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) expressed in HEK293 cell assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 15 minsAntagonist activity at beta2 adrenergic receptor (unknown origin) expressed in HEK293 cell assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 15 mins
ChEMBL 556 23 4 6 6.1 CC(C)NC[C@H](O)COc1ccccc1CCCCCCCCCCc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
155568878 175583 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assayAntagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assay
ChEMBL 457 15 4 5 3.3 COc1ccccc1CCCNC(=O)NCCCc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
CHEMBL4593049 175583 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assayAntagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assay
ChEMBL 457 15 4 5 3.3 COc1ccccc1CCCNC(=O)NCCCc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
155559932 174325 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assayAntagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assay
ChEMBL 427 14 4 4 3.3 CC(C)NC[C@H](O)COc1ccccc1CCCNC(=O)NCCCc1ccccc1 10.1021/acs.jmedchem.9b00595
CHEMBL4564495 174325 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assayAntagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assay
ChEMBL 427 14 4 4 3.3 CC(C)NC[C@H](O)COc1ccccc1CCCNC(=O)NCCCc1ccccc1 10.1021/acs.jmedchem.9b00595
10835216 110154 0 None -251 2 Rat 5.9 pIC50 = 5.9 Functional
Agonistic activity towards beta-2 adrenoceptor. Mean concentration required to produce 50% inhibition of uterine contractionAgonistic activity towards beta-2 adrenoceptor. Mean concentration required to produce 50% inhibition of uterine contraction
ChEMBL 406 9 5 5 3.6 C[C@H](NCCc1ccc(NC(C)(C)C(=O)O)cc1Cl)[C@H](O)c1ccc(O)cc1 10.1021/jm000455z
CHEMBL32586 110154 0 None -251 2 Rat 5.9 pIC50 = 5.9 Functional
Agonistic activity towards beta-2 adrenoceptor. Mean concentration required to produce 50% inhibition of uterine contractionAgonistic activity towards beta-2 adrenoceptor. Mean concentration required to produce 50% inhibition of uterine contraction
ChEMBL 406 9 5 5 3.6 C[C@H](NCCc1ccc(NC(C)(C)C(=O)O)cc1Cl)[C@H](O)c1ccc(O)cc1 10.1021/jm000455z
10693556 111839 0 None -2 2 Rat 5.9 pIC50 = 5.9 Functional
Agonistic activity towards beta-2 adrenoceptor. Mean concentration required to produce 50% inhibition of uterine contractionAgonistic activity towards beta-2 adrenoceptor. Mean concentration required to produce 50% inhibition of uterine contraction
ChEMBL 422 9 5 5 2.9 C[C@H](NCCc1ccc(NCC(=O)O)c(Br)c1)[C@H](O)c1ccc(O)cc1 10.1021/jm000455z
CHEMBL32939 111839 0 None -2 2 Rat 5.9 pIC50 = 5.9 Functional
Agonistic activity towards beta-2 adrenoceptor. Mean concentration required to produce 50% inhibition of uterine contractionAgonistic activity towards beta-2 adrenoceptor. Mean concentration required to produce 50% inhibition of uterine contraction
ChEMBL 422 9 5 5 2.9 C[C@H](NCCc1ccc(NCC(=O)O)c(Br)c1)[C@H](O)c1ccc(O)cc1 10.1021/jm000455z
9844606 109821 0 None -1000 2 Rat 4.9 pIC50 = 4.9 Functional
Agonistic activity towards beta-2 adrenoceptor. Mean concentration required to produce 50% inhibition of uterine contractionAgonistic activity towards beta-2 adrenoceptor. Mean concentration required to produce 50% inhibition of uterine contraction
ChEMBL 412 9 5 5 3.5 C[C@H](NCCc1cc(Cl)c(NCC(=O)O)c(Cl)c1)[C@H](O)c1ccc(O)cc1 10.1021/jm000455z
CHEMBL32391 109821 0 None -1000 2 Rat 4.9 pIC50 = 4.9 Functional
Agonistic activity towards beta-2 adrenoceptor. Mean concentration required to produce 50% inhibition of uterine contractionAgonistic activity towards beta-2 adrenoceptor. Mean concentration required to produce 50% inhibition of uterine contraction
ChEMBL 412 9 5 5 3.5 C[C@H](NCCc1cc(Cl)c(NCC(=O)O)c(Cl)c1)[C@H](O)c1ccc(O)cc1 10.1021/jm000455z
10666106 114022 0 None -30 2 Rat 5.8 pIC50 = 5.8 Functional
Agonistic activity towards beta-2 adrenoceptor. Mean concentration required to produce 50% inhibition of uterine contractionAgonistic activity towards beta-2 adrenoceptor. Mean concentration required to produce 50% inhibition of uterine contraction
ChEMBL 358 9 4 5 2.2 C[C@H](NCCc1ccc(N(C)CC(=O)O)cc1)[C@H](O)c1ccc(O)cc1 10.1021/jm000455z
CHEMBL33360 114022 0 None -30 2 Rat 5.8 pIC50 = 5.8 Functional
Agonistic activity towards beta-2 adrenoceptor. Mean concentration required to produce 50% inhibition of uterine contractionAgonistic activity towards beta-2 adrenoceptor. Mean concentration required to produce 50% inhibition of uterine contraction
ChEMBL 358 9 4 5 2.2 C[C@H](NCCc1ccc(N(C)CC(=O)O)cc1)[C@H](O)c1ccc(O)cc1 10.1021/jm000455z
155563970 174778 0 None 20 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assayAntagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assay
ChEMBL 530 18 6 7 2.2 CC(C)NC[C@H](O)COc1ccccc1CCNC(=O)NCCc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
CHEMBL4574652 174778 0 None 20 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assayAntagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assay
ChEMBL 530 18 6 7 2.2 CC(C)NC[C@H](O)COc1ccccc1CCNC(=O)NCCc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
9832011 104989 0 None -19 3 Human 6.8 pIC50 = 6.8 Functional
Compound was evaluated for its inhibitory activity against CHO cells expressing the cloned human beta-2 adrenergic receptor (AR) in the presence of [125I]-iodocyanopindololCompound was evaluated for its inhibitory activity against CHO cells expressing the cloned human beta-2 adrenergic receptor (AR) in the presence of [125I]-iodocyanopindolol
ChEMBL 644 13 6 7 6.5 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(-c3ccc(OCC4NCCc5cc(O)c(O)cc54)cc3)cc2)cc1 10.1016/s0960-894x(00)00459-5
CHEMBL312074 104989 0 None -19 3 Human 6.8 pIC50 = 6.8 Functional
Compound was evaluated for its inhibitory activity against CHO cells expressing the cloned human beta-2 adrenergic receptor (AR) in the presence of [125I]-iodocyanopindololCompound was evaluated for its inhibitory activity against CHO cells expressing the cloned human beta-2 adrenergic receptor (AR) in the presence of [125I]-iodocyanopindolol
ChEMBL 644 13 6 7 6.5 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(-c3ccc(OCC4NCCc5cc(O)c(O)cc54)cc3)cc2)cc1 10.1016/s0960-894x(00)00459-5
156009636 176581 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at ADRB2 endogenously expressed in HEK293 cells transfected with cAMP FRET biosensor assessed as inhibition of cimaterol-induced response pre-incubated for 45 mins under constant violet light conditions by FRET assayAntagonist activity at ADRB2 endogenously expressed in HEK293 cells transfected with cAMP FRET biosensor assessed as inhibition of cimaterol-induced response pre-incubated for 45 mins under constant violet light conditions by FRET assay
ChEMBL 370 9 3 6 3.8 CC(=O)Nc1ccc(/N=N/c2cccc(OC[C@@H](O)CNC(C)C)c2)cc1 10.1021/acs.jmedchem.0c00831
CHEMBL4634403 176581 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at ADRB2 endogenously expressed in HEK293 cells transfected with cAMP FRET biosensor assessed as inhibition of cimaterol-induced response pre-incubated for 45 mins under constant violet light conditions by FRET assayAntagonist activity at ADRB2 endogenously expressed in HEK293 cells transfected with cAMP FRET biosensor assessed as inhibition of cimaterol-induced response pre-incubated for 45 mins under constant violet light conditions by FRET assay
ChEMBL 370 9 3 6 3.8 CC(=O)Nc1ccc(/N=N/c2cccc(OC[C@@H](O)CNC(C)C)c2)cc1 10.1021/acs.jmedchem.0c00831
155545790 172903 0 None 79 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assayAntagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assay
ChEMBL 593 18 5 13 1.6 CC(C)NC[C@H](O)COc1ccccc1-n1cc(CNCc2cn(-c3ccccc3OC[C@@H](O)CNC(C)C)nn2)nn1 10.1021/acs.jmedchem.9b00595
CHEMBL4530266 172903 0 None 79 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assayAntagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assay
ChEMBL 593 18 5 13 1.6 CC(C)NC[C@H](O)COc1ccccc1-n1cc(CNCc2cn(-c3ccccc3OC[C@@H](O)CNC(C)C)nn2)nn1 10.1021/acs.jmedchem.9b00595
10787873 99398 0 None -3 2 Rat 5.8 pIC50 = 5.8 Functional
Agonistic activity towards beta-2 adrenoceptor. Mean concentration required to produce 50% inhibition of uterine contractionAgonistic activity towards beta-2 adrenoceptor. Mean concentration required to produce 50% inhibition of uterine contraction
ChEMBL 412 9 5 5 3.5 C[C@H](NCCc1ccc(NCC(=O)O)c(Cl)c1Cl)[C@H](O)c1ccc(O)cc1 10.1021/jm000455z
CHEMBL285888 99398 0 None -3 2 Rat 5.8 pIC50 = 5.8 Functional
Agonistic activity towards beta-2 adrenoceptor. Mean concentration required to produce 50% inhibition of uterine contractionAgonistic activity towards beta-2 adrenoceptor. Mean concentration required to produce 50% inhibition of uterine contraction
ChEMBL 412 9 5 5 3.5 C[C@H](NCCc1ccc(NCC(=O)O)c(Cl)c1Cl)[C@H](O)c1ccc(O)cc1 10.1021/jm000455z
105 3392 84 None 3 3 Guinea pig 7.8 pIC50 = 7.8 Functional
Agonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response after 30 minsAgonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response after 30 mins
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1021/jm100068m
2083 3392 84 None 3 3 Guinea pig 7.8 pIC50 = 7.8 Functional
Agonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response after 30 minsAgonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response after 30 mins
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1021/jm100068m
558 3392 84 None 3 3 Guinea pig 7.8 pIC50 = 7.8 Functional
Agonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response after 30 minsAgonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response after 30 mins
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1021/jm100068m
CHEMBL714 3392 84 None 3 3 Guinea pig 7.8 pIC50 = 7.8 Functional
Agonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response after 30 minsAgonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response after 30 mins
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1021/jm100068m
DB01001 3392 84 None 3 3 Guinea pig 7.8 pIC50 = 7.8 Functional
Agonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response after 30 minsAgonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response after 30 mins
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1021/jm100068m
155528927 170820 0 None 6 2 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) expressed in HEK293 cell assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 15 minsAntagonist activity at beta2 adrenergic receptor (unknown origin) expressed in HEK293 cell assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 15 mins
ChEMBL 649 22 5 13 2.1 CC(C)NC[C@H](O)COc1ccccc1CCn1cc(CNCc2cn(CCc3ccccc3OC[C@@H](O)CNC(C)C)nn2)nn1 10.1021/acs.jmedchem.9b00595
CHEMBL4462252 170820 0 None 6 2 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) expressed in HEK293 cell assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 15 minsAntagonist activity at beta2 adrenergic receptor (unknown origin) expressed in HEK293 cell assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 15 mins
ChEMBL 649 22 5 13 2.1 CC(C)NC[C@H](O)COc1ccccc1CCn1cc(CNCc2cn(CCc3ccccc3OC[C@@H](O)CNC(C)C)nn2)nn1 10.1021/acs.jmedchem.9b00595
155563970 174778 0 None 20 2 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) expressed in HEK293 cell assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 15 minsAntagonist activity at beta2 adrenergic receptor (unknown origin) expressed in HEK293 cell assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 15 mins
ChEMBL 530 18 6 7 2.2 CC(C)NC[C@H](O)COc1ccccc1CCNC(=O)NCCc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
CHEMBL4574652 174778 0 None 20 2 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) expressed in HEK293 cell assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 15 minsAntagonist activity at beta2 adrenergic receptor (unknown origin) expressed in HEK293 cell assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 15 mins
ChEMBL 530 18 6 7 2.2 CC(C)NC[C@H](O)COc1ccccc1CCNC(=O)NCCc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
204665 10125 9 None 4 2 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assayAntagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assay
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
CHEMBL1160734 10125 9 None 4 2 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assayAntagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assay
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
46221603 8456 0 None 7 2 Guinea pig 8.6 pIC50 = 8.6 Functional
Agonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response after 30 minsAgonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response after 30 mins
ChEMBL 396 6 4 6 2.0 COc1cc2c(cc1OC)CC(NC[C@H](O)c1ccc(O)c3[nH]c(=O)ccc13)C2 10.1021/jm100068m
CHEMBL1094486 8456 0 None 7 2 Guinea pig 8.6 pIC50 = 8.6 Functional
Agonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response after 30 minsAgonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response after 30 mins
ChEMBL 396 6 4 6 2.0 COc1cc2c(cc1OC)CC(NC[C@H](O)c1ccc(O)c3[nH]c(=O)ccc13)C2 10.1021/jm100068m
203685 30526 8 None 33 4 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) expressed in HEK293 cell assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 15 minsAntagonist activity at beta2 adrenergic receptor (unknown origin) expressed in HEK293 cell assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 15 mins
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OC[C@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
CHEMBL1395661 30526 8 None 33 4 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) expressed in HEK293 cell assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 15 minsAntagonist activity at beta2 adrenergic receptor (unknown origin) expressed in HEK293 cell assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 15 mins
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OC[C@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
155544582 172798 0 None 5 2 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assayAntagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assay
ChEMBL 528 21 4 6 5.3 CC(C)NC[C@H](O)COc1ccccc1CCCCCCCCc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
CHEMBL4527821 172798 0 None 5 2 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assayAntagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assay
ChEMBL 528 21 4 6 5.3 CC(C)NC[C@H](O)COc1ccccc1CCCCCCCCc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
155539613 172268 0 None 2 2 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assayAntagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assay
ChEMBL 677 24 5 13 2.9 CC(C)NC[C@H](O)COc1ccccc1CCCn1cc(CNCc2cn(CCCc3ccccc3OC[C@@H](O)CNC(C)C)nn2)nn1 10.1021/acs.jmedchem.9b00595
CHEMBL4514723 172268 0 None 2 2 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assayAntagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assay
ChEMBL 677 24 5 13 2.9 CC(C)NC[C@H](O)COc1ccccc1CCCn1cc(CNCc2cn(CCCc3ccccc3OC[C@@H](O)CNC(C)C)nn2)nn1 10.1021/acs.jmedchem.9b00595
46221397 8600 0 None -1 2 Guinea pig 7.7 pIC50 = 7.7 Functional
Agonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response after 30 minsAgonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response after 30 mins
ChEMBL 420 8 4 4 3.9 CCCc1cc2c(cc1CCC)CC(NC[C@H](O)c1ccc(O)c3[nH]c(=O)ccc13)C2 10.1021/jm100068m
CHEMBL1095778 8600 0 None -1 2 Guinea pig 7.7 pIC50 = 7.7 Functional
Agonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response after 30 minsAgonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response after 30 mins
ChEMBL 420 8 4 4 3.9 CCCc1cc2c(cc1CCC)CC(NC[C@H](O)c1ccc(O)c3[nH]c(=O)ccc13)C2 10.1021/jm100068m
52949488 17349 0 None -81 3 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as inhibition of isoproterenol-induced cyclic AMP formation by HTRF assayAntagonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as inhibition of isoproterenol-induced cyclic AMP formation by HTRF assay
ChEMBL 490 9 2 8 4.4 COc1ccccc1OCC(O)CNC1CCN(c2ncnc3scc(-c4ccccc4)c23)CC1 10.1016/j.bmcl.2010.08.039
CHEMBL1258023 17349 0 None -81 3 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as inhibition of isoproterenol-induced cyclic AMP formation by HTRF assayAntagonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as inhibition of isoproterenol-induced cyclic AMP formation by HTRF assay
ChEMBL 490 9 2 8 4.4 COc1ccccc1OCC(O)CNC1CCN(c2ncnc3scc(-c4ccccc4)c23)CC1 10.1016/j.bmcl.2010.08.039
155537285 171707 0 None 14 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) expressed in HEK293 cell assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 15 minsAntagonist activity at beta2 adrenergic receptor (unknown origin) expressed in HEK293 cell assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 15 mins
ChEMBL 558 19 6 8 1.2 CC(C)NC[C@H](O)COc1ccccc1CC(=O)NCCNC(=O)Cc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
CHEMBL4474813 171707 0 None 14 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) expressed in HEK293 cell assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 15 minsAntagonist activity at beta2 adrenergic receptor (unknown origin) expressed in HEK293 cell assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 15 mins
ChEMBL 558 19 6 8 1.2 CC(C)NC[C@H](O)COc1ccccc1CC(=O)NCCNC(=O)Cc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
155557081 173958 0 None 20 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assayAntagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assay
ChEMBL 614 23 6 8 2.7 CC(C)NC[C@@H](O)COc1ccccc1CCCC(=O)NCCNC(=O)CCCc1ccccc1OC[C@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
CHEMBL4556017 173958 0 None 20 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assayAntagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assay
ChEMBL 614 23 6 8 2.7 CC(C)NC[C@@H](O)COc1ccccc1CCCC(=O)NCCNC(=O)CCCc1ccccc1OC[C@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
53326195 58331 0 None -144 3 Human 5.7 pIC50 = 5.7 Functional
Agonist activity at human beta2 adrenergic receptorAgonist activity at human beta2 adrenergic receptor
ChEMBL 649 9 3 6 7.7 O=S(=O)(Nc1ccc(CC2CC[C@H]([C@H](O)c3ccccc3)N2)cc1)c1ccc(-c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1016/j.bmcl.2010.12.087
CHEMBL1684577 58331 0 None -144 3 Human 5.7 pIC50 = 5.7 Functional
Agonist activity at human beta2 adrenergic receptorAgonist activity at human beta2 adrenergic receptor
ChEMBL 649 9 3 6 7.7 O=S(=O)(Nc1ccc(CC2CC[C@H]([C@H](O)c3ccccc3)N2)cc1)c1ccc(-c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1016/j.bmcl.2010.12.087
10672048 120586 0 None -2 2 Rat 5.7 pIC50 = 5.7 Functional
Agonistic activity towards beta-2 adrenoceptor. Mean concentration required to produce 50% inhibition of uterine contractionAgonistic activity towards beta-2 adrenoceptor. Mean concentration required to produce 50% inhibition of uterine contraction
ChEMBL 470 9 5 5 2.7 C[C@H](NCCc1ccc(NCC(=O)O)c(I)c1)[C@H](O)c1ccc(O)cc1 10.1021/jm000455z
CHEMBL35738 120586 0 None -2 2 Rat 5.7 pIC50 = 5.7 Functional
Agonistic activity towards beta-2 adrenoceptor. Mean concentration required to produce 50% inhibition of uterine contractionAgonistic activity towards beta-2 adrenoceptor. Mean concentration required to produce 50% inhibition of uterine contraction
ChEMBL 470 9 5 5 2.7 C[C@H](NCCc1ccc(NCC(=O)O)c(I)c1)[C@H](O)c1ccc(O)cc1 10.1021/jm000455z
52944986 17416 0 None -26 3 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as inhibition of isoproterenol-induced cyclic AMP formation by HTRF assayAntagonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as inhibition of isoproterenol-induced cyclic AMP formation by HTRF assay
ChEMBL 478 8 2 7 4.5 OC(CNC1CCN(c2ncnc3scc(-c4ccccc4)c23)CC1)COc1ccccc1F 10.1016/j.bmcl.2010.08.039
CHEMBL1258257 17416 0 None -26 3 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as inhibition of isoproterenol-induced cyclic AMP formation by HTRF assayAntagonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as inhibition of isoproterenol-induced cyclic AMP formation by HTRF assay
ChEMBL 478 8 2 7 4.5 OC(CNC1CCN(c2ncnc3scc(-c4ccccc4)c23)CC1)COc1ccccc1F 10.1016/j.bmcl.2010.08.039
24936626 17212 0 None -112201 3 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as inhibition of isoproterenol-induced cyclic AMP formation by HTRF assayAntagonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as inhibition of isoproterenol-induced cyclic AMP formation by HTRF assay
ChEMBL 506 9 4 9 3.6 OCc1cc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)ccc1O 10.1016/j.bmcl.2010.08.039
CHEMBL1257555 17212 0 None -112201 3 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as inhibition of isoproterenol-induced cyclic AMP formation by HTRF assayAntagonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as inhibition of isoproterenol-induced cyclic AMP formation by HTRF assay
ChEMBL 506 9 4 9 3.6 OCc1cc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)ccc1O 10.1016/j.bmcl.2010.08.039
31729 204060 6 None 7 2 Rat 7.6 pIC50 = 7.6 Functional
Agonistic activity towards beta-2 adrenoceptor. Mean concentration required to produce 50% inhibition of uterine contractionAgonistic activity towards beta-2 adrenoceptor. Mean concentration required to produce 50% inhibition of uterine contraction
ChEMBL 287 6 4 4 2.4 CC(NCCc1ccc(O)cc1)C(O)c1ccc(O)cc1 10.1021/jm000455z
CHEMBL83063 204060 6 None 7 2 Rat 7.6 pIC50 = 7.6 Functional
Agonistic activity towards beta-2 adrenoceptor. Mean concentration required to produce 50% inhibition of uterine contractionAgonistic activity towards beta-2 adrenoceptor. Mean concentration required to produce 50% inhibition of uterine contraction
ChEMBL 287 6 4 4 2.4 CC(NCCc1ccc(O)cc1)C(O)c1ccc(O)cc1 10.1021/jm000455z
16717791 77247 0 None - 1 Guinea pig 6.6 pIC50 = 6.6 Functional
Agonist activity at beta2-adrenoceptor in guinea-pig tracheal-strip assessed as inhibition of electrically-stimulated muscle contractionAgonist activity at beta2-adrenoceptor in guinea-pig tracheal-strip assessed as inhibition of electrically-stimulated muscle contraction
ChEMBL 376 6 3 3 3.7 CCc1cc2c(cc1CC)CC(NCCc1ccc(O)c3[nH]c(=O)ccc13)C2 10.1016/j.bmcl.2012.07.096
CHEMBL2088198 77247 0 None - 1 Guinea pig 6.6 pIC50 = 6.6 Functional
Agonist activity at beta2-adrenoceptor in guinea-pig tracheal-strip assessed as inhibition of electrically-stimulated muscle contractionAgonist activity at beta2-adrenoceptor in guinea-pig tracheal-strip assessed as inhibition of electrically-stimulated muscle contraction
ChEMBL 376 6 3 3 3.7 CCc1cc2c(cc1CC)CC(NCCc1ccc(O)c3[nH]c(=O)ccc13)C2 10.1016/j.bmcl.2012.07.096
24937269 17450 0 None -9 3 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as inhibition of isoproterenol-induced cyclic AMP formation by HTRF assayAntagonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as inhibition of isoproterenol-induced cyclic AMP formation by HTRF assay
ChEMBL 490 9 3 8 3.8 OCc1cccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)c1 10.1016/j.bmcl.2010.08.039
CHEMBL1258371 17450 0 None -9 3 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as inhibition of isoproterenol-induced cyclic AMP formation by HTRF assayAntagonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as inhibition of isoproterenol-induced cyclic AMP formation by HTRF assay
ChEMBL 490 9 3 8 3.8 OCc1cccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)c1 10.1016/j.bmcl.2010.08.039
155515551 169398 0 None 1 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) expressed in HEK293 cell assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 15 minsAntagonist activity at beta2 adrenergic receptor (unknown origin) expressed in HEK293 cell assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 15 mins
ChEMBL 584 25 4 6 6.8 CC(C)NC[C@H](O)COc1ccccc1CCCCCCCCCCCCc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
CHEMBL4441975 169398 0 None 1 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) expressed in HEK293 cell assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 15 minsAntagonist activity at beta2 adrenergic receptor (unknown origin) expressed in HEK293 cell assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 15 mins
ChEMBL 584 25 4 6 6.8 CC(C)NC[C@H](O)COc1ccccc1CCCCCCCCCCCCc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
52949489 17350 0 None -12 3 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as inhibition of isoproterenol-induced cyclic AMP formation by HTRF assayAntagonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as inhibition of isoproterenol-induced cyclic AMP formation by HTRF assay
ChEMBL 490 9 2 8 4.4 COc1cccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)c1 10.1016/j.bmcl.2010.08.039
CHEMBL1258024 17350 0 None -12 3 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as inhibition of isoproterenol-induced cyclic AMP formation by HTRF assayAntagonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as inhibition of isoproterenol-induced cyclic AMP formation by HTRF assay
ChEMBL 490 9 2 8 4.4 COc1cccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)c1 10.1016/j.bmcl.2010.08.039
51346867 58336 0 None -616 3 Human 5.6 pIC50 = 5.6 Functional
Agonist activity at human beta2 adrenergic receptorAgonist activity at human beta2 adrenergic receptor
ChEMBL 649 9 3 6 7.7 O=S(=O)(Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1)c1ccc(-c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1016/j.bmcl.2010.12.087
CHEMBL1684583 58336 0 None -616 3 Human 5.6 pIC50 = 5.6 Functional
Agonist activity at human beta2 adrenergic receptorAgonist activity at human beta2 adrenergic receptor
ChEMBL 649 9 3 6 7.7 O=S(=O)(Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1)c1ccc(-c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1016/j.bmcl.2010.12.087
11797099 109960 0 None -19 2 Rat 6.6 pIC50 = 6.6 Functional
Agonistic activity towards beta-2 adrenoceptor. Mean concentration required to produce 50% inhibition of uterine contractionAgonistic activity towards beta-2 adrenoceptor. Mean concentration required to produce 50% inhibition of uterine contraction
ChEMBL 434 11 4 5 3.7 C[C@H](NCCc1ccc(N(CC(=O)O)Cc2ccccc2)cc1)[C@H](O)c1ccc(O)cc1 10.1021/jm000455z
CHEMBL32470 109960 0 None -19 2 Rat 6.6 pIC50 = 6.6 Functional
Agonistic activity towards beta-2 adrenoceptor. Mean concentration required to produce 50% inhibition of uterine contractionAgonistic activity towards beta-2 adrenoceptor. Mean concentration required to produce 50% inhibition of uterine contraction
ChEMBL 434 11 4 5 3.7 C[C@H](NCCc1ccc(N(CC(=O)O)Cc2ccccc2)cc1)[C@H](O)c1ccc(O)cc1 10.1021/jm000455z
11799609 114287 0 None -31 2 Rat 5.6 pIC50 = 5.6 Functional
Agonistic activity towards beta-2 adrenoceptor. Mean concentration required to produce 50% inhibition of uterine contractionAgonistic activity towards beta-2 adrenoceptor. Mean concentration required to produce 50% inhibition of uterine contraction
ChEMBL 500 9 5 5 3.7 C[C@H](NCCc1cc(Br)c(NCC(=O)O)c(Br)c1)[C@H](O)c1ccc(O)cc1 10.1021/jm000455z
CHEMBL33399 114287 0 None -31 2 Rat 5.6 pIC50 = 5.6 Functional
Agonistic activity towards beta-2 adrenoceptor. Mean concentration required to produce 50% inhibition of uterine contractionAgonistic activity towards beta-2 adrenoceptor. Mean concentration required to produce 50% inhibition of uterine contraction
ChEMBL 500 9 5 5 3.7 C[C@H](NCCc1cc(Br)c(NCC(=O)O)c(Br)c1)[C@H](O)c1ccc(O)cc1 10.1021/jm000455z
155537285 171707 0 None 14 2 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assayAntagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assay
ChEMBL 558 19 6 8 1.2 CC(C)NC[C@H](O)COc1ccccc1CC(=O)NCCNC(=O)Cc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
CHEMBL4474813 171707 0 None 14 2 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assayAntagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assay
ChEMBL 558 19 6 8 1.2 CC(C)NC[C@H](O)COc1ccccc1CC(=O)NCCNC(=O)Cc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
10283539 167291 0 None -346 3 Human 6.6 pIC50 = 6.6 Functional
Compound was tested for the antagonistic activity against Beta-2 adrenergic receptorCompound was tested for the antagonistic activity against Beta-2 adrenergic receptor
ChEMBL 697 14 6 9 2.8 CS(=O)(=O)Nc1cc(OC[C@@H](O)CNCC2CCN(S(=O)(=O)c3ccc(NC(=O)NCc4cc(F)ccc4F)cc3)CC2)ccc1O 10.1016/s0960-894x(02)00607-8
CHEMBL431048 167291 0 None -346 3 Human 6.6 pIC50 = 6.6 Functional
Compound was tested for the antagonistic activity against Beta-2 adrenergic receptorCompound was tested for the antagonistic activity against Beta-2 adrenergic receptor
ChEMBL 697 14 6 9 2.8 CS(=O)(=O)Nc1cc(OC[C@@H](O)CNCC2CCN(S(=O)(=O)c3ccc(NC(=O)NCc4cc(F)ccc4F)cc3)CC2)ccc1O 10.1016/s0960-894x(02)00607-8
53319639 58335 0 None -2 3 Human 5.6 pIC50 = 5.6 Functional
Agonist activity at human beta2 adrenergic receptorAgonist activity at human beta2 adrenergic receptor
ChEMBL 649 9 3 6 7.7 O=S(=O)(Nc1ccc(CC2CC[C@H]([C@@H](O)c3ccccc3)N2)cc1)c1ccc(-c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1016/j.bmcl.2010.12.087
CHEMBL1684582 58335 0 None -2 3 Human 5.6 pIC50 = 5.6 Functional
Agonist activity at human beta2 adrenergic receptorAgonist activity at human beta2 adrenergic receptor
ChEMBL 649 9 3 6 7.7 O=S(=O)(Nc1ccc(CC2CC[C@H]([C@@H](O)c3ccccc3)N2)cc1)c1ccc(-c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1016/j.bmcl.2010.12.087
156010391 176542 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at ADRB2 endogenously expressed in HEK293 cells transfected with cAMP FRET biosensor assessed as inhibition of cimaterol-induced response pre-incubated for 45 mins under constant violet light conditions by FRET assayAntagonist activity at ADRB2 endogenously expressed in HEK293 cells transfected with cAMP FRET biosensor assessed as inhibition of cimaterol-induced response pre-incubated for 45 mins under constant violet light conditions by FRET assay
ChEMBL 370 9 3 6 3.8 CC(=O)Nc1ccc(/N=N/c2ccccc2OC[C@@H](O)CNC(C)C)cc1 10.1021/acs.jmedchem.0c00831
CHEMBL4633760 176542 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at ADRB2 endogenously expressed in HEK293 cells transfected with cAMP FRET biosensor assessed as inhibition of cimaterol-induced response pre-incubated for 45 mins under constant violet light conditions by FRET assayAntagonist activity at ADRB2 endogenously expressed in HEK293 cells transfected with cAMP FRET biosensor assessed as inhibition of cimaterol-induced response pre-incubated for 45 mins under constant violet light conditions by FRET assay
ChEMBL 370 9 3 6 3.8 CC(=O)Nc1ccc(/N=N/c2ccccc2OC[C@@H](O)CNC(C)C)cc1 10.1021/acs.jmedchem.0c00831
14739905 206534 0 None -7 2 Dog 6.6 pIC50 = 6.6 Functional
Beta2-receptor selectivity in canine lung tissue in anesthetized dogsBeta2-receptor selectivity in canine lung tissue in anesthetized dogs
ChEMBL 353 10 2 6 2.3 OC(CNCCOc1ccc(-n2ccnc2)cc1)COc1ccccc1 10.1021/jm00172a033
CHEMBL98975 206534 0 None -7 2 Dog 6.6 pIC50 = 6.6 Functional
Beta2-receptor selectivity in canine lung tissue in anesthetized dogsBeta2-receptor selectivity in canine lung tissue in anesthetized dogs
ChEMBL 353 10 2 6 2.3 OC(CNCCOc1ccc(-n2ccnc2)cc1)COc1ccccc1 10.1021/jm00172a033
44281611 99885 0 None 2 2 Rat 6.6 pIC50 = 6.6 Functional
Agonistic activity towards beta-2 adrenoceptor. Mean concentration required to produce 50% inhibition of uterine contractionAgonistic activity towards beta-2 adrenoceptor. Mean concentration required to produce 50% inhibition of uterine contraction
ChEMBL 402 11 5 6 1.6 C[C@H](NCCc1ccc(N(CC(=O)O)CC(=O)O)cc1)[C@H](O)c1ccc(O)cc1 10.1021/jm000455z
CHEMBL289670 99885 0 None 2 2 Rat 6.6 pIC50 = 6.6 Functional
Agonistic activity towards beta-2 adrenoceptor. Mean concentration required to produce 50% inhibition of uterine contractionAgonistic activity towards beta-2 adrenoceptor. Mean concentration required to produce 50% inhibition of uterine contraction
ChEMBL 402 11 5 6 1.6 C[C@H](NCCc1ccc(N(CC(=O)O)CC(=O)O)cc1)[C@H](O)c1ccc(O)cc1 10.1021/jm000455z
53326197 58337 0 None -35 3 Human 6.5 pIC50 = 6.5 Functional
Agonist activity at human beta2 adrenergic receptorAgonist activity at human beta2 adrenergic receptor
ChEMBL 649 9 3 6 7.7 O=S(=O)(Nc1ccc(C[C@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1)c1ccc(-c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1016/j.bmcl.2010.12.087
CHEMBL1684584 58337 0 None -35 3 Human 6.5 pIC50 = 6.5 Functional
Agonist activity at human beta2 adrenergic receptorAgonist activity at human beta2 adrenergic receptor
ChEMBL 649 9 3 6 7.7 O=S(=O)(Nc1ccc(C[C@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1)c1ccc(-c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1016/j.bmcl.2010.12.087
155536373 171600 0 None 7 2 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) expressed in HEK293 cell assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 15 minsAntagonist activity at beta2 adrenergic receptor (unknown origin) expressed in HEK293 cell assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 15 mins
ChEMBL 500 19 4 6 4.5 CC(C)NC[C@H](O)COc1ccccc1CCCCCCc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
CHEMBL4473518 171600 0 None 7 2 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) expressed in HEK293 cell assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 15 minsAntagonist activity at beta2 adrenergic receptor (unknown origin) expressed in HEK293 cell assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 15 mins
ChEMBL 500 19 4 6 4.5 CC(C)NC[C@H](O)COc1ccccc1CCCCCCc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
155521390 170010 0 None 128 2 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) expressed in HEK293 cell assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 15 minsAntagonist activity at beta2 adrenergic receptor (unknown origin) expressed in HEK293 cell assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 15 mins
ChEMBL 586 21 6 8 2.0 CC(C)NC[C@H](O)COc1ccccc1CCC(=O)NCCNC(=O)CCc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
CHEMBL4450606 170010 0 None 128 2 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) expressed in HEK293 cell assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 15 minsAntagonist activity at beta2 adrenergic receptor (unknown origin) expressed in HEK293 cell assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 15 mins
ChEMBL 586 21 6 8 2.0 CC(C)NC[C@H](O)COc1ccccc1CCC(=O)NCCNC(=O)CCc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
2419 3394 80 None -22 6 Guinea pig 8.5 pIC50 = 8.5 Functional
Agonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response after 30 minsAgonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response after 30 mins
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/jm100068m
5152 3394 80 None -22 6 Guinea pig 8.5 pIC50 = 8.5 Functional
Agonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response after 30 minsAgonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response after 30 mins
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/jm100068m
559 3394 80 None -22 6 Guinea pig 8.5 pIC50 = 8.5 Functional
Agonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response after 30 minsAgonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response after 30 mins
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/jm100068m
CHEMBL1263 3394 80 None -22 6 Guinea pig 8.5 pIC50 = 8.5 Functional
Agonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response after 30 minsAgonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response after 30 mins
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/jm100068m
DB00938 3394 80 None -22 6 Guinea pig 8.5 pIC50 = 8.5 Functional
Agonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response after 30 minsAgonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response after 30 mins
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/jm100068m
155510718 168937 0 None 1 2 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assayAntagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assay
ChEMBL 556 23 4 6 6.1 CC(C)NC[C@H](O)COc1ccccc1CCCCCCCCCCc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
CHEMBL4434772 168937 0 None 1 2 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assayAntagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assay
ChEMBL 556 23 4 6 6.1 CC(C)NC[C@H](O)COc1ccccc1CCCCCCCCCCc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
155536373 171600 0 None 7 2 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assayAntagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assay
ChEMBL 500 19 4 6 4.5 CC(C)NC[C@H](O)COc1ccccc1CCCCCCc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
CHEMBL4473518 171600 0 None 7 2 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assayAntagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assay
ChEMBL 500 19 4 6 4.5 CC(C)NC[C@H](O)COc1ccccc1CCCCCCc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
155546387 172972 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assayAntagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assay
ChEMBL 513 18 4 6 3.0 COc1ccccc1CCCC(=O)NCCNC(=O)CCCc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
CHEMBL4532142 172972 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assayAntagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assay
ChEMBL 513 18 4 6 3.0 COc1ccccc1CCCC(=O)NCCNC(=O)CCCc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
70684846 77246 9 None - 1 Guinea pig 8.4 pIC50 = 8.4 Functional
Agonist activity at beta2-adrenoceptor in guinea-pig tracheal-strip assessed as inhibition of electrically-stimulated muscle contractionAgonist activity at beta2-adrenoceptor in guinea-pig tracheal-strip assessed as inhibition of electrically-stimulated muscle contraction
ChEMBL 394 6 4 4 3.2 CCc1cc2c(cc1CC)CC(NC[C@H](O)c1ccc(O)c3c1CCC(=O)N3)C2 10.1016/j.bmcl.2012.07.096
CHEMBL2088197 77246 9 None - 1 Guinea pig 8.4 pIC50 = 8.4 Functional
Agonist activity at beta2-adrenoceptor in guinea-pig tracheal-strip assessed as inhibition of electrically-stimulated muscle contractionAgonist activity at beta2-adrenoceptor in guinea-pig tracheal-strip assessed as inhibition of electrically-stimulated muscle contraction
ChEMBL 394 6 4 4 3.2 CCc1cc2c(cc1CC)CC(NC[C@H](O)c1ccc(O)c3c1CCC(=O)N3)C2 10.1016/j.bmcl.2012.07.096
24936491 17323 0 None -977 3 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as inhibition of isoproterenol-induced cyclic AMP formation by HTRF assayAntagonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as inhibition of isoproterenol-induced cyclic AMP formation by HTRF assay
ChEMBL 494 8 3 8 4.2 Oc1ccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccc(F)cc5)c34)CC2)cc1 10.1016/j.bmcl.2010.08.039
CHEMBL1257916 17323 0 None -977 3 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as inhibition of isoproterenol-induced cyclic AMP formation by HTRF assayAntagonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as inhibition of isoproterenol-induced cyclic AMP formation by HTRF assay
ChEMBL 494 8 3 8 4.2 Oc1ccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccc(F)cc5)c34)CC2)cc1 10.1016/j.bmcl.2010.08.039
46889854 7212 0 None 9 3 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human adrenergic beta2 receptor expressed in CHOK1 cells assessed as inhibition of cAMP accumulation by HTRF assayAntagonist activity at human adrenergic beta2 receptor expressed in CHOK1 cells assessed as inhibition of cAMP accumulation by HTRF assay
ChEMBL 446 7 2 4 4.8 O=C(c1ccc(F)cc1)C1CCN(CC(O)COc2cccc3[nH]c4ccccc4c23)CC1 10.1016/j.bmcl.2010.04.009
CHEMBL1086077 7212 0 None 9 3 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human adrenergic beta2 receptor expressed in CHOK1 cells assessed as inhibition of cAMP accumulation by HTRF assayAntagonist activity at human adrenergic beta2 receptor expressed in CHOK1 cells assessed as inhibition of cAMP accumulation by HTRF assay
ChEMBL 446 7 2 4 4.8 O=C(c1ccc(F)cc1)C1CCN(CC(O)COc2cccc3[nH]c4ccccc4c23)CC1 10.1016/j.bmcl.2010.04.009
9896817 102399 0 None -44 3 Human 4.5 pIC50 = 4.5 Functional
Compound was evaluated for its inhibitory activity against CHO cells expressing the cloned human beta-2 adrenergic receptor (AR) in the presence of [125I]-iodocyanopindololCompound was evaluated for its inhibitory activity against CHO cells expressing the cloned human beta-2 adrenergic receptor (AR) in the presence of [125I]-iodocyanopindolol
ChEMBL 628 12 6 6 6.7 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2cccc(-c3ccc(CC4NCCc5cc(O)c(O)cc54)cc3)c2)cc1 10.1016/s0960-894x(00)00459-5
CHEMBL305891 102399 0 None -44 3 Human 4.5 pIC50 = 4.5 Functional
Compound was evaluated for its inhibitory activity against CHO cells expressing the cloned human beta-2 adrenergic receptor (AR) in the presence of [125I]-iodocyanopindololCompound was evaluated for its inhibitory activity against CHO cells expressing the cloned human beta-2 adrenergic receptor (AR) in the presence of [125I]-iodocyanopindolol
ChEMBL 628 12 6 6 6.7 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2cccc(-c3ccc(CC4NCCc5cc(O)c(O)cc54)cc3)c2)cc1 10.1016/s0960-894x(00)00459-5
24936492 17352 0 None -323 3 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as inhibition of isoproterenol-induced cyclic AMP formation by HTRF assayAntagonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as inhibition of isoproterenol-induced cyclic AMP formation by HTRF assay
ChEMBL 482 8 3 9 4.1 Oc1ccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5cccs5)c34)CC2)cc1 10.1016/j.bmcl.2010.08.039
CHEMBL1258026 17352 0 None -323 3 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as inhibition of isoproterenol-induced cyclic AMP formation by HTRF assayAntagonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as inhibition of isoproterenol-induced cyclic AMP formation by HTRF assay
ChEMBL 482 8 3 9 4.1 Oc1ccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5cccs5)c34)CC2)cc1 10.1016/j.bmcl.2010.08.039
9929683 110810 0 None -3548 2 Rat 5.5 pIC50 = 5.5 Functional
Agonistic activity towards beta-2 adrenoceptor. Mean concentration required to produce 50% inhibition of uterine contractionAgonistic activity towards beta-2 adrenoceptor. Mean concentration required to produce 50% inhibition of uterine contraction
ChEMBL 378 9 5 5 2.8 C[C@H](NCCc1ccc(NCC(=O)O)c(Cl)c1)[C@H](O)c1ccc(O)cc1 10.1021/jm000455z
CHEMBL32670 110810 0 None -3548 2 Rat 5.5 pIC50 = 5.5 Functional
Agonistic activity towards beta-2 adrenoceptor. Mean concentration required to produce 50% inhibition of uterine contractionAgonistic activity towards beta-2 adrenoceptor. Mean concentration required to produce 50% inhibition of uterine contraction
ChEMBL 378 9 5 5 2.8 C[C@H](NCCc1ccc(NCC(=O)O)c(Cl)c1)[C@H](O)c1ccc(O)cc1 10.1021/jm000455z
9853471 203136 0 None -177 3 Human 5.5 pIC50 = 5.5 Functional
Compound was evaluated for its inhibitory activity against CHO cells expressing the cloned human beta-2 adrenergic receptor (AR) in the presence of [125I]-iodocyanopindololCompound was evaluated for its inhibitory activity against CHO cells expressing the cloned human beta-2 adrenergic receptor (AR) in the presence of [125I]-iodocyanopindolol
ChEMBL 628 12 6 6 6.7 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(-c3ccc(CC4NCCc5cc(O)c(O)cc54)cc3)cc2)cc1 10.1016/s0960-894x(00)00459-5
CHEMBL75604 203136 0 None -177 3 Human 5.5 pIC50 = 5.5 Functional
Compound was evaluated for its inhibitory activity against CHO cells expressing the cloned human beta-2 adrenergic receptor (AR) in the presence of [125I]-iodocyanopindololCompound was evaluated for its inhibitory activity against CHO cells expressing the cloned human beta-2 adrenergic receptor (AR) in the presence of [125I]-iodocyanopindolol
ChEMBL 628 12 6 6 6.7 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(-c3ccc(CC4NCCc5cc(O)c(O)cc54)cc3)cc2)cc1 10.1016/s0960-894x(00)00459-5
53326196 58333 0 None -1 3 Human 5.5 pIC50 = 5.5 Functional
Agonist activity at human beta2 adrenergic receptorAgonist activity at human beta2 adrenergic receptor
ChEMBL 649 9 3 6 7.7 O=S(=O)(Nc1ccc(CC2CC[C@@H]([C@@H](O)c3ccccc3)N2)cc1)c1ccc(-c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1016/j.bmcl.2010.12.087
CHEMBL1684580 58333 0 None -1 3 Human 5.5 pIC50 = 5.5 Functional
Agonist activity at human beta2 adrenergic receptorAgonist activity at human beta2 adrenergic receptor
ChEMBL 649 9 3 6 7.7 O=S(=O)(Nc1ccc(CC2CC[C@@H]([C@@H](O)c3ccccc3)N2)cc1)c1ccc(-c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1016/j.bmcl.2010.12.087
53326839 58334 0 None -43 3 Human 5.5 pIC50 = 5.5 Functional
Agonist activity at human beta2 adrenergic receptorAgonist activity at human beta2 adrenergic receptor
ChEMBL 649 9 3 6 7.7 O=S(=O)(Nc1ccc(CC2CC[C@@H]([C@H](O)c3ccccc3)N2)cc1)c1ccc(-c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1016/j.bmcl.2010.12.087
CHEMBL1684581 58334 0 None -43 3 Human 5.5 pIC50 = 5.5 Functional
Agonist activity at human beta2 adrenergic receptorAgonist activity at human beta2 adrenergic receptor
ChEMBL 649 9 3 6 7.7 O=S(=O)(Nc1ccc(CC2CC[C@@H]([C@H](O)c3ccccc3)N2)cc1)c1ccc(-c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1016/j.bmcl.2010.12.087
9873245 4434 0 None 12 3 Human 8.4 pIC50 = 8.4 Functional
Compound was tested for the antagonistic activity against Beta-2 adrenergic receptorCompound was tested for the antagonistic activity against Beta-2 adrenergic receptor
ChEMBL 590 17 5 7 4.3 CCCCCCCCNC(=O)Nc1ccc(S(=O)(=O)N2CCC(CNC[C@H](O)COc3ccc(O)cc3)CC2)cc1 10.1016/s0960-894x(02)00607-8
CHEMBL102194 4434 0 None 12 3 Human 8.4 pIC50 = 8.4 Functional
Compound was tested for the antagonistic activity against Beta-2 adrenergic receptorCompound was tested for the antagonistic activity against Beta-2 adrenergic receptor
ChEMBL 590 17 5 7 4.3 CCCCCCCCNC(=O)Nc1ccc(S(=O)(=O)N2CCC(CNC[C@H](O)COc3ccc(O)cc3)CC2)cc1 10.1016/s0960-894x(02)00607-8
155528927 170820 0 None 6 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assayAntagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assay
ChEMBL 649 22 5 13 2.1 CC(C)NC[C@H](O)COc1ccccc1CCn1cc(CNCc2cn(CCc3ccccc3OC[C@@H](O)CNC(C)C)nn2)nn1 10.1021/acs.jmedchem.9b00595
CHEMBL4462252 170820 0 None 6 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assayAntagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assay
ChEMBL 649 22 5 13 2.1 CC(C)NC[C@H](O)COc1ccccc1CCn1cc(CNCc2cn(CCc3ccccc3OC[C@@H](O)CNC(C)C)nn2)nn1 10.1021/acs.jmedchem.9b00595
44267518 13198 1 None -1 2 Dog 4.4 pIC50 = 4.4 Functional
Beta2-receptor selectivity in canine lung tissue in anesthetized dogsBeta2-receptor selectivity in canine lung tissue in anesthetized dogs
ChEMBL 446 12 3 8 1.7 CS(=O)(=O)Nc1ccc(OC[C@H](O)CNCCOc2ccc(-n3ccnc3)cc2)cc1 10.1021/jm00172a033
CHEMBL1192069 13198 1 None -1 2 Dog 4.4 pIC50 = 4.4 Functional
Beta2-receptor selectivity in canine lung tissue in anesthetized dogsBeta2-receptor selectivity in canine lung tissue in anesthetized dogs
ChEMBL 446 12 3 8 1.7 CS(=O)(=O)Nc1ccc(OC[C@H](O)CNCCOc2ccc(-n3ccnc3)cc2)cc1 10.1021/jm00172a033
CHEMBL543251 13198 1 None -1 2 Dog 4.4 pIC50 = 4.4 Functional
Beta2-receptor selectivity in canine lung tissue in anesthetized dogsBeta2-receptor selectivity in canine lung tissue in anesthetized dogs
ChEMBL 446 12 3 8 1.7 CS(=O)(=O)Nc1ccc(OC[C@H](O)CNCCOc2ccc(-n3ccnc3)cc2)cc1 10.1021/jm00172a033
14739906 205943 0 None -16 2 Dog 5.4 pIC50 = 5.4 Functional
Beta2-receptor selectivity in canine lung tissue in anesthetized dogsBeta2-receptor selectivity in canine lung tissue in anesthetized dogs
ChEMBL 411 13 2 7 2.5 COCCc1ccc(OCC(O)CNCCOc2ccc(-n3ccnc3)cc2)cc1 10.1021/jm00172a033
CHEMBL95457 205943 0 None -16 2 Dog 5.4 pIC50 = 5.4 Functional
Beta2-receptor selectivity in canine lung tissue in anesthetized dogsBeta2-receptor selectivity in canine lung tissue in anesthetized dogs
ChEMBL 411 13 2 7 2.5 COCCc1ccc(OCC(O)CNCCOc2ccc(-n3ccnc3)cc2)cc1 10.1021/jm00172a033
13208878 160681 0 None 5 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assayAntagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assay
ChEMBL 520 20 4 9 2.6 CC(C)NC[C@H](O)COc1ccccc1OCCOCCOc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
CHEMBL41189 160681 0 None 5 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assayAntagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assay
ChEMBL 520 20 4 9 2.6 CC(C)NC[C@H](O)COc1ccccc1OCCOCCOc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
130400 206634 9 None -19 2 Dog 4.3 pIC50 = 4.3 Functional
Beta2-receptor selectivity in canine lung tissue in anesthetized dogsBeta2-receptor selectivity in canine lung tissue in anesthetized dogs
ChEMBL 446 12 3 8 1.7 CS(=O)(=O)Nc1ccc(OCC(O)CNCCOc2ccc(-n3ccnc3)cc2)cc1 10.1021/jm00172a033
CHEMBL552615 206634 9 None -19 2 Dog 4.3 pIC50 = 4.3 Functional
Beta2-receptor selectivity in canine lung tissue in anesthetized dogsBeta2-receptor selectivity in canine lung tissue in anesthetized dogs
ChEMBL 446 12 3 8 1.7 CS(=O)(=O)Nc1ccc(OCC(O)CNCCOc2ccc(-n3ccnc3)cc2)cc1 10.1021/jm00172a033
CHEMBL99585 206634 9 None -19 2 Dog 4.3 pIC50 = 4.3 Functional
Beta2-receptor selectivity in canine lung tissue in anesthetized dogsBeta2-receptor selectivity in canine lung tissue in anesthetized dogs
ChEMBL 446 12 3 8 1.7 CS(=O)(=O)Nc1ccc(OCC(O)CNCCOc2ccc(-n3ccnc3)cc2)cc1 10.1021/jm00172a033
46221396 8455 0 None -1 2 Guinea pig 7.3 pIC50 = 7.3 Functional
Agonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response after 30 minsAgonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response after 30 mins
ChEMBL 364 4 4 4 2.6 Cc1cc2c(cc1C)CC(NC[C@H](O)c1ccc(O)c3[nH]c(=O)ccc13)C2 10.1021/jm100068m
CHEMBL1094483 8455 0 None -1 2 Guinea pig 7.3 pIC50 = 7.3 Functional
Agonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response after 30 minsAgonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response after 30 mins
ChEMBL 364 4 4 4 2.6 Cc1cc2c(cc1C)CC(NC[C@H](O)c1ccc(O)c3[nH]c(=O)ccc13)C2 10.1021/jm100068m
155544582 172798 0 None 5 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) expressed in HEK293 cell assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 15 minsAntagonist activity at beta2 adrenergic receptor (unknown origin) expressed in HEK293 cell assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 15 mins
ChEMBL 528 21 4 6 5.3 CC(C)NC[C@H](O)COc1ccccc1CCCCCCCCc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
CHEMBL4527821 172798 0 None 5 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) expressed in HEK293 cell assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 15 minsAntagonist activity at beta2 adrenergic receptor (unknown origin) expressed in HEK293 cell assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 15 mins
ChEMBL 528 21 4 6 5.3 CC(C)NC[C@H](O)COc1ccccc1CCCCCCCCc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
137 367 47 None 1 4 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assayAntagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assay
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1021/acs.jmedchem.9b00595
2119 367 47 None 1 4 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assayAntagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assay
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1021/acs.jmedchem.9b00595
563 367 47 None 1 4 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assayAntagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assay
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1021/acs.jmedchem.9b00595
66368 367 47 None 1 4 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assayAntagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assay
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1021/acs.jmedchem.9b00595
CHEMBL266195 367 47 None 1 4 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assayAntagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assay
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1021/acs.jmedchem.9b00595
DB00866 367 47 None 1 4 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assayAntagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assay
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1021/acs.jmedchem.9b00595
155539979 172306 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assayAntagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assay
ChEMBL 483 17 4 5 3.0 CC(C)NC[C@H](O)COc1ccccc1CCCC(=O)NCCNC(=O)CCCc1ccccc1 10.1021/acs.jmedchem.9b00595
CHEMBL4515576 172306 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assayAntagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assay
ChEMBL 483 17 4 5 3.0 CC(C)NC[C@H](O)COc1ccccc1CCCC(=O)NCCNC(=O)CCCc1ccccc1 10.1021/acs.jmedchem.9b00595
165193 3126 60 None 6 13 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human beta2 receptor expressed in CHO-K1 cells assessed as isoproterenol-induced cAMP level by HTRF assayAntagonist activity at human beta2 receptor expressed in CHO-K1 cells assessed as isoproterenol-induced cAMP level by HTRF assay
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/acs.jmedchem.5b01088
2303 3126 60 None 6 13 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human beta2 receptor expressed in CHO-K1 cells assessed as isoproterenol-induced cAMP level by HTRF assayAntagonist activity at human beta2 receptor expressed in CHO-K1 cells assessed as isoproterenol-induced cAMP level by HTRF assay
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/acs.jmedchem.5b01088
4946 3126 60 None 6 13 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human beta2 receptor expressed in CHO-K1 cells assessed as isoproterenol-induced cAMP level by HTRF assayAntagonist activity at human beta2 receptor expressed in CHO-K1 cells assessed as isoproterenol-induced cAMP level by HTRF assay
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/acs.jmedchem.5b01088
564 3126 60 None 6 13 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human beta2 receptor expressed in CHO-K1 cells assessed as isoproterenol-induced cAMP level by HTRF assayAntagonist activity at human beta2 receptor expressed in CHO-K1 cells assessed as isoproterenol-induced cAMP level by HTRF assay
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/acs.jmedchem.5b01088
62882 3126 60 None 6 13 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human beta2 receptor expressed in CHO-K1 cells assessed as isoproterenol-induced cAMP level by HTRF assayAntagonist activity at human beta2 receptor expressed in CHO-K1 cells assessed as isoproterenol-induced cAMP level by HTRF assay
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/acs.jmedchem.5b01088
63 3126 60 None 6 13 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human beta2 receptor expressed in CHO-K1 cells assessed as isoproterenol-induced cAMP level by HTRF assayAntagonist activity at human beta2 receptor expressed in CHO-K1 cells assessed as isoproterenol-induced cAMP level by HTRF assay
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/acs.jmedchem.5b01088
66366 3126 60 None 6 13 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human beta2 receptor expressed in CHO-K1 cells assessed as isoproterenol-induced cAMP level by HTRF assayAntagonist activity at human beta2 receptor expressed in CHO-K1 cells assessed as isoproterenol-induced cAMP level by HTRF assay
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/acs.jmedchem.5b01088
91536 3126 60 None 6 13 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human beta2 receptor expressed in CHO-K1 cells assessed as isoproterenol-induced cAMP level by HTRF assayAntagonist activity at human beta2 receptor expressed in CHO-K1 cells assessed as isoproterenol-induced cAMP level by HTRF assay
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/acs.jmedchem.5b01088
CHEMBL27 3126 60 None 6 13 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human beta2 receptor expressed in CHO-K1 cells assessed as isoproterenol-induced cAMP level by HTRF assayAntagonist activity at human beta2 receptor expressed in CHO-K1 cells assessed as isoproterenol-induced cAMP level by HTRF assay
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/acs.jmedchem.5b01088
CHEMBL452861 3126 60 None 6 13 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human beta2 receptor expressed in CHO-K1 cells assessed as isoproterenol-induced cAMP level by HTRF assayAntagonist activity at human beta2 receptor expressed in CHO-K1 cells assessed as isoproterenol-induced cAMP level by HTRF assay
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/acs.jmedchem.5b01088
DB00571 3126 60 None 6 13 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human beta2 receptor expressed in CHO-K1 cells assessed as isoproterenol-induced cAMP level by HTRF assayAntagonist activity at human beta2 receptor expressed in CHO-K1 cells assessed as isoproterenol-induced cAMP level by HTRF assay
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/acs.jmedchem.5b01088
208932 13431 8 None -43 2 Dog 4.3 pIC50 = 4.3 Functional
Beta2-receptor selectivity in canine lung tissue in anesthetized dogsBeta2-receptor selectivity in canine lung tissue in anesthetized dogs
ChEMBL 446 12 3 8 1.7 CS(=O)(=O)Nc1ccc(OC[C@@H](O)CNCCOc2ccc(-n3ccnc3)cc2)cc1 10.1021/jm00172a033
CHEMBL1193886 13431 8 None -43 2 Dog 4.3 pIC50 = 4.3 Functional
Beta2-receptor selectivity in canine lung tissue in anesthetized dogsBeta2-receptor selectivity in canine lung tissue in anesthetized dogs
ChEMBL 446 12 3 8 1.7 CS(=O)(=O)Nc1ccc(OC[C@@H](O)CNCCOc2ccc(-n3ccnc3)cc2)cc1 10.1021/jm00172a033
CHEMBL545363 13431 8 None -43 2 Dog 4.3 pIC50 = 4.3 Functional
Beta2-receptor selectivity in canine lung tissue in anesthetized dogsBeta2-receptor selectivity in canine lung tissue in anesthetized dogs
ChEMBL 446 12 3 8 1.7 CS(=O)(=O)Nc1ccc(OC[C@@H](O)CNCCOc2ccc(-n3ccnc3)cc2)cc1 10.1021/jm00172a033
127034966 135991 0 None 1 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human beta2 receptor expressed in CHO-K1 cells assessed as isoproterenol-induced cAMP level by HTRF assayAntagonist activity at human beta2 receptor expressed in CHO-K1 cells assessed as isoproterenol-induced cAMP level by HTRF assay
ChEMBL 260 5 2 4 1.6 CB1C=Cc2cccc(OCC(O)CN(C)C)c2N1 10.1021/acs.jmedchem.5b01088
CHEMBL3736433 135991 0 None 1 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human beta2 receptor expressed in CHO-K1 cells assessed as isoproterenol-induced cAMP level by HTRF assayAntagonist activity at human beta2 receptor expressed in CHO-K1 cells assessed as isoproterenol-induced cAMP level by HTRF assay
ChEMBL 260 5 2 4 1.6 CB1C=Cc2cccc(OCC(O)CN(C)C)c2N1 10.1021/acs.jmedchem.5b01088
14739907 163570 0 None -1 2 Dog 6.3 pIC50 = 6.3 Functional
Beta2-receptor selectivity in canine lung tissue in anesthetized dogsBeta2-receptor selectivity in canine lung tissue in anesthetized dogs
ChEMBL 367 10 2 6 2.6 Cc1cccc(OCC(O)CNCCOc2ccc(-n3ccnc3)cc2)c1 10.1021/jm00172a033
CHEMBL421005 163570 0 None -1 2 Dog 6.3 pIC50 = 6.3 Functional
Beta2-receptor selectivity in canine lung tissue in anesthetized dogsBeta2-receptor selectivity in canine lung tissue in anesthetized dogs
ChEMBL 367 10 2 6 2.6 Cc1cccc(OCC(O)CNCCOc2ccc(-n3ccnc3)cc2)c1 10.1021/jm00172a033
11611195 13325 0 None -70 3 Rat 6.3 pIC50 = 6.3 Functional
Inhibition of spontaneous contractions in isolated rat uterusInhibition of spontaneous contractions in isolated rat uterus
ChEMBL 407 10 3 6 3.2 CCOC(=O)COc1ccc(CCNC(C)C(O)c2ccc(O)cc2)cc1Cl 10.1021/jm020177z
CHEMBL1193081 13325 0 None -70 3 Rat 6.3 pIC50 = 6.3 Functional
Inhibition of spontaneous contractions in isolated rat uterusInhibition of spontaneous contractions in isolated rat uterus
ChEMBL 407 10 3 6 3.2 CCOC(=O)COc1ccc(CCNC(C)C(O)c2ccc(O)cc2)cc1Cl 10.1021/jm020177z
CHEMBL544427 13325 0 None -70 3 Rat 6.3 pIC50 = 6.3 Functional
Inhibition of spontaneous contractions in isolated rat uterusInhibition of spontaneous contractions in isolated rat uterus
ChEMBL 407 10 3 6 3.2 CCOC(=O)COc1ccc(CCNC(C)C(O)c2ccc(O)cc2)cc1Cl 10.1021/jm020177z
11611195 13325 0 None -70 3 Dog 6.3 pIC50 = 6.3 Functional
Agonistic activity for Beta-2 adrenergic receptor was assessed by it's inhibitory effect on spontaneous contractions in isolated rat uterusAgonistic activity for Beta-2 adrenergic receptor was assessed by it's inhibitory effect on spontaneous contractions in isolated rat uterus
ChEMBL 407 10 3 6 3.2 CCOC(=O)COc1ccc(CCNC(C)C(O)c2ccc(O)cc2)cc1Cl 10.1021/jm020177z
CHEMBL1193081 13325 0 None -70 3 Dog 6.3 pIC50 = 6.3 Functional
Agonistic activity for Beta-2 adrenergic receptor was assessed by it's inhibitory effect on spontaneous contractions in isolated rat uterusAgonistic activity for Beta-2 adrenergic receptor was assessed by it's inhibitory effect on spontaneous contractions in isolated rat uterus
ChEMBL 407 10 3 6 3.2 CCOC(=O)COc1ccc(CCNC(C)C(O)c2ccc(O)cc2)cc1Cl 10.1021/jm020177z
CHEMBL544427 13325 0 None -70 3 Dog 6.3 pIC50 = 6.3 Functional
Agonistic activity for Beta-2 adrenergic receptor was assessed by it's inhibitory effect on spontaneous contractions in isolated rat uterusAgonistic activity for Beta-2 adrenergic receptor was assessed by it's inhibitory effect on spontaneous contractions in isolated rat uterus
ChEMBL 407 10 3 6 3.2 CCOC(=O)COc1ccc(CCNC(C)C(O)c2ccc(O)cc2)cc1Cl 10.1021/jm020177z
24936488 17452 0 None -275 3 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as inhibition of isoproterenol-induced cyclic AMP formation by HTRF assayAntagonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as inhibition of isoproterenol-induced cyclic AMP formation by HTRF assay
ChEMBL 414 7 3 8 2.7 Cc1csc2ncnc(N3CCC(NCC(O)COc4ccc(O)cc4)CC3)c12 10.1016/j.bmcl.2010.08.039
CHEMBL1258373 17452 0 None -275 3 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as inhibition of isoproterenol-induced cyclic AMP formation by HTRF assayAntagonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as inhibition of isoproterenol-induced cyclic AMP formation by HTRF assay
ChEMBL 414 7 3 8 2.7 Cc1csc2ncnc(N3CCC(NCC(O)COc4ccc(O)cc4)CC3)c12 10.1016/j.bmcl.2010.08.039
14739908 106749 0 None -1 2 Dog 5.2 pIC50 = 5.2 Functional
Beta2-receptor selectivity in canine lung tissue in anesthetized dogsBeta2-receptor selectivity in canine lung tissue in anesthetized dogs
ChEMBL 416 10 3 7 1.9 CS(=O)(=O)Nc1ccc(C(O)CNCCOc2ccc(-n3ccnc3)cc2)cc1 10.1021/jm00172a033
CHEMBL316868 106749 0 None -1 2 Dog 5.2 pIC50 = 5.2 Functional
Beta2-receptor selectivity in canine lung tissue in anesthetized dogsBeta2-receptor selectivity in canine lung tissue in anesthetized dogs
ChEMBL 416 10 3 7 1.9 CS(=O)(=O)Nc1ccc(C(O)CNCCOc2ccc(-n3ccnc3)cc2)cc1 10.1021/jm00172a033
156009636 176581 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at ADRB2 endogenously expressed in HEK293 cells transfected with cAMP FRET biosensor assessed as inhibition of cimaterol-induced response pre-incubated for 45 mins under dark conditions by FRET assayAntagonist activity at ADRB2 endogenously expressed in HEK293 cells transfected with cAMP FRET biosensor assessed as inhibition of cimaterol-induced response pre-incubated for 45 mins under dark conditions by FRET assay
ChEMBL 370 9 3 6 3.8 CC(=O)Nc1ccc(/N=N/c2cccc(OC[C@@H](O)CNC(C)C)c2)cc1 10.1021/acs.jmedchem.0c00831
CHEMBL4634403 176581 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at ADRB2 endogenously expressed in HEK293 cells transfected with cAMP FRET biosensor assessed as inhibition of cimaterol-induced response pre-incubated for 45 mins under dark conditions by FRET assayAntagonist activity at ADRB2 endogenously expressed in HEK293 cells transfected with cAMP FRET biosensor assessed as inhibition of cimaterol-induced response pre-incubated for 45 mins under dark conditions by FRET assay
ChEMBL 370 9 3 6 3.8 CC(=O)Nc1ccc(/N=N/c2cccc(OC[C@@H](O)CNC(C)C)c2)cc1 10.1021/acs.jmedchem.0c00831
10915880 76878 0 None -10 3 Dog 4.2 pIC50 = 4.2 Functional
Agonistic activity for Beta-2 adrenergic receptor was assessed by it's inhibitory effect on spontaneous contractions in isolated rat uterusAgonistic activity for Beta-2 adrenergic receptor was assessed by it's inhibitory effect on spontaneous contractions in isolated rat uterus
ChEMBL 379 9 4 5 2.8 C[C@@H](NCCc1ccc(OCC(=O)O)c(Cl)c1)[C@H](O)c1ccc(O)cc1 10.1021/jm020177z
CHEMBL2079599 76878 0 None -10 3 Dog 4.2 pIC50 = 4.2 Functional
Agonistic activity for Beta-2 adrenergic receptor was assessed by it's inhibitory effect on spontaneous contractions in isolated rat uterusAgonistic activity for Beta-2 adrenergic receptor was assessed by it's inhibitory effect on spontaneous contractions in isolated rat uterus
ChEMBL 379 9 4 5 2.8 C[C@@H](NCCc1ccc(OCC(=O)O)c(Cl)c1)[C@H](O)c1ccc(O)cc1 10.1021/jm020177z
5581 101175 10 None -2 6 Human 8.2 pIC50 = 8.2 Functional
Compound was evaluated for its inhibitory activity against CHO cells expressing the cloned human beta-2 adrenergic receptor (AR) in the presence of [125I]-iodocyanopindololCompound was evaluated for its inhibitory activity against CHO cells expressing the cloned human beta-2 adrenergic receptor (AR) in the presence of [125I]-iodocyanopindolol
ChEMBL 345 5 3 6 2.6 COc1cc(CC2NCCc3cc(O)c(O)cc32)cc(OC)c1OC 10.1016/s0960-894x(00)00459-5
CHEMBL299175 101175 10 None -2 6 Human 8.2 pIC50 = 8.2 Functional
Compound was evaluated for its inhibitory activity against CHO cells expressing the cloned human beta-2 adrenergic receptor (AR) in the presence of [125I]-iodocyanopindololCompound was evaluated for its inhibitory activity against CHO cells expressing the cloned human beta-2 adrenergic receptor (AR) in the presence of [125I]-iodocyanopindolol
ChEMBL 345 5 3 6 2.6 COc1cc(CC2NCCc3cc(O)c(O)cc32)cc(OC)c1OC 10.1016/s0960-894x(00)00459-5
155515823 169445 0 None 24 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) expressed in HEK293 cell assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 15 minsAntagonist activity at beta2 adrenergic receptor (unknown origin) expressed in HEK293 cell assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 15 mins
ChEMBL 621 20 5 13 1.7 CC(C)NC[C@H](O)COc1ccccc1Cn1cc(CNCc2cn(Cc3ccccc3OC[C@@H](O)CNC(C)C)nn2)nn1 10.1021/acs.jmedchem.9b00595
CHEMBL4442559 169445 0 None 24 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) expressed in HEK293 cell assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 15 minsAntagonist activity at beta2 adrenergic receptor (unknown origin) expressed in HEK293 cell assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 15 mins
ChEMBL 621 20 5 13 1.7 CC(C)NC[C@H](O)COc1ccccc1Cn1cc(CNCc2cn(Cc3ccccc3OC[C@@H](O)CNC(C)C)nn2)nn1 10.1021/acs.jmedchem.9b00595
155565922 175209 0 None 4 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assayAntagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assay
ChEMBL 628 24 6 8 3.1 CC(C)NC[C@H](O)COc1ccccc1CCCC(=O)NCCCNC(=O)CCCc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
CHEMBL4584173 175209 0 None 4 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assayAntagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assay
ChEMBL 628 24 6 8 3.1 CC(C)NC[C@H](O)COc1ccccc1CCCC(=O)NCCCNC(=O)CCCc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
155569481 175632 0 None 8 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assayAntagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assay
ChEMBL 614 23 6 8 2.7 CC(C)NC[C@H](O)COc1ccccc1CCCC(=O)NCCNC(=O)CCCc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
CHEMBL4594173 175632 0 None 8 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assayAntagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assay
ChEMBL 614 23 6 8 2.7 CC(C)NC[C@H](O)COc1ccccc1CCCC(=O)NCCNC(=O)CCCc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
145990586 166279 0 None 1 3 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human beta2-adrenergic receptor expressed in CHO-K1 cells assessed as decrease in procaterol-induced cAMP accumulation after 20 mins by HTRF assayAntagonist activity at human beta2-adrenergic receptor expressed in CHO-K1 cells assessed as decrease in procaterol-induced cAMP accumulation after 20 mins by HTRF assay
ChEMBL 297 2 2 4 2.6 COc1cc2c3c(c1OC)-c1ccccc1[C@@H](O)[C@@H]3NCC2 10.1039/C7MD00656J
CHEMBL4285281 166279 0 None 1 3 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human beta2-adrenergic receptor expressed in CHO-K1 cells assessed as decrease in procaterol-induced cAMP accumulation after 20 mins by HTRF assayAntagonist activity at human beta2-adrenergic receptor expressed in CHO-K1 cells assessed as decrease in procaterol-induced cAMP accumulation after 20 mins by HTRF assay
ChEMBL 297 2 2 4 2.6 COc1cc2c3c(c1OC)-c1ccccc1[C@@H](O)[C@@H]3NCC2 10.1039/C7MD00656J
155515551 169398 0 None 1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assayAntagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assay
ChEMBL 584 25 4 6 6.8 CC(C)NC[C@H](O)COc1ccccc1CCCCCCCCCCCCc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
CHEMBL4441975 169398 0 None 1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assayAntagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assay
ChEMBL 584 25 4 6 6.8 CC(C)NC[C@H](O)COc1ccccc1CCCCCCCCCCCCc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
10915880 76878 0 None -10 3 Rat 4.2 pIC50 = 4.2 Functional
Inhibition of spontaneous contractions in isolated rat uterusInhibition of spontaneous contractions in isolated rat uterus
ChEMBL 379 9 4 5 2.8 C[C@@H](NCCc1ccc(OCC(=O)O)c(Cl)c1)[C@H](O)c1ccc(O)cc1 10.1021/jm020177z
CHEMBL2079599 76878 0 None -10 3 Rat 4.2 pIC50 = 4.2 Functional
Inhibition of spontaneous contractions in isolated rat uterusInhibition of spontaneous contractions in isolated rat uterus
ChEMBL 379 9 4 5 2.8 C[C@@H](NCCc1ccc(OCC(=O)O)c(Cl)c1)[C@H](O)c1ccc(O)cc1 10.1021/jm020177z
10809699 111833 0 None -8 2 Rat 7.2 pIC50 = 7.2 Functional
Agonistic activity towards beta-2 adrenoceptor. Mean concentration required to produce 50% inhibition of uterine contractionAgonistic activity towards beta-2 adrenoceptor. Mean concentration required to produce 50% inhibition of uterine contraction
ChEMBL 378 9 5 5 2.8 C[C@H](NCCc1ccc(NCC(=O)O)cc1Cl)[C@H](O)c1ccc(O)cc1 10.1021/jm000455z
CHEMBL32933 111833 0 None -8 2 Rat 7.2 pIC50 = 7.2 Functional
Agonistic activity towards beta-2 adrenoceptor. Mean concentration required to produce 50% inhibition of uterine contractionAgonistic activity towards beta-2 adrenoceptor. Mean concentration required to produce 50% inhibition of uterine contraction
ChEMBL 378 9 5 5 2.8 C[C@H](NCCc1ccc(NCC(=O)O)cc1Cl)[C@H](O)c1ccc(O)cc1 10.1021/jm000455z
155515823 169445 0 None 24 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assayAntagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assay
ChEMBL 621 20 5 13 1.7 CC(C)NC[C@H](O)COc1ccccc1Cn1cc(CNCc2cn(Cc3ccccc3OC[C@@H](O)CNC(C)C)nn2)nn1 10.1021/acs.jmedchem.9b00595
CHEMBL4442559 169445 0 None 24 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assayAntagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assay
ChEMBL 621 20 5 13 1.7 CC(C)NC[C@H](O)COc1ccccc1Cn1cc(CNCc2cn(Cc3ccccc3OC[C@@H](O)CNC(C)C)nn2)nn1 10.1021/acs.jmedchem.9b00595
155564992 174933 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assayAntagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assay
ChEMBL 407 15 4 5 1.8 CCCC(=O)NCCNC(=O)CCCc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
CHEMBL4578042 174933 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assayAntagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assay
ChEMBL 407 15 4 5 1.8 CCCC(=O)NCCNC(=O)CCCc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
11810992 25888 0 None -1698 3 Rat 5.2 pIC50 = 5.2 Functional
Inhibition of spontaneous contractions in isolated rat uterusInhibition of spontaneous contractions in isolated rat uterus
ChEMBL 379 9 4 5 2.8 C[C@@H](NCCc1ccc(OCC(=O)O)c(Cl)c1)[C@@H](O)c1ccc(O)cc1 10.1021/jm020177z
CHEMBL13560 25888 0 None -1698 3 Rat 5.2 pIC50 = 5.2 Functional
Inhibition of spontaneous contractions in isolated rat uterusInhibition of spontaneous contractions in isolated rat uterus
ChEMBL 379 9 4 5 2.8 C[C@@H](NCCc1ccc(OCC(=O)O)c(Cl)c1)[C@@H](O)c1ccc(O)cc1 10.1021/jm020177z
11791723 110063 0 None -26 2 Rat 6.2 pIC50 = 6.2 Functional
Agonistic activity towards beta-2 adrenoceptor. Mean concentration required to produce 50% inhibition of uterine contractionAgonistic activity towards beta-2 adrenoceptor. Mean concentration required to produce 50% inhibition of uterine contraction
ChEMBL 344 9 5 5 2.1 C[C@H](NCCc1ccc(NCC(=O)O)cc1)[C@H](O)c1ccc(O)cc1 10.1021/jm000455z
CHEMBL32532 110063 0 None -26 2 Rat 6.2 pIC50 = 6.2 Functional
Agonistic activity towards beta-2 adrenoceptor. Mean concentration required to produce 50% inhibition of uterine contractionAgonistic activity towards beta-2 adrenoceptor. Mean concentration required to produce 50% inhibition of uterine contraction
ChEMBL 344 9 5 5 2.1 C[C@H](NCCc1ccc(NCC(=O)O)cc1)[C@H](O)c1ccc(O)cc1 10.1021/jm000455z
11810992 25888 0 None -1698 3 Dog 5.2 pIC50 = 5.2 Functional
Agonistic activity for Beta-2 adrenergic receptor was assessed by it's inhibitory effect on spontaneous contractions in isolated rat uterusAgonistic activity for Beta-2 adrenergic receptor was assessed by it's inhibitory effect on spontaneous contractions in isolated rat uterus
ChEMBL 379 9 4 5 2.8 C[C@@H](NCCc1ccc(OCC(=O)O)c(Cl)c1)[C@@H](O)c1ccc(O)cc1 10.1021/jm020177z
CHEMBL13560 25888 0 None -1698 3 Dog 5.2 pIC50 = 5.2 Functional
Agonistic activity for Beta-2 adrenergic receptor was assessed by it's inhibitory effect on spontaneous contractions in isolated rat uterusAgonistic activity for Beta-2 adrenergic receptor was assessed by it's inhibitory effect on spontaneous contractions in isolated rat uterus
ChEMBL 379 9 4 5 2.8 C[C@@H](NCCc1ccc(OCC(=O)O)c(Cl)c1)[C@@H](O)c1ccc(O)cc1 10.1021/jm020177z
155518547 169712 0 None 107 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assayAntagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assay
ChEMBL 558 20 6 7 3.0 CC(C)NC[C@H](O)COc1ccccc1CCCNC(=O)NCCCc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
CHEMBL4446394 169712 0 None 107 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assayAntagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assay
ChEMBL 558 20 6 7 3.0 CC(C)NC[C@H](O)COc1ccccc1CCCNC(=O)NCCCc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
4183 1986 62 None -2 4 Guinea pig 8.1 pIC50 = 8.1 Functional
Agonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response after 30 minsAgonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response after 30 mins
ChEMBL 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O 10.1021/jm100068m
6918554 1986 62 None -2 4 Guinea pig 8.1 pIC50 = 8.1 Functional
Agonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response after 30 minsAgonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response after 30 mins
ChEMBL 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O 10.1021/jm100068m
7455 1986 62 None -2 4 Guinea pig 8.1 pIC50 = 8.1 Functional
Agonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response after 30 minsAgonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response after 30 mins
ChEMBL 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O 10.1021/jm100068m
CHEMBL1095777 1986 62 None -2 4 Guinea pig 8.1 pIC50 = 8.1 Functional
Agonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response after 30 minsAgonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response after 30 mins
ChEMBL 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O 10.1021/jm100068m
DB05039 1986 62 None -2 4 Guinea pig 8.1 pIC50 = 8.1 Functional
Agonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response after 30 minsAgonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response after 30 mins
ChEMBL 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O 10.1021/jm100068m
13208884 174053 0 None 1 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assayAntagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assay
ChEMBL 564 23 4 10 2.7 CC(C)NC[C@H](O)COc1ccccc1OCCOCCOCCOc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
CHEMBL4557995 174053 0 None 1 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assayAntagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assay
ChEMBL 564 23 4 10 2.7 CC(C)NC[C@H](O)COc1ccccc1OCCOCCOCCOc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
46221604 8457 0 None 1 2 Guinea pig 7.1 pIC50 = 7.1 Functional
Agonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response after 30 minsAgonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response after 30 mins
ChEMBL 392 6 4 4 3.1 CCc1ccc(CC)c2c1CC(NC[C@H](O)c1ccc(O)c3[nH]c(=O)ccc13)C2 10.1021/jm100068m
CHEMBL1094487 8457 0 None 1 2 Guinea pig 7.1 pIC50 = 7.1 Functional
Agonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response after 30 minsAgonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response after 30 mins
ChEMBL 392 6 4 4 3.1 CCc1ccc(CC)c2c1CC(NC[C@H](O)c1ccc(O)c3[nH]c(=O)ccc13)C2 10.1021/jm100068m
203685 30526 8 None 33 4 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assayAntagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assay
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OC[C@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
CHEMBL1395661 30526 8 None 33 4 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assayAntagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assay
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OC[C@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
155521390 170010 0 None 128 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assayAntagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assay
ChEMBL 586 21 6 8 2.0 CC(C)NC[C@H](O)COc1ccccc1CCC(=O)NCCNC(=O)CCc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
CHEMBL4450606 170010 0 None 128 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assayAntagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assay
ChEMBL 586 21 6 8 2.0 CC(C)NC[C@H](O)COc1ccccc1CCC(=O)NCCNC(=O)CCc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
53318280 58332 0 None -70 3 Human 6.1 pIC50 = 6.1 Functional
Agonist activity at human beta2 adrenergic receptorAgonist activity at human beta2 adrenergic receptor
ChEMBL 623 11 3 6 7.2 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2ccccc2)cc1)c1ccc(-c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1016/j.bmcl.2010.12.087
CHEMBL1684578 58332 0 None -70 3 Human 6.1 pIC50 = 6.1 Functional
Agonist activity at human beta2 adrenergic receptorAgonist activity at human beta2 adrenergic receptor
ChEMBL 623 11 3 6 7.2 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2ccccc2)cc1)c1ccc(-c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1016/j.bmcl.2010.12.087
155527605 170669 0 None 213 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assayAntagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assay
ChEMBL 600 22 6 8 2.4 CC(C)NC[C@H](O)COc1ccccc1CCC(=O)NCCCNC(=O)CCc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
CHEMBL4459989 170669 0 None 213 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assayAntagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assay
ChEMBL 600 22 6 8 2.4 CC(C)NC[C@H](O)COc1ccccc1CCC(=O)NCCCNC(=O)CCc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
155532901 171235 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assayAntagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assay
ChEMBL 351 12 4 4 2.1 CCCNC(=O)NCCCc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
CHEMBL4468271 171235 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assayAntagonist activity at beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assay
ChEMBL 351 12 4 4 2.1 CCCNC(=O)NCCCc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
52947562 17490 0 None -173 3 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as inhibition of isoproterenol-induced cyclic AMP formation by HTRF assayAntagonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as inhibition of isoproterenol-induced cyclic AMP formation by HTRF assay
ChEMBL 384 7 2 7 2.7 OC(CNC1CCN(c2ncnc3sccc23)CC1)COc1ccccc1 10.1016/j.bmcl.2010.08.039
CHEMBL1258486 17490 0 None -173 3 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as inhibition of isoproterenol-induced cyclic AMP formation by HTRF assayAntagonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as inhibition of isoproterenol-induced cyclic AMP formation by HTRF assay
ChEMBL 384 7 2 7 2.7 OC(CNC1CCN(c2ncnc3sccc23)CC1)COc1ccccc1 10.1016/j.bmcl.2010.08.039
567 715 10 None -25 7 Rat 8.0 pIC50 = 8.0 Functional
Inhibition of spontaneous contractions in isolated rat uterusInhibition of spontaneous contractions in isolated rat uterus
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1021/jm020177z
9841972 715 10 None -25 7 Rat 8.0 pIC50 = 8.0 Functional
Inhibition of spontaneous contractions in isolated rat uterusInhibition of spontaneous contractions in isolated rat uterus
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1021/jm020177z
CHEMBL284782 715 10 None -25 7 Rat 8.0 pIC50 = 8.0 Functional
Inhibition of spontaneous contractions in isolated rat uterusInhibition of spontaneous contractions in isolated rat uterus
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1021/jm020177z
567 715 10 None -2 7 Dog 8.0 pIC50 = 8.0 Functional
Agonistic activity for Beta-2 adrenergic receptor was assessed by it's inhibitory effect on spontaneous contractions in isolated rat uterusAgonistic activity for Beta-2 adrenergic receptor was assessed by it's inhibitory effect on spontaneous contractions in isolated rat uterus
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1021/jm020177z
9841972 715 10 None -2 7 Dog 8.0 pIC50 = 8.0 Functional
Agonistic activity for Beta-2 adrenergic receptor was assessed by it's inhibitory effect on spontaneous contractions in isolated rat uterusAgonistic activity for Beta-2 adrenergic receptor was assessed by it's inhibitory effect on spontaneous contractions in isolated rat uterus
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1021/jm020177z
CHEMBL284782 715 10 None -2 7 Dog 8.0 pIC50 = 8.0 Functional
Agonistic activity for Beta-2 adrenergic receptor was assessed by it's inhibitory effect on spontaneous contractions in isolated rat uterusAgonistic activity for Beta-2 adrenergic receptor was assessed by it's inhibitory effect on spontaneous contractions in isolated rat uterus
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1021/jm020177z
567 715 10 None -25 7 Rat 8.0 pIC50 = 8.0 Functional
Agonistic activity towards beta-2 adrenoceptor. Mean concentration required to produce 50% inhibition of uterine contractionAgonistic activity towards beta-2 adrenoceptor. Mean concentration required to produce 50% inhibition of uterine contraction
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1021/jm000455z
9841972 715 10 None -25 7 Rat 8.0 pIC50 = 8.0 Functional
Agonistic activity towards beta-2 adrenoceptor. Mean concentration required to produce 50% inhibition of uterine contractionAgonistic activity towards beta-2 adrenoceptor. Mean concentration required to produce 50% inhibition of uterine contraction
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1021/jm000455z
CHEMBL284782 715 10 None -25 7 Rat 8.0 pIC50 = 8.0 Functional
Agonistic activity towards beta-2 adrenoceptor. Mean concentration required to produce 50% inhibition of uterine contractionAgonistic activity towards beta-2 adrenoceptor. Mean concentration required to produce 50% inhibition of uterine contraction
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1021/jm000455z
146015362 932 6 None -17378 5 Rat 5.0 pIC50 = 5.0 Functional
Agonistic activity towards beta-2 adrenoceptor. Mean concentration required to produce 50% inhibition of uterine contractionAgonistic activity towards beta-2 adrenoceptor. Mean concentration required to produce 50% inhibition of uterine contraction
ChEMBL 421 8 4 6 2.2 C[C@H](Cc1ccc2c(c1)OC(O2)(C(=O)O)C(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1021/jm000455z
3462 932 6 None -17378 5 Rat 5.0 pIC50 = 5.0 Functional
Agonistic activity towards beta-2 adrenoceptor. Mean concentration required to produce 50% inhibition of uterine contractionAgonistic activity towards beta-2 adrenoceptor. Mean concentration required to produce 50% inhibition of uterine contraction
ChEMBL 421 8 4 6 2.2 C[C@H](Cc1ccc2c(c1)OC(O2)(C(=O)O)C(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1021/jm000455z
5486546 932 6 None -17378 5 Rat 5.0 pIC50 = 5.0 Functional
Agonistic activity towards beta-2 adrenoceptor. Mean concentration required to produce 50% inhibition of uterine contractionAgonistic activity towards beta-2 adrenoceptor. Mean concentration required to produce 50% inhibition of uterine contraction
ChEMBL 421 8 4 6 2.2 C[C@H](Cc1ccc2c(c1)OC(O2)(C(=O)O)C(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1021/jm000455z
CHEMBL1204876 932 6 None -17378 5 Rat 5.0 pIC50 = 5.0 Functional
Agonistic activity towards beta-2 adrenoceptor. Mean concentration required to produce 50% inhibition of uterine contractionAgonistic activity towards beta-2 adrenoceptor. Mean concentration required to produce 50% inhibition of uterine contraction
ChEMBL 421 8 4 6 2.2 C[C@H](Cc1ccc2c(c1)OC(O2)(C(=O)O)C(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1021/jm000455z
25271869 158073 2 None - 0 Human 10.7 pKd = 10.7 Functional
Partial agonist activity at human beta2-AR expressed in CHOK1 cells assessed as inhibition of cimaterol-induced CRE-SPAP production after 5 hrsPartial agonist activity at human beta2-AR expressed in CHOK1 cells assessed as inhibition of cimaterol-induced CRE-SPAP production after 5 hrs
ChEMBL 299 6 2 3 3.5 CC(C)(C)NC[C@@H](O)COc1ccccc1-c1ccccc1 10.1021/acsmedchemlett.6b00363
CHEMBL4092412 158073 2 None - 0 Human 10.7 pKd = 10.7 Functional
Partial agonist activity at human beta2-AR expressed in CHOK1 cells assessed as inhibition of cimaterol-induced CRE-SPAP production after 5 hrsPartial agonist activity at human beta2-AR expressed in CHOK1 cells assessed as inhibition of cimaterol-induced CRE-SPAP production after 5 hrs
ChEMBL 299 6 2 3 3.5 CC(C)(C)NC[C@@H](O)COc1ccccc1-c1ccccc1 10.1021/acsmedchemlett.6b00363
21595418 102153 0 None - 0 Guinea pig 10.2 pKd = 10.2 Functional
Antagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbacholAntagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbachol
ChEMBL 271 4 2 3 2.7 O[C@H](COc1cccc2ccccc12)[C@@H]1CCCCN1 10.1021/jm00119a011
CHEMBL304344 102153 0 None - 0 Guinea pig 10.2 pKd = 10.2 Functional
Antagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbacholAntagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbachol
ChEMBL 271 4 2 3 2.7 O[C@H](COc1cccc2ccccc12)[C@@H]1CCCCN1 10.1021/jm00119a011
165193 3126 60 None 6 13 Human 9.6 pKd = 9.6 Functional
Antagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm2008562
2303 3126 60 None 6 13 Human 9.6 pKd = 9.6 Functional
Antagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm2008562
4946 3126 60 None 6 13 Human 9.6 pKd = 9.6 Functional
Antagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm2008562
564 3126 60 None 6 13 Human 9.6 pKd = 9.6 Functional
Antagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm2008562
62882 3126 60 None 6 13 Human 9.6 pKd = 9.6 Functional
Antagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm2008562
63 3126 60 None 6 13 Human 9.6 pKd = 9.6 Functional
Antagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm2008562
66366 3126 60 None 6 13 Human 9.6 pKd = 9.6 Functional
Antagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm2008562
91536 3126 60 None 6 13 Human 9.6 pKd = 9.6 Functional
Antagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm2008562
CHEMBL27 3126 60 None 6 13 Human 9.6 pKd = 9.6 Functional
Antagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm2008562
CHEMBL452861 3126 60 None 6 13 Human 9.6 pKd = 9.6 Functional
Antagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm2008562
DB00571 3126 60 None 6 13 Human 9.6 pKd = 9.6 Functional
Antagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm2008562
33624 3749 29 None - 5 Guinea pig 9.6 pKd = 9.6 Functional
Beta-2 adrenergic receptor antagonistic activity on guinea pig tracheal chainsBeta-2 adrenergic receptor antagonistic activity on guinea pig tracheal chains
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C 10.1021/jm00350a009
4061 3749 29 None - 5 Guinea pig 9.6 pKd = 9.6 Functional
Beta-2 adrenergic receptor antagonistic activity on guinea pig tracheal chainsBeta-2 adrenergic receptor antagonistic activity on guinea pig tracheal chains
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C 10.1021/jm00350a009
565 3749 29 None - 5 Guinea pig 9.6 pKd = 9.6 Functional
Beta-2 adrenergic receptor antagonistic activity on guinea pig tracheal chainsBeta-2 adrenergic receptor antagonistic activity on guinea pig tracheal chains
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C 10.1021/jm00350a009
CHEMBL499 3749 29 None - 5 Guinea pig 9.6 pKd = 9.6 Functional
Beta-2 adrenergic receptor antagonistic activity on guinea pig tracheal chainsBeta-2 adrenergic receptor antagonistic activity on guinea pig tracheal chains
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C 10.1021/jm00350a009
DB00373 3749 29 None - 5 Guinea pig 9.6 pKd = 9.6 Functional
Beta-2 adrenergic receptor antagonistic activity on guinea pig tracheal chainsBeta-2 adrenergic receptor antagonistic activity on guinea pig tracheal chains
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C 10.1021/jm00350a009
54756927 65141 0 None - 0 Human 9.6 pKd = 9.6 Functional
Antagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 833 22 4 8 7.5 O=C(CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1)NCCCCNC[C@H](O)COc1cccc2ccccc12 10.1021/jm2008562
CHEMBL1830486 65141 0 None - 0 Human 9.6 pKd = 9.6 Functional
Antagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 833 22 4 8 7.5 O=C(CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1)NCCCCNC[C@H](O)COc1cccc2ccccc12 10.1021/jm2008562
137 367 47 None 1 4 Human 9.5 pKd = 9.5 Functional
Antagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1021/jm2008562
2119 367 47 None 1 4 Human 9.5 pKd = 9.5 Functional
Antagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1021/jm2008562
563 367 47 None 1 4 Human 9.5 pKd = 9.5 Functional
Antagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1021/jm2008562
66368 367 47 None 1 4 Human 9.5 pKd = 9.5 Functional
Antagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1021/jm2008562
CHEMBL266195 367 47 None 1 4 Human 9.5 pKd = 9.5 Functional
Antagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1021/jm2008562
DB00866 367 47 None 1 4 Human 9.5 pKd = 9.5 Functional
Antagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1021/jm2008562
54669764 65146 0 None - 0 Human 9.5 pKd = 9.5 Functional
Antagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 893 26 4 10 6.8 O=C(CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1)NCCOCCOCCNC[C@H](O)COc1cccc2ccccc12 10.1021/jm2008562
CHEMBL1830491 65146 0 None - 0 Human 9.5 pKd = 9.5 Functional
Antagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 893 26 4 10 6.8 O=C(CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1)NCCOCCOCCNC[C@H](O)COc1cccc2ccccc12 10.1021/jm2008562
145948125 167167 0 None - 0 Guinea pig 9.5 pKd = 9.5 Functional
Antagonist activity at adrenergic beta2 receptor in isolated guinea pig trachea assessed as inhibition of isoprenaline-induced bronchodilation incubated for 20 minsAntagonist activity at adrenergic beta2 receptor in isolated guinea pig trachea assessed as inhibition of isoprenaline-induced bronchodilation incubated for 20 mins
ChEMBL 341 5 2 5 3.1 CC(C)(C)NCC(O)COc1cccc2c(=O)c3ccccc3oc12 10.1016/j.bmc.2018.04.038
CHEMBL4129458 167167 0 None - 0 Guinea pig 9.5 pKd = 9.5 Functional
Antagonist activity at adrenergic beta2 receptor in isolated guinea pig trachea assessed as inhibition of isoprenaline-induced bronchodilation incubated for 20 minsAntagonist activity at adrenergic beta2 receptor in isolated guinea pig trachea assessed as inhibition of isoprenaline-induced bronchodilation incubated for 20 mins
ChEMBL 341 5 2 5 3.1 CC(C)(C)NCC(O)COc1cccc2c(=O)c3ccccc3oc12 10.1016/j.bmc.2018.04.038
CHEMBL4302853 167167 0 None - 0 Guinea pig 9.5 pKd = 9.5 Functional
Antagonist activity at adrenergic beta2 receptor in isolated guinea pig trachea assessed as inhibition of isoprenaline-induced bronchodilation incubated for 20 minsAntagonist activity at adrenergic beta2 receptor in isolated guinea pig trachea assessed as inhibition of isoprenaline-induced bronchodilation incubated for 20 mins
ChEMBL 341 5 2 5 3.1 CC(C)(C)NCC(O)COc1cccc2c(=O)c3ccccc3oc12 10.1016/j.bmc.2018.04.038
54758417 65140 0 None - 0 Human 9.4 pKd = 9.4 Functional
Antagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 805 20 4 8 6.7 O=C(CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1)NCCNC[C@H](O)COc1cccc2ccccc12 10.1021/jm2008562
CHEMBL1830485 65140 0 None - 0 Human 9.4 pKd = 9.4 Functional
Antagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 805 20 4 8 6.7 O=C(CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1)NCCNC[C@H](O)COc1cccc2ccccc12 10.1021/jm2008562
54757232 65170 0 None - 0 Human 9.4 pKd = 9.4 Functional
Antagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 883 28 4 10 6.3 C=CCc1ccccc1OC[C@@H](O)CNCCOCCOCCNC(=O)CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1 10.1021/jm2008562
CHEMBL1830618 65170 0 None - 0 Human 9.4 pKd = 9.4 Functional
Antagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 883 28 4 10 6.3 C=CCc1ccccc1OC[C@@H](O)CNCCOCCOCCNC(=O)CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1 10.1021/jm2008562
54757126 65147 0 None - 0 Human 9.4 pKd = 9.4 Functional
Antagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 893 26 4 10 6.8 O=C(CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1)NCCOCCOCCNCC(O)COc1cccc2ccccc12 10.1021/jm2008562
CHEMBL1830492 65147 0 None - 0 Human 9.4 pKd = 9.4 Functional
Antagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 893 26 4 10 6.8 O=C(CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1)NCCOCCOCCNCC(O)COc1cccc2ccccc12 10.1021/jm2008562
54757331 65171 0 None - 0 Human 9.2 pKd = 9.2 Functional
Antagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 883 28 4 10 6.3 C=CCc1ccccc1OCC(O)CNCCOCCOCCNC(=O)CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1 10.1021/jm2008562
CHEMBL1830619 65171 0 None - 0 Human 9.2 pKd = 9.2 Functional
Antagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 883 28 4 10 6.3 C=CCc1ccccc1OCC(O)CNCCOCCOCCNC(=O)CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1 10.1021/jm2008562
2176 3065 66 None 1 6 Human 9.2 pKd = 9.2 Functional
Antagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C 10.1021/jm2008562
4828 3065 66 None 1 6 Human 9.2 pKd = 9.2 Functional
Antagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C 10.1021/jm2008562
91 3065 66 None 1 6 Human 9.2 pKd = 9.2 Functional
Antagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C 10.1021/jm2008562
CHEMBL500 3065 66 None 1 6 Human 9.2 pKd = 9.2 Functional
Antagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C 10.1021/jm2008562
DB00960 3065 66 None 1 6 Human 9.2 pKd = 9.2 Functional
Antagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C 10.1021/jm2008562
57334265 70499 0 None - 1 Guinea pig 9.2 pKd = 9.2 Functional
Competitive antagonist activity at beta2-adrenoceptor in guinea pig tracheal ring in the presence of N-(5-((1R)-2-(4-(4-(3,4-dimethoxyphenol)-1-oxo-4a,5,6,7,8,8a-hexahydrophthalazin-2(1H)-yl)butylamino-1-hydroxyethyl)-2-hydroxyphenyl)formamideCompetitive antagonist activity at beta2-adrenoceptor in guinea pig tracheal ring in the presence of N-(5-((1R)-2-(4-(4-(3,4-dimethoxyphenol)-1-oxo-4a,5,6,7,8,8a-hexahydrophthalazin-2(1H)-yl)butylamino-1-hydroxyethyl)-2-hydroxyphenyl)formamide
ChEMBL 538 13 4 8 3.4 COc1ccc(C2=NN(CCCCNC[C@H](O)c3ccc(O)c(NC=O)c3)C(=O)C3CCCCC23)cc1OC 10.1016/j.bmcl.2012.01.013
CHEMBL1951067 70499 0 None - 1 Guinea pig 9.2 pKd = 9.2 Functional
Competitive antagonist activity at beta2-adrenoceptor in guinea pig tracheal ring in the presence of N-(5-((1R)-2-(4-(4-(3,4-dimethoxyphenol)-1-oxo-4a,5,6,7,8,8a-hexahydrophthalazin-2(1H)-yl)butylamino-1-hydroxyethyl)-2-hydroxyphenyl)formamideCompetitive antagonist activity at beta2-adrenoceptor in guinea pig tracheal ring in the presence of N-(5-((1R)-2-(4-(4-(3,4-dimethoxyphenol)-1-oxo-4a,5,6,7,8,8a-hexahydrophthalazin-2(1H)-yl)butylamino-1-hydroxyethyl)-2-hydroxyphenyl)formamide
ChEMBL 538 13 4 8 3.4 COc1ccc(C2=NN(CCCCNC[C@H](O)c3ccc(O)c(NC=O)c3)C(=O)C3CCCCC23)cc1OC 10.1016/j.bmcl.2012.01.013
54757026 65144 0 None - 0 Human 9.1 pKd = 9.1 Functional
Antagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 833 22 4 8 7.5 O=C(CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1)NCCCCNCC(O)COc1cccc2ccccc12 10.1021/jm2008562
CHEMBL1830489 65144 0 None - 0 Human 9.1 pKd = 9.1 Functional
Antagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 833 22 4 8 7.5 O=C(CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1)NCCCCNCC(O)COc1cccc2ccccc12 10.1021/jm2008562
13267804 202297 0 None - 0 Guinea pig 8.9 pKd = 8.9 Functional
Antagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbacholAntagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbachol
ChEMBL 271 4 2 3 2.7 O[C@H](COc1cccc2ccccc12)[C@H]1CCCCN1 10.1021/jm00119a011
CHEMBL69635 202297 0 None - 0 Guinea pig 8.9 pKd = 8.9 Functional
Antagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbacholAntagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbachol
ChEMBL 271 4 2 3 2.7 O[C@H](COc1cccc2ccccc12)[C@H]1CCCCN1 10.1021/jm00119a011
54757229 65169 0 None - 0 Human 8.8 pKd = 8.8 Functional
Antagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 795 22 4 8 6.3 C=CCc1ccccc1OCC(O)CNCCNC(=O)CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1 10.1021/jm2008562
CHEMBL1830617 65169 0 None - 0 Human 8.8 pKd = 8.8 Functional
Antagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 795 22 4 8 6.3 C=CCc1ccccc1OCC(O)CNCCNC(=O)CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1 10.1021/jm2008562
54756928 65142 0 None - 0 Human 8.8 pKd = 8.8 Functional
Antagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 889 26 4 8 9.1 O=C(CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1)NCCCCCCCCNC[C@H](O)COc1cccc2ccccc12 10.1021/jm2008562
CHEMBL1830487 65142 0 None - 0 Human 8.8 pKd = 8.8 Functional
Antagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 889 26 4 8 9.1 O=C(CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1)NCCCCCCCCNC[C@H](O)COc1cccc2ccccc12 10.1021/jm2008562
165193 3126 60 None -9 13 Dog 8.8 pKd = 8.8 Functional
Compound was evaluated for competitive antagonism of beta-2 adrenergic receptor in rat uterus measured as pA2 (-log KB)Compound was evaluated for competitive antagonism of beta-2 adrenergic receptor in rat uterus measured as pA2 (-log KB)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00373a008
2303 3126 60 None -9 13 Dog 8.8 pKd = 8.8 Functional
Compound was evaluated for competitive antagonism of beta-2 adrenergic receptor in rat uterus measured as pA2 (-log KB)Compound was evaluated for competitive antagonism of beta-2 adrenergic receptor in rat uterus measured as pA2 (-log KB)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00373a008
4946 3126 60 None -9 13 Dog 8.8 pKd = 8.8 Functional
Compound was evaluated for competitive antagonism of beta-2 adrenergic receptor in rat uterus measured as pA2 (-log KB)Compound was evaluated for competitive antagonism of beta-2 adrenergic receptor in rat uterus measured as pA2 (-log KB)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00373a008
564 3126 60 None -9 13 Dog 8.8 pKd = 8.8 Functional
Compound was evaluated for competitive antagonism of beta-2 adrenergic receptor in rat uterus measured as pA2 (-log KB)Compound was evaluated for competitive antagonism of beta-2 adrenergic receptor in rat uterus measured as pA2 (-log KB)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00373a008
62882 3126 60 None -9 13 Dog 8.8 pKd = 8.8 Functional
Compound was evaluated for competitive antagonism of beta-2 adrenergic receptor in rat uterus measured as pA2 (-log KB)Compound was evaluated for competitive antagonism of beta-2 adrenergic receptor in rat uterus measured as pA2 (-log KB)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00373a008
63 3126 60 None -9 13 Dog 8.8 pKd = 8.8 Functional
Compound was evaluated for competitive antagonism of beta-2 adrenergic receptor in rat uterus measured as pA2 (-log KB)Compound was evaluated for competitive antagonism of beta-2 adrenergic receptor in rat uterus measured as pA2 (-log KB)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00373a008
66366 3126 60 None -9 13 Dog 8.8 pKd = 8.8 Functional
Compound was evaluated for competitive antagonism of beta-2 adrenergic receptor in rat uterus measured as pA2 (-log KB)Compound was evaluated for competitive antagonism of beta-2 adrenergic receptor in rat uterus measured as pA2 (-log KB)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00373a008
91536 3126 60 None -9 13 Dog 8.8 pKd = 8.8 Functional
Compound was evaluated for competitive antagonism of beta-2 adrenergic receptor in rat uterus measured as pA2 (-log KB)Compound was evaluated for competitive antagonism of beta-2 adrenergic receptor in rat uterus measured as pA2 (-log KB)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00373a008
CHEMBL27 3126 60 None -9 13 Dog 8.8 pKd = 8.8 Functional
Compound was evaluated for competitive antagonism of beta-2 adrenergic receptor in rat uterus measured as pA2 (-log KB)Compound was evaluated for competitive antagonism of beta-2 adrenergic receptor in rat uterus measured as pA2 (-log KB)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00373a008
CHEMBL452861 3126 60 None -9 13 Dog 8.8 pKd = 8.8 Functional
Compound was evaluated for competitive antagonism of beta-2 adrenergic receptor in rat uterus measured as pA2 (-log KB)Compound was evaluated for competitive antagonism of beta-2 adrenergic receptor in rat uterus measured as pA2 (-log KB)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00373a008
DB00571 3126 60 None -9 13 Dog 8.8 pKd = 8.8 Functional
Compound was evaluated for competitive antagonism of beta-2 adrenergic receptor in rat uterus measured as pA2 (-log KB)Compound was evaluated for competitive antagonism of beta-2 adrenergic receptor in rat uterus measured as pA2 (-log KB)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00373a008
54757129 65148 0 None - 0 Human 8.7 pKd = 8.7 Functional
Antagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 795 22 4 8 6.3 C=CCc1ccccc1OC[C@@H](O)CNCCNC(=O)CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1 10.1021/jm2008562
CHEMBL1830493 65148 0 None - 0 Human 8.7 pKd = 8.7 Functional
Antagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 795 22 4 8 6.3 C=CCc1ccccc1OC[C@@H](O)CNCCNC(=O)CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1 10.1021/jm2008562
44287476 11892 0 None - 0 Guinea pig 8.0 pKd = 8.0 Functional
Antagonistic activity against beta-2 adrenergic receptor on isolated guinea pig tracheal stripsAntagonistic activity against beta-2 adrenergic receptor on isolated guinea pig tracheal strips
ChEMBL 230 7 2 4 1.9 CCC(CC)=NOCC(O)CNC(C)(C)C 10.1021/jm00380a001
CHEMBL1183311 11892 0 None - 0 Guinea pig 8.0 pKd = 8.0 Functional
Antagonistic activity against beta-2 adrenergic receptor on isolated guinea pig tracheal stripsAntagonistic activity against beta-2 adrenergic receptor on isolated guinea pig tracheal strips
ChEMBL 230 7 2 4 1.9 CCC(CC)=NOCC(O)CNC(C)(C)C 10.1021/jm00380a001
CHEMBL289858 11892 0 None - 0 Guinea pig 8.0 pKd = 8.0 Functional
Antagonistic activity against beta-2 adrenergic receptor on isolated guinea pig tracheal stripsAntagonistic activity against beta-2 adrenergic receptor on isolated guinea pig tracheal strips
ChEMBL 230 7 2 4 1.9 CCC(CC)=NOCC(O)CNC(C)(C)C 10.1021/jm00380a001
44371514 11581 0 None - 0 Guinea pig 6.0 pKd = 6 Functional
The apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pigThe apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pig
ChEMBL 216 8 2 4 1.5 CCC/C(C)=N\OCC(O)CNC(C)C 10.1021/jm00180a007
CHEMBL1181235 11581 0 None - 0 Guinea pig 6.0 pKd = 6 Functional
The apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pigThe apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pig
ChEMBL 216 8 2 4 1.5 CCC/C(C)=N\OCC(O)CNC(C)C 10.1021/jm00180a007
CHEMBL160282 11581 0 None - 0 Guinea pig 6.0 pKd = 6 Functional
The apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pigThe apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pig
ChEMBL 216 8 2 4 1.5 CCC/C(C)=N\OCC(O)CNC(C)C 10.1021/jm00180a007
44371562 49435 0 None - 0 Guinea pig 5.0 pKd = 5 Functional
Antagonist activity against beta-2 adrenergic receptor in isolated guinea pig tracheaAntagonist activity against beta-2 adrenergic receptor in isolated guinea pig trachea
ChEMBL 257 7 2 5 1.2 CC(C)NCC(O)COC(=O)Cc1cccs1 10.1021/jm00387a006
CHEMBL156683 49435 0 None - 0 Guinea pig 5.0 pKd = 5 Functional
Antagonist activity against beta-2 adrenergic receptor in isolated guinea pig tracheaAntagonist activity against beta-2 adrenergic receptor in isolated guinea pig trachea
ChEMBL 257 7 2 5 1.2 CC(C)NCC(O)COC(=O)Cc1cccs1 10.1021/jm00387a006
2685 875 15 None - 1 Human 6.0 pKd = 6.0 Functional
Antagonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrsAntagonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrs
ChEMBL 494 11 4 8 2.3 OC(COc1ccc(cc1)c1nc(cn1C)C(F)(F)F)CNCCOc1ccc(c(c1)C(=O)N)O 10.1021/jm400348g
541 875 15 None - 1 Human 6.0 pKd = 6.0 Functional
Antagonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrsAntagonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrs
ChEMBL 494 11 4 8 2.3 OC(COc1ccc(cc1)c1nc(cn1C)C(F)(F)F)CNCCOc1ccc(c(c1)C(=O)N)O 10.1021/jm400348g
CHEMBL280822 875 15 None - 1 Human 6.0 pKd = 6.0 Functional
Antagonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrsAntagonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrs
ChEMBL 494 11 4 8 2.3 OC(COc1ccc(cc1)c1nc(cn1C)C(F)(F)F)CNCCOc1ccc(c(c1)C(=O)N)O 10.1021/jm400348g
551640 201813 19 None - 0 Guinea pig 6.0 pKd = 6.0 Functional
Antagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbacholAntagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbachol
ChEMBL 223 7 2 3 1.6 CC(C)NCC(O)COCc1ccccc1 10.1021/jm00119a011
CHEMBL66331 201813 19 None - 0 Guinea pig 6.0 pKd = 6.0 Functional
Antagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbacholAntagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbachol
ChEMBL 223 7 2 3 1.6 CC(C)NCC(O)COCc1ccccc1 10.1021/jm00119a011
18047 201915 18 None - 0 Guinea pig 7.9 pKd = 7.9 Functional
Antagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbacholAntagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbachol
ChEMBL 223 6 2 3 1.7 Cc1cccc(OCC(O)CNC(C)C)c1 10.1021/jm00119a011
CHEMBL67096 201915 18 None - 0 Guinea pig 7.9 pKd = 7.9 Functional
Antagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbacholAntagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbachol
ChEMBL 223 6 2 3 1.7 Cc1cccc(OCC(O)CNC(C)C)c1 10.1021/jm00119a011
14201557 201865 0 None - 0 Guinea pig 7.0 pKd = 7.0 Functional
Antagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbacholAntagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbachol
ChEMBL 235 4 1 3 1.9 CN1CCCC[C@@H]1[C@H](O)COc1ccccc1 10.1021/jm00119a011
CHEMBL66724 201865 0 None - 0 Guinea pig 7.0 pKd = 7.0 Functional
Antagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbacholAntagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbachol
ChEMBL 235 4 1 3 1.9 CN1CCCC[C@@H]1[C@H](O)COc1ccccc1 10.1021/jm00119a011
145947665 167110 0 None - 1 Guinea pig 6.9 pKd = 6.9 Functional
Antagonist activity at adrenergic beta2 receptor in isolated guinea pig trachea assessed as inhibition of isoprenaline-induced bronchodilation incubated for 20 minsAntagonist activity at adrenergic beta2 receptor in isolated guinea pig trachea assessed as inhibition of isoprenaline-induced bronchodilation incubated for 20 mins
ChEMBL 405 8 2 6 3.5 COc1ccccc1CNCC(O)COc1cccc2c(=O)c3ccccc3oc12 10.1016/j.bmc.2018.04.038
CHEMBL4128794 167110 0 None - 1 Guinea pig 6.9 pKd = 6.9 Functional
Antagonist activity at adrenergic beta2 receptor in isolated guinea pig trachea assessed as inhibition of isoprenaline-induced bronchodilation incubated for 20 minsAntagonist activity at adrenergic beta2 receptor in isolated guinea pig trachea assessed as inhibition of isoprenaline-induced bronchodilation incubated for 20 mins
ChEMBL 405 8 2 6 3.5 COc1ccccc1CNCC(O)COc1cccc2c(=O)c3ccccc3oc12 10.1016/j.bmc.2018.04.038
CHEMBL4302144 167110 0 None - 1 Guinea pig 6.9 pKd = 6.9 Functional
Antagonist activity at adrenergic beta2 receptor in isolated guinea pig trachea assessed as inhibition of isoprenaline-induced bronchodilation incubated for 20 minsAntagonist activity at adrenergic beta2 receptor in isolated guinea pig trachea assessed as inhibition of isoprenaline-induced bronchodilation incubated for 20 mins
ChEMBL 405 8 2 6 3.5 COc1ccccc1CNCC(O)COc1cccc2c(=O)c3ccccc3oc12 10.1016/j.bmc.2018.04.038
12797747 201834 2 None - 0 Guinea pig 6.9 pKd = 6.9 Functional
Antagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbacholAntagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbachol
ChEMBL 251 9 2 3 2.0 CC(C)NCC(O)COCCCc1ccccc1 10.1021/jm00119a011
CHEMBL66449 201834 2 None - 0 Guinea pig 6.9 pKd = 6.9 Functional
Antagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbacholAntagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbachol
ChEMBL 251 9 2 3 2.0 CC(C)NCC(O)COCCCc1ccccc1 10.1021/jm00119a011
21595422 101735 0 None - 0 Guinea pig 6.9 pKd = 6.9 Functional
Antagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbacholAntagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbachol
ChEMBL 235 5 2 3 1.7 O[C@H](COCc1ccccc1)[C@@H]1CCCCN1 10.1021/jm00119a011
CHEMBL302935 101735 0 None - 0 Guinea pig 6.9 pKd = 6.9 Functional
Antagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbacholAntagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbachol
ChEMBL 235 5 2 3 1.7 O[C@H](COCc1ccccc1)[C@@H]1CCCCN1 10.1021/jm00119a011
56598967 87819 0 None -2238 3 Human 5.9 pKd = 5.9 Functional
Antagonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrsAntagonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrs
ChEMBL 457 14 4 6 3.2 O=C(NCCNCC(O)COc1ccc(OCCOC2CCCC2)cc1)Nc1ccccc1 10.1021/jm400348g
CHEMBL2348211 87819 0 None -2238 3 Human 5.9 pKd = 5.9 Functional
Antagonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrsAntagonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrs
ChEMBL 457 14 4 6 3.2 O=C(NCCNCC(O)COc1ccc(OCCOC2CCCC2)cc1)Nc1ccccc1 10.1021/jm400348g
134495 736 18 None - 1 Guinea pig 6.9 pKd = 6.9 Functional
Antagonist activity against beta-2 adrenergic receptor in isolated guinea pig tracheaAntagonist activity against beta-2 adrenergic receptor in isolated guinea pig trachea
ChEMBL 267 5 2 4 2.5 COc1ccc(cc1C(C(NC(C)(C)C)C)O)OC 10.1021/jm00387a006
18026 736 18 None - 1 Guinea pig 6.9 pKd = 6.9 Functional
Antagonist activity against beta-2 adrenergic receptor in isolated guinea pig tracheaAntagonist activity against beta-2 adrenergic receptor in isolated guinea pig trachea
ChEMBL 267 5 2 4 2.5 COc1ccc(cc1C(C(NC(C)(C)C)C)O)OC 10.1021/jm00387a006
9809 736 18 None - 1 Guinea pig 6.9 pKd = 6.9 Functional
Antagonist activity against beta-2 adrenergic receptor in isolated guinea pig tracheaAntagonist activity against beta-2 adrenergic receptor in isolated guinea pig trachea
ChEMBL 267 5 2 4 2.5 COc1ccc(cc1C(C(NC(C)(C)C)C)O)OC 10.1021/jm00387a006
CHEMBL289093 736 18 None - 1 Guinea pig 6.9 pKd = 6.9 Functional
Antagonist activity against beta-2 adrenergic receptor in isolated guinea pig tracheaAntagonist activity against beta-2 adrenergic receptor in isolated guinea pig trachea
ChEMBL 267 5 2 4 2.5 COc1ccc(cc1C(C(NC(C)(C)C)C)O)OC 10.1021/jm00387a006
134495 736 18 None - 1 Guinea pig 6.9 pKd = 6.9 Functional
Antagonistic activity against beta-2 adrenergic receptor on isolated guinea pig tracheal stripsAntagonistic activity against beta-2 adrenergic receptor on isolated guinea pig tracheal strips
ChEMBL 267 5 2 4 2.5 COc1ccc(cc1C(C(NC(C)(C)C)C)O)OC 10.1021/jm00380a001
18026 736 18 None - 1 Guinea pig 6.9 pKd = 6.9 Functional
Antagonistic activity against beta-2 adrenergic receptor on isolated guinea pig tracheal stripsAntagonistic activity against beta-2 adrenergic receptor on isolated guinea pig tracheal strips
ChEMBL 267 5 2 4 2.5 COc1ccc(cc1C(C(NC(C)(C)C)C)O)OC 10.1021/jm00380a001
9809 736 18 None - 1 Guinea pig 6.9 pKd = 6.9 Functional
Antagonistic activity against beta-2 adrenergic receptor on isolated guinea pig tracheal stripsAntagonistic activity against beta-2 adrenergic receptor on isolated guinea pig tracheal strips
ChEMBL 267 5 2 4 2.5 COc1ccc(cc1C(C(NC(C)(C)C)C)O)OC 10.1021/jm00380a001
CHEMBL289093 736 18 None - 1 Guinea pig 6.9 pKd = 6.9 Functional
Antagonistic activity against beta-2 adrenergic receptor on isolated guinea pig tracheal stripsAntagonistic activity against beta-2 adrenergic receptor on isolated guinea pig tracheal strips
ChEMBL 267 5 2 4 2.5 COc1ccc(cc1C(C(NC(C)(C)C)C)O)OC 10.1021/jm00380a001
3123920 2774 79 None - 0 Guinea pig 7.9 pKd = 7.9 Functional
Antagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbacholAntagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbachol
ChEMBL 209 6 2 3 1.4 OC(COc1ccccc1)CNC(C)C 10.1021/jm00119a011
546 2774 79 None - 0 Guinea pig 7.9 pKd = 7.9 Functional
Antagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbacholAntagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbachol
ChEMBL 209 6 2 3 1.4 OC(COc1ccccc1)CNC(C)C 10.1021/jm00119a011
CHEMBL7154 2774 79 None - 0 Guinea pig 7.9 pKd = 7.9 Functional
Antagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbacholAntagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbachol
ChEMBL 209 6 2 3 1.4 OC(COc1ccccc1)CNC(C)C 10.1021/jm00119a011
21595417 202192 0 None - 0 Guinea pig 7.9 pKd = 7.9 Functional
Antagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbacholAntagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbachol
ChEMBL 221 4 2 3 1.6 O[C@H](COc1ccccc1)[C@@H]1CCCCN1 10.1021/jm00119a011
CHEMBL68945 202192 0 None - 0 Guinea pig 7.9 pKd = 7.9 Functional
Antagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbacholAntagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbachol
ChEMBL 221 4 2 3 1.6 O[C@H](COc1ccccc1)[C@@H]1CCCCN1 10.1021/jm00119a011
168613 59987 21 None - 0 Guinea pig 7.9 pKd = 7.9 Functional
Beta-2 adrenergic receptor antagonistic activity on guinea pig tracheal chainsBeta-2 adrenergic receptor antagonistic activity on guinea pig tracheal chains
ChEMBL 316 6 2 8 0.5 CC(C)(C)NC[C@@H](O)COc1nsnc1N1CCOCC1 10.1021/jm00350a009
CHEMBL1744069 59987 21 None - 0 Guinea pig 7.9 pKd = 7.9 Functional
Beta-2 adrenergic receptor antagonistic activity on guinea pig tracheal chainsBeta-2 adrenergic receptor antagonistic activity on guinea pig tracheal chains
ChEMBL 316 6 2 8 0.5 CC(C)(C)NC[C@@H](O)COc1nsnc1N1CCOCC1 10.1021/jm00350a009
12733303 60059 0 None - 0 Guinea pig 5.9 pKd = 5.9 Functional
Antagonist activity of compound against Beta-2 adrenergic receptor in isolated guinea pig tracheaAntagonist activity of compound against Beta-2 adrenergic receptor in isolated guinea pig trachea
ChEMBL 261 3 1 4 2.1 OC(CN1CCCCC1)C1=COc2ccccc2O1 10.1021/jm00140a015
CHEMBL174882 60059 0 None - 0 Guinea pig 5.9 pKd = 5.9 Functional
Antagonist activity of compound against Beta-2 adrenergic receptor in isolated guinea pig tracheaAntagonist activity of compound against Beta-2 adrenergic receptor in isolated guinea pig trachea
ChEMBL 261 3 1 4 2.1 OC(CN1CCCCC1)C1=COc2ccccc2O1 10.1021/jm00140a015
56597179 87827 0 None -2754 3 Human 5.8 pKd = 5.8 Functional
Antagonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrsAntagonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrs
ChEMBL 473 14 5 7 2.9 O=C(NCCNCC(O)COc1ccc(OCCOC2CCCC2)cc1)Nc1ccc(O)cc1 10.1021/jm400348g
CHEMBL2348219 87827 0 None -2754 3 Human 5.8 pKd = 5.8 Functional
Antagonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrsAntagonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrs
ChEMBL 473 14 5 7 2.9 O=C(NCCNCC(O)COc1ccc(OCCOC2CCCC2)cc1)Nc1ccc(O)cc1 10.1021/jm400348g
21595419 101632 0 None - 0 Guinea pig 7.8 pKd = 7.8 Functional
Antagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbacholAntagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbachol
ChEMBL 271 4 2 3 2.7 O[C@H](COc1ccc2ccccc2c1)[C@@H]1CCCCN1 10.1021/jm00119a011
CHEMBL302339 101632 0 None - 0 Guinea pig 7.8 pKd = 7.8 Functional
Antagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbacholAntagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbachol
ChEMBL 271 4 2 3 2.7 O[C@H](COc1ccc2ccccc2c1)[C@@H]1CCCCN1 10.1021/jm00119a011
44287498 12282 0 None - 0 Guinea pig 6.8 pKd = 6.8 Functional
Antagonistic activity against beta-2 adrenergic receptor on isolated guinea pig tracheal stripsAntagonistic activity against beta-2 adrenergic receptor on isolated guinea pig tracheal strips
ChEMBL 214 6 2 4 1.3 CC(C)NCC(O)CON=C1CCCC1 10.1021/jm00380a001
CHEMBL1185760 12282 0 None - 0 Guinea pig 6.8 pKd = 6.8 Functional
Antagonistic activity against beta-2 adrenergic receptor on isolated guinea pig tracheal stripsAntagonistic activity against beta-2 adrenergic receptor on isolated guinea pig tracheal strips
ChEMBL 214 6 2 4 1.3 CC(C)NCC(O)CON=C1CCCC1 10.1021/jm00380a001
CHEMBL431713 12282 0 None - 0 Guinea pig 6.8 pKd = 6.8 Functional
Antagonistic activity against beta-2 adrenergic receptor on isolated guinea pig tracheal stripsAntagonistic activity against beta-2 adrenergic receptor on isolated guinea pig tracheal strips
ChEMBL 214 6 2 4 1.3 CC(C)NCC(O)CON=C1CCCC1 10.1021/jm00380a001
2769826 202113 22 None - 0 Guinea pig 7.8 pKd = 7.8 Functional
Antagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbacholAntagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbachol
ChEMBL 259 6 2 3 2.6 CC(C)NCC(O)COc1ccc2ccccc2c1 10.1021/jm00119a011
CHEMBL68419 202113 22 None - 0 Guinea pig 7.8 pKd = 7.8 Functional
Antagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbacholAntagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbachol
ChEMBL 259 6 2 3 2.6 CC(C)NCC(O)COc1ccc2ccccc2c1 10.1021/jm00119a011
2447484 102282 2 None - 2 Guinea pig 7.8 pKd = 7.8 Functional
Beta-2 adrenergic receptor antagonistic activity on guinea pig tracheal chainsBeta-2 adrenergic receptor antagonistic activity on guinea pig tracheal chains
ChEMBL 324 5 2 4 3.2 CC(C)(C)NC[C@H](O)CON=C1c2ccccc2-c2ccccc21 10.1021/jm00350a009
CHEMBL305153 102282 2 None - 2 Guinea pig 7.8 pKd = 7.8 Functional
Beta-2 adrenergic receptor antagonistic activity on guinea pig tracheal chainsBeta-2 adrenergic receptor antagonistic activity on guinea pig tracheal chains
ChEMBL 324 5 2 4 3.2 CC(C)(C)NC[C@H](O)CON=C1c2ccccc2-c2ccccc21 10.1021/jm00350a009
12733301 60074 1 None - 0 Guinea pig 6.8 pKd = 6.8 Functional
Antagonist activity of compound against Beta-2 adrenergic receptor in isolated guinea pig tracheaAntagonist activity of compound against Beta-2 adrenergic receptor in isolated guinea pig trachea
ChEMBL 235 4 2 4 1.7 CC(C)NCC(O)C1=COc2ccccc2O1 10.1021/jm00140a015
CHEMBL175010 60074 1 None - 0 Guinea pig 6.8 pKd = 6.8 Functional
Antagonist activity of compound against Beta-2 adrenergic receptor in isolated guinea pig tracheaAntagonist activity of compound against Beta-2 adrenergic receptor in isolated guinea pig trachea
ChEMBL 235 4 2 4 1.7 CC(C)NCC(O)C1=COc2ccccc2O1 10.1021/jm00140a015
1786 2474 79 None - 6 Guinea pig 6.8 pKd = 6.8 Functional
Beta-2 adrenergic receptor antagonistic activity on guinea pig tracheal chainsBeta-2 adrenergic receptor antagonistic activity on guinea pig tracheal chains
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm00350a009
4171 2474 79 None - 6 Guinea pig 6.8 pKd = 6.8 Functional
Beta-2 adrenergic receptor antagonistic activity on guinea pig tracheal chainsBeta-2 adrenergic receptor antagonistic activity on guinea pig tracheal chains
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm00350a009
553 2474 79 None - 6 Guinea pig 6.8 pKd = 6.8 Functional
Beta-2 adrenergic receptor antagonistic activity on guinea pig tracheal chainsBeta-2 adrenergic receptor antagonistic activity on guinea pig tracheal chains
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm00350a009
CHEMBL13 2474 79 None - 6 Guinea pig 6.8 pKd = 6.8 Functional
Beta-2 adrenergic receptor antagonistic activity on guinea pig tracheal chainsBeta-2 adrenergic receptor antagonistic activity on guinea pig tracheal chains
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm00350a009
DB00264 2474 79 None - 6 Guinea pig 6.8 pKd = 6.8 Functional
Beta-2 adrenergic receptor antagonistic activity on guinea pig tracheal chainsBeta-2 adrenergic receptor antagonistic activity on guinea pig tracheal chains
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm00350a009
12733304 127702 0 None - 0 Guinea pig 4.8 pKd = 4.8 Functional
Antagonist activity of compound against Beta-2 adrenergic receptor in isolated guinea pig tracheaAntagonist activity of compound against Beta-2 adrenergic receptor in isolated guinea pig trachea
ChEMBL 275 3 1 4 2.5 OC(CN1CCCCCC1)C1=COc2ccccc2O1 10.1021/jm00140a015
CHEMBL366558 127702 0 None - 0 Guinea pig 4.8 pKd = 4.8 Functional
Antagonist activity of compound against Beta-2 adrenergic receptor in isolated guinea pig tracheaAntagonist activity of compound against Beta-2 adrenergic receptor in isolated guinea pig trachea
ChEMBL 275 3 1 4 2.5 OC(CN1CCCCCC1)C1=COc2ccccc2O1 10.1021/jm00140a015
44287620 11106 0 None - 0 Guinea pig 6.8 pKd = 6.8 Functional
Antagonistic activity against beta-2 adrenergic receptor on isolated guinea pig tracheal stripsAntagonistic activity against beta-2 adrenergic receptor on isolated guinea pig tracheal strips
ChEMBL 228 5 2 4 1.7 CC(C)(C)NCC(O)CON=C1CCCC1 10.1021/jm00380a001
CHEMBL1178780 11106 0 None - 0 Guinea pig 6.8 pKd = 6.8 Functional
Antagonistic activity against beta-2 adrenergic receptor on isolated guinea pig tracheal stripsAntagonistic activity against beta-2 adrenergic receptor on isolated guinea pig tracheal strips
ChEMBL 228 5 2 4 1.7 CC(C)(C)NCC(O)CON=C1CCCC1 10.1021/jm00380a001
CHEMBL40971 11106 0 None - 0 Guinea pig 6.8 pKd = 6.8 Functional
Antagonistic activity against beta-2 adrenergic receptor on isolated guinea pig tracheal stripsAntagonistic activity against beta-2 adrenergic receptor on isolated guinea pig tracheal strips
ChEMBL 228 5 2 4 1.7 CC(C)(C)NCC(O)CON=C1CCCC1 10.1021/jm00380a001
12733305 60053 0 None - 0 Guinea pig 6.8 pKd = 6.8 Functional
Antagonist activity of compound against Beta-2 adrenergic receptor in isolated guinea pig tracheaAntagonist activity of compound against Beta-2 adrenergic receptor in isolated guinea pig trachea
ChEMBL 357 8 2 6 2.5 COc1ccc(CCNCC(O)C2=COc3ccccc3O2)cc1OC 10.1021/jm00140a015
CHEMBL174853 60053 0 None - 0 Guinea pig 6.8 pKd = 6.8 Functional
Antagonist activity of compound against Beta-2 adrenergic receptor in isolated guinea pig tracheaAntagonist activity of compound against Beta-2 adrenergic receptor in isolated guinea pig trachea
ChEMBL 357 8 2 6 2.5 COc1ccc(CCNCC(O)C2=COc3ccccc3O2)cc1OC 10.1021/jm00140a015
145946488 166965 0 None - 1 Guinea pig 7.7 pKd = 7.7 Functional
Antagonist activity at adrenergic beta2 receptor in isolated guinea pig trachea assessed as inhibition of isoprenaline-induced bronchodilation incubated for 20 minsAntagonist activity at adrenergic beta2 receptor in isolated guinea pig trachea assessed as inhibition of isoprenaline-induced bronchodilation incubated for 20 mins
ChEMBL 435 10 2 7 3.4 COc1ccccc1OCCNCC(O)COc1cccc2c(=O)c3ccccc3oc12 10.1016/j.bmc.2018.04.038
CHEMBL4127540 166965 0 None - 1 Guinea pig 7.7 pKd = 7.7 Functional
Antagonist activity at adrenergic beta2 receptor in isolated guinea pig trachea assessed as inhibition of isoprenaline-induced bronchodilation incubated for 20 minsAntagonist activity at adrenergic beta2 receptor in isolated guinea pig trachea assessed as inhibition of isoprenaline-induced bronchodilation incubated for 20 mins
ChEMBL 435 10 2 7 3.4 COc1ccccc1OCCNCC(O)COc1cccc2c(=O)c3ccccc3oc12 10.1016/j.bmc.2018.04.038
CHEMBL4300195 166965 0 None - 1 Guinea pig 7.7 pKd = 7.7 Functional
Antagonist activity at adrenergic beta2 receptor in isolated guinea pig trachea assessed as inhibition of isoprenaline-induced bronchodilation incubated for 20 minsAntagonist activity at adrenergic beta2 receptor in isolated guinea pig trachea assessed as inhibition of isoprenaline-induced bronchodilation incubated for 20 mins
ChEMBL 435 10 2 7 3.4 COc1ccccc1OCCNCC(O)COc1cccc2c(=O)c3ccccc3oc12 10.1016/j.bmc.2018.04.038
2447486 62716 1 None - 2 Guinea pig 7.7 pKd = 7.7 Functional
Beta-2 adrenergic receptor antagonistic activity on guinea pig tracheal chainsBeta-2 adrenergic receptor antagonistic activity on guinea pig tracheal chains
ChEMBL 324 5 2 4 3.2 CC(C)(C)NC[C@@H](O)CON=C1c2ccccc2-c2ccccc21 10.1021/jm00350a009
CHEMBL1788270 62716 1 None - 2 Guinea pig 7.7 pKd = 7.7 Functional
Beta-2 adrenergic receptor antagonistic activity on guinea pig tracheal chainsBeta-2 adrenergic receptor antagonistic activity on guinea pig tracheal chains
ChEMBL 324 5 2 4 3.2 CC(C)(C)NC[C@@H](O)CON=C1c2ccccc2-c2ccccc21 10.1021/jm00350a009
3486 3096 51 None - 0 Dog 6.7 pKd = 6.7 Functional
Cardioselectivity for the beta-2 adrenergic receptor was determined against isoprenaline (antagonism) in isolated rat atriaCardioselectivity for the beta-2 adrenergic receptor was determined against isoprenaline (antagonism) in isolated rat atria
ChEMBL 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C 10.1021/jm00389a008
4883 3096 51 None - 0 Dog 6.7 pKd = 6.7 Functional
Cardioselectivity for the beta-2 adrenergic receptor was determined against isoprenaline (antagonism) in isolated rat atriaCardioselectivity for the beta-2 adrenergic receptor was determined against isoprenaline (antagonism) in isolated rat atria
ChEMBL 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C 10.1021/jm00389a008
555 3096 51 None - 0 Dog 6.7 pKd = 6.7 Functional
Cardioselectivity for the beta-2 adrenergic receptor was determined against isoprenaline (antagonism) in isolated rat atriaCardioselectivity for the beta-2 adrenergic receptor was determined against isoprenaline (antagonism) in isolated rat atria
ChEMBL 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C 10.1021/jm00389a008
CHEMBL6995 3096 51 None - 0 Dog 6.7 pKd = 6.7 Functional
Cardioselectivity for the beta-2 adrenergic receptor was determined against isoprenaline (antagonism) in isolated rat atriaCardioselectivity for the beta-2 adrenergic receptor was determined against isoprenaline (antagonism) in isolated rat atria
ChEMBL 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C 10.1021/jm00389a008
DB01297 3096 51 None - 0 Dog 6.7 pKd = 6.7 Functional
Cardioselectivity for the beta-2 adrenergic receptor was determined against isoprenaline (antagonism) in isolated rat atriaCardioselectivity for the beta-2 adrenergic receptor was determined against isoprenaline (antagonism) in isolated rat atria
ChEMBL 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C 10.1021/jm00389a008
12606709 14213 0 None - 0 Guinea pig 6.7 pKd = 6.7 Functional
The apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pigThe apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pig
ChEMBL 296 5 2 4 3.0 CC(C)(C)NCC(O)CO/N=C1\CC2CCC1(C)C2(C)C 10.1021/jm00180a007
CHEMBL1161382 14213 0 None - 0 Guinea pig 6.7 pKd = 6.7 Functional
The apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pigThe apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pig
ChEMBL 296 5 2 4 3.0 CC(C)(C)NCC(O)CO/N=C1\CC2CCC1(C)C2(C)C 10.1021/jm00180a007
CHEMBL1200073 14213 0 None - 0 Guinea pig 6.7 pKd = 6.7 Functional
The apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pigThe apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pig
ChEMBL 296 5 2 4 3.0 CC(C)(C)NCC(O)CO/N=C1\CC2CCC1(C)C2(C)C 10.1021/jm00180a007
44371383 49332 0 None - 0 Guinea pig 7.7 pKd = 7.7 Functional
Antagonist activity against beta-2 adrenergic receptor in isolated guinea pig tracheaAntagonist activity against beta-2 adrenergic receptor in isolated guinea pig trachea
ChEMBL 257 5 2 5 1.7 CC(C)(C)NCC(O)COC(=O)c1cccs1 10.1021/jm00387a006
CHEMBL156603 49332 0 None - 0 Guinea pig 7.7 pKd = 7.7 Functional
Antagonist activity against beta-2 adrenergic receptor in isolated guinea pig tracheaAntagonist activity against beta-2 adrenergic receptor in isolated guinea pig trachea
ChEMBL 257 5 2 5 1.7 CC(C)(C)NCC(O)COC(=O)c1cccs1 10.1021/jm00387a006
12606705 11810 0 None - 0 Guinea pig 6.7 pKd = 6.7 Functional
The apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pigThe apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pig
ChEMBL 188 6 2 4 0.8 CC(C)=NOCC(O)CNC(C)C 10.1021/jm00180a007
CHEMBL1182729 11810 0 None - 0 Guinea pig 6.7 pKd = 6.7 Functional
The apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pigThe apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pig
ChEMBL 188 6 2 4 0.8 CC(C)=NOCC(O)CNC(C)C 10.1021/jm00180a007
CHEMBL263065 11810 0 None - 0 Guinea pig 6.7 pKd = 6.7 Functional
The apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pigThe apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pig
ChEMBL 188 6 2 4 0.8 CC(C)=NOCC(O)CNC(C)C 10.1021/jm00180a007
44287469 11877 0 None - 0 Guinea pig 8.6 pKd = 8.6 Functional
Antagonistic activity against beta-2 adrenergic receptor on isolated guinea pig tracheal stripsAntagonistic activity against beta-2 adrenergic receptor on isolated guinea pig tracheal strips
ChEMBL 258 9 2 4 2.7 CCCC(CCC)=NOCC(O)CNC(C)(C)C 10.1021/jm00380a001
CHEMBL1183268 11877 0 None - 0 Guinea pig 8.6 pKd = 8.6 Functional
Antagonistic activity against beta-2 adrenergic receptor on isolated guinea pig tracheal stripsAntagonistic activity against beta-2 adrenergic receptor on isolated guinea pig tracheal strips
ChEMBL 258 9 2 4 2.7 CCCC(CCC)=NOCC(O)CNC(C)(C)C 10.1021/jm00380a001
CHEMBL287766 11877 0 None - 0 Guinea pig 8.6 pKd = 8.6 Functional
Antagonistic activity against beta-2 adrenergic receptor on isolated guinea pig tracheal stripsAntagonistic activity against beta-2 adrenergic receptor on isolated guinea pig tracheal strips
ChEMBL 258 9 2 4 2.7 CCCC(CCC)=NOCC(O)CNC(C)(C)C 10.1021/jm00380a001
91565 9692 18 None - 0 Dog 8.6 pKd = 8.6 Functional
Compound was evaluated for competitive antagonism of beta-2 adrenergic receptor in rat uterus measured as pA2 (-log KB)Compound was evaluated for competitive antagonism of beta-2 adrenergic receptor in rat uterus measured as pA2 (-log KB)
ChEMBL 275 6 3 4 2.3 CC(C)NCC(O)COc1ccc(O)c2ccccc12 10.1021/jm00373a008
CHEMBL1137 9692 18 None - 0 Dog 8.6 pKd = 8.6 Functional
Compound was evaluated for competitive antagonism of beta-2 adrenergic receptor in rat uterus measured as pA2 (-log KB)Compound was evaluated for competitive antagonism of beta-2 adrenergic receptor in rat uterus measured as pA2 (-log KB)
ChEMBL 275 6 3 4 2.3 CC(C)NCC(O)COc1ccc(O)c2ccccc12 10.1021/jm00373a008
54757027 65145 0 None - 0 Human 8.6 pKd = 8.6 Functional
Antagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 889 26 4 8 9.1 O=C(CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1)NCCCCCCCCNCC(O)COc1cccc2ccccc12 10.1021/jm2008562
CHEMBL1830490 65145 0 None - 0 Human 8.6 pKd = 8.6 Functional
Antagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 889 26 4 8 9.1 O=C(CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1)NCCCCCCCCNCC(O)COc1cccc2ccccc12 10.1021/jm2008562
54756929 65143 0 None - 0 Human 8.6 pKd = 8.6 Functional
Antagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 805 20 4 8 6.7 O=C(CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1)NCCNCC(O)COc1cccc2ccccc12 10.1021/jm2008562
CHEMBL1830488 65143 0 None - 0 Human 8.6 pKd = 8.6 Functional
Antagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 805 20 4 8 6.7 O=C(CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1)NCCNCC(O)COc1cccc2ccccc12 10.1021/jm2008562
165193 3126 60 None -22 13 Guinea pig 8.6 pKd = 8.6 Functional
Antagonist activity at adrenergic beta2 receptor in isolated guinea pig trachea assessed as inhibition of isoprenaline-induced bronchodilation incubated for 20 minsAntagonist activity at adrenergic beta2 receptor in isolated guinea pig trachea assessed as inhibition of isoprenaline-induced bronchodilation incubated for 20 mins
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmc.2018.04.038
2303 3126 60 None -22 13 Guinea pig 8.6 pKd = 8.6 Functional
Antagonist activity at adrenergic beta2 receptor in isolated guinea pig trachea assessed as inhibition of isoprenaline-induced bronchodilation incubated for 20 minsAntagonist activity at adrenergic beta2 receptor in isolated guinea pig trachea assessed as inhibition of isoprenaline-induced bronchodilation incubated for 20 mins
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmc.2018.04.038
4946 3126 60 None -22 13 Guinea pig 8.6 pKd = 8.6 Functional
Antagonist activity at adrenergic beta2 receptor in isolated guinea pig trachea assessed as inhibition of isoprenaline-induced bronchodilation incubated for 20 minsAntagonist activity at adrenergic beta2 receptor in isolated guinea pig trachea assessed as inhibition of isoprenaline-induced bronchodilation incubated for 20 mins
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmc.2018.04.038
564 3126 60 None -22 13 Guinea pig 8.6 pKd = 8.6 Functional
Antagonist activity at adrenergic beta2 receptor in isolated guinea pig trachea assessed as inhibition of isoprenaline-induced bronchodilation incubated for 20 minsAntagonist activity at adrenergic beta2 receptor in isolated guinea pig trachea assessed as inhibition of isoprenaline-induced bronchodilation incubated for 20 mins
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmc.2018.04.038
62882 3126 60 None -22 13 Guinea pig 8.6 pKd = 8.6 Functional
Antagonist activity at adrenergic beta2 receptor in isolated guinea pig trachea assessed as inhibition of isoprenaline-induced bronchodilation incubated for 20 minsAntagonist activity at adrenergic beta2 receptor in isolated guinea pig trachea assessed as inhibition of isoprenaline-induced bronchodilation incubated for 20 mins
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmc.2018.04.038
63 3126 60 None -22 13 Guinea pig 8.6 pKd = 8.6 Functional
Antagonist activity at adrenergic beta2 receptor in isolated guinea pig trachea assessed as inhibition of isoprenaline-induced bronchodilation incubated for 20 minsAntagonist activity at adrenergic beta2 receptor in isolated guinea pig trachea assessed as inhibition of isoprenaline-induced bronchodilation incubated for 20 mins
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmc.2018.04.038
66366 3126 60 None -22 13 Guinea pig 8.6 pKd = 8.6 Functional
Antagonist activity at adrenergic beta2 receptor in isolated guinea pig trachea assessed as inhibition of isoprenaline-induced bronchodilation incubated for 20 minsAntagonist activity at adrenergic beta2 receptor in isolated guinea pig trachea assessed as inhibition of isoprenaline-induced bronchodilation incubated for 20 mins
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmc.2018.04.038
91536 3126 60 None -22 13 Guinea pig 8.6 pKd = 8.6 Functional
Antagonist activity at adrenergic beta2 receptor in isolated guinea pig trachea assessed as inhibition of isoprenaline-induced bronchodilation incubated for 20 minsAntagonist activity at adrenergic beta2 receptor in isolated guinea pig trachea assessed as inhibition of isoprenaline-induced bronchodilation incubated for 20 mins
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmc.2018.04.038
CHEMBL27 3126 60 None -22 13 Guinea pig 8.6 pKd = 8.6 Functional
Antagonist activity at adrenergic beta2 receptor in isolated guinea pig trachea assessed as inhibition of isoprenaline-induced bronchodilation incubated for 20 minsAntagonist activity at adrenergic beta2 receptor in isolated guinea pig trachea assessed as inhibition of isoprenaline-induced bronchodilation incubated for 20 mins
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmc.2018.04.038
CHEMBL452861 3126 60 None -22 13 Guinea pig 8.6 pKd = 8.6 Functional
Antagonist activity at adrenergic beta2 receptor in isolated guinea pig trachea assessed as inhibition of isoprenaline-induced bronchodilation incubated for 20 minsAntagonist activity at adrenergic beta2 receptor in isolated guinea pig trachea assessed as inhibition of isoprenaline-induced bronchodilation incubated for 20 mins
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmc.2018.04.038
DB00571 3126 60 None -22 13 Guinea pig 8.6 pKd = 8.6 Functional
Antagonist activity at adrenergic beta2 receptor in isolated guinea pig trachea assessed as inhibition of isoprenaline-induced bronchodilation incubated for 20 minsAntagonist activity at adrenergic beta2 receptor in isolated guinea pig trachea assessed as inhibition of isoprenaline-induced bronchodilation incubated for 20 mins
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmc.2018.04.038
44371406 11544 0 None - 0 Guinea pig 7.7 pKd = 7.7 Functional
The apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pigThe apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pig
ChEMBL 278 9 2 4 2.4 C/C(CCc1ccccc1)=N/OCC(O)CNC(C)C 10.1021/jm00180a007
CHEMBL1181107 11544 0 None - 0 Guinea pig 7.7 pKd = 7.7 Functional
The apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pigThe apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pig
ChEMBL 278 9 2 4 2.4 C/C(CCc1ccccc1)=N/OCC(O)CNC(C)C 10.1021/jm00180a007
CHEMBL155714 11544 0 None - 0 Guinea pig 7.7 pKd = 7.7 Functional
The apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pigThe apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pig
ChEMBL 278 9 2 4 2.4 C/C(CCc1ccccc1)=N/OCC(O)CNC(C)C 10.1021/jm00180a007
145947927 167178 0 None - 1 Guinea pig 7.7 pKd = 7.7 Functional
Antagonist activity at adrenergic beta2 receptor in isolated guinea pig trachea assessed as inhibition of isoprenaline-induced bronchodilation incubated for 20 minsAntagonist activity at adrenergic beta2 receptor in isolated guinea pig trachea assessed as inhibition of isoprenaline-induced bronchodilation incubated for 20 mins
ChEMBL 419 9 2 6 3.5 COc1ccccc1CCNCC(O)COc1cccc2c(=O)c3ccccc3oc12 10.1016/j.bmc.2018.04.038
CHEMBL4130151 167178 0 None - 1 Guinea pig 7.7 pKd = 7.7 Functional
Antagonist activity at adrenergic beta2 receptor in isolated guinea pig trachea assessed as inhibition of isoprenaline-induced bronchodilation incubated for 20 minsAntagonist activity at adrenergic beta2 receptor in isolated guinea pig trachea assessed as inhibition of isoprenaline-induced bronchodilation incubated for 20 mins
ChEMBL 419 9 2 6 3.5 COc1ccccc1CCNCC(O)COc1cccc2c(=O)c3ccccc3oc12 10.1016/j.bmc.2018.04.038
CHEMBL4302997 167178 0 None - 1 Guinea pig 7.7 pKd = 7.7 Functional
Antagonist activity at adrenergic beta2 receptor in isolated guinea pig trachea assessed as inhibition of isoprenaline-induced bronchodilation incubated for 20 minsAntagonist activity at adrenergic beta2 receptor in isolated guinea pig trachea assessed as inhibition of isoprenaline-induced bronchodilation incubated for 20 mins
ChEMBL 419 9 2 6 3.5 COc1ccccc1CCNCC(O)COc1cccc2c(=O)c3ccccc3oc12 10.1016/j.bmc.2018.04.038
12606706 92788 0 None - 0 Guinea pig 7.7 pKd = 7.7 Functional
The apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pigThe apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pig
ChEMBL 202 5 2 4 1.1 CC(C)=NOCC(O)CNC(C)(C)C 10.1021/jm00180a007
CHEMBL24480 92788 0 None - 0 Guinea pig 7.7 pKd = 7.7 Functional
The apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pigThe apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pig
ChEMBL 202 5 2 4 1.1 CC(C)=NOCC(O)CNC(C)(C)C 10.1021/jm00180a007
CHEMBL555848 92788 0 None - 0 Guinea pig 7.7 pKd = 7.7 Functional
The apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pigThe apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pig
ChEMBL 202 5 2 4 1.1 CC(C)=NOCC(O)CNC(C)(C)C 10.1021/jm00180a007
44287622 11881 0 None - 0 Guinea pig 7.6 pKd = 7.6 Functional
Antagonistic activity against beta-2 adrenergic receptor on isolated guinea pig tracheal stripsAntagonistic activity against beta-2 adrenergic receptor on isolated guinea pig tracheal strips
ChEMBL 258 7 2 4 2.4 CC(C)C(=NOCC(O)CNC(C)(C)C)C(C)C 10.1021/jm00380a001
CHEMBL1183276 11881 0 None - 0 Guinea pig 7.6 pKd = 7.6 Functional
Antagonistic activity against beta-2 adrenergic receptor on isolated guinea pig tracheal stripsAntagonistic activity against beta-2 adrenergic receptor on isolated guinea pig tracheal strips
ChEMBL 258 7 2 4 2.4 CC(C)C(=NOCC(O)CNC(C)(C)C)C(C)C 10.1021/jm00380a001
CHEMBL288140 11881 0 None - 0 Guinea pig 7.6 pKd = 7.6 Functional
Antagonistic activity against beta-2 adrenergic receptor on isolated guinea pig tracheal stripsAntagonistic activity against beta-2 adrenergic receptor on isolated guinea pig tracheal strips
ChEMBL 258 7 2 4 2.4 CC(C)C(=NOCC(O)CNC(C)(C)C)C(C)C 10.1021/jm00380a001
44307782 201857 3 None - 0 Guinea pig 6.7 pKd = 6.7 Functional
Antagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbacholAntagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbachol
ChEMBL 223 6 1 3 1.8 CC(C)N(C)CC(O)COc1ccccc1 10.1021/jm00119a011
CHEMBL66662 201857 3 None - 0 Guinea pig 6.7 pKd = 6.7 Functional
Antagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbacholAntagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbachol
ChEMBL 223 6 1 3 1.8 CC(C)N(C)CC(O)COc1ccccc1 10.1021/jm00119a011
44371537 50382 0 None - 0 Guinea pig 5.6 pKd = 5.6 Functional
Antagonist activity against beta-2 adrenergic receptor in isolated guinea pig tracheaAntagonist activity against beta-2 adrenergic receptor in isolated guinea pig trachea
ChEMBL 243 6 2 4 1.5 CC(C)NCC(O)COC(=O)C1CCCCC1 10.1021/jm00387a006
CHEMBL157557 50382 0 None - 0 Guinea pig 5.6 pKd = 5.6 Functional
Antagonist activity against beta-2 adrenergic receptor in isolated guinea pig tracheaAntagonist activity against beta-2 adrenergic receptor in isolated guinea pig trachea
ChEMBL 243 6 2 4 1.5 CC(C)NCC(O)COC(=O)C1CCCCC1 10.1021/jm00387a006
21595423 201812 0 None - 0 Guinea pig 7.6 pKd = 7.6 Functional
Antagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbacholAntagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbachol
ChEMBL 263 7 2 3 2.1 O[C@H](COCCCc1ccccc1)[C@@H]1CCCCN1 10.1021/jm00119a011
CHEMBL66324 201812 0 None - 0 Guinea pig 7.6 pKd = 7.6 Functional
Antagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbacholAntagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbachol
ChEMBL 263 7 2 3 2.1 O[C@H](COCCCc1ccccc1)[C@@H]1CCCCN1 10.1021/jm00119a011
44371561 49434 0 None - 0 Guinea pig 5.6 pKd = 5.6 Functional
Antagonist activity against beta-2 adrenergic receptor in isolated guinea pig tracheaAntagonist activity against beta-2 adrenergic receptor in isolated guinea pig trachea
ChEMBL 257 5 2 4 1.9 CC(C)(C)NCC(O)COC(=O)C1CCCCC1 10.1021/jm00387a006
CHEMBL156682 49434 0 None - 0 Guinea pig 5.6 pKd = 5.6 Functional
Antagonist activity against beta-2 adrenergic receptor in isolated guinea pig tracheaAntagonist activity against beta-2 adrenergic receptor in isolated guinea pig trachea
ChEMBL 257 5 2 4 1.9 CC(C)(C)NCC(O)COC(=O)C1CCCCC1 10.1021/jm00387a006
44371312 48978 2 None - 0 Guinea pig 4.6 pKd = 4.6 Functional
Antagonist activity against beta-2 adrenergic receptor in isolated guinea pig tracheaAntagonist activity against beta-2 adrenergic receptor in isolated guinea pig trachea
ChEMBL 203 5 2 4 0.7 CCC(=O)OCC(O)CNC(C)(C)C 10.1021/jm00387a006
CHEMBL156304 48978 2 None - 0 Guinea pig 4.6 pKd = 4.6 Functional
Antagonist activity against beta-2 adrenergic receptor in isolated guinea pig tracheaAntagonist activity against beta-2 adrenergic receptor in isolated guinea pig trachea
ChEMBL 203 5 2 4 0.7 CCC(=O)OCC(O)CNC(C)(C)C 10.1021/jm00387a006
5311116 2293 6 None -4365 3 Human 5.5 pKd = 5.5 Functional
Antagonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrsAntagonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrs
ChEMBL 484 15 5 8 2.2 N#Cc1cc(OCCOCC2CC2)ccc1OCC(CNCCNC(=O)Nc1ccc(cc1)O)O 10.1021/jm400348g
544 2293 6 None -4365 3 Human 5.5 pKd = 5.5 Functional
Antagonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrsAntagonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrs
ChEMBL 484 15 5 8 2.2 N#Cc1cc(OCCOCC2CC2)ccc1OCC(CNCCNC(=O)Nc1ccc(cc1)O)O 10.1021/jm400348g
CHEMBL207802 2293 6 None -4365 3 Human 5.5 pKd = 5.5 Functional
Antagonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrsAntagonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrs
ChEMBL 484 15 5 8 2.2 N#Cc1cc(OCCOCC2CC2)ccc1OCC(CNCCNC(=O)Nc1ccc(cc1)O)O 10.1021/jm400348g
14856222 172070 0 None - 0 Guinea pig 4.5 pKd = 4.5 Functional
Antagonist activity against beta-2 adrenergic receptor in isolated guinea pig tracheaAntagonist activity against beta-2 adrenergic receptor in isolated guinea pig trachea
ChEMBL 217 5 2 4 0.9 CC(C)C(=O)OCC(O)CNC(C)(C)C 10.1021/jm00387a006
CHEMBL449651 172070 0 None - 0 Guinea pig 4.5 pKd = 4.5 Functional
Antagonist activity against beta-2 adrenergic receptor in isolated guinea pig tracheaAntagonist activity against beta-2 adrenergic receptor in isolated guinea pig trachea
ChEMBL 217 5 2 4 0.9 CC(C)C(=O)OCC(O)CNC(C)(C)C 10.1021/jm00387a006
44381395 59161 0 None - 0 Dog 7.5 pKd = 7.5 Functional
Compound was evaluated for competitive antagonism of beta-2 adrenergic receptor in rat uterus measured as pA2 (-log KB)Compound was evaluated for competitive antagonism of beta-2 adrenergic receptor in rat uterus measured as pA2 (-log KB)
ChEMBL 289 6 2 5 1.2 CC(C)NCC(O)COC1=CC(=O)C(=O)c2ccccc21 10.1021/jm00373a008
CHEMBL171432 59161 0 None - 0 Dog 7.5 pKd = 7.5 Functional
Compound was evaluated for competitive antagonism of beta-2 adrenergic receptor in rat uterus measured as pA2 (-log KB)Compound was evaluated for competitive antagonism of beta-2 adrenergic receptor in rat uterus measured as pA2 (-log KB)
ChEMBL 289 6 2 5 1.2 CC(C)NCC(O)COC1=CC(=O)C(=O)c2ccccc21 10.1021/jm00373a008
44371486 14116 0 None - 0 Guinea pig 6.5 pKd = 6.5 Functional
The apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pigThe apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pig
ChEMBL 230 7 2 4 1.9 CCC/C(C)=N\OCC(O)CNC(C)(C)C 10.1021/jm00180a007
CHEMBL1161387 14116 0 None - 0 Guinea pig 6.5 pKd = 6.5 Functional
The apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pigThe apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pig
ChEMBL 230 7 2 4 1.9 CCC/C(C)=N\OCC(O)CNC(C)(C)C 10.1021/jm00180a007
CHEMBL1199437 14116 0 None - 0 Guinea pig 6.5 pKd = 6.5 Functional
The apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pigThe apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pig
ChEMBL 230 7 2 4 1.9 CCC/C(C)=N\OCC(O)CNC(C)(C)C 10.1021/jm00180a007
44287431 11109 0 None - 0 Guinea pig 8.5 pKd = 8.5 Functional
Antagonistic activity against beta-2 adrenergic receptor on isolated guinea pig tracheal stripsAntagonistic activity against beta-2 adrenergic receptor on isolated guinea pig tracheal strips
ChEMBL 244 8 2 4 2.0 CC(C)NCC(O)CON=C(C(C)C)C(C)C 10.1021/jm00380a001
CHEMBL1178793 11109 0 None - 0 Guinea pig 8.5 pKd = 8.5 Functional
Antagonistic activity against beta-2 adrenergic receptor on isolated guinea pig tracheal stripsAntagonistic activity against beta-2 adrenergic receptor on isolated guinea pig tracheal strips
ChEMBL 244 8 2 4 2.0 CC(C)NCC(O)CON=C(C(C)C)C(C)C 10.1021/jm00380a001
CHEMBL41839 11109 0 None - 0 Guinea pig 8.5 pKd = 8.5 Functional
Antagonistic activity against beta-2 adrenergic receptor on isolated guinea pig tracheal stripsAntagonistic activity against beta-2 adrenergic receptor on isolated guinea pig tracheal strips
ChEMBL 244 8 2 4 2.0 CC(C)NCC(O)CON=C(C(C)C)C(C)C 10.1021/jm00380a001
165193 3126 60 None -22 13 Guinea pig 8.5 pKd = 8.5 Functional
Antagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbacholAntagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbachol
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00119a011
2303 3126 60 None -22 13 Guinea pig 8.5 pKd = 8.5 Functional
Antagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbacholAntagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbachol
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00119a011
4946 3126 60 None -22 13 Guinea pig 8.5 pKd = 8.5 Functional
Antagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbacholAntagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbachol
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00119a011
564 3126 60 None -22 13 Guinea pig 8.5 pKd = 8.5 Functional
Antagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbacholAntagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbachol
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00119a011
62882 3126 60 None -22 13 Guinea pig 8.5 pKd = 8.5 Functional
Antagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbacholAntagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbachol
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00119a011
63 3126 60 None -22 13 Guinea pig 8.5 pKd = 8.5 Functional
Antagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbacholAntagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbachol
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00119a011
66366 3126 60 None -22 13 Guinea pig 8.5 pKd = 8.5 Functional
Antagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbacholAntagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbachol
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00119a011
91536 3126 60 None -22 13 Guinea pig 8.5 pKd = 8.5 Functional
Antagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbacholAntagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbachol
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00119a011
CHEMBL27 3126 60 None -22 13 Guinea pig 8.5 pKd = 8.5 Functional
Antagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbacholAntagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbachol
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00119a011
CHEMBL452861 3126 60 None -22 13 Guinea pig 8.5 pKd = 8.5 Functional
Antagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbacholAntagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbachol
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00119a011
DB00571 3126 60 None -22 13 Guinea pig 8.5 pKd = 8.5 Functional
Antagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbacholAntagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbachol
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00119a011
21595421 162904 0 None - 0 Guinea pig 8.5 pKd = 8.5 Functional
Antagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbacholAntagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbachol
ChEMBL 235 4 2 3 1.9 Cc1cccc(OC[C@@H](O)[C@@H]2CCCCN2)c1 10.1021/jm00119a011
CHEMBL419994 162904 0 None - 0 Guinea pig 8.5 pKd = 8.5 Functional
Antagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbacholAntagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbachol
ChEMBL 235 4 2 3 1.9 Cc1cccc(OC[C@@H](O)[C@@H]2CCCCN2)c1 10.1021/jm00119a011
165193 3126 60 None -22 13 Guinea pig 8.5 pKd = 8.5 Functional
The apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pigThe apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pig
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00180a007
2303 3126 60 None -22 13 Guinea pig 8.5 pKd = 8.5 Functional
The apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pigThe apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pig
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00180a007
4946 3126 60 None -22 13 Guinea pig 8.5 pKd = 8.5 Functional
The apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pigThe apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pig
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00180a007
564 3126 60 None -22 13 Guinea pig 8.5 pKd = 8.5 Functional
The apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pigThe apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pig
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00180a007
62882 3126 60 None -22 13 Guinea pig 8.5 pKd = 8.5 Functional
The apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pigThe apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pig
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00180a007
63 3126 60 None -22 13 Guinea pig 8.5 pKd = 8.5 Functional
The apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pigThe apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pig
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00180a007
66366 3126 60 None -22 13 Guinea pig 8.5 pKd = 8.5 Functional
The apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pigThe apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pig
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00180a007
91536 3126 60 None -22 13 Guinea pig 8.5 pKd = 8.5 Functional
The apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pigThe apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pig
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00180a007
CHEMBL27 3126 60 None -22 13 Guinea pig 8.5 pKd = 8.5 Functional
The apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pigThe apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pig
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00180a007
CHEMBL452861 3126 60 None -22 13 Guinea pig 8.5 pKd = 8.5 Functional
The apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pigThe apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pig
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00180a007
DB00571 3126 60 None -22 13 Guinea pig 8.5 pKd = 8.5 Functional
The apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pigThe apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pig
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00180a007
54758320 65172 0 None - 0 Human 7.5 pKd = 7.5 Functional
Antagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 794 20 5 8 6.1 O=C(CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1)NCCNCC(O)COc1cccc2[nH]ccc12 10.1021/jm2008562
CHEMBL1830620 65172 0 None - 0 Human 7.5 pKd = 7.5 Functional
Antagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 794 20 5 8 6.1 O=C(CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1)NCCNCC(O)COc1cccc2[nH]ccc12 10.1021/jm2008562
44371512 11551 0 None - 0 Guinea pig 7.5 pKd = 7.5 Functional
The apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pigThe apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pig
ChEMBL 292 8 2 4 2.8 C/C(CCc1ccccc1)=N/OCC(O)CNC(C)(C)C 10.1021/jm00180a007
CHEMBL1181139 11551 0 None - 0 Guinea pig 7.5 pKd = 7.5 Functional
The apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pigThe apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pig
ChEMBL 292 8 2 4 2.8 C/C(CCc1ccccc1)=N/OCC(O)CNC(C)(C)C 10.1021/jm00180a007
CHEMBL156871 11551 0 None - 0 Guinea pig 7.5 pKd = 7.5 Functional
The apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pigThe apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pig
ChEMBL 292 8 2 4 2.8 C/C(CCc1ccccc1)=N/OCC(O)CNC(C)(C)C 10.1021/jm00180a007
44276727 96852 0 None - 2 Guinea pig 7.5 pKd = 7.5 Functional
Beta-2 adrenergic receptor antagonistic activity on guinea pig tracheal chainsBeta-2 adrenergic receptor antagonistic activity on guinea pig tracheal chains
ChEMBL 263 6 2 3 2.2 Cc1ccc(OCC(O)CNC(C)C)c2c1CCC2 10.1021/jm00350a009
CHEMBL26917 96852 0 None - 2 Guinea pig 7.5 pKd = 7.5 Functional
Beta-2 adrenergic receptor antagonistic activity on guinea pig tracheal chainsBeta-2 adrenergic receptor antagonistic activity on guinea pig tracheal chains
ChEMBL 263 6 2 3 2.2 Cc1ccc(OCC(O)CNC(C)C)c2c1CCC2 10.1021/jm00350a009
12606710 13270 0 None - 0 Guinea pig 5.5 pKd = 5.5 Functional
The apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pigThe apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pig
ChEMBL 204 6 3 4 0.7 CC(C)NOCC(O)CNC(C)(C)C 10.1021/jm00180a007
CHEMBL1192661 13270 0 None - 0 Guinea pig 5.5 pKd = 5.5 Functional
The apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pigThe apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pig
ChEMBL 204 6 3 4 0.7 CC(C)NOCC(O)CNC(C)(C)C 10.1021/jm00180a007
CHEMBL543940 13270 0 None - 0 Guinea pig 5.5 pKd = 5.5 Functional
The apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pigThe apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pig
ChEMBL 204 6 3 4 0.7 CC(C)NOCC(O)CNC(C)(C)C 10.1021/jm00180a007
3486 3096 51 None - 0 Guinea pig 4.5 pKd = 4.5 Functional
Antagonist activity against beta-2 adrenergic receptor in isolated guinea pig tracheaAntagonist activity against beta-2 adrenergic receptor in isolated guinea pig trachea
ChEMBL 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C 10.1021/jm00387a006
4883 3096 51 None - 0 Guinea pig 4.5 pKd = 4.5 Functional
Antagonist activity against beta-2 adrenergic receptor in isolated guinea pig tracheaAntagonist activity against beta-2 adrenergic receptor in isolated guinea pig trachea
ChEMBL 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C 10.1021/jm00387a006
555 3096 51 None - 0 Guinea pig 4.5 pKd = 4.5 Functional
Antagonist activity against beta-2 adrenergic receptor in isolated guinea pig tracheaAntagonist activity against beta-2 adrenergic receptor in isolated guinea pig trachea
ChEMBL 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C 10.1021/jm00387a006
CHEMBL6995 3096 51 None - 0 Guinea pig 4.5 pKd = 4.5 Functional
Antagonist activity against beta-2 adrenergic receptor in isolated guinea pig tracheaAntagonist activity against beta-2 adrenergic receptor in isolated guinea pig trachea
ChEMBL 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C 10.1021/jm00387a006
DB01297 3096 51 None - 0 Guinea pig 4.5 pKd = 4.5 Functional
Antagonist activity against beta-2 adrenergic receptor in isolated guinea pig tracheaAntagonist activity against beta-2 adrenergic receptor in isolated guinea pig trachea
ChEMBL 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C 10.1021/jm00387a006
3486 3096 51 None - 0 Guinea pig 4.5 pKd = 4.5 Functional
Antagonistic activity against beta-2 adrenergic receptor on isolated guinea pig tracheal stripsAntagonistic activity against beta-2 adrenergic receptor on isolated guinea pig tracheal strips
ChEMBL 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C 10.1021/jm00380a001
4883 3096 51 None - 0 Guinea pig 4.5 pKd = 4.5 Functional
Antagonistic activity against beta-2 adrenergic receptor on isolated guinea pig tracheal stripsAntagonistic activity against beta-2 adrenergic receptor on isolated guinea pig tracheal strips
ChEMBL 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C 10.1021/jm00380a001
555 3096 51 None - 0 Guinea pig 4.5 pKd = 4.5 Functional
Antagonistic activity against beta-2 adrenergic receptor on isolated guinea pig tracheal stripsAntagonistic activity against beta-2 adrenergic receptor on isolated guinea pig tracheal strips
ChEMBL 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C 10.1021/jm00380a001
CHEMBL6995 3096 51 None - 0 Guinea pig 4.5 pKd = 4.5 Functional
Antagonistic activity against beta-2 adrenergic receptor on isolated guinea pig tracheal stripsAntagonistic activity against beta-2 adrenergic receptor on isolated guinea pig tracheal strips
ChEMBL 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C 10.1021/jm00380a001
DB01297 3096 51 None - 0 Guinea pig 4.5 pKd = 4.5 Functional
Antagonistic activity against beta-2 adrenergic receptor on isolated guinea pig tracheal stripsAntagonistic activity against beta-2 adrenergic receptor on isolated guinea pig tracheal strips
ChEMBL 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C 10.1021/jm00380a001
12606684 95615 3 None - 0 Guinea pig 7.5 pKd = 7.5 Functional
The apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pigThe apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pig
ChEMBL 203 6 2 3 1.4 CC(C)COCC(O)CNC(C)(C)C 10.1021/jm00180a007
CHEMBL1161388 95615 3 None - 0 Guinea pig 7.5 pKd = 7.5 Functional
The apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pigThe apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pig
ChEMBL 203 6 2 3 1.4 CC(C)COCC(O)CNC(C)(C)C 10.1021/jm00180a007
CHEMBL26003 95615 3 None - 0 Guinea pig 7.5 pKd = 7.5 Functional
The apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pigThe apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pig
ChEMBL 203 6 2 3 1.4 CC(C)COCC(O)CNC(C)(C)C 10.1021/jm00180a007
14201547 201862 0 None - 0 Guinea pig 7.5 pKd = 7.5 Functional
Antagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbacholAntagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbachol
ChEMBL 235 5 2 3 1.7 O[C@H](COCc1ccccc1)[C@H]1CCCCN1 10.1021/jm00119a011
CHEMBL66702 201862 0 None - 0 Guinea pig 7.5 pKd = 7.5 Functional
Antagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbacholAntagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbachol
ChEMBL 235 5 2 3 1.7 O[C@H](COCc1ccccc1)[C@H]1CCCCN1 10.1021/jm00119a011
12606701 11108 0 None - 0 Guinea pig 6.5 pKd = 6.5 Functional
The apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pigThe apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pig
ChEMBL 228 6 2 4 1.7 CC(C)NCC(O)CON=C1CCCCC1 10.1021/jm00180a007
CHEMBL1178787 11108 0 None - 0 Guinea pig 6.5 pKd = 6.5 Functional
The apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pigThe apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pig
ChEMBL 228 6 2 4 1.7 CC(C)NCC(O)CON=C1CCCCC1 10.1021/jm00180a007
CHEMBL41378 11108 0 None - 0 Guinea pig 6.5 pKd = 6.5 Functional
The apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pigThe apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pig
ChEMBL 228 6 2 4 1.7 CC(C)NCC(O)CON=C1CCCCC1 10.1021/jm00180a007
110857 12096 55 None - 0 Guinea pig 4.5 pKd = 4.5 Functional
The apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pigThe apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pig
ChEMBL 133 4 3 3 -0.7 CC(C)NCC(O)CO 10.1021/jm00180a007
CHEMBL1184370 12096 55 None - 0 Guinea pig 4.5 pKd = 4.5 Functional
The apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pigThe apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pig
ChEMBL 133 4 3 3 -0.7 CC(C)NCC(O)CO 10.1021/jm00180a007
CHEMBL346539 12096 55 None - 0 Guinea pig 4.5 pKd = 4.5 Functional
The apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pigThe apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pig
ChEMBL 133 4 3 3 -0.7 CC(C)NCC(O)CO 10.1021/jm00180a007
12606685 11547 0 None - 0 Guinea pig 5.5 pKd = 5.5 Functional
The apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pigThe apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pig
ChEMBL 189 7 2 3 1.0 CC(C)COCC(O)CNC(C)C 10.1021/jm00180a007
CHEMBL1181117 11547 0 None - 0 Guinea pig 5.5 pKd = 5.5 Functional
The apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pigThe apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pig
ChEMBL 189 7 2 3 1.0 CC(C)COCC(O)CNC(C)C 10.1021/jm00180a007
CHEMBL156258 11547 0 None - 0 Guinea pig 5.5 pKd = 5.5 Functional
The apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pigThe apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pig
ChEMBL 189 7 2 3 1.0 CC(C)COCC(O)CNC(C)C 10.1021/jm00180a007
12606702 11893 0 None - 0 Guinea pig 7.4 pKd = 7.4 Functional
Antagonistic activity against beta-2 adrenergic receptor on isolated guinea pig tracheal stripsAntagonistic activity against beta-2 adrenergic receptor on isolated guinea pig tracheal strips
ChEMBL 242 5 2 4 2.1 CC(C)(C)NCC(O)CON=C1CCCCC1 10.1021/jm00380a001
CHEMBL1161383 11893 0 None - 0 Guinea pig 7.4 pKd = 7.4 Functional
Antagonistic activity against beta-2 adrenergic receptor on isolated guinea pig tracheal stripsAntagonistic activity against beta-2 adrenergic receptor on isolated guinea pig tracheal strips
ChEMBL 242 5 2 4 2.1 CC(C)(C)NCC(O)CON=C1CCCCC1 10.1021/jm00380a001
CHEMBL1183312 11893 0 None - 0 Guinea pig 7.4 pKd = 7.4 Functional
Antagonistic activity against beta-2 adrenergic receptor on isolated guinea pig tracheal stripsAntagonistic activity against beta-2 adrenergic receptor on isolated guinea pig tracheal strips
ChEMBL 242 5 2 4 2.1 CC(C)(C)NCC(O)CON=C1CCCCC1 10.1021/jm00380a001
CHEMBL289868 11893 0 None - 0 Guinea pig 7.4 pKd = 7.4 Functional
Antagonistic activity against beta-2 adrenergic receptor on isolated guinea pig tracheal stripsAntagonistic activity against beta-2 adrenergic receptor on isolated guinea pig tracheal strips
ChEMBL 242 5 2 4 2.1 CC(C)(C)NCC(O)CON=C1CCCCC1 10.1021/jm00380a001
1531 2226 64 None - 7 Guinea pig 7.4 pKd = 7.4 Functional
The compound was evaluated for the antagonistic activity against beta-2 adrenergic receptor.The compound was evaluated for the antagonistic activity against beta-2 adrenergic receptor.
ChEMBL 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O 10.1021/jm00156a019
3869 2226 64 None - 7 Guinea pig 7.4 pKd = 7.4 Functional
The compound was evaluated for the antagonistic activity against beta-2 adrenergic receptor.The compound was evaluated for the antagonistic activity against beta-2 adrenergic receptor.
ChEMBL 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O 10.1021/jm00156a019
7207 2226 64 None - 7 Guinea pig 7.4 pKd = 7.4 Functional
The compound was evaluated for the antagonistic activity against beta-2 adrenergic receptor.The compound was evaluated for the antagonistic activity against beta-2 adrenergic receptor.
ChEMBL 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O 10.1021/jm00156a019
CHEMBL429 2226 64 None - 7 Guinea pig 7.4 pKd = 7.4 Functional
The compound was evaluated for the antagonistic activity against beta-2 adrenergic receptor.The compound was evaluated for the antagonistic activity against beta-2 adrenergic receptor.
ChEMBL 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O 10.1021/jm00156a019
DB00598 2226 64 None - 7 Guinea pig 7.4 pKd = 7.4 Functional
The compound was evaluated for the antagonistic activity against beta-2 adrenergic receptor.The compound was evaluated for the antagonistic activity against beta-2 adrenergic receptor.
ChEMBL 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O 10.1021/jm00156a019
44287467 11104 0 None - 0 Guinea pig 8.4 pKd = 8.4 Functional
Antagonistic activity against beta-2 adrenergic receptor on isolated guinea pig tracheal stripsAntagonistic activity against beta-2 adrenergic receptor on isolated guinea pig tracheal strips
ChEMBL 216 8 2 4 1.5 CCC(CC)=NOCC(O)CNC(C)C 10.1021/jm00380a001
CHEMBL1178777 11104 0 None - 0 Guinea pig 8.4 pKd = 8.4 Functional
Antagonistic activity against beta-2 adrenergic receptor on isolated guinea pig tracheal stripsAntagonistic activity against beta-2 adrenergic receptor on isolated guinea pig tracheal strips
ChEMBL 216 8 2 4 1.5 CCC(CC)=NOCC(O)CNC(C)C 10.1021/jm00380a001
CHEMBL40626 11104 0 None - 0 Guinea pig 8.4 pKd = 8.4 Functional
Antagonistic activity against beta-2 adrenergic receptor on isolated guinea pig tracheal stripsAntagonistic activity against beta-2 adrenergic receptor on isolated guinea pig tracheal strips
ChEMBL 216 8 2 4 1.5 CCC(CC)=NOCC(O)CNC(C)C 10.1021/jm00380a001
145947241 167060 0 None - 1 Guinea pig 7.4 pKd = 7.4 Functional
Antagonist activity at adrenergic beta2 receptor in isolated guinea pig trachea assessed as inhibition of isoprenaline-induced bronchodilation incubated for 20 minsAntagonist activity at adrenergic beta2 receptor in isolated guinea pig trachea assessed as inhibition of isoprenaline-induced bronchodilation incubated for 20 mins
ChEMBL 449 10 2 7 3.5 COc1ccc(CCNCC(O)COc2cccc3c(=O)c4ccccc4oc23)cc1OC 10.1016/j.bmc.2018.04.038
CHEMBL4128940 167060 0 None - 1 Guinea pig 7.4 pKd = 7.4 Functional
Antagonist activity at adrenergic beta2 receptor in isolated guinea pig trachea assessed as inhibition of isoprenaline-induced bronchodilation incubated for 20 minsAntagonist activity at adrenergic beta2 receptor in isolated guinea pig trachea assessed as inhibition of isoprenaline-induced bronchodilation incubated for 20 mins
ChEMBL 449 10 2 7 3.5 COc1ccc(CCNCC(O)COc2cccc3c(=O)c4ccccc4oc23)cc1OC 10.1016/j.bmc.2018.04.038
CHEMBL4301544 167060 0 None - 1 Guinea pig 7.4 pKd = 7.4 Functional
Antagonist activity at adrenergic beta2 receptor in isolated guinea pig trachea assessed as inhibition of isoprenaline-induced bronchodilation incubated for 20 minsAntagonist activity at adrenergic beta2 receptor in isolated guinea pig trachea assessed as inhibition of isoprenaline-induced bronchodilation incubated for 20 mins
ChEMBL 449 10 2 7 3.5 COc1ccc(CCNCC(O)COc2cccc3c(=O)c4ccccc4oc23)cc1OC 10.1016/j.bmc.2018.04.038
12606708 12954 0 None - 0 Guinea pig 6.4 pKd = 6.4 Functional
The apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pigThe apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pig
ChEMBL 282 6 2 4 2.6 CC(C)NCC(O)CO/N=C1\CC2CCC1(C)C2(C)C 10.1021/jm00180a007
CHEMBL1190195 12954 0 None - 0 Guinea pig 6.4 pKd = 6.4 Functional
The apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pigThe apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pig
ChEMBL 282 6 2 4 2.6 CC(C)NCC(O)CO/N=C1\CC2CCC1(C)C2(C)C 10.1021/jm00180a007
CHEMBL540337 12954 0 None - 0 Guinea pig 6.4 pKd = 6.4 Functional
The apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pigThe apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pig
ChEMBL 282 6 2 4 2.6 CC(C)NCC(O)CO/N=C1\CC2CCC1(C)C2(C)C 10.1021/jm00180a007
12606686 92413 3 None - 0 Guinea pig 6.4 pKd = 6.4 Functional
The apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pigThe apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pig
ChEMBL 189 5 2 3 1.2 CC(C)OCC(O)CNC(C)(C)C 10.1021/jm00180a007
CHEMBL1161385 92413 3 None - 0 Guinea pig 6.4 pKd = 6.4 Functional
The apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pigThe apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pig
ChEMBL 189 5 2 3 1.2 CC(C)OCC(O)CNC(C)(C)C 10.1021/jm00180a007
CHEMBL24391 92413 3 None - 0 Guinea pig 6.4 pKd = 6.4 Functional
The apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pigThe apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pig
ChEMBL 189 5 2 3 1.2 CC(C)OCC(O)CNC(C)(C)C 10.1021/jm00180a007
44371642 48938 0 None - 0 Guinea pig 5.4 pKd = 5.4 Functional
Antagonist activity against beta-2 adrenergic receptor in isolated guinea pig tracheaAntagonist activity against beta-2 adrenergic receptor in isolated guinea pig trachea
ChEMBL 203 6 2 4 0.5 CC(C)NCC(O)COC(=O)C(C)C 10.1021/jm00387a006
CHEMBL156271 48938 0 None - 0 Guinea pig 5.4 pKd = 5.4 Functional
Antagonist activity against beta-2 adrenergic receptor in isolated guinea pig tracheaAntagonist activity against beta-2 adrenergic receptor in isolated guinea pig trachea
ChEMBL 203 6 2 4 0.5 CC(C)NCC(O)COC(=O)C(C)C 10.1021/jm00387a006
165193 3126 60 None -22 13 Guinea pig 7.4 pKd = 7.4 Functional
Antagonist activity of compound against Beta-2 adrenergic receptor in isolated guinea pig tracheaAntagonist activity of compound against Beta-2 adrenergic receptor in isolated guinea pig trachea
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00140a015
2303 3126 60 None -22 13 Guinea pig 7.4 pKd = 7.4 Functional
Antagonist activity of compound against Beta-2 adrenergic receptor in isolated guinea pig tracheaAntagonist activity of compound against Beta-2 adrenergic receptor in isolated guinea pig trachea
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00140a015
4946 3126 60 None -22 13 Guinea pig 7.4 pKd = 7.4 Functional
Antagonist activity of compound against Beta-2 adrenergic receptor in isolated guinea pig tracheaAntagonist activity of compound against Beta-2 adrenergic receptor in isolated guinea pig trachea
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00140a015
564 3126 60 None -22 13 Guinea pig 7.4 pKd = 7.4 Functional
Antagonist activity of compound against Beta-2 adrenergic receptor in isolated guinea pig tracheaAntagonist activity of compound against Beta-2 adrenergic receptor in isolated guinea pig trachea
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00140a015
62882 3126 60 None -22 13 Guinea pig 7.4 pKd = 7.4 Functional
Antagonist activity of compound against Beta-2 adrenergic receptor in isolated guinea pig tracheaAntagonist activity of compound against Beta-2 adrenergic receptor in isolated guinea pig trachea
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00140a015
63 3126 60 None -22 13 Guinea pig 7.4 pKd = 7.4 Functional
Antagonist activity of compound against Beta-2 adrenergic receptor in isolated guinea pig tracheaAntagonist activity of compound against Beta-2 adrenergic receptor in isolated guinea pig trachea
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00140a015
66366 3126 60 None -22 13 Guinea pig 7.4 pKd = 7.4 Functional
Antagonist activity of compound against Beta-2 adrenergic receptor in isolated guinea pig tracheaAntagonist activity of compound against Beta-2 adrenergic receptor in isolated guinea pig trachea
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00140a015
91536 3126 60 None -22 13 Guinea pig 7.4 pKd = 7.4 Functional
Antagonist activity of compound against Beta-2 adrenergic receptor in isolated guinea pig tracheaAntagonist activity of compound against Beta-2 adrenergic receptor in isolated guinea pig trachea
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00140a015
CHEMBL27 3126 60 None -22 13 Guinea pig 7.4 pKd = 7.4 Functional
Antagonist activity of compound against Beta-2 adrenergic receptor in isolated guinea pig tracheaAntagonist activity of compound against Beta-2 adrenergic receptor in isolated guinea pig trachea
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00140a015
CHEMBL452861 3126 60 None -22 13 Guinea pig 7.4 pKd = 7.4 Functional
Antagonist activity of compound against Beta-2 adrenergic receptor in isolated guinea pig tracheaAntagonist activity of compound against Beta-2 adrenergic receptor in isolated guinea pig trachea
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00140a015
DB00571 3126 60 None -22 13 Guinea pig 7.4 pKd = 7.4 Functional
Antagonist activity of compound against Beta-2 adrenergic receptor in isolated guinea pig tracheaAntagonist activity of compound against Beta-2 adrenergic receptor in isolated guinea pig trachea
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00140a015
361497 48800 2 None - 0 Guinea pig 6.3 pKd = 6.3 Functional
Antagonist activity against beta-2 adrenergic receptor in isolated guinea pig tracheaAntagonist activity against beta-2 adrenergic receptor in isolated guinea pig trachea
ChEMBL 243 6 2 5 1.3 CC(C)NCC(O)COC(=O)c1cccs1 10.1021/jm00387a006
CHEMBL156147 48800 2 None - 0 Guinea pig 6.3 pKd = 6.3 Functional
Antagonist activity against beta-2 adrenergic receptor in isolated guinea pig tracheaAntagonist activity against beta-2 adrenergic receptor in isolated guinea pig trachea
ChEMBL 243 6 2 5 1.3 CC(C)NCC(O)COC(=O)c1cccs1 10.1021/jm00387a006
21595420 202008 0 None - 0 Guinea pig 7.3 pKd = 7.3 Functional
Antagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbacholAntagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbachol
ChEMBL 235 4 2 3 1.9 Cc1ccc(OC[C@@H](O)[C@@H]2CCCCN2)cc1 10.1021/jm00119a011
CHEMBL67631 202008 0 None - 0 Guinea pig 7.3 pKd = 7.3 Functional
Antagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbacholAntagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbachol
ChEMBL 235 4 2 3 1.9 Cc1ccc(OC[C@@H](O)[C@@H]2CCCCN2)cc1 10.1021/jm00119a011
127940 203166 4 None - 0 Guinea pig 7.3 pKd = 7.3 Functional
The compound was evaluated for the antagonistic activity against beta-2 adrenergic receptor.The compound was evaluated for the antagonistic activity against beta-2 adrenergic receptor.
ChEMBL 351 8 4 3 2.9 CC(CCc1ccccc1)NCC(O)c1cc(C(N)=O)c2[nH]ccc2c1 10.1021/jm00156a019
CHEMBL7585 203166 4 None - 0 Guinea pig 7.3 pKd = 7.3 Functional
The compound was evaluated for the antagonistic activity against beta-2 adrenergic receptor.The compound was evaluated for the antagonistic activity against beta-2 adrenergic receptor.
ChEMBL 351 8 4 3 2.9 CC(CCc1ccccc1)NCC(O)c1cc(C(N)=O)c2[nH]ccc2c1 10.1021/jm00156a019
44371426 14177 0 None - 0 Guinea pig 6.3 pKd = 6.3 Functional
The apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pigThe apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pig
ChEMBL 216 6 2 4 1.5 CC/C(C)=N\OCC(O)CNC(C)(C)C 10.1021/jm00180a007
CHEMBL1161384 14177 0 None - 0 Guinea pig 6.3 pKd = 6.3 Functional
The apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pigThe apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pig
ChEMBL 216 6 2 4 1.5 CC/C(C)=N\OCC(O)CNC(C)(C)C 10.1021/jm00180a007
CHEMBL1199902 14177 0 None - 0 Guinea pig 6.3 pKd = 6.3 Functional
The apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pigThe apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pig
ChEMBL 216 6 2 4 1.5 CC/C(C)=N\OCC(O)CNC(C)(C)C 10.1021/jm00180a007
123686 1942 44 None -74 3 Human 7.3 pKd = 7.3 Functional
Antagonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrsAntagonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrs
ChEMBL 354 9 4 5 1.7 C1=CC=C(C=C1)NC(=O)NCCNCC(COC2=CC=CC=C2C#N)O 10.1021/jm400348g
12581 1942 44 None -74 3 Human 7.3 pKd = 7.3 Functional
Antagonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrsAntagonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrs
ChEMBL 354 9 4 5 1.7 C1=CC=C(C=C1)NC(=O)NCCNCC(COC2=CC=CC=C2C#N)O 10.1021/jm400348g
CHEMBL11268 1942 44 None -74 3 Human 7.3 pKd = 7.3 Functional
Antagonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrsAntagonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrs
ChEMBL 354 9 4 5 1.7 C1=CC=C(C=C1)NC(=O)NCCNCC(COC2=CC=CC=C2C#N)O 10.1021/jm400348g
157717 59911 33 None - 1 Guinea pig 5.2 pKd = 5.2 Functional
Beta-2 adrenergic receptor antagonistic activity on guinea pig tracheal chainsBeta-2 adrenergic receptor antagonistic activity on guinea pig tracheal chains
ChEMBL 267 9 2 4 1.6 COCCc1ccc(OC[C@H](O)CNC(C)C)cc1 10.1021/jm00350a009
CHEMBL1741004 59911 33 None - 1 Guinea pig 5.2 pKd = 5.2 Functional
Beta-2 adrenergic receptor antagonistic activity on guinea pig tracheal chainsBeta-2 adrenergic receptor antagonistic activity on guinea pig tracheal chains
ChEMBL 267 9 2 4 1.6 COCCc1ccc(OC[C@H](O)CNC(C)C)cc1 10.1021/jm00350a009
CHEMBL2062339 59911 33 None - 1 Guinea pig 5.2 pKd = 5.2 Functional
Beta-2 adrenergic receptor antagonistic activity on guinea pig tracheal chainsBeta-2 adrenergic receptor antagonistic activity on guinea pig tracheal chains
ChEMBL 267 9 2 4 1.6 COCCc1ccc(OC[C@H](O)CNC(C)C)cc1 10.1021/jm00350a009
44287522 11105 0 None - 0 Guinea pig 8.2 pKd = 8.2 Functional
Antagonistic activity against beta-2 adrenergic receptor on isolated guinea pig tracheal stripsAntagonistic activity against beta-2 adrenergic receptor on isolated guinea pig tracheal strips
ChEMBL 244 10 2 4 2.3 CCCC(CCC)=NOCC(O)CNC(C)C 10.1021/jm00380a001
CHEMBL1178778 11105 0 None - 0 Guinea pig 8.2 pKd = 8.2 Functional
Antagonistic activity against beta-2 adrenergic receptor on isolated guinea pig tracheal stripsAntagonistic activity against beta-2 adrenergic receptor on isolated guinea pig tracheal strips
ChEMBL 244 10 2 4 2.3 CCCC(CCC)=NOCC(O)CNC(C)C 10.1021/jm00380a001
CHEMBL40783 11105 0 None - 0 Guinea pig 8.2 pKd = 8.2 Functional
Antagonistic activity against beta-2 adrenergic receptor on isolated guinea pig tracheal stripsAntagonistic activity against beta-2 adrenergic receptor on isolated guinea pig tracheal strips
ChEMBL 244 10 2 4 2.3 CCCC(CCC)=NOCC(O)CNC(C)C 10.1021/jm00380a001
4408839 13660 32 None - 0 Guinea pig 4.2 pKd = 4.2 Functional
The apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pigThe apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pig
ChEMBL 202 4 3 3 1.1 CC(C)(C)NCC(O)CNC(C)(C)C 10.1021/jm00180a007
CHEMBL1195496 13660 32 None - 0 Guinea pig 4.2 pKd = 4.2 Functional
The apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pigThe apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pig
ChEMBL 202 4 3 3 1.1 CC(C)(C)NCC(O)CNC(C)(C)C 10.1021/jm00180a007
CHEMBL554669 13660 32 None - 0 Guinea pig 4.2 pKd = 4.2 Functional
The apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pigThe apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pig
ChEMBL 202 4 3 3 1.1 CC(C)(C)NCC(O)CNC(C)(C)C 10.1021/jm00180a007
145947596 167127 0 None - 1 Guinea pig 6.2 pKd = 6.2 Functional
Antagonist activity at adrenergic beta2 receptor in isolated guinea pig trachea assessed as inhibition of isoprenaline-induced bronchodilation incubated for 20 minsAntagonist activity at adrenergic beta2 receptor in isolated guinea pig trachea assessed as inhibition of isoprenaline-induced bronchodilation incubated for 20 mins
ChEMBL 355 5 2 5 3.4 Cc1cccc2c(=O)c3ccc(OCC(O)CNC(C)(C)C)cc3oc12 10.1016/j.bmc.2018.04.038
CHEMBL4128231 167127 0 None - 1 Guinea pig 6.2 pKd = 6.2 Functional
Antagonist activity at adrenergic beta2 receptor in isolated guinea pig trachea assessed as inhibition of isoprenaline-induced bronchodilation incubated for 20 minsAntagonist activity at adrenergic beta2 receptor in isolated guinea pig trachea assessed as inhibition of isoprenaline-induced bronchodilation incubated for 20 mins
ChEMBL 355 5 2 5 3.4 Cc1cccc2c(=O)c3ccc(OCC(O)CNC(C)(C)C)cc3oc12 10.1016/j.bmc.2018.04.038
CHEMBL4302343 167127 0 None - 1 Guinea pig 6.2 pKd = 6.2 Functional
Antagonist activity at adrenergic beta2 receptor in isolated guinea pig trachea assessed as inhibition of isoprenaline-induced bronchodilation incubated for 20 minsAntagonist activity at adrenergic beta2 receptor in isolated guinea pig trachea assessed as inhibition of isoprenaline-induced bronchodilation incubated for 20 mins
ChEMBL 355 5 2 5 3.4 Cc1cccc2c(=O)c3ccc(OCC(O)CNC(C)(C)C)cc3oc12 10.1016/j.bmc.2018.04.038
121848 130175 4 None - 2 Guinea pig 7.2 pKd = 7.2 Functional
Beta-2 adrenergic receptor antagonistic activity on guinea pig tracheal chainsBeta-2 adrenergic receptor antagonistic activity on guinea pig tracheal chains
ChEMBL 324 5 2 4 3.2 CC(C)(C)NCC(O)CON=C1c2ccccc2-c2ccccc21 10.1021/jm00350a009
CHEMBL368457 130175 4 None - 2 Guinea pig 7.2 pKd = 7.2 Functional
Beta-2 adrenergic receptor antagonistic activity on guinea pig tracheal chainsBeta-2 adrenergic receptor antagonistic activity on guinea pig tracheal chains
ChEMBL 324 5 2 4 3.2 CC(C)(C)NCC(O)CON=C1c2ccccc2-c2ccccc21 10.1021/jm00350a009
155774 4021 33 None -64 3 Human 6.2 pKd = 6.2 Functional
Antagonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrsAntagonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrs
ChEMBL 339 8 4 6 -0.2 OC(COc1ccc(cc1)O)CNCCNC(=O)N1CCOCC1 10.1021/jm400348g
2848 4021 33 None -64 3 Human 6.2 pKd = 6.2 Functional
Antagonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrsAntagonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrs
ChEMBL 339 8 4 6 -0.2 OC(COc1ccc(cc1)O)CNCCNC(=O)N1CCOCC1 10.1021/jm400348g
538 4021 33 None -64 3 Human 6.2 pKd = 6.2 Functional
Antagonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrsAntagonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrs
ChEMBL 339 8 4 6 -0.2 OC(COc1ccc(cc1)O)CNCCNC(=O)N1CCOCC1 10.1021/jm400348g
CHEMBL75753 4021 33 None -64 3 Human 6.2 pKd = 6.2 Functional
Antagonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrsAntagonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrs
ChEMBL 339 8 4 6 -0.2 OC(COc1ccc(cc1)O)CNCCNC(=O)N1CCOCC1 10.1021/jm400348g
DB13781 4021 33 None -64 3 Human 6.2 pKd = 6.2 Functional
Antagonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrsAntagonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrs
ChEMBL 339 8 4 6 -0.2 OC(COc1ccc(cc1)O)CNCCNC(=O)N1CCOCC1 10.1021/jm400348g
2840793 201926 27 None - 0 Guinea pig 8.2 pKd = 8.2 Functional
Antagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbacholAntagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbachol
ChEMBL 223 6 2 3 1.7 Cc1ccc(OCC(O)CNC(C)C)cc1 10.1021/jm00119a011
CHEMBL67151 201926 27 None - 0 Guinea pig 8.2 pKd = 8.2 Functional
Antagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbacholAntagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbachol
ChEMBL 223 6 2 3 1.7 Cc1ccc(OCC(O)CNC(C)C)cc1 10.1021/jm00119a011
54758415 65173 0 None - 0 Human 8.1 pKd = 8.1 Functional
Antagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 882 26 5 10 6.1 O=C(CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1)NCCOCCOCCNCC(O)COc1cccc2[nH]ccc12 10.1021/jm2008562
CHEMBL1830621 65173 0 None - 0 Human 8.1 pKd = 8.1 Functional
Antagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
ChEMBL 882 26 5 10 6.1 O=C(CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1)NCCOCCOCCNCC(O)COc1cccc2[nH]ccc12 10.1021/jm2008562
56598831 88699 0 None -1023 3 Human 5.2 pKd = 5.2 Functional
Antagonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrsAntagonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrs
ChEMBL 459 15 5 7 2.3 O=C(NCCNCC(O)COc1ccc(OCCOCC2CC2)cc1)Nc1ccc(O)cc1 10.1021/jm400348g
CHEMBL2348220 88699 0 None -1023 3 Human 5.2 pKd = 5.2 Functional
Antagonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrsAntagonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrs
ChEMBL 459 15 5 7 2.3 O=C(NCCNCC(O)COc1ccc(OCCOCC2CC2)cc1)Nc1ccc(O)cc1 10.1021/jm400348g
CHEMBL2365796 88699 0 None -1023 3 Human 5.2 pKd = 5.2 Functional
Antagonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrsAntagonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrs
ChEMBL 459 15 5 7 2.3 O=C(NCCNCC(O)COc1ccc(OCCOCC2CC2)cc1)Nc1ccc(O)cc1 10.1021/jm400348g
12606701 11108 0 None - 0 Guinea pig 7.1 pKd = 7.1 Functional
Antagonistic activity against beta-2 adrenergic receptor on isolated guinea pig tracheal stripsAntagonistic activity against beta-2 adrenergic receptor on isolated guinea pig tracheal strips
ChEMBL 228 6 2 4 1.7 CC(C)NCC(O)CON=C1CCCCC1 10.1021/jm00380a001
CHEMBL1178787 11108 0 None - 0 Guinea pig 7.1 pKd = 7.1 Functional
Antagonistic activity against beta-2 adrenergic receptor on isolated guinea pig tracheal stripsAntagonistic activity against beta-2 adrenergic receptor on isolated guinea pig tracheal strips
ChEMBL 228 6 2 4 1.7 CC(C)NCC(O)CON=C1CCCCC1 10.1021/jm00380a001
CHEMBL41378 11108 0 None - 0 Guinea pig 7.1 pKd = 7.1 Functional
Antagonistic activity against beta-2 adrenergic receptor on isolated guinea pig tracheal stripsAntagonistic activity against beta-2 adrenergic receptor on isolated guinea pig tracheal strips
ChEMBL 228 6 2 4 1.7 CC(C)NCC(O)CON=C1CCCCC1 10.1021/jm00380a001
12778441 77948 0 None - 0 Guinea pig 7.1 pKd = 7.1 Functional
Beta-2 adrenergic receptor antagonistic activity on guinea pig tracheal chainsBeta-2 adrenergic receptor antagonistic activity on guinea pig tracheal chains
ChEMBL 338 7 2 4 3.6 CCC(C)(C)NC[C@H](O)CON=C1c2ccccc2-c2ccccc21 10.1021/jm00350a009
CHEMBL2110257 77948 0 None - 0 Guinea pig 7.1 pKd = 7.1 Functional
Beta-2 adrenergic receptor antagonistic activity on guinea pig tracheal chainsBeta-2 adrenergic receptor antagonistic activity on guinea pig tracheal chains
ChEMBL 338 7 2 4 3.6 CCC(C)(C)NC[C@H](O)CON=C1c2ccccc2-c2ccccc21 10.1021/jm00350a009
11768868 13035 4 None - 0 Guinea pig 4.1 pKd = 4.1 Functional
The apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pigThe apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pig
ChEMBL 161 4 2 3 0.4 COCC(O)CNC(C)(C)C 10.1021/jm00180a007
CHEMBL1190805 13035 4 None - 0 Guinea pig 4.1 pKd = 4.1 Functional
The apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pigThe apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pig
ChEMBL 161 4 2 3 0.4 COCC(O)CNC(C)(C)C 10.1021/jm00180a007
CHEMBL541607 13035 4 None - 0 Guinea pig 4.1 pKd = 4.1 Functional
The apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pigThe apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pig
ChEMBL 161 4 2 3 0.4 COCC(O)CNC(C)(C)C 10.1021/jm00180a007
12606703 13459 0 None - 0 Guinea pig 6.1 pKd = 6.1 Functional
The apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pigThe apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pig
ChEMBL 276 8 2 4 2.5 CC(/C=C/c1ccccc1)=N\OCC(O)CNC(C)C 10.1021/jm00180a007
CHEMBL1194069 13459 0 None - 0 Guinea pig 6.1 pKd = 6.1 Functional
The apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pigThe apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pig
ChEMBL 276 8 2 4 2.5 CC(/C=C/c1ccccc1)=N\OCC(O)CNC(C)C 10.1021/jm00180a007
CHEMBL545575 13459 0 None - 0 Guinea pig 6.1 pKd = 6.1 Functional
The apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pigThe apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pig
ChEMBL 276 8 2 4 2.5 CC(/C=C/c1ccccc1)=N\OCC(O)CNC(C)C 10.1021/jm00180a007
90831 12101 32 None - 0 Guinea pig 4.1 pKd = 4.1 Functional
The apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pigThe apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pig
ChEMBL 147 3 3 3 -0.3 CC(C)(C)NCC(O)CO 10.1021/jm00180a007
CHEMBL1184387 12101 32 None - 0 Guinea pig 4.1 pKd = 4.1 Functional
The apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pigThe apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pig
ChEMBL 147 3 3 3 -0.3 CC(C)(C)NCC(O)CO 10.1021/jm00180a007
CHEMBL347002 12101 32 None - 0 Guinea pig 4.1 pKd = 4.1 Functional
The apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pigThe apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pig
ChEMBL 147 3 3 3 -0.3 CC(C)(C)NCC(O)CO 10.1021/jm00180a007
44307572 201356 0 None - 0 Guinea pig 7.1 pKd = 7.1 Functional
Antagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbacholAntagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbachol
ChEMBL 235 4 1 3 1.9 CN1CCCC[C@H]1[C@H](O)COc1ccccc1 10.1021/jm00119a011
CHEMBL63582 201356 0 None - 0 Guinea pig 7.1 pKd = 7.1 Functional
Antagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbacholAntagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbachol
ChEMBL 235 4 1 3 1.9 CN1CCCC[C@H]1[C@H](O)COc1ccccc1 10.1021/jm00119a011
66653268 87809 0 None -3311 3 Human 6.1 pKd = 6.1 Functional
Antagonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrsAntagonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrs
ChEMBL 491 14 4 6 3.8 O=C(NCCNCC(O)COc1ccc(OCCOC2CCCC2)cc1)Nc1cccc(Cl)c1 10.1021/jm400348g
CHEMBL2348201 87809 0 None -3311 3 Human 6.1 pKd = 6.1 Functional
Antagonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrsAntagonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrs
ChEMBL 491 14 4 6 3.8 O=C(NCCNCC(O)COc1ccc(OCCOC2CCCC2)cc1)Nc1cccc(Cl)c1 10.1021/jm400348g
14201539 201820 0 None - 0 Guinea pig 7.1 pKd = 7.1 Functional
Antagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbacholAntagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbachol
ChEMBL 271 4 2 3 2.7 O[C@H](COc1ccc2ccccc2c1)[C@H]1CCCCN1 10.1021/jm00119a011
CHEMBL66384 201820 0 None - 0 Guinea pig 7.1 pKd = 7.1 Functional
Antagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbacholAntagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbachol
ChEMBL 271 4 2 3 2.7 O[C@H](COc1ccc2ccccc2c1)[C@H]1CCCCN1 10.1021/jm00119a011
12733302 165779 1 None - 0 Guinea pig 7.1 pKd = 7.1 Functional
Antagonist activity of compound against Beta-2 adrenergic receptor in isolated guinea pig tracheaAntagonist activity of compound against Beta-2 adrenergic receptor in isolated guinea pig trachea
ChEMBL 249 3 2 4 2.0 CC(C)(C)NCC(O)C1=COc2ccccc2O1 10.1021/jm00140a015
CHEMBL427310 165779 1 None - 0 Guinea pig 7.1 pKd = 7.1 Functional
Antagonist activity of compound against Beta-2 adrenergic receptor in isolated guinea pig tracheaAntagonist activity of compound against Beta-2 adrenergic receptor in isolated guinea pig trachea
ChEMBL 249 3 2 4 2.0 CC(C)(C)NCC(O)C1=COc2ccccc2O1 10.1021/jm00140a015
12606702 11893 0 None - 0 Guinea pig 7.1 pKd = 7.1 Functional
The apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pigThe apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pig
ChEMBL 242 5 2 4 2.1 CC(C)(C)NCC(O)CON=C1CCCCC1 10.1021/jm00180a007
CHEMBL1161383 11893 0 None - 0 Guinea pig 7.1 pKd = 7.1 Functional
The apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pigThe apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pig
ChEMBL 242 5 2 4 2.1 CC(C)(C)NCC(O)CON=C1CCCCC1 10.1021/jm00180a007
CHEMBL1183312 11893 0 None - 0 Guinea pig 7.1 pKd = 7.1 Functional
The apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pigThe apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pig
ChEMBL 242 5 2 4 2.1 CC(C)(C)NCC(O)CON=C1CCCCC1 10.1021/jm00180a007
CHEMBL289868 11893 0 None - 0 Guinea pig 7.1 pKd = 7.1 Functional
The apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pigThe apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pig
ChEMBL 242 5 2 4 2.1 CC(C)(C)NCC(O)CON=C1CCCCC1 10.1021/jm00180a007
12778440 59841 0 None - 0 Guinea pig 7.1 pKd = 7.1 Functional
Beta-2 adrenergic receptor antagonistic activity on guinea pig tracheal chainsBeta-2 adrenergic receptor antagonistic activity on guinea pig tracheal chains
ChEMBL 338 7 2 4 3.6 CCC(C)(C)NCC(O)CON=C1c2ccccc2-c2ccccc21 10.1021/jm00350a009
CHEMBL173976 59841 0 None - 0 Guinea pig 7.1 pKd = 7.1 Functional
Beta-2 adrenergic receptor antagonistic activity on guinea pig tracheal chainsBeta-2 adrenergic receptor antagonistic activity on guinea pig tracheal chains
ChEMBL 338 7 2 4 3.6 CCC(C)(C)NCC(O)CON=C1c2ccccc2-c2ccccc21 10.1021/jm00350a009
56598832 87826 0 None -4365 3 Human 6.1 pKd = 6.1 Functional
Antagonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrsAntagonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrs
ChEMBL 527 16 5 7 3.3 O=C(NCCNCC(O)COc1ccc(OCCOCCc2ccc(F)cc2)cc1)Nc1ccc(O)cc1 10.1021/jm400348g
CHEMBL2348218 87826 0 None -4365 3 Human 6.1 pKd = 6.1 Functional
Antagonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrsAntagonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrs
ChEMBL 527 16 5 7 3.3 O=C(NCCNCC(O)COc1ccc(OCCOCCc2ccc(F)cc2)cc1)Nc1ccc(O)cc1 10.1021/jm400348g
44371389 12094 0 None - 0 Guinea pig 6.1 pKd = 6.1 Functional
The apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pigThe apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pig
ChEMBL 202 7 2 4 1.1 CC/C(C)=N\OCC(O)CNC(C)C 10.1021/jm00180a007
CHEMBL1184362 12094 0 None - 0 Guinea pig 6.1 pKd = 6.1 Functional
The apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pigThe apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pig
ChEMBL 202 7 2 4 1.1 CC/C(C)=N\OCC(O)CNC(C)C 10.1021/jm00180a007
CHEMBL346326 12094 0 None - 0 Guinea pig 6.1 pKd = 6.1 Functional
The apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pigThe apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pig
ChEMBL 202 7 2 4 1.1 CC/C(C)=N\OCC(O)CNC(C)C 10.1021/jm00180a007
12606704 14186 0 None - 0 Guinea pig 8.0 pKd = 8.0 Functional
The apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pigThe apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pig
ChEMBL 290 7 2 4 2.8 CC(/C=C/c1ccccc1)=N\OCC(O)CNC(C)(C)C 10.1021/jm00180a007
CHEMBL1161386 14186 0 None - 0 Guinea pig 8.0 pKd = 8.0 Functional
The apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pigThe apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pig
ChEMBL 290 7 2 4 2.8 CC(/C=C/c1ccccc1)=N\OCC(O)CNC(C)(C)C 10.1021/jm00180a007
CHEMBL1199951 14186 0 None - 0 Guinea pig 8.0 pKd = 8.0 Functional
The apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pigThe apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pig
ChEMBL 290 7 2 4 2.8 CC(/C=C/c1ccccc1)=N\OCC(O)CNC(C)(C)C 10.1021/jm00180a007
157716 40260 40 None - 0 Guinea pig 7.0 pKd = 7.0 Functional
Beta-2 adrenergic receptor antagonistic activity on guinea pig tracheal chainsBeta-2 adrenergic receptor antagonistic activity on guinea pig tracheal chains
ChEMBL 267 9 2 4 1.6 COCCc1ccc(OC[C@@H](O)CNC(C)C)cc1 10.1021/jm00350a009
CHEMBL148306 40260 40 None - 0 Guinea pig 7.0 pKd = 7.0 Functional
Beta-2 adrenergic receptor antagonistic activity on guinea pig tracheal chainsBeta-2 adrenergic receptor antagonistic activity on guinea pig tracheal chains
ChEMBL 267 9 2 4 1.6 COCCc1ccc(OC[C@@H](O)CNC(C)C)cc1 10.1021/jm00350a009
12606687 12100 0 None - 0 Guinea pig 6.0 pKd = 6.0 Functional
The apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pigThe apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pig
ChEMBL 175 6 2 3 0.8 CC(C)NCC(O)COC(C)C 10.1021/jm00180a007
CHEMBL1184385 12100 0 None - 0 Guinea pig 6.0 pKd = 6.0 Functional
The apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pigThe apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pig
ChEMBL 175 6 2 3 0.8 CC(C)NCC(O)COC(C)C 10.1021/jm00180a007
CHEMBL346972 12100 0 None - 0 Guinea pig 6.0 pKd = 6.0 Functional
The apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pigThe apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pig
ChEMBL 175 6 2 3 0.8 CC(C)NCC(O)COC(C)C 10.1021/jm00180a007
36811 1421 34 None -3 7 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 301 7 4 4 3.0 CC(CCc1ccc(cc1)O)NCCc1ccc(c(c1)O)O None
535 1421 34 None -3 7 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 301 7 4 4 3.0 CC(CCc1ccc(cc1)O)NCCc1ccc(c(c1)O)O None
937 1421 34 None -3 7 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 301 7 4 4 3.0 CC(CCc1ccc(cc1)O)NCCc1ccc(c(c1)O)O None
CHEMBL926 1421 34 None -3 7 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 301 7 4 4 3.0 CC(CCc1ccc(cc1)O)NCCc1ccc(c(c1)O)O None
DB00841 1421 34 None -3 7 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 301 7 4 4 3.0 CC(CCc1ccc(cc1)O)NCCc1ccc(c(c1)O)O None
1155 1592 45 None 2 3 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O None
3343 1592 45 None 2 3 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O None
557 1592 45 None 2 3 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O None
CHEMBL32800 1592 45 None 2 3 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O None
DB01288 1592 45 None 2 3 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O None
2419 3394 80 None -22 6 Guinea pig 8.1 pEC50 = 8.1 Functional
Agonist activity at beta2 receptor in guinea pig trachea assessed as slow onset of inhibition of electrically stimulated contractionAgonist activity at beta2 receptor in guinea pig trachea assessed as slow onset of inhibition of electrically stimulated contraction
Drug Central 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O None
5152 3394 80 None -22 6 Guinea pig 8.1 pEC50 = 8.1 Functional
Agonist activity at beta2 receptor in guinea pig trachea assessed as slow onset of inhibition of electrically stimulated contractionAgonist activity at beta2 receptor in guinea pig trachea assessed as slow onset of inhibition of electrically stimulated contraction
Drug Central 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O None
559 3394 80 None -22 6 Guinea pig 8.1 pEC50 = 8.1 Functional
Agonist activity at beta2 receptor in guinea pig trachea assessed as slow onset of inhibition of electrically stimulated contractionAgonist activity at beta2 receptor in guinea pig trachea assessed as slow onset of inhibition of electrically stimulated contraction
Drug Central 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O None
CHEMBL1263 3394 80 None -22 6 Guinea pig 8.1 pEC50 = 8.1 Functional
Agonist activity at beta2 receptor in guinea pig trachea assessed as slow onset of inhibition of electrically stimulated contractionAgonist activity at beta2 receptor in guinea pig trachea assessed as slow onset of inhibition of electrically stimulated contraction
Drug Central 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O None
DB00938 3394 80 None -22 6 Guinea pig 8.1 pEC50 = 8.1 Functional
Agonist activity at beta2 receptor in guinea pig trachea assessed as slow onset of inhibition of electrically stimulated contractionAgonist activity at beta2 receptor in guinea pig trachea assessed as slow onset of inhibition of electrically stimulated contraction
Drug Central 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O None
1499 2052 43 None -165 36 Guinea pig 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
3779 2052 43 None -165 36 Guinea pig 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
536 2052 43 None -165 36 Guinea pig 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
CHEMBL434 2052 43 None -165 36 Guinea pig 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
DB01064 2052 43 None -165 36 Guinea pig 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
65772 215997 0 None -1 3 Guinea pig 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 345 5 3 6 2.6 COC1=CC(C[C@@H]2NCCC3=CC(O)=C(O)C=C23)=CC(OC)=C1OC None
688570 186268 18 None -1 2 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 287 6 4 4 2.4 C[C@@H](NCCc1ccc(O)cc1)[C@@H](O)c1ccc(O)cc1 None
CHEMBL489553 186268 18 None -1 2 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 287 6 4 4 2.4 C[C@@H](NCCc1ccc(O)cc1)[C@@H](O)c1ccc(O)cc1 None
688563 215988 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 290 5 4 4 2.0 CC[C@@H](NC(C)C)[C@@H](O)C1=C2C=CC(=O)NC2=C(O)C=C1 None
3083544 462 46 None -1 4 Guinea pig 8.1 pEC50 = 8.1 Functional
Agonist activity at beta2 receptor in guinea pig trachea assessed as fast onset of inhibition of electrically stimulated contractionAgonist activity at beta2 receptor in guinea pig trachea assessed as fast onset of inhibition of electrically stimulated contraction
Drug Central 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O None
4943 462 46 None -1 4 Guinea pig 8.1 pEC50 = 8.1 Functional
Agonist activity at beta2 receptor in guinea pig trachea assessed as fast onset of inhibition of electrically stimulated contractionAgonist activity at beta2 receptor in guinea pig trachea assessed as fast onset of inhibition of electrically stimulated contraction
Drug Central 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O None
7479 462 46 None -1 4 Guinea pig 8.1 pEC50 = 8.1 Functional
Agonist activity at beta2 receptor in guinea pig trachea assessed as fast onset of inhibition of electrically stimulated contractionAgonist activity at beta2 receptor in guinea pig trachea assessed as fast onset of inhibition of electrically stimulated contraction
Drug Central 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O None
CHEMBL1363 462 46 None -1 4 Guinea pig 8.1 pEC50 = 8.1 Functional
Agonist activity at beta2 receptor in guinea pig trachea assessed as fast onset of inhibition of electrically stimulated contractionAgonist activity at beta2 receptor in guinea pig trachea assessed as fast onset of inhibition of electrically stimulated contraction
Drug Central 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O None
DB01274 462 46 None -1 4 Guinea pig 8.1 pEC50 = 8.1 Functional
Agonist activity at beta2 receptor in guinea pig trachea assessed as fast onset of inhibition of electrically stimulated contractionAgonist activity at beta2 receptor in guinea pig trachea assessed as fast onset of inhibition of electrically stimulated contraction
Drug Central 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O None
10184665 3916 48 None 44 3 Human 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O None
4799 3916 48 None 44 3 Human 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O None
7353 3916 48 None 44 3 Human 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O None
CHEMBL1198857 3916 48 None 44 3 Human 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O None
DB09082 3916 48 None 44 3 Human 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O None
1499 2052 43 None -72 36 Human 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
3779 2052 43 None -72 36 Human 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
536 2052 43 None -72 36 Human 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
CHEMBL434 2052 43 None -72 36 Human 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
DB01064 2052 43 None -72 36 Human 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
3083544 462 46 None -1 4 Guinea pig 8.0 pEC50 = 8 Functional
Agonist activity at guinea pig trachea beta2-adrenergic receptor assessed as relaxation of histamine-induced tracheal ring contractionAgonist activity at guinea pig trachea beta2-adrenergic receptor assessed as relaxation of histamine-induced tracheal ring contraction
Drug Central 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O None
4943 462 46 None -1 4 Guinea pig 8.0 pEC50 = 8 Functional
Agonist activity at guinea pig trachea beta2-adrenergic receptor assessed as relaxation of histamine-induced tracheal ring contractionAgonist activity at guinea pig trachea beta2-adrenergic receptor assessed as relaxation of histamine-induced tracheal ring contraction
Drug Central 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O None
7479 462 46 None -1 4 Guinea pig 8.0 pEC50 = 8 Functional
Agonist activity at guinea pig trachea beta2-adrenergic receptor assessed as relaxation of histamine-induced tracheal ring contractionAgonist activity at guinea pig trachea beta2-adrenergic receptor assessed as relaxation of histamine-induced tracheal ring contraction
Drug Central 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O None
CHEMBL1363 462 46 None -1 4 Guinea pig 8.0 pEC50 = 8 Functional
Agonist activity at guinea pig trachea beta2-adrenergic receptor assessed as relaxation of histamine-induced tracheal ring contractionAgonist activity at guinea pig trachea beta2-adrenergic receptor assessed as relaxation of histamine-induced tracheal ring contraction
Drug Central 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O None
DB01274 462 46 None -1 4 Guinea pig 8.0 pEC50 = 8 Functional
Agonist activity at guinea pig trachea beta2-adrenergic receptor assessed as relaxation of histamine-induced tracheal ring contractionAgonist activity at guinea pig trachea beta2-adrenergic receptor assessed as relaxation of histamine-induced tracheal ring contraction
Drug Central 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O None
12065 621 21 None 6 2 Human 10.0 pEC50 = 10 Functional
Determined in an intracellular cAMP accumulation assay in CHO-K1 cells expressing hβ2-ARDetermined in an intracellular cAMP accumulation assay in CHO-K1 cells expressing hβ2-AR
Guide to Pharmacology 370 6 4 5 2.7 Cc1ccccc1CC(C)(C)NCC(c1c2c(c(cc1)O)NC(=O)CO2)O 19875286
45483813 621 21 None 6 2 Human 10.0 pEC50 = 10 Functional
Determined in an intracellular cAMP accumulation assay in CHO-K1 cells expressing hβ2-ARDetermined in an intracellular cAMP accumulation assay in CHO-K1 cells expressing hβ2-AR
Guide to Pharmacology 370 6 4 5 2.7 Cc1ccccc1CC(C)(C)NCC(c1c2c(c(cc1)O)NC(=O)CO2)O 19875286
CHEMBL579394 621 21 None 6 2 Human 10.0 pEC50 = 10 Functional
Determined in an intracellular cAMP accumulation assay in CHO-K1 cells expressing hβ2-ARDetermined in an intracellular cAMP accumulation assay in CHO-K1 cells expressing hβ2-AR
Guide to Pharmacology 370 6 4 5 2.7 Cc1ccccc1CC(C)(C)NCC(c1c2c(c(cc1)O)NC(=O)CO2)O 19875286
1239 1639 46 None -1 5 Human 10.1 pEC50 = 10.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 20590599
3410 1639 46 None -1 5 Human 10.1 pEC50 = 10.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 20590599
3465 1639 46 None -1 5 Human 10.1 pEC50 = 10.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 20590599
CHEMBL1256786 1639 46 None -1 5 Human 10.1 pEC50 = 10.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 20590599
DB00983 1639 46 None -1 5 Human 10.1 pEC50 = 10.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 20590599
9512 3566 35 None -316 3 Human 5.9 pEC50 = 5.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 410 9 4 4 4.4 Clc1cccc(c1)[C@H](CNCCNc1cccc(c1)c1cccc(c1)C(=O)O)O 16640337
9887812 3566 35 None -316 3 Human 5.9 pEC50 = 5.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 410 9 4 4 4.4 Clc1cccc(c1)[C@H](CNCCNc1cccc(c1)c1cccc(c1)C(=O)O)O 16640337
CHEMBL208427 3566 35 None -316 3 Human 5.9 pEC50 = 5.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 410 9 4 4 4.4 Clc1cccc(c1)[C@H](CNCCNc1cccc(c1)c1cccc(c1)C(=O)O)O 16640337
DB06190 3566 35 None -316 3 Human 5.9 pEC50 = 5.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 410 9 4 4 4.4 Clc1cccc(c1)[C@H](CNCCNc1cccc(c1)c1cccc(c1)C(=O)O)O 16640337
3464 3111 29 None - 1 Human 8.4 pEC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 290 5 4 4 2.0 CCC(C(c1ccc(c2c1ccc(=O)[nH]2)O)O)NC(C)C 20590599
4916 3111 29 None - 1 Human 8.4 pEC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 290 5 4 4 2.0 CCC(C(c1ccc(c2c1ccc(=O)[nH]2)O)O)NC(C)C 20590599
CHEMBL160519 3111 29 None - 1 Human 8.4 pEC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 290 5 4 4 2.0 CCC(C(c1ccc(c2c1ccc(=O)[nH]2)O)O)NC(C)C 20590599
DB01366 3111 29 None - 1 Human 8.4 pEC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 290 5 4 4 2.0 CCC(C(c1ccc(c2c1ccc(=O)[nH]2)O)O)NC(C)C 20590599
10184665 3916 48 None 44 3 Human 9.4 pEC50 = 9.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 20462258
4799 3916 48 None 44 3 Human 9.4 pEC50 = 9.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 20462258
7353 3916 48 None 44 3 Human 9.4 pEC50 = 9.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 20462258
CHEMBL1198857 3916 48 None 44 3 Human 9.4 pEC50 = 9.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 20462258
DB09082 3916 48 None 44 3 Human 9.4 pEC50 = 9.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 20462258
3466 4063 38 None - 1 Human 9.5 pEC50 = 9.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 378 8 4 5 2.4 OC(c1ccc(c(c1)NS(=O)(=O)C)O)CNC(Cc1ccccc1)(C)C 20590599
37990 4063 38 None - 1 Human 9.5 pEC50 = 9.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 378 8 4 5 2.4 OC(c1ccc(c(c1)NS(=O)(=O)C)O)CNC(Cc1ccccc1)(C)C 20590599
CHEMBL1243407 4063 38 None - 1 Human 9.5 pEC50 = 9.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 378 8 4 5 2.4 OC(c1ccc(c(c1)NS(=O)(=O)C)O)CNC(Cc1ccccc1)(C)C 20590599
2419 3394 80 None 17 6 Human 9.9 pEC50 = 9.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 20590599
5152 3394 80 None 17 6 Human 9.9 pEC50 = 9.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 20590599
559 3394 80 None 17 6 Human 9.9 pEC50 = 9.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 20590599
CHEMBL1263 3394 80 None 17 6 Human 9.9 pEC50 = 9.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 20590599
DB00938 3394 80 None 17 6 Human 9.9 pEC50 = 9.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 20590599
4382 2493 0 None -758 3 Human 5.0 pEC50 > 5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 396 9 4 6 2.8 O=C(Cc1csc(n1)N)Nc1ccc(cc1)CCNC[C@@H](c1ccccc1)O 17293563
7445 2493 0 None -758 3 Human 5.0 pEC50 > 5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 396 9 4 6 2.8 O=C(Cc1csc(n1)N)Nc1ccc(cc1)CCNC[C@@H](c1ccccc1)O 17293563
9865528 2493 0 None -758 3 Human 5.0 pEC50 > 5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 396 9 4 6 2.8 O=C(Cc1csc(n1)N)Nc1ccc(cc1)CCNC[C@@H](c1ccccc1)O 17293563
CHEMBL2095212 2493 0 None -758 3 Human 5.0 pEC50 > 5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 396 9 4 6 2.8 O=C(Cc1csc(n1)N)Nc1ccc(cc1)CCNC[C@@H](c1ccccc1)O 17293563
DB08893 2493 0 None -758 3 Human 5.0 pEC50 > 5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 396 9 4 6 2.8 O=C(Cc1csc(n1)N)Nc1ccc(cc1)CCNC[C@@H](c1ccccc1)O 17293563
443372 10123 23 None -3 8 Human 8.0 pIC50 = 8.0 Functional
Mitogenesis inhibition method: To measure beta2-AR mediated inhibition of mitogenesis, HEK-beta2-AR, 1321N1 or U87MG cells were seeded in a 96-well plate at approximately 5,000 cells/well. After 48 hours, the wells were rinsed twice and the medium was replaced with fresh medium containing 10 uL of drug in sterile water. After another 24 hours of incubation at 37° C., 0.25 uCi of [3H]-thymidine was added to each well. The cells were incubated for an additional 2 hours at 37° C., at which point 10 uL of 10x trypsin was added, and the resuspended cells were harvested using a Tomtec 96 harvester through glass fiber filters.Mitogenesis inhibition method: To measure beta2-AR mediated inhibition of mitogenesis, HEK-beta2-AR, 1321N1 or U87MG cells were seeded in a 96-well plate at approximately 5,000 cells/well. After 48 hours, the wells were rinsed twice and the medium was replaced with fresh medium containing 10 uL of drug in sterile water. After another 24 hours of incubation at 37° C., 0.25 uCi of [3H]-thymidine was added to each well. The cells were incubated for an additional 2 hours at 37° C., at which point 10 uL of 10x trypsin was added, and the resuspended cells were harvested using a Tomtec 96 harvester through glass fiber filters.
Drug Central 211 4 4 4 1.1 CC(C)NC[C@H](O)c1ccc(O)c(O)c1 None
CHEMBL1160723 10123 23 None -3 8 Human 8.0 pIC50 = 8.0 Functional
Mitogenesis inhibition method: To measure beta2-AR mediated inhibition of mitogenesis, HEK-beta2-AR, 1321N1 or U87MG cells were seeded in a 96-well plate at approximately 5,000 cells/well. After 48 hours, the wells were rinsed twice and the medium was replaced with fresh medium containing 10 uL of drug in sterile water. After another 24 hours of incubation at 37° C., 0.25 uCi of [3H]-thymidine was added to each well. The cells were incubated for an additional 2 hours at 37° C., at which point 10 uL of 10x trypsin was added, and the resuspended cells were harvested using a Tomtec 96 harvester through glass fiber filters.Mitogenesis inhibition method: To measure beta2-AR mediated inhibition of mitogenesis, HEK-beta2-AR, 1321N1 or U87MG cells were seeded in a 96-well plate at approximately 5,000 cells/well. After 48 hours, the wells were rinsed twice and the medium was replaced with fresh medium containing 10 uL of drug in sterile water. After another 24 hours of incubation at 37° C., 0.25 uCi of [3H]-thymidine was added to each well. The cells were incubated for an additional 2 hours at 37° C., at which point 10 uL of 10x trypsin was added, and the resuspended cells were harvested using a Tomtec 96 harvester through glass fiber filters.
Drug Central 211 4 4 4 1.1 CC(C)NC[C@H](O)c1ccc(O)c(O)c1 None
CHEMBL2062275 10123 23 None -3 8 Human 8.0 pIC50 = 8.0 Functional
Mitogenesis inhibition method: To measure beta2-AR mediated inhibition of mitogenesis, HEK-beta2-AR, 1321N1 or U87MG cells were seeded in a 96-well plate at approximately 5,000 cells/well. After 48 hours, the wells were rinsed twice and the medium was replaced with fresh medium containing 10 uL of drug in sterile water. After another 24 hours of incubation at 37° C., 0.25 uCi of [3H]-thymidine was added to each well. The cells were incubated for an additional 2 hours at 37° C., at which point 10 uL of 10x trypsin was added, and the resuspended cells were harvested using a Tomtec 96 harvester through glass fiber filters.Mitogenesis inhibition method: To measure beta2-AR mediated inhibition of mitogenesis, HEK-beta2-AR, 1321N1 or U87MG cells were seeded in a 96-well plate at approximately 5,000 cells/well. After 48 hours, the wells were rinsed twice and the medium was replaced with fresh medium containing 10 uL of drug in sterile water. After another 24 hours of incubation at 37° C., 0.25 uCi of [3H]-thymidine was added to each well. The cells were incubated for an additional 2 hours at 37° C., at which point 10 uL of 10x trypsin was added, and the resuspended cells were harvested using a Tomtec 96 harvester through glass fiber filters.
Drug Central 211 4 4 4 1.1 CC(C)NC[C@H](O)c1ccc(O)c(O)c1 None
1499 2052 43 None -85 36 Dog 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
3779 2052 43 None -85 36 Dog 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
536 2052 43 None -85 36 Dog 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
CHEMBL434 2052 43 None -85 36 Dog 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
DB01064 2052 43 None -85 36 Dog 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
1155 1592 45 None -2 3 Guinea pig 8.1 pIC50 = 8.1 Functional
In vitro inhibitory concentration Beta-2 adrenergic receptor in Guinea pig tracheaIn vitro inhibitory concentration Beta-2 adrenergic receptor in Guinea pig trachea
Drug Central 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O None
3343 1592 45 None -2 3 Guinea pig 8.1 pIC50 = 8.1 Functional
In vitro inhibitory concentration Beta-2 adrenergic receptor in Guinea pig tracheaIn vitro inhibitory concentration Beta-2 adrenergic receptor in Guinea pig trachea
Drug Central 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O None
557 1592 45 None -2 3 Guinea pig 8.1 pIC50 = 8.1 Functional
In vitro inhibitory concentration Beta-2 adrenergic receptor in Guinea pig tracheaIn vitro inhibitory concentration Beta-2 adrenergic receptor in Guinea pig trachea
Drug Central 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O None
CHEMBL32800 1592 45 None -2 3 Guinea pig 8.1 pIC50 = 8.1 Functional
In vitro inhibitory concentration Beta-2 adrenergic receptor in Guinea pig tracheaIn vitro inhibitory concentration Beta-2 adrenergic receptor in Guinea pig trachea
Drug Central 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O None
DB01288 1592 45 None -2 3 Guinea pig 8.1 pIC50 = 8.1 Functional
In vitro inhibitory concentration Beta-2 adrenergic receptor in Guinea pig tracheaIn vitro inhibitory concentration Beta-2 adrenergic receptor in Guinea pig trachea
Drug Central 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O None
165193 3126 60 None -9 13 Dog 8.1 pIC50 = 8.1 Functional
Tested for Beta-2 adrenergic receptor selectivity in canine lung tissue in anesthetized dogsTested for Beta-2 adrenergic receptor selectivity in canine lung tissue in anesthetized dogs
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
2303 3126 60 None -9 13 Dog 8.1 pIC50 = 8.1 Functional
Tested for Beta-2 adrenergic receptor selectivity in canine lung tissue in anesthetized dogsTested for Beta-2 adrenergic receptor selectivity in canine lung tissue in anesthetized dogs
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
4946 3126 60 None -9 13 Dog 8.1 pIC50 = 8.1 Functional
Tested for Beta-2 adrenergic receptor selectivity in canine lung tissue in anesthetized dogsTested for Beta-2 adrenergic receptor selectivity in canine lung tissue in anesthetized dogs
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
564 3126 60 None -9 13 Dog 8.1 pIC50 = 8.1 Functional
Tested for Beta-2 adrenergic receptor selectivity in canine lung tissue in anesthetized dogsTested for Beta-2 adrenergic receptor selectivity in canine lung tissue in anesthetized dogs
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
62882 3126 60 None -9 13 Dog 8.1 pIC50 = 8.1 Functional
Tested for Beta-2 adrenergic receptor selectivity in canine lung tissue in anesthetized dogsTested for Beta-2 adrenergic receptor selectivity in canine lung tissue in anesthetized dogs
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
63 3126 60 None -9 13 Dog 8.1 pIC50 = 8.1 Functional
Tested for Beta-2 adrenergic receptor selectivity in canine lung tissue in anesthetized dogsTested for Beta-2 adrenergic receptor selectivity in canine lung tissue in anesthetized dogs
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
66366 3126 60 None -9 13 Dog 8.1 pIC50 = 8.1 Functional
Tested for Beta-2 adrenergic receptor selectivity in canine lung tissue in anesthetized dogsTested for Beta-2 adrenergic receptor selectivity in canine lung tissue in anesthetized dogs
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
91536 3126 60 None -9 13 Dog 8.1 pIC50 = 8.1 Functional
Tested for Beta-2 adrenergic receptor selectivity in canine lung tissue in anesthetized dogsTested for Beta-2 adrenergic receptor selectivity in canine lung tissue in anesthetized dogs
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
CHEMBL27 3126 60 None -9 13 Dog 8.1 pIC50 = 8.1 Functional
Tested for Beta-2 adrenergic receptor selectivity in canine lung tissue in anesthetized dogsTested for Beta-2 adrenergic receptor selectivity in canine lung tissue in anesthetized dogs
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
CHEMBL452861 3126 60 None -9 13 Dog 8.1 pIC50 = 8.1 Functional
Tested for Beta-2 adrenergic receptor selectivity in canine lung tissue in anesthetized dogsTested for Beta-2 adrenergic receptor selectivity in canine lung tissue in anesthetized dogs
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
DB00571 3126 60 None -9 13 Dog 8.1 pIC50 = 8.1 Functional
Tested for Beta-2 adrenergic receptor selectivity in canine lung tissue in anesthetized dogsTested for Beta-2 adrenergic receptor selectivity in canine lung tissue in anesthetized dogs
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
4183 1986 62 None -2 4 Guinea pig 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O None
6918554 1986 62 None -2 4 Guinea pig 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O None
7455 1986 62 None -2 4 Guinea pig 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O None
CHEMBL1095777 1986 62 None -2 4 Guinea pig 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O None
DB05039 1986 62 None -2 4 Guinea pig 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O None
11504295 2867 40 None 1047 2 Human 10.0 pIC50 = 10 Functional
UnclassifiedUnclassified
Guide to Pharmacology 386 7 4 6 2.4 COc1ccc(cc1)CC(NC[C@@H](c1cc(O)cc2c1OCC(=O)N2)O)(C)C 20371707
4814 2867 40 None 1047 2 Human 10.0 pIC50 = 10 Functional
UnclassifiedUnclassified
Guide to Pharmacology 386 7 4 6 2.4 COc1ccc(cc1)CC(NC[C@@H](c1cc(O)cc2c1OCC(=O)N2)O)(C)C 20371707
7543 2867 40 None 1047 2 Human 10.0 pIC50 = 10 Functional
UnclassifiedUnclassified
Guide to Pharmacology 386 7 4 6 2.4 COc1ccc(cc1)CC(NC[C@@H](c1cc(O)cc2c1OCC(=O)N2)O)(C)C 20371707
CHEMBL605846 2867 40 None 1047 2 Human 10.0 pIC50 = 10 Functional
UnclassifiedUnclassified
Guide to Pharmacology 386 7 4 6 2.4 COc1ccc(cc1)CC(NC[C@@H](c1cc(O)cc2c1OCC(=O)N2)O)(C)C 20371707
DB09080 2867 40 None 1047 2 Human 10.0 pIC50 = 10 Functional
UnclassifiedUnclassified
Guide to Pharmacology 386 7 4 6 2.4 COc1ccc(cc1)CC(NC[C@@H](c1cc(O)cc2c1OCC(=O)N2)O)(C)C 20371707
12582 935 40 None -23 4 Human 6.2 pIC50 = 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 276 3 3 3 3.0 CC(C)(C)NCC(C1=CC(=C(C(=C1)Cl)N)Cl)O 19245211
12582 935 40 None -23 4 Human 6.2 pIC50 = 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 276 3 3 3 3.0 CC(C)(C)NCC(C1=CC(=C(C(=C1)Cl)N)Cl)O 20590599
12582 935 40 None -23 4 Human 6.2 pIC50 = 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 276 3 3 3 3.0 CC(C)(C)NCC(C1=CC(=C(C(=C1)Cl)N)Cl)O 25324048
2783 935 40 None -23 4 Human 6.2 pIC50 = 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 276 3 3 3 3.0 CC(C)(C)NCC(C1=CC(=C(C(=C1)Cl)N)Cl)O 19245211
2783 935 40 None -23 4 Human 6.2 pIC50 = 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 276 3 3 3 3.0 CC(C)(C)NCC(C1=CC(=C(C(=C1)Cl)N)Cl)O 20590599
2783 935 40 None -23 4 Human 6.2 pIC50 = 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 276 3 3 3 3.0 CC(C)(C)NCC(C1=CC(=C(C(=C1)Cl)N)Cl)O 25324048
CHEMBL49080 935 40 None -23 4 Human 6.2 pIC50 = 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 276 3 3 3 3.0 CC(C)(C)NCC(C1=CC(=C(C(=C1)Cl)N)Cl)O 19245211
CHEMBL49080 935 40 None -23 4 Human 6.2 pIC50 = 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 276 3 3 3 3.0 CC(C)(C)NCC(C1=CC(=C(C(=C1)Cl)N)Cl)O 20590599
CHEMBL49080 935 40 None -23 4 Human 6.2 pIC50 = 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 276 3 3 3 3.0 CC(C)(C)NCC(C1=CC(=C(C(=C1)Cl)N)Cl)O 25324048
DB01407 935 40 None -23 4 Human 6.2 pIC50 = 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 276 3 3 3 3.0 CC(C)(C)NCC(C1=CC(=C(C(=C1)Cl)N)Cl)O 19245211
DB01407 935 40 None -23 4 Human 6.2 pIC50 = 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 276 3 3 3 3.0 CC(C)(C)NCC(C1=CC(=C(C(=C1)Cl)N)Cl)O 20590599
DB01407 935 40 None -23 4 Human 6.2 pIC50 = 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 276 3 3 3 3.0 CC(C)(C)NCC(C1=CC(=C(C(=C1)Cl)N)Cl)O 25324048
134495 736 18 None - 1 Rat 6.5 pKB = 6.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 267 5 2 4 2.5 COc1ccc(cc1C(C(NC(C)(C)C)C)O)OC 15908513
18026 736 18 None - 1 Rat 6.5 pKB = 6.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 267 5 2 4 2.5 COc1ccc(cc1C(C(NC(C)(C)C)C)O)OC 15908513
9809 736 18 None - 1 Rat 6.5 pKB = 6.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 267 5 2 4 2.5 COc1ccc(cc1C(C(NC(C)(C)C)C)O)OC 15908513
CHEMBL289093 736 18 None - 1 Rat 6.5 pKB = 6.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 267 5 2 4 2.5 COc1ccc(cc1C(C(NC(C)(C)C)C)O)OC 15908513




Ligands Receptor Assay information Chemical information
Sel. page Common
name
GPCRdb ID #Vendors Reference
ligand
Fold selectivity
(Affinity)
# tested GPCRs
(Affinity)
Species p-value
(-log)
Type Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI
9892481 69875 11 None - 2 Guinea pig 10.3 pEC50 = 10.3 Binding
Agonist activity at beta2 receptor in guinea pig trachea assessed as fast onset of inhibition of electrically stimulated contractionAgonist activity at beta2 receptor in guinea pig trachea assessed as fast onset of inhibition of electrically stimulated contraction
ChEMBL 435 12 6 6 3.0 O=CNc1cc([C@@H](O)CNCCc2ccc(NC[C@H](O)c3ccccc3)cc2)ccc1O 10.1016/j.bmcl.2014.04.069
CHEMBL1940832 69875 11 None - 2 Guinea pig 10.3 pEC50 = 10.3 Binding
Agonist activity at beta2 receptor in guinea pig trachea assessed as fast onset of inhibition of electrically stimulated contractionAgonist activity at beta2 receptor in guinea pig trachea assessed as fast onset of inhibition of electrically stimulated contraction
ChEMBL 435 12 6 6 3.0 O=CNc1cc([C@@H](O)CNCCc2ccc(NC[C@H](O)c3ccccc3)cc2)ccc1O 10.1016/j.bmcl.2014.04.069
2419 3394 80 None 16 6 Human 10.1 pEC50 = 10.1 Binding
Agonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GSK5 and coelenterazine 400a by BRET assayAgonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GSK5 and coelenterazine 400a by BRET assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/acs.jmedchem.9b00349
5152 3394 80 None 16 6 Human 10.1 pEC50 = 10.1 Binding
Agonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GSK5 and coelenterazine 400a by BRET assayAgonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GSK5 and coelenterazine 400a by BRET assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/acs.jmedchem.9b00349
559 3394 80 None 16 6 Human 10.1 pEC50 = 10.1 Binding
Agonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GSK5 and coelenterazine 400a by BRET assayAgonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GSK5 and coelenterazine 400a by BRET assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/acs.jmedchem.9b00349
CHEMBL1263 3394 80 None 16 6 Human 10.1 pEC50 = 10.1 Binding
Agonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GSK5 and coelenterazine 400a by BRET assayAgonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GSK5 and coelenterazine 400a by BRET assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/acs.jmedchem.9b00349
DB00938 3394 80 None 16 6 Human 10.1 pEC50 = 10.1 Binding
Agonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GSK5 and coelenterazine 400a by BRET assayAgonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GSK5 and coelenterazine 400a by BRET assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/acs.jmedchem.9b00349
2419 3394 80 None 16 6 Human 9.9 pEC50 = 9.9 Binding
Agonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GSK2 and coelenterazine 400a by BRET assayAgonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GSK2 and coelenterazine 400a by BRET assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/acs.jmedchem.9b00349
5152 3394 80 None 16 6 Human 9.9 pEC50 = 9.9 Binding
Agonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GSK2 and coelenterazine 400a by BRET assayAgonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GSK2 and coelenterazine 400a by BRET assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/acs.jmedchem.9b00349
559 3394 80 None 16 6 Human 9.9 pEC50 = 9.9 Binding
Agonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GSK2 and coelenterazine 400a by BRET assayAgonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GSK2 and coelenterazine 400a by BRET assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/acs.jmedchem.9b00349
CHEMBL1263 3394 80 None 16 6 Human 9.9 pEC50 = 9.9 Binding
Agonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GSK2 and coelenterazine 400a by BRET assayAgonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GSK2 and coelenterazine 400a by BRET assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/acs.jmedchem.9b00349
DB00938 3394 80 None 16 6 Human 9.9 pEC50 = 9.9 Binding
Agonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GSK2 and coelenterazine 400a by BRET assayAgonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GSK2 and coelenterazine 400a by BRET assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/acs.jmedchem.9b00349
3083544 462 46 None - 5 Guinea pig 9.9 pEC50 = 9.9 Binding
Agonist activity at guinea pig trachea beta2-adrenergic receptor assessed as relaxation of histamine-induced tracheal ring contractionAgonist activity at guinea pig trachea beta2-adrenergic receptor assessed as relaxation of histamine-induced tracheal ring contraction
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2013.11.028
4943 462 46 None - 5 Guinea pig 9.9 pEC50 = 9.9 Binding
Agonist activity at guinea pig trachea beta2-adrenergic receptor assessed as relaxation of histamine-induced tracheal ring contractionAgonist activity at guinea pig trachea beta2-adrenergic receptor assessed as relaxation of histamine-induced tracheal ring contraction
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2013.11.028
7479 462 46 None - 5 Guinea pig 9.9 pEC50 = 9.9 Binding
Agonist activity at guinea pig trachea beta2-adrenergic receptor assessed as relaxation of histamine-induced tracheal ring contractionAgonist activity at guinea pig trachea beta2-adrenergic receptor assessed as relaxation of histamine-induced tracheal ring contraction
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2013.11.028
CHEMBL1363 462 46 None - 5 Guinea pig 9.9 pEC50 = 9.9 Binding
Agonist activity at guinea pig trachea beta2-adrenergic receptor assessed as relaxation of histamine-induced tracheal ring contractionAgonist activity at guinea pig trachea beta2-adrenergic receptor assessed as relaxation of histamine-induced tracheal ring contraction
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2013.11.028
DB01274 462 46 None - 5 Guinea pig 9.9 pEC50 = 9.9 Binding
Agonist activity at guinea pig trachea beta2-adrenergic receptor assessed as relaxation of histamine-induced tracheal ring contractionAgonist activity at guinea pig trachea beta2-adrenergic receptor assessed as relaxation of histamine-induced tracheal ring contraction
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2013.11.028
3083544 462 46 None - 5 Guinea pig 9.9 pEC50 = 9.9 Binding
Agonist activity at guinea pig trachea beta2-adrenergic receptor assessed as relaxation of histamine-induced tracheal ring contractionAgonist activity at guinea pig trachea beta2-adrenergic receptor assessed as relaxation of histamine-induced tracheal ring contraction
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2013.11.028
4943 462 46 None - 5 Guinea pig 9.9 pEC50 = 9.9 Binding
Agonist activity at guinea pig trachea beta2-adrenergic receptor assessed as relaxation of histamine-induced tracheal ring contractionAgonist activity at guinea pig trachea beta2-adrenergic receptor assessed as relaxation of histamine-induced tracheal ring contraction
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2013.11.028
7479 462 46 None - 5 Guinea pig 9.9 pEC50 = 9.9 Binding
Agonist activity at guinea pig trachea beta2-adrenergic receptor assessed as relaxation of histamine-induced tracheal ring contractionAgonist activity at guinea pig trachea beta2-adrenergic receptor assessed as relaxation of histamine-induced tracheal ring contraction
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2013.11.028
CHEMBL1363 462 46 None - 5 Guinea pig 9.9 pEC50 = 9.9 Binding
Agonist activity at guinea pig trachea beta2-adrenergic receptor assessed as relaxation of histamine-induced tracheal ring contractionAgonist activity at guinea pig trachea beta2-adrenergic receptor assessed as relaxation of histamine-induced tracheal ring contraction
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2013.11.028
DB01274 462 46 None - 5 Guinea pig 9.9 pEC50 = 9.9 Binding
Agonist activity at guinea pig trachea beta2-adrenergic receptor assessed as relaxation of histamine-induced tracheal ring contractionAgonist activity at guinea pig trachea beta2-adrenergic receptor assessed as relaxation of histamine-induced tracheal ring contraction
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2013.11.028
10372836 101912 34 None - 1 Human 9.6 pEC50 = 9.6 Binding
Agonist activity at human beta2 adrenoceptorAgonist activity at human beta2 adrenoceptor
ChEMBL 739 13 6 9 6.4 COc1cc(NC(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/acs.jmedchem.8b01520
CHEMBL3039518 101912 34 None - 1 Human 9.6 pEC50 = 9.6 Binding
Agonist activity at human beta2 adrenoceptorAgonist activity at human beta2 adrenoceptor
ChEMBL 739 13 6 9 6.4 COc1cc(NC(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/acs.jmedchem.8b01520
54591014 145225 3 None - 0 Human 9.6 pEC50 = 9.6 Binding
Agonist activity at human beta2 adrenoceptorAgonist activity at human beta2 adrenoceptor
ChEMBL 810 15 6 13 6.1 COc1cc(NC(=O)OCCN(C)[C@H]2CC[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/acs.jmedchem.8b01520
CHEMBL3916700 145225 3 None - 0 Human 9.6 pEC50 = 9.6 Binding
Agonist activity at human beta2 adrenoceptorAgonist activity at human beta2 adrenoceptor
ChEMBL 810 15 6 13 6.1 COc1cc(NC(=O)OCCN(C)[C@H]2CC[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/acs.jmedchem.8b01520
71558565 166872 5 None - 0 Human 9.6 pEC50 = 9.6 Binding
Agonist activity at human beta2 adrenoceptorAgonist activity at human beta2 adrenoceptor
ChEMBL 742 14 5 13 5.0 CN(CCCn1nnc2cc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)ccc21)[C@H]1CC[C@H](OC(=O)C(O)(c2cccs2)c2cccs2)CC1 10.1021/acs.jmedchem.8b01520
CHEMBL4297483 166872 5 None - 0 Human 9.6 pEC50 = 9.6 Binding
Agonist activity at human beta2 adrenoceptorAgonist activity at human beta2 adrenoceptor
ChEMBL 742 14 5 13 5.0 CN(CCCn1nnc2cc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)ccc21)[C@H]1CC[C@H](OC(=O)C(O)(c2cccs2)c2cccs2)CC1 10.1021/acs.jmedchem.8b01520
155531077 171044 2 None - 0 Human 9.6 pEC50 = 9.6 Binding
Agonist activity at human beta2 adrenoceptorAgonist activity at human beta2 adrenoceptor
ChEMBL 669 10 4 10 4.4 CC(C)c1ncc(C(=O)N2CCOC3(CCN(Cc4ccc(F)c(CCNC[C@H](O)c5ccc(O)c6[nH]c(=O)sc56)c4)CC3)C2)s1 10.1021/acs.jmedchem.8b01520
CHEMBL4465556 171044 2 None - 0 Human 9.6 pEC50 = 9.6 Binding
Agonist activity at human beta2 adrenoceptorAgonist activity at human beta2 adrenoceptor
ChEMBL 669 10 4 10 4.4 CC(C)c1ncc(C(=O)N2CCOC3(CCN(Cc4ccc(F)c(CCNC[C@H](O)c5ccc(O)c6[nH]c(=O)sc56)c4)CC3)C2)s1 10.1021/acs.jmedchem.8b01520
11962616 219 7 None - 0 Human 9.2 pEC50 = 9.2 Binding
Inhibition of 3H]CGP12177 binding to human beta2 adrenoceptor expressed in sf9 cell membranes incubated for 60 mins by scintillation counting methodInhibition of 3H]CGP12177 binding to human beta2 adrenoceptor expressed in sf9 cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 460 13 4 5 4.2 O=c1ccc2c([nH]1)c(O)ccc2[C@H](CNCCCCCCOCC(c1ccccc1)(F)F)O 10.1021/acs.jmedchem.0c01195
9326 219 7 None - 0 Human 9.2 pEC50 = 9.2 Binding
Inhibition of 3H]CGP12177 binding to human beta2 adrenoceptor expressed in sf9 cell membranes incubated for 60 mins by scintillation counting methodInhibition of 3H]CGP12177 binding to human beta2 adrenoceptor expressed in sf9 cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 460 13 4 5 4.2 O=c1ccc2c([nH]1)c(O)ccc2[C@H](CNCCCCCCOCC(c1ccccc1)(F)F)O 10.1021/acs.jmedchem.0c01195
CHEMBL3039530 219 7 None - 0 Human 9.2 pEC50 = 9.2 Binding
Inhibition of 3H]CGP12177 binding to human beta2 adrenoceptor expressed in sf9 cell membranes incubated for 60 mins by scintillation counting methodInhibition of 3H]CGP12177 binding to human beta2 adrenoceptor expressed in sf9 cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 460 13 4 5 4.2 O=c1ccc2c([nH]1)c(O)ccc2[C@H](CNCCCCCCOCC(c1ccccc1)(F)F)O 10.1021/acs.jmedchem.0c01195
DB12100 219 7 None - 0 Human 9.2 pEC50 = 9.2 Binding
Inhibition of 3H]CGP12177 binding to human beta2 adrenoceptor expressed in sf9 cell membranes incubated for 60 mins by scintillation counting methodInhibition of 3H]CGP12177 binding to human beta2 adrenoceptor expressed in sf9 cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 460 13 4 5 4.2 O=c1ccc2c([nH]1)c(O)ccc2[C@H](CNCCCCCCOCC(c1ccccc1)(F)F)O 10.1021/acs.jmedchem.0c01195
22337156 87114 0 None - 0 Guinea pig 9.2 pEC50 = 9.2 Binding
Agonist activity at beta2-adrenoceptor in guinea pig trachea assessed as relaxation of histamine-induced precontracted tracheal ringsAgonist activity at beta2-adrenoceptor in guinea pig trachea assessed as relaxation of histamine-induced precontracted tracheal rings
ChEMBL 553 14 4 8 4.1 COc1ccc(C2=NN(CCCCCCNCC(O)c3ccc(O)c(CO)c3)C(=O)C3CCCCC23)cc1OC 10.1016/j.bmcl.2012.11.058
CHEMBL2335415 87114 0 None - 0 Guinea pig 9.2 pEC50 = 9.2 Binding
Agonist activity at beta2-adrenoceptor in guinea pig trachea assessed as relaxation of histamine-induced precontracted tracheal ringsAgonist activity at beta2-adrenoceptor in guinea pig trachea assessed as relaxation of histamine-induced precontracted tracheal rings
ChEMBL 553 14 4 8 4.1 COc1ccc(C2=NN(CCCCCCNCC(O)c3ccc(O)c(CO)c3)C(=O)C3CCCCC23)cc1OC 10.1016/j.bmcl.2012.11.058
71562381 87111 0 None - 0 Guinea pig 9.2 pEC50 = 9.2 Binding
Agonist activity at beta2-adrenoceptor in guinea pig trachea assessed as relaxation of histamine-induced precontracted tracheal ringsAgonist activity at beta2-adrenoceptor in guinea pig trachea assessed as relaxation of histamine-induced precontracted tracheal rings
ChEMBL 497 10 4 8 2.6 COc1ccc(C2=NN(CCNCC(O)c3ccc(O)c(CO)c3)C(=O)C3CCCCC23)cc1OC 10.1016/j.bmcl.2012.11.058
CHEMBL2335412 87111 0 None - 0 Guinea pig 9.2 pEC50 = 9.2 Binding
Agonist activity at beta2-adrenoceptor in guinea pig trachea assessed as relaxation of histamine-induced precontracted tracheal ringsAgonist activity at beta2-adrenoceptor in guinea pig trachea assessed as relaxation of histamine-induced precontracted tracheal rings
ChEMBL 497 10 4 8 2.6 COc1ccc(C2=NN(CCNCC(O)c3ccc(O)c(CO)c3)C(=O)C3CCCCC23)cc1OC 10.1016/j.bmcl.2012.11.058
71562382 87112 0 None - 0 Guinea pig 9.2 pEC50 = 9.2 Binding
Agonist activity at beta2-adrenoceptor in guinea pig trachea assessed as relaxation of histamine-induced precontracted tracheal ringsAgonist activity at beta2-adrenoceptor in guinea pig trachea assessed as relaxation of histamine-induced precontracted tracheal rings
ChEMBL 525 12 4 8 3.4 COc1ccc(C2=NN(CCCCNCC(O)c3ccc(O)c(CO)c3)C(=O)C3CCCCC23)cc1OC 10.1016/j.bmcl.2012.11.058
CHEMBL2335413 87112 0 None - 0 Guinea pig 9.2 pEC50 = 9.2 Binding
Agonist activity at beta2-adrenoceptor in guinea pig trachea assessed as relaxation of histamine-induced precontracted tracheal ringsAgonist activity at beta2-adrenoceptor in guinea pig trachea assessed as relaxation of histamine-induced precontracted tracheal rings
ChEMBL 525 12 4 8 3.4 COc1ccc(C2=NN(CCCCNCC(O)c3ccc(O)c(CO)c3)C(=O)C3CCCCC23)cc1OC 10.1016/j.bmcl.2012.11.058
2419 3394 80 None 16 6 Human 9.1 pEC50 = 9.1 Binding
Agonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring Rluc2-117-GalphaS/GFP10-Ggamma/Gbeta1 assessed as activation of GalphaS incubated for 5 mins in presence of coelenterazine 400a by BRET assayAgonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring Rluc2-117-GalphaS/GFP10-Ggamma/Gbeta1 assessed as activation of GalphaS incubated for 5 mins in presence of coelenterazine 400a by BRET assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/acs.jmedchem.9b00349
5152 3394 80 None 16 6 Human 9.1 pEC50 = 9.1 Binding
Agonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring Rluc2-117-GalphaS/GFP10-Ggamma/Gbeta1 assessed as activation of GalphaS incubated for 5 mins in presence of coelenterazine 400a by BRET assayAgonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring Rluc2-117-GalphaS/GFP10-Ggamma/Gbeta1 assessed as activation of GalphaS incubated for 5 mins in presence of coelenterazine 400a by BRET assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/acs.jmedchem.9b00349
559 3394 80 None 16 6 Human 9.1 pEC50 = 9.1 Binding
Agonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring Rluc2-117-GalphaS/GFP10-Ggamma/Gbeta1 assessed as activation of GalphaS incubated for 5 mins in presence of coelenterazine 400a by BRET assayAgonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring Rluc2-117-GalphaS/GFP10-Ggamma/Gbeta1 assessed as activation of GalphaS incubated for 5 mins in presence of coelenterazine 400a by BRET assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/acs.jmedchem.9b00349
CHEMBL1263 3394 80 None 16 6 Human 9.1 pEC50 = 9.1 Binding
Agonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring Rluc2-117-GalphaS/GFP10-Ggamma/Gbeta1 assessed as activation of GalphaS incubated for 5 mins in presence of coelenterazine 400a by BRET assayAgonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring Rluc2-117-GalphaS/GFP10-Ggamma/Gbeta1 assessed as activation of GalphaS incubated for 5 mins in presence of coelenterazine 400a by BRET assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/acs.jmedchem.9b00349
DB00938 3394 80 None 16 6 Human 9.1 pEC50 = 9.1 Binding
Agonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring Rluc2-117-GalphaS/GFP10-Ggamma/Gbeta1 assessed as activation of GalphaS incubated for 5 mins in presence of coelenterazine 400a by BRET assayAgonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring Rluc2-117-GalphaS/GFP10-Ggamma/Gbeta1 assessed as activation of GalphaS incubated for 5 mins in presence of coelenterazine 400a by BRET assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/acs.jmedchem.9b00349
71562383 87113 0 None - 0 Guinea pig 9.1 pEC50 = 9.1 Binding
Agonist activity at beta2-adrenoceptor in guinea pig trachea assessed as relaxation of histamine-induced precontracted tracheal ringsAgonist activity at beta2-adrenoceptor in guinea pig trachea assessed as relaxation of histamine-induced precontracted tracheal rings
ChEMBL 539 13 4 8 3.7 COc1ccc(C2=NN(CCCCCNCC(O)c3ccc(O)c(CO)c3)C(=O)C3CCCCC23)cc1OC 10.1016/j.bmcl.2012.11.058
CHEMBL2335414 87113 0 None - 0 Guinea pig 9.1 pEC50 = 9.1 Binding
Agonist activity at beta2-adrenoceptor in guinea pig trachea assessed as relaxation of histamine-induced precontracted tracheal ringsAgonist activity at beta2-adrenoceptor in guinea pig trachea assessed as relaxation of histamine-induced precontracted tracheal rings
ChEMBL 539 13 4 8 3.7 COc1ccc(C2=NN(CCCCCNCC(O)c3ccc(O)c(CO)c3)C(=O)C3CCCCC23)cc1OC 10.1016/j.bmcl.2012.11.058
72948092 103780 0 None - 0 Guinea pig 9.0 pEC50 = 9 Binding
Agonist activity at guinea pig trachea beta2-adrenergic receptor assessed as relaxation of histamine-induced tracheal ring contractionAgonist activity at guinea pig trachea beta2-adrenergic receptor assessed as relaxation of histamine-induced tracheal ring contraction
ChEMBL 700 19 4 9 6.2 COc1ccc(C2=NN(CCCCCCOc3ccc(C[C@@H](C)NC[C@H](O)c4ccc(O)c(NC=O)c4)cc3)C(=O)C3CCCCC23)cc1OC 10.1016/j.bmcl.2013.11.028
CHEMBL3099249 103780 0 None - 0 Guinea pig 9.0 pEC50 = 9 Binding
Agonist activity at guinea pig trachea beta2-adrenergic receptor assessed as relaxation of histamine-induced tracheal ring contractionAgonist activity at guinea pig trachea beta2-adrenergic receptor assessed as relaxation of histamine-induced tracheal ring contraction
ChEMBL 700 19 4 9 6.2 COc1ccc(C2=NN(CCCCCCOc3ccc(C[C@@H](C)NC[C@H](O)c4ccc(O)c(NC=O)c4)cc3)C(=O)C3CCCCC23)cc1OC 10.1016/j.bmcl.2013.11.028
72948092 103780 0 None - 0 Guinea pig 9.0 pEC50 = 9.0 Binding
Agonist activity at guinea pig trachea beta2-adrenergic receptor assessed as relaxation of histamine-induced tracheal ring contractionAgonist activity at guinea pig trachea beta2-adrenergic receptor assessed as relaxation of histamine-induced tracheal ring contraction
ChEMBL 700 19 4 9 6.2 COc1ccc(C2=NN(CCCCCCOc3ccc(C[C@@H](C)NC[C@H](O)c4ccc(O)c(NC=O)c4)cc3)C(=O)C3CCCCC23)cc1OC 10.1016/j.bmcl.2013.11.028
CHEMBL3099249 103780 0 None - 0 Guinea pig 9.0 pEC50 = 9.0 Binding
Agonist activity at guinea pig trachea beta2-adrenergic receptor assessed as relaxation of histamine-induced tracheal ring contractionAgonist activity at guinea pig trachea beta2-adrenergic receptor assessed as relaxation of histamine-induced tracheal ring contraction
ChEMBL 700 19 4 9 6.2 COc1ccc(C2=NN(CCCCCCOc3ccc(C[C@@H](C)NC[C@H](O)c4ccc(O)c(NC=O)c4)cc3)C(=O)C3CCCCC23)cc1OC 10.1016/j.bmcl.2013.11.028
1239 1639 46 None - 4 Guinea pig 8.8 pEC50 = 8.8 Binding
Agonist activity at beta2 receptor in guinea pig trachea assessed as fast onset of inhibition of electrically stimulated contractionAgonist activity at beta2 receptor in guinea pig trachea assessed as fast onset of inhibition of electrically stimulated contraction
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.04.069
3410 1639 46 None - 4 Guinea pig 8.8 pEC50 = 8.8 Binding
Agonist activity at beta2 receptor in guinea pig trachea assessed as fast onset of inhibition of electrically stimulated contractionAgonist activity at beta2 receptor in guinea pig trachea assessed as fast onset of inhibition of electrically stimulated contraction
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.04.069
3465 1639 46 None - 4 Guinea pig 8.8 pEC50 = 8.8 Binding
Agonist activity at beta2 receptor in guinea pig trachea assessed as fast onset of inhibition of electrically stimulated contractionAgonist activity at beta2 receptor in guinea pig trachea assessed as fast onset of inhibition of electrically stimulated contraction
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.04.069
CHEMBL1256786 1639 46 None - 4 Guinea pig 8.8 pEC50 = 8.8 Binding
Agonist activity at beta2 receptor in guinea pig trachea assessed as fast onset of inhibition of electrically stimulated contractionAgonist activity at beta2 receptor in guinea pig trachea assessed as fast onset of inhibition of electrically stimulated contraction
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.04.069
DB00983 1639 46 None - 4 Guinea pig 8.8 pEC50 = 8.8 Binding
Agonist activity at beta2 receptor in guinea pig trachea assessed as fast onset of inhibition of electrically stimulated contractionAgonist activity at beta2 receptor in guinea pig trachea assessed as fast onset of inhibition of electrically stimulated contraction
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.04.069
71562034 87109 0 None - 0 Guinea pig 8.7 pEC50 = 8.7 Binding
Agonist activity at beta2-adrenoceptor in guinea pig trachea assessed as relaxation of histamine-induced precontracted tracheal ringsAgonist activity at beta2-adrenoceptor in guinea pig trachea assessed as relaxation of histamine-induced precontracted tracheal rings
ChEMBL 563 14 5 8 4.7 COc1ccc(C(=O)Nc2c(Cl)cncc2Cl)cc1OCCCCCNCC(O)c1ccc(O)c(CO)c1 10.1016/j.bmcl.2012.11.058
CHEMBL2335410 87109 0 None - 0 Guinea pig 8.7 pEC50 = 8.7 Binding
Agonist activity at beta2-adrenoceptor in guinea pig trachea assessed as relaxation of histamine-induced precontracted tracheal ringsAgonist activity at beta2-adrenoceptor in guinea pig trachea assessed as relaxation of histamine-induced precontracted tracheal rings
ChEMBL 563 14 5 8 4.7 COc1ccc(C(=O)Nc2c(Cl)cncc2Cl)cc1OCCCCCNCC(O)c1ccc(O)c(CO)c1 10.1016/j.bmcl.2012.11.058
10128077 111764 0 None - 0 Guinea pig 8.7 pEC50 = 8.7 Binding
Agonist activity at beta2 receptor in guinea pig trachea assessed as slow onset of inhibition of electrically stimulated contractionAgonist activity at beta2 receptor in guinea pig trachea assessed as slow onset of inhibition of electrically stimulated contraction
ChEMBL 484 11 5 6 5.2 COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c(CO)c3)cc2)cc1-c1ccccc1 10.1016/j.bmcl.2014.04.069
CHEMBL3290997 111764 0 None - 0 Guinea pig 8.7 pEC50 = 8.7 Binding
Agonist activity at beta2 receptor in guinea pig trachea assessed as slow onset of inhibition of electrically stimulated contractionAgonist activity at beta2 receptor in guinea pig trachea assessed as slow onset of inhibition of electrically stimulated contraction
ChEMBL 484 11 5 6 5.2 COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c(CO)c3)cc2)cc1-c1ccccc1 10.1016/j.bmcl.2014.04.069
9871386 111766 4 None - 1 Guinea pig 8.7 pEC50 = 8.7 Binding
Agonist activity at beta2 receptor in guinea pig trachea assessed as slow onset of inhibition of electrically stimulated contractionAgonist activity at beta2 receptor in guinea pig trachea assessed as slow onset of inhibition of electrically stimulated contraction
ChEMBL 521 10 5 6 5.5 COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1-c1ccccc1 10.1016/j.bmcl.2014.04.069
CHEMBL3290999 111766 4 None - 1 Guinea pig 8.7 pEC50 = 8.7 Binding
Agonist activity at beta2 receptor in guinea pig trachea assessed as slow onset of inhibition of electrically stimulated contractionAgonist activity at beta2 receptor in guinea pig trachea assessed as slow onset of inhibition of electrically stimulated contraction
ChEMBL 521 10 5 6 5.5 COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1-c1ccccc1 10.1016/j.bmcl.2014.04.069
72947900 103781 0 None - 0 Guinea pig 8.0 pEC50 = 8 Binding
Agonist activity at guinea pig trachea beta2-adrenergic receptor assessed as relaxation of histamine-induced tracheal ring contractionAgonist activity at guinea pig trachea beta2-adrenergic receptor assessed as relaxation of histamine-induced tracheal ring contraction
ChEMBL 672 17 4 9 5.4 COc1ccc(C2=NN(CCCCOc3ccc(CC(C)NCC(O)c4ccc(O)c(NC=O)c4)cc3)C(=O)C3CCCCC23)cc1OC 10.1016/j.bmcl.2013.11.028
CHEMBL3099250 103781 0 None - 0 Guinea pig 8.0 pEC50 = 8 Binding
Agonist activity at guinea pig trachea beta2-adrenergic receptor assessed as relaxation of histamine-induced tracheal ring contractionAgonist activity at guinea pig trachea beta2-adrenergic receptor assessed as relaxation of histamine-induced tracheal ring contraction
ChEMBL 672 17 4 9 5.4 COc1ccc(C2=NN(CCCCOc3ccc(CC(C)NCC(O)c4ccc(O)c(NC=O)c4)cc3)C(=O)C3CCCCC23)cc1OC 10.1016/j.bmcl.2013.11.028
72947900 103781 0 None - 0 Guinea pig 8.0 pEC50 = 8.0 Binding
Agonist activity at guinea pig trachea beta2-adrenergic receptor assessed as relaxation of histamine-induced tracheal ring contractionAgonist activity at guinea pig trachea beta2-adrenergic receptor assessed as relaxation of histamine-induced tracheal ring contraction
ChEMBL 672 17 4 9 5.4 COc1ccc(C2=NN(CCCCOc3ccc(CC(C)NCC(O)c4ccc(O)c(NC=O)c4)cc3)C(=O)C3CCCCC23)cc1OC 10.1016/j.bmcl.2013.11.028
CHEMBL3099250 103781 0 None - 0 Guinea pig 8.0 pEC50 = 8.0 Binding
Agonist activity at guinea pig trachea beta2-adrenergic receptor assessed as relaxation of histamine-induced tracheal ring contractionAgonist activity at guinea pig trachea beta2-adrenergic receptor assessed as relaxation of histamine-induced tracheal ring contraction
ChEMBL 672 17 4 9 5.4 COc1ccc(C2=NN(CCCCOc3ccc(CC(C)NCC(O)c4ccc(O)c(NC=O)c4)cc3)C(=O)C3CCCCC23)cc1OC 10.1016/j.bmcl.2013.11.028
127045855 139121 0 None 1 6 Human 7.0 pEC50 = 7 Binding
Agonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GSK5 and coelenterazine 400a by BRET assayAgonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GSK5 and coelenterazine 400a by BRET assay
ChEMBL 319 8 4 6 1.8 COc1ccccc1OCCNC[C@H](O)c1ccc(O)c(O)c1 10.1021/acs.jmedchem.9b00349
CHEMBL3797876 139121 0 None 1 6 Human 7.0 pEC50 = 7 Binding
Agonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GSK5 and coelenterazine 400a by BRET assayAgonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GSK5 and coelenterazine 400a by BRET assay
ChEMBL 319 8 4 6 1.8 COc1ccccc1OCCNC[C@H](O)c1ccc(O)c(O)c1 10.1021/acs.jmedchem.9b00349
127046950 139502 0 None 3 6 Human 7.0 pEC50 = 7 Binding
Agonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring Rluc2-117-GalphaS/GFP10-Ggamma/Gbeta1 assessed as activation of GalphaS incubated for 5 mins in presence of coelenterazine 400a by BRET assayAgonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring Rluc2-117-GalphaS/GFP10-Ggamma/Gbeta1 assessed as activation of GalphaS incubated for 5 mins in presence of coelenterazine 400a by BRET assay
ChEMBL 437 12 4 6 4.0 COc1cc(CCNC[C@H](O)c2ccc(O)c(O)c2)ccc1OCCCc1ccccc1 10.1021/acs.jmedchem.9b00349
CHEMBL3800303 139502 0 None 3 6 Human 7.0 pEC50 = 7 Binding
Agonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring Rluc2-117-GalphaS/GFP10-Ggamma/Gbeta1 assessed as activation of GalphaS incubated for 5 mins in presence of coelenterazine 400a by BRET assayAgonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring Rluc2-117-GalphaS/GFP10-Ggamma/Gbeta1 assessed as activation of GalphaS incubated for 5 mins in presence of coelenterazine 400a by BRET assay
ChEMBL 437 12 4 6 4.0 COc1cc(CCNC[C@H](O)c2ccc(O)c(O)c2)ccc1OCCCc1ccccc1 10.1021/acs.jmedchem.9b00349
15133334 118067 0 None - 0 Guinea pig 5.9 pEC50 = 5.9 Binding
Inhibitory activity against Beta-2 adrenergic receptor in guinea pig trachea after treatment with the compoundInhibitory activity against Beta-2 adrenergic receptor in guinea pig trachea after treatment with the compound
ChEMBL 471 5 3 6 3.2 COc1cc(CC2NCCc3cc(O)c(O)c(I)c32)cc(OC)c1OC 10.1021/jm00081a007
CHEMBL341654 118067 0 None - 0 Guinea pig 5.9 pEC50 = 5.9 Binding
Inhibitory activity against Beta-2 adrenergic receptor in guinea pig trachea after treatment with the compoundInhibitory activity against Beta-2 adrenergic receptor in guinea pig trachea after treatment with the compound
ChEMBL 471 5 3 6 3.2 COc1cc(CC2NCCc3cc(O)c(O)c(I)c32)cc(OC)c1OC 10.1021/jm00081a007
164612037 184785 0 None -1 20 Human 4.9 pEC50 = 4.9 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysis
ChEMBL 326 8 4 4 1.8 CCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1021/acs.jmedchem.1c00692
CHEMBL4860528 184785 0 None -1 20 Human 4.9 pEC50 = 4.9 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysis
ChEMBL 326 8 4 4 1.8 CCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1021/acs.jmedchem.1c00692
10217757 111765 0 None - 0 Guinea pig 7.9 pEC50 = 7.9 Binding
Agonist activity at beta2 receptor in guinea pig trachea assessed as slow onset of inhibition of electrically stimulated contractionAgonist activity at beta2 receptor in guinea pig trachea assessed as slow onset of inhibition of electrically stimulated contraction
ChEMBL 497 12 5 6 5.2 COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c(NC=O)c3)cc2)cc1-c1ccccc1 10.1016/j.bmcl.2014.04.069
CHEMBL3290998 111765 0 None - 0 Guinea pig 7.9 pEC50 = 7.9 Binding
Agonist activity at beta2 receptor in guinea pig trachea assessed as slow onset of inhibition of electrically stimulated contractionAgonist activity at beta2 receptor in guinea pig trachea assessed as slow onset of inhibition of electrically stimulated contraction
ChEMBL 497 12 5 6 5.2 COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c(NC=O)c3)cc2)cc1-c1ccccc1 10.1016/j.bmcl.2014.04.069
72947901 103782 0 None - 0 Guinea pig 7.9 pEC50 = 7.9 Binding
Agonist activity at guinea pig trachea beta2-adrenergic receptor assessed as relaxation of histamine-induced tracheal ring contractionAgonist activity at guinea pig trachea beta2-adrenergic receptor assessed as relaxation of histamine-induced tracheal ring contraction
ChEMBL 686 18 4 9 5.8 COc1ccc(C2=NN(CCCCCOc3ccc(CC(C)NCC(O)c4ccc(O)c(NC=O)c4)cc3)C(=O)C3CCCCC23)cc1OC 10.1016/j.bmcl.2013.11.028
CHEMBL3099251 103782 0 None - 0 Guinea pig 7.9 pEC50 = 7.9 Binding
Agonist activity at guinea pig trachea beta2-adrenergic receptor assessed as relaxation of histamine-induced tracheal ring contractionAgonist activity at guinea pig trachea beta2-adrenergic receptor assessed as relaxation of histamine-induced tracheal ring contraction
ChEMBL 686 18 4 9 5.8 COc1ccc(C2=NN(CCCCCOc3ccc(CC(C)NCC(O)c4ccc(O)c(NC=O)c4)cc3)C(=O)C3CCCCC23)cc1OC 10.1016/j.bmcl.2013.11.028
44610056 123460 0 None - 5 Guinea pig 7.9 pEC50 = 7.9 Binding
Agonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of histamine-induced contractionAgonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of histamine-induced contraction
ChEMBL 704 14 5 9 5.5 O=c1ccc2c([C@@H](O)CNCCc3ccc(CCN4CCC(Cn5cnc([C@](O)(c6ccccc6)C6CCCCC6)n5)CC4)cc3)ccc(O)c2[nH]1 10.1016/j.bmcl.2015.10.008
CHEMBL3629360 123460 0 None - 5 Guinea pig 7.9 pEC50 = 7.9 Binding
Agonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of histamine-induced contractionAgonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of histamine-induced contraction
ChEMBL 704 14 5 9 5.5 O=c1ccc2c([C@@H](O)CNCCc3ccc(CCN4CCC(Cn5cnc([C@](O)(c6ccccc6)C6CCCCC6)n5)CC4)cc3)ccc(O)c2[nH]1 10.1016/j.bmcl.2015.10.008
1499 2052 43 None -33 17 Human 6.9 pEC50 = 6.9 Binding
Agonist activity at PK-tagged beta2 receptor (unknown origin) transfected in HEK293 cells after 90 mins by beta-arrestin assayAgonist activity at PK-tagged beta2 receptor (unknown origin) transfected in HEK293 cells after 90 mins by beta-arrestin assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2016.04.028
3779 2052 43 None -33 17 Human 6.9 pEC50 = 6.9 Binding
Agonist activity at PK-tagged beta2 receptor (unknown origin) transfected in HEK293 cells after 90 mins by beta-arrestin assayAgonist activity at PK-tagged beta2 receptor (unknown origin) transfected in HEK293 cells after 90 mins by beta-arrestin assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2016.04.028
536 2052 43 None -33 17 Human 6.9 pEC50 = 6.9 Binding
Agonist activity at PK-tagged beta2 receptor (unknown origin) transfected in HEK293 cells after 90 mins by beta-arrestin assayAgonist activity at PK-tagged beta2 receptor (unknown origin) transfected in HEK293 cells after 90 mins by beta-arrestin assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2016.04.028
CHEMBL434 2052 43 None -33 17 Human 6.9 pEC50 = 6.9 Binding
Agonist activity at PK-tagged beta2 receptor (unknown origin) transfected in HEK293 cells after 90 mins by beta-arrestin assayAgonist activity at PK-tagged beta2 receptor (unknown origin) transfected in HEK293 cells after 90 mins by beta-arrestin assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2016.04.028
DB01064 2052 43 None -33 17 Human 6.9 pEC50 = 6.9 Binding
Agonist activity at PK-tagged beta2 receptor (unknown origin) transfected in HEK293 cells after 90 mins by beta-arrestin assayAgonist activity at PK-tagged beta2 receptor (unknown origin) transfected in HEK293 cells after 90 mins by beta-arrestin assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2016.04.028
146025802 169000 0 None -1 2 Human 4.9 pEC50 = 4.9 Binding
Agonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring Rluc2-117-GalphaS/GFP10-Ggamma/Gbeta1 assessed as activation of GalphaS incubated for 5 mins in presence of coelenterazine 400a by BRET assayAgonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring Rluc2-117-GalphaS/GFP10-Ggamma/Gbeta1 assessed as activation of GalphaS incubated for 5 mins in presence of coelenterazine 400a by BRET assay
ChEMBL 349 10 4 7 1.5 COc1ccccc1OCCNC[C@H](O)COc1ccc(O)c(O)c1 10.1021/acs.jmedchem.9b00349
CHEMBL4435895 169000 0 None -1 2 Human 4.9 pEC50 = 4.9 Binding
Agonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring Rluc2-117-GalphaS/GFP10-Ggamma/Gbeta1 assessed as activation of GalphaS incubated for 5 mins in presence of coelenterazine 400a by BRET assayAgonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring Rluc2-117-GalphaS/GFP10-Ggamma/Gbeta1 assessed as activation of GalphaS incubated for 5 mins in presence of coelenterazine 400a by BRET assay
ChEMBL 349 10 4 7 1.5 COc1ccccc1OCCNC[C@H](O)COc1ccc(O)c(O)c1 10.1021/acs.jmedchem.9b00349
146025803 175593 0 None -1 2 Human 4.9 pEC50 = 4.9 Binding
Agonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring Rluc2-117-GalphaS/GFP10-Ggamma/Gbeta1 assessed as activation of GalphaS incubated for 5 mins in presence of coelenterazine 400a by BRET assayAgonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring Rluc2-117-GalphaS/GFP10-Ggamma/Gbeta1 assessed as activation of GalphaS incubated for 5 mins in presence of coelenterazine 400a by BRET assay
ChEMBL 467 14 4 7 3.7 COc1cc(CCNC[C@H](O)COc2ccc(O)c(O)c2)ccc1OCCCc1ccccc1 10.1021/acs.jmedchem.9b00349
CHEMBL4593181 175593 0 None -1 2 Human 4.9 pEC50 = 4.9 Binding
Agonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring Rluc2-117-GalphaS/GFP10-Ggamma/Gbeta1 assessed as activation of GalphaS incubated for 5 mins in presence of coelenterazine 400a by BRET assayAgonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring Rluc2-117-GalphaS/GFP10-Ggamma/Gbeta1 assessed as activation of GalphaS incubated for 5 mins in presence of coelenterazine 400a by BRET assay
ChEMBL 467 14 4 7 3.7 COc1cc(CCNC[C@H](O)COc2ccc(O)c(O)c2)ccc1OCCCc1ccccc1 10.1021/acs.jmedchem.9b00349
15133335 35055 0 None - 0 Guinea pig 6.9 pEC50 = 6.9 Binding
Inhibitory activity against Beta-2 adrenergic receptor in guinea pig trachea after treatment with the compoundInhibitory activity against Beta-2 adrenergic receptor in guinea pig trachea after treatment with the compound
ChEMBL 413 5 3 6 3.6 COc1cc(CC2NCCc3c2cc(O)c(O)c3C(F)(F)F)cc(OC)c1OC 10.1021/jm00081a007
CHEMBL143645 35055 0 None - 0 Guinea pig 6.9 pEC50 = 6.9 Binding
Inhibitory activity against Beta-2 adrenergic receptor in guinea pig trachea after treatment with the compoundInhibitory activity against Beta-2 adrenergic receptor in guinea pig trachea after treatment with the compound
ChEMBL 413 5 3 6 3.6 COc1cc(CC2NCCc3c2cc(O)c(O)c3C(F)(F)F)cc(OC)c1OC 10.1021/jm00081a007
127045853 139250 0 None 20 6 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at PK-tagged beta2 receptor (unknown origin) transfected in HEK293 cells after 90 mins by beta-arrestin assayAgonist activity at PK-tagged beta2 receptor (unknown origin) transfected in HEK293 cells after 90 mins by beta-arrestin assay
ChEMBL 492 12 4 7 3.6 COc1cc(CCNC[C@H](O)c2ccc(O)c3c2OCC(=O)N3)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
CHEMBL3798748 139250 0 None 20 6 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at PK-tagged beta2 receptor (unknown origin) transfected in HEK293 cells after 90 mins by beta-arrestin assayAgonist activity at PK-tagged beta2 receptor (unknown origin) transfected in HEK293 cells after 90 mins by beta-arrestin assay
ChEMBL 492 12 4 7 3.6 COc1cc(CCNC[C@H](O)c2ccc(O)c3c2OCC(=O)N3)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
127045855 139121 0 None 1 6 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GSK2 and coelenterazine 400a by BRET assayAgonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GSK2 and coelenterazine 400a by BRET assay
ChEMBL 319 8 4 6 1.8 COc1ccccc1OCCNC[C@H](O)c1ccc(O)c(O)c1 10.1021/acs.jmedchem.9b00349
CHEMBL3797876 139121 0 None 1 6 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GSK2 and coelenterazine 400a by BRET assayAgonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GSK2 and coelenterazine 400a by BRET assay
ChEMBL 319 8 4 6 1.8 COc1ccccc1OCCNC[C@H](O)c1ccc(O)c(O)c1 10.1021/acs.jmedchem.9b00349
443372 10123 23 None -1 3 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GSK5 and coelenterazine 400a by BRET assayAgonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GSK5 and coelenterazine 400a by BRET assay
ChEMBL 211 4 4 4 1.1 CC(C)NC[C@H](O)c1ccc(O)c(O)c1 10.1021/acs.jmedchem.9b00349
CHEMBL1160723 10123 23 None -1 3 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GSK5 and coelenterazine 400a by BRET assayAgonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GSK5 and coelenterazine 400a by BRET assay
ChEMBL 211 4 4 4 1.1 CC(C)NC[C@H](O)c1ccc(O)c(O)c1 10.1021/acs.jmedchem.9b00349
CHEMBL2062275 10123 23 None -1 3 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GSK5 and coelenterazine 400a by BRET assayAgonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GSK5 and coelenterazine 400a by BRET assay
ChEMBL 211 4 4 4 1.1 CC(C)NC[C@H](O)c1ccc(O)c(O)c1 10.1021/acs.jmedchem.9b00349
10310047 111758 0 None - 2 Guinea pig 6.7 pEC50 = 6.7 Binding
Agonist activity at beta2 receptor in guinea pig trachea assessed as slow onset of inhibition of electrically stimulated contractionAgonist activity at beta2 receptor in guinea pig trachea assessed as slow onset of inhibition of electrically stimulated contraction
ChEMBL 422 11 5 6 3.9 CCOc1ccc(Nc2ccc(CCNCC(O)c3ccc(O)c(CO)c3)cc2)cc1 10.1016/j.bmcl.2014.04.069
CHEMBL3290991 111758 0 None - 2 Guinea pig 6.7 pEC50 = 6.7 Binding
Agonist activity at beta2 receptor in guinea pig trachea assessed as slow onset of inhibition of electrically stimulated contractionAgonist activity at beta2 receptor in guinea pig trachea assessed as slow onset of inhibition of electrically stimulated contraction
ChEMBL 422 11 5 6 3.9 CCOc1ccc(Nc2ccc(CCNCC(O)c3ccc(O)c(CO)c3)cc2)cc1 10.1016/j.bmcl.2014.04.069
146025803 175593 0 None -1 2 Human 5.7 pEC50 = 5.7 Binding
Agonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GSK5 and coelenterazine 400a by BRET assayAgonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GSK5 and coelenterazine 400a by BRET assay
ChEMBL 467 14 4 7 3.7 COc1cc(CCNC[C@H](O)COc2ccc(O)c(O)c2)ccc1OCCCc1ccccc1 10.1021/acs.jmedchem.9b00349
CHEMBL4593181 175593 0 None -1 2 Human 5.7 pEC50 = 5.7 Binding
Agonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GSK5 and coelenterazine 400a by BRET assayAgonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GSK5 and coelenterazine 400a by BRET assay
ChEMBL 467 14 4 7 3.7 COc1cc(CCNC[C@H](O)COc2ccc(O)c(O)c2)ccc1OCCCc1ccccc1 10.1021/acs.jmedchem.9b00349
2419 3394 80 None - 6 Guinea pig 8.6 pEC50 = 8.6 Binding
Agonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of histamine-induced contractionAgonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of histamine-induced contraction
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2015.10.008
5152 3394 80 None - 6 Guinea pig 8.6 pEC50 = 8.6 Binding
Agonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of histamine-induced contractionAgonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of histamine-induced contraction
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2015.10.008
559 3394 80 None - 6 Guinea pig 8.6 pEC50 = 8.6 Binding
Agonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of histamine-induced contractionAgonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of histamine-induced contraction
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2015.10.008
CHEMBL1263 3394 80 None - 6 Guinea pig 8.6 pEC50 = 8.6 Binding
Agonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of histamine-induced contractionAgonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of histamine-induced contraction
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2015.10.008
DB00938 3394 80 None - 6 Guinea pig 8.6 pEC50 = 8.6 Binding
Agonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of histamine-induced contractionAgonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of histamine-induced contraction
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2015.10.008
71562033 87108 0 None - 0 Guinea pig 8.6 pEC50 = 8.6 Binding
Agonist activity at beta2-adrenoceptor in guinea pig trachea assessed as relaxation of histamine-induced precontracted tracheal ringsAgonist activity at beta2-adrenoceptor in guinea pig trachea assessed as relaxation of histamine-induced precontracted tracheal rings
ChEMBL 549 13 5 8 4.3 COc1ccc(C(=O)Nc2c(Cl)cncc2Cl)cc1OCCCCNCC(O)c1ccc(O)c(CO)c1 10.1016/j.bmcl.2012.11.058
CHEMBL2335409 87108 0 None - 0 Guinea pig 8.6 pEC50 = 8.6 Binding
Agonist activity at beta2-adrenoceptor in guinea pig trachea assessed as relaxation of histamine-induced precontracted tracheal ringsAgonist activity at beta2-adrenoceptor in guinea pig trachea assessed as relaxation of histamine-induced precontracted tracheal rings
ChEMBL 549 13 5 8 4.3 COc1ccc(C(=O)Nc2c(Cl)cncc2Cl)cc1OCCCCNCC(O)c1ccc(O)c(CO)c1 10.1016/j.bmcl.2012.11.058
127045855 139121 0 None 1 6 Human 6.7 pEC50 = 6.7 Binding
Agonist activity at PK-tagged beta2 receptor (unknown origin) transfected in HEK293 cells after 90 mins by beta-arrestin assayAgonist activity at PK-tagged beta2 receptor (unknown origin) transfected in HEK293 cells after 90 mins by beta-arrestin assay
ChEMBL 319 8 4 6 1.8 COc1ccccc1OCCNC[C@H](O)c1ccc(O)c(O)c1 10.1016/j.bmc.2016.04.028
CHEMBL3797876 139121 0 None 1 6 Human 6.7 pEC50 = 6.7 Binding
Agonist activity at PK-tagged beta2 receptor (unknown origin) transfected in HEK293 cells after 90 mins by beta-arrestin assayAgonist activity at PK-tagged beta2 receptor (unknown origin) transfected in HEK293 cells after 90 mins by beta-arrestin assay
ChEMBL 319 8 4 6 1.8 COc1ccccc1OCCNC[C@H](O)c1ccc(O)c(O)c1 10.1016/j.bmc.2016.04.028
102262219 139516 0 None 12 6 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at PK-tagged beta2 receptor (unknown origin) transfected in HEK293 cells after 90 mins by beta-arrestin assayAgonist activity at PK-tagged beta2 receptor (unknown origin) transfected in HEK293 cells after 90 mins by beta-arrestin assay
ChEMBL 488 12 4 6 4.1 COc1cc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
CHEMBL3800400 139516 0 None 12 6 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at PK-tagged beta2 receptor (unknown origin) transfected in HEK293 cells after 90 mins by beta-arrestin assayAgonist activity at PK-tagged beta2 receptor (unknown origin) transfected in HEK293 cells after 90 mins by beta-arrestin assay
ChEMBL 488 12 4 6 4.1 COc1cc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
127047221 139387 0 None -3 6 Human 5.7 pEC50 = 5.7 Binding
Agonist activity at PK-tagged beta2 receptor (unknown origin) transfected in HEK293 cells after 90 mins by beta-arrestin assayAgonist activity at PK-tagged beta2 receptor (unknown origin) transfected in HEK293 cells after 90 mins by beta-arrestin assay
ChEMBL 319 8 4 6 1.8 COc1ccccc1OCCNC[C@@H](O)c1ccc(O)c(O)c1 10.1016/j.bmc.2016.04.028
CHEMBL3799593 139387 0 None -3 6 Human 5.7 pEC50 = 5.7 Binding
Agonist activity at PK-tagged beta2 receptor (unknown origin) transfected in HEK293 cells after 90 mins by beta-arrestin assayAgonist activity at PK-tagged beta2 receptor (unknown origin) transfected in HEK293 cells after 90 mins by beta-arrestin assay
ChEMBL 319 8 4 6 1.8 COc1ccccc1OCCNC[C@@H](O)c1ccc(O)c(O)c1 10.1016/j.bmc.2016.04.028
15133333 37016 0 None - 0 Guinea pig 5.7 pEC50 = 5.7 Binding
Inhibitory activity against Beta-2 adrenergic receptor in guinea pig trachea after treatment with the compoundInhibitory activity against Beta-2 adrenergic receptor in guinea pig trachea after treatment with the compound
ChEMBL 471 5 3 6 3.2 COc1cc(CC2NCCc3c2cc(O)c(O)c3I)cc(OC)c1OC 10.1021/jm00081a007
CHEMBL145381 37016 0 None - 0 Guinea pig 5.7 pEC50 = 5.7 Binding
Inhibitory activity against Beta-2 adrenergic receptor in guinea pig trachea after treatment with the compoundInhibitory activity against Beta-2 adrenergic receptor in guinea pig trachea after treatment with the compound
ChEMBL 471 5 3 6 3.2 COc1cc(CC2NCCc3c2cc(O)c(O)c3I)cc(OC)c1OC 10.1021/jm00081a007
10339796 121154 0 None - 0 Guinea pig 6.6 pEC50 = 6.6 Binding
Inhibitory activity against Beta-2 adrenergic receptor in guinea pig trachea after treatment with the compoundInhibitory activity against Beta-2 adrenergic receptor in guinea pig trachea after treatment with the compound
ChEMBL 381 5 3 6 2.8 COc1cc(CC2NCCc3c(F)c(O)c(O)c(F)c32)cc(OC)c1OC 10.1021/jm00081a007
CHEMBL358648 121154 0 None - 0 Guinea pig 6.6 pEC50 = 6.6 Binding
Inhibitory activity against Beta-2 adrenergic receptor in guinea pig trachea after treatment with the compoundInhibitory activity against Beta-2 adrenergic receptor in guinea pig trachea after treatment with the compound
ChEMBL 381 5 3 6 2.8 COc1cc(CC2NCCc3c(F)c(O)c(O)c(F)c32)cc(OC)c1OC 10.1021/jm00081a007
443372 10123 23 None -1 3 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GSK2 and coelenterazine 400a by BRET assayAgonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GSK2 and coelenterazine 400a by BRET assay
ChEMBL 211 4 4 4 1.1 CC(C)NC[C@H](O)c1ccc(O)c(O)c1 10.1021/acs.jmedchem.9b00349
CHEMBL1160723 10123 23 None -1 3 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GSK2 and coelenterazine 400a by BRET assayAgonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GSK2 and coelenterazine 400a by BRET assay
ChEMBL 211 4 4 4 1.1 CC(C)NC[C@H](O)c1ccc(O)c(O)c1 10.1021/acs.jmedchem.9b00349
CHEMBL2062275 10123 23 None -1 3 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GSK2 and coelenterazine 400a by BRET assayAgonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GSK2 and coelenterazine 400a by BRET assay
ChEMBL 211 4 4 4 1.1 CC(C)NC[C@H](O)c1ccc(O)c(O)c1 10.1021/acs.jmedchem.9b00349
44328703 10118 0 None 1 2 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GSK5 and coelenterazine 400a by BRET assayAgonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GSK5 and coelenterazine 400a by BRET assay
ChEMBL 241 6 4 5 0.8 CC(C)NC[C@H](O)COc1ccc(O)c(O)c1 10.1021/acs.jmedchem.9b00349
CHEMBL1160694 10118 0 None 1 2 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GSK5 and coelenterazine 400a by BRET assayAgonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GSK5 and coelenterazine 400a by BRET assay
ChEMBL 241 6 4 5 0.8 CC(C)NC[C@H](O)COc1ccc(O)c(O)c1 10.1021/acs.jmedchem.9b00349
5581 101175 10 None 1 7 Guinea pig 7.6 pEC50 = 7.6 Binding
Inhibitory activity against Beta-2 adrenergic receptor in guinea pig trachea after treatment with the compoundInhibitory activity against Beta-2 adrenergic receptor in guinea pig trachea after treatment with the compound
ChEMBL 345 5 3 6 2.6 COc1cc(CC2NCCc3cc(O)c(O)cc32)cc(OC)c1OC 10.1021/jm00081a007
CHEMBL299175 101175 10 None 1 7 Guinea pig 7.6 pEC50 = 7.6 Binding
Inhibitory activity against Beta-2 adrenergic receptor in guinea pig trachea after treatment with the compoundInhibitory activity against Beta-2 adrenergic receptor in guinea pig trachea after treatment with the compound
ChEMBL 345 5 3 6 2.6 COc1cc(CC2NCCc3cc(O)c(O)cc32)cc(OC)c1OC 10.1021/jm00081a007
127046950 139502 0 None 3 6 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at PK-tagged beta2 receptor (unknown origin) transfected in HEK293 cells after 90 mins by beta-arrestin assayAgonist activity at PK-tagged beta2 receptor (unknown origin) transfected in HEK293 cells after 90 mins by beta-arrestin assay
ChEMBL 437 12 4 6 4.0 COc1cc(CCNC[C@H](O)c2ccc(O)c(O)c2)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
CHEMBL3800303 139502 0 None 3 6 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at PK-tagged beta2 receptor (unknown origin) transfected in HEK293 cells after 90 mins by beta-arrestin assayAgonist activity at PK-tagged beta2 receptor (unknown origin) transfected in HEK293 cells after 90 mins by beta-arrestin assay
ChEMBL 437 12 4 6 4.0 COc1cc(CCNC[C@H](O)c2ccc(O)c(O)c2)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
127045855 139121 0 None 1 6 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of coelenterazine 400a by BRET assayAgonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of coelenterazine 400a by BRET assay
ChEMBL 319 8 4 6 1.8 COc1ccccc1OCCNC[C@H](O)c1ccc(O)c(O)c1 10.1021/acs.jmedchem.9b00349
CHEMBL3797876 139121 0 None 1 6 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of coelenterazine 400a by BRET assayAgonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of coelenterazine 400a by BRET assay
ChEMBL 319 8 4 6 1.8 COc1ccccc1OCCNC[C@H](O)c1ccc(O)c(O)c1 10.1021/acs.jmedchem.9b00349
1499 2052 43 None -9 17 Guinea pig 7.5 pEC50 = 7.5 Binding
Agonist activity at beta2-adrenoceptor in guinea pig trachea assessed as relaxation of histamine-induced precontracted tracheal ringsAgonist activity at beta2-adrenoceptor in guinea pig trachea assessed as relaxation of histamine-induced precontracted tracheal rings
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmcl.2012.11.058
3779 2052 43 None -9 17 Guinea pig 7.5 pEC50 = 7.5 Binding
Agonist activity at beta2-adrenoceptor in guinea pig trachea assessed as relaxation of histamine-induced precontracted tracheal ringsAgonist activity at beta2-adrenoceptor in guinea pig trachea assessed as relaxation of histamine-induced precontracted tracheal rings
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmcl.2012.11.058
536 2052 43 None -9 17 Guinea pig 7.5 pEC50 = 7.5 Binding
Agonist activity at beta2-adrenoceptor in guinea pig trachea assessed as relaxation of histamine-induced precontracted tracheal ringsAgonist activity at beta2-adrenoceptor in guinea pig trachea assessed as relaxation of histamine-induced precontracted tracheal rings
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmcl.2012.11.058
CHEMBL434 2052 43 None -9 17 Guinea pig 7.5 pEC50 = 7.5 Binding
Agonist activity at beta2-adrenoceptor in guinea pig trachea assessed as relaxation of histamine-induced precontracted tracheal ringsAgonist activity at beta2-adrenoceptor in guinea pig trachea assessed as relaxation of histamine-induced precontracted tracheal rings
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmcl.2012.11.058
DB01064 2052 43 None -9 17 Guinea pig 7.5 pEC50 = 7.5 Binding
Agonist activity at beta2-adrenoceptor in guinea pig trachea assessed as relaxation of histamine-induced precontracted tracheal ringsAgonist activity at beta2-adrenoceptor in guinea pig trachea assessed as relaxation of histamine-induced precontracted tracheal rings
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmcl.2012.11.058
82021510 169146 2 None - 0 Guinea pig 5.6 pEC50 = 5.6 Binding
Agonist activity at beta2 adrenergic receptor in guinea pig tracheal smooth muscle assessed as inhibition of histamine-induced tracheal smooth muscle contraction by measuring spasmolysis preincubated for 15 mins in presence of beta adrenergic receptor antagonist propranolol followed by histamine additionAgonist activity at beta2 adrenergic receptor in guinea pig tracheal smooth muscle assessed as inhibition of histamine-induced tracheal smooth muscle contraction by measuring spasmolysis preincubated for 15 mins in presence of beta adrenergic receptor antagonist propranolol followed by histamine addition
ChEMBL 221 2 3 3 2.3 CC(C)CC1NCCc2cc(O)c(O)cc21 10.1021/acs.jnatprod.9b00418
CHEMBL4438390 169146 2 None - 0 Guinea pig 5.6 pEC50 = 5.6 Binding
Agonist activity at beta2 adrenergic receptor in guinea pig tracheal smooth muscle assessed as inhibition of histamine-induced tracheal smooth muscle contraction by measuring spasmolysis preincubated for 15 mins in presence of beta adrenergic receptor antagonist propranolol followed by histamine additionAgonist activity at beta2 adrenergic receptor in guinea pig tracheal smooth muscle assessed as inhibition of histamine-induced tracheal smooth muscle contraction by measuring spasmolysis preincubated for 15 mins in presence of beta adrenergic receptor antagonist propranolol followed by histamine addition
ChEMBL 221 2 3 3 2.3 CC(C)CC1NCCc2cc(O)c(O)cc21 10.1021/acs.jnatprod.9b00418
13720716 62709 0 None 1 2 Guinea pig 6.5 pEC50 = 6.5 Binding
Inhibitory activity against Beta-2 adrenergic receptor in guinea pig tracheaInhibitory activity against Beta-2 adrenergic receptor in guinea pig trachea
ChEMBL 363 5 3 6 2.7 COc1cc(C[C@@H]2NCCc3cc(O)c(O)c(F)c32)cc(OC)c1OC 10.1021/jm00081a007
CHEMBL1788251 62709 0 None 1 2 Guinea pig 6.5 pEC50 = 6.5 Binding
Inhibitory activity against Beta-2 adrenergic receptor in guinea pig tracheaInhibitory activity against Beta-2 adrenergic receptor in guinea pig trachea
ChEMBL 363 5 3 6 2.7 COc1cc(C[C@@H]2NCCc3cc(O)c(O)c(F)c32)cc(OC)c1OC 10.1021/jm00081a007
71562154 87110 0 None - 0 Guinea pig 8.5 pEC50 = 8.5 Binding
Agonist activity at beta2-adrenoceptor in guinea pig trachea assessed as relaxation of histamine-induced precontracted tracheal ringsAgonist activity at beta2-adrenoceptor in guinea pig trachea assessed as relaxation of histamine-induced precontracted tracheal rings
ChEMBL 577 15 5 8 5.1 COc1ccc(C(=O)Nc2c(Cl)cncc2Cl)cc1OCCCCCCNCC(O)c1ccc(O)c(CO)c1 10.1016/j.bmcl.2012.11.058
CHEMBL2335411 87110 0 None - 0 Guinea pig 8.5 pEC50 = 8.5 Binding
Agonist activity at beta2-adrenoceptor in guinea pig trachea assessed as relaxation of histamine-induced precontracted tracheal ringsAgonist activity at beta2-adrenoceptor in guinea pig trachea assessed as relaxation of histamine-induced precontracted tracheal rings
ChEMBL 577 15 5 8 5.1 COc1ccc(C(=O)Nc2c(Cl)cncc2Cl)cc1OCCCCCCNCC(O)c1ccc(O)c(CO)c1 10.1016/j.bmcl.2012.11.058
71562032 87107 0 None - 0 Guinea pig 8.5 pEC50 = 8.5 Binding
Agonist activity at beta2-adrenoceptor in guinea pig trachea assessed as relaxation of histamine-induced precontracted tracheal ringsAgonist activity at beta2-adrenoceptor in guinea pig trachea assessed as relaxation of histamine-induced precontracted tracheal rings
ChEMBL 535 12 5 8 3.9 COc1ccc(C(=O)Nc2c(Cl)cncc2Cl)cc1OCCCNCC(O)c1ccc(O)c(CO)c1 10.1016/j.bmcl.2012.11.058
CHEMBL2335408 87107 0 None - 0 Guinea pig 8.5 pEC50 = 8.5 Binding
Agonist activity at beta2-adrenoceptor in guinea pig trachea assessed as relaxation of histamine-induced precontracted tracheal ringsAgonist activity at beta2-adrenoceptor in guinea pig trachea assessed as relaxation of histamine-induced precontracted tracheal rings
ChEMBL 535 12 5 8 3.9 COc1ccc(C(=O)Nc2c(Cl)cncc2Cl)cc1OCCCNCC(O)c1ccc(O)c(CO)c1 10.1016/j.bmcl.2012.11.058
2419 3394 80 None - 6 Guinea pig 7.5 pEC50 = 7.5 Binding
Agonist activity at beta2 receptor in guinea pig trachea assessed as slow onset of inhibition of electrically stimulated contractionAgonist activity at beta2 receptor in guinea pig trachea assessed as slow onset of inhibition of electrically stimulated contraction
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2014.04.069
5152 3394 80 None - 6 Guinea pig 7.5 pEC50 = 7.5 Binding
Agonist activity at beta2 receptor in guinea pig trachea assessed as slow onset of inhibition of electrically stimulated contractionAgonist activity at beta2 receptor in guinea pig trachea assessed as slow onset of inhibition of electrically stimulated contraction
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2014.04.069
559 3394 80 None - 6 Guinea pig 7.5 pEC50 = 7.5 Binding
Agonist activity at beta2 receptor in guinea pig trachea assessed as slow onset of inhibition of electrically stimulated contractionAgonist activity at beta2 receptor in guinea pig trachea assessed as slow onset of inhibition of electrically stimulated contraction
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2014.04.069
CHEMBL1263 3394 80 None - 6 Guinea pig 7.5 pEC50 = 7.5 Binding
Agonist activity at beta2 receptor in guinea pig trachea assessed as slow onset of inhibition of electrically stimulated contractionAgonist activity at beta2 receptor in guinea pig trachea assessed as slow onset of inhibition of electrically stimulated contraction
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2014.04.069
DB00938 3394 80 None - 6 Guinea pig 7.5 pEC50 = 7.5 Binding
Agonist activity at beta2 receptor in guinea pig trachea assessed as slow onset of inhibition of electrically stimulated contractionAgonist activity at beta2 receptor in guinea pig trachea assessed as slow onset of inhibition of electrically stimulated contraction
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2014.04.069
1499 2052 43 None -9 17 Guinea pig 7.5 pEC50 = 7.5 Binding
Agonist activity at guinea pig trachea beta2-adrenergic receptor assessed as relaxation of histamine-induced tracheal ring contractionAgonist activity at guinea pig trachea beta2-adrenergic receptor assessed as relaxation of histamine-induced tracheal ring contraction
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmcl.2013.11.028
3779 2052 43 None -9 17 Guinea pig 7.5 pEC50 = 7.5 Binding
Agonist activity at guinea pig trachea beta2-adrenergic receptor assessed as relaxation of histamine-induced tracheal ring contractionAgonist activity at guinea pig trachea beta2-adrenergic receptor assessed as relaxation of histamine-induced tracheal ring contraction
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmcl.2013.11.028
536 2052 43 None -9 17 Guinea pig 7.5 pEC50 = 7.5 Binding
Agonist activity at guinea pig trachea beta2-adrenergic receptor assessed as relaxation of histamine-induced tracheal ring contractionAgonist activity at guinea pig trachea beta2-adrenergic receptor assessed as relaxation of histamine-induced tracheal ring contraction
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmcl.2013.11.028
CHEMBL434 2052 43 None -9 17 Guinea pig 7.5 pEC50 = 7.5 Binding
Agonist activity at guinea pig trachea beta2-adrenergic receptor assessed as relaxation of histamine-induced tracheal ring contractionAgonist activity at guinea pig trachea beta2-adrenergic receptor assessed as relaxation of histamine-induced tracheal ring contraction
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmcl.2013.11.028
DB01064 2052 43 None -9 17 Guinea pig 7.5 pEC50 = 7.5 Binding
Agonist activity at guinea pig trachea beta2-adrenergic receptor assessed as relaxation of histamine-induced tracheal ring contractionAgonist activity at guinea pig trachea beta2-adrenergic receptor assessed as relaxation of histamine-induced tracheal ring contraction
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmcl.2013.11.028
1499 2052 43 None -9 17 Guinea pig 7.5 pEC50 = 7.5 Binding
Agonist activity at guinea pig trachea beta2-adrenergic receptor assessed as relaxation of histamine-induced tracheal ring contractionAgonist activity at guinea pig trachea beta2-adrenergic receptor assessed as relaxation of histamine-induced tracheal ring contraction
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmcl.2013.11.028
3779 2052 43 None -9 17 Guinea pig 7.5 pEC50 = 7.5 Binding
Agonist activity at guinea pig trachea beta2-adrenergic receptor assessed as relaxation of histamine-induced tracheal ring contractionAgonist activity at guinea pig trachea beta2-adrenergic receptor assessed as relaxation of histamine-induced tracheal ring contraction
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmcl.2013.11.028
536 2052 43 None -9 17 Guinea pig 7.5 pEC50 = 7.5 Binding
Agonist activity at guinea pig trachea beta2-adrenergic receptor assessed as relaxation of histamine-induced tracheal ring contractionAgonist activity at guinea pig trachea beta2-adrenergic receptor assessed as relaxation of histamine-induced tracheal ring contraction
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmcl.2013.11.028
CHEMBL434 2052 43 None -9 17 Guinea pig 7.5 pEC50 = 7.5 Binding
Agonist activity at guinea pig trachea beta2-adrenergic receptor assessed as relaxation of histamine-induced tracheal ring contractionAgonist activity at guinea pig trachea beta2-adrenergic receptor assessed as relaxation of histamine-induced tracheal ring contraction
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmcl.2013.11.028
DB01064 2052 43 None -9 17 Guinea pig 7.5 pEC50 = 7.5 Binding
Agonist activity at guinea pig trachea beta2-adrenergic receptor assessed as relaxation of histamine-induced tracheal ring contractionAgonist activity at guinea pig trachea beta2-adrenergic receptor assessed as relaxation of histamine-induced tracheal ring contraction
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmcl.2013.11.028
44328703 10118 0 None 1 2 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GSK2 and coelenterazine 400a by BRET assayAgonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GSK2 and coelenterazine 400a by BRET assay
ChEMBL 241 6 4 5 0.8 CC(C)NC[C@H](O)COc1ccc(O)c(O)c1 10.1021/acs.jmedchem.9b00349
CHEMBL1160694 10118 0 None 1 2 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GSK2 and coelenterazine 400a by BRET assayAgonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GSK2 and coelenterazine 400a by BRET assay
ChEMBL 241 6 4 5 0.8 CC(C)NC[C@H](O)COc1ccc(O)c(O)c1 10.1021/acs.jmedchem.9b00349
13720717 77483 0 None 3 2 Guinea pig 5.5 pEC50 = 5.5 Binding
Inhibitory activity against Beta-2 adrenergic receptor in guinea pig tracheaInhibitory activity against Beta-2 adrenergic receptor in guinea pig trachea
ChEMBL 363 5 3 6 2.7 COc1cc(C[C@H]2NCCc3cc(O)c(O)c(F)c32)cc(OC)c1OC 10.1021/jm00081a007
CHEMBL2092996 77483 0 None 3 2 Guinea pig 5.5 pEC50 = 5.5 Binding
Inhibitory activity against Beta-2 adrenergic receptor in guinea pig tracheaInhibitory activity against Beta-2 adrenergic receptor in guinea pig trachea
ChEMBL 363 5 3 6 2.7 COc1cc(C[C@H]2NCCc3cc(O)c(O)c(F)c32)cc(OC)c1OC 10.1021/jm00081a007
168290235 192356 0 None -4 20 Human 4.5 pEC50 = 4.5 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysis
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5201074 192356 0 None -4 20 Human 4.5 pEC50 = 4.5 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysis
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222491 192356 0 None -4 20 Human 4.5 pEC50 = 4.5 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysis
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
168295528 192419 0 None -1 20 Human 4.4 pEC50 = 4.4 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysis
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5206565 192419 0 None -1 20 Human 4.4 pEC50 = 4.4 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysis
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222872 192419 0 None -1 20 Human 4.4 pEC50 = 4.4 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysis
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
127046950 139502 0 None 3 6 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GSK5 and coelenterazine 400a by BRET assayAgonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GSK5 and coelenterazine 400a by BRET assay
ChEMBL 437 12 4 6 4.0 COc1cc(CCNC[C@H](O)c2ccc(O)c(O)c2)ccc1OCCCc1ccccc1 10.1021/acs.jmedchem.9b00349
CHEMBL3800303 139502 0 None 3 6 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GSK5 and coelenterazine 400a by BRET assayAgonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GSK5 and coelenterazine 400a by BRET assay
ChEMBL 437 12 4 6 4.0 COc1cc(CCNC[C@H](O)c2ccc(O)c(O)c2)ccc1OCCCc1ccccc1 10.1021/acs.jmedchem.9b00349
443372 10123 23 None -1 3 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of coelenterazine 400a by BRET assayAgonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of coelenterazine 400a by BRET assay
ChEMBL 211 4 4 4 1.1 CC(C)NC[C@H](O)c1ccc(O)c(O)c1 10.1021/acs.jmedchem.9b00349
CHEMBL1160723 10123 23 None -1 3 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of coelenterazine 400a by BRET assayAgonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of coelenterazine 400a by BRET assay
ChEMBL 211 4 4 4 1.1 CC(C)NC[C@H](O)c1ccc(O)c(O)c1 10.1021/acs.jmedchem.9b00349
CHEMBL2062275 10123 23 None -1 3 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of coelenterazine 400a by BRET assayAgonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of coelenterazine 400a by BRET assay
ChEMBL 211 4 4 4 1.1 CC(C)NC[C@H](O)c1ccc(O)c(O)c1 10.1021/acs.jmedchem.9b00349
72947902 103779 0 None - 0 Guinea pig 8.3 pEC50 = 8.3 Binding
Agonist activity at guinea pig trachea beta2-adrenergic receptor assessed as relaxation of histamine-induced tracheal ring contractionAgonist activity at guinea pig trachea beta2-adrenergic receptor assessed as relaxation of histamine-induced tracheal ring contraction
ChEMBL 700 19 4 9 6.2 COc1ccc(C2=NN(CCCCCCOc3ccc(CC(C)NCC(O)c4ccc(O)c(NC=O)c4)cc3)C(=O)C3CCCCC23)cc1OC 10.1016/j.bmcl.2013.11.028
CHEMBL3099248 103779 0 None - 0 Guinea pig 8.3 pEC50 = 8.3 Binding
Agonist activity at guinea pig trachea beta2-adrenergic receptor assessed as relaxation of histamine-induced tracheal ring contractionAgonist activity at guinea pig trachea beta2-adrenergic receptor assessed as relaxation of histamine-induced tracheal ring contraction
ChEMBL 700 19 4 9 6.2 COc1ccc(C2=NN(CCCCCCOc3ccc(CC(C)NCC(O)c4ccc(O)c(NC=O)c4)cc3)C(=O)C3CCCCC23)cc1OC 10.1016/j.bmcl.2013.11.028
72947902 103779 0 None - 0 Guinea pig 8.3 pEC50 = 8.3 Binding
Agonist activity at guinea pig trachea beta2-adrenergic receptor assessed as relaxation of histamine-induced tracheal ring contractionAgonist activity at guinea pig trachea beta2-adrenergic receptor assessed as relaxation of histamine-induced tracheal ring contraction
ChEMBL 700 19 4 9 6.2 COc1ccc(C2=NN(CCCCCCOc3ccc(CC(C)NCC(O)c4ccc(O)c(NC=O)c4)cc3)C(=O)C3CCCCC23)cc1OC 10.1016/j.bmcl.2013.11.028
CHEMBL3099248 103779 0 None - 0 Guinea pig 8.3 pEC50 = 8.3 Binding
Agonist activity at guinea pig trachea beta2-adrenergic receptor assessed as relaxation of histamine-induced tracheal ring contractionAgonist activity at guinea pig trachea beta2-adrenergic receptor assessed as relaxation of histamine-induced tracheal ring contraction
ChEMBL 700 19 4 9 6.2 COc1ccc(C2=NN(CCCCCCOc3ccc(CC(C)NCC(O)c4ccc(O)c(NC=O)c4)cc3)C(=O)C3CCCCC23)cc1OC 10.1016/j.bmcl.2013.11.028
24764458 108841 2 None - 1 Guinea pig 8.2 pEC50 = 8.2 Binding
Agonist activity at beta-2 adrenoceptor in guinea pig trachea assessed as inhibition of histamine-induced muscle contractionAgonist activity at beta-2 adrenoceptor in guinea pig trachea assessed as inhibition of histamine-induced muscle contraction
ChEMBL 716 18 6 9 6.9 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3ccc(O)c(Cl)c3)CC2)ccc1O 10.1039/C1MD00140J
CHEMBL3219042 108841 2 None - 1 Guinea pig 8.2 pEC50 = 8.2 Binding
Agonist activity at beta-2 adrenoceptor in guinea pig trachea assessed as inhibition of histamine-induced muscle contractionAgonist activity at beta-2 adrenoceptor in guinea pig trachea assessed as inhibition of histamine-induced muscle contraction
ChEMBL 716 18 6 9 6.9 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3ccc(O)c(Cl)c3)CC2)ccc1O 10.1039/C1MD00140J
127046950 139502 0 None 3 6 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GSK2 and coelenterazine 400a by BRET assayAgonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GSK2 and coelenterazine 400a by BRET assay
ChEMBL 437 12 4 6 4.0 COc1cc(CCNC[C@H](O)c2ccc(O)c(O)c2)ccc1OCCCc1ccccc1 10.1021/acs.jmedchem.9b00349
CHEMBL3800303 139502 0 None 3 6 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GSK2 and coelenterazine 400a by BRET assayAgonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GSK2 and coelenterazine 400a by BRET assay
ChEMBL 437 12 4 6 4.0 COc1cc(CCNC[C@H](O)c2ccc(O)c(O)c2)ccc1OCCCc1ccccc1 10.1021/acs.jmedchem.9b00349
127046948 139527 0 None 13 6 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at PK-tagged beta2 receptor (unknown origin) transfected in HEK293 cells after 90 mins by beta-arrestin assayAgonist activity at PK-tagged beta2 receptor (unknown origin) transfected in HEK293 cells after 90 mins by beta-arrestin assay
ChEMBL 488 12 4 6 4.1 COc1cc(CCNC[C@@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
CHEMBL3800468 139527 0 None 13 6 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at PK-tagged beta2 receptor (unknown origin) transfected in HEK293 cells after 90 mins by beta-arrestin assayAgonist activity at PK-tagged beta2 receptor (unknown origin) transfected in HEK293 cells after 90 mins by beta-arrestin assay
ChEMBL 488 12 4 6 4.1 COc1cc(CCNC[C@@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
127045854 139021 0 None 13 6 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at PK-tagged beta2 receptor (unknown origin) transfected in HEK293 cells after 90 mins by beta-arrestin assayAgonist activity at PK-tagged beta2 receptor (unknown origin) transfected in HEK293 cells after 90 mins by beta-arrestin assay
ChEMBL 492 12 4 7 3.6 COc1cc(CCNC[C@@H](O)c2ccc(O)c3c2OCC(=O)N3)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
CHEMBL3797205 139021 0 None 13 6 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at PK-tagged beta2 receptor (unknown origin) transfected in HEK293 cells after 90 mins by beta-arrestin assayAgonist activity at PK-tagged beta2 receptor (unknown origin) transfected in HEK293 cells after 90 mins by beta-arrestin assay
ChEMBL 492 12 4 7 3.6 COc1cc(CCNC[C@@H](O)c2ccc(O)c3c2OCC(=O)N3)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
443372 10123 23 None -1 3 Human 8.2 pEC50 = 8.2 Binding
Agonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring Rluc2-117-GalphaS/GFP10-Ggamma/Gbeta1 assessed as activation of GalphaS incubated for 5 mins in presence of coelenterazine 400a by BRET assayAgonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring Rluc2-117-GalphaS/GFP10-Ggamma/Gbeta1 assessed as activation of GalphaS incubated for 5 mins in presence of coelenterazine 400a by BRET assay
ChEMBL 211 4 4 4 1.1 CC(C)NC[C@H](O)c1ccc(O)c(O)c1 10.1021/acs.jmedchem.9b00349
CHEMBL1160723 10123 23 None -1 3 Human 8.2 pEC50 = 8.2 Binding
Agonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring Rluc2-117-GalphaS/GFP10-Ggamma/Gbeta1 assessed as activation of GalphaS incubated for 5 mins in presence of coelenterazine 400a by BRET assayAgonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring Rluc2-117-GalphaS/GFP10-Ggamma/Gbeta1 assessed as activation of GalphaS incubated for 5 mins in presence of coelenterazine 400a by BRET assay
ChEMBL 211 4 4 4 1.1 CC(C)NC[C@H](O)c1ccc(O)c(O)c1 10.1021/acs.jmedchem.9b00349
CHEMBL2062275 10123 23 None -1 3 Human 8.2 pEC50 = 8.2 Binding
Agonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring Rluc2-117-GalphaS/GFP10-Ggamma/Gbeta1 assessed as activation of GalphaS incubated for 5 mins in presence of coelenterazine 400a by BRET assayAgonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring Rluc2-117-GalphaS/GFP10-Ggamma/Gbeta1 assessed as activation of GalphaS incubated for 5 mins in presence of coelenterazine 400a by BRET assay
ChEMBL 211 4 4 4 1.1 CC(C)NC[C@H](O)c1ccc(O)c(O)c1 10.1021/acs.jmedchem.9b00349
127045855 139121 0 None 1 6 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring Rluc2-117-GalphaS/GFP10-Ggamma/Gbeta1 assessed as activation of GalphaS incubated for 5 mins in presence of coelenterazine 400a by BRET assayAgonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring Rluc2-117-GalphaS/GFP10-Ggamma/Gbeta1 assessed as activation of GalphaS incubated for 5 mins in presence of coelenterazine 400a by BRET assay
ChEMBL 319 8 4 6 1.8 COc1ccccc1OCCNC[C@H](O)c1ccc(O)c(O)c1 10.1021/acs.jmedchem.9b00349
CHEMBL3797876 139121 0 None 1 6 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring Rluc2-117-GalphaS/GFP10-Ggamma/Gbeta1 assessed as activation of GalphaS incubated for 5 mins in presence of coelenterazine 400a by BRET assayAgonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring Rluc2-117-GalphaS/GFP10-Ggamma/Gbeta1 assessed as activation of GalphaS incubated for 5 mins in presence of coelenterazine 400a by BRET assay
ChEMBL 319 8 4 6 1.8 COc1ccccc1OCCNC[C@H](O)c1ccc(O)c(O)c1 10.1021/acs.jmedchem.9b00349
146025802 169000 0 None -1 2 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GSK5 and coelenterazine 400a by BRET assayAgonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GSK5 and coelenterazine 400a by BRET assay
ChEMBL 349 10 4 7 1.5 COc1ccccc1OCCNC[C@H](O)COc1ccc(O)c(O)c1 10.1021/acs.jmedchem.9b00349
CHEMBL4435895 169000 0 None -1 2 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GSK5 and coelenterazine 400a by BRET assayAgonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GSK5 and coelenterazine 400a by BRET assay
ChEMBL 349 10 4 7 1.5 COc1ccccc1OCCNC[C@H](O)COc1ccc(O)c(O)c1 10.1021/acs.jmedchem.9b00349
168294767 192407 0 None -1 20 Human 4.2 pEC50 = 4.2 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysis
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5207281 192407 0 None -1 20 Human 4.2 pEC50 = 4.2 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysis
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222802 192407 0 None -1 20 Human 4.2 pEC50 = 4.2 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysis
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
127046951 139359 0 None 11 6 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at PK-tagged beta2 receptor (unknown origin) transfected in HEK293 cells after 90 mins by beta-arrestin assayAgonist activity at PK-tagged beta2 receptor (unknown origin) transfected in HEK293 cells after 90 mins by beta-arrestin assay
ChEMBL 437 12 4 6 4.0 COc1cc(CCNC[C@@H](O)c2ccc(O)c(O)c2)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
CHEMBL3799427 139359 0 None 11 6 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at PK-tagged beta2 receptor (unknown origin) transfected in HEK293 cells after 90 mins by beta-arrestin assayAgonist activity at PK-tagged beta2 receptor (unknown origin) transfected in HEK293 cells after 90 mins by beta-arrestin assay
ChEMBL 437 12 4 6 4.0 COc1cc(CCNC[C@@H](O)c2ccc(O)c(O)c2)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
1499 2052 43 None -9 17 Guinea pig 8.1 pEC50 = 8.1 Binding
Agonist activity at beta2 adrenergic receptor in guinea pig tracheal smooth muscle assessed as inhibition of histamine-induced tracheal smooth muscle contraction by measuring spasmolysis preincubated for 15 mins in presence of beta adrenergic receptor antagonist propranolol followed by histamine additionAgonist activity at beta2 adrenergic receptor in guinea pig tracheal smooth muscle assessed as inhibition of histamine-induced tracheal smooth muscle contraction by measuring spasmolysis preincubated for 15 mins in presence of beta adrenergic receptor antagonist propranolol followed by histamine addition
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/acs.jnatprod.9b00418
3779 2052 43 None -9 17 Guinea pig 8.1 pEC50 = 8.1 Binding
Agonist activity at beta2 adrenergic receptor in guinea pig tracheal smooth muscle assessed as inhibition of histamine-induced tracheal smooth muscle contraction by measuring spasmolysis preincubated for 15 mins in presence of beta adrenergic receptor antagonist propranolol followed by histamine additionAgonist activity at beta2 adrenergic receptor in guinea pig tracheal smooth muscle assessed as inhibition of histamine-induced tracheal smooth muscle contraction by measuring spasmolysis preincubated for 15 mins in presence of beta adrenergic receptor antagonist propranolol followed by histamine addition
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/acs.jnatprod.9b00418
536 2052 43 None -9 17 Guinea pig 8.1 pEC50 = 8.1 Binding
Agonist activity at beta2 adrenergic receptor in guinea pig tracheal smooth muscle assessed as inhibition of histamine-induced tracheal smooth muscle contraction by measuring spasmolysis preincubated for 15 mins in presence of beta adrenergic receptor antagonist propranolol followed by histamine additionAgonist activity at beta2 adrenergic receptor in guinea pig tracheal smooth muscle assessed as inhibition of histamine-induced tracheal smooth muscle contraction by measuring spasmolysis preincubated for 15 mins in presence of beta adrenergic receptor antagonist propranolol followed by histamine addition
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/acs.jnatprod.9b00418
CHEMBL434 2052 43 None -9 17 Guinea pig 8.1 pEC50 = 8.1 Binding
Agonist activity at beta2 adrenergic receptor in guinea pig tracheal smooth muscle assessed as inhibition of histamine-induced tracheal smooth muscle contraction by measuring spasmolysis preincubated for 15 mins in presence of beta adrenergic receptor antagonist propranolol followed by histamine additionAgonist activity at beta2 adrenergic receptor in guinea pig tracheal smooth muscle assessed as inhibition of histamine-induced tracheal smooth muscle contraction by measuring spasmolysis preincubated for 15 mins in presence of beta adrenergic receptor antagonist propranolol followed by histamine addition
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/acs.jnatprod.9b00418
DB01064 2052 43 None -9 17 Guinea pig 8.1 pEC50 = 8.1 Binding
Agonist activity at beta2 adrenergic receptor in guinea pig tracheal smooth muscle assessed as inhibition of histamine-induced tracheal smooth muscle contraction by measuring spasmolysis preincubated for 15 mins in presence of beta adrenergic receptor antagonist propranolol followed by histamine additionAgonist activity at beta2 adrenergic receptor in guinea pig tracheal smooth muscle assessed as inhibition of histamine-induced tracheal smooth muscle contraction by measuring spasmolysis preincubated for 15 mins in presence of beta adrenergic receptor antagonist propranolol followed by histamine addition
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/acs.jnatprod.9b00418
127046950 139502 0 None 3 6 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of coelenterazine 400a by BRET assayAgonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of coelenterazine 400a by BRET assay
ChEMBL 437 12 4 6 4.0 COc1cc(CCNC[C@H](O)c2ccc(O)c(O)c2)ccc1OCCCc1ccccc1 10.1021/acs.jmedchem.9b00349
CHEMBL3800303 139502 0 None 3 6 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of coelenterazine 400a by BRET assayAgonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of coelenterazine 400a by BRET assay
ChEMBL 437 12 4 6 4.0 COc1cc(CCNC[C@H](O)c2ccc(O)c(O)c2)ccc1OCCCc1ccccc1 10.1021/acs.jmedchem.9b00349
146025802 169000 0 None -1 2 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GSK2 and coelenterazine 400a by BRET assayAgonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GSK2 and coelenterazine 400a by BRET assay
ChEMBL 349 10 4 7 1.5 COc1ccccc1OCCNC[C@H](O)COc1ccc(O)c(O)c1 10.1021/acs.jmedchem.9b00349
CHEMBL4435895 169000 0 None -1 2 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GSK2 and coelenterazine 400a by BRET assayAgonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GSK2 and coelenterazine 400a by BRET assay
ChEMBL 349 10 4 7 1.5 COc1ccccc1OCCNC[C@H](O)COc1ccc(O)c(O)c1 10.1021/acs.jmedchem.9b00349
44328703 10118 0 None 1 2 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring Rluc2-117-GalphaS/GFP10-Ggamma/Gbeta1 assessed as activation of GalphaS incubated for 5 mins in presence of coelenterazine 400a by BRET assayAgonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring Rluc2-117-GalphaS/GFP10-Ggamma/Gbeta1 assessed as activation of GalphaS incubated for 5 mins in presence of coelenterazine 400a by BRET assay
ChEMBL 241 6 4 5 0.8 CC(C)NC[C@H](O)COc1ccc(O)c(O)c1 10.1021/acs.jmedchem.9b00349
CHEMBL1160694 10118 0 None 1 2 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring Rluc2-117-GalphaS/GFP10-Ggamma/Gbeta1 assessed as activation of GalphaS incubated for 5 mins in presence of coelenterazine 400a by BRET assayAgonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring Rluc2-117-GalphaS/GFP10-Ggamma/Gbeta1 assessed as activation of GalphaS incubated for 5 mins in presence of coelenterazine 400a by BRET assay
ChEMBL 241 6 4 5 0.8 CC(C)NC[C@H](O)COc1ccc(O)c(O)c1 10.1021/acs.jmedchem.9b00349
162647610 179341 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at recombinant human beta2 adrenergic receptor expressed in CHO cells in presence of [3H](-)CGP12177Agonist activity at recombinant human beta2 adrenergic receptor expressed in CHO cells in presence of [3H](-)CGP12177
ChEMBL 849 14 7 10 7.1 COc1cccc(Nc2c(C(N)=O)ccc3c(C)cc(S(=O)(=O)c4cccc(C(=O)Nc5ccc(C#CCCCNC[C@@H](O)c6ccc(O)c7[nH]c(=O)ccc67)cc5)c4)cc23)c1 10.1021/acs.jmedchem.9b02170
CHEMBL4746212 179341 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at recombinant human beta2 adrenergic receptor expressed in CHO cells in presence of [3H](-)CGP12177Agonist activity at recombinant human beta2 adrenergic receptor expressed in CHO cells in presence of [3H](-)CGP12177
ChEMBL 849 14 7 10 7.1 COc1cccc(Nc2c(C(N)=O)ccc3c(C)cc(S(=O)(=O)c4cccc(C(=O)Nc5ccc(C#CCCCNC[C@@H](O)c6ccc(O)c7[nH]c(=O)ccc67)cc5)c4)cc23)c1 10.1021/acs.jmedchem.9b02170
177511 101059 20 None - 2 Guinea pig 6.1 pEC50 = 6.1 Binding
Agonist activity at beta2 adrenergic receptor in guinea pig tracheal smooth muscle assessed as inhibition of histamine-induced tracheal smooth muscle contraction by measuring spasmolysis preincubated for 15 mins in presence of beta adrenergic receptor antagonist propranolol followed by histamine additionAgonist activity at beta2 adrenergic receptor in guinea pig tracheal smooth muscle assessed as inhibition of histamine-induced tracheal smooth muscle contraction by measuring spasmolysis preincubated for 15 mins in presence of beta adrenergic receptor antagonist propranolol followed by histamine addition
ChEMBL 255 2 3 3 2.5 Oc1cc2c(cc1O)C(Cc1ccccc1)NCC2 10.1021/acs.jnatprod.9b00418
CHEMBL298285 101059 20 None - 2 Guinea pig 6.1 pEC50 = 6.1 Binding
Agonist activity at beta2 adrenergic receptor in guinea pig tracheal smooth muscle assessed as inhibition of histamine-induced tracheal smooth muscle contraction by measuring spasmolysis preincubated for 15 mins in presence of beta adrenergic receptor antagonist propranolol followed by histamine additionAgonist activity at beta2 adrenergic receptor in guinea pig tracheal smooth muscle assessed as inhibition of histamine-induced tracheal smooth muscle contraction by measuring spasmolysis preincubated for 15 mins in presence of beta adrenergic receptor antagonist propranolol followed by histamine addition
ChEMBL 255 2 3 3 2.5 Oc1cc2c(cc1O)C(Cc1ccccc1)NCC2 10.1021/acs.jnatprod.9b00418
68550025 110984 2 None - 1 Guinea pig 8.9 pED50 = 8.9 Binding
Agonist activity at beta-2 adrenergic receptor in guinea pig trachea assessed as relaxation of spontaneously contracted muscleAgonist activity at beta-2 adrenergic receptor in guinea pig trachea assessed as relaxation of spontaneously contracted muscle
ChEMBL 225 3 4 4 1.5 CC(C)(C)NC[C@H](O)c1ccc(O)c(O)c1 10.1021/jm00215a014
CHEMBL3247803 110984 2 None - 1 Guinea pig 8.9 pED50 = 8.9 Binding
Agonist activity at beta-2 adrenergic receptor in guinea pig trachea assessed as relaxation of spontaneously contracted muscleAgonist activity at beta-2 adrenergic receptor in guinea pig trachea assessed as relaxation of spontaneously contracted muscle
ChEMBL 225 3 4 4 1.5 CC(C)(C)NC[C@H](O)c1ccc(O)c(O)c1 10.1021/jm00215a014
CHEMBL3277145 110984 2 None - 1 Guinea pig 8.9 pED50 = 8.9 Binding
Agonist activity at beta-2 adrenergic receptor in guinea pig trachea assessed as relaxation of spontaneously contracted muscleAgonist activity at beta-2 adrenergic receptor in guinea pig trachea assessed as relaxation of spontaneously contracted muscle
ChEMBL 225 3 4 4 1.5 CC(C)(C)NC[C@H](O)c1ccc(O)c(O)c1 10.1021/jm00215a014
25104 10082 19 None 467 2 Guinea pig 8.9 pED50 = 8.9 Binding
Agonist activity at beta-2 adrenergic receptor in guinea pig tracheal chain assessed as relaxation of spontaneously contracted tracheal smooth muscleAgonist activity at beta-2 adrenergic receptor in guinea pig tracheal chain assessed as relaxation of spontaneously contracted tracheal smooth muscle
ChEMBL 225 3 4 4 1.5 CC(C)(C)NCC(O)c1ccc(O)c(O)c1 10.1021/jm00220a007
CHEMBL1159715 10082 19 None 467 2 Guinea pig 8.9 pED50 = 8.9 Binding
Agonist activity at beta-2 adrenergic receptor in guinea pig tracheal chain assessed as relaxation of spontaneously contracted tracheal smooth muscleAgonist activity at beta-2 adrenergic receptor in guinea pig tracheal chain assessed as relaxation of spontaneously contracted tracheal smooth muscle
ChEMBL 225 3 4 4 1.5 CC(C)(C)NCC(O)c1ccc(O)c(O)c1 10.1021/jm00220a007
21484489 112090 0 None - 0 Guinea pig 8.2 pED50 = 8.2 Binding
Agonist activity at beta-2 adrenergic receptor in guinea pig trachea assessed as relaxation of spontaneously contracted muscleAgonist activity at beta-2 adrenergic receptor in guinea pig trachea assessed as relaxation of spontaneously contracted muscle
ChEMBL 332 7 4 6 0.9 CC(C)(C)NCC(O)COc1ccc(O)c(NS(C)(=O)=O)c1 10.1021/jm00215a014
CHEMBL3247801 112090 0 None - 0 Guinea pig 8.2 pED50 = 8.2 Binding
Agonist activity at beta-2 adrenergic receptor in guinea pig trachea assessed as relaxation of spontaneously contracted muscleAgonist activity at beta-2 adrenergic receptor in guinea pig trachea assessed as relaxation of spontaneously contracted muscle
ChEMBL 332 7 4 6 0.9 CC(C)(C)NCC(O)COc1ccc(O)c(NS(C)(=O)=O)c1 10.1021/jm00215a014
CHEMBL3301974 112090 0 None - 0 Guinea pig 8.2 pED50 = 8.2 Binding
Agonist activity at beta-2 adrenergic receptor in guinea pig trachea assessed as relaxation of spontaneously contracted muscleAgonist activity at beta-2 adrenergic receptor in guinea pig trachea assessed as relaxation of spontaneously contracted muscle
ChEMBL 332 7 4 6 0.9 CC(C)(C)NCC(O)COc1ccc(O)c(NS(C)(=O)=O)c1 10.1021/jm00215a014
1499 2052 43 None -9 17 Guinea pig 8.2 pED50 = 8.2 Binding
Agonist activity at beta-2 adrenergic receptor in guinea pig trachea assessed as relaxation of spontaneously contracted muscleAgonist activity at beta-2 adrenergic receptor in guinea pig trachea assessed as relaxation of spontaneously contracted muscle
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm00215a014
3779 2052 43 None -9 17 Guinea pig 8.2 pED50 = 8.2 Binding
Agonist activity at beta-2 adrenergic receptor in guinea pig trachea assessed as relaxation of spontaneously contracted muscleAgonist activity at beta-2 adrenergic receptor in guinea pig trachea assessed as relaxation of spontaneously contracted muscle
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm00215a014
536 2052 43 None -9 17 Guinea pig 8.2 pED50 = 8.2 Binding
Agonist activity at beta-2 adrenergic receptor in guinea pig trachea assessed as relaxation of spontaneously contracted muscleAgonist activity at beta-2 adrenergic receptor in guinea pig trachea assessed as relaxation of spontaneously contracted muscle
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm00215a014
CHEMBL434 2052 43 None -9 17 Guinea pig 8.2 pED50 = 8.2 Binding
Agonist activity at beta-2 adrenergic receptor in guinea pig trachea assessed as relaxation of spontaneously contracted muscleAgonist activity at beta-2 adrenergic receptor in guinea pig trachea assessed as relaxation of spontaneously contracted muscle
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm00215a014
DB01064 2052 43 None -9 17 Guinea pig 8.2 pED50 = 8.2 Binding
Agonist activity at beta-2 adrenergic receptor in guinea pig trachea assessed as relaxation of spontaneously contracted muscleAgonist activity at beta-2 adrenergic receptor in guinea pig trachea assessed as relaxation of spontaneously contracted muscle
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm00215a014
1499 2052 43 None -9 17 Guinea pig 8.2 pED50 = 8.2 Binding
Agonist activity at beta-2 adrenergic receptor in guinea pig tracheal chain assessed as relaxation of spontaneously contracted tracheal smooth muscleAgonist activity at beta-2 adrenergic receptor in guinea pig tracheal chain assessed as relaxation of spontaneously contracted tracheal smooth muscle
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm00220a007
3779 2052 43 None -9 17 Guinea pig 8.2 pED50 = 8.2 Binding
Agonist activity at beta-2 adrenergic receptor in guinea pig tracheal chain assessed as relaxation of spontaneously contracted tracheal smooth muscleAgonist activity at beta-2 adrenergic receptor in guinea pig tracheal chain assessed as relaxation of spontaneously contracted tracheal smooth muscle
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm00220a007
536 2052 43 None -9 17 Guinea pig 8.2 pED50 = 8.2 Binding
Agonist activity at beta-2 adrenergic receptor in guinea pig tracheal chain assessed as relaxation of spontaneously contracted tracheal smooth muscleAgonist activity at beta-2 adrenergic receptor in guinea pig tracheal chain assessed as relaxation of spontaneously contracted tracheal smooth muscle
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm00220a007
CHEMBL434 2052 43 None -9 17 Guinea pig 8.2 pED50 = 8.2 Binding
Agonist activity at beta-2 adrenergic receptor in guinea pig tracheal chain assessed as relaxation of spontaneously contracted tracheal smooth muscleAgonist activity at beta-2 adrenergic receptor in guinea pig tracheal chain assessed as relaxation of spontaneously contracted tracheal smooth muscle
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm00220a007
DB01064 2052 43 None -9 17 Guinea pig 8.2 pED50 = 8.2 Binding
Agonist activity at beta-2 adrenergic receptor in guinea pig tracheal chain assessed as relaxation of spontaneously contracted tracheal smooth muscleAgonist activity at beta-2 adrenergic receptor in guinea pig tracheal chain assessed as relaxation of spontaneously contracted tracheal smooth muscle
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm00220a007
443372 10123 23 None -1 3 Human 10.3 pIC50 = 10.3 Binding
Mitogenesis inhibition method: To measure beta2-AR mediated inhibition of mitogenesis, HEK-beta2-AR, 1321N1 or U87MG cells were seeded in a 96-well plate at approximately 5,000 cells/well. After 48 hours, the wells were rinsed twice and the medium was replaced with fresh medium containing 10 uL of drug in sterile water. After another 24 hours of incubation at 37° C., 0.25 uCi of [3H]-thymidine was added to each well. The cells were incubated for an additional 2 hours at 37° C., at which point 10 uL of 10x trypsin was added, and the resuspended cells were harvested using a Tomtec 96 harvester through glass fiber filters.Mitogenesis inhibition method: To measure beta2-AR mediated inhibition of mitogenesis, HEK-beta2-AR, 1321N1 or U87MG cells were seeded in a 96-well plate at approximately 5,000 cells/well. After 48 hours, the wells were rinsed twice and the medium was replaced with fresh medium containing 10 uL of drug in sterile water. After another 24 hours of incubation at 37° C., 0.25 uCi of [3H]-thymidine was added to each well. The cells were incubated for an additional 2 hours at 37° C., at which point 10 uL of 10x trypsin was added, and the resuspended cells were harvested using a Tomtec 96 harvester through glass fiber filters.
ChEMBL 211 4 4 4 1.1 CC(C)NC[C@H](O)c1ccc(O)c(O)c1 nan
CHEMBL1160723 10123 23 None -1 3 Human 10.3 pIC50 = 10.3 Binding
Mitogenesis inhibition method: To measure beta2-AR mediated inhibition of mitogenesis, HEK-beta2-AR, 1321N1 or U87MG cells were seeded in a 96-well plate at approximately 5,000 cells/well. After 48 hours, the wells were rinsed twice and the medium was replaced with fresh medium containing 10 uL of drug in sterile water. After another 24 hours of incubation at 37° C., 0.25 uCi of [3H]-thymidine was added to each well. The cells were incubated for an additional 2 hours at 37° C., at which point 10 uL of 10x trypsin was added, and the resuspended cells were harvested using a Tomtec 96 harvester through glass fiber filters.Mitogenesis inhibition method: To measure beta2-AR mediated inhibition of mitogenesis, HEK-beta2-AR, 1321N1 or U87MG cells were seeded in a 96-well plate at approximately 5,000 cells/well. After 48 hours, the wells were rinsed twice and the medium was replaced with fresh medium containing 10 uL of drug in sterile water. After another 24 hours of incubation at 37° C., 0.25 uCi of [3H]-thymidine was added to each well. The cells were incubated for an additional 2 hours at 37° C., at which point 10 uL of 10x trypsin was added, and the resuspended cells were harvested using a Tomtec 96 harvester through glass fiber filters.
ChEMBL 211 4 4 4 1.1 CC(C)NC[C@H](O)c1ccc(O)c(O)c1 nan
CHEMBL2062275 10123 23 None -1 3 Human 10.3 pIC50 = 10.3 Binding
Mitogenesis inhibition method: To measure beta2-AR mediated inhibition of mitogenesis, HEK-beta2-AR, 1321N1 or U87MG cells were seeded in a 96-well plate at approximately 5,000 cells/well. After 48 hours, the wells were rinsed twice and the medium was replaced with fresh medium containing 10 uL of drug in sterile water. After another 24 hours of incubation at 37° C., 0.25 uCi of [3H]-thymidine was added to each well. The cells were incubated for an additional 2 hours at 37° C., at which point 10 uL of 10x trypsin was added, and the resuspended cells were harvested using a Tomtec 96 harvester through glass fiber filters.Mitogenesis inhibition method: To measure beta2-AR mediated inhibition of mitogenesis, HEK-beta2-AR, 1321N1 or U87MG cells were seeded in a 96-well plate at approximately 5,000 cells/well. After 48 hours, the wells were rinsed twice and the medium was replaced with fresh medium containing 10 uL of drug in sterile water. After another 24 hours of incubation at 37° C., 0.25 uCi of [3H]-thymidine was added to each well. The cells were incubated for an additional 2 hours at 37° C., at which point 10 uL of 10x trypsin was added, and the resuspended cells were harvested using a Tomtec 96 harvester through glass fiber filters.
ChEMBL 211 4 4 4 1.1 CC(C)NC[C@H](O)c1ccc(O)c(O)c1 nan
688468 141788 7 None 190 2 Human 9.9 pIC50 = 9.9 Binding
Mitogenesis inhibition method: To measure beta2-AR mediated inhibition of mitogenesis, HEK-beta2-AR, 1321N1 or U87MG cells were seeded in a 96-well plate at approximately 5,000 cells/well. After 48 hours, the wells were rinsed twice and the medium was replaced with fresh medium containing 10 uL of drug in sterile water. After another 24 hours of incubation at 37° C., 0.25 uCi of [3H]-thymidine was added to each well. The cells were incubated for an additional 2 hours at 37° C., at which point 10 uL of 10x trypsin was added, and the resuspended cells were harvested using a Tomtec 96 harvester through glass fiber filters.Mitogenesis inhibition method: To measure beta2-AR mediated inhibition of mitogenesis, HEK-beta2-AR, 1321N1 or U87MG cells were seeded in a 96-well plate at approximately 5,000 cells/well. After 48 hours, the wells were rinsed twice and the medium was replaced with fresh medium containing 10 uL of drug in sterile water. After another 24 hours of incubation at 37° C., 0.25 uCi of [3H]-thymidine was added to each well. The cells were incubated for an additional 2 hours at 37° C., at which point 10 uL of 10x trypsin was added, and the resuspended cells were harvested using a Tomtec 96 harvester through glass fiber filters.
ChEMBL 303 6 5 5 2.1 C[C@H](Cc1ccc(O)cc1)NC[C@H](O)c1cc(O)cc(O)c1 nan
CHEMBL388570 141788 7 None 190 2 Human 9.9 pIC50 = 9.9 Binding
Mitogenesis inhibition method: To measure beta2-AR mediated inhibition of mitogenesis, HEK-beta2-AR, 1321N1 or U87MG cells were seeded in a 96-well plate at approximately 5,000 cells/well. After 48 hours, the wells were rinsed twice and the medium was replaced with fresh medium containing 10 uL of drug in sterile water. After another 24 hours of incubation at 37° C., 0.25 uCi of [3H]-thymidine was added to each well. The cells were incubated for an additional 2 hours at 37° C., at which point 10 uL of 10x trypsin was added, and the resuspended cells were harvested using a Tomtec 96 harvester through glass fiber filters.Mitogenesis inhibition method: To measure beta2-AR mediated inhibition of mitogenesis, HEK-beta2-AR, 1321N1 or U87MG cells were seeded in a 96-well plate at approximately 5,000 cells/well. After 48 hours, the wells were rinsed twice and the medium was replaced with fresh medium containing 10 uL of drug in sterile water. After another 24 hours of incubation at 37° C., 0.25 uCi of [3H]-thymidine was added to each well. The cells were incubated for an additional 2 hours at 37° C., at which point 10 uL of 10x trypsin was added, and the resuspended cells were harvested using a Tomtec 96 harvester through glass fiber filters.
ChEMBL 303 6 5 5 2.1 C[C@H](Cc1ccc(O)cc1)NC[C@H](O)c1cc(O)cc(O)c1 nan
16735257 85290 0 None 151 2 Human 9.8 pIC50 = 9.8 Binding
Mitogenesis inhibition method: To measure beta2-AR mediated inhibition of mitogenesis, HEK-beta2-AR, 1321N1 or U87MG cells were seeded in a 96-well plate at approximately 5,000 cells/well. After 48 hours, the wells were rinsed twice and the medium was replaced with fresh medium containing 10 uL of drug in sterile water. After another 24 hours of incubation at 37° C., 0.25 uCi of [3H]-thymidine was added to each well. The cells were incubated for an additional 2 hours at 37° C., at which point 10 uL of 10x trypsin was added, and the resuspended cells were harvested using a Tomtec 96 harvester through glass fiber filters.Mitogenesis inhibition method: To measure beta2-AR mediated inhibition of mitogenesis, HEK-beta2-AR, 1321N1 or U87MG cells were seeded in a 96-well plate at approximately 5,000 cells/well. After 48 hours, the wells were rinsed twice and the medium was replaced with fresh medium containing 10 uL of drug in sterile water. After another 24 hours of incubation at 37° C., 0.25 uCi of [3H]-thymidine was added to each well. The cells were incubated for an additional 2 hours at 37° C., at which point 10 uL of 10x trypsin was added, and the resuspended cells were harvested using a Tomtec 96 harvester through glass fiber filters.
ChEMBL 317 7 4 5 2.4 COc1ccc(C[C@@H](C)NC[C@H](O)c2cc(O)cc(O)c2)cc1 nan
CHEMBL228992 85290 0 None 151 2 Human 9.8 pIC50 = 9.8 Binding
Mitogenesis inhibition method: To measure beta2-AR mediated inhibition of mitogenesis, HEK-beta2-AR, 1321N1 or U87MG cells were seeded in a 96-well plate at approximately 5,000 cells/well. After 48 hours, the wells were rinsed twice and the medium was replaced with fresh medium containing 10 uL of drug in sterile water. After another 24 hours of incubation at 37° C., 0.25 uCi of [3H]-thymidine was added to each well. The cells were incubated for an additional 2 hours at 37° C., at which point 10 uL of 10x trypsin was added, and the resuspended cells were harvested using a Tomtec 96 harvester through glass fiber filters.Mitogenesis inhibition method: To measure beta2-AR mediated inhibition of mitogenesis, HEK-beta2-AR, 1321N1 or U87MG cells were seeded in a 96-well plate at approximately 5,000 cells/well. After 48 hours, the wells were rinsed twice and the medium was replaced with fresh medium containing 10 uL of drug in sterile water. After another 24 hours of incubation at 37° C., 0.25 uCi of [3H]-thymidine was added to each well. The cells were incubated for an additional 2 hours at 37° C., at which point 10 uL of 10x trypsin was added, and the resuspended cells were harvested using a Tomtec 96 harvester through glass fiber filters.
ChEMBL 317 7 4 5 2.4 COc1ccc(C[C@@H](C)NC[C@H](O)c2cc(O)cc(O)c2)cc1 nan
57398562 70002 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 477 11 5 6 4.1 CC(CNCc1ccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)cc1)c1ccccc1 10.1016/j.bmcl.2011.10.049
CHEMBL1945036 70002 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 477 11 5 6 4.1 CC(CNCc1ccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)cc1)c1ccccc1 10.1016/j.bmcl.2011.10.049
24901141 70180 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 531 11 5 6 4.8 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3cccc(CNCCc4c(Cl)cccc4Cl)c3)c2s1 10.1016/j.bmcl.2011.10.049
CHEMBL1947157 70180 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 531 11 5 6 4.8 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3cccc(CNCCc4c(Cl)cccc4Cl)c3)c2s1 10.1016/j.bmcl.2011.10.049
2585 788 100 None 1 22 Human 9.6 pIC50 = 9.6 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
522 788 100 None 1 22 Human 9.6 pIC50 = 9.6 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
551 788 100 None 1 22 Human 9.6 pIC50 = 9.6 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
CHEMBL723 788 100 None 1 22 Human 9.6 pIC50 = 9.6 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
DB01136 788 100 None 1 22 Human 9.6 pIC50 = 9.6 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
33624 3749 29 None 1 9 Human 9.5 pIC50 = 9.5 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C nan
4061 3749 29 None 1 9 Human 9.5 pIC50 = 9.5 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C nan
565 3749 29 None 1 9 Human 9.5 pIC50 = 9.5 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C nan
CHEMBL499 3749 29 None 1 9 Human 9.5 pIC50 = 9.5 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C nan
DB00373 3749 29 None 1 9 Human 9.5 pIC50 = 9.5 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C nan
49864396 15448 0 None - 3 Guinea pig 9.5 pIC50 = 9.5 Binding
Agonist activity at adrenergic beta2 receptor in electrically-stimulated Dunkin-Hartley guinea pig tracheal strip assessed as inhibition of contractionAgonist activity at adrenergic beta2 receptor in electrically-stimulated Dunkin-Hartley guinea pig tracheal strip assessed as inhibition of contraction
ChEMBL 362 5 4 5 3.3 O=c1[nH]c2c(O)ccc([C@@H](O)CN[C@@H]3CCC[C@@H]3C3CCCC3)c2s1 10.1016/j.bmcl.2014.06.014
CHEMBL1221682 15448 0 None - 3 Guinea pig 9.5 pIC50 = 9.5 Binding
Agonist activity at adrenergic beta2 receptor in electrically-stimulated Dunkin-Hartley guinea pig tracheal strip assessed as inhibition of contractionAgonist activity at adrenergic beta2 receptor in electrically-stimulated Dunkin-Hartley guinea pig tracheal strip assessed as inhibition of contraction
ChEMBL 362 5 4 5 3.3 O=c1[nH]c2c(O)ccc([C@@H](O)CN[C@@H]3CCC[C@@H]3C3CCCC3)c2s1 10.1016/j.bmcl.2014.06.014
165193 3126 60 None 1 43 Human 9.5 pIC50 = 9.5 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
2303 3126 60 None 1 43 Human 9.5 pIC50 = 9.5 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
4946 3126 60 None 1 43 Human 9.5 pIC50 = 9.5 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
564 3126 60 None 1 43 Human 9.5 pIC50 = 9.5 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
62882 3126 60 None 1 43 Human 9.5 pIC50 = 9.5 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
63 3126 60 None 1 43 Human 9.5 pIC50 = 9.5 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
66366 3126 60 None 1 43 Human 9.5 pIC50 = 9.5 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
91536 3126 60 None 1 43 Human 9.5 pIC50 = 9.5 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
CHEMBL27 3126 60 None 1 43 Human 9.5 pIC50 = 9.5 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
CHEMBL452861 3126 60 None 1 43 Human 9.5 pIC50 = 9.5 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
DB00571 3126 60 None 1 43 Human 9.5 pIC50 = 9.5 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
54673702 149087 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 μg/well for beta1 and 5 μg/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 μl, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 μM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 μg/well for beta1 and 5 μg/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 μl, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 μM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.
ChEMBL 814 15 6 14 5.6 COc1cc(NC(=O)OCCN(C)[C@H]2CC[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2c1OCC(=O)N2 nan
CHEMBL3947244 149087 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 μg/well for beta1 and 5 μg/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 μl, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 μM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 μg/well for beta1 and 5 μg/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 μl, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 μM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.
ChEMBL 814 15 6 14 5.6 COc1cc(NC(=O)OCCN(C)[C@H]2CC[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2c1OCC(=O)N2 nan
1239 1639 46 None - 4 Guinea pig 9.4 pIC50 = 9.4 Binding
Agonist activity at adrenergic beta2 receptor in electrically-stimulated Dunkin-Hartley guinea pig tracheal strip assessed as inhibition of contractionAgonist activity at adrenergic beta2 receptor in electrically-stimulated Dunkin-Hartley guinea pig tracheal strip assessed as inhibition of contraction
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.06.014
3410 1639 46 None - 4 Guinea pig 9.4 pIC50 = 9.4 Binding
Agonist activity at adrenergic beta2 receptor in electrically-stimulated Dunkin-Hartley guinea pig tracheal strip assessed as inhibition of contractionAgonist activity at adrenergic beta2 receptor in electrically-stimulated Dunkin-Hartley guinea pig tracheal strip assessed as inhibition of contraction
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.06.014
3465 1639 46 None - 4 Guinea pig 9.4 pIC50 = 9.4 Binding
Agonist activity at adrenergic beta2 receptor in electrically-stimulated Dunkin-Hartley guinea pig tracheal strip assessed as inhibition of contractionAgonist activity at adrenergic beta2 receptor in electrically-stimulated Dunkin-Hartley guinea pig tracheal strip assessed as inhibition of contraction
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.06.014
CHEMBL1256786 1639 46 None - 4 Guinea pig 9.4 pIC50 = 9.4 Binding
Agonist activity at adrenergic beta2 receptor in electrically-stimulated Dunkin-Hartley guinea pig tracheal strip assessed as inhibition of contractionAgonist activity at adrenergic beta2 receptor in electrically-stimulated Dunkin-Hartley guinea pig tracheal strip assessed as inhibition of contraction
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.06.014
DB00983 1639 46 None - 4 Guinea pig 9.4 pIC50 = 9.4 Binding
Agonist activity at adrenergic beta2 receptor in electrically-stimulated Dunkin-Hartley guinea pig tracheal strip assessed as inhibition of contractionAgonist activity at adrenergic beta2 receptor in electrically-stimulated Dunkin-Hartley guinea pig tracheal strip assessed as inhibition of contraction
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.06.014
3682 188837 7 None 1 8 Human 9.3 pIC50 = 9.3 Binding
Binding affinity to human adrenergic beta2 receptor by radioligand displacement assayBinding affinity to human adrenergic beta2 receptor by radioligand displacement assay
ChEMBL 277 6 2 3 2.6 Cc1ccc(OCC(O)C(C)NC(C)C)c2c1CCC2 10.1016/j.ejmech.2013.01.044
CHEMBL1256784 188837 7 None 1 8 Human 9.3 pIC50 = 9.3 Binding
Binding affinity to human adrenergic beta2 receptor by radioligand displacement assayBinding affinity to human adrenergic beta2 receptor by radioligand displacement assay
ChEMBL 277 6 2 3 2.6 Cc1ccc(OCC(O)C(C)NC(C)C)c2c1CCC2 10.1016/j.ejmech.2013.01.044
CHEMBL513389 188837 7 None 1 8 Human 9.3 pIC50 = 9.3 Binding
Binding affinity to human adrenergic beta2 receptor by radioligand displacement assayBinding affinity to human adrenergic beta2 receptor by radioligand displacement assay
ChEMBL 277 6 2 3 2.6 Cc1ccc(OCC(O)C(C)NC(C)C)c2c1CCC2 10.1016/j.ejmech.2013.01.044
24901144 69971 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 481 11 5 6 3.6 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3cccc(CNCCc4ccccc4F)c3)c2s1 10.1016/j.bmcl.2011.10.049
CHEMBL1944691 69971 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 481 11 5 6 3.6 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3cccc(CNCCc4ccccc4F)c3)c2s1 10.1016/j.bmcl.2011.10.049
24900872 70004 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 478 12 5 7 3.3 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3cccc(CNCCCc4ccccn4)c3)c2s1 10.1016/j.bmcl.2011.10.049
CHEMBL1945038 70004 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 478 12 5 7 3.3 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3cccc(CNCCCc4ccccn4)c3)c2s1 10.1016/j.bmcl.2011.10.049
2176 3065 66 None -2 27 Human 9.3 pIC50 = 9.3 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C nan
4828 3065 66 None -2 27 Human 9.3 pIC50 = 9.3 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C nan
91 3065 66 None -2 27 Human 9.3 pIC50 = 9.3 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C nan
CHEMBL500 3065 66 None -2 27 Human 9.3 pIC50 = 9.3 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C nan
DB00960 3065 66 None -2 27 Human 9.3 pIC50 = 9.3 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C nan
24901210 69970 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 497 11 5 6 4.1 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3cccc(CNCCc4ccccc4Cl)c3)c2s1 10.1016/j.bmcl.2011.10.049
CHEMBL1944690 69970 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 497 11 5 6 4.1 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3cccc(CNCCc4ccccc4Cl)c3)c2s1 10.1016/j.bmcl.2011.10.049
24901209 69997 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 516 11 6 6 4.3 Cc1cccc2c(CCNCc3cccc(CCNC[C@H](O)c4ccc(O)c5[nH]c(=O)sc45)c3)c[nH]c12 10.1016/j.bmcl.2011.10.049
CHEMBL1945031 69997 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 516 11 6 6 4.3 Cc1cccc2c(CCNCc3cccc(CCNC[C@H](O)c4ccc(O)c5[nH]c(=O)sc45)c3)c[nH]c12 10.1016/j.bmcl.2011.10.049
57400446 70144 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 515 11 4 5 5.3 O=c1[nH]c2c(O)ccc(CCNCCc3cccc(CNCCc4c(Cl)cccc4Cl)c3)c2s1 10.1016/j.bmcl.2011.10.049
CHEMBL1946768 70144 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 515 11 4 5 5.3 O=c1[nH]c2c(O)ccc(CCNCCc3cccc(CNCCc4c(Cl)cccc4Cl)c3)c2s1 10.1016/j.bmcl.2011.10.049
3682 188837 7 None 1 8 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H](-)CGP12177 from human recombinant Beta-2 adrenergic receptor expressed in CHO cellsDisplacement of [3H](-)CGP12177 from human recombinant Beta-2 adrenergic receptor expressed in CHO cells
ChEMBL 277 6 2 3 2.6 Cc1ccc(OCC(O)C(C)NC(C)C)c2c1CCC2 10.1016/j.bmc.2016.03.006
CHEMBL1256784 188837 7 None 1 8 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H](-)CGP12177 from human recombinant Beta-2 adrenergic receptor expressed in CHO cellsDisplacement of [3H](-)CGP12177 from human recombinant Beta-2 adrenergic receptor expressed in CHO cells
ChEMBL 277 6 2 3 2.6 Cc1ccc(OCC(O)C(C)NC(C)C)c2c1CCC2 10.1016/j.bmc.2016.03.006
CHEMBL513389 188837 7 None 1 8 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H](-)CGP12177 from human recombinant Beta-2 adrenergic receptor expressed in CHO cellsDisplacement of [3H](-)CGP12177 from human recombinant Beta-2 adrenergic receptor expressed in CHO cells
ChEMBL 277 6 2 3 2.6 Cc1ccc(OCC(O)C(C)NC(C)C)c2c1CCC2 10.1016/j.bmc.2016.03.006
5311179 1935 18 None 85 3 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]CGP 12177 from human recombinant beta2 adrenergic receptor expressed in CHO cells measured after 120 mins by scintillation counting methodDisplacement of [3H]CGP 12177 from human recombinant beta2 adrenergic receptor expressed in CHO cells measured after 120 mins by scintillation counting method
ChEMBL 277 6 2 3 2.6 Cc1c2CCCc2c(cc1)OC[C@H]([C@H](C)NC(C)C)O 10.1016/j.bmc.2016.11.014
543 1935 18 None 85 3 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]CGP 12177 from human recombinant beta2 adrenergic receptor expressed in CHO cells measured after 120 mins by scintillation counting methodDisplacement of [3H]CGP 12177 from human recombinant beta2 adrenergic receptor expressed in CHO cells measured after 120 mins by scintillation counting method
ChEMBL 277 6 2 3 2.6 Cc1c2CCCc2c(cc1)OC[C@H]([C@H](C)NC(C)C)O 10.1016/j.bmc.2016.11.014
5484725 1935 18 None 85 3 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]CGP 12177 from human recombinant beta2 adrenergic receptor expressed in CHO cells measured after 120 mins by scintillation counting methodDisplacement of [3H]CGP 12177 from human recombinant beta2 adrenergic receptor expressed in CHO cells measured after 120 mins by scintillation counting method
ChEMBL 277 6 2 3 2.6 Cc1c2CCCc2c(cc1)OC[C@H]([C@H](C)NC(C)C)O 10.1016/j.bmc.2016.11.014
CHEMBL1233766 1935 18 None 85 3 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]CGP 12177 from human recombinant beta2 adrenergic receptor expressed in CHO cells measured after 120 mins by scintillation counting methodDisplacement of [3H]CGP 12177 from human recombinant beta2 adrenergic receptor expressed in CHO cells measured after 120 mins by scintillation counting method
ChEMBL 277 6 2 3 2.6 Cc1c2CCCc2c(cc1)OC[C@H]([C@H](C)NC(C)C)O 10.1016/j.bmc.2016.11.014
CHEMBL198059 1935 18 None 85 3 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]CGP 12177 from human recombinant beta2 adrenergic receptor expressed in CHO cells measured after 120 mins by scintillation counting methodDisplacement of [3H]CGP 12177 from human recombinant beta2 adrenergic receptor expressed in CHO cells measured after 120 mins by scintillation counting method
ChEMBL 277 6 2 3 2.6 Cc1c2CCCc2c(cc1)OC[C@H]([C@H](C)NC(C)C)O 10.1016/j.bmc.2016.11.014
165193 3126 60 None 1 43 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]CGP12177 from human recombinant beta2 adrenergic receptor expressed in CHO cells after 60 minsDisplacement of [3H]CGP12177 from human recombinant beta2 adrenergic receptor expressed in CHO cells after 60 mins
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmcl.2013.01.025
2303 3126 60 None 1 43 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]CGP12177 from human recombinant beta2 adrenergic receptor expressed in CHO cells after 60 minsDisplacement of [3H]CGP12177 from human recombinant beta2 adrenergic receptor expressed in CHO cells after 60 mins
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmcl.2013.01.025
4946 3126 60 None 1 43 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]CGP12177 from human recombinant beta2 adrenergic receptor expressed in CHO cells after 60 minsDisplacement of [3H]CGP12177 from human recombinant beta2 adrenergic receptor expressed in CHO cells after 60 mins
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmcl.2013.01.025
564 3126 60 None 1 43 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]CGP12177 from human recombinant beta2 adrenergic receptor expressed in CHO cells after 60 minsDisplacement of [3H]CGP12177 from human recombinant beta2 adrenergic receptor expressed in CHO cells after 60 mins
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmcl.2013.01.025
62882 3126 60 None 1 43 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]CGP12177 from human recombinant beta2 adrenergic receptor expressed in CHO cells after 60 minsDisplacement of [3H]CGP12177 from human recombinant beta2 adrenergic receptor expressed in CHO cells after 60 mins
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmcl.2013.01.025
63 3126 60 None 1 43 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]CGP12177 from human recombinant beta2 adrenergic receptor expressed in CHO cells after 60 minsDisplacement of [3H]CGP12177 from human recombinant beta2 adrenergic receptor expressed in CHO cells after 60 mins
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmcl.2013.01.025
66366 3126 60 None 1 43 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]CGP12177 from human recombinant beta2 adrenergic receptor expressed in CHO cells after 60 minsDisplacement of [3H]CGP12177 from human recombinant beta2 adrenergic receptor expressed in CHO cells after 60 mins
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmcl.2013.01.025
91536 3126 60 None 1 43 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]CGP12177 from human recombinant beta2 adrenergic receptor expressed in CHO cells after 60 minsDisplacement of [3H]CGP12177 from human recombinant beta2 adrenergic receptor expressed in CHO cells after 60 mins
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmcl.2013.01.025
CHEMBL27 3126 60 None 1 43 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]CGP12177 from human recombinant beta2 adrenergic receptor expressed in CHO cells after 60 minsDisplacement of [3H]CGP12177 from human recombinant beta2 adrenergic receptor expressed in CHO cells after 60 mins
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmcl.2013.01.025
CHEMBL452861 3126 60 None 1 43 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]CGP12177 from human recombinant beta2 adrenergic receptor expressed in CHO cells after 60 minsDisplacement of [3H]CGP12177 from human recombinant beta2 adrenergic receptor expressed in CHO cells after 60 mins
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmcl.2013.01.025
DB00571 3126 60 None 1 43 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]CGP12177 from human recombinant beta2 adrenergic receptor expressed in CHO cells after 60 minsDisplacement of [3H]CGP12177 from human recombinant beta2 adrenergic receptor expressed in CHO cells after 60 mins
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmcl.2013.01.025
39468 2270 33 None 3 7 Human 9.1 pIC50 = 9.1 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 291 5 2 4 2.3 O[C@H](COc1cccc2c1CCCC2=O)CNC(C)(C)C nan
431 2270 33 None 3 7 Human 9.1 pIC50 = 9.1 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 291 5 2 4 2.3 O[C@H](COc1cccc2c1CCCC2=O)CNC(C)(C)C nan
570 2270 33 None 3 7 Human 9.1 pIC50 = 9.1 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 291 5 2 4 2.3 O[C@H](COc1cccc2c1CCCC2=O)CNC(C)(C)C nan
CHEMBL1201237 2270 33 None 3 7 Human 9.1 pIC50 = 9.1 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 291 5 2 4 2.3 O[C@H](COc1cccc2c1CCCC2=O)CNC(C)(C)C nan
DB01210 2270 33 None 3 7 Human 9.1 pIC50 = 9.1 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 291 5 2 4 2.3 O[C@H](COc1cccc2c1CCCC2=O)CNC(C)(C)C nan
24901211 69973 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 493 12 5 7 3.5 COc1ccccc1CCNCc1cccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)c1 10.1016/j.bmcl.2011.10.049
CHEMBL1944693 69973 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 493 12 5 7 3.5 COc1ccccc1CCNCc1cccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)c1 10.1016/j.bmcl.2011.10.049
24900426 70003 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 477 12 5 6 3.9 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3cccc(CNCCCc4ccccc4)c3)c2s1 10.1016/j.bmcl.2011.10.049
CHEMBL1945037 70003 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 477 12 5 6 3.9 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3cccc(CNCCCc4ccccc4)c3)c2s1 10.1016/j.bmcl.2011.10.049
57393349 70174 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 523 11 4 5 6.2 C[C@@H](NCc1ccccc1-c1ccc(CCNCCc2ccc(O)c3[nH]c(=O)sc23)cc1)c1ccccc1 10.1016/j.bmcl.2011.10.049
CHEMBL1947151 70174 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 523 11 4 5 6.2 C[C@@H](NCc1ccccc1-c1ccc(CCNCCc2ccc(O)c3[nH]c(=O)sc23)cc1)c1ccccc1 10.1016/j.bmcl.2011.10.049
44186438 185754 0 None - 0 Human 9.0 pIC50 = 9 Binding
Binding affinity to beta2 adrenoceptorBinding affinity to beta2 adrenoceptor
ChEMBL 397 9 2 4 4.4 COc1ccc(CC(C)(C)NC[C@H](O)COc2cccc(Cl)c2Cl)cc1 10.1021/jm900364m
CHEMBL487508 185754 0 None - 0 Human 9.0 pIC50 = 9 Binding
Binding affinity to beta2 adrenoceptorBinding affinity to beta2 adrenoceptor
ChEMBL 397 9 2 4 4.4 COc1ccc(CC(C)(C)NC[C@H](O)COc2cccc(Cl)c2Cl)cc1 10.1021/jm900364m
24900813 70008 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 467 10 5 6 3.6 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3cccc(CNCc4ccccc4F)c3)c2s1 10.1016/j.bmcl.2011.10.049
CHEMBL1945042 70008 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 467 10 5 6 3.6 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3cccc(CNCc4ccccc4F)c3)c2s1 10.1016/j.bmcl.2011.10.049
71278078 143945 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 μg/well for beta1 and 5 μg/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 μl, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 μM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 μg/well for beta1 and 5 μg/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 μl, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 μM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.
ChEMBL 796 15 6 12 6.2 COc1cc(NC(=O)OCCN(C)[C@H]2CC[C@H](OC(=O)[C@](O)(c3cccs3)C3CCCC3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3906808 143945 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 μg/well for beta1 and 5 μg/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 μl, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 μM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 μg/well for beta1 and 5 μg/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 μl, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 μM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.
ChEMBL 796 15 6 12 6.2 COc1cc(NC(=O)OCCN(C)[C@H]2CC[C@H](OC(=O)[C@](O)(c3cccs3)C3CCCC3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
165193 3126 60 None 1 43 Human 9.0 pIC50 = 9.0 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
2303 3126 60 None 1 43 Human 9.0 pIC50 = 9.0 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
4946 3126 60 None 1 43 Human 9.0 pIC50 = 9.0 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
564 3126 60 None 1 43 Human 9.0 pIC50 = 9.0 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
62882 3126 60 None 1 43 Human 9.0 pIC50 = 9.0 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
63 3126 60 None 1 43 Human 9.0 pIC50 = 9.0 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
66366 3126 60 None 1 43 Human 9.0 pIC50 = 9.0 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
91536 3126 60 None 1 43 Human 9.0 pIC50 = 9.0 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
CHEMBL27 3126 60 None 1 43 Human 9.0 pIC50 = 9.0 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
CHEMBL452861 3126 60 None 1 43 Human 9.0 pIC50 = 9.0 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
DB00571 3126 60 None 1 43 Human 9.0 pIC50 = 9.0 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
16735272 85371 0 None 46 2 Human 8.9 pIC50 = 8.9 Binding
Mitogenesis inhibition method: To measure beta2-AR mediated inhibition of mitogenesis, HEK-beta2-AR, 1321N1 or U87MG cells were seeded in a 96-well plate at approximately 5,000 cells/well. After 48 hours, the wells were rinsed twice and the medium was replaced with fresh medium containing 10 uL of drug in sterile water. After another 24 hours of incubation at 37° C., 0.25 uCi of [3H]-thymidine was added to each well. The cells were incubated for an additional 2 hours at 37° C., at which point 10 uL of 10x trypsin was added, and the resuspended cells were harvested using a Tomtec 96 harvester through glass fiber filters.Mitogenesis inhibition method: To measure beta2-AR mediated inhibition of mitogenesis, HEK-beta2-AR, 1321N1 or U87MG cells were seeded in a 96-well plate at approximately 5,000 cells/well. After 48 hours, the wells were rinsed twice and the medium was replaced with fresh medium containing 10 uL of drug in sterile water. After another 24 hours of incubation at 37° C., 0.25 uCi of [3H]-thymidine was added to each well. The cells were incubated for an additional 2 hours at 37° C., at which point 10 uL of 10x trypsin was added, and the resuspended cells were harvested using a Tomtec 96 harvester through glass fiber filters.
ChEMBL 337 6 4 4 3.5 C[C@@H](Cc1cccc2ccccc12)NC[C@H](O)c1cc(O)cc(O)c1 nan
CHEMBL229614 85371 0 None 46 2 Human 8.9 pIC50 = 8.9 Binding
Mitogenesis inhibition method: To measure beta2-AR mediated inhibition of mitogenesis, HEK-beta2-AR, 1321N1 or U87MG cells were seeded in a 96-well plate at approximately 5,000 cells/well. After 48 hours, the wells were rinsed twice and the medium was replaced with fresh medium containing 10 uL of drug in sterile water. After another 24 hours of incubation at 37° C., 0.25 uCi of [3H]-thymidine was added to each well. The cells were incubated for an additional 2 hours at 37° C., at which point 10 uL of 10x trypsin was added, and the resuspended cells were harvested using a Tomtec 96 harvester through glass fiber filters.Mitogenesis inhibition method: To measure beta2-AR mediated inhibition of mitogenesis, HEK-beta2-AR, 1321N1 or U87MG cells were seeded in a 96-well plate at approximately 5,000 cells/well. After 48 hours, the wells were rinsed twice and the medium was replaced with fresh medium containing 10 uL of drug in sterile water. After another 24 hours of incubation at 37° C., 0.25 uCi of [3H]-thymidine was added to each well. The cells were incubated for an additional 2 hours at 37° C., at which point 10 uL of 10x trypsin was added, and the resuspended cells were harvested using a Tomtec 96 harvester through glass fiber filters.
ChEMBL 337 6 4 4 3.5 C[C@@H](Cc1cccc2ccccc12)NC[C@H](O)c1cc(O)cc(O)c1 nan
3682 188837 7 None 1 8 Human 8.9 pIC50 = 8.9 Binding
Displacement of radiolabeled ICI 118551 from human adrenergic beta2 receptorDisplacement of radiolabeled ICI 118551 from human adrenergic beta2 receptor
ChEMBL 277 6 2 3 2.6 Cc1ccc(OCC(O)C(C)NC(C)C)c2c1CCC2 10.1021/jm8007618
CHEMBL1256784 188837 7 None 1 8 Human 8.9 pIC50 = 8.9 Binding
Displacement of radiolabeled ICI 118551 from human adrenergic beta2 receptorDisplacement of radiolabeled ICI 118551 from human adrenergic beta2 receptor
ChEMBL 277 6 2 3 2.6 Cc1ccc(OCC(O)C(C)NC(C)C)c2c1CCC2 10.1021/jm8007618
CHEMBL513389 188837 7 None 1 8 Human 8.9 pIC50 = 8.9 Binding
Displacement of radiolabeled ICI 118551 from human adrenergic beta2 receptorDisplacement of radiolabeled ICI 118551 from human adrenergic beta2 receptor
ChEMBL 277 6 2 3 2.6 Cc1ccc(OCC(O)C(C)NC(C)C)c2c1CCC2 10.1021/jm8007618
54673528 152212 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 μg/well for beta1 and 5 μg/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 μl, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 μM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 μg/well for beta1 and 5 μg/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 μl, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 μM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.
ChEMBL 790 15 6 11 6.1 COc1cc(NC(=O)OCCN(C)[C@H]2CC[C@H](OC(=O)[C@](O)(c3ccccc3)C3CCCC3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3973386 152212 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 μg/well for beta1 and 5 μg/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 μl, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 μM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 μg/well for beta1 and 5 μg/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 μl, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 μM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.
ChEMBL 790 15 6 11 6.1 COc1cc(NC(=O)OCCN(C)[C@H]2CC[C@H](OC(=O)[C@](O)(c3ccccc3)C3CCCC3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
44583033 184938 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding affinity to beta2 adrenoceptorBinding affinity to beta2 adrenoceptor
ChEMBL 385 9 4 5 2.2 COc1ccc(CC(C)(C)NC[C@H](O)COc2cccc3[nH]c(=O)[nH]c23)cc1 10.1021/jm900364m
CHEMBL486278 184938 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding affinity to beta2 adrenoceptorBinding affinity to beta2 adrenoceptor
ChEMBL 385 9 4 5 2.2 COc1ccc(CC(C)(C)NC[C@H](O)COc2cccc3[nH]c(=O)[nH]c23)cc1 10.1021/jm900364m
121347973 151084 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 ug/well for beta1 and 5 ug/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 ul, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 uM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 ug/well for beta1 and 5 ug/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 ul, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 uM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.
ChEMBL 732 14 5 13 4.6 CN(CCCn1nnc2cc(CNC[C@H](O)c3ccc(O)c4c3OCC(=O)N4)ccc21)[C@H]1CC[C@H](OC(=O)[C@](O)(c2cccs2)C2CCCC2)CC1 nan
CHEMBL3963770 151084 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 ug/well for beta1 and 5 ug/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 ul, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 uM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 ug/well for beta1 and 5 ug/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 ul, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 uM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.
ChEMBL 732 14 5 13 4.6 CN(CCCn1nnc2cc(CNC[C@H](O)c3ccc(O)c4c3OCC(=O)N4)ccc21)[C@H]1CC[C@H](OC(=O)[C@](O)(c2cccs2)C2CCCC2)CC1 nan
145990586 166279 0 None 1 11 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]-CGP-12177 from human beta2-adrenergic receptorDisplacement of [3H]-CGP-12177 from human beta2-adrenergic receptor
ChEMBL 297 2 2 4 2.6 COc1cc2c3c(c1OC)-c1ccccc1[C@@H](O)[C@@H]3NCC2 10.1039/C7MD00656J
CHEMBL4285281 166279 0 None 1 11 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]-CGP-12177 from human beta2-adrenergic receptorDisplacement of [3H]-CGP-12177 from human beta2-adrenergic receptor
ChEMBL 297 2 2 4 2.6 COc1cc2c3c(c1OC)-c1ccccc1[C@@H](O)[C@@H]3NCC2 10.1039/C7MD00656J
53380559 63295 0 None - 1 Human 8.8 pIC50 = 8.8 Binding
Mitogenesis inhibition method: To measure beta2-AR mediated inhibition of mitogenesis, HEK-beta2-AR, 1321N1 or U87MG cells were seeded in a 96-well plate at approximately 5,000 cells/well. After 48 hours, the wells were rinsed twice and the medium was replaced with fresh medium containing 10 uL of drug in sterile water. After another 24 hours of incubation at 37° C., 0.25 uCi of [3H]-thymidine was added to each well. The cells were incubated for an additional 2 hours at 37° C., at which point 10 uL of 10x trypsin was added, and the resuspended cells were harvested using a Tomtec 96 harvester through glass fiber filters.Mitogenesis inhibition method: To measure beta2-AR mediated inhibition of mitogenesis, HEK-beta2-AR, 1321N1 or U87MG cells were seeded in a 96-well plate at approximately 5,000 cells/well. After 48 hours, the wells were rinsed twice and the medium was replaced with fresh medium containing 10 uL of drug in sterile water. After another 24 hours of incubation at 37° C., 0.25 uCi of [3H]-thymidine was added to each well. The cells were incubated for an additional 2 hours at 37° C., at which point 10 uL of 10x trypsin was added, and the resuspended cells were harvested using a Tomtec 96 harvester through glass fiber filters.
ChEMBL 317 7 5 5 2.4 CC[C@H](Cc1ccc(O)cc1)NC[C@H](O)c1cc(O)cc(O)c1 nan
CHEMBL1800936 63295 0 None - 1 Human 8.8 pIC50 = 8.8 Binding
Mitogenesis inhibition method: To measure beta2-AR mediated inhibition of mitogenesis, HEK-beta2-AR, 1321N1 or U87MG cells were seeded in a 96-well plate at approximately 5,000 cells/well. After 48 hours, the wells were rinsed twice and the medium was replaced with fresh medium containing 10 uL of drug in sterile water. After another 24 hours of incubation at 37° C., 0.25 uCi of [3H]-thymidine was added to each well. The cells were incubated for an additional 2 hours at 37° C., at which point 10 uL of 10x trypsin was added, and the resuspended cells were harvested using a Tomtec 96 harvester through glass fiber filters.Mitogenesis inhibition method: To measure beta2-AR mediated inhibition of mitogenesis, HEK-beta2-AR, 1321N1 or U87MG cells were seeded in a 96-well plate at approximately 5,000 cells/well. After 48 hours, the wells were rinsed twice and the medium was replaced with fresh medium containing 10 uL of drug in sterile water. After another 24 hours of incubation at 37° C., 0.25 uCi of [3H]-thymidine was added to each well. The cells were incubated for an additional 2 hours at 37° C., at which point 10 uL of 10x trypsin was added, and the resuspended cells were harvested using a Tomtec 96 harvester through glass fiber filters.
ChEMBL 317 7 5 5 2.4 CC[C@H](Cc1ccc(O)cc1)NC[C@H](O)c1cc(O)cc(O)c1 nan
71565927 146116 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 ug/well for beta1 and 5 ug/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 ul, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 uM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 ug/well for beta1 and 5 ug/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 ul, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 uM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.
ChEMBL 758 12 4 11 6.3 CN(CCCn1c(=O)oc2cc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)ccc21)[C@H]1CC[C@H](OC(=O)C2(C)c3ccccc3Oc3ccccc32)CC1 nan
CHEMBL3923686 146116 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 ug/well for beta1 and 5 ug/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 ul, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 uM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 ug/well for beta1 and 5 ug/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 ul, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 uM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.
ChEMBL 758 12 4 11 6.3 CN(CCCn1c(=O)oc2cc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)ccc21)[C@H]1CC[C@H](OC(=O)C2(C)c3ccccc3Oc3ccccc32)CC1 nan
16735495 85345 0 None 14 2 Human 8.8 pIC50 = 8.8 Binding
Mitogenesis inhibition method: To measure beta2-AR mediated inhibition of mitogenesis, HEK-beta2-AR, 1321N1 or U87MG cells were seeded in a 96-well plate at approximately 5,000 cells/well. After 48 hours, the wells were rinsed twice and the medium was replaced with fresh medium containing 10 uL of drug in sterile water. After another 24 hours of incubation at 37° C., 0.25 uCi of [3H]-thymidine was added to each well. The cells were incubated for an additional 2 hours at 37° C., at which point 10 uL of 10x trypsin was added, and the resuspended cells were harvested using a Tomtec 96 harvester through glass fiber filters.Mitogenesis inhibition method: To measure beta2-AR mediated inhibition of mitogenesis, HEK-beta2-AR, 1321N1 or U87MG cells were seeded in a 96-well plate at approximately 5,000 cells/well. After 48 hours, the wells were rinsed twice and the medium was replaced with fresh medium containing 10 uL of drug in sterile water. After another 24 hours of incubation at 37° C., 0.25 uCi of [3H]-thymidine was added to each well. The cells were incubated for an additional 2 hours at 37° C., at which point 10 uL of 10x trypsin was added, and the resuspended cells were harvested using a Tomtec 96 harvester through glass fiber filters.
ChEMBL 337 6 4 4 3.5 C[C@H](Cc1cccc2ccccc12)NC[C@H](O)c1cc(O)cc(O)c1 nan
CHEMBL229401 85345 0 None 14 2 Human 8.8 pIC50 = 8.8 Binding
Mitogenesis inhibition method: To measure beta2-AR mediated inhibition of mitogenesis, HEK-beta2-AR, 1321N1 or U87MG cells were seeded in a 96-well plate at approximately 5,000 cells/well. After 48 hours, the wells were rinsed twice and the medium was replaced with fresh medium containing 10 uL of drug in sterile water. After another 24 hours of incubation at 37° C., 0.25 uCi of [3H]-thymidine was added to each well. The cells were incubated for an additional 2 hours at 37° C., at which point 10 uL of 10x trypsin was added, and the resuspended cells were harvested using a Tomtec 96 harvester through glass fiber filters.Mitogenesis inhibition method: To measure beta2-AR mediated inhibition of mitogenesis, HEK-beta2-AR, 1321N1 or U87MG cells were seeded in a 96-well plate at approximately 5,000 cells/well. After 48 hours, the wells were rinsed twice and the medium was replaced with fresh medium containing 10 uL of drug in sterile water. After another 24 hours of incubation at 37° C., 0.25 uCi of [3H]-thymidine was added to each well. The cells were incubated for an additional 2 hours at 37° C., at which point 10 uL of 10x trypsin was added, and the resuspended cells were harvested using a Tomtec 96 harvester through glass fiber filters.
ChEMBL 337 6 4 4 3.5 C[C@H](Cc1cccc2ccccc12)NC[C@H](O)c1cc(O)cc(O)c1 nan
127 3066 45 None -2 15 Human 8.8 pIC50 = 8.8 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 248 6 3 3 1.9 O[C@H](COc1cccc2c1cc[nH]2)CNC(C)C nan
688095 3066 45 None -2 15 Human 8.8 pIC50 = 8.8 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 248 6 3 3 1.9 O[C@H](COc1cccc2c1cc[nH]2)CNC(C)C nan
CHEMBL117405 3066 45 None -2 15 Human 8.8 pIC50 = 8.8 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 248 6 3 3 1.9 O[C@H](COc1cccc2c1cc[nH]2)CNC(C)C nan
24900942 70031 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 493 12 5 7 3.5 COc1ccccc1CNCCc1cccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)c1 10.1016/j.bmcl.2011.10.049
CHEMBL1945299 70031 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 493 12 5 7 3.5 COc1ccccc1CNCCc1cccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)c1 10.1016/j.bmcl.2011.10.049
54591014 145225 3 None - 0 Human 8.8 pIC50 = 8.8 Binding
Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 μg/well for beta1 and 5 μg/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 μl, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 μM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 μg/well for beta1 and 5 μg/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 μl, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 μM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.
ChEMBL 810 15 6 13 6.1 COc1cc(NC(=O)OCCN(C)[C@H]2CC[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3916700 145225 3 None - 0 Human 8.8 pIC50 = 8.8 Binding
Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 μg/well for beta1 and 5 μg/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 μl, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 μM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 μg/well for beta1 and 5 μg/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 μl, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 μM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.
ChEMBL 810 15 6 13 6.1 COc1cc(NC(=O)OCCN(C)[C@H]2CC[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
53379897 63300 0 None 40 2 Human 8.7 pIC50 = 8.7 Binding
Mitogenesis inhibition method: To measure beta2-AR mediated inhibition of mitogenesis, HEK-beta2-AR, 1321N1 or U87MG cells were seeded in a 96-well plate at approximately 5,000 cells/well. After 48 hours, the wells were rinsed twice and the medium was replaced with fresh medium containing 10 uL of drug in sterile water. After another 24 hours of incubation at 37° C., 0.25 uCi of [3H]-thymidine was added to each well. The cells were incubated for an additional 2 hours at 37° C., at which point 10 uL of 10x trypsin was added, and the resuspended cells were harvested using a Tomtec 96 harvester through glass fiber filters.Mitogenesis inhibition method: To measure beta2-AR mediated inhibition of mitogenesis, HEK-beta2-AR, 1321N1 or U87MG cells were seeded in a 96-well plate at approximately 5,000 cells/well. After 48 hours, the wells were rinsed twice and the medium was replaced with fresh medium containing 10 uL of drug in sterile water. After another 24 hours of incubation at 37° C., 0.25 uCi of [3H]-thymidine was added to each well. The cells were incubated for an additional 2 hours at 37° C., at which point 10 uL of 10x trypsin was added, and the resuspended cells were harvested using a Tomtec 96 harvester through glass fiber filters.
ChEMBL 337 6 4 4 3.5 C[C@H](Cc1ccc2ccccc2c1)NC[C@H](O)c1cc(O)cc(O)c1 nan
CHEMBL1800961 63300 0 None 40 2 Human 8.7 pIC50 = 8.7 Binding
Mitogenesis inhibition method: To measure beta2-AR mediated inhibition of mitogenesis, HEK-beta2-AR, 1321N1 or U87MG cells were seeded in a 96-well plate at approximately 5,000 cells/well. After 48 hours, the wells were rinsed twice and the medium was replaced with fresh medium containing 10 uL of drug in sterile water. After another 24 hours of incubation at 37° C., 0.25 uCi of [3H]-thymidine was added to each well. The cells were incubated for an additional 2 hours at 37° C., at which point 10 uL of 10x trypsin was added, and the resuspended cells were harvested using a Tomtec 96 harvester through glass fiber filters.Mitogenesis inhibition method: To measure beta2-AR mediated inhibition of mitogenesis, HEK-beta2-AR, 1321N1 or U87MG cells were seeded in a 96-well plate at approximately 5,000 cells/well. After 48 hours, the wells were rinsed twice and the medium was replaced with fresh medium containing 10 uL of drug in sterile water. After another 24 hours of incubation at 37° C., 0.25 uCi of [3H]-thymidine was added to each well. The cells were incubated for an additional 2 hours at 37° C., at which point 10 uL of 10x trypsin was added, and the resuspended cells were harvested using a Tomtec 96 harvester through glass fiber filters.
ChEMBL 337 6 4 4 3.5 C[C@H](Cc1ccc2ccccc2c1)NC[C@H](O)c1cc(O)cc(O)c1 nan
24901349 69972 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 481 11 5 6 3.6 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3ccc(CNCCc4ccccc4F)cc3)c2s1 10.1016/j.bmcl.2011.10.049
CHEMBL1944692 69972 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 481 11 5 6 3.6 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3ccc(CNCCc4ccccc4F)cc3)c2s1 10.1016/j.bmcl.2011.10.049
24901351 69974 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 493 12 5 7 3.5 COc1ccccc1CCNCc1ccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)cc1 10.1016/j.bmcl.2011.10.049
CHEMBL1944694 69974 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 493 12 5 7 3.5 COc1ccccc1CCNCc1ccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)cc1 10.1016/j.bmcl.2011.10.049
24901347 69975 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 463 11 5 6 3.5 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3ccc(CNCCc4ccccc4)cc3)c2s1 10.1016/j.bmcl.2011.10.049
CHEMBL1944695 69975 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 463 11 5 6 3.5 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3ccc(CNCCc4ccccc4)cc3)c2s1 10.1016/j.bmcl.2011.10.049
24901413 69998 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 516 11 6 6 4.3 Cc1cccc2c(CCNCc3ccc(CCNC[C@H](O)c4ccc(O)c5[nH]c(=O)sc45)cc3)c[nH]c12 10.1016/j.bmcl.2011.10.049
CHEMBL1945032 69998 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 516 11 6 6 4.3 Cc1cccc2c(CCNCc3ccc(CCNC[C@H](O)c4ccc(O)c5[nH]c(=O)sc45)cc3)c[nH]c12 10.1016/j.bmcl.2011.10.049
24901143 70007 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 483 10 5 6 4.1 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3cccc(CNCc4ccccc4Cl)c3)c2s1 10.1016/j.bmcl.2011.10.049
CHEMBL1945041 70007 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 483 10 5 6 4.1 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3cccc(CNCc4ccccc4Cl)c3)c2s1 10.1016/j.bmcl.2011.10.049
57403815 70178 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 539 11 5 6 5.7 C[C@@H](NCc1ccccc1-c1ccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)cc1)c1ccccc1 10.1016/j.bmcl.2011.10.049
CHEMBL1947155 70178 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 539 11 5 6 5.7 C[C@@H](NCc1ccccc1-c1ccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)cc1)c1ccccc1 10.1016/j.bmcl.2011.10.049
44268249 19299 0 None - 0 Human 8.0 pIC50 = 8 Binding
Binding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandBinding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligand
ChEMBL 331 9 4 5 2.4 C[C@@H](CCc1ccc(O)cc1)NC[C@H](O)COc1ccc(O)cc1 10.1016/s0960-894x(98)00169-3
CHEMBL12994 19299 0 None - 0 Human 8.0 pIC50 = 8 Binding
Binding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandBinding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligand
ChEMBL 331 9 4 5 2.4 C[C@@H](CCc1ccc(O)cc1)NC[C@H](O)COc1ccc(O)cc1 10.1016/s0960-894x(98)00169-3
24900424 70179 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 525 11 5 6 5.1 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3cccc(-c4cccc(CNCc5ccccc5)c4)c3)c2s1 10.1016/j.bmcl.2011.10.049
CHEMBL1947156 70179 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 525 11 5 6 5.1 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3cccc(-c4cccc(CNCc5ccccc5)c4)c3)c2s1 10.1016/j.bmcl.2011.10.049
155566405 175354 0 None 3 2 Human 7.0 pIC50 = 7 Binding
Antagonist activity at human recombinant beta2 adrenoreceptor expressed in CHOK1 cells incubated for 30 mins by HTRFAntagonist activity at human recombinant beta2 adrenoreceptor expressed in CHOK1 cells incubated for 30 mins by HTRF
ChEMBL 426 21 3 8 0.8 C=CCc1ccccc1OCC(O)CNCCOCCOCCOCCOCCN 10.1039/C8MD00412A
CHEMBL4587648 175354 0 None 3 2 Human 7.0 pIC50 = 7 Binding
Antagonist activity at human recombinant beta2 adrenoreceptor expressed in CHOK1 cells incubated for 30 mins by HTRFAntagonist activity at human recombinant beta2 adrenoreceptor expressed in CHOK1 cells incubated for 30 mins by HTRF
ChEMBL 426 21 3 8 0.8 C=CCc1ccccc1OCC(O)CNCCOCCOCCOCCOCCN 10.1039/C8MD00412A
44268273 96620 0 None - 0 Human 7.0 pIC50 = 7 Binding
Binding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandBinding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligand
ChEMBL 476 11 4 6 3.4 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1)c1ccccc1Cl 10.1016/s0960-894x(98)00169-3
CHEMBL267306 96620 0 None - 0 Human 7.0 pIC50 = 7 Binding
Binding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandBinding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligand
ChEMBL 476 11 4 6 3.4 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1)c1ccccc1Cl 10.1016/s0960-894x(98)00169-3
46882084 5689 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counter
ChEMBL 465 11 3 4 5.0 O=C(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(CCc2ccccc2)cc1 10.1016/j.bmcl.2010.01.130
CHEMBL1078695 5689 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counter
ChEMBL 465 11 3 4 5.0 O=C(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(CCc2ccccc2)cc1 10.1016/j.bmcl.2010.01.130
57395241 70139 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 448 11 4 6 3.4 O=c1[nH]c2c(O)ccc(CCNCCc3ccc(CNCCc4ccccn4)cc3)c2s1 10.1016/j.bmcl.2011.10.049
CHEMBL1946763 70139 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 448 11 4 6 3.4 O=c1[nH]c2c(O)ccc(CCNCCc3ccc(CNCCc4ccccn4)cc3)c2s1 10.1016/j.bmcl.2011.10.049
44307166 102235 0 None - 0 Human 7.0 pIC50 = 7 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cell
ChEMBL 570 11 3 5 3.8 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2ccc(F)cc2)cc1)c1ccc(I)cc1 10.1016/s0960-894x(98)00381-3
CHEMBL304878 102235 0 None - 0 Human 7.0 pIC50 = 7 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cell
ChEMBL 570 11 3 5 3.8 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2ccc(F)cc2)cc1)c1ccc(I)cc1 10.1016/s0960-894x(98)00381-3
44298315 192685 0 None - 0 Human 7.0 pIC50 = 7 Binding
In vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 454 11 1 6 5.5 CCCCCCCCc1nc(N2CCc3cc(S(=O)(=O)Nc4ccccc4)ccc32)no1 10.1016/s0960-894x(99)00277-2
CHEMBL52407 192685 0 None - 0 Human 7.0 pIC50 = 7 Binding
In vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 454 11 1 6 5.5 CCCCCCCCc1nc(N2CCc3cc(S(=O)(=O)Nc4ccccc4)ccc32)no1 10.1016/s0960-894x(99)00277-2
44335833 5491 0 None - 0 Human 6.0 pIC50 = 6 Binding
Beta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindolol
ChEMBL 448 9 3 6 3.3 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1cnc2ccccc2c1 10.1016/s0960-894x(98)00571-x
CHEMBL107681 5491 0 None - 0 Human 6.0 pIC50 = 6 Binding
Beta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindolol
ChEMBL 448 9 3 6 3.3 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1cnc2ccccc2c1 10.1016/s0960-894x(98)00571-x
44335498 107044 0 None - 0 Human 6.0 pIC50 = 6 Binding
Beta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindolol
ChEMBL 447 9 3 5 3.9 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc2ccccc2c1 10.1016/s0960-894x(98)00571-x
CHEMBL318802 107044 0 None - 0 Human 6.0 pIC50 = 6 Binding
Beta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindolol
ChEMBL 447 9 3 5 3.9 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc2ccccc2c1 10.1016/s0960-894x(98)00571-x
44301866 100096 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindololBinding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindolol
ChEMBL 606 18 3 7 6.7 CCCCCCCCc1csc(Cc2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)n1 10.1016/s0960-894x(00)00390-5
CHEMBL291593 100096 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindololBinding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindolol
ChEMBL 606 18 3 7 6.7 CCCCCCCCc1csc(Cc2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)n1 10.1016/s0960-894x(00)00390-5
10438390 201702 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity for clone human Beta-2 adrenergic receptor from CHO cell membranes in the presence of I-iodocyanopindololBinding affinity for clone human Beta-2 adrenergic receptor from CHO cell membranes in the presence of I-iodocyanopindolol
ChEMBL 590 12 3 8 4.2 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-n2ncc(Cc3ccc(F)c(F)c3)n2)cc1 10.1016/s0960-894x(00)00422-4
CHEMBL65513 201702 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity for clone human Beta-2 adrenergic receptor from CHO cell membranes in the presence of I-iodocyanopindololBinding affinity for clone human Beta-2 adrenergic receptor from CHO cell membranes in the presence of I-iodocyanopindolol
ChEMBL 590 12 3 8 4.2 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-n2ncc(Cc3ccc(F)c(F)c3)n2)cc1 10.1016/s0960-894x(00)00422-4
14998852 55374 0 None - 0 Dog 6.0 pIC50 = 6 Binding
Binding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprololBinding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprolol
ChEMBL 360 6 3 5 1.9 CS(=O)(=O)Nc1ccc(NCC2CN(c3ccccc3)CCN2)cc1 10.1021/jm00082a016
CHEMBL162182 55374 0 None - 0 Dog 6.0 pIC50 = 6 Binding
Binding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprololBinding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprolol
ChEMBL 360 6 3 5 1.9 CS(=O)(=O)Nc1ccc(NCC2CN(c3ccccc3)CCN2)cc1 10.1021/jm00082a016
12043155 99268 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards Beta-2 adrenergic receptor prepared from CHO cells expressing the cloned human receptor in the presence of [125I]iodocyanopindololBinding affinity towards Beta-2 adrenergic receptor prepared from CHO cells expressing the cloned human receptor in the presence of [125I]iodocyanopindolol
ChEMBL 549 14 3 8 4.8 CC(C)CCCc1nc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)no1 10.1016/s0960-894x(00)00267-5
CHEMBL284965 99268 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards Beta-2 adrenergic receptor prepared from CHO cells expressing the cloned human receptor in the presence of [125I]iodocyanopindololBinding affinity towards Beta-2 adrenergic receptor prepared from CHO cells expressing the cloned human receptor in the presence of [125I]iodocyanopindolol
ChEMBL 549 14 3 8 4.8 CC(C)CCCc1nc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)no1 10.1016/s0960-894x(00)00267-5
44281276 99344 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards Beta-2 adrenergic receptor prepared from CHO cells expressing the cloned human receptor in the presence of [125I]iodocyanopindololBinding affinity towards Beta-2 adrenergic receptor prepared from CHO cells expressing the cloned human receptor in the presence of [125I]iodocyanopindolol
ChEMBL 549 15 3 8 4.9 CCCCCCc1nc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)no1 10.1016/s0960-894x(00)00267-5
CHEMBL285481 99344 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards Beta-2 adrenergic receptor prepared from CHO cells expressing the cloned human receptor in the presence of [125I]iodocyanopindololBinding affinity towards Beta-2 adrenergic receptor prepared from CHO cells expressing the cloned human receptor in the presence of [125I]iodocyanopindolol
ChEMBL 549 15 3 8 4.9 CCCCCCc1nc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)no1 10.1016/s0960-894x(00)00267-5
44377315 57062 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindololBinding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindolol
ChEMBL 605 14 3 6 5.4 O=C1N(CCCC2CCCCC2)CCN1c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(99)00072-4
CHEMBL165177 57062 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindololBinding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindolol
ChEMBL 605 14 3 6 5.4 O=C1N(CCCC2CCCCC2)CCN1c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(99)00072-4
44377687 57128 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindololBinding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindolol
ChEMBL 579 16 3 6 5.0 CCCCCCCN1CCN(c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)C1=O 10.1016/s0960-894x(99)00072-4
CHEMBL165513 57128 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindololBinding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindolol
ChEMBL 579 16 3 6 5.0 CCCCCCCN1CCN(c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)C1=O 10.1016/s0960-894x(99)00072-4
44377316 119544 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindololBinding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindolol
ChEMBL 591 13 3 6 5.0 O=C1N(CCC2CCCCC2)CCN1c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(99)00072-4
CHEMBL350590 119544 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindololBinding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindolol
ChEMBL 591 13 3 6 5.0 O=C1N(CCC2CCCCC2)CCN1c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(99)00072-4
1499 2052 43 None - 17 Dog 6.0 pIC50 = 6 Binding
Compound was evaluated for its binding affinity towards beta-2 adrenergic receptor in rat soleus membrane by displacing (-)-isoproterenol (50 uM)Compound was evaluated for its binding affinity towards beta-2 adrenergic receptor in rat soleus membrane by displacing (-)-isoproterenol (50 uM)
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm00094a025
3779 2052 43 None - 17 Dog 6.0 pIC50 = 6 Binding
Compound was evaluated for its binding affinity towards beta-2 adrenergic receptor in rat soleus membrane by displacing (-)-isoproterenol (50 uM)Compound was evaluated for its binding affinity towards beta-2 adrenergic receptor in rat soleus membrane by displacing (-)-isoproterenol (50 uM)
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm00094a025
536 2052 43 None - 17 Dog 6.0 pIC50 = 6 Binding
Compound was evaluated for its binding affinity towards beta-2 adrenergic receptor in rat soleus membrane by displacing (-)-isoproterenol (50 uM)Compound was evaluated for its binding affinity towards beta-2 adrenergic receptor in rat soleus membrane by displacing (-)-isoproterenol (50 uM)
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm00094a025
CHEMBL434 2052 43 None - 17 Dog 6.0 pIC50 = 6 Binding
Compound was evaluated for its binding affinity towards beta-2 adrenergic receptor in rat soleus membrane by displacing (-)-isoproterenol (50 uM)Compound was evaluated for its binding affinity towards beta-2 adrenergic receptor in rat soleus membrane by displacing (-)-isoproterenol (50 uM)
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm00094a025
DB01064 2052 43 None - 17 Dog 6.0 pIC50 = 6 Binding
Compound was evaluated for its binding affinity towards beta-2 adrenergic receptor in rat soleus membrane by displacing (-)-isoproterenol (50 uM)Compound was evaluated for its binding affinity towards beta-2 adrenergic receptor in rat soleus membrane by displacing (-)-isoproterenol (50 uM)
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm00094a025
44306985 202015 0 None - 0 Human 6.0 pIC50 = 6 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cell
ChEMBL 460 11 4 7 2.2 Nc1ccc(OC[C@@H](O)CNCCc2ccc(NS(=O)(=O)c3ccc(F)cc3)cc2)cn1 10.1016/s0960-894x(98)00381-3
CHEMBL67672 202015 0 None - 0 Human 6.0 pIC50 = 6 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cell
ChEMBL 460 11 4 7 2.2 Nc1ccc(OC[C@@H](O)CNCCc2ccc(NS(=O)(=O)c3ccc(F)cc3)cc2)cn1 10.1016/s0960-894x(98)00381-3
44268572 25446 0 None - 0 Human 6.0 pIC50 = 6 Binding
In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.
ChEMBL 572 16 6 8 2.9 COCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/s0960-894x(98)00170-x
CHEMBL13521 25446 0 None - 0 Human 6.0 pIC50 = 6 Binding
In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.
ChEMBL 572 16 6 8 2.9 COCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/s0960-894x(98)00170-x
44285225 153030 0 None - 0 Human 6.0 pIC50 = 6 Binding
In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.
ChEMBL 562 13 3 7 5.8 CC(C)(C)CCCc1ncc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)o1 10.1016/s0960-894x(00)00277-8
CHEMBL39804 153030 0 None - 0 Human 6.0 pIC50 = 6 Binding
In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.
ChEMBL 562 13 3 7 5.8 CC(C)(C)CCCc1ncc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)o1 10.1016/s0960-894x(00)00277-8
44298781 100214 0 None - 0 Human 6.0 pIC50 = 6 Binding
In vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 443 10 1 3 5.3 CCCCCCCCN(C)C(=O)N1CCc2cc(S(=O)(=O)Nc3ccccc3)ccc21 10.1016/s0960-894x(99)00277-2
CHEMBL292407 100214 0 None - 0 Human 6.0 pIC50 = 6 Binding
In vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 443 10 1 3 5.3 CCCCCCCCN(C)C(=O)N1CCc2cc(S(=O)(=O)Nc3ccccc3)ccc21 10.1016/s0960-894x(99)00277-2
44298695 100455 0 None - 0 Human 6.0 pIC50 = 6 Binding
In vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 414 10 1 3 5.1 CCCCCCCCC(=O)N1CCc2cc(S(=O)(=O)Nc3ccccc3)ccc21 10.1016/s0960-894x(99)00277-2
CHEMBL294008 100455 0 None - 0 Human 6.0 pIC50 = 6 Binding
In vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 414 10 1 3 5.1 CCCCCCCCC(=O)N1CCc2cc(S(=O)(=O)Nc3ccccc3)ccc21 10.1016/s0960-894x(99)00277-2
44335496 4718 0 None - 0 Human 5.0 pIC50 = 5 Binding
Beta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindolol
ChEMBL 335 8 3 5 1.3 CS(=O)(=O)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/s0960-894x(98)00571-x
CHEMBL104127 4718 0 None - 0 Human 5.0 pIC50 = 5 Binding
Beta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindolol
ChEMBL 335 8 3 5 1.3 CS(=O)(=O)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/s0960-894x(98)00571-x
44335628 4752 0 None - 0 Human 5.0 pIC50 = 5 Binding
Beta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindolol
ChEMBL 498 12 4 7 3.7 CCCOC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(98)00571-x
CHEMBL104222 4752 0 None - 0 Human 5.0 pIC50 = 5 Binding
Beta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindolol
ChEMBL 498 12 4 7 3.7 CCCOC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(98)00571-x
44335603 106933 0 None - 0 Human 5.0 pIC50 = 5 Binding
Beta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindolol
ChEMBL 538 16 4 6 5.0 CCCCCCCC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(98)00571-x
CHEMBL318165 106933 0 None - 0 Human 5.0 pIC50 = 5 Binding
Beta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindolol
ChEMBL 538 16 4 6 5.0 CCCCCCCC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(98)00571-x
44335651 108059 0 None - 0 Human 5.0 pIC50 = 5 Binding
Beta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindolol
ChEMBL 431 9 3 5 3.4 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(Cl)cc1 10.1016/s0960-894x(98)00571-x
CHEMBL320228 108059 0 None - 0 Human 5.0 pIC50 = 5 Binding
Beta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindolol
ChEMBL 431 9 3 5 3.4 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(Cl)cc1 10.1016/s0960-894x(98)00571-x
44377412 119636 0 None - 0 Human 5.0 pIC50 = 5 Binding
Binding affinity towards Beta-2 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindololBinding affinity towards Beta-2 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindolol
ChEMBL 580 15 4 9 3.0 CCCCCCn1c(=O)[nH]n(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)c1=O 10.1016/s0960-894x(99)00073-6
CHEMBL351467 119636 0 None - 0 Human 5.0 pIC50 = 5 Binding
Binding affinity towards Beta-2 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindololBinding affinity towards Beta-2 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindolol
ChEMBL 580 15 4 9 3.0 CCCCCCn1c(=O)[nH]n(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)c1=O 10.1016/s0960-894x(99)00073-6
44281037 112826 0 None - 0 Human 5.0 pIC50 = 5 Binding
Binding affinity towards Beta-2 adrenergic receptor prepared from CHO cells expressing the cloned human receptor in the presence of [125I]iodocyanopindololBinding affinity towards Beta-2 adrenergic receptor prepared from CHO cells expressing the cloned human receptor in the presence of [125I]iodocyanopindolol
ChEMBL 479 10 3 8 3.1 Cc1nc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)no1 10.1016/s0960-894x(00)00267-5
CHEMBL33168 112826 0 None - 0 Human 5.0 pIC50 = 5 Binding
Binding affinity towards Beta-2 adrenergic receptor prepared from CHO cells expressing the cloned human receptor in the presence of [125I]iodocyanopindololBinding affinity towards Beta-2 adrenergic receptor prepared from CHO cells expressing the cloned human receptor in the presence of [125I]iodocyanopindolol
ChEMBL 479 10 3 8 3.1 Cc1nc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)no1 10.1016/s0960-894x(00)00267-5
44377755 119436 0 None - 0 Human 5.0 pIC50 = 5 Binding
Binding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindololBinding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindolol
ChEMBL 589 13 3 8 4.0 O=c1n(CCCC(F)(F)F)ccn1-c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(99)00072-4
CHEMBL349689 119436 0 None - 0 Human 5.0 pIC50 = 5 Binding
Binding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindololBinding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindolol
ChEMBL 589 13 3 8 4.0 O=c1n(CCCC(F)(F)F)ccn1-c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(99)00072-4
57403553 69843 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of [3H]dihydroalprenolol from beta2-adrenoceptor after 90 mins by liquid scintillation countingDisplacement of [3H]dihydroalprenolol from beta2-adrenoceptor after 90 mins by liquid scintillation counting
ChEMBL 420 13 8 8 0.8 OCc1cc(C(O)CNCCCCNCC(O)c2ccc(O)c(CO)c2)ccc1O 10.1016/j.bmcl.2011.11.072
CHEMBL1940682 69843 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of [3H]dihydroalprenolol from beta2-adrenoceptor after 90 mins by liquid scintillation countingDisplacement of [3H]dihydroalprenolol from beta2-adrenoceptor after 90 mins by liquid scintillation counting
ChEMBL 420 13 8 8 0.8 OCc1cc(C(O)CNCCCCNCC(O)c2ccc(O)c(CO)c2)ccc1O 10.1016/j.bmcl.2011.11.072
9956562 69851 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of [3H]dihydroalprenolol from beta2-adrenoceptor after 90 mins by liquid scintillation countingDisplacement of [3H]dihydroalprenolol from beta2-adrenoceptor after 90 mins by liquid scintillation counting
ChEMBL 474 12 8 8 1.8 OCc1cc(C(O)CNCC2CCCC(CNCC(O)c3ccc(O)c(CO)c3)C2)ccc1O 10.1016/j.bmcl.2011.11.072
CHEMBL1940808 69851 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of [3H]dihydroalprenolol from beta2-adrenoceptor after 90 mins by liquid scintillation countingDisplacement of [3H]dihydroalprenolol from beta2-adrenoceptor after 90 mins by liquid scintillation counting
ChEMBL 474 12 8 8 1.8 OCc1cc(C(O)CNCC2CCCC(CNCC(O)c3ccc(O)c(CO)c3)C2)ccc1O 10.1016/j.bmcl.2011.11.072
44298767 100419 0 None - 0 Human 5.0 pIC50 = 5 Binding
In vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 553 15 4 6 4.5 CCCCCCNC(=O)N(C)c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(99)00277-2
CHEMBL293818 100419 0 None - 0 Human 5.0 pIC50 = 5 Binding
In vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 553 15 4 6 4.5 CCCCCCNC(=O)N(C)c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(99)00277-2
10553898 168859 0 None - 0 Dog 5.0 pIC50 = 5 Binding
Inhibition of beta-2 adrenergic receptor isolated from rat lung homogenatesInhibition of beta-2 adrenergic receptor isolated from rat lung homogenates
ChEMBL 400 8 2 4 3.3 OC(CNc1ccc(I)cc1)CON=C(C1CC1)C1CC1 10.1021/jm970338c
CHEMBL44261 168859 0 None - 0 Dog 5.0 pIC50 = 5 Binding
Inhibition of beta-2 adrenergic receptor isolated from rat lung homogenatesInhibition of beta-2 adrenergic receptor isolated from rat lung homogenates
ChEMBL 400 8 2 4 3.3 OC(CNc1ccc(I)cc1)CON=C(C1CC1)C1CC1 10.1021/jm970338c
24229559 163608 53 None - 1 Human 5.0 pIC50 = 5 Binding
Inhibition of beta2 adrenoreceptor (unknown origin)Inhibition of beta2 adrenoreceptor (unknown origin)
ChEMBL 185 2 1 3 1.6 NCc1ccc(-c2ncccn2)cc1 10.1021/acs.jmedchem.9b01581
CHEMBL4210507 163608 53 None - 1 Human 5.0 pIC50 = 5 Binding
Inhibition of beta2 adrenoreceptor (unknown origin)Inhibition of beta2 adrenoreceptor (unknown origin)
ChEMBL 185 2 1 3 1.6 NCc1ccc(-c2ncccn2)cc1 10.1021/acs.jmedchem.9b01581
44461488 203654 0 None - 0 Human 4.0 pIC50 = 4 Binding
Binding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindololBinding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindolol
ChEMBL 606 13 3 7 3.0 O=C(CCN1CCN(c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)C1=O)N1CCCC1 10.1016/s0960-894x(99)00072-4
CHEMBL79915 203654 0 None - 0 Human 4.0 pIC50 = 4 Binding
Binding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindololBinding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindolol
ChEMBL 606 13 3 7 3.0 O=C(CCN1CCN(c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)C1=O)N1CCCC1 10.1016/s0960-894x(99)00072-4
57400044 69854 0 None - 0 Human 4.0 pIC50 = 4 Binding
Displacement of [3H]dihydroalprenolol from beta2-adrenoceptor after 90 mins by liquid scintillation countingDisplacement of [3H]dihydroalprenolol from beta2-adrenoceptor after 90 mins by liquid scintillation counting
ChEMBL 496 14 8 8 1.8 OCc1cc(C(O)CNCCc2ccc(CCNCC(O)c3ccc(O)c(CO)c3)cc2)ccc1O 10.1016/j.bmcl.2011.11.072
CHEMBL1940811 69854 0 None - 0 Human 4.0 pIC50 = 4 Binding
Displacement of [3H]dihydroalprenolol from beta2-adrenoceptor after 90 mins by liquid scintillation countingDisplacement of [3H]dihydroalprenolol from beta2-adrenoceptor after 90 mins by liquid scintillation counting
ChEMBL 496 14 8 8 1.8 OCc1cc(C(O)CNCCc2ccc(CCNCC(O)c3ccc(O)c(CO)c3)cc2)ccc1O 10.1016/j.bmcl.2011.11.072
208932 13431 8 None - 0 Dog 4.0 pIC50 = 4 Binding
In vitro Beta-2 adrenergic receptor affinity in partially purified membrane fractions from canine lung tissue using [SH]dihydroalprenolol (4.5 nM)In vitro Beta-2 adrenergic receptor affinity in partially purified membrane fractions from canine lung tissue using [SH]dihydroalprenolol (4.5 nM)
ChEMBL 446 12 3 8 1.7 CS(=O)(=O)Nc1ccc(OC[C@@H](O)CNCCOc2ccc(-n3ccnc3)cc2)cc1 10.1021/jm00166a002
CHEMBL1193886 13431 8 None - 0 Dog 4.0 pIC50 = 4 Binding
In vitro Beta-2 adrenergic receptor affinity in partially purified membrane fractions from canine lung tissue using [SH]dihydroalprenolol (4.5 nM)In vitro Beta-2 adrenergic receptor affinity in partially purified membrane fractions from canine lung tissue using [SH]dihydroalprenolol (4.5 nM)
ChEMBL 446 12 3 8 1.7 CS(=O)(=O)Nc1ccc(OC[C@@H](O)CNCCOc2ccc(-n3ccnc3)cc2)cc1 10.1021/jm00166a002
CHEMBL545363 13431 8 None - 0 Dog 4.0 pIC50 = 4 Binding
In vitro Beta-2 adrenergic receptor affinity in partially purified membrane fractions from canine lung tissue using [SH]dihydroalprenolol (4.5 nM)In vitro Beta-2 adrenergic receptor affinity in partially purified membrane fractions from canine lung tissue using [SH]dihydroalprenolol (4.5 nM)
ChEMBL 446 12 3 8 1.7 CS(=O)(=O)Nc1ccc(OC[C@@H](O)CNCCOc2ccc(-n3ccnc3)cc2)cc1 10.1021/jm00166a002
9962058 203064 0 None - 0 Human 4.0 pIC50 = 4 Binding
Inhibitory activity against CHO cells expressing human Beta-2 adrenergic receptor with [125I]-iodocyanopindololInhibitory activity against CHO cells expressing human Beta-2 adrenergic receptor with [125I]-iodocyanopindolol
ChEMBL 628 12 6 6 6.7 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(-c3cccc(CC4NCCc5cc(O)c(O)cc54)c3)cc2)cc1 10.1016/s0960-894x(00)00459-5
CHEMBL74860 203064 0 None - 0 Human 4.0 pIC50 = 4 Binding
Inhibitory activity against CHO cells expressing human Beta-2 adrenergic receptor with [125I]-iodocyanopindololInhibitory activity against CHO cells expressing human Beta-2 adrenergic receptor with [125I]-iodocyanopindolol
ChEMBL 628 12 6 6 6.7 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(-c3cccc(CC4NCCc5cc(O)c(O)cc54)c3)cc2)cc1 10.1016/s0960-894x(00)00459-5
50994950 136565 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of [125I]CYP from human beta-2 adrenergic receptor expressed in CHO cell membrane after 1 hr by scintillation counting methodDisplacement of [125I]CYP from human beta-2 adrenergic receptor expressed in CHO cell membrane after 1 hr by scintillation counting method
ChEMBL 450 7 2 5 3.5 CCOC(=O)C1CCN(C(=O)c2ccc(C[C@@H]3CC[C@H]([C@H](O)c4ccccc4)N3)cc2)CC1 10.1016/j.bmcl.2015.11.030
CHEMBL3747487 136565 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of [125I]CYP from human beta-2 adrenergic receptor expressed in CHO cell membrane after 1 hr by scintillation counting methodDisplacement of [125I]CYP from human beta-2 adrenergic receptor expressed in CHO cell membrane after 1 hr by scintillation counting method
ChEMBL 450 7 2 5 3.5 CCOC(=O)C1CCN(C(=O)c2ccc(C[C@@H]3CC[C@H]([C@H](O)c4ccccc4)N3)cc2)CC1 10.1016/j.bmcl.2015.11.030
44268367 20622 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandBinding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligand
ChEMBL 344 9 4 5 1.9 CC(=O)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/s0960-894x(98)00169-3
CHEMBL13102 20622 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandBinding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligand
ChEMBL 344 9 4 5 1.9 CC(=O)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/s0960-894x(98)00169-3
53495160 174380 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Inhibition of beta2 adrenoceptor (unknown origin)Inhibition of beta2 adrenoceptor (unknown origin)
ChEMBL 850 14 7 11 6.5 COc1cccc(Nc2c(C(N)=O)cnc3c(C)cc(S(=O)(=O)c4cccc(C(=O)Nc5ccc(C#CCCCNC[C@H](O)c6ccc(O)c7[nH]c(=O)ccc67)cc5)c4)cc23)c1 10.1021/acs.jmedchem.8b01520
CHEMBL4565954 174380 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Inhibition of beta2 adrenoceptor (unknown origin)Inhibition of beta2 adrenoceptor (unknown origin)
ChEMBL 850 14 7 11 6.5 COc1cccc(Nc2c(C(N)=O)cnc3c(C)cc(S(=O)(=O)c4cccc(C(=O)Nc5ccc(C#CCCCNC[C@H](O)c6ccc(O)c7[nH]c(=O)ccc67)cc5)c4)cc23)c1 10.1021/acs.jmedchem.8b01520
10437614 100462 6 None - 0 Human 7.0 pIC50 = 7.0 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cell
ChEMBL 553 11 3 6 3.1 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2cccnc2)cc1)c1ccc(I)cc1 10.1016/s0960-894x(98)00381-3
CHEMBL294042 100462 6 None - 0 Human 7.0 pIC50 = 7.0 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cell
ChEMBL 553 11 3 6 3.1 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2cccnc2)cc1)c1ccc(I)cc1 10.1016/s0960-894x(98)00381-3
44307340 102109 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cell
ChEMBL 470 12 4 7 2.6 CCc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(N)nc3)cc2)cc1 10.1016/s0960-894x(98)00381-3
CHEMBL304090 102109 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cell
ChEMBL 470 12 4 7 2.6 CCc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(N)nc3)cc2)cc1 10.1016/s0960-894x(98)00381-3
44268464 19198 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.
ChEMBL 585 17 5 8 4.9 CCCCCCOC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/s0960-894x(98)00170-x
CHEMBL12939 19198 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.
ChEMBL 585 17 5 8 4.9 CCCCCCOC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/s0960-894x(98)00170-x
44268478 162252 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.
ChEMBL 561 13 5 7 4.0 O=C(Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1)c1ccccc1 10.1016/s0960-894x(98)00170-x
CHEMBL417250 162252 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.
ChEMBL 561 13 5 7 4.0 O=C(Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1)c1ccccc1 10.1016/s0960-894x(98)00170-x
46881750 7130 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counter
ChEMBL 401 8 4 5 3.1 O=C(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1nc2ccccc2[nH]1 10.1016/j.bmcl.2010.01.130
CHEMBL1085693 7130 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counter
ChEMBL 401 8 4 5 3.1 O=C(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1nc2ccccc2[nH]1 10.1016/j.bmcl.2010.01.130
46881576 7747 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counter
ChEMBL 416 9 3 6 3.3 O=C(Cc1nc2ccccc2o1)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/j.bmcl.2010.01.130
CHEMBL1089725 7747 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counter
ChEMBL 416 9 3 6 3.3 O=C(Cc1nc2ccccc2o1)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/j.bmcl.2010.01.130
9992825 83937 16 None - 1 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]CGP1217 from human recombinant adrenergic beta2 receptor transfected in insect Sf9 cells by scintillation countingDisplacement of [3H]CGP1217 from human recombinant adrenergic beta2 receptor transfected in insect Sf9 cells by scintillation counting
ChEMBL 261 2 3 4 1.1 CC(C)NC1CCn2c(=O)[nH]c3cccc(c32)C1O 10.1021/jm801211c
CHEMBL2218907 83937 16 None - 1 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]CGP1217 from human recombinant adrenergic beta2 receptor transfected in insect Sf9 cells by scintillation countingDisplacement of [3H]CGP1217 from human recombinant adrenergic beta2 receptor transfected in insect Sf9 cells by scintillation counting
ChEMBL 261 2 3 4 1.1 CC(C)NC1CCn2c(=O)[nH]c3cccc(c32)C1O 10.1021/jm801211c
127041558 136480 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of [125I]CYP from human beta-2 adrenergic receptor expressed in CHO cell membrane after 1 hr by scintillation counting methodDisplacement of [125I]CYP from human beta-2 adrenergic receptor expressed in CHO cell membrane after 1 hr by scintillation counting method
ChEMBL 476 5 2 5 4.0 CC1(C)CC2(CCN(C(=O)c3ccc(C[C@@H]4CC[C@H]([C@H](O)c5ccccc5)N4)cc3)CC2)C(=O)O1 10.1016/j.bmcl.2015.11.030
CHEMBL3746280 136480 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of [125I]CYP from human beta-2 adrenergic receptor expressed in CHO cell membrane after 1 hr by scintillation counting methodDisplacement of [125I]CYP from human beta-2 adrenergic receptor expressed in CHO cell membrane after 1 hr by scintillation counting method
ChEMBL 476 5 2 5 4.0 CC1(C)CC2(CCN(C(=O)c3ccc(C[C@@H]4CC[C@H]([C@H](O)c5ccccc5)N4)cc3)CC2)C(=O)O1 10.1016/j.bmcl.2015.11.030
122238756 146483 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 ug/well for beta1 and 5 ug/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 ul, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 uM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 ug/well for beta1 and 5 ug/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 ul, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 uM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.
ChEMBL 734 14 5 10 6.2 CN(CCCn1c(=O)oc2cc(CNC[C@H](O)c3ccc(O)c(NC=O)c3)ccc21)[C@H]1CC[C@H](c2cccc3c2C(C)(C(=O)O)c2ccccc2O3)CC1 nan
CHEMBL3926721 146483 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 ug/well for beta1 and 5 ug/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 ul, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 uM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 ug/well for beta1 and 5 ug/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 ul, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 uM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.
ChEMBL 734 14 5 10 6.2 CN(CCCn1c(=O)oc2cc(CNC[C@H](O)c3ccc(O)c(NC=O)c3)ccc21)[C@H]1CC[C@H](c2cccc3c2C(C)(C(=O)O)c2ccccc2O3)CC1 nan
118710941 113239 0 None - 3 Guinea pig 7.9 pIC50 = 7.9 Binding
Agonist activity at adrenergic beta2 receptor in electrically-stimulated Dunkin-Hartley guinea pig tracheal strip assessed as inhibition of contractionAgonist activity at adrenergic beta2 receptor in electrically-stimulated Dunkin-Hartley guinea pig tracheal strip assessed as inhibition of contraction
ChEMBL 370 5 4 5 3.3 O=c1[nH]c2c(O)ccc([C@@H](O)CN[C@@H]3CCC[C@@H]3c3ccccc3)c2s1 10.1016/j.bmcl.2014.06.014
CHEMBL3323659 113239 0 None - 3 Guinea pig 7.9 pIC50 = 7.9 Binding
Agonist activity at adrenergic beta2 receptor in electrically-stimulated Dunkin-Hartley guinea pig tracheal strip assessed as inhibition of contractionAgonist activity at adrenergic beta2 receptor in electrically-stimulated Dunkin-Hartley guinea pig tracheal strip assessed as inhibition of contraction
ChEMBL 370 5 4 5 3.3 O=c1[nH]c2c(O)ccc([C@@H](O)CN[C@@H]3CCC[C@@H]3c3ccccc3)c2s1 10.1016/j.bmcl.2014.06.014
68807656 113246 0 None - 3 Guinea pig 7.9 pIC50 = 7.9 Binding
Agonist activity at adrenergic beta2 receptor in electrically-stimulated Dunkin-Hartley guinea pig tracheal strip assessed as inhibition of contractionAgonist activity at adrenergic beta2 receptor in electrically-stimulated Dunkin-Hartley guinea pig tracheal strip assessed as inhibition of contraction
ChEMBL 372 8 4 5 3.1 CCCc1cccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)c1 10.1016/j.bmcl.2014.06.014
CHEMBL3323666 113246 0 None - 3 Guinea pig 7.9 pIC50 = 7.9 Binding
Agonist activity at adrenergic beta2 receptor in electrically-stimulated Dunkin-Hartley guinea pig tracheal strip assessed as inhibition of contractionAgonist activity at adrenergic beta2 receptor in electrically-stimulated Dunkin-Hartley guinea pig tracheal strip assessed as inhibition of contraction
ChEMBL 372 8 4 5 3.1 CCCc1cccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)c1 10.1016/j.bmcl.2014.06.014
24901416 70001 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 481 11 5 6 3.6 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3ccccc3CNCCc3ccccc3F)c2s1 10.1016/j.bmcl.2011.10.049
CHEMBL1945035 70001 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 481 11 5 6 3.6 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3ccccc3CNCCc3ccccc3F)c2s1 10.1016/j.bmcl.2011.10.049
57398768 70141 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 459 10 4 5 4.3 O=c1[nH]c2c(O)ccc(CCNCCc3cccc(CN[C@H]4C[C@@H]4c4ccccc4)c3)c2s1 10.1016/j.bmcl.2011.10.049
CHEMBL1946765 70141 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 459 10 4 5 4.3 O=c1[nH]c2c(O)ccc(CCNCCc3cccc(CN[C@H]4C[C@@H]4c4ccccc4)c3)c2s1 10.1016/j.bmcl.2011.10.049
71558416 150783 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 ug/well for beta1 and 5 ug/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 ul, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 uM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 ug/well for beta1 and 5 ug/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 ul, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 uM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.
ChEMBL 757 14 6 12 4.9 CN(CCCn1c(=O)[nH]c2cc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)ccc21)[C@H]1CC[C@H](OC(=O)C(O)(c2cccs2)c2cccs2)CC1 nan
CHEMBL3961014 150783 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 ug/well for beta1 and 5 ug/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 ul, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 uM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 ug/well for beta1 and 5 ug/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 ul, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 uM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.
ChEMBL 757 14 6 12 4.9 CN(CCCn1c(=O)[nH]c2cc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)ccc21)[C@H]1CC[C@H](OC(=O)C(O)(c2cccs2)c2cccs2)CC1 nan
16118894 2203 3 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandBinding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligand
ChEMBL 568 11 4 6 3.4 O[C@H](COc1ccc(cc1)O)CNCCc1ccc(cc1)NS(=O)(=O)c1ccc(cc1)I 10.1016/s0960-894x(98)00169-3
3467 2203 3 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandBinding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligand
ChEMBL 568 11 4 6 3.4 O[C@H](COc1ccc(cc1)O)CNCCc1ccc(cc1)NS(=O)(=O)c1ccc(cc1)I 10.1016/s0960-894x(98)00169-3
CHEMBL276257 2203 3 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandBinding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligand
ChEMBL 568 11 4 6 3.4 O[C@H](COc1ccc(cc1)O)CNCCc1ccc(cc1)NS(=O)(=O)c1ccc(cc1)I 10.1016/s0960-894x(98)00169-3
9912580 17886 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandBinding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligand
ChEMBL 470 13 4 6 2.9 O=S(=O)(CCc1ccccc1)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/s0960-894x(98)00169-3
CHEMBL12674 17886 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandBinding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligand
ChEMBL 470 13 4 6 2.9 O=S(=O)(CCc1ccccc1)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/s0960-894x(98)00169-3
16118894 2203 3 None - 0 Human 6.9 pIC50 = 6.9 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cell
ChEMBL 568 11 4 6 3.4 O[C@H](COc1ccc(cc1)O)CNCCc1ccc(cc1)NS(=O)(=O)c1ccc(cc1)I 10.1016/s0960-894x(98)00381-3
3467 2203 3 None - 0 Human 6.9 pIC50 = 6.9 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cell
ChEMBL 568 11 4 6 3.4 O[C@H](COc1ccc(cc1)O)CNCCc1ccc(cc1)NS(=O)(=O)c1ccc(cc1)I 10.1016/s0960-894x(98)00381-3
CHEMBL276257 2203 3 None - 0 Human 6.9 pIC50 = 6.9 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cell
ChEMBL 568 11 4 6 3.4 O[C@H](COc1ccc(cc1)O)CNCCc1ccc(cc1)NS(=O)(=O)c1ccc(cc1)I 10.1016/s0960-894x(98)00381-3
44268498 97882 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.
ChEMBL 612 17 4 7 4.8 CCCCCCN(C)C(=O)N(C)c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/s0960-894x(98)00170-x
CHEMBL275114 97882 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.
ChEMBL 612 17 4 7 4.8 CCCCCCN(C)C(=O)N(C)c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/s0960-894x(98)00170-x
44349378 18324 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cells
ChEMBL 545 11 4 7 4.2 O=[N+]([O-])/C=C(\Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)Nc1cccc(I)c1 10.1016/s0960-894x(00)00669-7
CHEMBL127428 18324 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cells
ChEMBL 545 11 4 7 4.2 O=[N+]([O-])/C=C(\Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)Nc1cccc(I)c1 10.1016/s0960-894x(00)00669-7
44349379 18327 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cells
ChEMBL 462 12 5 8 2.6 NC(=O)c1cccc(N/C(=C/[N+](=O)[O-])Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)c1 10.1016/s0960-894x(00)00669-7
CHEMBL127451 18327 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cells
ChEMBL 462 12 5 8 2.6 NC(=O)c1cccc(N/C(=C/[N+](=O)[O-])Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)c1 10.1016/s0960-894x(00)00669-7
10722793 112835 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity was evaluated on chinese hamster ovary (CHO) cells expressing the cloned human beta-2 adrenergic receptor in the presence of [125I]- iodocyanopindolol.Binding affinity was evaluated on chinese hamster ovary (CHO) cells expressing the cloned human beta-2 adrenergic receptor in the presence of [125I]- iodocyanopindolol.
ChEMBL 640 12 3 8 6.4 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3ccc(OC(F)(F)F)cc3)cs2)cc1 10.1021/jm000286i
CHEMBL331744 112835 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity was evaluated on chinese hamster ovary (CHO) cells expressing the cloned human beta-2 adrenergic receptor in the presence of [125I]- iodocyanopindolol.Binding affinity was evaluated on chinese hamster ovary (CHO) cells expressing the cloned human beta-2 adrenergic receptor in the presence of [125I]- iodocyanopindolol.
ChEMBL 640 12 3 8 6.4 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3ccc(OC(F)(F)F)cc3)cs2)cc1 10.1021/jm000286i
44285226 99373 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.
ChEMBL 548 15 3 7 5.5 CCCCCCc1ncc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)o1 10.1016/s0960-894x(00)00277-8
CHEMBL285713 99373 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.
ChEMBL 548 15 3 7 5.5 CCCCCCc1ncc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)o1 10.1016/s0960-894x(00)00277-8
14739892 206499 0 None - 0 Dog 5.9 pIC50 = 5.9 Binding
Tested for Beta-2 adrenergic receptor selectivity in canine lung tissue in anesthetized dogsTested for Beta-2 adrenergic receptor selectivity in canine lung tissue in anesthetized dogs
ChEMBL 337 8 2 5 2.7 Cc1ccccc1OCC(O)CNCc1ccc(-n2ccnc2)cc1 10.1021/jm00172a033
CHEMBL98773 206499 0 None - 0 Dog 5.9 pIC50 = 5.9 Binding
Tested for Beta-2 adrenergic receptor selectivity in canine lung tissue in anesthetized dogsTested for Beta-2 adrenergic receptor selectivity in canine lung tissue in anesthetized dogs
ChEMBL 337 8 2 5 2.7 Cc1ccccc1OCC(O)CNCc1ccc(-n2ccnc2)cc1 10.1021/jm00172a033
10347866 84569 1 None - 0 Human 4.9 pIC50 = 4.9 Binding
Binding affinity towards Beta-2 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindololBinding affinity towards Beta-2 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindolol
ChEMBL 563 15 3 8 4.3 CCCCCCn1ccn(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)c1=O 10.1016/s0960-894x(99)00073-6
CHEMBL22386 84569 1 None - 0 Human 4.9 pIC50 = 4.9 Binding
Binding affinity towards Beta-2 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindololBinding affinity towards Beta-2 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindolol
ChEMBL 563 15 3 8 4.3 CCCCCCn1ccn(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)c1=O 10.1016/s0960-894x(99)00073-6
44281074 114618 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Binding affinity towards Beta-2 adrenergic receptor prepared from CHO cells expressing the cloned human receptor in the presence of [125I]iodocyanopindololBinding affinity towards Beta-2 adrenergic receptor prepared from CHO cells expressing the cloned human receptor in the presence of [125I]iodocyanopindolol
ChEMBL 549 14 3 9 3.7 CCC(=O)CCc1nc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)no1 10.1016/s0960-894x(00)00267-5
CHEMBL33438 114618 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Binding affinity towards Beta-2 adrenergic receptor prepared from CHO cells expressing the cloned human receptor in the presence of [125I]iodocyanopindololBinding affinity towards Beta-2 adrenergic receptor prepared from CHO cells expressing the cloned human receptor in the presence of [125I]iodocyanopindolol
ChEMBL 549 14 3 9 3.7 CCC(=O)CCc1nc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)no1 10.1016/s0960-894x(00)00267-5
10347866 84569 1 None - 0 Human 4.9 pIC50 = 4.9 Binding
Binding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindololBinding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindolol
ChEMBL 563 15 3 8 4.3 CCCCCCn1ccn(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)c1=O 10.1016/s0960-894x(99)00072-4
CHEMBL22386 84569 1 None - 0 Human 4.9 pIC50 = 4.9 Binding
Binding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindololBinding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindolol
ChEMBL 563 15 3 8 4.3 CCCCCCn1ccn(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)c1=O 10.1016/s0960-894x(99)00072-4
10103956 11081 0 None - 2 Guinea pig 4.9 pIC50 = 4.9 Binding
Inhibitory concentration against beta-2-adrenergic receptor in isolated guinea pig tracheal stripsInhibitory concentration against beta-2-adrenergic receptor in isolated guinea pig tracheal strips
ChEMBL 188 7 2 4 0.8 CC/C=N/OCC(O)CNC(C)C 10.1021/jm00036a018
CHEMBL1178707 11081 0 None - 2 Guinea pig 4.9 pIC50 = 4.9 Binding
Inhibitory concentration against beta-2-adrenergic receptor in isolated guinea pig tracheal stripsInhibitory concentration against beta-2-adrenergic receptor in isolated guinea pig tracheal strips
ChEMBL 188 7 2 4 0.8 CC/C=N/OCC(O)CNC(C)C 10.1021/jm00036a018
CHEMBL38114 11081 0 None - 2 Guinea pig 4.9 pIC50 = 4.9 Binding
Inhibitory concentration against beta-2-adrenergic receptor in isolated guinea pig tracheal stripsInhibitory concentration against beta-2-adrenergic receptor in isolated guinea pig tracheal strips
ChEMBL 188 7 2 4 0.8 CC/C=N/OCC(O)CNC(C)C 10.1021/jm00036a018
24900811 70006 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 479 11 5 7 3.5 COc1ccccc1CNCc1ccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)cc1 10.1016/j.bmcl.2011.10.049
CHEMBL1945040 70006 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 479 11 5 7 3.5 COc1ccccc1CNCc1ccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)cc1 10.1016/j.bmcl.2011.10.049
57391792 70140 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 523 10 3 6 5.0 O=c1[nH]c2c(O)ccc(CCNCCc3ccc(CN4CC[C@@H](Oc5ccc(Cl)cc5)C4)cc3)c2s1 10.1016/j.bmcl.2011.10.049
CHEMBL1946764 70140 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 523 10 3 6 5.0 O=c1[nH]c2c(O)ccc(CCNCCc3ccc(CN4CC[C@@H](Oc5ccc(Cl)cc5)C4)cc3)c2s1 10.1016/j.bmcl.2011.10.049
57395240 70138 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 465 11 4 5 4.1 O=c1[nH]c2c(O)ccc(CCNCCc3ccc(CNCCc4ccccc4F)cc3)c2s1 10.1016/j.bmcl.2011.10.049
CHEMBL1946762 70138 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 465 11 4 5 4.1 O=c1[nH]c2c(O)ccc(CCNCCc3ccc(CNCCc4ccccc4F)cc3)c2s1 10.1016/j.bmcl.2011.10.049
11819522 11896 0 None - 2 Guinea pig 4.9 pIC50 = 4.9 Binding
Inhibitory concentration against beta-2-adrenergic receptor in isolated guinea pig tracheal stripsInhibitory concentration against beta-2-adrenergic receptor in isolated guinea pig tracheal strips
ChEMBL 174 6 2 4 0.4 C/C=N/OCC(O)CNC(C)C 10.1021/jm00036a018
CHEMBL1183318 11896 0 None - 2 Guinea pig 4.9 pIC50 = 4.9 Binding
Inhibitory concentration against beta-2-adrenergic receptor in isolated guinea pig tracheal stripsInhibitory concentration against beta-2-adrenergic receptor in isolated guinea pig tracheal strips
ChEMBL 174 6 2 4 0.4 C/C=N/OCC(O)CNC(C)C 10.1021/jm00036a018
CHEMBL290153 11896 0 None - 2 Guinea pig 4.9 pIC50 = 4.9 Binding
Inhibitory concentration against beta-2-adrenergic receptor in isolated guinea pig tracheal stripsInhibitory concentration against beta-2-adrenergic receptor in isolated guinea pig tracheal strips
ChEMBL 174 6 2 4 0.4 C/C=N/OCC(O)CNC(C)C 10.1021/jm00036a018
121347950 150688 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 ug/well for beta1 and 5 ug/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 ul, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 uM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 ug/well for beta1 and 5 ug/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 ul, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 uM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.
ChEMBL 728 14 5 12 5.1 CN(CCCn1nnc2cc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)ccc21)[C@H]1CC[C@H](OC(=O)[C@](O)(c2cccs2)C2CCCC2)CC1 nan
CHEMBL3960091 150688 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 ug/well for beta1 and 5 ug/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 ul, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 uM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 ug/well for beta1 and 5 ug/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 ul, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 uM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.
ChEMBL 728 14 5 12 5.1 CN(CCCn1nnc2cc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)ccc21)[C@H]1CC[C@H](OC(=O)[C@](O)(c2cccs2)C2CCCC2)CC1 nan
54673020 151042 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 μg/well for beta1 and 5 μg/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 μl, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 μM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 μg/well for beta1 and 5 μg/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 μl, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 μM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.
ChEMBL 766 14 6 11 5.5 CN(CCC(=O)Nc1cc(F)c(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1F)[C@H]1CC[C@H](OC(=O)C(O)(c2cccs2)c2cccs2)CC1 nan
CHEMBL3963417 151042 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 μg/well for beta1 and 5 μg/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 μl, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 μM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 μg/well for beta1 and 5 μg/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 μl, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 μM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.
ChEMBL 766 14 6 11 5.5 CN(CCC(=O)Nc1cc(F)c(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1F)[C@H]1CC[C@H](OC(=O)C(O)(c2cccs2)c2cccs2)CC1 nan
44268275 19398 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandBinding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligand
ChEMBL 484 14 4 6 3.3 O=S(=O)(CCCc1ccccc1)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/s0960-894x(98)00169-3
CHEMBL13003 19398 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandBinding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligand
ChEMBL 484 14 4 6 3.3 O=S(=O)(CCCc1ccccc1)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/s0960-894x(98)00169-3
44268520 21024 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.
ChEMBL 591 14 5 8 4.5 O=C(Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1)OCc1ccccc1 10.1016/s0960-894x(98)00170-x
CHEMBL13132 21024 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.
ChEMBL 591 14 5 8 4.5 O=C(Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1)OCc1ccccc1 10.1016/s0960-894x(98)00170-x
12049916 201296 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity for clone human Beta-2 adrenergic receptor from CHO cell membranes in the presence of I-iodocyanopindololBinding affinity for clone human Beta-2 adrenergic receptor from CHO cell membranes in the presence of I-iodocyanopindolol
ChEMBL 576 11 3 8 4.3 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-n2ncc(-c3ccc(F)c(F)c3)n2)cc1 10.1016/s0960-894x(00)00422-4
CHEMBL63138 201296 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity for clone human Beta-2 adrenergic receptor from CHO cell membranes in the presence of I-iodocyanopindololBinding affinity for clone human Beta-2 adrenergic receptor from CHO cell membranes in the presence of I-iodocyanopindolol
ChEMBL 576 11 3 8 4.3 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-n2ncc(-c3ccc(F)c(F)c3)n2)cc1 10.1016/s0960-894x(00)00422-4
10258518 101468 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cells
ChEMBL 633 17 3 8 6.8 CCCCCCCCc1csc(N2CCc3cc(S(=O)(=O)Nc4ccc(CCNC[C@H](O)c5cccnc5)cc4)ccc32)n1 10.1016/s0960-894x(00)00669-7
CHEMBL301231 101468 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cells
ChEMBL 633 17 3 8 6.8 CCCCCCCCc1csc(N2CCc3cc(S(=O)(=O)Nc4ccc(CCNC[C@H](O)c5cccnc5)cc4)ccc32)n1 10.1016/s0960-894x(00)00669-7
567 715 10 None - 5 Rat 5.9 pIC50 = 5.9 Binding
Compound was evaluated for its binding affinity towards Beta-2 adrenergic receptor in rat soleus membrane by displacing (-)-isoproterenol (50 uM)Compound was evaluated for its binding affinity towards Beta-2 adrenergic receptor in rat soleus membrane by displacing (-)-isoproterenol (50 uM)
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1021/jm00094a025
9841972 715 10 None - 5 Rat 5.9 pIC50 = 5.9 Binding
Compound was evaluated for its binding affinity towards Beta-2 adrenergic receptor in rat soleus membrane by displacing (-)-isoproterenol (50 uM)Compound was evaluated for its binding affinity towards Beta-2 adrenergic receptor in rat soleus membrane by displacing (-)-isoproterenol (50 uM)
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1021/jm00094a025
CHEMBL284782 715 10 None - 5 Rat 5.9 pIC50 = 5.9 Binding
Compound was evaluated for its binding affinity towards Beta-2 adrenergic receptor in rat soleus membrane by displacing (-)-isoproterenol (50 uM)Compound was evaluated for its binding affinity towards Beta-2 adrenergic receptor in rat soleus membrane by displacing (-)-isoproterenol (50 uM)
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1021/jm00094a025
12582 935 40 None -11 5 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]CGP1217 from human recombinant adrenergic beta2 receptor transfected in insect Sf9 cells by scintillation countingDisplacement of [3H]CGP1217 from human recombinant adrenergic beta2 receptor transfected in insect Sf9 cells by scintillation counting
ChEMBL 276 3 3 3 3.0 CC(C)(C)NCC(C1=CC(=C(C(=C1)Cl)N)Cl)O 10.1021/jm801211c
2783 935 40 None -11 5 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]CGP1217 from human recombinant adrenergic beta2 receptor transfected in insect Sf9 cells by scintillation countingDisplacement of [3H]CGP1217 from human recombinant adrenergic beta2 receptor transfected in insect Sf9 cells by scintillation counting
ChEMBL 276 3 3 3 3.0 CC(C)(C)NCC(C1=CC(=C(C(=C1)Cl)N)Cl)O 10.1021/jm801211c
CHEMBL49080 935 40 None -11 5 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]CGP1217 from human recombinant adrenergic beta2 receptor transfected in insect Sf9 cells by scintillation countingDisplacement of [3H]CGP1217 from human recombinant adrenergic beta2 receptor transfected in insect Sf9 cells by scintillation counting
ChEMBL 276 3 3 3 3.0 CC(C)(C)NCC(C1=CC(=C(C(=C1)Cl)N)Cl)O 10.1021/jm801211c
DB01407 935 40 None -11 5 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]CGP1217 from human recombinant adrenergic beta2 receptor transfected in insect Sf9 cells by scintillation countingDisplacement of [3H]CGP1217 from human recombinant adrenergic beta2 receptor transfected in insect Sf9 cells by scintillation counting
ChEMBL 276 3 3 3 3.0 CC(C)(C)NCC(C1=CC(=C(C(=C1)Cl)N)Cl)O 10.1021/jm801211c
44306991 201978 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cell
ChEMBL 493 11 4 8 2.6 Nc1ccc(OC[C@@H](O)CNCCc2ccc(NS(=O)(=O)c3cnc4ccccc4c3)cc2)cn1 10.1016/s0960-894x(98)00381-3
CHEMBL67461 201978 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cell
ChEMBL 493 11 4 8 2.6 Nc1ccc(OC[C@@H](O)CNCCc2ccc(NS(=O)(=O)c3cnc4ccccc4c3)cc2)cn1 10.1016/s0960-894x(98)00381-3
44298533 193324 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
In vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 469 11 1 5 6.5 CCCCCCCCc1csc(N2CCc3cc(S(=O)(=O)Nc4ccccc4)ccc32)n1 10.1016/s0960-894x(99)00277-2
CHEMBL54821 193324 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
In vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 469 11 1 5 6.5 CCCCCCCCc1csc(N2CCc3cc(S(=O)(=O)Nc4ccccc4)ccc32)n1 10.1016/s0960-894x(99)00277-2
44377753 119412 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Binding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindololBinding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindolol
ChEMBL 605 12 3 8 4.0 O=c1n(Cc2ccc(F)c(F)c2)ccn1-c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(99)00072-4
CHEMBL349505 119412 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Binding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindololBinding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindolol
ChEMBL 605 12 3 8 4.0 O=c1n(Cc2ccc(F)c(F)c2)ccn1-c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(99)00072-4
46881575 7687 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counter
ChEMBL 416 9 3 7 2.3 O=C(Cn1nc2ccccc2n1)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/j.bmcl.2010.01.130
CHEMBL1089387 7687 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counter
ChEMBL 416 9 3 7 2.3 O=C(Cn1nc2ccccc2n1)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/j.bmcl.2010.01.130
127041869 136569 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of [125I]CYP from human beta-2 adrenergic receptor expressed in CHO cell membrane after 1 hr by scintillation counting methodDisplacement of [125I]CYP from human beta-2 adrenergic receptor expressed in CHO cell membrane after 1 hr by scintillation counting method
ChEMBL 448 7 2 5 3.0 CCOC(=O)[C@@H]1[C@H]2CN(C(=O)c3ccc(C[C@@H]4CC[C@H]([C@H](O)c5ccccc5)N4)cc3)C[C@H]21 10.1016/j.bmcl.2015.11.030
CHEMBL3747546 136569 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of [125I]CYP from human beta-2 adrenergic receptor expressed in CHO cell membrane after 1 hr by scintillation counting methodDisplacement of [125I]CYP from human beta-2 adrenergic receptor expressed in CHO cell membrane after 1 hr by scintillation counting method
ChEMBL 448 7 2 5 3.0 CCOC(=O)[C@@H]1[C@H]2CN(C(=O)c3ccc(C[C@@H]4CC[C@H]([C@H](O)c5ccccc5)N4)cc3)C[C@H]21 10.1016/j.bmcl.2015.11.030
10406968 113245 0 None - 3 Guinea pig 7.9 pIC50 = 7.9 Binding
Agonist activity at adrenergic beta2 receptor in electrically-stimulated Dunkin-Hartley guinea pig tracheal strip assessed as inhibition of contractionAgonist activity at adrenergic beta2 receptor in electrically-stimulated Dunkin-Hartley guinea pig tracheal strip assessed as inhibition of contraction
ChEMBL 372 8 4 5 3.1 CCCc1ccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)cc1 10.1016/j.bmcl.2014.06.014
CHEMBL3323665 113245 0 None - 3 Guinea pig 7.9 pIC50 = 7.9 Binding
Agonist activity at adrenergic beta2 receptor in electrically-stimulated Dunkin-Hartley guinea pig tracheal strip assessed as inhibition of contractionAgonist activity at adrenergic beta2 receptor in electrically-stimulated Dunkin-Hartley guinea pig tracheal strip assessed as inhibition of contraction
ChEMBL 372 8 4 5 3.1 CCCc1ccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)cc1 10.1016/j.bmcl.2014.06.014
9956563 197172 1 None - 0 Human 7.9 pIC50 = 7.9 Binding
Inhibition of beta2 adrenergic receptorInhibition of beta2 adrenergic receptor
ChEMBL 474 12 2 6 4.6 CCOC(=O)CCc1ccc(OC[C@H](O)CNC(C)(C)Cc2ccc3ccccc3c2)c(C#N)c1 10.1021/jm900563e
CHEMBL1204009 197172 1 None - 0 Human 7.9 pIC50 = 7.9 Binding
Inhibition of beta2 adrenergic receptorInhibition of beta2 adrenergic receptor
ChEMBL 474 12 2 6 4.6 CCOC(=O)CCc1ccc(OC[C@H](O)CNC(C)(C)Cc2ccc3ccccc3c2)c(C#N)c1 10.1021/jm900563e
CHEMBL583889 197172 1 None - 0 Human 7.9 pIC50 = 7.9 Binding
Inhibition of beta2 adrenergic receptorInhibition of beta2 adrenergic receptor
ChEMBL 474 12 2 6 4.6 CCOC(=O)CCc1ccc(OC[C@H](O)CNC(C)(C)Cc2ccc3ccccc3c2)c(C#N)c1 10.1021/jm900563e
16736096 141552 0 None 19 2 Human 7.8 pIC50 = 7.8 Binding
Mitogenesis inhibition method: To measure beta2-AR mediated inhibition of mitogenesis, HEK-beta2-AR, 1321N1 or U87MG cells were seeded in a 96-well plate at approximately 5,000 cells/well. After 48 hours, the wells were rinsed twice and the medium was replaced with fresh medium containing 10 uL of drug in sterile water. After another 24 hours of incubation at 37° C., 0.25 uCi of [3H]-thymidine was added to each well. The cells were incubated for an additional 2 hours at 37° C., at which point 10 uL of 10x trypsin was added, and the resuspended cells were harvested using a Tomtec 96 harvester through glass fiber filters.Mitogenesis inhibition method: To measure beta2-AR mediated inhibition of mitogenesis, HEK-beta2-AR, 1321N1 or U87MG cells were seeded in a 96-well plate at approximately 5,000 cells/well. After 48 hours, the wells were rinsed twice and the medium was replaced with fresh medium containing 10 uL of drug in sterile water. After another 24 hours of incubation at 37° C., 0.25 uCi of [3H]-thymidine was added to each well. The cells were incubated for an additional 2 hours at 37° C., at which point 10 uL of 10x trypsin was added, and the resuspended cells were harvested using a Tomtec 96 harvester through glass fiber filters.
ChEMBL 337 6 4 4 3.5 C[C@H](Cc1cccc2ccccc12)NC[C@@H](O)c1cc(O)cc(O)c1 nan
CHEMBL388177 141552 0 None 19 2 Human 7.8 pIC50 = 7.8 Binding
Mitogenesis inhibition method: To measure beta2-AR mediated inhibition of mitogenesis, HEK-beta2-AR, 1321N1 or U87MG cells were seeded in a 96-well plate at approximately 5,000 cells/well. After 48 hours, the wells were rinsed twice and the medium was replaced with fresh medium containing 10 uL of drug in sterile water. After another 24 hours of incubation at 37° C., 0.25 uCi of [3H]-thymidine was added to each well. The cells were incubated for an additional 2 hours at 37° C., at which point 10 uL of 10x trypsin was added, and the resuspended cells were harvested using a Tomtec 96 harvester through glass fiber filters.Mitogenesis inhibition method: To measure beta2-AR mediated inhibition of mitogenesis, HEK-beta2-AR, 1321N1 or U87MG cells were seeded in a 96-well plate at approximately 5,000 cells/well. After 48 hours, the wells were rinsed twice and the medium was replaced with fresh medium containing 10 uL of drug in sterile water. After another 24 hours of incubation at 37° C., 0.25 uCi of [3H]-thymidine was added to each well. The cells were incubated for an additional 2 hours at 37° C., at which point 10 uL of 10x trypsin was added, and the resuspended cells were harvested using a Tomtec 96 harvester through glass fiber filters.
ChEMBL 337 6 4 4 3.5 C[C@H](Cc1cccc2ccccc12)NC[C@@H](O)c1cc(O)cc(O)c1 nan
71558563 143236 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 ug/well for beta1 and 5 ug/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 ul, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 uM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 ug/well for beta1 and 5 ug/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 ul, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 uM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.
ChEMBL 758 14 5 13 5.2 CN(CCCn1c(=O)oc2cc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)ccc21)[C@H]1CC[C@H](OC(=O)C(O)(c2cccs2)c2cccs2)CC1 nan
CHEMBL3900995 143236 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 ug/well for beta1 and 5 ug/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 ul, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 uM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 ug/well for beta1 and 5 ug/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 ul, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 uM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.
ChEMBL 758 14 5 13 5.2 CN(CCCn1c(=O)oc2cc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)ccc21)[C@H]1CC[C@H](OC(=O)C(O)(c2cccs2)c2cccs2)CC1 nan
10205362 116441 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cells
ChEMBL 468 8 4 5 4.4 N#CN/C(=N\c1cc(Cl)cc(Cl)c1)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/s0960-894x(00)00669-7
CHEMBL338618 116441 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cells
ChEMBL 468 8 4 5 4.4 N#CN/C(=N\c1cc(Cl)cc(Cl)c1)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/s0960-894x(00)00669-7
44298852 101260 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
In vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 435 9 1 4 5.7 CCCCCCc1cccc(N2CCc3cc(S(=O)(=O)Nc4ccccc4)ccc32)n1 10.1016/s0960-894x(99)00277-2
CHEMBL299719 101260 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
In vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 435 9 1 4 5.7 CCCCCCc1cccc(N2CCc3cc(S(=O)(=O)Nc4ccccc4)ccc32)n1 10.1016/s0960-894x(99)00277-2
25070577 111162 3 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity to adrenergic beta-2 receptor (unknown origin)Binding affinity to adrenergic beta-2 receptor (unknown origin)
ChEMBL 304 3 2 4 2.3 CNc1nc(C(F)(F)c2ccccc2)nc2c1CCNCC2 10.1021/jm5003292
CHEMBL3286557 111162 3 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity to adrenergic beta-2 receptor (unknown origin)Binding affinity to adrenergic beta-2 receptor (unknown origin)
ChEMBL 304 3 2 4 2.3 CNc1nc(C(F)(F)c2ccccc2)nc2c1CCNCC2 10.1021/jm5003292
12017006 99918 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.
ChEMBL 608 11 3 7 6.1 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2coc(-c3ccc(C(F)(F)F)cc3)n2)cc1 10.1016/s0960-894x(00)00277-8
CHEMBL290053 99918 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.
ChEMBL 608 11 3 7 6.1 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2coc(-c3ccc(C(F)(F)F)cc3)n2)cc1 10.1016/s0960-894x(00)00277-8
44281277 99702 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity towards Beta-2 adrenergic receptor prepared from CHO cells expressing the cloned human receptor in the presence of [125I]iodocyanopindololBinding affinity towards Beta-2 adrenergic receptor prepared from CHO cells expressing the cloned human receptor in the presence of [125I]iodocyanopindolol
ChEMBL 563 16 3 8 5.3 CCCCCCCc1nc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)no1 10.1016/s0960-894x(00)00267-5
CHEMBL288083 99702 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity towards Beta-2 adrenergic receptor prepared from CHO cells expressing the cloned human receptor in the presence of [125I]iodocyanopindololBinding affinity towards Beta-2 adrenergic receptor prepared from CHO cells expressing the cloned human receptor in the presence of [125I]iodocyanopindolol
ChEMBL 563 16 3 8 5.3 CCCCCCCc1nc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)no1 10.1016/s0960-894x(00)00267-5
44281400 109857 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindolol
ChEMBL 607 13 3 9 4.7 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2noc(COc3ccc(F)c(F)c3)n2)cc1 10.1016/s0960-894x(00)00268-7
CHEMBL32411 109857 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindolol
ChEMBL 607 13 3 9 4.7 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2noc(COc3ccc(F)c(F)c3)n2)cc1 10.1016/s0960-894x(00)00268-7
2249 509 106 None -33 12 Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C nan
255 509 106 None -33 12 Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C nan
548 509 106 None -33 12 Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C nan
CHEMBL24 509 106 None -33 12 Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C nan
DB00335 509 106 None -33 12 Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C nan
24900812 70009 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 450 10 5 7 2.8 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3cccc(CNCc4ccccn4)c3)c2s1 10.1016/j.bmcl.2011.10.049
CHEMBL1945043 70009 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 450 10 5 7 2.8 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3cccc(CNCc4ccccn4)c3)c2s1 10.1016/j.bmcl.2011.10.049
57402061 70173 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 521 9 3 5 5.9 O=c1[nH]c2c(O)ccc(CCNCCc3ccc(-c4cccc(CN5Cc6ccccc6C5)c4)cc3)c2s1 10.1016/j.bmcl.2011.10.049
CHEMBL1947150 70173 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 521 9 3 5 5.9 O=c1[nH]c2c(O)ccc(CCNCCc3ccc(-c4cccc(CN5Cc6ccccc6C5)c4)cc3)c2s1 10.1016/j.bmcl.2011.10.049
44268322 18768 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandBinding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligand
ChEMBL 303 8 4 5 1.7 Oc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/s0960-894x(98)00169-3
CHEMBL12876 18768 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandBinding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligand
ChEMBL 303 8 4 5 1.7 Oc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/s0960-894x(98)00169-3
44307396 202046 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cell
ChEMBL 582 12 3 6 3.7 COc1ccc(OC[C@@H](O)CNCCc2ccc(NS(=O)(=O)c3ccc(I)cc3)cc2)cc1 10.1016/s0960-894x(98)00381-3
CHEMBL67886 202046 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cell
ChEMBL 582 12 3 6 3.7 COc1ccc(OC[C@@H](O)CNCCc2ccc(NS(=O)(=O)c3ccc(I)cc3)cc2)cc1 10.1016/s0960-894x(98)00381-3
44280903 99485 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindolol
ChEMBL 605 12 3 8 5.5 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2noc(Cc3ccc4ccccc4c3)n2)cc1 10.1016/s0960-894x(00)00268-7
CHEMBL286437 99485 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindolol
ChEMBL 605 12 3 8 5.5 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2noc(Cc3ccc4ccccc4c3)n2)cc1 10.1016/s0960-894x(00)00268-7
44281218 155158 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindolol
ChEMBL 645 13 5 9 4.0 CNC(=O)NC(c1ccc(F)cc1)c1nc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)no1 10.1016/s0960-894x(00)00268-7
CHEMBL405245 155158 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindolol
ChEMBL 645 13 5 9 4.0 CNC(=O)NC(c1ccc(F)cc1)c1nc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)no1 10.1016/s0960-894x(00)00268-7
44298823 100796 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
In vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 462 11 1 3 7.1 CCCCCCCCc1cccc(N2CCc3cc(S(=O)(=O)Nc4ccccc4)ccc32)c1 10.1016/s0960-894x(99)00277-2
CHEMBL296380 100796 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
In vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 462 11 1 3 7.1 CCCCCCCCc1cccc(N2CCc3cc(S(=O)(=O)Nc4ccccc4)ccc32)c1 10.1016/s0960-894x(99)00277-2
10673684 161646 0 None - 0 Dog 5.8 pIC50 = 5.8 Binding
Inhibition of beta-2 adrenergic receptor isolated from rat lung homogenatesInhibition of beta-2 adrenergic receptor isolated from rat lung homogenates
ChEMBL 526 18 4 8 4.1 CC(C)(Cc1ccc(NCC(O)CON=C(C2CC2)C2CC2)cc1)NCC(O)CON=C(C1CC1)C1CC1 10.1021/jm970338c
CHEMBL41628 161646 0 None - 0 Dog 5.8 pIC50 = 5.8 Binding
Inhibition of beta-2 adrenergic receptor isolated from rat lung homogenatesInhibition of beta-2 adrenergic receptor isolated from rat lung homogenates
ChEMBL 526 18 4 8 4.1 CC(C)(Cc1ccc(NCC(O)CON=C(C2CC2)C2CC2)cc1)NCC(O)CON=C(C1CC1)C1CC1 10.1021/jm970338c
24882564 154803 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Binding affinity to GST tagged human beta 2 adrenergic receptor PDZ1 domainBinding affinity to GST tagged human beta 2 adrenergic receptor PDZ1 domain
ChEMBL 409 10 3 4 4.2 Cc1cc2c(CO)c(CCCCC(=O)O)n(CCc3ccccc3)c2cc1C(=O)O 10.1016/j.bmcl.2007.12.038
CHEMBL403297 154803 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Binding affinity to GST tagged human beta 2 adrenergic receptor PDZ1 domainBinding affinity to GST tagged human beta 2 adrenergic receptor PDZ1 domain
ChEMBL 409 10 3 4 4.2 Cc1cc2c(CO)c(CCCCC(=O)O)n(CCc3ccccc3)c2cc1C(=O)O 10.1016/j.bmcl.2007.12.038
44281424 99829 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Binding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindolol
ChEMBL 587 12 3 9 4.2 O=C(c1ccc(F)cc1)c1nc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)no1 10.1016/s0960-894x(00)00268-7
CHEMBL289249 99829 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Binding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindolol
ChEMBL 587 12 3 9 4.2 O=C(c1ccc(F)cc1)c1nc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)no1 10.1016/s0960-894x(00)00268-7
46845698 5690 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counter
ChEMBL 444 9 3 5 4.1 Cc1ccc(N2CCCC2)c(C(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)c1 10.1016/j.bmcl.2010.01.130
CHEMBL1078696 5690 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counter
ChEMBL 444 9 3 5 4.1 Cc1ccc(N2CCCC2)c(C(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)c1 10.1016/j.bmcl.2010.01.130
46881573 8174 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counter
ChEMBL 415 9 3 6 2.9 O=C(Cn1ncc2ccccc21)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/j.bmcl.2010.01.130
CHEMBL1092502 8174 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counter
ChEMBL 415 9 3 6 2.9 O=C(Cn1ncc2ccccc21)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/j.bmcl.2010.01.130
36811 1421 34 None -51 7 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 301 7 4 4 3.0 CC(CCc1ccc(cc1)O)NCCc1ccc(c(c1)O)O nan
535 1421 34 None -51 7 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 301 7 4 4 3.0 CC(CCc1ccc(cc1)O)NCCc1ccc(c(c1)O)O nan
937 1421 34 None -51 7 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 301 7 4 4 3.0 CC(CCc1ccc(cc1)O)NCCc1ccc(c(c1)O)O nan
CHEMBL926 1421 34 None -51 7 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 301 7 4 4 3.0 CC(CCc1ccc(cc1)O)NCCc1ccc(c(c1)O)O nan
DB00841 1421 34 None -51 7 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 301 7 4 4 3.0 CC(CCc1ccc(cc1)O)NCCc1ccc(c(c1)O)O nan
10081581 11080 0 None - 2 Guinea pig 5.8 pIC50 = 5.8 Binding
Inhibitory concentration against beta-2-adrenergic receptor in isolated guinea pig tracheal stripsInhibitory concentration against beta-2-adrenergic receptor in isolated guinea pig tracheal strips
ChEMBL 202 6 2 4 1.1 CC/C=N/OCC(O)CNC(C)(C)C 10.1021/jm00036a018
CHEMBL1178704 11080 0 None - 2 Guinea pig 5.8 pIC50 = 5.8 Binding
Inhibitory concentration against beta-2-adrenergic receptor in isolated guinea pig tracheal stripsInhibitory concentration against beta-2-adrenergic receptor in isolated guinea pig tracheal strips
ChEMBL 202 6 2 4 1.1 CC/C=N/OCC(O)CNC(C)(C)C 10.1021/jm00036a018
CHEMBL38033 11080 0 None - 2 Guinea pig 5.8 pIC50 = 5.8 Binding
Inhibitory concentration against beta-2-adrenergic receptor in isolated guinea pig tracheal stripsInhibitory concentration against beta-2-adrenergic receptor in isolated guinea pig tracheal strips
ChEMBL 202 6 2 4 1.1 CC/C=N/OCC(O)CNC(C)(C)C 10.1021/jm00036a018
9984028 119208 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Receptor binding assay(Beta-2 adrenergic receptor) carried out with membranes prepared from human recombinant Sf9 cells expressing the cloned human receptor in the presence of [125I]iodocyanopindololReceptor binding assay(Beta-2 adrenergic receptor) carried out with membranes prepared from human recombinant Sf9 cells expressing the cloned human receptor in the presence of [125I]iodocyanopindolol
ChEMBL 515 11 4 6 3.8 Cc1ccc(S(=O)(=O)NC(=O)Cc2cccc(NC[C@@H](C)NC[C@H](O)c3cccc(Cl)c3)c2)cc1 10.1021/jm0101500
CHEMBL347582 119208 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Receptor binding assay(Beta-2 adrenergic receptor) carried out with membranes prepared from human recombinant Sf9 cells expressing the cloned human receptor in the presence of [125I]iodocyanopindololReceptor binding assay(Beta-2 adrenergic receptor) carried out with membranes prepared from human recombinant Sf9 cells expressing the cloned human receptor in the presence of [125I]iodocyanopindolol
ChEMBL 515 11 4 6 3.8 Cc1ccc(S(=O)(=O)NC(=O)Cc2cccc(NC[C@@H](C)NC[C@H](O)c3cccc(Cl)c3)c2)cc1 10.1021/jm0101500
1531 2226 64 None -1 15 Human 7.8 pIC50 = 7.8 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O nan
3869 2226 64 None -1 15 Human 7.8 pIC50 = 7.8 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O nan
7207 2226 64 None -1 15 Human 7.8 pIC50 = 7.8 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O nan
CHEMBL429 2226 64 None -1 15 Human 7.8 pIC50 = 7.8 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O nan
DB00598 2226 64 None -1 15 Human 7.8 pIC50 = 7.8 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O nan
12049918 101727 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity for clone human Beta-2 adrenergic receptor from CHO cell membranes in the presence of I-iodocyanopindololBinding affinity for clone human Beta-2 adrenergic receptor from CHO cell membranes in the presence of I-iodocyanopindolol
ChEMBL 624 12 3 9 4.9 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-n2ncc(-c3ccc(OC(F)(F)F)cc3)n2)cc1 10.1016/s0960-894x(00)00422-4
CHEMBL302893 101727 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity for clone human Beta-2 adrenergic receptor from CHO cell membranes in the presence of I-iodocyanopindololBinding affinity for clone human Beta-2 adrenergic receptor from CHO cell membranes in the presence of I-iodocyanopindolol
ChEMBL 624 12 3 9 4.9 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-n2ncc(-c3ccc(OC(F)(F)F)cc3)n2)cc1 10.1016/s0960-894x(00)00422-4
183520 166012 3 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]-CGP-12177 from human beta2-adrenergic receptorDisplacement of [3H]-CGP-12177 from human beta2-adrenergic receptor
ChEMBL 297 2 2 4 2.6 COc1cc2c3c(c1OC)-c1ccccc1[C@H](O)[C@H]3NCC2 10.1039/C7MD00656J
CHEMBL4279962 166012 3 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]-CGP-12177 from human beta2-adrenergic receptorDisplacement of [3H]-CGP-12177 from human beta2-adrenergic receptor
ChEMBL 297 2 2 4 2.6 COc1cc2c3c(c1OC)-c1ccccc1[C@H](O)[C@H]3NCC2 10.1039/C7MD00656J
9873257 84507 12 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibitory activity against cloned human Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol in CHO cells by receptor binding assayInhibitory activity against cloned human Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol in CHO cells by receptor binding assay
ChEMBL 591 14 3 10 3.5 O=c1n(CCCC2CCCC2)nnn1-c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(99)00182-1
CHEMBL22375 84507 12 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibitory activity against cloned human Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol in CHO cells by receptor binding assayInhibitory activity against cloned human Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol in CHO cells by receptor binding assay
ChEMBL 591 14 3 10 3.5 O=c1n(CCCC2CCCC2)nnn1-c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(99)00182-1
44301886 100597 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Binding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindololBinding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindolol
ChEMBL 607 16 4 8 4.7 CC(=O)NCCCCCc1csc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)n1 10.1016/s0960-894x(00)00390-5
CHEMBL294849 100597 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Binding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindololBinding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindolol
ChEMBL 607 16 4 8 4.7 CC(=O)NCCCCCc1csc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)n1 10.1016/s0960-894x(00)00390-5
415628 206441 89 None - 5 Dog 4.8 pIC50 = 4.8 Binding
Binding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprololBinding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprolol
ChEMBL 196 1 1 2 1.8 Clc1ccccc1N1CCNCC1 10.1021/jm00082a016
CHEMBL9841 206441 89 None - 5 Dog 4.8 pIC50 = 4.8 Binding
Binding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprololBinding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprolol
ChEMBL 196 1 1 2 1.8 Clc1ccccc1N1CCNCC1 10.1021/jm00082a016
46845699 5712 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counter
ChEMBL 444 9 3 5 4.1 Cc1ccc(C(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)c(N2CCCC2)c1 10.1016/j.bmcl.2010.01.130
CHEMBL1078876 5712 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counter
ChEMBL 444 9 3 5 4.1 Cc1ccc(C(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)c(N2CCCC2)c1 10.1016/j.bmcl.2010.01.130
46881872 7650 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counter
ChEMBL 411 10 4 7 2.6 CNc1nc(CC(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cs1 10.1016/j.bmcl.2010.01.130
CHEMBL1089052 7650 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counter
ChEMBL 411 10 4 7 2.6 CNc1nc(CC(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cs1 10.1016/j.bmcl.2010.01.130
9938030 99550 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindolol
ChEMBL 573 12 3 8 4.5 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2noc(Cc3ccc(F)cc3)n2)cc1 10.1016/s0960-894x(00)00268-7
CHEMBL286859 99550 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindolol
ChEMBL 573 12 3 8 4.5 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2noc(Cc3ccc(F)cc3)n2)cc1 10.1016/s0960-894x(00)00268-7
165193 3126 60 None -1 43 Dog 7.8 pIC50 = 7.8 Binding
Tested for Beta-2 adrenergic receptor selectivity in canine lung tissue in anesthetized dogsTested for Beta-2 adrenergic receptor selectivity in canine lung tissue in anesthetized dogs
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00172a033
2303 3126 60 None -1 43 Dog 7.8 pIC50 = 7.8 Binding
Tested for Beta-2 adrenergic receptor selectivity in canine lung tissue in anesthetized dogsTested for Beta-2 adrenergic receptor selectivity in canine lung tissue in anesthetized dogs
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00172a033
4946 3126 60 None -1 43 Dog 7.8 pIC50 = 7.8 Binding
Tested for Beta-2 adrenergic receptor selectivity in canine lung tissue in anesthetized dogsTested for Beta-2 adrenergic receptor selectivity in canine lung tissue in anesthetized dogs
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00172a033
564 3126 60 None -1 43 Dog 7.8 pIC50 = 7.8 Binding
Tested for Beta-2 adrenergic receptor selectivity in canine lung tissue in anesthetized dogsTested for Beta-2 adrenergic receptor selectivity in canine lung tissue in anesthetized dogs
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00172a033
62882 3126 60 None -1 43 Dog 7.8 pIC50 = 7.8 Binding
Tested for Beta-2 adrenergic receptor selectivity in canine lung tissue in anesthetized dogsTested for Beta-2 adrenergic receptor selectivity in canine lung tissue in anesthetized dogs
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00172a033
63 3126 60 None -1 43 Dog 7.8 pIC50 = 7.8 Binding
Tested for Beta-2 adrenergic receptor selectivity in canine lung tissue in anesthetized dogsTested for Beta-2 adrenergic receptor selectivity in canine lung tissue in anesthetized dogs
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00172a033
66366 3126 60 None -1 43 Dog 7.8 pIC50 = 7.8 Binding
Tested for Beta-2 adrenergic receptor selectivity in canine lung tissue in anesthetized dogsTested for Beta-2 adrenergic receptor selectivity in canine lung tissue in anesthetized dogs
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00172a033
91536 3126 60 None -1 43 Dog 7.8 pIC50 = 7.8 Binding
Tested for Beta-2 adrenergic receptor selectivity in canine lung tissue in anesthetized dogsTested for Beta-2 adrenergic receptor selectivity in canine lung tissue in anesthetized dogs
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00172a033
CHEMBL27 3126 60 None -1 43 Dog 7.8 pIC50 = 7.8 Binding
Tested for Beta-2 adrenergic receptor selectivity in canine lung tissue in anesthetized dogsTested for Beta-2 adrenergic receptor selectivity in canine lung tissue in anesthetized dogs
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00172a033
CHEMBL452861 3126 60 None -1 43 Dog 7.8 pIC50 = 7.8 Binding
Tested for Beta-2 adrenergic receptor selectivity in canine lung tissue in anesthetized dogsTested for Beta-2 adrenergic receptor selectivity in canine lung tissue in anesthetized dogs
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00172a033
DB00571 3126 60 None -1 43 Dog 7.8 pIC50 = 7.8 Binding
Tested for Beta-2 adrenergic receptor selectivity in canine lung tissue in anesthetized dogsTested for Beta-2 adrenergic receptor selectivity in canine lung tissue in anesthetized dogs
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00172a033
44276727 96852 0 None - 3 Bovine 7.8 pIC50 = 7.8 Binding
Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-2 adrenergic receptor in calf lung membranes.Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-2 adrenergic receptor in calf lung membranes.
ChEMBL 263 6 2 3 2.2 Cc1ccc(OCC(O)CNC(C)C)c2c1CCC2 10.1021/jm00350a009
CHEMBL26917 96852 0 None - 3 Bovine 7.8 pIC50 = 7.8 Binding
Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-2 adrenergic receptor in calf lung membranes.Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-2 adrenergic receptor in calf lung membranes.
ChEMBL 263 6 2 3 2.2 Cc1ccc(OCC(O)CNC(C)C)c2c1CCC2 10.1021/jm00350a009
56663519 63299 0 None - 1 Human 7.8 pIC50 = 7.8 Binding
Mitogenesis inhibition method: To measure beta2-AR mediated inhibition of mitogenesis, HEK-beta2-AR, 1321N1 or U87MG cells were seeded in a 96-well plate at approximately 5,000 cells/well. After 48 hours, the wells were rinsed twice and the medium was replaced with fresh medium containing 10 uL of drug in sterile water. After another 24 hours of incubation at 37° C., 0.25 uCi of [3H]-thymidine was added to each well. The cells were incubated for an additional 2 hours at 37° C., at which point 10 uL of 10x trypsin was added, and the resuspended cells were harvested using a Tomtec 96 harvester through glass fiber filters.Mitogenesis inhibition method: To measure beta2-AR mediated inhibition of mitogenesis, HEK-beta2-AR, 1321N1 or U87MG cells were seeded in a 96-well plate at approximately 5,000 cells/well. After 48 hours, the wells were rinsed twice and the medium was replaced with fresh medium containing 10 uL of drug in sterile water. After another 24 hours of incubation at 37° C., 0.25 uCi of [3H]-thymidine was added to each well. The cells were incubated for an additional 2 hours at 37° C., at which point 10 uL of 10x trypsin was added, and the resuspended cells were harvested using a Tomtec 96 harvester through glass fiber filters.
ChEMBL 317 7 5 5 2.4 CC[C@@H](Cc1ccc(O)cc1)NC[C@H](O)c1cc(O)cc(O)c1 nan
CHEMBL1800960 63299 0 None - 1 Human 7.8 pIC50 = 7.8 Binding
Mitogenesis inhibition method: To measure beta2-AR mediated inhibition of mitogenesis, HEK-beta2-AR, 1321N1 or U87MG cells were seeded in a 96-well plate at approximately 5,000 cells/well. After 48 hours, the wells were rinsed twice and the medium was replaced with fresh medium containing 10 uL of drug in sterile water. After another 24 hours of incubation at 37° C., 0.25 uCi of [3H]-thymidine was added to each well. The cells were incubated for an additional 2 hours at 37° C., at which point 10 uL of 10x trypsin was added, and the resuspended cells were harvested using a Tomtec 96 harvester through glass fiber filters.Mitogenesis inhibition method: To measure beta2-AR mediated inhibition of mitogenesis, HEK-beta2-AR, 1321N1 or U87MG cells were seeded in a 96-well plate at approximately 5,000 cells/well. After 48 hours, the wells were rinsed twice and the medium was replaced with fresh medium containing 10 uL of drug in sterile water. After another 24 hours of incubation at 37° C., 0.25 uCi of [3H]-thymidine was added to each well. The cells were incubated for an additional 2 hours at 37° C., at which point 10 uL of 10x trypsin was added, and the resuspended cells were harvested using a Tomtec 96 harvester through glass fiber filters.
ChEMBL 317 7 5 5 2.4 CC[C@@H](Cc1ccc(O)cc1)NC[C@H](O)c1cc(O)cc(O)c1 nan
44268320 18227 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandBinding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligand
ChEMBL 456 11 4 6 3.1 Cc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/s0960-894x(98)00169-3
CHEMBL12718 18227 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandBinding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligand
ChEMBL 456 11 4 6 3.1 Cc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/s0960-894x(98)00169-3
10119061 17759 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cells
ChEMBL 526 8 4 5 3.7 N#CN/C(=N\c1ccc(I)cc1)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/s0960-894x(00)00669-7
CHEMBL126055 17759 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cells
ChEMBL 526 8 4 5 3.7 N#CN/C(=N\c1ccc(I)cc1)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/s0960-894x(00)00669-7
44268495 24811 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.
ChEMBL 612 19 6 7 5.2 CCCCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/s0960-894x(98)00170-x
CHEMBL13467 24811 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.
ChEMBL 612 19 6 7 5.2 CCCCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/s0960-894x(98)00170-x
11758172 100454 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindololBinding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindolol
ChEMBL 592 11 3 7 5.8 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3ccc(F)c(F)c3)cs2)cc1 10.1016/s0960-894x(00)00390-5
CHEMBL293994 100454 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindololBinding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindolol
ChEMBL 592 11 3 7 5.8 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3ccc(F)c(F)c3)cs2)cc1 10.1016/s0960-894x(00)00390-5
11758172 100454 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity was evaluated on chinese hamster ovary (CHO) cells expressing the cloned human beta-2 adrenergic receptor in the presence of [125I]- iodocyanopindolol.Binding affinity was evaluated on chinese hamster ovary (CHO) cells expressing the cloned human beta-2 adrenergic receptor in the presence of [125I]- iodocyanopindolol.
ChEMBL 592 11 3 7 5.8 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3ccc(F)c(F)c3)cs2)cc1 10.1021/jm000286i
CHEMBL293994 100454 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity was evaluated on chinese hamster ovary (CHO) cells expressing the cloned human beta-2 adrenergic receptor in the presence of [125I]- iodocyanopindolol.Binding affinity was evaluated on chinese hamster ovary (CHO) cells expressing the cloned human beta-2 adrenergic receptor in the presence of [125I]- iodocyanopindolol.
ChEMBL 592 11 3 7 5.8 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3ccc(F)c(F)c3)cs2)cc1 10.1021/jm000286i
46881982 5660 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counter
ChEMBL 465 11 3 4 5.0 O=C(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccccc1CCc1ccccc1 10.1016/j.bmcl.2010.01.130
CHEMBL1078465 5660 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counter
ChEMBL 465 11 3 4 5.0 O=C(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccccc1CCc1ccccc1 10.1016/j.bmcl.2010.01.130
46881651 6768 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counter
ChEMBL 458 10 3 6 4.3 O=C(Cc1nc(-c2ccccc2)cs1)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/j.bmcl.2010.01.130
CHEMBL1084137 6768 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counter
ChEMBL 458 10 3 6 4.3 O=C(Cc1nc(-c2ccccc2)cs1)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/j.bmcl.2010.01.130
46881618 7917 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counter
ChEMBL 458 10 3 6 4.3 O=C(Cc1csc(-c2ccccc2)n1)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/j.bmcl.2010.01.130
CHEMBL1090746 7917 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counter
ChEMBL 458 10 3 6 4.3 O=C(Cc1csc(-c2ccccc2)n1)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/j.bmcl.2010.01.130
46917559 1523 8 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of beta2 adrenergic receptorInhibition of beta2 adrenergic receptor
ChEMBL 513 11 3 4 6.2 O[C@H](CNC(Cc1ccc(c(c1)F)Cl)(C)C)CO[C@@H](c1ccccc1c1ccc(c(c1)C)C(=O)O)C 10.1021/ml100268k
9474 1523 8 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of beta2 adrenergic receptorInhibition of beta2 adrenergic receptor
ChEMBL 513 11 3 4 6.2 O[C@H](CNC(Cc1ccc(c(c1)F)Cl)(C)C)CO[C@@H](c1ccccc1c1ccc(c(c1)C)C(=O)O)C 10.1021/ml100268k
CHEMBL1672973 1523 8 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of beta2 adrenergic receptorInhibition of beta2 adrenergic receptor
ChEMBL 513 11 3 4 6.2 O[C@H](CNC(Cc1ccc(c(c1)F)Cl)(C)C)CO[C@@H](c1ccccc1c1ccc(c(c1)C)C(=O)O)C 10.1021/ml100268k
71559319 151958 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 ug/well for beta1 and 5 ug/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 ul, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 uM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 ug/well for beta1 and 5 ug/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 ul, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 uM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.
ChEMBL 760 16 6 12 4.4 CN(CCNC(=O)COc1ccc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1)[C@H]1CC[C@H](OC(=O)C(O)(c2cccs2)c2cccs2)CC1 nan
CHEMBL3971284 151958 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 ug/well for beta1 and 5 ug/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 ul, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 uM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 ug/well for beta1 and 5 ug/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 ul, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 uM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.
ChEMBL 760 16 6 12 4.4 CN(CCNC(=O)COc1ccc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1)[C@H]1CC[C@H](OC(=O)C(O)(c2cccs2)c2cccs2)CC1 nan
10075383 96645 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandBinding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligand
ChEMBL 520 11 4 6 3.5 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1)c1ccc(Br)cc1 10.1016/s0960-894x(98)00169-3
CHEMBL267545 96645 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandBinding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligand
ChEMBL 520 11 4 6 3.5 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1)c1ccc(Br)cc1 10.1016/s0960-894x(98)00169-3
9917962 167382 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cells
ChEMBL 684 11 4 9 6.8 N#CN/C(=N\c1ccc2c(c1)CCN2c1nc(-c2ccc(OC(F)(F)F)cc2)cs1)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/s0960-894x(00)00669-7
CHEMBL431678 167382 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cells
ChEMBL 684 11 4 9 6.8 N#CN/C(=N\c1ccc2c(c1)CCN2c1nc(-c2ccc(OC(F)(F)F)cc2)cs1)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/s0960-894x(00)00669-7
44298821 193315 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
In vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 453 11 1 5 6.1 CCCCCCCCc1cnc(N2CCc3cc(S(=O)(=O)Nc4ccccc4)ccc32)o1 10.1016/s0960-894x(99)00277-2
CHEMBL54749 193315 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
In vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 453 11 1 5 6.1 CCCCCCCCc1cnc(N2CCc3cc(S(=O)(=O)Nc4ccccc4)ccc32)o1 10.1016/s0960-894x(99)00277-2
10746499 113947 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity was evaluated on chinese hamster ovary (CHO) cells expressing the cloned human beta-2 adrenergic receptor in the presence of [125I]- iodocyanopindolol.Binding affinity was evaluated on chinese hamster ovary (CHO) cells expressing the cloned human beta-2 adrenergic receptor in the presence of [125I]- iodocyanopindolol.
ChEMBL 624 11 3 7 6.6 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3ccccc3C(F)(F)F)cs2)cc1 10.1021/jm000286i
CHEMBL333417 113947 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity was evaluated on chinese hamster ovary (CHO) cells expressing the cloned human beta-2 adrenergic receptor in the presence of [125I]- iodocyanopindolol.Binding affinity was evaluated on chinese hamster ovary (CHO) cells expressing the cloned human beta-2 adrenergic receptor in the presence of [125I]- iodocyanopindolol.
ChEMBL 624 11 3 7 6.6 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3ccccc3C(F)(F)F)cs2)cc1 10.1021/jm000286i
10099346 140529 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.
ChEMBL 560 13 3 7 5.5 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2cnc(CCC3CCCC3)o2)cc1 10.1016/s0960-894x(00)00277-8
CHEMBL38254 140529 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.
ChEMBL 560 13 3 7 5.5 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2cnc(CCC3CCCC3)o2)cc1 10.1016/s0960-894x(00)00277-8
1355 1972 82 None - 16 Dog 4.8 pIC50 = 4.8 Binding
Binding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprololBinding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprolol
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm00082a016
142 1972 82 None - 16 Dog 4.8 pIC50 = 4.8 Binding
Binding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprololBinding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprolol
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm00082a016
CHEMBL478 1972 82 None - 16 Dog 4.8 pIC50 = 4.8 Binding
Binding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprololBinding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprolol
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm00082a016
DB12110 1972 82 None - 16 Dog 4.8 pIC50 = 4.8 Binding
Binding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprololBinding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprolol
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm00082a016
53246941 69064 36 None - 0 Human 5.7 pIC50 = 5.7 Binding
Selectivity interaction (Enzyme panel (receptors, ion channels, other enzymes)) EUB0000679a ADRB2Selectivity interaction (Enzyme panel (receptors, ion channels, other enzymes)) EUB0000679a ADRB2
ChEMBL 458 6 2 6 3.9 C[C@@H]1CCNC(=O)c2cc3ccc(C(=O)Nc4nc5ccccc5n4CCCN(C)C)cc3n21 nan
CHEMBL1933288 69064 36 None - 0 Human 5.7 pIC50 = 5.7 Binding
Selectivity interaction (Enzyme panel (receptors, ion channels, other enzymes)) EUB0000679a ADRB2Selectivity interaction (Enzyme panel (receptors, ion channels, other enzymes)) EUB0000679a ADRB2
ChEMBL 458 6 2 6 3.9 C[C@@H]1CCNC(=O)c2cc3ccc(C(=O)Nc4nc5ccccc5n4CCCN(C)C)cc3n21 nan
688469 142383 2 None - 1 Human 6.7 pIC50 = 6.7 Binding
Mitogenesis inhibition method: To measure beta2-AR mediated inhibition of mitogenesis, HEK-beta2-AR, 1321N1 or U87MG cells were seeded in a 96-well plate at approximately 5,000 cells/well. After 48 hours, the wells were rinsed twice and the medium was replaced with fresh medium containing 10 uL of drug in sterile water. After another 24 hours of incubation at 37° C., 0.25 uCi of [3H]-thymidine was added to each well. The cells were incubated for an additional 2 hours at 37° C., at which point 10 uL of 10x trypsin was added, and the resuspended cells were harvested using a Tomtec 96 harvester through glass fiber filters.Mitogenesis inhibition method: To measure beta2-AR mediated inhibition of mitogenesis, HEK-beta2-AR, 1321N1 or U87MG cells were seeded in a 96-well plate at approximately 5,000 cells/well. After 48 hours, the wells were rinsed twice and the medium was replaced with fresh medium containing 10 uL of drug in sterile water. After another 24 hours of incubation at 37° C., 0.25 uCi of [3H]-thymidine was added to each well. The cells were incubated for an additional 2 hours at 37° C., at which point 10 uL of 10x trypsin was added, and the resuspended cells were harvested using a Tomtec 96 harvester through glass fiber filters.
ChEMBL 303 6 5 5 2.1 C[C@@H](Cc1ccc(O)cc1)NC[C@@H](O)c1cc(O)cc(O)c1 nan
CHEMBL389390 142383 2 None - 1 Human 6.7 pIC50 = 6.7 Binding
Mitogenesis inhibition method: To measure beta2-AR mediated inhibition of mitogenesis, HEK-beta2-AR, 1321N1 or U87MG cells were seeded in a 96-well plate at approximately 5,000 cells/well. After 48 hours, the wells were rinsed twice and the medium was replaced with fresh medium containing 10 uL of drug in sterile water. After another 24 hours of incubation at 37° C., 0.25 uCi of [3H]-thymidine was added to each well. The cells were incubated for an additional 2 hours at 37° C., at which point 10 uL of 10x trypsin was added, and the resuspended cells were harvested using a Tomtec 96 harvester through glass fiber filters.Mitogenesis inhibition method: To measure beta2-AR mediated inhibition of mitogenesis, HEK-beta2-AR, 1321N1 or U87MG cells were seeded in a 96-well plate at approximately 5,000 cells/well. After 48 hours, the wells were rinsed twice and the medium was replaced with fresh medium containing 10 uL of drug in sterile water. After another 24 hours of incubation at 37° C., 0.25 uCi of [3H]-thymidine was added to each well. The cells were incubated for an additional 2 hours at 37° C., at which point 10 uL of 10x trypsin was added, and the resuspended cells were harvested using a Tomtec 96 harvester through glass fiber filters.
ChEMBL 303 6 5 5 2.1 C[C@@H](Cc1ccc(O)cc1)NC[C@@H](O)c1cc(O)cc(O)c1 nan
155526570 170586 0 None 999 2 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at human recombinant beta2 adrenoreceptor expressed in CHOK1 cells incubated for 30 mins by HTRFAntagonist activity at human recombinant beta2 adrenoreceptor expressed in CHOK1 cells incubated for 30 mins by HTRF
ChEMBL 471 20 4 8 1.2 CC(C)NCC(O)COc1ccccc1CCCSCC(=O)NCCOCCOCCN 10.1039/C8MD00412A
CHEMBL4458797 170586 0 None 999 2 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at human recombinant beta2 adrenoreceptor expressed in CHOK1 cells incubated for 30 mins by HTRFAntagonist activity at human recombinant beta2 adrenoreceptor expressed in CHOK1 cells incubated for 30 mins by HTRF
ChEMBL 471 20 4 8 1.2 CC(C)NCC(O)COc1ccccc1CCCSCC(=O)NCCOCCOCCN 10.1039/C8MD00412A
44268308 17910 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandBinding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligand
ChEMBL 472 12 4 7 2.8 COc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/s0960-894x(98)00169-3
CHEMBL12686 17910 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandBinding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligand
ChEMBL 472 12 4 7 2.8 COc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/s0960-894x(98)00169-3
9933039 162483 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandBinding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligand
ChEMBL 442 11 4 6 2.8 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1)c1ccccc1 10.1016/s0960-894x(98)00169-3
CHEMBL417613 162483 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandBinding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligand
ChEMBL 442 11 4 6 2.8 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1)c1ccccc1 10.1016/s0960-894x(98)00169-3
3931 2208 42 None 3 2 Human 6.7 pIC50 = 6.7 Binding
In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.
ChEMBL 584 17 6 7 4.5 CCCCCCNC(=O)Nc1ccc(cc1)S(=O)(=O)Nc1ccc(cc1)CCNC[C@@H](COc1ccc(cc1)O)O 10.1016/s0960-894x(98)00170-x
9829836 2208 42 None 3 2 Human 6.7 pIC50 = 6.7 Binding
In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.
ChEMBL 584 17 6 7 4.5 CCCCCCNC(=O)Nc1ccc(cc1)S(=O)(=O)Nc1ccc(cc1)CCNC[C@@H](COc1ccc(cc1)O)O 10.1016/s0960-894x(98)00170-x
CHEMBL12998 2208 42 None 3 2 Human 6.7 pIC50 = 6.7 Binding
In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.
ChEMBL 584 17 6 7 4.5 CCCCCCNC(=O)Nc1ccc(cc1)S(=O)(=O)Nc1ccc(cc1)CCNC[C@@H](COc1ccc(cc1)O)O 10.1016/s0960-894x(98)00170-x
44301618 197393 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindololBinding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindolol
ChEMBL 574 11 3 7 5.7 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3ccc(F)cc3)cs2)cc1 10.1016/s0960-894x(00)00390-5
CHEMBL58798 197393 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindololBinding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindolol
ChEMBL 574 11 3 7 5.7 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3ccc(F)cc3)cs2)cc1 10.1016/s0960-894x(00)00390-5
57398769 70143 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 477 12 4 6 4.0 COc1ccccc1CCNCc1ccc(CCNCCc2ccc(O)c3[nH]c(=O)sc23)cc1 10.1016/j.bmcl.2011.10.049
CHEMBL1946767 70143 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 477 12 4 6 4.0 COc1ccccc1CCNCc1ccc(CCNCCc2ccc(O)c3[nH]c(=O)sc23)cc1 10.1016/j.bmcl.2011.10.049
2810 67245 50 None 1 2 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 213 4 2 2 2.4 CC(C)NCC(O)c1ccccc1Cl nan
CHEMBL1902627 67245 50 None 1 2 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 213 4 2 2 2.4 CC(C)NCC(O)c1ccccc1Cl nan
105 3392 84 None -10 6 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]dihydroalprenolol from beta2-adrenoceptor after 90 mins by liquid scintillation countingDisplacement of [3H]dihydroalprenolol from beta2-adrenoceptor after 90 mins by liquid scintillation counting
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1016/j.bmcl.2011.11.072
2083 3392 84 None -10 6 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]dihydroalprenolol from beta2-adrenoceptor after 90 mins by liquid scintillation countingDisplacement of [3H]dihydroalprenolol from beta2-adrenoceptor after 90 mins by liquid scintillation counting
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1016/j.bmcl.2011.11.072
558 3392 84 None -10 6 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]dihydroalprenolol from beta2-adrenoceptor after 90 mins by liquid scintillation countingDisplacement of [3H]dihydroalprenolol from beta2-adrenoceptor after 90 mins by liquid scintillation counting
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1016/j.bmcl.2011.11.072
CHEMBL714 3392 84 None -10 6 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]dihydroalprenolol from beta2-adrenoceptor after 90 mins by liquid scintillation countingDisplacement of [3H]dihydroalprenolol from beta2-adrenoceptor after 90 mins by liquid scintillation counting
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1016/j.bmcl.2011.11.072
DB01001 3392 84 None -10 6 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]dihydroalprenolol from beta2-adrenoceptor after 90 mins by liquid scintillation countingDisplacement of [3H]dihydroalprenolol from beta2-adrenoceptor after 90 mins by liquid scintillation counting
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1016/j.bmcl.2011.11.072
9846763 69856 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]dihydroalprenolol from beta2-adrenoceptor after 90 mins by liquid scintillation countingDisplacement of [3H]dihydroalprenolol from beta2-adrenoceptor after 90 mins by liquid scintillation counting
ChEMBL 454 11 8 8 2.1 OCc1cc(C(O)CNCc2ccc(NCC(O)c3ccc(O)c(CO)c3)cc2)ccc1O 10.1016/j.bmcl.2011.11.072
CHEMBL1940813 69856 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]dihydroalprenolol from beta2-adrenoceptor after 90 mins by liquid scintillation countingDisplacement of [3H]dihydroalprenolol from beta2-adrenoceptor after 90 mins by liquid scintillation counting
ChEMBL 454 11 8 8 2.1 OCc1cc(C(O)CNCc2ccc(NCC(O)c3ccc(O)c(CO)c3)cc2)ccc1O 10.1016/j.bmcl.2011.11.072
12972976 69845 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Displacement of [3H]dihydroalprenolol from beta2-adrenoceptor after 90 mins by liquid scintillation countingDisplacement of [3H]dihydroalprenolol from beta2-adrenoceptor after 90 mins by liquid scintillation counting
ChEMBL 542 12 8 8 3.5 OCc1cc(C(O)CNC2CCC(CC3CCC(NCC(O)c4ccc(O)c(CO)c4)CC3)CC2)ccc1O 10.1016/j.bmcl.2011.11.072
CHEMBL1940685 69845 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Displacement of [3H]dihydroalprenolol from beta2-adrenoceptor after 90 mins by liquid scintillation countingDisplacement of [3H]dihydroalprenolol from beta2-adrenoceptor after 90 mins by liquid scintillation counting
ChEMBL 542 12 8 8 3.5 OCc1cc(C(O)CNC2CCC(CC3CCC(NCC(O)c4ccc(O)c(CO)c4)CC3)CC2)ccc1O 10.1016/j.bmcl.2011.11.072
21093243 69853 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Displacement of [3H]dihydroalprenolol from beta2-adrenoceptor after 90 mins by liquid scintillation countingDisplacement of [3H]dihydroalprenolol from beta2-adrenoceptor after 90 mins by liquid scintillation counting
ChEMBL 468 12 8 8 1.7 OCc1cc(C(O)CNCc2cccc(CNCC(O)c3ccc(O)c(CO)c3)c2)ccc1O 10.1016/j.bmcl.2011.11.072
CHEMBL1940810 69853 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Displacement of [3H]dihydroalprenolol from beta2-adrenoceptor after 90 mins by liquid scintillation countingDisplacement of [3H]dihydroalprenolol from beta2-adrenoceptor after 90 mins by liquid scintillation counting
ChEMBL 468 12 8 8 1.7 OCc1cc(C(O)CNCc2cccc(CNCC(O)c3ccc(O)c(CO)c3)c2)ccc1O 10.1016/j.bmcl.2011.11.072
16736091 85291 0 None 66 2 Human 8.7 pIC50 = 8.7 Binding
Mitogenesis inhibition method: To measure beta2-AR mediated inhibition of mitogenesis, HEK-beta2-AR, 1321N1 or U87MG cells were seeded in a 96-well plate at approximately 5,000 cells/well. After 48 hours, the wells were rinsed twice and the medium was replaced with fresh medium containing 10 uL of drug in sterile water. After another 24 hours of incubation at 37° C., 0.25 uCi of [3H]-thymidine was added to each well. The cells were incubated for an additional 2 hours at 37° C., at which point 10 uL of 10x trypsin was added, and the resuspended cells were harvested using a Tomtec 96 harvester through glass fiber filters.Mitogenesis inhibition method: To measure beta2-AR mediated inhibition of mitogenesis, HEK-beta2-AR, 1321N1 or U87MG cells were seeded in a 96-well plate at approximately 5,000 cells/well. After 48 hours, the wells were rinsed twice and the medium was replaced with fresh medium containing 10 uL of drug in sterile water. After another 24 hours of incubation at 37° C., 0.25 uCi of [3H]-thymidine was added to each well. The cells were incubated for an additional 2 hours at 37° C., at which point 10 uL of 10x trypsin was added, and the resuspended cells were harvested using a Tomtec 96 harvester through glass fiber filters.
ChEMBL 317 7 4 5 2.4 COc1ccc(C[C@H](C)NC[C@H](O)c2cc(O)cc(O)c2)cc1 nan
CHEMBL228996 85291 0 None 66 2 Human 8.7 pIC50 = 8.7 Binding
Mitogenesis inhibition method: To measure beta2-AR mediated inhibition of mitogenesis, HEK-beta2-AR, 1321N1 or U87MG cells were seeded in a 96-well plate at approximately 5,000 cells/well. After 48 hours, the wells were rinsed twice and the medium was replaced with fresh medium containing 10 uL of drug in sterile water. After another 24 hours of incubation at 37° C., 0.25 uCi of [3H]-thymidine was added to each well. The cells were incubated for an additional 2 hours at 37° C., at which point 10 uL of 10x trypsin was added, and the resuspended cells were harvested using a Tomtec 96 harvester through glass fiber filters.Mitogenesis inhibition method: To measure beta2-AR mediated inhibition of mitogenesis, HEK-beta2-AR, 1321N1 or U87MG cells were seeded in a 96-well plate at approximately 5,000 cells/well. After 48 hours, the wells were rinsed twice and the medium was replaced with fresh medium containing 10 uL of drug in sterile water. After another 24 hours of incubation at 37° C., 0.25 uCi of [3H]-thymidine was added to each well. The cells were incubated for an additional 2 hours at 37° C., at which point 10 uL of 10x trypsin was added, and the resuspended cells were harvested using a Tomtec 96 harvester through glass fiber filters.
ChEMBL 317 7 4 5 2.4 COc1ccc(C[C@H](C)NC[C@H](O)c2cc(O)cc(O)c2)cc1 nan
54672858 150929 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 μg/well for beta1 and 5 μg/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 μl, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 μM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 μg/well for beta1 and 5 μg/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 μl, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 μM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.
ChEMBL 794 16 7 12 5.9 COc1cc(NC(=O)CCCN[C@H]2CC[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3962171 150929 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 μg/well for beta1 and 5 μg/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 μl, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 μM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 μg/well for beta1 and 5 μg/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 μl, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 μM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.
ChEMBL 794 16 7 12 5.9 COc1cc(NC(=O)CCCN[C@H]2CC[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
71524764 143895 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 ug/well for beta1 and 5 ug/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 ul, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 uM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 ug/well for beta1 and 5 ug/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 ul, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 uM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.
ChEMBL 833 16 5 14 6.5 COc1cc(-c2noc(CCCN(C)[C@H]3CC[C@H](OC(=O)C(O)(c4cccs4)c4cccs4)CC3)n2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3906438 143895 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 ug/well for beta1 and 5 ug/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 ul, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 uM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 ug/well for beta1 and 5 ug/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 ul, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 uM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.
ChEMBL 833 16 5 14 6.5 COc1cc(-c2noc(CCCN(C)[C@H]3CC[C@H](OC(=O)C(O)(c4cccs4)c4cccs4)CC3)n2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
54675236 142165 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 μg/well for beta1 and 5 μg/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 μl, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 μM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 μg/well for beta1 and 5 μg/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 μl, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 μM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.
ChEMBL 808 15 6 12 6.3 COc1cc(NC(=O)CCN(C)[C@H]2CC[C@](C)(OC(=O)C(O)(c3cccs3)c3cccs3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3892218 142165 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 μg/well for beta1 and 5 μg/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 μl, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 μM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 μg/well for beta1 and 5 μg/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 μl, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 μM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.
ChEMBL 808 15 6 12 6.3 COc1cc(NC(=O)CCN(C)[C@H]2CC[C@](C)(OC(=O)C(O)(c3cccs3)c3cccs3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
11647002 15447 0 None - 3 Guinea pig 8.7 pIC50 = 8.7 Binding
Agonist activity at adrenergic beta2 receptor in electrically-stimulated Dunkin-Hartley guinea pig tracheal strip assessed as inhibition of contractionAgonist activity at adrenergic beta2 receptor in electrically-stimulated Dunkin-Hartley guinea pig tracheal strip assessed as inhibition of contraction
ChEMBL 400 7 4 6 3.1 O=c1[nH]c2c(O)ccc([C@@H](O)CN[C@H]3CCC[C@@H]3OCc3ccccc3)c2s1 10.1016/j.bmcl.2014.06.014
CHEMBL1221681 15447 0 None - 3 Guinea pig 8.7 pIC50 = 8.7 Binding
Agonist activity at adrenergic beta2 receptor in electrically-stimulated Dunkin-Hartley guinea pig tracheal strip assessed as inhibition of contractionAgonist activity at adrenergic beta2 receptor in electrically-stimulated Dunkin-Hartley guinea pig tracheal strip assessed as inhibition of contraction
ChEMBL 400 7 4 6 3.1 O=c1[nH]c2c(O)ccc([C@@H](O)CN[C@H]3CCC[C@@H]3OCc3ccccc3)c2s1 10.1016/j.bmcl.2014.06.014
3682 188837 7 None 1 8 Human 8.6 pIC50 = 8.6 Binding
Percent inhibition against Beta-2 adrenergic receptor at 1 uMPercent inhibition against Beta-2 adrenergic receptor at 1 uM
ChEMBL 277 6 2 3 2.6 Cc1ccc(OCC(O)C(C)NC(C)C)c2c1CCC2 10.1021/jm058018d
CHEMBL1256784 188837 7 None 1 8 Human 8.6 pIC50 = 8.6 Binding
Percent inhibition against Beta-2 adrenergic receptor at 1 uMPercent inhibition against Beta-2 adrenergic receptor at 1 uM
ChEMBL 277 6 2 3 2.6 Cc1ccc(OCC(O)C(C)NC(C)C)c2c1CCC2 10.1021/jm058018d
CHEMBL513389 188837 7 None 1 8 Human 8.6 pIC50 = 8.6 Binding
Percent inhibition against Beta-2 adrenergic receptor at 1 uMPercent inhibition against Beta-2 adrenergic receptor at 1 uM
ChEMBL 277 6 2 3 2.6 Cc1ccc(OCC(O)C(C)NC(C)C)c2c1CCC2 10.1021/jm058018d
3682 188837 7 None 1 8 Human 8.6 pIC50 = 8.6 Binding
Inhibition of human alpha2 adrenoceptorInhibition of human alpha2 adrenoceptor
ChEMBL 277 6 2 3 2.6 Cc1ccc(OCC(O)C(C)NC(C)C)c2c1CCC2 10.1016/j.bmc.2010.07.034
CHEMBL1256784 188837 7 None 1 8 Human 8.6 pIC50 = 8.6 Binding
Inhibition of human alpha2 adrenoceptorInhibition of human alpha2 adrenoceptor
ChEMBL 277 6 2 3 2.6 Cc1ccc(OCC(O)C(C)NC(C)C)c2c1CCC2 10.1016/j.bmc.2010.07.034
CHEMBL513389 188837 7 None 1 8 Human 8.6 pIC50 = 8.6 Binding
Inhibition of human alpha2 adrenoceptorInhibition of human alpha2 adrenoceptor
ChEMBL 277 6 2 3 2.6 Cc1ccc(OCC(O)C(C)NC(C)C)c2c1CCC2 10.1016/j.bmc.2010.07.034
24900685 69999 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 464 11 5 7 2.9 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3cccc(CNCCc4ccccn4)c3)c2s1 10.1016/j.bmcl.2011.10.049
CHEMBL1945033 69999 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 464 11 5 7 2.9 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3cccc(CNCCc4ccccn4)c3)c2s1 10.1016/j.bmcl.2011.10.049
71556977 142000 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 ug/well for beta1 and 5 ug/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 ul, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 uM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 ug/well for beta1 and 5 ug/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 ul, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 uM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.
ChEMBL 769 15 5 13 5.9 CN(CCCc1nc(-c2ccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)no1)[C@H]1CC[C@H](OC(=O)C(O)(c2cccs2)c2cccs2)CC1 nan
CHEMBL3890898 142000 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 ug/well for beta1 and 5 ug/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 ul, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 uM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 ug/well for beta1 and 5 ug/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 ul, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 uM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.
ChEMBL 769 15 5 13 5.9 CN(CCCc1nc(-c2ccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)no1)[C@H]1CC[C@H](OC(=O)C(O)(c2cccs2)c2cccs2)CC1 nan
137 367 47 None - 12 Bovine 8.5 pIC50 = 8.5 Binding
Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-2 adrenergic receptor in calf lung membranes.Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-2 adrenergic receptor in calf lung membranes.
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1021/jm00350a009
2119 367 47 None - 12 Bovine 8.5 pIC50 = 8.5 Binding
Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-2 adrenergic receptor in calf lung membranes.Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-2 adrenergic receptor in calf lung membranes.
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1021/jm00350a009
563 367 47 None - 12 Bovine 8.5 pIC50 = 8.5 Binding
Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-2 adrenergic receptor in calf lung membranes.Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-2 adrenergic receptor in calf lung membranes.
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1021/jm00350a009
66368 367 47 None - 12 Bovine 8.5 pIC50 = 8.5 Binding
Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-2 adrenergic receptor in calf lung membranes.Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-2 adrenergic receptor in calf lung membranes.
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1021/jm00350a009
CHEMBL266195 367 47 None - 12 Bovine 8.5 pIC50 = 8.5 Binding
Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-2 adrenergic receptor in calf lung membranes.Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-2 adrenergic receptor in calf lung membranes.
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1021/jm00350a009
DB00866 367 47 None - 12 Bovine 8.5 pIC50 = 8.5 Binding
Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-2 adrenergic receptor in calf lung membranes.Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-2 adrenergic receptor in calf lung membranes.
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1021/jm00350a009
118710945 113243 0 None - 3 Guinea pig 7.7 pIC50 = 7.7 Binding
Agonist activity at adrenergic beta2 receptor in electrically-stimulated Dunkin-Hartley guinea pig tracheal strip assessed as inhibition of contractionAgonist activity at adrenergic beta2 receptor in electrically-stimulated Dunkin-Hartley guinea pig tracheal strip assessed as inhibition of contraction
ChEMBL 398 6 4 5 3.8 CCc1cccc([C@H]2CCC[C@H]2NC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)c1 10.1016/j.bmcl.2014.06.014
CHEMBL3323663 113243 0 None - 3 Guinea pig 7.7 pIC50 = 7.7 Binding
Agonist activity at adrenergic beta2 receptor in electrically-stimulated Dunkin-Hartley guinea pig tracheal strip assessed as inhibition of contractionAgonist activity at adrenergic beta2 receptor in electrically-stimulated Dunkin-Hartley guinea pig tracheal strip assessed as inhibition of contraction
ChEMBL 398 6 4 5 3.8 CCc1cccc([C@H]2CCC[C@H]2NC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)c1 10.1016/j.bmcl.2014.06.014
44268305 97832 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandBinding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligand
ChEMBL 345 10 3 5 2.8 COc1ccc(CC[C@H](C)NC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/s0960-894x(98)00169-3
CHEMBL274782 97832 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandBinding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligand
ChEMBL 345 10 3 5 2.8 COc1ccc(CC[C@H](C)NC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/s0960-894x(98)00169-3
44112 120764 41 None -1 7 Human 7.7 pIC50 = 7.7 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 380 7 2 4 4.5 Cc1cc2c(OCC(CNC(C)(C)C)OC(=O)c3ccccc3)cccc2[nH]1 nan
CHEMBL357995 120764 41 None -1 7 Human 7.7 pIC50 = 7.7 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 380 7 2 4 4.5 Cc1cc2c(OCC(CNC(C)(C)C)OC(=O)c3ccccc3)cccc2[nH]1 nan
145986860 166551 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]-CGP-12177 from human beta2-adrenergic receptorDisplacement of [3H]-CGP-12177 from human beta2-adrenergic receptor
ChEMBL 311 2 2 4 2.8 COc1cc2c3c(c1OC)-c1ccccc1[C@@H](O)[C@]3(C)NCC2 10.1039/C7MD00656J
CHEMBL4290197 166551 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]-CGP-12177 from human beta2-adrenergic receptorDisplacement of [3H]-CGP-12177 from human beta2-adrenergic receptor
ChEMBL 311 2 2 4 2.8 COc1cc2c3c(c1OC)-c1ccccc1[C@@H](O)[C@]3(C)NCC2 10.1039/C7MD00656J
2447486 62716 1 None - 2 Bovine 7.7 pIC50 = 7.7 Binding
Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-2 adrenergic receptor in calf lung membranes.Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-2 adrenergic receptor in calf lung membranes.
ChEMBL 324 5 2 4 3.2 CC(C)(C)NC[C@@H](O)CON=C1c2ccccc2-c2ccccc21 10.1021/jm00350a009
CHEMBL1788270 62716 1 None - 2 Bovine 7.7 pIC50 = 7.7 Binding
Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-2 adrenergic receptor in calf lung membranes.Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-2 adrenergic receptor in calf lung membranes.
ChEMBL 324 5 2 4 3.2 CC(C)(C)NC[C@@H](O)CON=C1c2ccccc2-c2ccccc21 10.1021/jm00350a009
44335534 4743 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Beta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindolol
ChEMBL 559 13 5 6 4.1 O=C(NCCc1ccccc1)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(98)00571-x
CHEMBL104193 4743 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Beta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindolol
ChEMBL 559 13 5 6 4.1 O=C(NCCc1ccccc1)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(98)00571-x
10112732 16618 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cells
ChEMBL 418 8 4 5 3.3 N#CN/C(=N\c1cccc(F)c1)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/s0960-894x(00)00669-7
CHEMBL124668 16618 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cells
ChEMBL 418 8 4 5 3.3 N#CN/C(=N\c1cccc(F)c1)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/s0960-894x(00)00669-7
44268604 36379 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.
ChEMBL 598 18 6 7 4.9 CCCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/s0960-894x(98)00170-x
CHEMBL144870 36379 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.
ChEMBL 598 18 6 7 4.9 CCCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/s0960-894x(98)00170-x
9831168 202986 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory activity against CHO cells expressing human Beta-2 adrenergic receptor with [125I]-iodocyanopindololInhibitory activity against CHO cells expressing human Beta-2 adrenergic receptor with [125I]-iodocyanopindolol
ChEMBL 552 11 6 6 5.0 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC3NCCc4cc(O)c(O)cc43)cc2)cc1 10.1016/s0960-894x(00)00459-5
CHEMBL74085 202986 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory activity against CHO cells expressing human Beta-2 adrenergic receptor with [125I]-iodocyanopindololInhibitory activity against CHO cells expressing human Beta-2 adrenergic receptor with [125I]-iodocyanopindolol
ChEMBL 552 11 6 6 5.0 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC3NCCc4cc(O)c(O)cc43)cc2)cc1 10.1016/s0960-894x(00)00459-5
44335562 108041 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Beta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindolol
ChEMBL 558 14 4 6 4.7 O=C(CCCc1ccccc1)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(98)00571-x
CHEMBL320138 108041 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Beta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindolol
ChEMBL 558 14 4 6 4.7 O=C(CCCc1ccccc1)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(98)00571-x
44301819 100580 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindololBinding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindolol
ChEMBL 612 11 3 7 6.8 CC(C)(C)c1ccc(-c2csc(-c3ccc(S(=O)(=O)Nc4ccc(CCNC[C@H](O)c5cccnc5)cc4)cc3)n2)cc1 10.1016/s0960-894x(00)00390-5
CHEMBL294753 100580 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindololBinding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindolol
ChEMBL 612 11 3 7 6.8 CC(C)(C)c1ccc(-c2csc(-c3ccc(S(=O)(=O)Nc4ccc(CCNC[C@H](O)c5cccnc5)cc4)cc3)n2)cc1 10.1016/s0960-894x(00)00390-5
11342656 200963 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindololBinding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindolol
ChEMBL 634 13 3 7 6.5 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(Cc2nc(Cc3ccc4ccccc4c3)cs2)cc1 10.1016/s0960-894x(00)00390-5
CHEMBL61429 200963 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindololBinding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindolol
ChEMBL 634 13 3 7 6.5 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(Cc2nc(Cc3ccc4ccccc4c3)cs2)cc1 10.1016/s0960-894x(00)00390-5
44281219 111509 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindolol
ChEMBL 588 12 4 9 4.0 NC(c1ccc(F)cc1)c1nc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)no1 10.1016/s0960-894x(00)00268-7
CHEMBL32891 111509 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindolol
ChEMBL 588 12 4 9 4.0 NC(c1ccc(F)cc1)c1nc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)no1 10.1016/s0960-894x(00)00268-7
44281468 161322 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindolol
ChEMBL 623 12 3 8 5.4 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2noc(Cc3ccc(C(F)(F)F)cc3)n2)cc1 10.1016/s0960-894x(00)00268-7
CHEMBL415039 161322 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindolol
ChEMBL 623 12 3 8 5.4 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2noc(Cc3ccc(C(F)(F)F)cc3)n2)cc1 10.1016/s0960-894x(00)00268-7
44377513 56201 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity towards Beta-2 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindololBinding affinity towards Beta-2 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindolol
ChEMBL 592 17 3 9 4.5 CCCCCCCCn1ncn(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)c1=O 10.1016/s0960-894x(99)00073-6
CHEMBL163531 56201 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity towards Beta-2 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindololBinding affinity towards Beta-2 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindolol
ChEMBL 592 17 3 9 4.5 CCCCCCCCn1ncn(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)c1=O 10.1016/s0960-894x(99)00073-6
44461706 204197 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity towards Beta-2 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindololBinding affinity towards Beta-2 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindolol
ChEMBL 579 15 3 7 4.1 CCCCCCN1C(=O)CN(c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)C1=O 10.1016/s0960-894x(99)00073-6
CHEMBL84117 204197 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity towards Beta-2 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindololBinding affinity towards Beta-2 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindolol
ChEMBL 579 15 3 7 4.1 CCCCCCN1C(=O)CN(c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)C1=O 10.1016/s0960-894x(99)00073-6
44377637 55228 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindololBinding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindolol
ChEMBL 633 14 3 6 5.3 O=C1N(CCCc2ccc(Cl)cc2)CCN1c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(99)00072-4
CHEMBL162043 55228 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindololBinding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindolol
ChEMBL 633 14 3 6 5.3 O=C1N(CCCc2ccc(Cl)cc2)CCN1c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(99)00072-4
44377677 56570 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindololBinding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindolol
ChEMBL 495 10 3 6 2.6 CN1CCN(c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)C1=O 10.1016/s0960-894x(99)00072-4
CHEMBL164401 56570 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindololBinding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindolol
ChEMBL 495 10 3 6 2.6 CN1CCN(c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)C1=O 10.1016/s0960-894x(99)00072-4
15523861 57206 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindololBinding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindolol
ChEMBL 599 14 3 6 4.6 O=C1N(CCCc2ccccc2)CCN1c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(99)00072-4
CHEMBL166188 57206 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindololBinding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindolol
ChEMBL 599 14 3 6 4.6 O=C1N(CCCc2ccccc2)CCN1c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(99)00072-4
44268482 97635 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.
ChEMBL 499 12 5 7 2.7 CC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/s0960-894x(98)00170-x
CHEMBL273428 97635 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.
ChEMBL 499 12 5 7 2.7 CC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/s0960-894x(98)00170-x
44298718 195401 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
In vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 386 8 1 3 4.3 CCCCCCC(=O)N1CCc2cc(S(=O)(=O)Nc3ccccc3)ccc21 10.1016/s0960-894x(99)00277-2
CHEMBL56752 195401 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
In vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 386 8 1 3 4.3 CCCCCCC(=O)N1CCc2cc(S(=O)(=O)Nc3ccccc3)ccc21 10.1016/s0960-894x(99)00277-2
10545491 160293 0 None - 0 Dog 5.7 pIC50 = 5.7 Binding
Inhibition of beta-2 adrenergic receptor isolated from rat lung homogenatesInhibition of beta-2 adrenergic receptor isolated from rat lung homogenates
ChEMBL 345 10 3 5 2.7 CC(C)(Cc1ccc(N)cc1)NCC(O)CON=C(C1CC1)C1CC1 10.1021/jm970338c
CHEMBL41149 160293 0 None - 0 Dog 5.7 pIC50 = 5.7 Binding
Inhibition of beta-2 adrenergic receptor isolated from rat lung homogenatesInhibition of beta-2 adrenergic receptor isolated from rat lung homogenates
ChEMBL 345 10 3 5 2.7 CC(C)(Cc1ccc(N)cc1)NCC(O)CON=C(C1CC1)C1CC1 10.1021/jm970338c
12017018 141794 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.
ChEMBL 638 13 3 8 6.0 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2coc(COc3ccc(C(F)(F)F)cc3)n2)cc1 10.1016/s0960-894x(00)00277-8
CHEMBL38861 141794 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.
ChEMBL 638 13 3 8 6.0 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2coc(COc3ccc(C(F)(F)F)cc3)n2)cc1 10.1016/s0960-894x(00)00277-8
44268349 20361 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandBinding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligand
ChEMBL 456 12 4 6 2.9 O=S(=O)(Cc1ccccc1)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/s0960-894x(98)00169-3
CHEMBL13079 20361 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandBinding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligand
ChEMBL 456 12 4 6 2.9 O=S(=O)(Cc1ccccc1)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/s0960-894x(98)00169-3
19360455 186482 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity to beta2 adrenoceptorBinding affinity to beta2 adrenoceptor
ChEMBL 397 9 2 4 4.4 COc1ccc(CC(C)(C)NCC(O)COc2cccc(Cl)c2Cl)cc1 10.1021/jm900364m
CHEMBL491251 186482 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity to beta2 adrenoceptorBinding affinity to beta2 adrenoceptor
ChEMBL 397 9 2 4 4.4 COc1ccc(CC(C)(C)NCC(O)COc2cccc(Cl)c2Cl)cc1 10.1021/jm900364m
19360456 188110 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity to beta2 adrenoceptorBinding affinity to beta2 adrenoceptor
ChEMBL 354 9 2 5 2.9 COc1ccc(CC(C)(C)NCC(O)COc2ccccc2C#N)cc1 10.1021/jm900364m
CHEMBL504479 188110 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity to beta2 adrenoceptorBinding affinity to beta2 adrenoceptor
ChEMBL 354 9 2 5 2.9 COc1ccc(CC(C)(C)NCC(O)COc2ccccc2C#N)cc1 10.1021/jm900364m
145981443 165987 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]-CGP-12177 from human beta2-adrenergic receptorDisplacement of [3H]-CGP-12177 from human beta2-adrenergic receptor
ChEMBL 297 2 2 4 2.6 COc1cc2c3c(c1OC)-c1ccccc1[C@@H](O)[C@H]3NCC2 10.1039/C7MD00656J
CHEMBL4279531 165987 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]-CGP-12177 from human beta2-adrenergic receptorDisplacement of [3H]-CGP-12177 from human beta2-adrenergic receptor
ChEMBL 297 2 2 4 2.6 COc1cc2c3c(c1OC)-c1ccccc1[C@@H](O)[C@H]3NCC2 10.1039/C7MD00656J
44268479 20674 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.
ChEMBL 543 13 5 8 3.7 CC(C)OC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/s0960-894x(98)00170-x
CHEMBL13106 20674 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.
ChEMBL 543 13 5 8 3.7 CC(C)OC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/s0960-894x(98)00170-x
44301867 100097 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindololBinding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindolol
ChEMBL 613 12 4 8 5.5 CC(=O)Nc1ccc(-c2csc(-c3ccc(S(=O)(=O)Nc4ccc(CCNC[C@H](O)c5cccnc5)cc4)cc3)n2)cc1 10.1016/s0960-894x(00)00390-5
CHEMBL291594 100097 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindololBinding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindolol
ChEMBL 613 12 4 8 5.5 CC(=O)Nc1ccc(-c2csc(-c3ccc(S(=O)(=O)Nc4ccc(CCNC[C@H](O)c5cccnc5)cc4)cc3)n2)cc1 10.1016/s0960-894x(00)00390-5
10483845 201374 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Binding affinity for clone human Beta-2 adrenergic receptor from CHO cell membranes in the presence of I-iodocyanopindololBinding affinity for clone human Beta-2 adrenergic receptor from CHO cell membranes in the presence of I-iodocyanopindolol
ChEMBL 608 11 3 8 5.0 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-n2ncc(-c3ccc(C(F)(F)F)cc3)n2)cc1 10.1016/s0960-894x(00)00422-4
CHEMBL63760 201374 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Binding affinity for clone human Beta-2 adrenergic receptor from CHO cell membranes in the presence of I-iodocyanopindololBinding affinity for clone human Beta-2 adrenergic receptor from CHO cell membranes in the presence of I-iodocyanopindolol
ChEMBL 608 11 3 8 5.0 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-n2ncc(-c3ccc(C(F)(F)F)cc3)n2)cc1 10.1016/s0960-894x(00)00422-4
12017002 141155 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.
ChEMBL 558 11 3 7 5.2 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2cnc(-c3ccc(F)cc3)o2)cc1 10.1016/s0960-894x(00)00277-8
CHEMBL38562 141155 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.
ChEMBL 558 11 3 7 5.2 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2cnc(-c3ccc(F)cc3)o2)cc1 10.1016/s0960-894x(00)00277-8
118710943 113241 0 None - 3 Guinea pig 7.7 pIC50 = 7.7 Binding
Agonist activity at adrenergic beta2 receptor in electrically-stimulated Dunkin-Hartley guinea pig tracheal strip assessed as inhibition of contractionAgonist activity at adrenergic beta2 receptor in electrically-stimulated Dunkin-Hartley guinea pig tracheal strip assessed as inhibition of contraction
ChEMBL 384 5 4 5 3.6 Cc1cccc([C@H]2CCC[C@H]2NC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)c1 10.1016/j.bmcl.2014.06.014
CHEMBL3323661 113241 0 None - 3 Guinea pig 7.7 pIC50 = 7.7 Binding
Agonist activity at adrenergic beta2 receptor in electrically-stimulated Dunkin-Hartley guinea pig tracheal strip assessed as inhibition of contractionAgonist activity at adrenergic beta2 receptor in electrically-stimulated Dunkin-Hartley guinea pig tracheal strip assessed as inhibition of contraction
ChEMBL 384 5 4 5 3.6 Cc1cccc([C@H]2CCC[C@H]2NC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)c1 10.1016/j.bmcl.2014.06.014
155552089 173437 0 None 10 2 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at human recombinant beta2 adrenoreceptor expressed in CHOK1 cells incubated for 30 mins by HTRFAntagonist activity at human recombinant beta2 adrenoreceptor expressed in CHOK1 cells incubated for 30 mins by HTRF
ChEMBL 571 21 4 9 2.8 CC(C)NCC(O)COc1ccccc1CCCSCC(=O)NCCOCCOCCNC(=O)OC(C)(C)C 10.1039/C8MD00412A
CHEMBL4542960 173437 0 None 10 2 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at human recombinant beta2 adrenoreceptor expressed in CHOK1 cells incubated for 30 mins by HTRFAntagonist activity at human recombinant beta2 adrenoreceptor expressed in CHOK1 cells incubated for 30 mins by HTRF
ChEMBL 571 21 4 9 2.8 CC(C)NCC(O)COc1ccccc1CCCSCC(=O)NCCOCCOCCNC(=O)OC(C)(C)C 10.1039/C8MD00412A
71558567 142137 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 ug/well for beta1 and 5 ug/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 ul, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 uM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 ug/well for beta1 and 5 ug/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 ul, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 uM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.
ChEMBL 740 14 5 11 6.2 CN(CCCn1ccc2cc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)ccc21)[C@H]1CC[C@H](OC(=O)C(O)(c2cccs2)c2cccs2)CC1 nan
CHEMBL3892021 142137 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 ug/well for beta1 and 5 ug/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 ul, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 uM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 ug/well for beta1 and 5 ug/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 ul, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 uM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.
ChEMBL 740 14 5 11 6.2 CN(CCCn1ccc2cc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)ccc21)[C@H]1CC[C@H](OC(=O)C(O)(c2cccs2)c2cccs2)CC1 nan
44268352 15349 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandBinding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligand
ChEMBL 380 10 4 6 1.3 CS(=O)(=O)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/s0960-894x(98)00169-3
CHEMBL12188 15349 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandBinding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligand
ChEMBL 380 10 4 6 1.3 CS(=O)(=O)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/s0960-894x(98)00169-3
44349237 162875 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cells
ChEMBL 511 13 4 8 5.3 O=[N+]([O-])/C=C(\Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)Nc1cccc(Oc2ccccc2)c1 10.1016/s0960-894x(00)00669-7
CHEMBL419787 162875 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cells
ChEMBL 511 13 4 8 5.3 O=[N+]([O-])/C=C(\Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)Nc1cccc(Oc2ccccc2)c1 10.1016/s0960-894x(00)00669-7
44268509 19208 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.
ChEMBL 513 13 5 7 3.1 CCC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/s0960-894x(98)00170-x
CHEMBL12943 19208 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.
ChEMBL 513 13 5 7 3.1 CCC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/s0960-894x(98)00170-x
44472591 137481 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125]I-cyanopindolol from human recombinant beta2 adrenergic receptor after 1 hr by scintillation counting methodDisplacement of [125]I-cyanopindolol from human recombinant beta2 adrenergic receptor after 1 hr by scintillation counting method
ChEMBL 468 7 3 6 3.4 O=C(Cn1cnc2ccccc2c1=O)Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1 10.1021/acs.jmedchem.5b01372
CHEMBL3764774 137481 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125]I-cyanopindolol from human recombinant beta2 adrenergic receptor after 1 hr by scintillation counting methodDisplacement of [125]I-cyanopindolol from human recombinant beta2 adrenergic receptor after 1 hr by scintillation counting method
ChEMBL 468 7 3 6 3.4 O=C(Cn1cnc2ccccc2c1=O)Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1 10.1021/acs.jmedchem.5b01372
12017007 157821 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.
ChEMBL 576 11 3 7 5.3 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2coc(-c3ccc(F)c(F)c3)n2)cc1 10.1016/s0960-894x(00)00277-8
CHEMBL40898 157821 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.
ChEMBL 576 11 3 7 5.3 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2coc(-c3ccc(F)c(F)c3)n2)cc1 10.1016/s0960-894x(00)00277-8
104903 56035 14 None -5 6 Human 4.6 pIC50 = 4.6 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 624 6 0 8 5.5 C[C@@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)C3=CC[C@]2(C)[C@H]1C(=O)CN1CCN(c2cc(N3CCCC3)nc(N3CCCC3)n2)CC1 nan
CHEMBL1630578 56035 14 None -5 6 Human 4.6 pIC50 = 4.6 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 624 6 0 8 5.5 C[C@@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)C3=CC[C@]2(C)[C@H]1C(=O)CN1CCN(c2cc(N3CCCC3)nc(N3CCCC3)n2)CC1 nan
16735495 85345 0 None 14 2 Human 6.6 pIC50 = 6.6 Binding
Mitogenesis inhibition method: To measure beta2-AR mediated inhibition of mitogenesis, HEK-beta2-AR, 1321N1 or U87MG cells were seeded in a 96-well plate at approximately 5,000 cells/well. After 48 hours, the wells were rinsed twice and the medium was replaced with fresh medium containing 10 uL of drug in sterile water. After another 24 hours of incubation at 37° C., 0.25 uCi of [3H]-thymidine was added to each well. The cells were incubated for an additional 2 hours at 37° C., at which point 10 uL of 10x trypsin was added, and the resuspended cells were harvested using a Tomtec 96 harvester through glass fiber filters.Mitogenesis inhibition method: To measure beta2-AR mediated inhibition of mitogenesis, HEK-beta2-AR, 1321N1 or U87MG cells were seeded in a 96-well plate at approximately 5,000 cells/well. After 48 hours, the wells were rinsed twice and the medium was replaced with fresh medium containing 10 uL of drug in sterile water. After another 24 hours of incubation at 37° C., 0.25 uCi of [3H]-thymidine was added to each well. The cells were incubated for an additional 2 hours at 37° C., at which point 10 uL of 10x trypsin was added, and the resuspended cells were harvested using a Tomtec 96 harvester through glass fiber filters.
ChEMBL 337 6 4 4 3.5 C[C@H](Cc1cccc2ccccc12)NC[C@H](O)c1cc(O)cc(O)c1 nan
CHEMBL229401 85345 0 None 14 2 Human 6.6 pIC50 = 6.6 Binding
Mitogenesis inhibition method: To measure beta2-AR mediated inhibition of mitogenesis, HEK-beta2-AR, 1321N1 or U87MG cells were seeded in a 96-well plate at approximately 5,000 cells/well. After 48 hours, the wells were rinsed twice and the medium was replaced with fresh medium containing 10 uL of drug in sterile water. After another 24 hours of incubation at 37° C., 0.25 uCi of [3H]-thymidine was added to each well. The cells were incubated for an additional 2 hours at 37° C., at which point 10 uL of 10x trypsin was added, and the resuspended cells were harvested using a Tomtec 96 harvester through glass fiber filters.Mitogenesis inhibition method: To measure beta2-AR mediated inhibition of mitogenesis, HEK-beta2-AR, 1321N1 or U87MG cells were seeded in a 96-well plate at approximately 5,000 cells/well. After 48 hours, the wells were rinsed twice and the medium was replaced with fresh medium containing 10 uL of drug in sterile water. After another 24 hours of incubation at 37° C., 0.25 uCi of [3H]-thymidine was added to each well. The cells were incubated for an additional 2 hours at 37° C., at which point 10 uL of 10x trypsin was added, and the resuspended cells were harvested using a Tomtec 96 harvester through glass fiber filters.
ChEMBL 337 6 4 4 3.5 C[C@H](Cc1cccc2ccccc12)NC[C@H](O)c1cc(O)cc(O)c1 nan
118710935 113233 0 None - 3 Guinea pig 7.6 pIC50 = 7.6 Binding
Agonist activity at adrenergic beta2 receptor in electrically-stimulated Dunkin-Hartley guinea pig tracheal strip assessed as inhibition of contractionAgonist activity at adrenergic beta2 receptor in electrically-stimulated Dunkin-Hartley guinea pig tracheal strip assessed as inhibition of contraction
ChEMBL 362 5 4 5 3.3 O=c1[nH]c2c(O)ccc([C@@H](O)CN[C@H]3CCC[C@H]3C3CCCC3)c2s1 10.1016/j.bmcl.2014.06.014
CHEMBL3323653 113233 0 None - 3 Guinea pig 7.6 pIC50 = 7.6 Binding
Agonist activity at adrenergic beta2 receptor in electrically-stimulated Dunkin-Hartley guinea pig tracheal strip assessed as inhibition of contractionAgonist activity at adrenergic beta2 receptor in electrically-stimulated Dunkin-Hartley guinea pig tracheal strip assessed as inhibition of contraction
ChEMBL 362 5 4 5 3.3 O=c1[nH]c2c(O)ccc([C@@H](O)CN[C@H]3CCC[C@H]3C3CCCC3)c2s1 10.1016/j.bmcl.2014.06.014
9930235 192596 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity to beta2 adrenoceptorBinding affinity to beta2 adrenoceptor
ChEMBL 388 9 2 5 3.6 COc1ccc(CC(C)(C)NCC(O)COc2cccc(Cl)c2C#N)cc1 10.1021/jm900364m
CHEMBL523475 192596 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity to beta2 adrenoceptorBinding affinity to beta2 adrenoceptor
ChEMBL 388 9 2 5 3.6 COc1ccc(CC(C)(C)NCC(O)COc2cccc(Cl)c2C#N)cc1 10.1021/jm900364m
44268365 98104 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandBinding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligand
ChEMBL 406 10 4 5 3.2 O=C(Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1)c1ccccc1 10.1016/s0960-894x(98)00169-3
CHEMBL276659 98104 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandBinding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligand
ChEMBL 406 10 4 5 3.2 O=C(Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1)c1ccccc1 10.1016/s0960-894x(98)00169-3
44307063 201634 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cell
ChEMBL 505 11 3 6 3.2 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2cccnc2)cc1)c1ccc(Br)cc1 10.1016/s0960-894x(98)00381-3
CHEMBL64935 201634 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cell
ChEMBL 505 11 3 6 3.2 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2cccnc2)cc1)c1ccc(Br)cc1 10.1016/s0960-894x(98)00381-3
44268470 24651 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.
ChEMBL 527 14 5 7 3.5 CCCC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/s0960-894x(98)00170-x
CHEMBL13453 24651 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.
ChEMBL 527 14 5 7 3.5 CCCC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/s0960-894x(98)00170-x
44268563 96724 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.
ChEMBL 569 17 5 7 4.7 CCCCCCC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/s0960-894x(98)00170-x
CHEMBL268289 96724 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.
ChEMBL 569 17 5 7 4.7 CCCCCCC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/s0960-894x(98)00170-x
11556330 162648 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindololBinding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindolol
ChEMBL 620 12 3 7 6.6 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(Cc3ccc4ccccc4c3)cs2)cc1 10.1016/s0960-894x(00)00390-5
CHEMBL418308 162648 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindololBinding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindolol
ChEMBL 620 12 3 7 6.6 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(Cc3ccc4ccccc4c3)cs2)cc1 10.1016/s0960-894x(00)00390-5
10099459 203973 1 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity towards Beta-2 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindololBinding affinity towards Beta-2 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindolol
ChEMBL 565 15 3 6 4.6 CCCCCCN1CCN(c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)C1=O 10.1016/s0960-894x(99)00073-6
CHEMBL82296 203973 1 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity towards Beta-2 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindololBinding affinity towards Beta-2 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindolol
ChEMBL 565 15 3 6 4.6 CCCCCCN1CCN(c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)C1=O 10.1016/s0960-894x(99)00073-6
10099459 203973 1 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindololBinding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindolol
ChEMBL 565 15 3 6 4.6 CCCCCCN1CCN(c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)C1=O 10.1016/s0960-894x(99)00072-4
CHEMBL82296 203973 1 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindololBinding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindolol
ChEMBL 565 15 3 6 4.6 CCCCCCN1CCN(c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)C1=O 10.1016/s0960-894x(99)00072-4
3038500 9235 8 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity was evaluated on chinese hamster ovary (CHO) cells expressing the cloned human beta-2 adrenergic receptor in the presence of [125I]- iodocyanopindolol.Binding affinity was evaluated on chinese hamster ovary (CHO) cells expressing the cloned human beta-2 adrenergic receptor in the presence of [125I]- iodocyanopindolol.
ChEMBL 624 11 3 7 6.6 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/jm000286i
CHEMBL111201 9235 8 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity was evaluated on chinese hamster ovary (CHO) cells expressing the cloned human beta-2 adrenergic receptor in the presence of [125I]- iodocyanopindolol.Binding affinity was evaluated on chinese hamster ovary (CHO) cells expressing the cloned human beta-2 adrenergic receptor in the presence of [125I]- iodocyanopindolol.
ChEMBL 624 11 3 7 6.6 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/jm000286i
3038500 9235 8 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counter
ChEMBL 624 11 3 7 6.6 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1016/j.bmcl.2010.01.130
CHEMBL111201 9235 8 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counter
ChEMBL 624 11 3 7 6.6 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1016/j.bmcl.2010.01.130
14664348 12726 0 None - 0 Dog 4.6 pIC50 = 4.6 Binding
In vitro Beta-2 adrenergic receptor affinity in partially purified membrane fractions from canine lung tissue using [SH]dihydroalprenolol (4.5 nM)In vitro Beta-2 adrenergic receptor affinity in partially purified membrane fractions from canine lung tissue using [SH]dihydroalprenolol (4.5 nM)
ChEMBL 474 12 3 8 2.4 CC(C)(COc1ccc(-n2ccnc2)cc1)NCC(O)COc1ccc(NS(C)(=O)=O)cc1 10.1021/jm00166a002
CHEMBL1188606 12726 0 None - 0 Dog 4.6 pIC50 = 4.6 Binding
In vitro Beta-2 adrenergic receptor affinity in partially purified membrane fractions from canine lung tissue using [SH]dihydroalprenolol (4.5 nM)In vitro Beta-2 adrenergic receptor affinity in partially purified membrane fractions from canine lung tissue using [SH]dihydroalprenolol (4.5 nM)
ChEMBL 474 12 3 8 2.4 CC(C)(COc1ccc(-n2ccnc2)cc1)NCC(O)COc1ccc(NS(C)(=O)=O)cc1 10.1021/jm00166a002
CHEMBL536800 12726 0 None - 0 Dog 4.6 pIC50 = 4.6 Binding
In vitro Beta-2 adrenergic receptor affinity in partially purified membrane fractions from canine lung tissue using [SH]dihydroalprenolol (4.5 nM)In vitro Beta-2 adrenergic receptor affinity in partially purified membrane fractions from canine lung tissue using [SH]dihydroalprenolol (4.5 nM)
ChEMBL 474 12 3 8 2.4 CC(C)(COc1ccc(-n2ccnc2)cc1)NCC(O)COc1ccc(NS(C)(=O)=O)cc1 10.1021/jm00166a002
121848 130175 4 None - 2 Bovine 7.6 pIC50 = 7.6 Binding
Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-2 adrenergic receptor in calf lung membranes.Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-2 adrenergic receptor in calf lung membranes.
ChEMBL 324 5 2 4 3.2 CC(C)(C)NCC(O)CON=C1c2ccccc2-c2ccccc21 10.1021/jm00350a009
CHEMBL368457 130175 4 None - 2 Bovine 7.6 pIC50 = 7.6 Binding
Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-2 adrenergic receptor in calf lung membranes.Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-2 adrenergic receptor in calf lung membranes.
ChEMBL 324 5 2 4 3.2 CC(C)(C)NCC(O)CON=C1c2ccccc2-c2ccccc21 10.1021/jm00350a009
44268268 18449 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandBinding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligand
ChEMBL 493 11 4 7 3.3 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1)c1cnc2ccccc2c1 10.1016/s0960-894x(98)00169-3
CHEMBL12769 18449 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandBinding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligand
ChEMBL 493 11 4 7 3.3 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1)c1cnc2ccccc2c1 10.1016/s0960-894x(98)00169-3
44298843 194978 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
In vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 435 9 1 4 5.7 CCCCCCc1ccc(N2CCc3cc(S(=O)(=O)Nc4ccccc4)ccc32)nc1 10.1016/s0960-894x(99)00277-2
CHEMBL56449 194978 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
In vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 435 9 1 4 5.7 CCCCCCc1ccc(N2CCc3cc(S(=O)(=O)Nc4ccccc4)ccc32)nc1 10.1016/s0960-894x(99)00277-2
44349323 16602 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cells
ChEMBL 437 11 4 7 3.7 O=[N+]([O-])/C=C(\Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)Nc1cccc(F)c1 10.1016/s0960-894x(00)00669-7
CHEMBL124584 16602 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cells
ChEMBL 437 11 4 7 3.7 O=[N+]([O-])/C=C(\Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)Nc1cccc(F)c1 10.1016/s0960-894x(00)00669-7
44281073 118688 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Binding affinity towards Beta-2 adrenergic receptor prepared from CHO cells expressing the cloned human receptor in the presence of [125I]iodocyanopindololBinding affinity towards Beta-2 adrenergic receptor prepared from CHO cells expressing the cloned human receptor in the presence of [125I]iodocyanopindolol
ChEMBL 551 14 4 9 3.5 CCC(O)CCc1nc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)no1 10.1016/s0960-894x(00)00267-5
CHEMBL34328 118688 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Binding affinity towards Beta-2 adrenergic receptor prepared from CHO cells expressing the cloned human receptor in the presence of [125I]iodocyanopindololBinding affinity towards Beta-2 adrenergic receptor prepared from CHO cells expressing the cloned human receptor in the presence of [125I]iodocyanopindolol
ChEMBL 551 14 4 9 3.5 CCC(O)CCc1nc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)no1 10.1016/s0960-894x(00)00267-5
1499 2052 43 None -33 17 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C nan
3779 2052 43 None -33 17 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C nan
536 2052 43 None -33 17 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C nan
CHEMBL434 2052 43 None -33 17 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C nan
DB01064 2052 43 None -33 17 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C nan
76332892 105421 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]-cyanopindolol from recombinant human beta-2 adrenergic receptor expressed in CHO cell membranes after 1 hr by scintillation counting analysisDisplacement of [125I]-cyanopindolol from recombinant human beta-2 adrenergic receptor expressed in CHO cell membranes after 1 hr by scintillation counting analysis
ChEMBL 528 7 3 6 5.4 O=C(Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3cccnc3)N2)cc1)[C@@H]1CCc2sc(-c3ccc(F)cc3)nc21 10.1021/jm4017224
CHEMBL3128185 105421 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]-cyanopindolol from recombinant human beta-2 adrenergic receptor expressed in CHO cell membranes after 1 hr by scintillation counting analysisDisplacement of [125I]-cyanopindolol from recombinant human beta-2 adrenergic receptor expressed in CHO cell membranes after 1 hr by scintillation counting analysis
ChEMBL 528 7 3 6 5.4 O=C(Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3cccnc3)N2)cc1)[C@@H]1CCc2sc(-c3ccc(F)cc3)nc21 10.1021/jm4017224
24900751 70022 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 493 12 5 7 3.8 CCOc1ccccc1CNCc1cccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)c1 10.1016/j.bmcl.2011.10.049
CHEMBL1945290 70022 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 493 12 5 7 3.8 CCOc1ccccc1CNCc1cccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)c1 10.1016/j.bmcl.2011.10.049
24900749 70023 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 493 11 4 7 3.8 COc1ccccc1CN(C)Cc1cccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)c1 10.1016/j.bmcl.2011.10.049
CHEMBL1945291 70023 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 493 11 4 7 3.8 COc1ccccc1CN(C)Cc1cccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)c1 10.1016/j.bmcl.2011.10.049
24901283 70024 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 417 11 5 7 1.9 COCCNCc1cccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)c1 10.1016/j.bmcl.2011.10.049
CHEMBL1945292 70024 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 417 11 5 7 1.9 COCCNCc1cccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)c1 10.1016/j.bmcl.2011.10.049
44268281 16684 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandBinding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligand
ChEMBL 436 14 4 6 2.9 CCCCCS(=O)(=O)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/s0960-894x(98)00169-3
CHEMBL12498 16684 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandBinding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligand
ChEMBL 436 14 4 6 2.9 CCCCCS(=O)(=O)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/s0960-894x(98)00169-3
44301803 167232 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindololBinding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindolol
ChEMBL 588 12 3 7 5.6 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(Cc3ccc(F)cc3)cs2)cc1 10.1016/s0960-894x(00)00390-5
CHEMBL430594 167232 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindololBinding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindolol
ChEMBL 588 12 3 7 5.6 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(Cc3ccc(F)cc3)cs2)cc1 10.1016/s0960-894x(00)00390-5
12049917 201328 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity for clone human Beta-2 adrenergic receptor from CHO cell membranes in the presence of I-iodocyanopindololBinding affinity for clone human Beta-2 adrenergic receptor from CHO cell membranes in the presence of I-iodocyanopindolol
ChEMBL 588 12 3 9 4.1 COc1ccc(-c2cnn(-c3ccc(S(=O)(=O)Nc4ccc(CCNC[C@H](O)c5cccnc5)cc4)cc3)n2)cc1F 10.1016/s0960-894x(00)00422-4
CHEMBL63357 201328 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity for clone human Beta-2 adrenergic receptor from CHO cell membranes in the presence of I-iodocyanopindololBinding affinity for clone human Beta-2 adrenergic receptor from CHO cell membranes in the presence of I-iodocyanopindolol
ChEMBL 588 12 3 9 4.1 COc1ccc(-c2cnn(-c3ccc(S(=O)(=O)Nc4ccc(CCNC[C@H](O)c5cccnc5)cc4)cc3)n2)cc1F 10.1016/s0960-894x(00)00422-4
15483880 99138 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindolol
ChEMBL 591 12 3 8 4.7 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(Cc3ccc(F)c(F)c3)no2)cc1 10.1016/s0960-894x(00)00268-7
CHEMBL28405 99138 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindolol
ChEMBL 591 12 3 8 4.7 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(Cc3ccc(F)c(F)c3)no2)cc1 10.1016/s0960-894x(00)00268-7
44281395 99455 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindolol
ChEMBL 587 13 4 10 4.1 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2noc(COc3ccccc3O)n2)cc1 10.1016/s0960-894x(00)00268-7
CHEMBL286231 99455 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindolol
ChEMBL 587 13 4 10 4.1 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2noc(COc3ccccc3O)n2)cc1 10.1016/s0960-894x(00)00268-7
44281407 99828 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindolol
ChEMBL 666 14 4 10 3.6 CS(=O)(=O)NC(c1ccc(F)cc1)c1nc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)no1 10.1016/s0960-894x(00)00268-7
CHEMBL289248 99828 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindolol
ChEMBL 666 14 4 10 3.6 CS(=O)(=O)NC(c1ccc(F)cc1)c1nc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)no1 10.1016/s0960-894x(00)00268-7
44281470 113062 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindolol
ChEMBL 589 12 4 9 4.0 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2noc(C(O)c3ccc(F)cc3)n2)cc1 10.1016/s0960-894x(00)00268-7
CHEMBL33224 113062 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindolol
ChEMBL 589 12 4 9 4.0 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2noc(C(O)c3ccc(F)cc3)n2)cc1 10.1016/s0960-894x(00)00268-7
44280858 99339 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity towards Beta-2 adrenergic receptor prepared from CHO cells expressing the cloned human receptor in the presence of [125I]iodocyanopindololBinding affinity towards Beta-2 adrenergic receptor prepared from CHO cells expressing the cloned human receptor in the presence of [125I]iodocyanopindolol
ChEMBL 577 17 3 8 5.7 CCCCCCCCc1nc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)no1 10.1016/s0960-894x(00)00267-5
CHEMBL285458 99339 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity towards Beta-2 adrenergic receptor prepared from CHO cells expressing the cloned human receptor in the presence of [125I]iodocyanopindololBinding affinity towards Beta-2 adrenergic receptor prepared from CHO cells expressing the cloned human receptor in the presence of [125I]iodocyanopindolol
ChEMBL 577 17 3 8 5.7 CCCCCCCCc1nc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)no1 10.1016/s0960-894x(00)00267-5
12017015 122565 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.
ChEMBL 546 12 3 7 5.1 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2cnc(CC3CCCC3)o2)cc1 10.1016/s0960-894x(00)00277-8
CHEMBL36101 122565 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.
ChEMBL 546 12 3 7 5.1 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2cnc(CC3CCCC3)o2)cc1 10.1016/s0960-894x(00)00277-8
44298306 101516 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
In vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 435 6 1 3 4.1 CN(CCc1ccccc1)C(=O)N1CCc2cc(S(=O)(=O)Nc3ccccc3)ccc21 10.1016/s0960-894x(99)00277-2
CHEMBL301594 101516 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
In vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 435 6 1 3 4.1 CN(CCc1ccccc1)C(=O)N1CCc2cc(S(=O)(=O)Nc3ccccc3)ccc21 10.1016/s0960-894x(99)00277-2
9804668 69855 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]dihydroalprenolol from beta2-adrenoceptor after 90 mins by liquid scintillation countingDisplacement of [3H]dihydroalprenolol from beta2-adrenoceptor after 90 mins by liquid scintillation counting
ChEMBL 468 12 8 8 2.1 OCc1cc(C(O)CNCCc2ccc(NCC(O)c3ccc(O)c(CO)c3)cc2)ccc1O 10.1016/j.bmcl.2011.11.072
CHEMBL1940812 69855 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]dihydroalprenolol from beta2-adrenoceptor after 90 mins by liquid scintillation countingDisplacement of [3H]dihydroalprenolol from beta2-adrenoceptor after 90 mins by liquid scintillation counting
ChEMBL 468 12 8 8 2.1 OCc1cc(C(O)CNCCc2ccc(NCC(O)c3ccc(O)c(CO)c3)cc2)ccc1O 10.1016/j.bmcl.2011.11.072
22986860 69857 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]dihydroalprenolol from beta2-adrenoceptor after 90 mins by liquid scintillation countingDisplacement of [3H]dihydroalprenolol from beta2-adrenoceptor after 90 mins by liquid scintillation counting
ChEMBL 376 10 4 4 3.7 OC(CNCCc1ccc(NCC(O)c2ccccc2)cc1)c1ccccc1 10.1016/j.bmcl.2011.11.072
CHEMBL1940814 69857 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]dihydroalprenolol from beta2-adrenoceptor after 90 mins by liquid scintillation countingDisplacement of [3H]dihydroalprenolol from beta2-adrenoceptor after 90 mins by liquid scintillation counting
ChEMBL 376 10 4 4 3.7 OC(CNCCc1ccc(NCC(O)c2ccccc2)cc1)c1ccccc1 10.1016/j.bmcl.2011.11.072
57401436 70043 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 479 11 5 7 3.5 COc1ccccc1CNCc1ccc(CCNC[C@@H](O)c2ccc(O)c3[nH]c(=O)sc23)cc1 10.1016/j.bmcl.2011.10.049
CHEMBL1945504 70043 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 479 11 5 7 3.5 COc1ccccc1CNCc1ccc(CCNC[C@@H](O)c2ccc(O)c3[nH]c(=O)sc23)cc1 10.1016/j.bmcl.2011.10.049
76322045 105420 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]-cyanopindolol from recombinant human beta-2 adrenergic receptor expressed in CHO cell membranes after 1 hr by scintillation counting analysisDisplacement of [125I]-cyanopindolol from recombinant human beta-2 adrenergic receptor expressed in CHO cell membranes after 1 hr by scintillation counting analysis
ChEMBL 527 7 3 5 6.0 O=C(Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1)[C@@H]1CCc2sc(-c3ccc(F)cc3)nc21 10.1021/jm4017224
CHEMBL3128184 105420 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]-cyanopindolol from recombinant human beta-2 adrenergic receptor expressed in CHO cell membranes after 1 hr by scintillation counting analysisDisplacement of [125I]-cyanopindolol from recombinant human beta-2 adrenergic receptor expressed in CHO cell membranes after 1 hr by scintillation counting analysis
ChEMBL 527 7 3 5 6.0 O=C(Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1)[C@@H]1CCc2sc(-c3ccc(F)cc3)nc21 10.1021/jm4017224
1786 2474 79 None -25 11 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O nan
4171 2474 79 None -25 11 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O nan
553 2474 79 None -25 11 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O nan
CHEMBL13 2474 79 None -25 11 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O nan
DB00264 2474 79 None -25 11 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O nan
44349588 116449 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cells
ChEMBL 628 16 4 7 8.0 CCCCCCCCc1csc(N2CCc3cc(N/C(S)=N/c4ccc(CCNC[C@H](O)c5cccnc5)cc4)ccc32)n1 10.1016/s0960-894x(00)00669-7
CHEMBL338664 116449 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cells
ChEMBL 628 16 4 7 8.0 CCCCCCCCc1csc(N2CCc3cc(N/C(S)=N/c4ccc(CCNC[C@H](O)c5cccnc5)cc4)ccc32)n1 10.1016/s0960-894x(00)00669-7
10841171 116510 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity was evaluated on chinese hamster ovary (CHO) cells expressing the cloned human beta-2 adrenergic receptor in the presence of [125I]- iodocyanopindolol.Binding affinity was evaluated on chinese hamster ovary (CHO) cells expressing the cloned human beta-2 adrenergic receptor in the presence of [125I]- iodocyanopindolol.
ChEMBL 592 11 3 7 5.8 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3ccc(F)cc3F)cs2)cc1 10.1021/jm000286i
CHEMBL338976 116510 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity was evaluated on chinese hamster ovary (CHO) cells expressing the cloned human beta-2 adrenergic receptor in the presence of [125I]- iodocyanopindolol.Binding affinity was evaluated on chinese hamster ovary (CHO) cells expressing the cloned human beta-2 adrenergic receptor in the presence of [125I]- iodocyanopindolol.
ChEMBL 592 11 3 7 5.8 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3ccc(F)cc3F)cs2)cc1 10.1021/jm000286i
14739893 4198 0 None - 0 Dog 4.6 pIC50 = 4.6 Binding
Tested for Beta-2 adrenergic receptor selectivity in canine lung tissue in anesthetized dogsTested for Beta-2 adrenergic receptor selectivity in canine lung tissue in anesthetized dogs
ChEMBL 416 10 3 7 1.8 CS(=O)(=O)Nc1ccc(OCC(O)CNCc2ccc(-n3ccnc3)cc2)cc1 10.1021/jm00172a033
CHEMBL100624 4198 0 None - 0 Dog 4.6 pIC50 = 4.6 Binding
Tested for Beta-2 adrenergic receptor selectivity in canine lung tissue in anesthetized dogsTested for Beta-2 adrenergic receptor selectivity in canine lung tissue in anesthetized dogs
ChEMBL 416 10 3 7 1.8 CS(=O)(=O)Nc1ccc(OCC(O)CNCc2ccc(-n3ccnc3)cc2)cc1 10.1021/jm00172a033
10076885 99310 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity towards Beta-2 adrenergic receptor prepared from CHO cells expressing the cloned human receptor in the presence of [125I]iodocyanopindololBinding affinity towards Beta-2 adrenergic receptor prepared from CHO cells expressing the cloned human receptor in the presence of [125I]iodocyanopindolol
ChEMBL 577 14 3 9 4.3 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2noc(CCOC3CCCC3)n2)cc1 10.1016/s0960-894x(00)00267-5
CHEMBL285242 99310 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity towards Beta-2 adrenergic receptor prepared from CHO cells expressing the cloned human receptor in the presence of [125I]iodocyanopindololBinding affinity towards Beta-2 adrenergic receptor prepared from CHO cells expressing the cloned human receptor in the presence of [125I]iodocyanopindolol
ChEMBL 577 14 3 9 4.3 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2noc(CCOC3CCCC3)n2)cc1 10.1016/s0960-894x(00)00267-5
10442852 11095 0 None - 2 Guinea pig 6.6 pIC50 = 6.6 Binding
Inhibitory concentration against beta-2-adrenergic receptor in isolated guinea pig tracheal stripsInhibitory concentration against beta-2-adrenergic receptor in isolated guinea pig tracheal strips
ChEMBL 202 6 2 4 1.1 CCCO/N=C/C(O)CNC(C)(C)C 10.1021/jm00036a018
CHEMBL1178755 11095 0 None - 2 Guinea pig 6.6 pIC50 = 6.6 Binding
Inhibitory concentration against beta-2-adrenergic receptor in isolated guinea pig tracheal stripsInhibitory concentration against beta-2-adrenergic receptor in isolated guinea pig tracheal strips
ChEMBL 202 6 2 4 1.1 CCCO/N=C/C(O)CNC(C)(C)C 10.1021/jm00036a018
CHEMBL39706 11095 0 None - 2 Guinea pig 6.6 pIC50 = 6.6 Binding
Inhibitory concentration against beta-2-adrenergic receptor in isolated guinea pig tracheal stripsInhibitory concentration against beta-2-adrenergic receptor in isolated guinea pig tracheal strips
ChEMBL 202 6 2 4 1.1 CCCO/N=C/C(O)CNC(C)(C)C 10.1021/jm00036a018
44285634 99929 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.
ChEMBL 576 17 3 7 6.3 CCCCCCCCc1ncc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)o1 10.1016/s0960-894x(00)00277-8
CHEMBL290131 99929 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.
ChEMBL 576 17 3 7 6.3 CCCCCCCCc1ncc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)o1 10.1016/s0960-894x(00)00277-8
3157 1437 69 None -97 12 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 nan
7170 1437 69 None -97 12 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 nan
954 1437 69 None -97 12 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 nan
CHEMBL707 1437 69 None -97 12 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 nan
DB00590 1437 69 None -97 12 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 nan
1043 1545 13 None -20892 29 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
149 1545 13 None -20892 29 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
8223 1545 13 None -20892 29 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
CHEMBL442 1545 13 None -20892 29 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
DB00696 1545 13 None -20892 29 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
44303198 201459 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cell
ChEMBL 568 11 4 7 2.6 Nc1ccc(OC[C@@H](O)CNCCc2ccc(NS(=O)(=O)c3ccc(I)cc3)cc2)cn1 10.1016/s0960-894x(98)00381-3
CHEMBL64201 201459 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cell
ChEMBL 568 11 4 7 2.6 Nc1ccc(OC[C@@H](O)CNCCc2ccc(NS(=O)(=O)c3ccc(I)cc3)cc2)cn1 10.1016/s0960-894x(98)00381-3
165193 3126 60 None -4 43 Guinea pig 7.5 pIC50 = 7.5 Binding
Inhibitory activity against beta-2 adrenergic receptor in guinea pig tracheal strip is determinedInhibitory activity against beta-2 adrenergic receptor in guinea pig tracheal strip is determined
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00073a006
2303 3126 60 None -4 43 Guinea pig 7.5 pIC50 = 7.5 Binding
Inhibitory activity against beta-2 adrenergic receptor in guinea pig tracheal strip is determinedInhibitory activity against beta-2 adrenergic receptor in guinea pig tracheal strip is determined
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00073a006
4946 3126 60 None -4 43 Guinea pig 7.5 pIC50 = 7.5 Binding
Inhibitory activity against beta-2 adrenergic receptor in guinea pig tracheal strip is determinedInhibitory activity against beta-2 adrenergic receptor in guinea pig tracheal strip is determined
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00073a006
564 3126 60 None -4 43 Guinea pig 7.5 pIC50 = 7.5 Binding
Inhibitory activity against beta-2 adrenergic receptor in guinea pig tracheal strip is determinedInhibitory activity against beta-2 adrenergic receptor in guinea pig tracheal strip is determined
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00073a006
62882 3126 60 None -4 43 Guinea pig 7.5 pIC50 = 7.5 Binding
Inhibitory activity against beta-2 adrenergic receptor in guinea pig tracheal strip is determinedInhibitory activity against beta-2 adrenergic receptor in guinea pig tracheal strip is determined
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00073a006
63 3126 60 None -4 43 Guinea pig 7.5 pIC50 = 7.5 Binding
Inhibitory activity against beta-2 adrenergic receptor in guinea pig tracheal strip is determinedInhibitory activity against beta-2 adrenergic receptor in guinea pig tracheal strip is determined
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00073a006
66366 3126 60 None -4 43 Guinea pig 7.5 pIC50 = 7.5 Binding
Inhibitory activity against beta-2 adrenergic receptor in guinea pig tracheal strip is determinedInhibitory activity against beta-2 adrenergic receptor in guinea pig tracheal strip is determined
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00073a006
91536 3126 60 None -4 43 Guinea pig 7.5 pIC50 = 7.5 Binding
Inhibitory activity against beta-2 adrenergic receptor in guinea pig tracheal strip is determinedInhibitory activity against beta-2 adrenergic receptor in guinea pig tracheal strip is determined
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00073a006
CHEMBL27 3126 60 None -4 43 Guinea pig 7.5 pIC50 = 7.5 Binding
Inhibitory activity against beta-2 adrenergic receptor in guinea pig tracheal strip is determinedInhibitory activity against beta-2 adrenergic receptor in guinea pig tracheal strip is determined
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00073a006
CHEMBL452861 3126 60 None -4 43 Guinea pig 7.5 pIC50 = 7.5 Binding
Inhibitory activity against beta-2 adrenergic receptor in guinea pig tracheal strip is determinedInhibitory activity against beta-2 adrenergic receptor in guinea pig tracheal strip is determined
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00073a006
DB00571 3126 60 None -4 43 Guinea pig 7.5 pIC50 = 7.5 Binding
Inhibitory activity against beta-2 adrenergic receptor in guinea pig tracheal strip is determinedInhibitory activity against beta-2 adrenergic receptor in guinea pig tracheal strip is determined
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00073a006
44268324 16590 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandBinding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligand
ChEMBL 476 11 4 6 3.4 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1)c1ccc(Cl)cc1 10.1016/s0960-894x(98)00169-3
CHEMBL12450 16590 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandBinding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligand
ChEMBL 476 11 4 6 3.4 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1)c1ccc(Cl)cc1 10.1016/s0960-894x(98)00169-3
1028 287 69 None -89 30 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O nan
139148732 287 69 None -89 30 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O nan
479 287 69 None -89 30 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O nan
5816 287 69 None -89 30 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O nan
CHEMBL679 287 69 None -89 30 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O nan
DB00668 287 69 None -89 30 Human 6.6 pIC50 = 6.6 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O nan
44268569 97729 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.
ChEMBL 598 17 5 7 4.5 CCCCCCNC(=O)N(C)c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/s0960-894x(98)00170-x
CHEMBL274143 97729 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.
ChEMBL 598 17 5 7 4.5 CCCCCCNC(=O)N(C)c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/s0960-894x(98)00170-x
81430 198400 100 None - 1 Dog 4.5 pIC50 = 4.5 Binding
Binding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprololBinding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprolol
ChEMBL 192 2 1 3 1.1 COc1cccc(N2CCNCC2)c1 10.1021/jm00082a016
CHEMBL59597 198400 100 None - 1 Dog 4.5 pIC50 = 4.5 Binding
Binding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprololBinding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprolol
ChEMBL 192 2 1 3 1.1 COc1cccc(N2CCNCC2)c1 10.1021/jm00082a016
91965 206280 88 None - 2 Dog 4.5 pIC50 = 4.5 Binding
Binding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprololBinding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprolol
ChEMBL 176 1 1 2 1.4 Cc1ccccc1N1CCNCC1 10.1021/jm00082a016
CHEMBL9746 206280 88 None - 2 Dog 4.5 pIC50 = 4.5 Binding
Binding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprololBinding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprolol
ChEMBL 176 1 1 2 1.4 Cc1ccccc1N1CCNCC1 10.1021/jm00082a016
3682 188837 7 None 1 8 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]CGP1217 from human recombinant adrenergic beta2 receptor transfected in insect Sf9 cells by scintillation countingDisplacement of [3H]CGP1217 from human recombinant adrenergic beta2 receptor transfected in insect Sf9 cells by scintillation counting
ChEMBL 277 6 2 3 2.6 Cc1ccc(OCC(O)C(C)NC(C)C)c2c1CCC2 10.1021/jm801211c
CHEMBL1256784 188837 7 None 1 8 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]CGP1217 from human recombinant adrenergic beta2 receptor transfected in insect Sf9 cells by scintillation countingDisplacement of [3H]CGP1217 from human recombinant adrenergic beta2 receptor transfected in insect Sf9 cells by scintillation counting
ChEMBL 277 6 2 3 2.6 Cc1ccc(OCC(O)C(C)NC(C)C)c2c1CCC2 10.1021/jm801211c
CHEMBL513389 188837 7 None 1 8 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]CGP1217 from human recombinant adrenergic beta2 receptor transfected in insect Sf9 cells by scintillation countingDisplacement of [3H]CGP1217 from human recombinant adrenergic beta2 receptor transfected in insect Sf9 cells by scintillation counting
ChEMBL 277 6 2 3 2.6 Cc1ccc(OCC(O)C(C)NC(C)C)c2c1CCC2 10.1021/jm801211c
71566170 144369 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 ug/well for beta1 and 5 ug/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 ul, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 uM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 ug/well for beta1 and 5 ug/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 ul, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 uM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.
ChEMBL 774 17 7 12 4.5 CC(Cc1ccc(OCC(=O)NCCN[C@H]2CC[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)CC2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3910208 144369 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 ug/well for beta1 and 5 ug/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 ul, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 uM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 ug/well for beta1 and 5 ug/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 ul, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 uM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.
ChEMBL 774 17 7 12 4.5 CC(Cc1ccc(OCC(=O)NCCN[C@H]2CC[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)CC2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
16735261 85292 0 None 47 2 Human 8.5 pIC50 = 8.5 Binding
Mitogenesis inhibition method: To measure beta2-AR mediated inhibition of mitogenesis, HEK-beta2-AR, 1321N1 or U87MG cells were seeded in a 96-well plate at approximately 5,000 cells/well. After 48 hours, the wells were rinsed twice and the medium was replaced with fresh medium containing 10 uL of drug in sterile water. After another 24 hours of incubation at 37° C., 0.25 uCi of [3H]-thymidine was added to each well. The cells were incubated for an additional 2 hours at 37° C., at which point 10 uL of 10x trypsin was added, and the resuspended cells were harvested using a Tomtec 96 harvester through glass fiber filters.Mitogenesis inhibition method: To measure beta2-AR mediated inhibition of mitogenesis, HEK-beta2-AR, 1321N1 or U87MG cells were seeded in a 96-well plate at approximately 5,000 cells/well. After 48 hours, the wells were rinsed twice and the medium was replaced with fresh medium containing 10 uL of drug in sterile water. After another 24 hours of incubation at 37° C., 0.25 uCi of [3H]-thymidine was added to each well. The cells were incubated for an additional 2 hours at 37° C., at which point 10 uL of 10x trypsin was added, and the resuspended cells were harvested using a Tomtec 96 harvester through glass fiber filters.
ChEMBL 317 7 4 5 2.4 COc1ccc(C[C@@H](C)NC[C@@H](O)c2cc(O)cc(O)c2)cc1 nan
CHEMBL228998 85292 0 None 47 2 Human 8.5 pIC50 = 8.5 Binding
Mitogenesis inhibition method: To measure beta2-AR mediated inhibition of mitogenesis, HEK-beta2-AR, 1321N1 or U87MG cells were seeded in a 96-well plate at approximately 5,000 cells/well. After 48 hours, the wells were rinsed twice and the medium was replaced with fresh medium containing 10 uL of drug in sterile water. After another 24 hours of incubation at 37° C., 0.25 uCi of [3H]-thymidine was added to each well. The cells were incubated for an additional 2 hours at 37° C., at which point 10 uL of 10x trypsin was added, and the resuspended cells were harvested using a Tomtec 96 harvester through glass fiber filters.Mitogenesis inhibition method: To measure beta2-AR mediated inhibition of mitogenesis, HEK-beta2-AR, 1321N1 or U87MG cells were seeded in a 96-well plate at approximately 5,000 cells/well. After 48 hours, the wells were rinsed twice and the medium was replaced with fresh medium containing 10 uL of drug in sterile water. After another 24 hours of incubation at 37° C., 0.25 uCi of [3H]-thymidine was added to each well. The cells were incubated for an additional 2 hours at 37° C., at which point 10 uL of 10x trypsin was added, and the resuspended cells were harvested using a Tomtec 96 harvester through glass fiber filters.
ChEMBL 317 7 4 5 2.4 COc1ccc(C[C@@H](C)NC[C@@H](O)c2cc(O)cc(O)c2)cc1 nan
16738927 70000 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 464 11 5 7 2.9 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3ccc(CNCCc4ccccn4)cc3)c2s1 10.1016/j.bmcl.2011.10.049
CHEMBL1945034 70000 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 464 11 5 7 2.9 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3ccc(CNCCc4ccccn4)cc3)c2s1 10.1016/j.bmcl.2011.10.049
137 367 47 None -3 12 Human 8.5 pIC50 = 8.5 Binding
Antagonist activity at human recombinant beta2 adrenoreceptor expressed in CHOK1 cells incubated for 30 mins by HTRFAntagonist activity at human recombinant beta2 adrenoreceptor expressed in CHOK1 cells incubated for 30 mins by HTRF
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1039/C8MD00412A
2119 367 47 None -3 12 Human 8.5 pIC50 = 8.5 Binding
Antagonist activity at human recombinant beta2 adrenoreceptor expressed in CHOK1 cells incubated for 30 mins by HTRFAntagonist activity at human recombinant beta2 adrenoreceptor expressed in CHOK1 cells incubated for 30 mins by HTRF
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1039/C8MD00412A
563 367 47 None -3 12 Human 8.5 pIC50 = 8.5 Binding
Antagonist activity at human recombinant beta2 adrenoreceptor expressed in CHOK1 cells incubated for 30 mins by HTRFAntagonist activity at human recombinant beta2 adrenoreceptor expressed in CHOK1 cells incubated for 30 mins by HTRF
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1039/C8MD00412A
66368 367 47 None -3 12 Human 8.5 pIC50 = 8.5 Binding
Antagonist activity at human recombinant beta2 adrenoreceptor expressed in CHOK1 cells incubated for 30 mins by HTRFAntagonist activity at human recombinant beta2 adrenoreceptor expressed in CHOK1 cells incubated for 30 mins by HTRF
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1039/C8MD00412A
CHEMBL266195 367 47 None -3 12 Human 8.5 pIC50 = 8.5 Binding
Antagonist activity at human recombinant beta2 adrenoreceptor expressed in CHOK1 cells incubated for 30 mins by HTRFAntagonist activity at human recombinant beta2 adrenoreceptor expressed in CHOK1 cells incubated for 30 mins by HTRF
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1039/C8MD00412A
DB00866 367 47 None -3 12 Human 8.5 pIC50 = 8.5 Binding
Antagonist activity at human recombinant beta2 adrenoreceptor expressed in CHOK1 cells incubated for 30 mins by HTRFAntagonist activity at human recombinant beta2 adrenoreceptor expressed in CHOK1 cells incubated for 30 mins by HTRF
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1039/C8MD00412A
2419 3394 80 None - 6 Guinea pig 8.5 pIC50 = 8.5 Binding
Agonist activity at adrenergic beta2 receptor in electrically-stimulated Dunkin-Hartley guinea pig tracheal strip assessed as inhibition of contractionAgonist activity at adrenergic beta2 receptor in electrically-stimulated Dunkin-Hartley guinea pig tracheal strip assessed as inhibition of contraction
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2014.06.014
5152 3394 80 None - 6 Guinea pig 8.5 pIC50 = 8.5 Binding
Agonist activity at adrenergic beta2 receptor in electrically-stimulated Dunkin-Hartley guinea pig tracheal strip assessed as inhibition of contractionAgonist activity at adrenergic beta2 receptor in electrically-stimulated Dunkin-Hartley guinea pig tracheal strip assessed as inhibition of contraction
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2014.06.014
559 3394 80 None - 6 Guinea pig 8.5 pIC50 = 8.5 Binding
Agonist activity at adrenergic beta2 receptor in electrically-stimulated Dunkin-Hartley guinea pig tracheal strip assessed as inhibition of contractionAgonist activity at adrenergic beta2 receptor in electrically-stimulated Dunkin-Hartley guinea pig tracheal strip assessed as inhibition of contraction
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2014.06.014
CHEMBL1263 3394 80 None - 6 Guinea pig 8.5 pIC50 = 8.5 Binding
Agonist activity at adrenergic beta2 receptor in electrically-stimulated Dunkin-Hartley guinea pig tracheal strip assessed as inhibition of contractionAgonist activity at adrenergic beta2 receptor in electrically-stimulated Dunkin-Hartley guinea pig tracheal strip assessed as inhibition of contraction
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2014.06.014
DB00938 3394 80 None - 6 Guinea pig 8.5 pIC50 = 8.5 Binding
Agonist activity at adrenergic beta2 receptor in electrically-stimulated Dunkin-Hartley guinea pig tracheal strip assessed as inhibition of contractionAgonist activity at adrenergic beta2 receptor in electrically-stimulated Dunkin-Hartley guinea pig tracheal strip assessed as inhibition of contraction
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2014.06.014
53380558 63302 2 None - 1 Human 8.4 pIC50 = 8.4 Binding
Mitogenesis inhibition method: To measure beta2-AR mediated inhibition of mitogenesis, HEK-beta2-AR, 1321N1 or U87MG cells were seeded in a 96-well plate at approximately 5,000 cells/well. After 48 hours, the wells were rinsed twice and the medium was replaced with fresh medium containing 10 uL of drug in sterile water. After another 24 hours of incubation at 37° C., 0.25 uCi of [3H]-thymidine was added to each well. The cells were incubated for an additional 2 hours at 37° C., at which point 10 uL of 10x trypsin was added, and the resuspended cells were harvested using a Tomtec 96 harvester through glass fiber filters.Mitogenesis inhibition method: To measure beta2-AR mediated inhibition of mitogenesis, HEK-beta2-AR, 1321N1 or U87MG cells were seeded in a 96-well plate at approximately 5,000 cells/well. After 48 hours, the wells were rinsed twice and the medium was replaced with fresh medium containing 10 uL of drug in sterile water. After another 24 hours of incubation at 37° C., 0.25 uCi of [3H]-thymidine was added to each well. The cells were incubated for an additional 2 hours at 37° C., at which point 10 uL of 10x trypsin was added, and the resuspended cells were harvested using a Tomtec 96 harvester through glass fiber filters.
ChEMBL 367 7 4 5 3.5 COc1ccc(C[C@@H](C)NC[C@H](O)c2cc(O)cc(O)c2)c2ccccc12 nan
CHEMBL1800963 63302 2 None - 1 Human 8.4 pIC50 = 8.4 Binding
Mitogenesis inhibition method: To measure beta2-AR mediated inhibition of mitogenesis, HEK-beta2-AR, 1321N1 or U87MG cells were seeded in a 96-well plate at approximately 5,000 cells/well. After 48 hours, the wells were rinsed twice and the medium was replaced with fresh medium containing 10 uL of drug in sterile water. After another 24 hours of incubation at 37° C., 0.25 uCi of [3H]-thymidine was added to each well. The cells were incubated for an additional 2 hours at 37° C., at which point 10 uL of 10x trypsin was added, and the resuspended cells were harvested using a Tomtec 96 harvester through glass fiber filters.Mitogenesis inhibition method: To measure beta2-AR mediated inhibition of mitogenesis, HEK-beta2-AR, 1321N1 or U87MG cells were seeded in a 96-well plate at approximately 5,000 cells/well. After 48 hours, the wells were rinsed twice and the medium was replaced with fresh medium containing 10 uL of drug in sterile water. After another 24 hours of incubation at 37° C., 0.25 uCi of [3H]-thymidine was added to each well. The cells were incubated for an additional 2 hours at 37° C., at which point 10 uL of 10x trypsin was added, and the resuspended cells were harvested using a Tomtec 96 harvester through glass fiber filters.
ChEMBL 367 7 4 5 3.5 COc1ccc(C[C@@H](C)NC[C@H](O)c2cc(O)cc(O)c2)c2ccccc12 nan
24901348 69969 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 531 11 5 6 4.8 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3ccc(CNCCc4c(Cl)cccc4Cl)cc3)c2s1 10.1016/j.bmcl.2011.10.049
CHEMBL1944689 69969 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 531 11 5 6 4.8 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3ccc(CNCCc4c(Cl)cccc4Cl)cc3)c2s1 10.1016/j.bmcl.2011.10.049
24900937 70026 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 413 8 4 6 2.8 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3cccc(CN4CCCC4)c3)c2s1 10.1016/j.bmcl.2011.10.049
CHEMBL1945294 70026 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 413 8 4 6 2.8 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3cccc(CN4CCCC4)c3)c2s1 10.1016/j.bmcl.2011.10.049
24901140 70176 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 503 9 4 6 4.5 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3cccc(CN4CCC(c5ccccc5)CC4)c3)c2s1 10.1016/j.bmcl.2011.10.049
CHEMBL1947153 70176 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 503 9 4 6 4.5 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3cccc(CN4CCC(c5ccccc5)CC4)c3)c2s1 10.1016/j.bmcl.2011.10.049
14823035 141019 2 None - 3 Rat 7.5 pIC50 = 7.5 Binding
Compound was evaluated for its binding affinity towards Beta-2 adrenergic receptor in rat soleus membrane by displacing (-)-isoproterenol (50 uM)Compound was evaluated for its binding affinity towards Beta-2 adrenergic receptor in rat soleus membrane by displacing (-)-isoproterenol (50 uM)
ChEMBL 377 9 2 5 3.1 COC(=O)COc1ccc(C[C@@H](C)NC[C@H](O)c2cccc(Cl)c2)cc1 10.1021/jm00094a025
CHEMBL38486 141019 2 None - 3 Rat 7.5 pIC50 = 7.5 Binding
Compound was evaluated for its binding affinity towards Beta-2 adrenergic receptor in rat soleus membrane by displacing (-)-isoproterenol (50 uM)Compound was evaluated for its binding affinity towards Beta-2 adrenergic receptor in rat soleus membrane by displacing (-)-isoproterenol (50 uM)
ChEMBL 377 9 2 5 3.1 COC(=O)COc1ccc(C[C@@H](C)NC[C@H](O)c2cccc(Cl)c2)cc1 10.1021/jm00094a025
2447484 102282 2 None - 2 Bovine 7.5 pIC50 = 7.5 Binding
Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-2 adrenergic receptor in calf lung membranes.Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-2 adrenergic receptor in calf lung membranes.
ChEMBL 324 5 2 4 3.2 CC(C)(C)NC[C@H](O)CON=C1c2ccccc2-c2ccccc21 10.1021/jm00350a009
CHEMBL305153 102282 2 None - 2 Bovine 7.5 pIC50 = 7.5 Binding
Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-2 adrenergic receptor in calf lung membranes.Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-2 adrenergic receptor in calf lung membranes.
ChEMBL 324 5 2 4 3.2 CC(C)(C)NC[C@H](O)CON=C1c2ccccc2-c2ccccc21 10.1021/jm00350a009
44338637 109024 0 None - 0 Guinea pig 6.5 pIC50 = 6.5 Binding
Beta-2 adrenergic receptor blocking was assessed from 50% inhibition of the isoproterenol submaximal response on isolated Guinea pig trachea(IT)Beta-2 adrenergic receptor blocking was assessed from 50% inhibition of the isoproterenol submaximal response on isolated Guinea pig trachea(IT)
ChEMBL 346 7 2 5 2.8 COC12CCCCC1c1ccccc1/C2=N/OCC(O)CNC(C)C 10.1021/jm00122a008
CHEMBL322130 109024 0 None - 0 Guinea pig 6.5 pIC50 = 6.5 Binding
Beta-2 adrenergic receptor blocking was assessed from 50% inhibition of the isoproterenol submaximal response on isolated Guinea pig trachea(IT)Beta-2 adrenergic receptor blocking was assessed from 50% inhibition of the isoproterenol submaximal response on isolated Guinea pig trachea(IT)
ChEMBL 346 7 2 5 2.8 COC12CCCCC1c1ccccc1/C2=N/OCC(O)CNC(C)C 10.1021/jm00122a008
9802994 185753 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity to beta2 adrenoceptorBinding affinity to beta2 adrenoceptor
ChEMBL 397 9 2 4 4.4 COc1ccc(CC(C)(C)NC[C@@H](O)COc2cccc(Cl)c2Cl)cc1 10.1021/jm900364m
CHEMBL487507 185753 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity to beta2 adrenoceptorBinding affinity to beta2 adrenoceptor
ChEMBL 397 9 2 4 4.4 COc1ccc(CC(C)(C)NC[C@@H](O)COc2cccc(Cl)c2Cl)cc1 10.1021/jm900364m
44313090 102682 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibitory activity against CHO cells expressing human Beta-2 adrenergic receptor with [125I]-iodocyanopindololInhibitory activity against CHO cells expressing human Beta-2 adrenergic receptor with [125I]-iodocyanopindolol
ChEMBL 568 12 6 7 4.9 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(OCC3NCCc4cc(O)c(O)cc43)cc2)cc1 10.1016/s0960-894x(00)00459-5
CHEMBL308126 102682 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibitory activity against CHO cells expressing human Beta-2 adrenergic receptor with [125I]-iodocyanopindololInhibitory activity against CHO cells expressing human Beta-2 adrenergic receptor with [125I]-iodocyanopindolol
ChEMBL 568 12 6 7 4.9 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(OCC3NCCc4cc(O)c(O)cc43)cc2)cc1 10.1016/s0960-894x(00)00459-5
44312949 202060 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibitory activity against CHO cells expressing human Beta-2 adrenergic receptor with [125I]-iodocyanopindololInhibitory activity against CHO cells expressing human Beta-2 adrenergic receptor with [125I]-iodocyanopindolol
ChEMBL 602 11 6 6 6.2 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc3cc(CC4NCCc5cc(O)c(O)cc54)ccc3c2)cc1 10.1016/s0960-894x(00)00459-5
CHEMBL67998 202060 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibitory activity against CHO cells expressing human Beta-2 adrenergic receptor with [125I]-iodocyanopindololInhibitory activity against CHO cells expressing human Beta-2 adrenergic receptor with [125I]-iodocyanopindolol
ChEMBL 602 11 6 6 6.2 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc3cc(CC4NCCc5cc(O)c(O)cc54)ccc3c2)cc1 10.1016/s0960-894x(00)00459-5
567 715 10 None -4 5 Human 5.5 pIC50 = 5.5 Binding
Beta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindolol
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1016/s0960-894x(98)00571-x
9841972 715 10 None -4 5 Human 5.5 pIC50 = 5.5 Binding
Beta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindolol
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1016/s0960-894x(98)00571-x
CHEMBL284782 715 10 None -4 5 Human 5.5 pIC50 = 5.5 Binding
Beta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindolol
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1016/s0960-894x(98)00571-x
3931 2208 42 None 3 2 Human 5.5 pIC50 = 5.5 Binding
Beta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindolol
ChEMBL 584 17 6 7 4.5 CCCCCCNC(=O)Nc1ccc(cc1)S(=O)(=O)Nc1ccc(cc1)CCNC[C@@H](COc1ccc(cc1)O)O 10.1016/s0960-894x(98)00571-x
9829836 2208 42 None 3 2 Human 5.5 pIC50 = 5.5 Binding
Beta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindolol
ChEMBL 584 17 6 7 4.5 CCCCCCNC(=O)Nc1ccc(cc1)S(=O)(=O)Nc1ccc(cc1)CCNC[C@@H](COc1ccc(cc1)O)O 10.1016/s0960-894x(98)00571-x
CHEMBL12998 2208 42 None 3 2 Human 5.5 pIC50 = 5.5 Binding
Beta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindolol
ChEMBL 584 17 6 7 4.5 CCCCCCNC(=O)Nc1ccc(cc1)S(=O)(=O)Nc1ccc(cc1)CCNC[C@@H](COc1ccc(cc1)O)O 10.1016/s0960-894x(98)00571-x
9915238 196479 1 None - 0 Human 5.5 pIC50 = 5.5 Binding
Beta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindolol
ChEMBL 539 15 5 6 4.5 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(98)00571-x
CHEMBL57486 196479 1 None - 0 Human 5.5 pIC50 = 5.5 Binding
Beta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindolol
ChEMBL 539 15 5 6 4.5 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(98)00571-x
44268358 19213 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandBinding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligand
ChEMBL 510 11 4 6 4.1 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1)c1ccc(Cl)c(Cl)c1 10.1016/s0960-894x(98)00169-3
CHEMBL12945 19213 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandBinding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligand
ChEMBL 510 11 4 6 4.1 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1)c1ccc(Cl)c(Cl)c1 10.1016/s0960-894x(98)00169-3
44268327 97834 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandBinding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligand
ChEMBL 448 11 4 6 3.0 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1)C1CCCCC1 10.1016/s0960-894x(98)00169-3
CHEMBL274807 97834 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandBinding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligand
ChEMBL 448 11 4 6 3.0 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1)C1CCCCC1 10.1016/s0960-894x(98)00169-3
44301831 100482 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindololBinding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindolol
ChEMBL 590 14 3 7 6.4 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(CCCC3CCCC3)cs2)cc1 10.1016/s0960-894x(00)00390-5
CHEMBL294172 100482 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindololBinding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindolol
ChEMBL 590 14 3 7 6.4 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(CCCC3CCCC3)cs2)cc1 10.1016/s0960-894x(00)00390-5
44301805 100534 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindololBinding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindolol
ChEMBL 557 11 3 8 4.9 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3cccnc3)cs2)cc1 10.1016/s0960-894x(00)00390-5
CHEMBL294492 100534 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindololBinding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindolol
ChEMBL 557 11 3 8 4.9 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3cccnc3)cs2)cc1 10.1016/s0960-894x(00)00390-5
44301832 199380 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindololBinding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindolol
ChEMBL 592 17 3 7 6.8 CCCCCCCCc1csc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)n1 10.1016/s0960-894x(00)00390-5
CHEMBL60281 199380 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindololBinding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindolol
ChEMBL 592 17 3 7 6.8 CCCCCCCCc1csc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)n1 10.1016/s0960-894x(00)00390-5
44281467 118848 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindolol
ChEMBL 648 14 4 10 3.8 CS(=O)(=O)Nc1ccc(Cc2nc(-c3ccc(S(=O)(=O)Nc4ccc(CCNC[C@H](O)c5cccnc5)cc4)cc3)no2)cc1 10.1016/s0960-894x(00)00268-7
CHEMBL34441 118848 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindolol
ChEMBL 648 14 4 10 3.8 CS(=O)(=O)Nc1ccc(Cc2nc(-c3ccc(S(=O)(=O)Nc4ccc(CCNC[C@H](O)c5cccnc5)cc4)cc3)no2)cc1 10.1016/s0960-894x(00)00268-7
44461468 105136 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity towards Beta-2 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindololBinding affinity towards Beta-2 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindolol
ChEMBL 608 17 4 9 3.7 CCCCCCCCn1c(=O)[nH]n(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)c1=O 10.1016/s0960-894x(99)00073-6
CHEMBL312364 105136 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity towards Beta-2 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindololBinding affinity towards Beta-2 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindolol
ChEMBL 608 17 4 9 3.7 CCCCCCCCn1c(=O)[nH]n(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)c1=O 10.1016/s0960-894x(99)00073-6
10007337 116187 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity towards Beta-2 adrenergic receptor prepared from CHO cells expressing the cloned human receptor in the presence of [125I]iodocyanopindololBinding affinity towards Beta-2 adrenergic receptor prepared from CHO cells expressing the cloned human receptor in the presence of [125I]iodocyanopindolol
ChEMBL 535 14 3 8 4.5 CCCCCc1nc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)no1 10.1016/s0960-894x(00)00267-5
CHEMBL33725 116187 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity towards Beta-2 adrenergic receptor prepared from CHO cells expressing the cloned human receptor in the presence of [125I]iodocyanopindololBinding affinity towards Beta-2 adrenergic receptor prepared from CHO cells expressing the cloned human receptor in the presence of [125I]iodocyanopindolol
ChEMBL 535 14 3 8 4.5 CCCCCc1nc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)no1 10.1016/s0960-894x(00)00267-5
9985523 98691 0 None - 5 Human 5.5 pIC50 = 5.5 Binding
Binding affinity towards cloned human Beta-2 adrenergic receptorBinding affinity towards cloned human Beta-2 adrenergic receptor
ChEMBL 572 17 2 6 6.2 NCCCCCOC[C@H]1O[C@@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2ccccc2)C[C@@H]1OCc1ccccc1 10.1021/jm960281e
CHEMBL281200 98691 0 None - 5 Human 5.5 pIC50 = 5.5 Binding
Binding affinity towards cloned human Beta-2 adrenergic receptorBinding affinity towards cloned human Beta-2 adrenergic receptor
ChEMBL 572 17 2 6 6.2 NCCCCCOC[C@H]1O[C@@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2ccccc2)C[C@@H]1OCc1ccccc1 10.1021/jm960281e
9852911 98911 0 None - 6 Human 5.5 pIC50 = 5.5 Binding
Binding affinity towards cloned human Beta-2 adrenergic receptorBinding affinity towards cloned human Beta-2 adrenergic receptor
ChEMBL 678 20 2 7 7.4 NCCCCCOC[C@H]1O[C@@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2ccccc2)[C@@H](OCc2ccccc2)[C@@H]1OCc1ccccc1 10.1021/jm960281e
CHEMBL282618 98911 0 None - 6 Human 5.5 pIC50 = 5.5 Binding
Binding affinity towards cloned human Beta-2 adrenergic receptorBinding affinity towards cloned human Beta-2 adrenergic receptor
ChEMBL 678 20 2 7 7.4 NCCCCCOC[C@H]1O[C@@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2ccccc2)[C@@H](OCc2ccccc2)[C@@H]1OCc1ccccc1 10.1021/jm960281e
46881938 6672 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counter
ChEMBL 443 9 3 4 5.2 O=C(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccccc1C1CCCCC1 10.1016/j.bmcl.2010.01.130
CHEMBL1083832 6672 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counter
ChEMBL 443 9 3 4 5.2 O=C(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccccc1C1CCCCC1 10.1016/j.bmcl.2010.01.130
44285685 99739 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.
ChEMBL 478 10 3 7 3.7 Cc1ncc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)o1 10.1016/s0960-894x(00)00277-8
CHEMBL288418 99739 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.
ChEMBL 478 10 3 7 3.7 Cc1ncc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)o1 10.1016/s0960-894x(00)00277-8
12017003 141386 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.
ChEMBL 576 11 3 7 5.3 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2cnc(-c3ccc(F)c(F)c3)o2)cc1 10.1016/s0960-894x(00)00277-8
CHEMBL38704 141386 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.
ChEMBL 576 11 3 7 5.3 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2cnc(-c3ccc(F)c(F)c3)o2)cc1 10.1016/s0960-894x(00)00277-8
9915238 196479 1 None - 0 Human 5.5 pIC50 = 5.5 Binding
In vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 539 15 5 6 4.5 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(99)00277-2
CHEMBL57486 196479 1 None - 0 Human 5.5 pIC50 = 5.5 Binding
In vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 539 15 5 6 4.5 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(99)00277-2
44285692 136690 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.
ChEMBL 478 10 3 7 3.7 Cc1nc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)co1 10.1016/s0960-894x(00)00277-8
CHEMBL37512 136690 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.
ChEMBL 478 10 3 7 3.7 Cc1nc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)co1 10.1016/s0960-894x(00)00277-8
1599 2299 47 None -131 16 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 nan
3955 2299 47 None -131 16 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 nan
7215 2299 47 None -131 16 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 nan
CHEMBL841 2299 47 None -131 16 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 nan
DB00836 2299 47 None -131 16 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 nan
13864389 4982 2 None - 2 Guinea pig 4.5 pIC50 = 4.5 Binding
Inhibitory activity against beta-2 adrenergic receptor in guinea pig tracheal strip is determinedInhibitory activity against beta-2 adrenergic receptor in guinea pig tracheal strip is determined
ChEMBL 195 1 3 4 0.7 NCC1OCCc2cc(O)c(O)cc21 10.1021/jm00073a006
CHEMBL105383 4982 2 None - 2 Guinea pig 4.5 pIC50 = 4.5 Binding
Inhibitory activity against beta-2 adrenergic receptor in guinea pig tracheal strip is determinedInhibitory activity against beta-2 adrenergic receptor in guinea pig tracheal strip is determined
ChEMBL 195 1 3 4 0.7 NCC1OCCc2cc(O)c(O)cc21 10.1021/jm00073a006
57402248 70145 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 487 9 3 5 5.1 O=c1[nH]c2c(O)ccc(CCNCCc3cccc(CN4CCC(c5ccccc5)CC4)c3)c2s1 10.1016/j.bmcl.2011.10.049
CHEMBL1946769 70145 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 487 9 3 5 5.1 O=c1[nH]c2c(O)ccc(CCNCCc3cccc(CN4CCC(c5ccccc5)CC4)c3)c2s1 10.1016/j.bmcl.2011.10.049
57393350 70175 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 509 11 4 5 5.6 O=c1[nH]c2c(O)ccc(CCNCCc3cccc(-c4cccc(CNCc5ccccc5)c4)c3)c2s1 10.1016/j.bmcl.2011.10.049
CHEMBL1947152 70175 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 509 11 4 5 5.6 O=c1[nH]c2c(O)ccc(CCNCCc3cccc(-c4cccc(CNCc5ccccc5)c4)c3)c2s1 10.1016/j.bmcl.2011.10.049
12017012 99348 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.
ChEMBL 622 12 3 7 6.0 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2coc(Cc3ccc(C(F)(F)F)cc3)n2)cc1 10.1016/s0960-894x(00)00277-8
CHEMBL285520 99348 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.
ChEMBL 622 12 3 7 6.0 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2coc(Cc3ccc(C(F)(F)F)cc3)n2)cc1 10.1016/s0960-894x(00)00277-8
44338127 7564 0 None - 0 Guinea pig 5.5 pIC50 = 5.5 Binding
Beta-2 adrenergic receptor blocking was assessed from 50% inhibition of the isoproterenol submaximal response on isolated Guinea pig trachea(IT)Beta-2 adrenergic receptor blocking was assessed from 50% inhibition of the isoproterenol submaximal response on isolated Guinea pig trachea(IT)
ChEMBL 390 8 3 6 2.6 CC(C)(C)NCC(O)CO/N=C1/c2ccccc2C2CCCCC12OCCO 10.1021/jm00122a008
CHEMBL108843 7564 0 None - 0 Guinea pig 5.5 pIC50 = 5.5 Binding
Beta-2 adrenergic receptor blocking was assessed from 50% inhibition of the isoproterenol submaximal response on isolated Guinea pig trachea(IT)Beta-2 adrenergic receptor blocking was assessed from 50% inhibition of the isoproterenol submaximal response on isolated Guinea pig trachea(IT)
ChEMBL 390 8 3 6 2.6 CC(C)(C)NCC(O)CO/N=C1/c2ccccc2C2CCCCC12OCCO 10.1021/jm00122a008
44338499 108136 0 None - 0 Guinea pig 5.5 pIC50 = 5.5 Binding
Beta-2 adrenergic receptor blocking was assessed from 50% inhibition of the isoproterenol submaximal response on isolated Guinea pig trachea(IT)Beta-2 adrenergic receptor blocking was assessed from 50% inhibition of the isoproterenol submaximal response on isolated Guinea pig trachea(IT)
ChEMBL 346 5 3 5 2.6 CC(C)(C)NCC(O)CO/N=C1/c2ccccc2C2CCCCC12O 10.1021/jm00122a008
CHEMBL320704 108136 0 None - 0 Guinea pig 5.5 pIC50 = 5.5 Binding
Beta-2 adrenergic receptor blocking was assessed from 50% inhibition of the isoproterenol submaximal response on isolated Guinea pig trachea(IT)Beta-2 adrenergic receptor blocking was assessed from 50% inhibition of the isoproterenol submaximal response on isolated Guinea pig trachea(IT)
ChEMBL 346 5 3 5 2.6 CC(C)(C)NCC(O)CO/N=C1/c2ccccc2C2CCCCC12O 10.1021/jm00122a008
14998847 55276 0 None - 0 Dog 4.5 pIC50 = 4.5 Binding
Binding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprololBinding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprolol
ChEMBL 388 6 3 5 1.3 CS(=O)(=O)Nc1ccc(C(=O)NCC2CNCCN2c2ccccc2)cc1 10.1021/jm00082a016
CHEMBL162095 55276 0 None - 0 Dog 4.5 pIC50 = 4.5 Binding
Binding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprololBinding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprolol
ChEMBL 388 6 3 5 1.3 CS(=O)(=O)Nc1ccc(C(=O)NCC2CNCCN2c2ccccc2)cc1 10.1021/jm00082a016
24900874 70025 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 417 11 5 7 1.9 COCCNCc1ccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)cc1 10.1016/j.bmcl.2011.10.049
CHEMBL1945293 70025 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 417 11 5 7 1.9 COCCNCc1ccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)cc1 10.1016/j.bmcl.2011.10.049
12017016 99690 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.
ChEMBL 574 14 3 7 5.9 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2cnc(CCCC3CCCC3)o2)cc1 10.1016/s0960-894x(00)00277-8
CHEMBL287947 99690 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.
ChEMBL 574 14 3 7 5.9 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2cnc(CCCC3CCCC3)o2)cc1 10.1016/s0960-894x(00)00277-8
71612644 132829 0 None -2 2 Human 4.5 pIC50 = 4.5 Binding
Inhibition Assay: Human recombinant adrenergic β2 receptors expressed in CHO cells are used in modified Tris-HCl buffer pH 7.4. A 50 aliquot is incubated with 0.2 nM [3H]CGP-12177 for 60 minutes at 25° C. Non-specific binding is estimated in the presence of 10 μM ICI-118551. Receptors are filtered and washed, the filters are then counted to determine [3H]CGP-12177 specifically bound. Compounds are screened at 10 μM.Inhibition Assay: Human recombinant adrenergic β2 receptors expressed in CHO cells are used in modified Tris-HCl buffer pH 7.4. A 50 aliquot is incubated with 0.2 nM [3H]CGP-12177 for 60 minutes at 25° C. Non-specific binding is estimated in the presence of 10 μM ICI-118551. Receptors are filtered and washed, the filters are then counted to determine [3H]CGP-12177 specifically bound. Compounds are screened at 10 μM.
ChEMBL 303 7 2 5 0.5 N#CC1CCCN1C(=O)CNCC(O)COc1ccccc1 nan
CHEMBL3704833 132829 0 None -2 2 Human 4.5 pIC50 = 4.5 Binding
Inhibition Assay: Human recombinant adrenergic β2 receptors expressed in CHO cells are used in modified Tris-HCl buffer pH 7.4. A 50 aliquot is incubated with 0.2 nM [3H]CGP-12177 for 60 minutes at 25° C. Non-specific binding is estimated in the presence of 10 μM ICI-118551. Receptors are filtered and washed, the filters are then counted to determine [3H]CGP-12177 specifically bound. Compounds are screened at 10 μM.Inhibition Assay: Human recombinant adrenergic β2 receptors expressed in CHO cells are used in modified Tris-HCl buffer pH 7.4. A 50 aliquot is incubated with 0.2 nM [3H]CGP-12177 for 60 minutes at 25° C. Non-specific binding is estimated in the presence of 10 μM ICI-118551. Receptors are filtered and washed, the filters are then counted to determine [3H]CGP-12177 specifically bound. Compounds are screened at 10 μM.
ChEMBL 303 7 2 5 0.5 N#CC1CCCN1C(=O)CNCC(O)COc1ccccc1 nan
44461718 204138 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity towards Beta-2 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindololBinding affinity towards Beta-2 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindolol
ChEMBL 591 17 3 8 5.1 CCCCCCCCn1ccn(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)c1=O 10.1016/s0960-894x(99)00073-6
CHEMBL83753 204138 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity towards Beta-2 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindololBinding affinity towards Beta-2 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindolol
ChEMBL 591 17 3 8 5.1 CCCCCCCCn1ccn(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)c1=O 10.1016/s0960-894x(99)00073-6
44461718 204138 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindololBinding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindolol
ChEMBL 591 17 3 8 5.1 CCCCCCCCn1ccn(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)c1=O 10.1016/s0960-894x(99)00072-4
CHEMBL83753 204138 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindololBinding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindolol
ChEMBL 591 17 3 8 5.1 CCCCCCCCn1ccn(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)c1=O 10.1016/s0960-894x(99)00072-4
10455 3218 34 None - 1 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]CGP1217 from human recombinant adrenergic beta2 receptor transfected in insect Sf9 cells by scintillation countingDisplacement of [3H]CGP1217 from human recombinant adrenergic beta2 receptor transfected in insect Sf9 cells by scintillation counting
ChEMBL 301 7 4 4 2.7 CC(NCC(c1ccc(cc1)O)O)CCc1ccc(cc1)O 10.1021/jm801211c
56052 3218 34 None - 1 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]CGP1217 from human recombinant adrenergic beta2 receptor transfected in insect Sf9 cells by scintillation countingDisplacement of [3H]CGP1217 from human recombinant adrenergic beta2 receptor transfected in insect Sf9 cells by scintillation counting
ChEMBL 301 7 4 4 2.7 CC(NCC(c1ccc(cc1)O)O)CCc1ccc(cc1)O 10.1021/jm801211c
CHEMBL509336 3218 34 None - 1 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]CGP1217 from human recombinant adrenergic beta2 receptor transfected in insect Sf9 cells by scintillation countingDisplacement of [3H]CGP1217 from human recombinant adrenergic beta2 receptor transfected in insect Sf9 cells by scintillation counting
ChEMBL 301 7 4 4 2.7 CC(NCC(c1ccc(cc1)O)O)CCc1ccc(cc1)O 10.1021/jm801211c
DB11541 3218 34 None - 1 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]CGP1217 from human recombinant adrenergic beta2 receptor transfected in insect Sf9 cells by scintillation countingDisplacement of [3H]CGP1217 from human recombinant adrenergic beta2 receptor transfected in insect Sf9 cells by scintillation counting
ChEMBL 301 7 4 4 2.7 CC(NCC(c1ccc(cc1)O)O)CCc1ccc(cc1)O 10.1021/jm801211c
12017010 162638 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.
ChEMBL 572 12 3 7 5.1 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2coc(Cc3ccc(F)cc3)n2)cc1 10.1016/s0960-894x(00)00277-8
CHEMBL418234 162638 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.
ChEMBL 572 12 3 7 5.1 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2coc(Cc3ccc(F)cc3)n2)cc1 10.1016/s0960-894x(00)00277-8
44458134 84395 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibitory activity against cloned human Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol in CHO cells by receptor binding assayInhibitory activity against cloned human Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol in CHO cells by receptor binding assay
ChEMBL 565 15 3 10 3.1 CCCCCCn1nnn(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)c1=O 10.1016/s0960-894x(99)00182-1
CHEMBL22345 84395 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibitory activity against cloned human Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol in CHO cells by receptor binding assayInhibitory activity against cloned human Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol in CHO cells by receptor binding assay
ChEMBL 565 15 3 10 3.1 CCCCCCn1nnn(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)c1=O 10.1016/s0960-894x(99)00182-1
10464801 11094 0 None - 2 Guinea pig 5.5 pIC50 = 5.5 Binding
Inhibitory concentration against beta-2-adrenergic receptor in isolated guinea pig tracheal stripsInhibitory concentration against beta-2-adrenergic receptor in isolated guinea pig tracheal strips
ChEMBL 174 6 2 4 0.4 CCO/N=C/C(O)CNC(C)C 10.1021/jm00036a018
CHEMBL1178754 11094 0 None - 2 Guinea pig 5.5 pIC50 = 5.5 Binding
Inhibitory concentration against beta-2-adrenergic receptor in isolated guinea pig tracheal stripsInhibitory concentration against beta-2-adrenergic receptor in isolated guinea pig tracheal strips
ChEMBL 174 6 2 4 0.4 CCO/N=C/C(O)CNC(C)C 10.1021/jm00036a018
CHEMBL39682 11094 0 None - 2 Guinea pig 5.5 pIC50 = 5.5 Binding
Inhibitory concentration against beta-2-adrenergic receptor in isolated guinea pig tracheal stripsInhibitory concentration against beta-2-adrenergic receptor in isolated guinea pig tracheal strips
ChEMBL 174 6 2 4 0.4 CCO/N=C/C(O)CNC(C)C 10.1021/jm00036a018
16735259 85207 0 None - 1 Human 6.5 pIC50 = 6.5 Binding
Mitogenesis inhibition method: To measure beta2-AR mediated inhibition of mitogenesis, HEK-beta2-AR, 1321N1 or U87MG cells were seeded in a 96-well plate at approximately 5,000 cells/well. After 48 hours, the wells were rinsed twice and the medium was replaced with fresh medium containing 10 uL of drug in sterile water. After another 24 hours of incubation at 37° C., 0.25 uCi of [3H]-thymidine was added to each well. The cells were incubated for an additional 2 hours at 37° C., at which point 10 uL of 10x trypsin was added, and the resuspended cells were harvested using a Tomtec 96 harvester through glass fiber filters.Mitogenesis inhibition method: To measure beta2-AR mediated inhibition of mitogenesis, HEK-beta2-AR, 1321N1 or U87MG cells were seeded in a 96-well plate at approximately 5,000 cells/well. After 48 hours, the wells were rinsed twice and the medium was replaced with fresh medium containing 10 uL of drug in sterile water. After another 24 hours of incubation at 37° C., 0.25 uCi of [3H]-thymidine was added to each well. The cells were incubated for an additional 2 hours at 37° C., at which point 10 uL of 10x trypsin was added, and the resuspended cells were harvested using a Tomtec 96 harvester through glass fiber filters.
ChEMBL 317 7 4 5 2.4 COc1ccc(C[C@H](C)NC[C@@H](O)c2cc(O)cc(O)c2)cc1 nan
CHEMBL228417 85207 0 None - 1 Human 6.5 pIC50 = 6.5 Binding
Mitogenesis inhibition method: To measure beta2-AR mediated inhibition of mitogenesis, HEK-beta2-AR, 1321N1 or U87MG cells were seeded in a 96-well plate at approximately 5,000 cells/well. After 48 hours, the wells were rinsed twice and the medium was replaced with fresh medium containing 10 uL of drug in sterile water. After another 24 hours of incubation at 37° C., 0.25 uCi of [3H]-thymidine was added to each well. The cells were incubated for an additional 2 hours at 37° C., at which point 10 uL of 10x trypsin was added, and the resuspended cells were harvested using a Tomtec 96 harvester through glass fiber filters.Mitogenesis inhibition method: To measure beta2-AR mediated inhibition of mitogenesis, HEK-beta2-AR, 1321N1 or U87MG cells were seeded in a 96-well plate at approximately 5,000 cells/well. After 48 hours, the wells were rinsed twice and the medium was replaced with fresh medium containing 10 uL of drug in sterile water. After another 24 hours of incubation at 37° C., 0.25 uCi of [3H]-thymidine was added to each well. The cells were incubated for an additional 2 hours at 37° C., at which point 10 uL of 10x trypsin was added, and the resuspended cells were harvested using a Tomtec 96 harvester through glass fiber filters.
ChEMBL 317 7 4 5 2.4 COc1ccc(C[C@H](C)NC[C@@H](O)c2cc(O)cc(O)c2)cc1 nan
118638354 145042 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 ug/well for beta1 and 5 ug/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 ul, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 uM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 ug/well for beta1 and 5 ug/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 ul, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 uM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.
ChEMBL 774 17 5 11 5.3 CN(CCN(C)[C@H]1CC[C@H](OC(C(=O)O)(c2cccs2)c2cccs2)CC1)C(=O)COc1ccc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1 nan
CHEMBL3915401 145042 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 ug/well for beta1 and 5 ug/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 ul, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 uM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 ug/well for beta1 and 5 ug/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 ul, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 uM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.
ChEMBL 774 17 5 11 5.3 CN(CCN(C)[C@H]1CC[C@H](OC(C(=O)O)(c2cccs2)c2cccs2)CC1)C(=O)COc1ccc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1 nan
44298787 193071 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 443 12 2 5 6.6 CCCCCCCCc1csc(Nc2ccc(S(=O)(=O)Nc3ccccc3)cc2)n1 10.1016/s0960-894x(99)00277-2
CHEMBL53679 193071 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 443 12 2 5 6.6 CCCCCCCCc1csc(Nc2ccc(S(=O)(=O)Nc3ccccc3)cc2)n1 10.1016/s0960-894x(99)00277-2
44349357 159350 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cells
ChEMBL 469 11 4 7 4.7 O=[N+]([O-])/C=C(\Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)Nc1ccc2ccccc2c1 10.1016/s0960-894x(00)00669-7
CHEMBL410702 159350 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cells
ChEMBL 469 11 4 7 4.7 O=[N+]([O-])/C=C(\Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)Nc1ccc2ccccc2c1 10.1016/s0960-894x(00)00669-7
131847 55771 7 None - 0 Dog 5.5 pIC50 = 5.5 Binding
Binding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprololBinding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprolol
ChEMBL 388 6 3 5 1.3 CS(=O)(=O)Nc1ccc(C(=O)NCC2CN(c3ccccc3)CCN2)cc1 10.1021/jm00082a016
CHEMBL162513 55771 7 None - 0 Dog 5.5 pIC50 = 5.5 Binding
Binding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprololBinding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprolol
ChEMBL 388 6 3 5 1.3 CS(=O)(=O)Nc1ccc(C(=O)NCC2CN(c3ccccc3)CCN2)cc1 10.1021/jm00082a016
1346 83 108 None - 9 Dog 4.5 pIC50 = 4.5 Binding
Binding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprololBinding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprolol
ChEMBL 192 2 1 3 1.1 COc1ccccc1N1CCNCC1 10.1021/jm00082a016
280 83 108 None - 9 Dog 4.5 pIC50 = 4.5 Binding
Binding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprololBinding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprolol
ChEMBL 192 2 1 3 1.1 COc1ccccc1N1CCNCC1 10.1021/jm00082a016
9899402 83 108 None - 9 Dog 4.5 pIC50 = 4.5 Binding
Binding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprololBinding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprolol
ChEMBL 192 2 1 3 1.1 COc1ccccc1N1CCNCC1 10.1021/jm00082a016
CHEMBL9666 83 108 None - 9 Dog 4.5 pIC50 = 4.5 Binding
Binding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprololBinding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprolol
ChEMBL 192 2 1 3 1.1 COc1ccccc1N1CCNCC1 10.1021/jm00082a016
1836 2544 56 None -53 15 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 nan
3340 2544 56 None -53 15 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 nan
5281040 2544 56 None -53 15 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 nan
CHEMBL787 2544 56 None -53 15 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 nan
DB00471 2544 56 None -53 15 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 nan
44338529 108135 0 None - 0 Guinea pig 7.5 pIC50 = 7.5 Binding
Beta-2 adrenergic receptor blocking was assessed from 50% inhibition of the isoproterenol submaximal response on isolated Guinea pig trachea(IT)Beta-2 adrenergic receptor blocking was assessed from 50% inhibition of the isoproterenol submaximal response on isolated Guinea pig trachea(IT)
ChEMBL 360 7 2 5 3.2 COC12CCCCCC1c1ccccc1/C2=N/OCC(O)CNC(C)C 10.1021/jm00122a008
CHEMBL320696 108135 0 None - 0 Guinea pig 7.5 pIC50 = 7.5 Binding
Beta-2 adrenergic receptor blocking was assessed from 50% inhibition of the isoproterenol submaximal response on isolated Guinea pig trachea(IT)Beta-2 adrenergic receptor blocking was assessed from 50% inhibition of the isoproterenol submaximal response on isolated Guinea pig trachea(IT)
ChEMBL 360 7 2 5 3.2 COC12CCCCCC1c1ccccc1/C2=N/OCC(O)CNC(C)C 10.1021/jm00122a008
44338131 108165 0 None - 0 Guinea pig 7.5 pIC50 = 7.5 Binding
Beta-2 adrenergic receptor blocking was assessed from 50% inhibition of the isoproterenol submaximal response on isolated Guinea pig trachea(IT)Beta-2 adrenergic receptor blocking was assessed from 50% inhibition of the isoproterenol submaximal response on isolated Guinea pig trachea(IT)
ChEMBL 360 6 2 5 3.2 COC12CCCCC1c1ccccc1/C2=N/OCC(O)CNC(C)(C)C 10.1021/jm00122a008
CHEMBL320761 108165 0 None - 0 Guinea pig 7.5 pIC50 = 7.5 Binding
Beta-2 adrenergic receptor blocking was assessed from 50% inhibition of the isoproterenol submaximal response on isolated Guinea pig trachea(IT)Beta-2 adrenergic receptor blocking was assessed from 50% inhibition of the isoproterenol submaximal response on isolated Guinea pig trachea(IT)
ChEMBL 360 6 2 5 3.2 COC12CCCCC1c1ccccc1/C2=N/OCC(O)CNC(C)(C)C 10.1021/jm00122a008
44268568 24716 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.
ChEMBL 570 16 6 7 4.1 CCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/s0960-894x(98)00170-x
CHEMBL13459 24716 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.
ChEMBL 570 16 6 7 4.1 CCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/s0960-894x(98)00170-x
44281097 114222 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindolol
ChEMBL 607 13 3 9 4.7 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(COc3ccc(F)c(F)c3)no2)cc1 10.1016/s0960-894x(00)00268-7
CHEMBL33384 114222 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindolol
ChEMBL 607 13 3 9 4.7 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(COc3ccc(F)c(F)c3)no2)cc1 10.1016/s0960-894x(00)00268-7
14998849 56206 0 None - 0 Dog 5.5 pIC50 = 5.5 Binding
Binding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprololBinding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprolol
ChEMBL 418 7 3 6 1.3 COc1cccc(N2CCNC(CNC(=O)c3ccc(NS(C)(=O)=O)cc3)C2)c1 10.1021/jm00082a016
CHEMBL163587 56206 0 None - 0 Dog 5.5 pIC50 = 5.5 Binding
Binding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprololBinding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprolol
ChEMBL 418 7 3 6 1.3 COc1cccc(N2CCNC(CNC(=O)c3ccc(NS(C)(=O)=O)cc3)C2)c1 10.1021/jm00082a016
44377636 119580 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindololBinding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindolol
ChEMBL 607 12 3 6 4.5 O=C1N(Cc2ccc(F)c(F)c2)CCN1c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(99)00072-4
CHEMBL350931 119580 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindololBinding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindolol
ChEMBL 607 12 3 6 4.5 O=C1N(Cc2ccc(F)c(F)c2)CCN1c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(99)00072-4
12017017 126946 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.
ChEMBL 606 13 3 8 5.3 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2coc(COc3ccc(F)c(F)c3)n2)cc1 10.1016/s0960-894x(00)00277-8
CHEMBL36609 126946 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.
ChEMBL 606 13 3 8 5.3 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2coc(COc3ccc(F)c(F)c3)n2)cc1 10.1016/s0960-894x(00)00277-8
12017001 146500 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.
ChEMBL 540 11 3 7 5.1 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2cnc(-c3ccccc3)o2)cc1 10.1016/s0960-894x(00)00277-8
CHEMBL39269 146500 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.
ChEMBL 540 11 3 7 5.1 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2cnc(-c3ccccc3)o2)cc1 10.1016/s0960-894x(00)00277-8
54592027 143449 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 μg/well for beta1 and 5 μg/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 μl, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 μM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 μg/well for beta1 and 5 μg/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 μl, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 μM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.
ChEMBL 717 15 5 11 5.3 CN(CCOc1ccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1)C1CCC(OC(=O)C(O)(c2cccs2)c2cccs2)CC1 nan
CHEMBL3902803 143449 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 μg/well for beta1 and 5 μg/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 μl, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 μM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 μg/well for beta1 and 5 μg/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 μl, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 μM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.
ChEMBL 717 15 5 11 5.3 CN(CCOc1ccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1)C1CCC(OC(=O)C(O)(c2cccs2)c2cccs2)CC1 nan
44306956 201647 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cell
ChEMBL 495 11 3 6 3.8 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2cccnc2)cc1)c1ccc(Cl)c(Cl)c1 10.1016/s0960-894x(98)00381-3
CHEMBL65042 201647 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cell
ChEMBL 495 11 3 6 3.8 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2cccnc2)cc1)c1ccc(Cl)c(Cl)c1 10.1016/s0960-894x(98)00381-3
46881839 6519 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counter
ChEMBL 517 11 3 6 5.1 O=C(Cn1nc(-c2ccccc2)cc1-c1ccccc1)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/j.bmcl.2010.01.130
CHEMBL1083216 6519 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counter
ChEMBL 517 11 3 6 5.1 O=C(Cn1nc(-c2ccccc2)cc1-c1ccccc1)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/j.bmcl.2010.01.130
44298728 193105 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
In vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 401 8 2 3 4.1 CCCCCCNC(=O)N1CCc2cc(S(=O)(=O)Nc3ccccc3)ccc21 10.1016/s0960-894x(99)00277-2
CHEMBL53842 193105 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
In vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 401 8 2 3 4.1 CCCCCCNC(=O)N1CCc2cc(S(=O)(=O)Nc3ccccc3)ccc21 10.1016/s0960-894x(99)00277-2
44268274 18647 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandBinding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligand
ChEMBL 476 11 4 6 3.4 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1)c1cccc(Cl)c1 10.1016/s0960-894x(98)00169-3
CHEMBL12813 18647 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandBinding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligand
ChEMBL 476 11 4 6 3.4 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1)c1cccc(Cl)c1 10.1016/s0960-894x(98)00169-3
44349356 116470 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cells
ChEMBL 469 11 4 7 4.7 O=[N+]([O-])/C=C(\Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)Nc1cccc2ccccc12 10.1016/s0960-894x(00)00669-7
CHEMBL338748 116470 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cells
ChEMBL 469 11 4 7 4.7 O=[N+]([O-])/C=C(\Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)Nc1cccc2ccccc12 10.1016/s0960-894x(00)00669-7
44461705 204130 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity towards Beta-2 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindololBinding affinity towards Beta-2 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindolol
ChEMBL 607 17 3 7 4.9 CCCCCCCCN1C(=O)CN(c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)C1=O 10.1016/s0960-894x(99)00073-6
CHEMBL83698 204130 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity towards Beta-2 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindololBinding affinity towards Beta-2 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindolol
ChEMBL 607 17 3 7 4.9 CCCCCCCCN1C(=O)CN(c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)C1=O 10.1016/s0960-894x(99)00073-6
12017005 99792 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.
ChEMBL 560 13 3 7 5.5 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2coc(CCC3CCCC3)n2)cc1 10.1016/s0960-894x(00)00277-8
CHEMBL288917 99792 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.
ChEMBL 560 13 3 7 5.5 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2coc(CCC3CCCC3)n2)cc1 10.1016/s0960-894x(00)00277-8
155524193 170317 0 None 22 2 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at human recombinant beta2 adrenoreceptor expressed in CHOK1 cells incubated for 30 mins by HTRFAntagonist activity at human recombinant beta2 adrenoreceptor expressed in CHOK1 cells incubated for 30 mins by HTRF
ChEMBL 685 25 7 11 0.1 CC(C)NCC(O)COc1ccccc1CCCSCC(=O)NCCOCCOCCNC(=O)C1C(C(=O)O)C(C(=O)O)C1C(=O)O 10.1039/C8MD00412A
CHEMBL4454523 170317 0 None 22 2 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at human recombinant beta2 adrenoreceptor expressed in CHOK1 cells incubated for 30 mins by HTRFAntagonist activity at human recombinant beta2 adrenoreceptor expressed in CHOK1 cells incubated for 30 mins by HTRF
ChEMBL 685 25 7 11 0.1 CC(C)NCC(O)COc1ccccc1CCCSCC(=O)NCCOCCOCCNC(=O)C1C(C(=O)O)C(C(=O)O)C1C(=O)O 10.1039/C8MD00412A
12049919 201401 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity for clone human Beta-2 adrenergic receptor from CHO cell membranes in the presence of I-iodocyanopindololBinding affinity for clone human Beta-2 adrenergic receptor from CHO cell membranes in the presence of I-iodocyanopindolol
ChEMBL 572 12 3 8 4.1 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-n2ncc(Cc3cccc(F)c3)n2)cc1 10.1016/s0960-894x(00)00422-4
CHEMBL63963 201401 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity for clone human Beta-2 adrenergic receptor from CHO cell membranes in the presence of I-iodocyanopindololBinding affinity for clone human Beta-2 adrenergic receptor from CHO cell membranes in the presence of I-iodocyanopindolol
ChEMBL 572 12 3 8 4.1 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-n2ncc(Cc3cccc(F)c3)n2)cc1 10.1016/s0960-894x(00)00422-4
15523859 204207 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity towards Beta-2 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindololBinding affinity towards Beta-2 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindolol
ChEMBL 593 17 3 6 5.4 CCCCCCCCN1CCN(c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)C1=O 10.1016/s0960-894x(99)00073-6
CHEMBL84190 204207 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity towards Beta-2 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindololBinding affinity towards Beta-2 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindolol
ChEMBL 593 17 3 6 5.4 CCCCCCCCN1CCN(c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)C1=O 10.1016/s0960-894x(99)00073-6
15523859 204207 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindololBinding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindolol
ChEMBL 593 17 3 6 5.4 CCCCCCCCN1CCN(c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)C1=O 10.1016/s0960-894x(99)00072-4
CHEMBL84190 204207 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindololBinding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindolol
ChEMBL 593 17 3 6 5.4 CCCCCCCCN1CCN(c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)C1=O 10.1016/s0960-894x(99)00072-4
44306959 201385 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cell
ChEMBL 520 11 4 7 2.8 Nc1ccc(OC[C@@H](O)CNCCc2ccc(NS(=O)(=O)c3ccc(Br)cc3)cc2)cn1 10.1016/s0960-894x(98)00381-3
CHEMBL63842 201385 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cell
ChEMBL 520 11 4 7 2.8 Nc1ccc(OC[C@@H](O)CNCCc2ccc(NS(=O)(=O)c3ccc(Br)cc3)cc2)cn1 10.1016/s0960-894x(98)00381-3
44307196 201884 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cell
ChEMBL 510 11 4 7 3.3 Nc1ccc(OC[C@@H](O)CNCCc2ccc(NS(=O)(=O)c3ccc(Cl)c(Cl)c3)cc2)cn1 10.1016/s0960-894x(98)00381-3
CHEMBL66859 201884 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cell
ChEMBL 510 11 4 7 3.3 Nc1ccc(OC[C@@H](O)CNCCc2ccc(NS(=O)(=O)c3ccc(Cl)c(Cl)c3)cc2)cn1 10.1016/s0960-894x(98)00381-3
14998858 119528 0 None - 0 Dog 5.4 pIC50 = 5.4 Binding
Binding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprololBinding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprolol
ChEMBL 422 6 3 5 1.9 CS(=O)(=O)Nc1ccc(C(=O)NCC2CN(c3cccc(Cl)c3)CCN2)cc1 10.1021/jm00082a016
CHEMBL350432 119528 0 None - 0 Dog 5.4 pIC50 = 5.4 Binding
Binding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprololBinding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprolol
ChEMBL 422 6 3 5 1.9 CS(=O)(=O)Nc1ccc(C(=O)NCC2CN(c3cccc(Cl)c3)CCN2)cc1 10.1021/jm00082a016
9932018 69858 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]dihydroalprenolol from beta2-adrenoceptor after 90 mins by liquid scintillation countingDisplacement of [3H]dihydroalprenolol from beta2-adrenoceptor after 90 mins by liquid scintillation counting
ChEMBL 422 11 6 6 2.9 OCc1cc(C(O)CNCCc2ccc(NCC(O)c3ccccc3)cc2)ccc1O 10.1016/j.bmcl.2011.11.072
CHEMBL1940815 69858 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]dihydroalprenolol from beta2-adrenoceptor after 90 mins by liquid scintillation countingDisplacement of [3H]dihydroalprenolol from beta2-adrenoceptor after 90 mins by liquid scintillation counting
ChEMBL 422 11 6 6 2.9 OCc1cc(C(O)CNCCc2ccc(NCC(O)c3ccccc3)cc2)ccc1O 10.1016/j.bmcl.2011.11.072
71558718 144177 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 ug/well for beta1 and 5 ug/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 ul, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 uM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 ug/well for beta1 and 5 ug/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 ul, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 uM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.
ChEMBL 774 14 5 13 5.7 CN(CCCn1c(=O)sc2cc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)ccc21)[C@H]1CC[C@H](OC(=O)C(O)(c2cccs2)c2cccs2)CC1 nan
CHEMBL3908788 144177 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 ug/well for beta1 and 5 ug/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 ul, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 uM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 ug/well for beta1 and 5 ug/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 ul, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 uM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.
ChEMBL 774 14 5 13 5.7 CN(CCCn1c(=O)sc2cc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)ccc21)[C@H]1CC[C@H](OC(=O)C(O)(c2cccs2)c2cccs2)CC1 nan
6918446 2823 52 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibition of beta2 adrenergic receptorInhibition of beta2 adrenergic receptor
ChEMBL 408 8 2 4 4.7 N#Cc1c(cccc1Cl)OC[C@@H](CNC(Cc1ccc2c(c1)cccc2)(C)C)O 10.1021/jm900563e
716 2823 52 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibition of beta2 adrenergic receptorInhibition of beta2 adrenergic receptor
ChEMBL 408 8 2 4 4.7 N#Cc1c(cccc1Cl)OC[C@@H](CNC(Cc1ccc2c(c1)cccc2)(C)C)O 10.1021/jm900563e
CHEMBL180672 2823 52 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibition of beta2 adrenergic receptorInhibition of beta2 adrenergic receptor
ChEMBL 408 8 2 4 4.7 N#Cc1c(cccc1Cl)OC[C@@H](CNC(Cc1ccc2c(c1)cccc2)(C)C)O 10.1021/jm900563e
DB05695 2823 52 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibition of beta2 adrenergic receptorInhibition of beta2 adrenergic receptor
ChEMBL 408 8 2 4 4.7 N#Cc1c(cccc1Cl)OC[C@@H](CNC(Cc1ccc2c(c1)cccc2)(C)C)O 10.1021/jm900563e
56677231 63293 0 None 234 2 Human 8.4 pIC50 = 8.4 Binding
Mitogenesis inhibition method: To measure beta2-AR mediated inhibition of mitogenesis, HEK-beta2-AR, 1321N1 or U87MG cells were seeded in a 96-well plate at approximately 5,000 cells/well. After 48 hours, the wells were rinsed twice and the medium was replaced with fresh medium containing 10 uL of drug in sterile water. After another 24 hours of incubation at 37° C., 0.25 uCi of [3H]-thymidine was added to each well. The cells were incubated for an additional 2 hours at 37° C., at which point 10 uL of 10x trypsin was added, and the resuspended cells were harvested using a Tomtec 96 harvester through glass fiber filters.Mitogenesis inhibition method: To measure beta2-AR mediated inhibition of mitogenesis, HEK-beta2-AR, 1321N1 or U87MG cells were seeded in a 96-well plate at approximately 5,000 cells/well. After 48 hours, the wells were rinsed twice and the medium was replaced with fresh medium containing 10 uL of drug in sterile water. After another 24 hours of incubation at 37° C., 0.25 uCi of [3H]-thymidine was added to each well. The cells were incubated for an additional 2 hours at 37° C., at which point 10 uL of 10x trypsin was added, and the resuspended cells were harvested using a Tomtec 96 harvester through glass fiber filters.
ChEMBL 367 7 4 5 3.5 COc1ccc(C[C@H](C)NC[C@H](O)c2cc(O)cc(O)c2)c2ccccc12 nan
CHEMBL1800934 63293 0 None 234 2 Human 8.4 pIC50 = 8.4 Binding
Mitogenesis inhibition method: To measure beta2-AR mediated inhibition of mitogenesis, HEK-beta2-AR, 1321N1 or U87MG cells were seeded in a 96-well plate at approximately 5,000 cells/well. After 48 hours, the wells were rinsed twice and the medium was replaced with fresh medium containing 10 uL of drug in sterile water. After another 24 hours of incubation at 37° C., 0.25 uCi of [3H]-thymidine was added to each well. The cells were incubated for an additional 2 hours at 37° C., at which point 10 uL of 10x trypsin was added, and the resuspended cells were harvested using a Tomtec 96 harvester through glass fiber filters.Mitogenesis inhibition method: To measure beta2-AR mediated inhibition of mitogenesis, HEK-beta2-AR, 1321N1 or U87MG cells were seeded in a 96-well plate at approximately 5,000 cells/well. After 48 hours, the wells were rinsed twice and the medium was replaced with fresh medium containing 10 uL of drug in sterile water. After another 24 hours of incubation at 37° C., 0.25 uCi of [3H]-thymidine was added to each well. The cells were incubated for an additional 2 hours at 37° C., at which point 10 uL of 10x trypsin was added, and the resuspended cells were harvested using a Tomtec 96 harvester through glass fiber filters.
ChEMBL 367 7 4 5 3.5 COc1ccc(C[C@H](C)NC[C@H](O)c2cc(O)cc(O)c2)c2ccccc12 nan
54673189 148618 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 μg/well for beta1 and 5 μg/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 μl, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 μM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 μg/well for beta1 and 5 μg/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 μl, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 μM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.
ChEMBL 801 15 6 14 5.3 COc1cc(NC(=O)OCCN(C)[C@H]2CC[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)CC2)c(C#N)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3943564 148618 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 μg/well for beta1 and 5 μg/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 μl, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 μM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 μg/well for beta1 and 5 μg/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 μl, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 μM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.
ChEMBL 801 15 6 14 5.3 COc1cc(NC(=O)OCCN(C)[C@H]2CC[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)CC2)c(C#N)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
54672859 147502 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 μg/well for beta1 and 5 μg/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 μl, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 μM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 μg/well for beta1 and 5 μg/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 μl, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 μM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.
ChEMBL 778 15 6 12 5.4 COc1cc(NC(=O)CCN(C)[C@H]2CC[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)CC2)c(F)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3934681 147502 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 μg/well for beta1 and 5 μg/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 μl, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 μM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 μg/well for beta1 and 5 μg/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 μl, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 μM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.
ChEMBL 778 15 6 12 5.4 COc1cc(NC(=O)CCN(C)[C@H]2CC[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)CC2)c(F)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
10206782 16661 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cells
ChEMBL 492 10 4 6 4.9 N#CN/C(=N\c1cccc(Oc2ccccc2)c1)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/s0960-894x(00)00669-7
CHEMBL124863 16661 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cells
ChEMBL 492 10 4 6 4.9 N#CN/C(=N\c1cccc(Oc2ccccc2)c1)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/s0960-894x(00)00669-7
10160636 112986 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cells
ChEMBL 443 9 5 6 2.2 N#CN/C(=N\c1ccc(CCNC[C@H](O)c2cccnc2)cc1)Nc1cccc(C(N)=O)c1 10.1016/s0960-894x(00)00669-7
CHEMBL332010 112986 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cells
ChEMBL 443 9 5 6 2.2 N#CN/C(=N\c1ccc(CCNC[C@H](O)c2cccnc2)cc1)Nc1cccc(C(N)=O)c1 10.1016/s0960-894x(00)00669-7
46882030 5676 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counter
ChEMBL 427 9 4 5 3.6 O=C(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1cccc(-c2ncc[nH]2)c1 10.1016/j.bmcl.2010.01.130
CHEMBL1078576 5676 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counter
ChEMBL 427 9 4 5 3.6 O=C(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1cccc(-c2ncc[nH]2)c1 10.1016/j.bmcl.2010.01.130
46882031 5703 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counter
ChEMBL 465 11 3 4 5.0 O=C(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1cccc(CCc2ccccc2)c1 10.1016/j.bmcl.2010.01.130
CHEMBL1078749 5703 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counter
ChEMBL 465 11 3 4 5.0 O=C(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1cccc(CCc2ccccc2)c1 10.1016/j.bmcl.2010.01.130
46881900 7691 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counter
ChEMBL 437 9 3 4 4.9 O=C(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1cccc(-c2ccccc2)c1 10.1016/j.bmcl.2010.01.130
CHEMBL1089396 7691 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counter
ChEMBL 437 9 3 4 4.9 O=C(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1cccc(-c2ccccc2)c1 10.1016/j.bmcl.2010.01.130
44268534 19153 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.
ChEMBL 529 13 5 8 3.3 CCOC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/s0960-894x(98)00170-x
CHEMBL12911 19153 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.
ChEMBL 529 13 5 8 3.3 CCOC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/s0960-894x(98)00170-x
44268632 24008 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.
ChEMBL 514 12 6 7 2.5 CNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/s0960-894x(98)00170-x
CHEMBL13398 24008 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.
ChEMBL 514 12 6 7 2.5 CNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/s0960-894x(98)00170-x
44301804 167607 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Binding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindololBinding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindolol
ChEMBL 557 11 3 8 4.9 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3ccccn3)cs2)cc1 10.1016/s0960-894x(00)00390-5
CHEMBL433248 167607 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Binding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindololBinding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindolol
ChEMBL 557 11 3 8 4.9 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3ccccn3)cs2)cc1 10.1016/s0960-894x(00)00390-5
15483879 99309 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Binding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindolol
ChEMBL 573 12 3 8 4.5 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(Cc3ccc(F)cc3)no2)cc1 10.1016/s0960-894x(00)00268-7
CHEMBL285240 99309 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Binding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindolol
ChEMBL 573 12 3 8 4.5 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(Cc3ccc(F)cc3)no2)cc1 10.1016/s0960-894x(00)00268-7
44285529 150373 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.
ChEMBL 534 14 3 7 5.1 CCCCCc1ncc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)o1 10.1016/s0960-894x(00)00277-8
CHEMBL39577 150373 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.
ChEMBL 534 14 3 7 5.1 CCCCCc1ncc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)o1 10.1016/s0960-894x(00)00277-8
83111 57061 78 None - 0 Dog 4.4 pIC50 = 4.4 Binding
Binding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprololBinding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprolol
ChEMBL 176 1 1 2 1.4 Cc1cccc(N2CCNCC2)c1 10.1021/jm00082a016
CHEMBL165175 57061 78 None - 0 Dog 4.4 pIC50 = 4.4 Binding
Binding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprololBinding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprolol
ChEMBL 176 1 1 2 1.4 Cc1cccc(N2CCNCC2)c1 10.1021/jm00082a016
10375227 11098 0 None - 2 Guinea pig 5.4 pIC50 = 5.4 Binding
Inhibitory concentration against beta-2-adrenergic receptor in isolated guinea pig tracheal stripsInhibitory concentration against beta-2-adrenergic receptor in isolated guinea pig tracheal strips
ChEMBL 188 5 2 4 0.8 C/C=N/OCC(O)CNC(C)(C)C 10.1021/jm00036a018
CHEMBL1178761 11098 0 None - 2 Guinea pig 5.4 pIC50 = 5.4 Binding
Inhibitory concentration against beta-2-adrenergic receptor in isolated guinea pig tracheal stripsInhibitory concentration against beta-2-adrenergic receptor in isolated guinea pig tracheal strips
ChEMBL 188 5 2 4 0.8 C/C=N/OCC(O)CNC(C)(C)C 10.1021/jm00036a018
CHEMBL39873 11098 0 None - 2 Guinea pig 5.4 pIC50 = 5.4 Binding
Inhibitory concentration against beta-2-adrenergic receptor in isolated guinea pig tracheal stripsInhibitory concentration against beta-2-adrenergic receptor in isolated guinea pig tracheal strips
ChEMBL 188 5 2 4 0.8 C/C=N/OCC(O)CNC(C)(C)C 10.1021/jm00036a018
12582 935 40 None -11 5 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 276 3 3 3 3.0 CC(C)(C)NCC(C1=CC(=C(C(=C1)Cl)N)Cl)O nan
2783 935 40 None -11 5 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 276 3 3 3 3.0 CC(C)(C)NCC(C1=CC(=C(C(=C1)Cl)N)Cl)O nan
CHEMBL49080 935 40 None -11 5 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 276 3 3 3 3.0 CC(C)(C)NCC(C1=CC(=C(C(=C1)Cl)N)Cl)O nan
DB01407 935 40 None -11 5 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 276 3 3 3 3.0 CC(C)(C)NCC(C1=CC(=C(C(=C1)Cl)N)Cl)O nan
1588 2284 24 None -50 44 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
28864 2284 24 None -50 44 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
43 2284 24 None -50 44 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
CHEMBL157138 2284 24 None -50 44 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
DB00589 2284 24 None -50 44 Human 7.4 pIC50 = 7.4 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
44335548 109264 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Beta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindolol
ChEMBL 567 17 5 6 5.2 CCCCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(98)00571-x
CHEMBL323113 109264 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Beta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindolol
ChEMBL 567 17 5 6 5.2 CCCCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(98)00571-x
44307007 100298 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cell
ChEMBL 469 12 3 6 3.6 CC(C)c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3cccnc3)cc2)cc1 10.1016/s0960-894x(98)00381-3
CHEMBL292947 100298 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cell
ChEMBL 469 12 3 6 3.6 CC(C)c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3cccnc3)cc2)cc1 10.1016/s0960-894x(98)00381-3
44298314 100678 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
In vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 452 8 1 6 5.1 O=S(=O)(Nc1ccccc1)c1ccc2c(c1)CCN2c1noc(CCCC2CCCC2)n1 10.1016/s0960-894x(99)00277-2
CHEMBL295502 100678 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
In vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 452 8 1 6 5.1 O=S(=O)(Nc1ccccc1)c1ccc2c(c1)CCN2c1noc(CCCC2CCCC2)n1 10.1016/s0960-894x(99)00277-2
14998853 119608 0 None - 0 Dog 4.4 pIC50 = 4.4 Binding
Binding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprololBinding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprolol
ChEMBL 360 6 3 5 1.9 CS(=O)(=O)Nc1ccc(NCC2CNCCN2c2ccccc2)cc1 10.1021/jm00082a016
CHEMBL351183 119608 0 None - 0 Dog 4.4 pIC50 = 4.4 Binding
Binding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprololBinding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprolol
ChEMBL 360 6 3 5 1.9 CS(=O)(=O)Nc1ccc(NCC2CNCCN2c2ccccc2)cc1 10.1021/jm00082a016
44307064 201635 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cell
ChEMBL 461 11 3 6 3.1 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2cccnc2)cc1)c1ccc(Cl)cc1 10.1016/s0960-894x(98)00381-3
CHEMBL64936 201635 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cell
ChEMBL 461 11 3 6 3.1 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2cccnc2)cc1)c1ccc(Cl)cc1 10.1016/s0960-894x(98)00381-3
44307144 201906 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cell
ChEMBL 569 17 5 7 4.2 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3cccnc3)cc2)cc1 10.1016/s0960-894x(98)00381-3
CHEMBL67015 201906 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cell
ChEMBL 569 17 5 7 4.2 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3cccnc3)cc2)cc1 10.1016/s0960-894x(98)00381-3
44268556 23916 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.
ChEMBL 515 12 5 8 2.9 COC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/s0960-894x(98)00170-x
CHEMBL13389 23916 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.
ChEMBL 515 12 5 8 2.9 COC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/s0960-894x(98)00170-x
6918446 2823 52 None - 0 Human 5.4 pIC50 = 5.4 Binding
Binding affinity to beta2 adrenoceptorBinding affinity to beta2 adrenoceptor
ChEMBL 408 8 2 4 4.7 N#Cc1c(cccc1Cl)OC[C@@H](CNC(Cc1ccc2c(c1)cccc2)(C)C)O 10.1021/jm900364m
716 2823 52 None - 0 Human 5.4 pIC50 = 5.4 Binding
Binding affinity to beta2 adrenoceptorBinding affinity to beta2 adrenoceptor
ChEMBL 408 8 2 4 4.7 N#Cc1c(cccc1Cl)OC[C@@H](CNC(Cc1ccc2c(c1)cccc2)(C)C)O 10.1021/jm900364m
CHEMBL180672 2823 52 None - 0 Human 5.4 pIC50 = 5.4 Binding
Binding affinity to beta2 adrenoceptorBinding affinity to beta2 adrenoceptor
ChEMBL 408 8 2 4 4.7 N#Cc1c(cccc1Cl)OC[C@@H](CNC(Cc1ccc2c(c1)cccc2)(C)C)O 10.1021/jm900364m
DB05695 2823 52 None - 0 Human 5.4 pIC50 = 5.4 Binding
Binding affinity to beta2 adrenoceptorBinding affinity to beta2 adrenoceptor
ChEMBL 408 8 2 4 4.7 N#Cc1c(cccc1Cl)OC[C@@H](CNC(Cc1ccc2c(c1)cccc2)(C)C)O 10.1021/jm900364m
14998855 55397 0 None - 0 Dog 5.4 pIC50 = 5.4 Binding
Binding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprololBinding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprolol
ChEMBL 402 6 2 5 1.3 CN(c1ccc(C(=O)NCC2CN(c3ccccc3)CCN2)cc1)S(C)(=O)=O 10.1021/jm00082a016
CHEMBL162200 55397 0 None - 0 Dog 5.4 pIC50 = 5.4 Binding
Binding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprololBinding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprolol
ChEMBL 402 6 2 5 1.3 CN(c1ccc(C(=O)NCC2CN(c3ccccc3)CCN2)cc1)S(C)(=O)=O 10.1021/jm00082a016
14998848 119569 0 None - 0 Dog 5.4 pIC50 = 5.4 Binding
Binding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprololBinding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprolol
ChEMBL 361 5 2 5 2.1 O=C(NCC1CN(c2ccccc2)CCN1)c1ccc(-n2ccnc2)cc1 10.1021/jm00082a016
CHEMBL350847 119569 0 None - 0 Dog 5.4 pIC50 = 5.4 Binding
Binding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprololBinding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprolol
ChEMBL 361 5 2 5 2.1 O=C(NCC1CN(c2ccccc2)CCN1)c1ccc(-n2ccnc2)cc1 10.1021/jm00082a016
2464 3570 52 None -7 6 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C nan
5253 3570 52 None -7 6 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C nan
7297 3570 52 None -7 6 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C nan
CHEMBL471 3570 52 None -7 6 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C nan
DB00489 3570 52 None -7 6 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C nan
9990035 11901 0 None - 2 Guinea pig 5.4 pIC50 = 5.4 Binding
Inhibitory concentration against beta-2-adrenergic receptor in isolated guinea pig tracheal stripsInhibitory concentration against beta-2-adrenergic receptor in isolated guinea pig tracheal strips
ChEMBL 188 7 2 4 0.8 CCCO/N=C/C(O)CNC(C)C 10.1021/jm00036a018
CHEMBL1183337 11901 0 None - 2 Guinea pig 5.4 pIC50 = 5.4 Binding
Inhibitory concentration against beta-2-adrenergic receptor in isolated guinea pig tracheal stripsInhibitory concentration against beta-2-adrenergic receptor in isolated guinea pig tracheal strips
ChEMBL 188 7 2 4 0.8 CCCO/N=C/C(O)CNC(C)C 10.1021/jm00036a018
CHEMBL291115 11901 0 None - 2 Guinea pig 5.4 pIC50 = 5.4 Binding
Inhibitory concentration against beta-2-adrenergic receptor in isolated guinea pig tracheal stripsInhibitory concentration against beta-2-adrenergic receptor in isolated guinea pig tracheal strips
ChEMBL 188 7 2 4 0.8 CCCO/N=C/C(O)CNC(C)C 10.1021/jm00036a018
44338543 5849 0 None - 0 Guinea pig 6.4 pIC50 = 6.4 Binding
Beta-2 adrenergic receptor blocking was assessed from 50% inhibition of the isoproterenol submaximal response on isolated Guinea pig trachea(IT)Beta-2 adrenergic receptor blocking was assessed from 50% inhibition of the isoproterenol submaximal response on isolated Guinea pig trachea(IT)
ChEMBL 374 6 2 5 3.6 COC12CCCCCC1c1ccccc1/C2=N/OCC(O)CNC(C)(C)C 10.1021/jm00122a008
CHEMBL107981 5849 0 None - 0 Guinea pig 6.4 pIC50 = 6.4 Binding
Beta-2 adrenergic receptor blocking was assessed from 50% inhibition of the isoproterenol submaximal response on isolated Guinea pig trachea(IT)Beta-2 adrenergic receptor blocking was assessed from 50% inhibition of the isoproterenol submaximal response on isolated Guinea pig trachea(IT)
ChEMBL 374 6 2 5 3.6 COC12CCCCCC1c1ccccc1/C2=N/OCC(O)CNC(C)(C)C 10.1021/jm00122a008
44338613 110876 0 None - 0 Guinea pig 6.4 pIC50 = 6.4 Binding
Beta-2 adrenergic receptor blocking was assessed from 50% inhibition of the isoproterenol submaximal response on isolated Guinea pig trachea(IT)Beta-2 adrenergic receptor blocking was assessed from 50% inhibition of the isoproterenol submaximal response on isolated Guinea pig trachea(IT)
ChEMBL 360 5 3 5 2.9 CC(C)(C)NCC(O)CO/N=C1/c2ccccc2C2CCCCCC12O 10.1021/jm00122a008
CHEMBL327091 110876 0 None - 0 Guinea pig 6.4 pIC50 = 6.4 Binding
Beta-2 adrenergic receptor blocking was assessed from 50% inhibition of the isoproterenol submaximal response on isolated Guinea pig trachea(IT)Beta-2 adrenergic receptor blocking was assessed from 50% inhibition of the isoproterenol submaximal response on isolated Guinea pig trachea(IT)
ChEMBL 360 5 3 5 2.9 CC(C)(C)NCC(O)CO/N=C1/c2ccccc2C2CCCCCC12O 10.1021/jm00122a008
44298769 195421 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
In vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 457 12 1 5 6.6 CCCCCCCCc1csc(N(C)c2ccc(S(=O)(=O)Nc3ccccc3)cc2)n1 10.1016/s0960-894x(99)00277-2
CHEMBL56767 195421 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
In vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 457 12 1 5 6.6 CCCCCCCCc1csc(N(C)c2ccc(S(=O)(=O)Nc3ccccc3)cc2)n1 10.1016/s0960-894x(99)00277-2
14739889 206024 0 None - 0 Dog 5.4 pIC50 = 5.4 Binding
Tested for Beta-2 adrenergic receptor selectivity in canine lung tissue in anesthetized dogsTested for Beta-2 adrenergic receptor selectivity in canine lung tissue in anesthetized dogs
ChEMBL 364 9 3 5 1.9 Cc1cccc(OCC(O)CNCc2ccc(NS(C)(=O)=O)cc2)c1 10.1021/jm00172a033
CHEMBL95966 206024 0 None - 0 Dog 5.4 pIC50 = 5.4 Binding
Tested for Beta-2 adrenergic receptor selectivity in canine lung tissue in anesthetized dogsTested for Beta-2 adrenergic receptor selectivity in canine lung tissue in anesthetized dogs
ChEMBL 364 9 3 5 1.9 Cc1cccc(OCC(O)CNCc2ccc(NS(C)(=O)=O)cc2)c1 10.1021/jm00172a033
12043158 162666 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
Binding affinity towards Beta-2 adrenergic receptor prepared from CHO cells expressing the cloned human receptor in the presence of [125I]iodocyanopindololBinding affinity towards Beta-2 adrenergic receptor prepared from CHO cells expressing the cloned human receptor in the presence of [125I]iodocyanopindolol
ChEMBL 551 14 4 9 3.5 CC(O)CCCc1nc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)no1 10.1016/s0960-894x(00)00267-5
CHEMBL418411 162666 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
Binding affinity towards Beta-2 adrenergic receptor prepared from CHO cells expressing the cloned human receptor in the presence of [125I]iodocyanopindololBinding affinity towards Beta-2 adrenergic receptor prepared from CHO cells expressing the cloned human receptor in the presence of [125I]iodocyanopindolol
ChEMBL 551 14 4 9 3.5 CC(O)CCCc1nc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)no1 10.1016/s0960-894x(00)00267-5
44338578 110073 0 None - 0 Guinea pig 6.4 pIC50 = 6.4 Binding
Beta-2 adrenergic receptor blocking was assessed from 50% inhibition of the isoproterenol submaximal response on isolated Guinea pig trachea(IT)Beta-2 adrenergic receptor blocking was assessed from 50% inhibition of the isoproterenol submaximal response on isolated Guinea pig trachea(IT)
ChEMBL 378 6 2 5 3.4 COC12CCCCC1c1ccc(F)cc1/C2=N/OCC(O)CNC(C)(C)C 10.1021/jm00122a008
CHEMBL325371 110073 0 None - 0 Guinea pig 6.4 pIC50 = 6.4 Binding
Beta-2 adrenergic receptor blocking was assessed from 50% inhibition of the isoproterenol submaximal response on isolated Guinea pig trachea(IT)Beta-2 adrenergic receptor blocking was assessed from 50% inhibition of the isoproterenol submaximal response on isolated Guinea pig trachea(IT)
ChEMBL 378 6 2 5 3.4 COC12CCCCC1c1ccc(F)cc1/C2=N/OCC(O)CNC(C)(C)C 10.1021/jm00122a008
44268539 20212 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.
ChEMBL 527 13 5 7 3.4 CC(C)C(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/s0960-894x(98)00170-x
CHEMBL13068 20212 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.
ChEMBL 527 13 5 7 3.4 CC(C)C(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/s0960-894x(98)00170-x
44298850 167609 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
In vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 461 8 1 4 6.1 O=S(=O)(Nc1ccccc1)c1ccc2c(c1)CCN2c1cccc(CCCC2CCCC2)n1 10.1016/s0960-894x(99)00277-2
CHEMBL433252 167609 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
In vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 461 8 1 4 6.1 O=S(=O)(Nc1ccccc1)c1ccc2c(c1)CCN2c1cccc(CCCC2CCCC2)n1 10.1016/s0960-894x(99)00277-2
44280904 99486 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Binding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindolol
ChEMBL 632 13 3 9 5.5 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2noc(Cc3ccc(-c4ccccn4)cc3)n2)cc1 10.1016/s0960-894x(00)00268-7
CHEMBL286438 99486 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Binding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindolol
ChEMBL 632 13 3 9 5.5 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2noc(Cc3ccc(-c4ccccn4)cc3)n2)cc1 10.1016/s0960-894x(00)00268-7
14998851 119542 0 None - 0 Dog 5.4 pIC50 = 5.4 Binding
Binding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprololBinding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprolol
ChEMBL 361 6 2 5 1.9 CS(=O)(=O)Nc1ccc(OCC2CN(c3ccccc3)CCN2)cc1 10.1021/jm00082a016
CHEMBL350581 119542 0 None - 0 Dog 5.4 pIC50 = 5.4 Binding
Binding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprololBinding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprolol
ChEMBL 361 6 2 5 1.9 CS(=O)(=O)Nc1ccc(OCC2CN(c3ccccc3)CCN2)cc1 10.1021/jm00082a016
44461486 203642 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Binding affinity towards Beta-2 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindololBinding affinity towards Beta-2 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindolol
ChEMBL 564 15 3 9 3.7 CCCCCCn1cnn(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)c1=O 10.1016/s0960-894x(99)00073-6
CHEMBL79806 203642 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Binding affinity towards Beta-2 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindololBinding affinity towards Beta-2 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindolol
ChEMBL 564 15 3 9 3.7 CCCCCCn1cnn(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)c1=O 10.1016/s0960-894x(99)00073-6
44298849 194768 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
In vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 434 9 1 3 6.3 CCCCCCc1cccc(N2CCc3cc(S(=O)(=O)Nc4ccccc4)ccc32)c1 10.1016/s0960-894x(99)00277-2
CHEMBL56308 194768 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
In vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 434 9 1 3 6.3 CCCCCCc1cccc(N2CCc3cc(S(=O)(=O)Nc4ccccc4)ccc32)c1 10.1016/s0960-894x(99)00277-2
14998846 56076 0 None - 0 Dog 5.3 pIC50 = 5.3 Binding
Binding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprololBinding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprolol
ChEMBL 374 7 3 5 1.6 CS(=O)(=O)Nc1ccc(CNCC2CN(c3ccccc3)CCN2)cc1 10.1021/jm00082a016
CHEMBL163153 56076 0 None - 0 Dog 5.3 pIC50 = 5.3 Binding
Binding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprololBinding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprolol
ChEMBL 374 7 3 5 1.6 CS(=O)(=O)Nc1ccc(CNCC2CN(c3ccccc3)CCN2)cc1 10.1021/jm00082a016
14739891 205986 0 None - 0 Dog 4.3 pIC50 = 4.3 Binding
Tested for Beta-2 adrenergic receptor selectivity in canine lung tissue in anesthetized dogsTested for Beta-2 adrenergic receptor selectivity in canine lung tissue in anesthetized dogs
ChEMBL 408 12 3 6 1.8 COCCc1ccc(OCC(O)CNCc2ccc(NS(C)(=O)=O)cc2)cc1 10.1021/jm00172a033
CHEMBL95727 205986 0 None - 0 Dog 4.3 pIC50 = 4.3 Binding
Tested for Beta-2 adrenergic receptor selectivity in canine lung tissue in anesthetized dogsTested for Beta-2 adrenergic receptor selectivity in canine lung tissue in anesthetized dogs
ChEMBL 408 12 3 6 1.8 COCCc1ccc(OCC(O)CNCc2ccc(NS(C)(=O)=O)cc2)cc1 10.1021/jm00172a033
10416448 201693 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity for clone human Beta-2 adrenergic receptor from CHO cell membranes in the presence of I-iodocyanopindololBinding affinity for clone human Beta-2 adrenergic receptor from CHO cell membranes in the presence of I-iodocyanopindolol
ChEMBL 622 12 3 8 4.9 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-n2ncc(Cc3ccc(C(F)(F)F)cc3)n2)cc1 10.1016/s0960-894x(00)00422-4
CHEMBL65461 201693 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity for clone human Beta-2 adrenergic receptor from CHO cell membranes in the presence of I-iodocyanopindololBinding affinity for clone human Beta-2 adrenergic receptor from CHO cell membranes in the presence of I-iodocyanopindolol
ChEMBL 622 12 3 8 4.9 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-n2ncc(Cc3ccc(C(F)(F)F)cc3)n2)cc1 10.1016/s0960-894x(00)00422-4
46882028 5666 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counter
ChEMBL 467 11 3 5 4.8 O=C(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccccc1COc1ccccc1 10.1016/j.bmcl.2010.01.130
CHEMBL1078495 5666 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counter
ChEMBL 467 11 3 5 4.8 O=C(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccccc1COc1ccccc1 10.1016/j.bmcl.2010.01.130
12017004 99680 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.
ChEMBL 590 12 3 7 5.3 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2cnc(Cc3ccc(F)c(F)c3)o2)cc1 10.1016/s0960-894x(00)00277-8
CHEMBL287880 99680 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.
ChEMBL 590 12 3 7 5.3 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2cnc(Cc3ccc(F)c(F)c3)o2)cc1 10.1016/s0960-894x(00)00277-8
44301979 100382 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Binding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindololBinding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindolol
ChEMBL 607 11 3 8 6.1 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3cnc4ccccc4c3)cs2)cc1 10.1016/s0960-894x(00)00390-5
CHEMBL293577 100382 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Binding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindololBinding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindolol
ChEMBL 607 11 3 8 6.1 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3cnc4ccccc4c3)cs2)cc1 10.1016/s0960-894x(00)00390-5
130400 206634 9 None - 0 Dog 4.3 pIC50 = 4.3 Binding
In vitro Beta-2 adrenergic receptor affinity in partially purified membrane fractions from canine lung tissue using [SH]dihydroalprenolol (4.5 nM)In vitro Beta-2 adrenergic receptor affinity in partially purified membrane fractions from canine lung tissue using [SH]dihydroalprenolol (4.5 nM)
ChEMBL 446 12 3 8 1.7 CS(=O)(=O)Nc1ccc(OCC(O)CNCCOc2ccc(-n3ccnc3)cc2)cc1 10.1021/jm00166a002
CHEMBL552615 206634 9 None - 0 Dog 4.3 pIC50 = 4.3 Binding
In vitro Beta-2 adrenergic receptor affinity in partially purified membrane fractions from canine lung tissue using [SH]dihydroalprenolol (4.5 nM)In vitro Beta-2 adrenergic receptor affinity in partially purified membrane fractions from canine lung tissue using [SH]dihydroalprenolol (4.5 nM)
ChEMBL 446 12 3 8 1.7 CS(=O)(=O)Nc1ccc(OCC(O)CNCCOc2ccc(-n3ccnc3)cc2)cc1 10.1021/jm00166a002
CHEMBL99585 206634 9 None - 0 Dog 4.3 pIC50 = 4.3 Binding
In vitro Beta-2 adrenergic receptor affinity in partially purified membrane fractions from canine lung tissue using [SH]dihydroalprenolol (4.5 nM)In vitro Beta-2 adrenergic receptor affinity in partially purified membrane fractions from canine lung tissue using [SH]dihydroalprenolol (4.5 nM)
ChEMBL 446 12 3 8 1.7 CS(=O)(=O)Nc1ccc(OCC(O)CNCCOc2ccc(-n3ccnc3)cc2)cc1 10.1021/jm00166a002
44281396 99484 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindolol
ChEMBL 589 13 3 9 4.5 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2noc(COc3ccc(F)cc3)n2)cc1 10.1016/s0960-894x(00)00268-7
CHEMBL286435 99484 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindolol
ChEMBL 589 13 3 9 4.5 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2noc(COc3ccc(F)cc3)n2)cc1 10.1016/s0960-894x(00)00268-7
44307378 202094 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cell
ChEMBL 478 11 3 7 3.0 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2cccnc2)cc1)c1cnc2ccccc2c1 10.1016/s0960-894x(98)00381-3
CHEMBL68334 202094 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cell
ChEMBL 478 11 3 7 3.0 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2cccnc2)cc1)c1cnc2ccccc2c1 10.1016/s0960-894x(98)00381-3
44301880 196952 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Binding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindololBinding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindolol
ChEMBL 596 11 3 8 6.3 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3cc4ccccc4o3)cs2)cc1 10.1016/s0960-894x(00)00390-5
CHEMBL57908 196952 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Binding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindololBinding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindolol
ChEMBL 596 11 3 8 6.3 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3cc4ccccc4o3)cs2)cc1 10.1016/s0960-894x(00)00390-5
14739897 206585 0 None - 0 Dog 4.3 pIC50 = 4.3 Binding
Tested for Beta-2 adrenergic receptor selectivity in canine lung tissue in anesthetized dogsTested for Beta-2 adrenergic receptor selectivity in canine lung tissue in anesthetized dogs
ChEMBL 419 8 2 6 1.9 Cc1cccc(OCC(O)CN2CCN(c3ccc(NS(C)(=O)=O)cc3)CC2)c1 10.1021/jm00172a033
CHEMBL99331 206585 0 None - 0 Dog 4.3 pIC50 = 4.3 Binding
Tested for Beta-2 adrenergic receptor selectivity in canine lung tissue in anesthetized dogsTested for Beta-2 adrenergic receptor selectivity in canine lung tissue in anesthetized dogs
ChEMBL 419 8 2 6 1.9 Cc1cccc(OCC(O)CN2CCN(c3ccc(NS(C)(=O)=O)cc3)CC2)c1 10.1021/jm00172a033
2419 3394 80 None 16 6 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]dihydroalprenolol from beta2-adrenoceptor after 90 mins by liquid scintillation countingDisplacement of [3H]dihydroalprenolol from beta2-adrenoceptor after 90 mins by liquid scintillation counting
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.11.072
5152 3394 80 None 16 6 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]dihydroalprenolol from beta2-adrenoceptor after 90 mins by liquid scintillation countingDisplacement of [3H]dihydroalprenolol from beta2-adrenoceptor after 90 mins by liquid scintillation counting
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.11.072
559 3394 80 None 16 6 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]dihydroalprenolol from beta2-adrenoceptor after 90 mins by liquid scintillation countingDisplacement of [3H]dihydroalprenolol from beta2-adrenoceptor after 90 mins by liquid scintillation counting
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.11.072
CHEMBL1263 3394 80 None 16 6 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]dihydroalprenolol from beta2-adrenoceptor after 90 mins by liquid scintillation countingDisplacement of [3H]dihydroalprenolol from beta2-adrenoceptor after 90 mins by liquid scintillation counting
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.11.072
DB00938 3394 80 None 16 6 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]dihydroalprenolol from beta2-adrenoceptor after 90 mins by liquid scintillation countingDisplacement of [3H]dihydroalprenolol from beta2-adrenoceptor after 90 mins by liquid scintillation counting
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.11.072
24900750 70021 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 479 11 5 7 3.5 COc1ccc(CNCc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)sc34)c2)cc1 10.1016/j.bmcl.2011.10.049
CHEMBL1945289 70021 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 479 11 5 7 3.5 COc1ccc(CNCc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)sc34)c2)cc1 10.1016/j.bmcl.2011.10.049
54673354 148182 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 μg/well for beta1 and 5 μg/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 μl, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 μM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 μg/well for beta1 and 5 μg/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 μl, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 μM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.
ChEMBL 808 16 6 12 5.9 COc1cc(NC(=O)CCN(C)[C@H]2CC[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)CC2)c(Cl)cc1CCNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3940214 148182 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 μg/well for beta1 and 5 μg/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 μl, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 μM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 μg/well for beta1 and 5 μg/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 μl, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 μM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.
ChEMBL 808 16 6 12 5.9 COc1cc(NC(=O)CCN(C)[C@H]2CC[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)CC2)c(Cl)cc1CCNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
71566009 143763 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 ug/well for beta1 and 5 ug/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 ul, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 uM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 ug/well for beta1 and 5 ug/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 ul, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 uM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.
ChEMBL 838 17 5 13 5.4 COc1cc(OCC(=O)N(C)CCN(C)[C@H]2CC[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3905320 143763 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 ug/well for beta1 and 5 ug/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 ul, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 uM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 ug/well for beta1 and 5 ug/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 ul, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 uM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.
ChEMBL 838 17 5 13 5.4 COc1cc(OCC(=O)N(C)CCN(C)[C@H]2CC[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
118710937 113235 0 None - 3 Guinea pig 8.2 pIC50 = 8.2 Binding
Agonist activity at adrenergic beta2 receptor in electrically-stimulated Dunkin-Hartley guinea pig tracheal strip assessed as inhibition of contractionAgonist activity at adrenergic beta2 receptor in electrically-stimulated Dunkin-Hartley guinea pig tracheal strip assessed as inhibition of contraction
ChEMBL 376 5 4 5 3.7 O=c1[nH]c2c(O)ccc([C@@H](O)CN[C@@H]3CCC[C@@H]3C3CCCCC3)c2s1 10.1016/j.bmcl.2014.06.014
CHEMBL3323655 113235 0 None - 3 Guinea pig 8.2 pIC50 = 8.2 Binding
Agonist activity at adrenergic beta2 receptor in electrically-stimulated Dunkin-Hartley guinea pig tracheal strip assessed as inhibition of contractionAgonist activity at adrenergic beta2 receptor in electrically-stimulated Dunkin-Hartley guinea pig tracheal strip assessed as inhibition of contraction
ChEMBL 376 5 4 5 3.7 O=c1[nH]c2c(O)ccc([C@@H](O)CN[C@@H]3CCC[C@@H]3C3CCCCC3)c2s1 10.1016/j.bmcl.2014.06.014
10282871 16357 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cells
ChEMBL 636 16 4 8 7.2 CCCCCCCCc1csc(N2CCc3cc(N/C(=N/c4ccc(CCNC[C@H](O)c5cccnc5)cc4)NC#N)ccc32)n1 10.1016/s0960-894x(00)00669-7
CHEMBL123745 16357 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cells
ChEMBL 636 16 4 8 7.2 CCCCCCCCc1csc(N2CCc3cc(N/C(=N/c4ccc(CCNC[C@H](O)c5cccnc5)cc4)NC#N)ccc32)n1 10.1016/s0960-894x(00)00669-7
44349629 18323 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cells
ChEMBL 450 8 4 5 4.3 N#CN/C(=N\c1ccc2ccccc2c1)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/s0960-894x(00)00669-7
CHEMBL127422 18323 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cells
ChEMBL 450 8 4 5 4.3 N#CN/C(=N\c1ccc2ccccc2c1)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/s0960-894x(00)00669-7
44307113 168806 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cell
ChEMBL 552 11 3 5 3.7 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1)c1ccc(I)cc1 10.1016/s0960-894x(98)00381-3
CHEMBL442172 168806 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cell
ChEMBL 552 11 3 5 3.7 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1)c1ccc(I)cc1 10.1016/s0960-894x(98)00381-3
155545397 172802 0 None 5 2 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity at human recombinant beta2 adrenoreceptor expressed in CHOK1 cells incubated for 30 mins by HTRFAntagonist activity at human recombinant beta2 adrenoreceptor expressed in CHOK1 cells incubated for 30 mins by HTRF
ChEMBL 1266 41 6 18 5.4 C=CCc1ccccc1OCC(O)CNCCOCCOCCOCCOCCNC(=O)CCCCCC1(C)C(/C=C/C=C/C=C2/N(CCCS(=O)(=O)O)c3ccc(S(=O)(=O)O)cc3C2(C)C)=[N+](CCCS(=O)(=O)[O-])c2ccc(S(=O)(=O)O)cc21 10.1039/C8MD00412A
CHEMBL4527905 172802 0 None 5 2 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity at human recombinant beta2 adrenoreceptor expressed in CHOK1 cells incubated for 30 mins by HTRFAntagonist activity at human recombinant beta2 adrenoreceptor expressed in CHOK1 cells incubated for 30 mins by HTRF
ChEMBL 1266 41 6 18 5.4 C=CCc1ccccc1OCC(O)CNCCOCCOCCOCCOCCNC(=O)CCCCCC1(C)C(/C=C/C=C/C=C2/N(CCCS(=O)(=O)O)c3ccc(S(=O)(=O)O)cc3C2(C)C)=[N+](CCCS(=O)(=O)[O-])c2ccc(S(=O)(=O)O)cc21 10.1039/C8MD00412A
44268254 19798 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandBinding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligand
ChEMBL 302 8 4 5 1.5 Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/s0960-894x(98)00169-3
CHEMBL13034 19798 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandBinding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligand
ChEMBL 302 8 4 5 1.5 Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/s0960-894x(98)00169-3
44268295 98079 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandBinding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligand
ChEMBL 408 12 4 6 2.1 CCCS(=O)(=O)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/s0960-894x(98)00169-3
CHEMBL276480 98079 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandBinding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligand
ChEMBL 408 12 4 6 2.1 CCCS(=O)(=O)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/s0960-894x(98)00169-3
44335572 5088 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Beta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindolol
ChEMBL 475 9 3 5 3.5 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(Br)cc1 10.1016/s0960-894x(98)00571-x
CHEMBL105968 5088 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Beta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindolol
ChEMBL 475 9 3 5 3.5 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(Br)cc1 10.1016/s0960-894x(98)00571-x
12049921 201874 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity for clone human Beta-2 adrenergic receptor from CHO cell membranes in the presence of I-iodocyanopindololBinding affinity for clone human Beta-2 adrenergic receptor from CHO cell membranes in the presence of I-iodocyanopindolol
ChEMBL 590 12 3 8 4.2 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-n2ncc(Cc3c(F)cccc3F)n2)cc1 10.1016/s0960-894x(00)00422-4
CHEMBL66789 201874 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity for clone human Beta-2 adrenergic receptor from CHO cell membranes in the presence of I-iodocyanopindololBinding affinity for clone human Beta-2 adrenergic receptor from CHO cell membranes in the presence of I-iodocyanopindolol
ChEMBL 590 12 3 8 4.2 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-n2ncc(Cc3c(F)cccc3F)n2)cc1 10.1016/s0960-894x(00)00422-4
44281371 99645 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindolol
ChEMBL 655 14 3 10 5.3 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2noc(COc3ccc(OC(F)(F)F)cc3)n2)cc1 10.1016/s0960-894x(00)00268-7
CHEMBL287567 99645 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindolol
ChEMBL 655 14 3 10 5.3 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2noc(COc3ccc(OC(F)(F)F)cc3)n2)cc1 10.1016/s0960-894x(00)00268-7
44281425 99830 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindolol
ChEMBL 612 13 4 9 4.3 CC(=O)Nc1ccc(Cc2nc(-c3ccc(S(=O)(=O)Nc4ccc(CCNC[C@H](O)c5cccnc5)cc4)cc3)no2)cc1 10.1016/s0960-894x(00)00268-7
CHEMBL289250 99830 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindolol
ChEMBL 612 13 4 9 4.3 CC(=O)Nc1ccc(Cc2nc(-c3ccc(S(=O)(=O)Nc4ccc(CCNC[C@H](O)c5cccnc5)cc4)cc3)no2)cc1 10.1016/s0960-894x(00)00268-7
44281384 118794 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindolol
ChEMBL 601 14 3 10 4.4 COc1ccc(OCc2nc(-c3ccc(S(=O)(=O)Nc4ccc(CCNC[C@H](O)c5cccnc5)cc4)cc3)no2)cc1 10.1016/s0960-894x(00)00268-7
CHEMBL34406 118794 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindolol
ChEMBL 601 14 3 10 4.4 COc1ccc(OCc2nc(-c3ccc(S(=O)(=O)Nc4ccc(CCNC[C@H](O)c5cccnc5)cc4)cc3)no2)cc1 10.1016/s0960-894x(00)00268-7
2464 3570 52 None - 6 Dog 5.3 pIC50 = 5.3 Binding
Binding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprololBinding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprolol
ChEMBL 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C 10.1021/jm00082a016
5253 3570 52 None - 6 Dog 5.3 pIC50 = 5.3 Binding
Binding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprololBinding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprolol
ChEMBL 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C 10.1021/jm00082a016
7297 3570 52 None - 6 Dog 5.3 pIC50 = 5.3 Binding
Binding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprololBinding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprolol
ChEMBL 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C 10.1021/jm00082a016
CHEMBL471 3570 52 None - 6 Dog 5.3 pIC50 = 5.3 Binding
Binding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprololBinding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprolol
ChEMBL 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C 10.1021/jm00082a016
DB00489 3570 52 None - 6 Dog 5.3 pIC50 = 5.3 Binding
Binding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprololBinding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprolol
ChEMBL 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C 10.1021/jm00082a016
44308088 201894 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity towards Beta-2 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindololBinding affinity towards Beta-2 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindolol
ChEMBL 607 17 3 7 4.9 CCCCCCCCN1CC(=O)N(c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)C1=O 10.1016/s0960-894x(99)00073-6
CHEMBL66936 201894 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity towards Beta-2 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindololBinding affinity towards Beta-2 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindolol
ChEMBL 607 17 3 7 4.9 CCCCCCCCN1CC(=O)N(c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)C1=O 10.1016/s0960-894x(99)00073-6
44377517 56921 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindololBinding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindolol
ChEMBL 551 14 3 6 4.2 CCCCCN1CCN(c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)C1=O 10.1016/s0960-894x(99)00072-4
CHEMBL165015 56921 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindololBinding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindolol
ChEMBL 551 14 3 6 4.2 CCCCCN1CCN(c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)C1=O 10.1016/s0960-894x(99)00072-4
15523860 119653 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindololBinding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindolol
ChEMBL 593 15 3 6 5.2 CCCCC(C)(C)CN1CCN(c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)C1=O 10.1016/s0960-894x(99)00072-4
CHEMBL351596 119653 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindololBinding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindolol
ChEMBL 593 15 3 6 5.2 CCCCC(C)(C)CN1CCN(c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)C1=O 10.1016/s0960-894x(99)00072-4
44377650 119687 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindololBinding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindolol
ChEMBL 577 13 3 6 4.6 O=C1N(CCC2CCCC2)CCN1c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(99)00072-4
CHEMBL351967 119687 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindololBinding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindolol
ChEMBL 577 13 3 6 4.6 O=C1N(CCC2CCCC2)CCN1c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(99)00072-4
10841426 116359 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity was evaluated on chinese hamster ovary (CHO) cells expressing the cloned human beta-2 adrenergic receptor in the presence of [125I]- iodocyanopindolol.Binding affinity was evaluated on chinese hamster ovary (CHO) cells expressing the cloned human beta-2 adrenergic receptor in the presence of [125I]- iodocyanopindolol.
ChEMBL 610 11 3 7 6.0 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3cc(F)c(F)c(F)c3)cs2)cc1 10.1021/jm000286i
CHEMBL338216 116359 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity was evaluated on chinese hamster ovary (CHO) cells expressing the cloned human beta-2 adrenergic receptor in the presence of [125I]- iodocyanopindolol.Binding affinity was evaluated on chinese hamster ovary (CHO) cells expressing the cloned human beta-2 adrenergic receptor in the presence of [125I]- iodocyanopindolol.
ChEMBL 610 11 3 7 6.0 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3cc(F)c(F)c(F)c3)cs2)cc1 10.1021/jm000286i
2464 3570 52 None - 6 Dog 5.3 pIC50 = 5.3 Binding
In vitro Beta-2 adrenergic receptor affinity in partially purified membrane fractions from canine lung tissue using [SH]dihydroalprenolol (4.5 nM)In vitro Beta-2 adrenergic receptor affinity in partially purified membrane fractions from canine lung tissue using [SH]dihydroalprenolol (4.5 nM)
ChEMBL 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C 10.1021/jm00166a002
5253 3570 52 None - 6 Dog 5.3 pIC50 = 5.3 Binding
In vitro Beta-2 adrenergic receptor affinity in partially purified membrane fractions from canine lung tissue using [SH]dihydroalprenolol (4.5 nM)In vitro Beta-2 adrenergic receptor affinity in partially purified membrane fractions from canine lung tissue using [SH]dihydroalprenolol (4.5 nM)
ChEMBL 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C 10.1021/jm00166a002
7297 3570 52 None - 6 Dog 5.3 pIC50 = 5.3 Binding
In vitro Beta-2 adrenergic receptor affinity in partially purified membrane fractions from canine lung tissue using [SH]dihydroalprenolol (4.5 nM)In vitro Beta-2 adrenergic receptor affinity in partially purified membrane fractions from canine lung tissue using [SH]dihydroalprenolol (4.5 nM)
ChEMBL 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C 10.1021/jm00166a002
CHEMBL471 3570 52 None - 6 Dog 5.3 pIC50 = 5.3 Binding
In vitro Beta-2 adrenergic receptor affinity in partially purified membrane fractions from canine lung tissue using [SH]dihydroalprenolol (4.5 nM)In vitro Beta-2 adrenergic receptor affinity in partially purified membrane fractions from canine lung tissue using [SH]dihydroalprenolol (4.5 nM)
ChEMBL 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C 10.1021/jm00166a002
DB00489 3570 52 None - 6 Dog 5.3 pIC50 = 5.3 Binding
In vitro Beta-2 adrenergic receptor affinity in partially purified membrane fractions from canine lung tissue using [SH]dihydroalprenolol (4.5 nM)In vitro Beta-2 adrenergic receptor affinity in partially purified membrane fractions from canine lung tissue using [SH]dihydroalprenolol (4.5 nM)
ChEMBL 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C 10.1021/jm00166a002
44268571 24412 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.
ChEMBL 582 13 6 7 4.2 O=C(Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1)NC1CCCCC1 10.1016/s0960-894x(98)00170-x
CHEMBL13432 24412 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.
ChEMBL 582 13 6 7 4.2 O=C(Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1)NC1CCCCC1 10.1016/s0960-894x(98)00170-x
44335844 4787 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Beta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindolol
ChEMBL 363 9 3 5 2.1 CC(C)S(=O)(=O)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/s0960-894x(98)00571-x
CHEMBL104377 4787 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Beta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindolol
ChEMBL 363 9 3 5 2.1 CC(C)S(=O)(=O)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/s0960-894x(98)00571-x
44302005 100082 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Binding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindololBinding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindolol
ChEMBL 595 11 4 7 6.0 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3c[nH]c4ccccc34)cs2)cc1 10.1016/s0960-894x(00)00390-5
CHEMBL291516 100082 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Binding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindololBinding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindolol
ChEMBL 595 11 4 7 6.0 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3c[nH]c4ccccc34)cs2)cc1 10.1016/s0960-894x(00)00390-5
44377665 167759 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Binding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindololBinding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindolol
ChEMBL 567 15 3 7 3.4 COCCCCN1CCN(c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)C1=O 10.1016/s0960-894x(99)00072-4
CHEMBL434284 167759 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Binding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindololBinding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindolol
ChEMBL 567 15 3 7 3.4 COCCCCN1CCN(c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)C1=O 10.1016/s0960-894x(99)00072-4
57397010 70137 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 515 11 4 5 5.3 O=c1[nH]c2c(O)ccc(CCNCCc3ccc(CNCCc4c(Cl)cccc4Cl)cc3)c2s1 10.1016/j.bmcl.2011.10.049
CHEMBL1946761 70137 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 515 11 4 5 5.3 O=c1[nH]c2c(O)ccc(CCNCCc3ccc(CNCCc4c(Cl)cccc4Cl)cc3)c2s1 10.1016/j.bmcl.2011.10.049
9803612 69846 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]dihydroalprenolol from beta2-adrenoceptor after 90 mins by liquid scintillation countingDisplacement of [3H]dihydroalprenolol from beta2-adrenoceptor after 90 mins by liquid scintillation counting
ChEMBL 446 10 8 8 1.3 OCc1cc(C(O)CN[C@H]2CC[C@H](NCC(O)c3ccc(O)c(CO)c3)CC2)ccc1O 10.1016/j.bmcl.2011.11.072
CHEMBL1940686 69846 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]dihydroalprenolol from beta2-adrenoceptor after 90 mins by liquid scintillation countingDisplacement of [3H]dihydroalprenolol from beta2-adrenoceptor after 90 mins by liquid scintillation counting
ChEMBL 446 10 8 8 1.3 OCc1cc(C(O)CN[C@H]2CC[C@H](NCC(O)c3ccc(O)c(CO)c3)CC2)ccc1O 10.1016/j.bmcl.2011.11.072
10346448 119312 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Receptor binding assay(Beta-2 adrenergic receptor) carried out with membranes prepared from human recombinant Sf9 cells expressing the cloned human receptor in the presence of [125I]iodocyanopindololReceptor binding assay(Beta-2 adrenergic receptor) carried out with membranes prepared from human recombinant Sf9 cells expressing the cloned human receptor in the presence of [125I]iodocyanopindolol
ChEMBL 515 11 4 6 3.8 Cc1ccc(S(=O)(=O)NC(=O)Cc2ccc(NC[C@@H](C)NC[C@H](O)c3cccc(Cl)c3)cc2)cc1 10.1021/jm0101500
CHEMBL348501 119312 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Receptor binding assay(Beta-2 adrenergic receptor) carried out with membranes prepared from human recombinant Sf9 cells expressing the cloned human receptor in the presence of [125I]iodocyanopindololReceptor binding assay(Beta-2 adrenergic receptor) carried out with membranes prepared from human recombinant Sf9 cells expressing the cloned human receptor in the presence of [125I]iodocyanopindolol
ChEMBL 515 11 4 6 3.8 Cc1ccc(S(=O)(=O)NC(=O)Cc2ccc(NC[C@@H](C)NC[C@H](O)c3cccc(Cl)c3)cc2)cc1 10.1021/jm0101500
54417230 69852 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Displacement of [3H]dihydroalprenolol from beta2-adrenoceptor after 90 mins by liquid scintillation countingDisplacement of [3H]dihydroalprenolol from beta2-adrenoceptor after 90 mins by liquid scintillation counting
ChEMBL 468 12 8 8 1.7 OCc1cc(C(O)CNCc2ccc(CNCC(O)c3ccc(O)c(CO)c3)cc2)ccc1O 10.1016/j.bmcl.2011.11.072
CHEMBL1940809 69852 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Displacement of [3H]dihydroalprenolol from beta2-adrenoceptor after 90 mins by liquid scintillation countingDisplacement of [3H]dihydroalprenolol from beta2-adrenoceptor after 90 mins by liquid scintillation counting
ChEMBL 468 12 8 8 1.7 OCc1cc(C(O)CNCc2ccc(CNCC(O)c3ccc(O)c(CO)c3)cc2)ccc1O 10.1016/j.bmcl.2011.11.072
44298288 101099 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
In vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 441 9 1 5 5.8 CCCCCCc1csc(N2CCc3cc(S(=O)(=O)Nc4ccccc4)ccc32)n1 10.1016/s0960-894x(99)00277-2
CHEMBL298594 101099 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
In vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 441 9 1 5 5.8 CCCCCCc1csc(N2CCc3cc(S(=O)(=O)Nc4ccccc4)ccc32)n1 10.1016/s0960-894x(99)00277-2
44280957 112046 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Binding affinity towards Beta-2 adrenergic receptor prepared from CHO cells expressing the cloned human receptor in the presence of [125I]iodocyanopindololBinding affinity towards Beta-2 adrenergic receptor prepared from CHO cells expressing the cloned human receptor in the presence of [125I]iodocyanopindolol
ChEMBL 590 13 3 9 3.4 O=C(CCc1nc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)no1)N1CCCC1 10.1016/s0960-894x(00)00267-5
CHEMBL32996 112046 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Binding affinity towards Beta-2 adrenergic receptor prepared from CHO cells expressing the cloned human receptor in the presence of [125I]iodocyanopindololBinding affinity towards Beta-2 adrenergic receptor prepared from CHO cells expressing the cloned human receptor in the presence of [125I]iodocyanopindolol
ChEMBL 590 13 3 9 3.4 O=C(CCc1nc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)no1)N1CCCC1 10.1016/s0960-894x(00)00267-5
2291 3123 52 None -3 12 Human 7.3 pIC50 = 7.3 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O nan
2561 3123 52 None -3 12 Human 7.3 pIC50 = 7.3 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O nan
4932 3123 52 None -3 12 Human 7.3 pIC50 = 7.3 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O nan
CHEMBL631 3123 52 None -3 12 Human 7.3 pIC50 = 7.3 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O nan
DB01182 3123 52 None -3 12 Human 7.3 pIC50 = 7.3 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O nan
44298256 195426 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
In vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 426 9 1 6 4.7 CCCCCCc1nc(N2CCc3cc(S(=O)(=O)Nc4ccccc4)ccc32)no1 10.1016/s0960-894x(99)00277-2
CHEMBL56768 195426 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
In vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 426 9 1 6 4.7 CCCCCCc1nc(N2CCc3cc(S(=O)(=O)Nc4ccccc4)ccc32)no1 10.1016/s0960-894x(99)00277-2
44307343 201900 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cell
ChEMBL 457 12 3 7 2.5 COc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3cccnc3)cc2)cc1 10.1016/s0960-894x(98)00381-3
CHEMBL66964 201900 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cell
ChEMBL 457 12 3 7 2.5 COc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3cccnc3)cc2)cc1 10.1016/s0960-894x(98)00381-3
50995330 136466 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]CYP from human beta-2 adrenergic receptor expressed in CHO cell membrane after 1 hr by scintillation counting methodDisplacement of [125I]CYP from human beta-2 adrenergic receptor expressed in CHO cell membrane after 1 hr by scintillation counting method
ChEMBL 422 7 4 6 3.1 Nc1nc(CNC(=O)c2ccc(C[C@@H]3CC[C@H]([C@H](O)c4ccccc4)N3)cc2)cs1 10.1016/j.bmcl.2015.11.030
CHEMBL3746068 136466 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]CYP from human beta-2 adrenergic receptor expressed in CHO cell membrane after 1 hr by scintillation counting methodDisplacement of [125I]CYP from human beta-2 adrenergic receptor expressed in CHO cell membrane after 1 hr by scintillation counting method
ChEMBL 422 7 4 6 3.1 Nc1nc(CNC(=O)c2ccc(C[C@@H]3CC[C@H]([C@H](O)c4ccccc4)N3)cc2)cs1 10.1016/j.bmcl.2015.11.030
2464 3570 52 None - 6 Dog 5.3 pIC50 = 5.3 Binding
Tested for Beta-2 adrenergic receptor selectivity in canine lung tissue in anesthetized dogsTested for Beta-2 adrenergic receptor selectivity in canine lung tissue in anesthetized dogs
ChEMBL 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C 10.1021/jm00172a033
5253 3570 52 None - 6 Dog 5.3 pIC50 = 5.3 Binding
Tested for Beta-2 adrenergic receptor selectivity in canine lung tissue in anesthetized dogsTested for Beta-2 adrenergic receptor selectivity in canine lung tissue in anesthetized dogs
ChEMBL 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C 10.1021/jm00172a033
7297 3570 52 None - 6 Dog 5.3 pIC50 = 5.3 Binding
Tested for Beta-2 adrenergic receptor selectivity in canine lung tissue in anesthetized dogsTested for Beta-2 adrenergic receptor selectivity in canine lung tissue in anesthetized dogs
ChEMBL 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C 10.1021/jm00172a033
CHEMBL471 3570 52 None - 6 Dog 5.3 pIC50 = 5.3 Binding
Tested for Beta-2 adrenergic receptor selectivity in canine lung tissue in anesthetized dogsTested for Beta-2 adrenergic receptor selectivity in canine lung tissue in anesthetized dogs
ChEMBL 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C 10.1021/jm00172a033
DB00489 3570 52 None - 6 Dog 5.3 pIC50 = 5.3 Binding
Tested for Beta-2 adrenergic receptor selectivity in canine lung tissue in anesthetized dogsTested for Beta-2 adrenergic receptor selectivity in canine lung tissue in anesthetized dogs
ChEMBL 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C 10.1021/jm00172a033
44298497 193022 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
In vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 464 11 1 5 5.9 CCCCCCCCc1ccnc(N2CCc3cc(S(=O)(=O)Nc4ccccc4)ccc32)n1 10.1016/s0960-894x(99)00277-2
CHEMBL53359 193022 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
In vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 464 11 1 5 5.9 CCCCCCCCc1ccnc(N2CCc3cc(S(=O)(=O)Nc4ccccc4)ccc32)n1 10.1016/s0960-894x(99)00277-2
44377957 57183 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindololBinding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindolol
ChEMBL 537 13 3 6 3.8 CCCCN1CCN(c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)C1=O 10.1016/s0960-894x(99)00072-4
CHEMBL166013 57183 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindololBinding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindolol
ChEMBL 537 13 3 6 3.8 CCCCN1CCN(c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)C1=O 10.1016/s0960-894x(99)00072-4
46881902 7749 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counter
ChEMBL 430 9 3 5 3.8 O=C(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccccc1N1CCCC1 10.1016/j.bmcl.2010.01.130
CHEMBL1089735 7749 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counter
ChEMBL 430 9 3 5 3.8 O=C(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccccc1N1CCCC1 10.1016/j.bmcl.2010.01.130
9826638 201599 1 None - 0 Human 6.3 pIC50 = 6.3 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cell
ChEMBL 484 12 4 7 3.2 CC(C)c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(N)nc3)cc2)cc1 10.1016/s0960-894x(98)00381-3
CHEMBL64760 201599 1 None - 0 Human 6.3 pIC50 = 6.3 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cell
ChEMBL 484 12 4 7 3.2 CC(C)c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(N)nc3)cc2)cc1 10.1016/s0960-894x(98)00381-3
44268605 97949 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.
ChEMBL 542 14 6 7 3.3 CCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/s0960-894x(98)00170-x
CHEMBL275511 97949 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.
ChEMBL 542 14 6 7 3.3 CCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/s0960-894x(98)00170-x
44281408 112802 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindolol
ChEMBL 646 13 4 10 4.4 COC(=O)NC(c1ccc(F)cc1)c1nc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)no1 10.1016/s0960-894x(00)00268-7
CHEMBL33155 112802 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindolol
ChEMBL 646 13 4 10 4.4 COC(=O)NC(c1ccc(F)cc1)c1nc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)no1 10.1016/s0960-894x(00)00268-7
12828562 109205 0 None - 2 Guinea pig 5.3 pIC50 = 5.3 Binding
Inhibitory activity against beta-2 adrenergic receptor in guinea pig tracheal strip is determinedInhibitory activity against beta-2 adrenergic receptor in guinea pig tracheal strip is determined
ChEMBL 237 3 3 4 1.7 CC(C)NCC1OCCc2cc(O)c(O)cc21 10.1021/jm00073a006
CHEMBL322842 109205 0 None - 2 Guinea pig 5.3 pIC50 = 5.3 Binding
Inhibitory activity against beta-2 adrenergic receptor in guinea pig tracheal strip is determinedInhibitory activity against beta-2 adrenergic receptor in guinea pig tracheal strip is determined
ChEMBL 237 3 3 4 1.7 CC(C)NCC1OCCc2cc(O)c(O)cc21 10.1021/jm00073a006
44281255 114982 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindolol
ChEMBL 639 13 3 9 5.3 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2noc(Cc3cccc(OC(F)(F)F)c3)n2)cc1 10.1016/s0960-894x(00)00268-7
CHEMBL33515 114982 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindolol
ChEMBL 639 13 3 9 5.3 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2noc(Cc3cccc(OC(F)(F)F)c3)n2)cc1 10.1016/s0960-894x(00)00268-7
9958539 102618 0 None 1 3 Human 7.3 pIC50 = 7.3 Binding
Inhibitory activity against CHO cells expressing human Beta-2 adrenergic receptor with [125I]-iodocyanopindololInhibitory activity against CHO cells expressing human Beta-2 adrenergic receptor with [125I]-iodocyanopindolol
ChEMBL 527 3 2 5 3.4 COc1c(I)cc(CC2NCCc3nc(N)sc32)cc1I 10.1016/s0960-894x(00)00459-5
CHEMBL307647 102618 0 None 1 3 Human 7.3 pIC50 = 7.3 Binding
Inhibitory activity against CHO cells expressing human Beta-2 adrenergic receptor with [125I]-iodocyanopindololInhibitory activity against CHO cells expressing human Beta-2 adrenergic receptor with [125I]-iodocyanopindolol
ChEMBL 527 3 2 5 3.4 COc1c(I)cc(CC2NCCc3nc(N)sc32)cc1I 10.1016/s0960-894x(00)00459-5
44349367 16725 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cells
ChEMBL 487 11 4 7 4.9 O=[N+]([O-])/C=C(\Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)Nc1cc(Cl)cc(Cl)c1 10.1016/s0960-894x(00)00669-7
CHEMBL125246 16725 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cells
ChEMBL 487 11 4 7 4.9 O=[N+]([O-])/C=C(\Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)Nc1cc(Cl)cc(Cl)c1 10.1016/s0960-894x(00)00669-7
67972106 136551 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]CYP from human beta-2 adrenergic receptor expressed in CHO cell membrane after 1 hr by scintillation counting methodDisplacement of [125I]CYP from human beta-2 adrenergic receptor expressed in CHO cell membrane after 1 hr by scintillation counting method
ChEMBL 448 5 2 5 3.3 O=C(c1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1)N1CCC2(CCOC2=O)CC1 10.1016/j.bmcl.2015.11.030
CHEMBL3747244 136551 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]CYP from human beta-2 adrenergic receptor expressed in CHO cell membrane after 1 hr by scintillation counting methodDisplacement of [125I]CYP from human beta-2 adrenergic receptor expressed in CHO cell membrane after 1 hr by scintillation counting method
ChEMBL 448 5 2 5 3.3 O=C(c1ccc(C[C@@H]2CC[C@H]([C@H](O)c3ccccc3)N2)cc1)N1CCC2(CCOC2=O)CC1 10.1016/j.bmcl.2015.11.030
80447 56917 113 None - 0 Dog 4.3 pIC50 = 4.3 Binding
Binding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprololBinding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprolol
ChEMBL 207 2 1 4 1.0 O=[N+]([O-])c1ccc(N2CCNCC2)cc1 10.1021/jm00082a016
CHEMBL165012 56917 113 None - 0 Dog 4.3 pIC50 = 4.3 Binding
Binding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprololBinding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprolol
ChEMBL 207 2 1 4 1.0 O=[N+]([O-])c1ccc(N2CCNCC2)cc1 10.1021/jm00082a016
10138809 168508 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cells
ChEMBL 450 8 4 5 4.3 N#CN/C(=N\c1cccc2ccccc12)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/s0960-894x(00)00669-7
CHEMBL439794 168508 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cells
ChEMBL 450 8 4 5 4.3 N#CN/C(=N\c1cccc2ccccc12)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/s0960-894x(00)00669-7
44457929 84339 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibitory activity against cloned human Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol in CHO cells by receptor binding assayInhibitory activity against cloned human Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol in CHO cells by receptor binding assay
ChEMBL 593 17 3 10 3.9 CCCCCCCCn1nnn(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)c1=O 10.1016/s0960-894x(99)00182-1
CHEMBL22318 84339 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibitory activity against cloned human Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol in CHO cells by receptor binding assayInhibitory activity against cloned human Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol in CHO cells by receptor binding assay
ChEMBL 593 17 3 10 3.9 CCCCCCCCn1nnn(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)c1=O 10.1016/s0960-894x(99)00182-1
44301818 201053 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Binding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindololBinding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindolol
ChEMBL 572 11 4 8 5.2 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3ccc(O)cc3)cs2)cc1 10.1016/s0960-894x(00)00390-5
CHEMBL61962 201053 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Binding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindololBinding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindolol
ChEMBL 572 11 4 8 5.2 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3ccc(O)cc3)cs2)cc1 10.1016/s0960-894x(00)00390-5
12043159 99538 0 None - 0 Human 4.2 pIC50 = 4.2 Binding
Binding affinity towards Beta-2 adrenergic receptor prepared from CHO cells expressing the cloned human receptor in the presence of [125I]iodocyanopindololBinding affinity towards Beta-2 adrenergic receptor prepared from CHO cells expressing the cloned human receptor in the presence of [125I]iodocyanopindolol
ChEMBL 549 14 3 9 3.7 CC(=O)CCCc1nc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)no1 10.1016/s0960-894x(00)00267-5
CHEMBL286800 99538 0 None - 0 Human 4.2 pIC50 = 4.2 Binding
Binding affinity towards Beta-2 adrenergic receptor prepared from CHO cells expressing the cloned human receptor in the presence of [125I]iodocyanopindololBinding affinity towards Beta-2 adrenergic receptor prepared from CHO cells expressing the cloned human receptor in the presence of [125I]iodocyanopindolol
ChEMBL 549 14 3 9 3.7 CC(=O)CCCc1nc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)no1 10.1016/s0960-894x(00)00267-5
14664343 10987 0 None - 0 Dog 4.2 pIC50 = 4.2 Binding
In vitro Beta-2 adrenergic receptor affinity in partially purified membrane fractions from canine lung tissue using [SH]dihydroalprenolol (4.5 nM)In vitro Beta-2 adrenergic receptor affinity in partially purified membrane fractions from canine lung tissue using [SH]dihydroalprenolol (4.5 nM)
ChEMBL 460 12 3 8 2.0 Cc1nccn1-c1ccc(OCCNCC(O)COc2ccc(NS(C)(=O)=O)cc2)cc1 10.1021/jm00166a002
CHEMBL11629 10987 0 None - 0 Dog 4.2 pIC50 = 4.2 Binding
In vitro Beta-2 adrenergic receptor affinity in partially purified membrane fractions from canine lung tissue using [SH]dihydroalprenolol (4.5 nM)In vitro Beta-2 adrenergic receptor affinity in partially purified membrane fractions from canine lung tissue using [SH]dihydroalprenolol (4.5 nM)
ChEMBL 460 12 3 8 2.0 Cc1nccn1-c1ccc(OCCNCC(O)COc2ccc(NS(C)(=O)=O)cc2)cc1 10.1021/jm00166a002
CHEMBL1178024 10987 0 None - 0 Dog 4.2 pIC50 = 4.2 Binding
In vitro Beta-2 adrenergic receptor affinity in partially purified membrane fractions from canine lung tissue using [SH]dihydroalprenolol (4.5 nM)In vitro Beta-2 adrenergic receptor affinity in partially purified membrane fractions from canine lung tissue using [SH]dihydroalprenolol (4.5 nM)
ChEMBL 460 12 3 8 2.0 Cc1nccn1-c1ccc(OCCNCC(O)COc2ccc(NS(C)(=O)=O)cc2)cc1 10.1021/jm00166a002
44268277 22093 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandBinding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligand
ChEMBL 408 11 4 6 2.1 CC(C)S(=O)(=O)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/s0960-894x(98)00169-3
CHEMBL13238 22093 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandBinding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligand
ChEMBL 408 11 4 6 2.1 CC(C)S(=O)(=O)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/s0960-894x(98)00169-3
688467 85357 2 None 14 2 Human 8.2 pIC50 = 8.2 Binding
Mitogenesis inhibition method: To measure beta2-AR mediated inhibition of mitogenesis, HEK-beta2-AR, 1321N1 or U87MG cells were seeded in a 96-well plate at approximately 5,000 cells/well. After 48 hours, the wells were rinsed twice and the medium was replaced with fresh medium containing 10 uL of drug in sterile water. After another 24 hours of incubation at 37° C., 0.25 uCi of [3H]-thymidine was added to each well. The cells were incubated for an additional 2 hours at 37° C., at which point 10 uL of 10x trypsin was added, and the resuspended cells were harvested using a Tomtec 96 harvester through glass fiber filters.Mitogenesis inhibition method: To measure beta2-AR mediated inhibition of mitogenesis, HEK-beta2-AR, 1321N1 or U87MG cells were seeded in a 96-well plate at approximately 5,000 cells/well. After 48 hours, the wells were rinsed twice and the medium was replaced with fresh medium containing 10 uL of drug in sterile water. After another 24 hours of incubation at 37° C., 0.25 uCi of [3H]-thymidine was added to each well. The cells were incubated for an additional 2 hours at 37° C., at which point 10 uL of 10x trypsin was added, and the resuspended cells were harvested using a Tomtec 96 harvester through glass fiber filters.
ChEMBL 303 6 5 5 2.1 C[C@@H](Cc1ccc(O)cc1)NC[C@H](O)c1cc(O)cc(O)c1 nan
CHEMBL229476 85357 2 None 14 2 Human 8.2 pIC50 = 8.2 Binding
Mitogenesis inhibition method: To measure beta2-AR mediated inhibition of mitogenesis, HEK-beta2-AR, 1321N1 or U87MG cells were seeded in a 96-well plate at approximately 5,000 cells/well. After 48 hours, the wells were rinsed twice and the medium was replaced with fresh medium containing 10 uL of drug in sterile water. After another 24 hours of incubation at 37° C., 0.25 uCi of [3H]-thymidine was added to each well. The cells were incubated for an additional 2 hours at 37° C., at which point 10 uL of 10x trypsin was added, and the resuspended cells were harvested using a Tomtec 96 harvester through glass fiber filters.Mitogenesis inhibition method: To measure beta2-AR mediated inhibition of mitogenesis, HEK-beta2-AR, 1321N1 or U87MG cells were seeded in a 96-well plate at approximately 5,000 cells/well. After 48 hours, the wells were rinsed twice and the medium was replaced with fresh medium containing 10 uL of drug in sterile water. After another 24 hours of incubation at 37° C., 0.25 uCi of [3H]-thymidine was added to each well. The cells were incubated for an additional 2 hours at 37° C., at which point 10 uL of 10x trypsin was added, and the resuspended cells were harvested using a Tomtec 96 harvester through glass fiber filters.
ChEMBL 303 6 5 5 2.1 C[C@@H](Cc1ccc(O)cc1)NC[C@H](O)c1cc(O)cc(O)c1 nan
24900689 70005 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 479 11 5 7 3.5 COc1ccccc1CNCc1cccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)c1 10.1016/j.bmcl.2011.10.049
CHEMBL1945039 70005 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 479 11 5 7 3.5 COc1ccccc1CNCc1cccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)c1 10.1016/j.bmcl.2011.10.049
57391554 70010 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 479 11 5 7 3.5 COc1cccc(CNCc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)sc34)c2)c1 10.1016/j.bmcl.2011.10.049
CHEMBL1945044 70010 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 479 11 5 7 3.5 COc1cccc(CNCc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)sc34)c2)c1 10.1016/j.bmcl.2011.10.049
24901284 70028 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 545 12 5 6 5.2 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCCc3cccc(CNCCc4c(Cl)cccc4Cl)c3)c2s1 10.1016/j.bmcl.2011.10.049
CHEMBL1945296 70028 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 545 12 5 6 5.2 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCCc3cccc(CNCCc4c(Cl)cccc4Cl)c3)c2s1 10.1016/j.bmcl.2011.10.049
54592025 147450 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 μg/well for beta1 and 5 μg/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 μl, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 μM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 μg/well for beta1 and 5 μg/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 μl, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 μM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.
ChEMBL 695 18 5 10 6.4 CN(CCCCCCCCCNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12)C1CCC(OC(=O)C(O)(c2cccs2)c2cccs2)CC1 nan
CHEMBL3934254 147450 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 μg/well for beta1 and 5 μg/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 μl, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 μM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 μg/well for beta1 and 5 μg/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 μl, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 μM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.
ChEMBL 695 18 5 10 6.4 CN(CCCCCCCCCNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12)C1CCC(OC(=O)C(O)(c2cccs2)c2cccs2)CC1 nan
118710948 113248 0 None - 3 Guinea pig 8.2 pIC50 = 8.2 Binding
Agonist activity at adrenergic beta2 receptor in electrically-stimulated Dunkin-Hartley guinea pig tracheal strip assessed as inhibition of contractionAgonist activity at adrenergic beta2 receptor in electrically-stimulated Dunkin-Hartley guinea pig tracheal strip assessed as inhibition of contraction
ChEMBL 386 9 4 5 3.5 CCCCc1cccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)c1 10.1016/j.bmcl.2014.06.014
CHEMBL3323668 113248 0 None - 3 Guinea pig 8.2 pIC50 = 8.2 Binding
Agonist activity at adrenergic beta2 receptor in electrically-stimulated Dunkin-Hartley guinea pig tracheal strip assessed as inhibition of contractionAgonist activity at adrenergic beta2 receptor in electrically-stimulated Dunkin-Hartley guinea pig tracheal strip assessed as inhibition of contraction
ChEMBL 386 9 4 5 3.5 CCCCc1cccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)c1 10.1016/j.bmcl.2014.06.014
54590927 149303 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 μg/well for beta1 and 5 μg/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 μl, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 μM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 μg/well for beta1 and 5 μg/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 μl, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 μM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.
ChEMBL 764 14 6 11 5.9 CN(CCC(=O)Nc1ccc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1Cl)[C@H]1CC[C@H](OC(=O)C(O)(c2cccs2)c2cccs2)CC1 nan
CHEMBL3948979 149303 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 μg/well for beta1 and 5 μg/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 μl, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 μM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 μg/well for beta1 and 5 μg/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 μl, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 μM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.
ChEMBL 764 14 6 11 5.9 CN(CCC(=O)Nc1ccc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1Cl)[C@H]1CC[C@H](OC(=O)C(O)(c2cccs2)c2cccs2)CC1 nan
667688 85358 4 None - 1 Human 8.2 pIC50 = 8.2 Binding
Mitogenesis inhibition method: To measure beta2-AR mediated inhibition of mitogenesis, HEK-beta2-AR, 1321N1 or U87MG cells were seeded in a 96-well plate at approximately 5,000 cells/well. After 48 hours, the wells were rinsed twice and the medium was replaced with fresh medium containing 10 uL of drug in sterile water. After another 24 hours of incubation at 37° C., 0.25 uCi of [3H]-thymidine was added to each well. The cells were incubated for an additional 2 hours at 37° C., at which point 10 uL of 10x trypsin was added, and the resuspended cells were harvested using a Tomtec 96 harvester through glass fiber filters.Mitogenesis inhibition method: To measure beta2-AR mediated inhibition of mitogenesis, HEK-beta2-AR, 1321N1 or U87MG cells were seeded in a 96-well plate at approximately 5,000 cells/well. After 48 hours, the wells were rinsed twice and the medium was replaced with fresh medium containing 10 uL of drug in sterile water. After another 24 hours of incubation at 37° C., 0.25 uCi of [3H]-thymidine was added to each well. The cells were incubated for an additional 2 hours at 37° C., at which point 10 uL of 10x trypsin was added, and the resuspended cells were harvested using a Tomtec 96 harvester through glass fiber filters.
ChEMBL 303 6 5 5 2.1 C[C@H](Cc1ccc(O)cc1)NC[C@@H](O)c1cc(O)cc(O)c1 nan
CHEMBL229477 85358 4 None - 1 Human 8.2 pIC50 = 8.2 Binding
Mitogenesis inhibition method: To measure beta2-AR mediated inhibition of mitogenesis, HEK-beta2-AR, 1321N1 or U87MG cells were seeded in a 96-well plate at approximately 5,000 cells/well. After 48 hours, the wells were rinsed twice and the medium was replaced with fresh medium containing 10 uL of drug in sterile water. After another 24 hours of incubation at 37° C., 0.25 uCi of [3H]-thymidine was added to each well. The cells were incubated for an additional 2 hours at 37° C., at which point 10 uL of 10x trypsin was added, and the resuspended cells were harvested using a Tomtec 96 harvester through glass fiber filters.Mitogenesis inhibition method: To measure beta2-AR mediated inhibition of mitogenesis, HEK-beta2-AR, 1321N1 or U87MG cells were seeded in a 96-well plate at approximately 5,000 cells/well. After 48 hours, the wells were rinsed twice and the medium was replaced with fresh medium containing 10 uL of drug in sterile water. After another 24 hours of incubation at 37° C., 0.25 uCi of [3H]-thymidine was added to each well. The cells were incubated for an additional 2 hours at 37° C., at which point 10 uL of 10x trypsin was added, and the resuspended cells were harvested using a Tomtec 96 harvester through glass fiber filters.
ChEMBL 303 6 5 5 2.1 C[C@H](Cc1ccc(O)cc1)NC[C@@H](O)c1cc(O)cc(O)c1 nan
155531982 171114 0 None 6 2 Human 8.2 pIC50 = 8.2 Binding
Antagonist activity at human recombinant beta2 adrenoreceptor expressed in CHOK1 cells incubated for 30 mins by HTRFAntagonist activity at human recombinant beta2 adrenoreceptor expressed in CHOK1 cells incubated for 30 mins by HTRF
ChEMBL 526 22 3 9 2.3 C=CCc1ccccc1OCC(O)CNCCOCCOCCOCCOCCNC(=O)OC(C)(C)C 10.1039/C8MD00412A
CHEMBL4466532 171114 0 None 6 2 Human 8.2 pIC50 = 8.2 Binding
Antagonist activity at human recombinant beta2 adrenoreceptor expressed in CHOK1 cells incubated for 30 mins by HTRFAntagonist activity at human recombinant beta2 adrenoreceptor expressed in CHOK1 cells incubated for 30 mins by HTRF
ChEMBL 526 22 3 9 2.3 C=CCc1ccccc1OCC(O)CNCCOCCOCCOCCOCCNC(=O)OC(C)(C)C 10.1039/C8MD00412A
46881901 7748 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counter
ChEMBL 437 9 3 4 4.9 O=C(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2010.01.130
CHEMBL1089734 7748 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counter
ChEMBL 437 9 3 4 4.9 O=C(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2010.01.130
1155 1592 45 None -2 5 Guinea pig 7.2 pIC50 = 7.2 Binding
In vitro inhibitory concentration Beta-2 adrenergic receptor in Guinea pig tracheaIn vitro inhibitory concentration Beta-2 adrenergic receptor in Guinea pig trachea
ChEMBL 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 10.1016/s0960-894x(03)00538-9
3343 1592 45 None -2 5 Guinea pig 7.2 pIC50 = 7.2 Binding
In vitro inhibitory concentration Beta-2 adrenergic receptor in Guinea pig tracheaIn vitro inhibitory concentration Beta-2 adrenergic receptor in Guinea pig trachea
ChEMBL 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 10.1016/s0960-894x(03)00538-9
557 1592 45 None -2 5 Guinea pig 7.2 pIC50 = 7.2 Binding
In vitro inhibitory concentration Beta-2 adrenergic receptor in Guinea pig tracheaIn vitro inhibitory concentration Beta-2 adrenergic receptor in Guinea pig trachea
ChEMBL 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 10.1016/s0960-894x(03)00538-9
CHEMBL32800 1592 45 None -2 5 Guinea pig 7.2 pIC50 = 7.2 Binding
In vitro inhibitory concentration Beta-2 adrenergic receptor in Guinea pig tracheaIn vitro inhibitory concentration Beta-2 adrenergic receptor in Guinea pig trachea
ChEMBL 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 10.1016/s0960-894x(03)00538-9
DB01288 1592 45 None -2 5 Guinea pig 7.2 pIC50 = 7.2 Binding
In vitro inhibitory concentration Beta-2 adrenergic receptor in Guinea pig tracheaIn vitro inhibitory concentration Beta-2 adrenergic receptor in Guinea pig trachea
ChEMBL 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 10.1016/s0960-894x(03)00538-9
10360435 205374 0 None - 0 Guinea pig 7.2 pIC50 = 7.2 Binding
In vitro inhibitory concentration Beta-2 adrenergic receptor in Guinea pig tracheaIn vitro inhibitory concentration Beta-2 adrenergic receptor in Guinea pig trachea
ChEMBL 349 9 4 5 2.7 CC(Cc1ccc(OCCF)cc1)NCC(O)c1cc(O)cc(O)c1 10.1016/s0960-894x(03)00538-9
CHEMBL92103 205374 0 None - 0 Guinea pig 7.2 pIC50 = 7.2 Binding
In vitro inhibitory concentration Beta-2 adrenergic receptor in Guinea pig tracheaIn vitro inhibitory concentration Beta-2 adrenergic receptor in Guinea pig trachea
ChEMBL 349 9 4 5 2.7 CC(Cc1ccc(OCCF)cc1)NCC(O)c1cc(O)cc(O)c1 10.1016/s0960-894x(03)00538-9
46881796 5507 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counter
ChEMBL 401 8 3 6 2.8 O=C(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1cccc2ccnn12 10.1016/j.bmcl.2010.01.130
CHEMBL1077273 5507 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counter
ChEMBL 401 8 3 6 2.8 O=C(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1cccc2ccnn12 10.1016/j.bmcl.2010.01.130
46882029 5667 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counter
ChEMBL 454 11 3 5 4.2 O=C(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1cccc(CCn2cccc2)c1 10.1016/j.bmcl.2010.01.130
CHEMBL1078496 5667 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counter
ChEMBL 454 11 3 5 4.2 O=C(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1cccc(CCn2cccc2)c1 10.1016/j.bmcl.2010.01.130
44335499 4908 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Beta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindolol
ChEMBL 439 10 3 5 3.9 CC(C)c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(98)00571-x
CHEMBL104981 4908 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Beta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindolol
ChEMBL 439 10 3 5 3.9 CC(C)c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(98)00571-x
46881530 7227 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counter
ChEMBL 415 9 4 5 3.0 O=C(Cc1nc2ccccc2[nH]1)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/j.bmcl.2010.01.130
CHEMBL1086149 7227 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counter
ChEMBL 415 9 4 5 3.0 O=C(Cc1nc2ccccc2[nH]1)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/j.bmcl.2010.01.130
117628769 144481 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 ug/well for beta1 and 5 ug/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 ul, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 uM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 ug/well for beta1 and 5 ug/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 ul, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 uM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.
ChEMBL 772 15 5 13 5.2 CN(CCCn1c(=O)oc2cc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)ccc21)[C@H]1CC[C@H](OC(=O)C(O)(c2cccs2)c2cccs2)CC1 nan
CHEMBL3911114 144481 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 ug/well for beta1 and 5 ug/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 ul, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 uM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 ug/well for beta1 and 5 ug/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 ul, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 uM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.
ChEMBL 772 15 5 13 5.2 CN(CCCn1c(=O)oc2cc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)ccc21)[C@H]1CC[C@H](OC(=O)C(O)(c2cccs2)c2cccs2)CC1 nan
44301764 100152 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindololBinding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindolol
ChEMBL 564 15 3 7 6.0 CCCCCCc1csc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)n1 10.1016/s0960-894x(00)00390-5
CHEMBL291992 100152 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindololBinding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindolol
ChEMBL 564 15 3 7 6.0 CCCCCCc1csc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)n1 10.1016/s0960-894x(00)00390-5
12049926 201384 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity for clone human Beta-2 adrenergic receptor from CHO cell membranes in the presence of I-iodocyanopindololBinding affinity for clone human Beta-2 adrenergic receptor from CHO cell membranes in the presence of I-iodocyanopindolol
ChEMBL 654 14 3 10 4.8 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-n2ncc(COc3ccc(OC(F)(F)F)cc3)n2)cc1 10.1016/s0960-894x(00)00422-4
CHEMBL63825 201384 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity for clone human Beta-2 adrenergic receptor from CHO cell membranes in the presence of I-iodocyanopindololBinding affinity for clone human Beta-2 adrenergic receptor from CHO cell membranes in the presence of I-iodocyanopindolol
ChEMBL 654 14 3 10 4.8 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-n2ncc(COc3ccc(OC(F)(F)F)cc3)n2)cc1 10.1016/s0960-894x(00)00422-4
3086576 176371 29 None 40 2 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]CGP1217 from human recombinant adrenergic beta2 receptor transfected in insect Sf9 cells by scintillation countingDisplacement of [3H]CGP1217 from human recombinant adrenergic beta2 receptor transfected in insect Sf9 cells by scintillation counting
ChEMBL 261 2 3 4 1.1 CC(C)N[C@@H]1CCn2c(=O)[nH]c3cccc(c32)[C@H]1O 10.1021/jm801211c
CHEMBL462313 176371 29 None 40 2 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]CGP1217 from human recombinant adrenergic beta2 receptor transfected in insect Sf9 cells by scintillation countingDisplacement of [3H]CGP1217 from human recombinant adrenergic beta2 receptor transfected in insect Sf9 cells by scintillation counting
ChEMBL 261 2 3 4 1.1 CC(C)N[C@@H]1CCn2c(=O)[nH]c3cccc(c32)[C@H]1O 10.1021/jm801211c
CHEMBL513390 176371 29 None 40 2 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]CGP1217 from human recombinant adrenergic beta2 receptor transfected in insect Sf9 cells by scintillation countingDisplacement of [3H]CGP1217 from human recombinant adrenergic beta2 receptor transfected in insect Sf9 cells by scintillation counting
ChEMBL 261 2 3 4 1.1 CC(C)N[C@@H]1CCn2c(=O)[nH]c3cccc(c32)[C@H]1O 10.1021/jm801211c
44307333 201970 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cell
ChEMBL 472 12 4 8 2.0 COc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(N)nc3)cc2)cc1 10.1016/s0960-894x(98)00381-3
CHEMBL67416 201970 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cell
ChEMBL 472 12 4 8 2.0 COc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(N)nc3)cc2)cc1 10.1016/s0960-894x(98)00381-3
44298515 194165 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
In vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 436 9 1 5 5.1 CCCCCCc1ccnc(N2CCc3cc(S(=O)(=O)Nc4ccccc4)ccc32)n1 10.1016/s0960-894x(99)00277-2
CHEMBL55852 194165 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
In vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 436 9 1 5 5.1 CCCCCCc1ccnc(N2CCc3cc(S(=O)(=O)Nc4ccccc4)ccc32)n1 10.1016/s0960-894x(99)00277-2
15123375 57174 3 None - 0 Dog 5.2 pIC50 = 5.2 Binding
Binding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprololBinding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprolol
ChEMBL 295 4 2 3 1.9 O=C(NCC1CN(c2ccccc2)CCN1)c1ccccc1 10.1021/jm00082a016
CHEMBL165901 57174 3 None - 0 Dog 5.2 pIC50 = 5.2 Binding
Binding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprololBinding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprolol
ChEMBL 295 4 2 3 1.9 O=C(NCC1CN(c2ccccc2)CCN1)c1ccccc1 10.1021/jm00082a016
44268214 18367 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandBinding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligand
ChEMBL 331 10 3 5 2.4 COc1ccc(CCCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/s0960-894x(98)00169-3
CHEMBL12762 18367 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandBinding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligand
ChEMBL 331 10 3 5 2.4 COc1ccc(CCCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/s0960-894x(98)00169-3
44298851 100075 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
In vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 463 11 1 4 6.5 CCCCCCCCc1cccc(N2CCc3cc(S(=O)(=O)Nc4ccccc4)ccc32)n1 10.1016/s0960-894x(99)00277-2
CHEMBL291467 100075 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
In vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 463 11 1 4 6.5 CCCCCCCCc1cccc(N2CCc3cc(S(=O)(=O)Nc4ccccc4)ccc32)n1 10.1016/s0960-894x(99)00277-2
57401435 70042 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 458 11 5 6 2.8 O=c1ccc2c([C@@H](O)CNCCc3cccc(CNCCc4ccccn4)c3)ccc(O)c2[nH]1 10.1016/j.bmcl.2011.10.049
CHEMBL1945503 70042 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 458 11 5 6 2.8 O=c1ccc2c([C@@H](O)CNCCc3cccc(CNCCc4ccccn4)c3)ccc(O)c2[nH]1 10.1016/j.bmcl.2011.10.049
24900423 70177 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 537 9 4 6 5.3 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3ccc(-c4cccc(CN5Cc6ccccc6C5)c4)cc3)c2s1 10.1016/j.bmcl.2011.10.049
CHEMBL1947154 70177 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 537 9 4 6 5.3 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3ccc(-c4cccc(CN5Cc6ccccc6C5)c4)cc3)c2s1 10.1016/j.bmcl.2011.10.049
44268341 22541 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandBinding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligand
ChEMBL 492 11 4 6 3.9 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1)c1ccc2ccccc2c1 10.1016/s0960-894x(98)00169-3
CHEMBL13278 22541 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandBinding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligand
ChEMBL 492 11 4 6 3.9 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1)c1ccc2ccccc2c1 10.1016/s0960-894x(98)00169-3
14998850 119475 0 None - 0 Dog 6.2 pIC50 = 6.2 Binding
Binding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprololBinding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprolol
ChEMBL 418 7 3 6 1.3 COc1ccccc1N1CCNC(CNC(=O)c2ccc(NS(C)(=O)=O)cc2)C1 10.1021/jm00082a016
CHEMBL349978 119475 0 None - 0 Dog 6.2 pIC50 = 6.2 Binding
Binding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprololBinding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprolol
ChEMBL 418 7 3 6 1.3 COc1ccccc1N1CCNC(CNC(=O)c2ccc(NS(C)(=O)=O)cc2)C1 10.1021/jm00082a016
44306992 202057 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cell
ChEMBL 442 11 4 7 2.0 Nc1ccc(OC[C@@H](O)CNCCc2ccc(NS(=O)(=O)c3ccccc3)cc2)cn1 10.1016/s0960-894x(98)00381-3
CHEMBL67993 202057 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cell
ChEMBL 442 11 4 7 2.0 Nc1ccc(OC[C@@H](O)CNCCc2ccc(NS(=O)(=O)c3ccccc3)cc2)cn1 10.1016/s0960-894x(98)00381-3
12017011 99887 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.
ChEMBL 590 12 3 7 5.3 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2coc(Cc3ccc(F)c(F)c3)n2)cc1 10.1016/s0960-894x(00)00277-8
CHEMBL289689 99887 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.
ChEMBL 590 12 3 7 5.3 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2coc(Cc3ccc(F)c(F)c3)n2)cc1 10.1016/s0960-894x(00)00277-8
44298731 196394 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
In vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 429 10 2 3 4.9 CCCCCCCCNC(=O)N1CCc2cc(S(=O)(=O)Nc3ccccc3)ccc21 10.1016/s0960-894x(99)00277-2
CHEMBL57430 196394 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
In vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 429 10 2 3 4.9 CCCCCCCCNC(=O)N1CCc2cc(S(=O)(=O)Nc3ccccc3)ccc21 10.1016/s0960-894x(99)00277-2
57395043 70033 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 420 12 5 5 3.1 OCc1cc([C@@H](O)CNCCc2ccc(CNCCc3ccccc3)cc2)ccc1O 10.1016/j.bmcl.2011.10.049
CHEMBL1945300 70033 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 420 12 5 5 3.1 OCc1cc([C@@H](O)CNCCc2ccc(CNCCc3ccccc3)cc2)ccc1O 10.1016/j.bmcl.2011.10.049
44301842 197183 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Binding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindololBinding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindolol
ChEMBL 606 11 3 7 6.7 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3ccc4ccccc4c3)cs2)cc1 10.1016/s0960-894x(00)00390-5
CHEMBL58407 197183 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Binding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindololBinding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindolol
ChEMBL 606 11 3 7 6.7 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3ccc4ccccc4c3)cs2)cc1 10.1016/s0960-894x(00)00390-5
44307205 202110 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cell
ChEMBL 584 17 6 8 3.7 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(N)nc3)cc2)cc1 10.1016/s0960-894x(98)00381-3
CHEMBL68408 202110 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cell
ChEMBL 584 17 6 8 3.7 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(N)nc3)cc2)cc1 10.1016/s0960-894x(98)00381-3
44280860 99439 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Binding affinity towards Beta-2 adrenergic receptor prepared from CHO cells expressing the cloned human receptor in the presence of [125I]iodocyanopindololBinding affinity towards Beta-2 adrenergic receptor prepared from CHO cells expressing the cloned human receptor in the presence of [125I]iodocyanopindolol
ChEMBL 521 13 3 8 4.1 CCCCc1nc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)no1 10.1016/s0960-894x(00)00267-5
CHEMBL286139 99439 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Binding affinity towards Beta-2 adrenergic receptor prepared from CHO cells expressing the cloned human receptor in the presence of [125I]iodocyanopindololBinding affinity towards Beta-2 adrenergic receptor prepared from CHO cells expressing the cloned human receptor in the presence of [125I]iodocyanopindolol
ChEMBL 521 13 3 8 4.1 CCCCc1nc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)no1 10.1016/s0960-894x(00)00267-5
44461489 203631 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Binding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindololBinding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindolol
ChEMBL 591 13 3 6 4.3 O=C1N(CCCC(F)(F)F)CCN1c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(99)00072-4
CHEMBL79675 203631 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Binding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindololBinding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindolol
ChEMBL 591 13 3 6 4.3 O=C1N(CCCC(F)(F)F)CCN1c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(99)00072-4
44298752 195173 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
In vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 415 8 1 3 4.5 CCCCCCN(C)C(=O)N1CCc2cc(S(=O)(=O)Nc3ccccc3)ccc21 10.1016/s0960-894x(99)00277-2
CHEMBL56594 195173 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
In vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 415 8 1 3 4.5 CCCCCCN(C)C(=O)N1CCc2cc(S(=O)(=O)Nc3ccccc3)ccc21 10.1016/s0960-894x(99)00277-2
2369 615 75 None - 8 Bovine 6.2 pIC50 = 6.2 Binding
Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-2 adrenergic receptor in calf lung membranes.Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-2 adrenergic receptor in calf lung membranes.
ChEMBL 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C 10.1021/jm00350a009
356 615 75 None - 8 Bovine 6.2 pIC50 = 6.2 Binding
Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-2 adrenergic receptor in calf lung membranes.Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-2 adrenergic receptor in calf lung membranes.
ChEMBL 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C 10.1021/jm00350a009
549 615 75 None - 8 Bovine 6.2 pIC50 = 6.2 Binding
Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-2 adrenergic receptor in calf lung membranes.Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-2 adrenergic receptor in calf lung membranes.
ChEMBL 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C 10.1021/jm00350a009
CHEMBL423 615 75 None - 8 Bovine 6.2 pIC50 = 6.2 Binding
Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-2 adrenergic receptor in calf lung membranes.Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-2 adrenergic receptor in calf lung membranes.
ChEMBL 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C 10.1021/jm00350a009
DB00195 615 75 None - 8 Bovine 6.2 pIC50 = 6.2 Binding
Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-2 adrenergic receptor in calf lung membranes.Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-2 adrenergic receptor in calf lung membranes.
ChEMBL 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C 10.1021/jm00350a009
44349646 16675 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cells
ChEMBL 636 16 4 8 7.2 CCCCCCCCc1csc(N2CCc3ccc(N/C(=N/c4ccc(CCNC[C@H](O)c5cccnc5)cc4)NC#N)cc32)n1 10.1016/s0960-894x(00)00669-7
CHEMBL124929 16675 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cells
ChEMBL 636 16 4 8 7.2 CCCCCCCCc1csc(N2CCc3ccc(N/C(=N/c4ccc(CCNC[C@H](O)c5cccnc5)cc4)NC#N)cc32)n1 10.1016/s0960-894x(00)00669-7
12043157 116237 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity towards Beta-2 adrenergic receptor prepared from CHO cells expressing the cloned human receptor in the presence of [125I]iodocyanopindololBinding affinity towards Beta-2 adrenergic receptor prepared from CHO cells expressing the cloned human receptor in the presence of [125I]iodocyanopindolol
ChEMBL 589 14 3 8 5.7 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2noc(CCCC3CCCCC3)n2)cc1 10.1016/s0960-894x(00)00267-5
CHEMBL33755 116237 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity towards Beta-2 adrenergic receptor prepared from CHO cells expressing the cloned human receptor in the presence of [125I]iodocyanopindololBinding affinity towards Beta-2 adrenergic receptor prepared from CHO cells expressing the cloned human receptor in the presence of [125I]iodocyanopindolol
ChEMBL 589 14 3 8 5.7 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2noc(CCCC3CCCCC3)n2)cc1 10.1016/s0960-894x(00)00267-5
14739901 205991 0 None - 0 Dog 5.2 pIC50 = 5.2 Binding
Tested for Beta-2 adrenergic receptor selectivity in canine lung tissue in anesthetized dogsTested for Beta-2 adrenergic receptor selectivity in canine lung tissue in anesthetized dogs
ChEMBL 419 8 2 6 1.9 Cc1ccccc1OCC(O)CN1CCN(c2ccc(NS(C)(=O)=O)cc2)CC1 10.1021/jm00172a033
CHEMBL95754 205991 0 None - 0 Dog 5.2 pIC50 = 5.2 Binding
Tested for Beta-2 adrenergic receptor selectivity in canine lung tissue in anesthetized dogsTested for Beta-2 adrenergic receptor selectivity in canine lung tissue in anesthetized dogs
ChEMBL 419 8 2 6 1.9 Cc1ccccc1OCC(O)CN1CCN(c2ccc(NS(C)(=O)=O)cc2)CC1 10.1021/jm00172a033
9871525 16715 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cells
ChEMBL 526 8 4 5 3.7 N#CN/C(=N\c1cccc(I)c1)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/s0960-894x(00)00669-7
CHEMBL125168 16715 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cells
ChEMBL 526 8 4 5 3.7 N#CN/C(=N\c1cccc(I)c1)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/s0960-894x(00)00669-7
3038500 9235 8 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125]I-cyanopindolol from human recombinant beta2 adrenergic receptor after 1 hr by scintillation counting methodDisplacement of [125]I-cyanopindolol from human recombinant beta2 adrenergic receptor after 1 hr by scintillation counting method
ChEMBL 624 11 3 7 6.6 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/acs.jmedchem.5b01372
CHEMBL111201 9235 8 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125]I-cyanopindolol from human recombinant beta2 adrenergic receptor after 1 hr by scintillation counting methodDisplacement of [125]I-cyanopindolol from human recombinant beta2 adrenergic receptor after 1 hr by scintillation counting method
ChEMBL 624 11 3 7 6.6 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/acs.jmedchem.5b01372
46881698 7074 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counter
ChEMBL 458 10 3 5 2.9 O=C(CN1CC(c2ccccc2)CC1=O)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/j.bmcl.2010.01.130
CHEMBL1085444 7074 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counter
ChEMBL 458 10 3 5 2.9 O=C(CN1CC(c2ccccc2)CC1=O)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/j.bmcl.2010.01.130
12049924 202091 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity for clone human Beta-2 adrenergic receptor from CHO cell membranes in the presence of I-iodocyanopindololBinding affinity for clone human Beta-2 adrenergic receptor from CHO cell membranes in the presence of I-iodocyanopindolol
ChEMBL 606 13 3 9 4.2 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-n2ncc(COc3ccc(F)c(F)c3)n2)cc1 10.1016/s0960-894x(00)00422-4
CHEMBL68301 202091 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity for clone human Beta-2 adrenergic receptor from CHO cell membranes in the presence of I-iodocyanopindololBinding affinity for clone human Beta-2 adrenergic receptor from CHO cell membranes in the presence of I-iodocyanopindolol
ChEMBL 606 13 3 9 4.2 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-n2ncc(COc3ccc(F)c(F)c3)n2)cc1 10.1016/s0960-894x(00)00422-4
46881981 5648 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counter
ChEMBL 454 11 3 5 4.2 O=C(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccccc1CCn1cccc1 10.1016/j.bmcl.2010.01.130
CHEMBL1078395 5648 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counter
ChEMBL 454 11 3 5 4.2 O=C(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccccc1CCn1cccc1 10.1016/j.bmcl.2010.01.130
44281469 99642 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindolol
ChEMBL 573 12 3 8 4.5 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2noc(Cc3cccc(F)c3)n2)cc1 10.1016/s0960-894x(00)00268-7
CHEMBL287561 99642 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindolol
ChEMBL 573 12 3 8 4.5 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2noc(Cc3cccc(F)c3)n2)cc1 10.1016/s0960-894x(00)00268-7
4183 1986 62 None - 3 Guinea pig 8.1 pIC50 = 8.1 Binding
Agonist activity at adrenergic beta2 receptor in electrically-stimulated Dunkin-Hartley guinea pig tracheal strip assessed as inhibition of contractionAgonist activity at adrenergic beta2 receptor in electrically-stimulated Dunkin-Hartley guinea pig tracheal strip assessed as inhibition of contraction
ChEMBL 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O 10.1016/j.bmcl.2014.06.014
6918554 1986 62 None - 3 Guinea pig 8.1 pIC50 = 8.1 Binding
Agonist activity at adrenergic beta2 receptor in electrically-stimulated Dunkin-Hartley guinea pig tracheal strip assessed as inhibition of contractionAgonist activity at adrenergic beta2 receptor in electrically-stimulated Dunkin-Hartley guinea pig tracheal strip assessed as inhibition of contraction
ChEMBL 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O 10.1016/j.bmcl.2014.06.014
7455 1986 62 None - 3 Guinea pig 8.1 pIC50 = 8.1 Binding
Agonist activity at adrenergic beta2 receptor in electrically-stimulated Dunkin-Hartley guinea pig tracheal strip assessed as inhibition of contractionAgonist activity at adrenergic beta2 receptor in electrically-stimulated Dunkin-Hartley guinea pig tracheal strip assessed as inhibition of contraction
ChEMBL 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O 10.1016/j.bmcl.2014.06.014
CHEMBL1095777 1986 62 None - 3 Guinea pig 8.1 pIC50 = 8.1 Binding
Agonist activity at adrenergic beta2 receptor in electrically-stimulated Dunkin-Hartley guinea pig tracheal strip assessed as inhibition of contractionAgonist activity at adrenergic beta2 receptor in electrically-stimulated Dunkin-Hartley guinea pig tracheal strip assessed as inhibition of contraction
ChEMBL 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O 10.1016/j.bmcl.2014.06.014
DB05039 1986 62 None - 3 Guinea pig 8.1 pIC50 = 8.1 Binding
Agonist activity at adrenergic beta2 receptor in electrically-stimulated Dunkin-Hartley guinea pig tracheal strip assessed as inhibition of contractionAgonist activity at adrenergic beta2 receptor in electrically-stimulated Dunkin-Hartley guinea pig tracheal strip assessed as inhibition of contraction
ChEMBL 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O 10.1016/j.bmcl.2014.06.014
57400229 70030 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 497 12 5 7 3.5 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCOc3cccc(CNCCc4ccccc4F)c3)c2s1 10.1016/j.bmcl.2011.10.049
CHEMBL1945298 70030 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 497 12 5 7 3.5 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCOc3cccc(CNCCc4ccccc4F)c3)c2s1 10.1016/j.bmcl.2011.10.049
44268496 97910 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.
ChEMBL 542 13 6 7 3.3 CC(C)NC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/s0960-894x(98)00170-x
CHEMBL275291 97910 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.
ChEMBL 542 13 6 7 3.3 CC(C)NC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/s0960-894x(98)00170-x
44303192 201585 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Beta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindolol
ChEMBL 523 9 3 5 3.4 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(I)cc1 10.1016/s0960-894x(98)00571-x
CHEMBL64697 201585 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Beta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindolol
ChEMBL 523 9 3 5 3.4 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(I)cc1 10.1016/s0960-894x(98)00571-x
44461717 105187 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Binding affinity towards Beta-2 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindololBinding affinity towards Beta-2 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindolol
ChEMBL 577 15 3 8 4.6 CCCCCCn1c(C)cn(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)c1=O 10.1016/s0960-894x(99)00073-6
CHEMBL312546 105187 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Binding affinity towards Beta-2 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindololBinding affinity towards Beta-2 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindolol
ChEMBL 577 15 3 8 4.6 CCCCCCn1c(C)cn(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)c1=O 10.1016/s0960-894x(99)00073-6
44461716 203591 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Binding affinity towards Beta-2 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindololBinding affinity towards Beta-2 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindolol
ChEMBL 605 17 3 8 5.4 CCCCCCCCn1c(C)cn(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)c1=O 10.1016/s0960-894x(99)00073-6
CHEMBL79363 203591 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Binding affinity towards Beta-2 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindololBinding affinity towards Beta-2 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindolol
ChEMBL 605 17 3 8 5.4 CCCCCCCCn1c(C)cn(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)c1=O 10.1016/s0960-894x(99)00073-6
44298700 101463 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
In vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 345 3 1 3 2.5 CN(C)C(=O)N1CCc2cc(S(=O)(=O)Nc3ccccc3)ccc21 10.1016/s0960-894x(99)00277-2
CHEMBL301202 101463 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
In vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 345 3 1 3 2.5 CN(C)C(=O)N1CCc2cc(S(=O)(=O)Nc3ccccc3)ccc21 10.1016/s0960-894x(99)00277-2
97478 9821 96 None - 0 Dog 4.2 pIC50 = 4.2 Binding
Binding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprololBinding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprolol
ChEMBL 196 1 1 2 1.8 Clc1ccc(N2CCNCC2)cc1 10.1021/jm00082a016
CHEMBL114478 9821 96 None - 0 Dog 4.2 pIC50 = 4.2 Binding
Binding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprololBinding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprolol
ChEMBL 196 1 1 2 1.8 Clc1ccc(N2CCNCC2)cc1 10.1021/jm00082a016
44349645 113006 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cells
ChEMBL 684 11 4 9 6.8 N#CN/C(=N\c1ccc2c(c1)N(c1nc(-c3ccc(OC(F)(F)F)cc3)cs1)CC2)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/s0960-894x(00)00669-7
CHEMBL332132 113006 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cells
ChEMBL 684 11 4 9 6.8 N#CN/C(=N\c1ccc2c(c1)N(c1nc(-c3ccc(OC(F)(F)F)cc3)cs1)CC2)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/s0960-894x(00)00669-7
44313150 103288 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibitory activity against CHO cells expressing human Beta-2 adrenergic receptor with [125I]-iodocyanopindololInhibitory activity against CHO cells expressing human Beta-2 adrenergic receptor with [125I]-iodocyanopindolol
ChEMBL 628 12 6 6 6.7 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2cccc(-c3cccc(CC4NCCc5cc(O)c(O)cc54)c3)c2)cc1 10.1016/s0960-894x(00)00459-5
CHEMBL308868 103288 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibitory activity against CHO cells expressing human Beta-2 adrenergic receptor with [125I]-iodocyanopindololInhibitory activity against CHO cells expressing human Beta-2 adrenergic receptor with [125I]-iodocyanopindolol
ChEMBL 628 12 6 6 6.7 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2cccc(-c3cccc(CC4NCCc5cc(O)c(O)cc54)c3)c2)cc1 10.1016/s0960-894x(00)00459-5
9810596 16605 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Binding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cells
ChEMBL 734 11 4 9 8.0 N#CN/C(=N\c1ccc2c(c1)CCN2c1nc(-c2ccc(OC(F)(F)F)cc2)cs1)Nc1ccc2cc(CCNC[C@H](O)c3cccnc3)ccc2c1 10.1016/s0960-894x(00)00669-7
CHEMBL124597 16605 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Binding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cells
ChEMBL 734 11 4 9 8.0 N#CN/C(=N\c1ccc2c(c1)CCN2c1nc(-c2ccc(OC(F)(F)F)cc2)cs1)Nc1ccc2cc(CCNC[C@H](O)c3cccnc3)ccc2c1 10.1016/s0960-894x(00)00669-7
155527302 170651 0 None 1 2 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at human recombinant beta2 adrenoreceptor expressed in CHOK1 cells incubated for 30 mins by HTRFAntagonist activity at human recombinant beta2 adrenoreceptor expressed in CHOK1 cells incubated for 30 mins by HTRF
ChEMBL 355 12 2 6 2.3 COC(=O)CSCCCc1ccccc1OCC(O)CNC(C)C 10.1039/C8MD00412A
CHEMBL4459696 170651 0 None 1 2 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at human recombinant beta2 adrenoreceptor expressed in CHOK1 cells incubated for 30 mins by HTRFAntagonist activity at human recombinant beta2 adrenoreceptor expressed in CHOK1 cells incubated for 30 mins by HTRF
ChEMBL 355 12 2 6 2.3 COC(=O)CSCCCc1ccccc1OCC(O)CNC(C)C 10.1039/C8MD00412A
42629372 63301 0 None 52 2 Human 7.1 pIC50 = 7.1 Binding
Mitogenesis inhibition method: To measure beta2-AR mediated inhibition of mitogenesis, HEK-beta2-AR, 1321N1 or U87MG cells were seeded in a 96-well plate at approximately 5,000 cells/well. After 48 hours, the wells were rinsed twice and the medium was replaced with fresh medium containing 10 uL of drug in sterile water. After another 24 hours of incubation at 37° C., 0.25 uCi of [3H]-thymidine was added to each well. The cells were incubated for an additional 2 hours at 37° C., at which point 10 uL of 10x trypsin was added, and the resuspended cells were harvested using a Tomtec 96 harvester through glass fiber filters.Mitogenesis inhibition method: To measure beta2-AR mediated inhibition of mitogenesis, HEK-beta2-AR, 1321N1 or U87MG cells were seeded in a 96-well plate at approximately 5,000 cells/well. After 48 hours, the wells were rinsed twice and the medium was replaced with fresh medium containing 10 uL of drug in sterile water. After another 24 hours of incubation at 37° C., 0.25 uCi of [3H]-thymidine was added to each well. The cells were incubated for an additional 2 hours at 37° C., at which point 10 uL of 10x trypsin was added, and the resuspended cells were harvested using a Tomtec 96 harvester through glass fiber filters.
ChEMBL 337 6 4 4 3.5 C[C@@H](Cc1ccc2ccccc2c1)NC[C@H](O)c1cc(O)cc(O)c1 nan
CHEMBL1800962 63301 0 None 52 2 Human 7.1 pIC50 = 7.1 Binding
Mitogenesis inhibition method: To measure beta2-AR mediated inhibition of mitogenesis, HEK-beta2-AR, 1321N1 or U87MG cells were seeded in a 96-well plate at approximately 5,000 cells/well. After 48 hours, the wells were rinsed twice and the medium was replaced with fresh medium containing 10 uL of drug in sterile water. After another 24 hours of incubation at 37° C., 0.25 uCi of [3H]-thymidine was added to each well. The cells were incubated for an additional 2 hours at 37° C., at which point 10 uL of 10x trypsin was added, and the resuspended cells were harvested using a Tomtec 96 harvester through glass fiber filters.Mitogenesis inhibition method: To measure beta2-AR mediated inhibition of mitogenesis, HEK-beta2-AR, 1321N1 or U87MG cells were seeded in a 96-well plate at approximately 5,000 cells/well. After 48 hours, the wells were rinsed twice and the medium was replaced with fresh medium containing 10 uL of drug in sterile water. After another 24 hours of incubation at 37° C., 0.25 uCi of [3H]-thymidine was added to each well. The cells were incubated for an additional 2 hours at 37° C., at which point 10 uL of 10x trypsin was added, and the resuspended cells were harvested using a Tomtec 96 harvester through glass fiber filters.
ChEMBL 337 6 4 4 3.5 C[C@@H](Cc1ccc2ccccc2c1)NC[C@H](O)c1cc(O)cc(O)c1 nan
44281530 99346 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindolol
ChEMBL 609 12 3 8 4.8 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2noc(Cc3cc(F)c(F)c(F)c3)n2)cc1 10.1016/s0960-894x(00)00268-7
CHEMBL285499 99346 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindolol
ChEMBL 609 12 3 8 4.8 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2noc(Cc3cc(F)c(F)c(F)c3)n2)cc1 10.1016/s0960-894x(00)00268-7
44268570 97730 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.
ChEMBL 598 17 5 7 4.8 CCCCCCN(C)C(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/s0960-894x(98)00170-x
CHEMBL274144 97730 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-2 adrenergic receptor in the presence of [125I]iodocyanopindolol.
ChEMBL 598 17 5 7 4.8 CCCCCCN(C)C(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/s0960-894x(98)00170-x
12049925 98228 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity for clone human Beta-2 adrenergic receptor from CHO cell membranes in the presence of I-iodocyanopindololBinding affinity for clone human Beta-2 adrenergic receptor from CHO cell membranes in the presence of I-iodocyanopindolol
ChEMBL 638 13 3 9 4.9 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-n2ncc(COc3ccc(C(F)(F)F)cc3)n2)cc1 10.1016/s0960-894x(00)00422-4
CHEMBL277613 98228 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity for clone human Beta-2 adrenergic receptor from CHO cell membranes in the presence of I-iodocyanopindololBinding affinity for clone human Beta-2 adrenergic receptor from CHO cell membranes in the presence of I-iodocyanopindolol
ChEMBL 638 13 3 9 4.9 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-n2ncc(COc3ccc(C(F)(F)F)cc3)n2)cc1 10.1016/s0960-894x(00)00422-4
44377514 56205 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity towards Beta-2 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindololBinding affinity towards Beta-2 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindolol
ChEMBL 592 17 3 9 4.5 CCCCCCCCn1cnn(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)c1=O 10.1016/s0960-894x(99)00073-6
CHEMBL163579 56205 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity towards Beta-2 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindololBinding affinity towards Beta-2 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindolol
ChEMBL 592 17 3 9 4.5 CCCCCCCCn1cnn(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)c1=O 10.1016/s0960-894x(99)00073-6
44298761 193334 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
In vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 331 3 2 3 2.2 CNC(=O)N1CCc2cc(S(=O)(=O)Nc3ccccc3)ccc21 10.1016/s0960-894x(99)00277-2
CHEMBL54885 193334 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
In vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 331 3 2 3 2.2 CNC(=O)N1CCc2cc(S(=O)(=O)Nc3ccccc3)ccc21 10.1016/s0960-894x(99)00277-2
44307379 201942 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cell
ChEMBL 427 11 3 6 2.5 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2cccnc2)cc1)c1ccccc1 10.1016/s0960-894x(98)00381-3
CHEMBL67251 201942 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cell
ChEMBL 427 11 3 6 2.5 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2cccnc2)cc1)c1ccccc1 10.1016/s0960-894x(98)00381-3
44298290 167632 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 371 4 1 5 3.9 Cc1csc(N2CCc3cc(S(=O)(=O)Nc4ccccc4)ccc32)n1 10.1016/s0960-894x(99)00277-2
CHEMBL433454 167632 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 371 4 1 5 3.9 Cc1csc(N2CCc3cc(S(=O)(=O)Nc4ccccc4)ccc32)n1 10.1016/s0960-894x(99)00277-2
15483883 99755 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindolol
ChEMBL 589 13 3 9 4.5 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(COc3ccc(F)cc3)no2)cc1 10.1016/s0960-894x(00)00268-7
CHEMBL288550 99755 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindolol
ChEMBL 589 13 3 9 4.5 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(COc3ccc(F)cc3)no2)cc1 10.1016/s0960-894x(00)00268-7
44298822 193316 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
In vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 460 8 1 3 6.7 O=S(=O)(Nc1ccccc1)c1ccc2c(c1)CCN2c1cccc(CCCC2CCCC2)c1 10.1016/s0960-894x(99)00277-2
CHEMBL54750 193316 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
In vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 460 8 1 3 6.7 O=S(=O)(Nc1ccccc1)c1ccc2c(c1)CCN2c1cccc(CCCC2CCCC2)c1 10.1016/s0960-894x(99)00277-2
21138 97986 34 None -1 7 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 259 6 2 3 2.6 CC(C)NC[C@@H](O)COc1cccc2ccccc12 nan
CHEMBL275742 97986 34 None -1 7 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 259 6 2 3 2.6 CC(C)NC[C@@H](O)COc1cccc2ccccc12 nan
10054165 84338 1 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindololBinding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindolol
ChEMBL 591 14 3 6 5.0 O=C1N(CCCC2CCCC2)CCN1c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(99)00072-4
CHEMBL22317 84338 1 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindololBinding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindolol
ChEMBL 591 14 3 6 5.0 O=C1N(CCCC2CCCC2)CCN1c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(99)00072-4
44377754 119432 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindololBinding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindolol
ChEMBL 589 14 3 8 4.7 O=c1n(CCCC2CCCC2)ccn1-c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(99)00072-4
CHEMBL349651 119432 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindololBinding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindolol
ChEMBL 589 14 3 8 4.7 O=c1n(CCCC2CCCC2)ccn1-c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(99)00072-4
10651078 17745 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity was evaluated on chinese hamster ovary (CHO) cells expressing the cloned human beta-2 adrenergic receptor in the presence of [125I]- iodocyanopindolol.Binding affinity was evaluated on chinese hamster ovary (CHO) cells expressing the cloned human beta-2 adrenergic receptor in the presence of [125I]- iodocyanopindolol.
ChEMBL 592 11 3 7 5.8 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3cccc(F)c3F)cs2)cc1 10.1021/jm000286i
CHEMBL125963 17745 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity was evaluated on chinese hamster ovary (CHO) cells expressing the cloned human beta-2 adrenergic receptor in the presence of [125I]- iodocyanopindolol.Binding affinity was evaluated on chinese hamster ovary (CHO) cells expressing the cloned human beta-2 adrenergic receptor in the presence of [125I]- iodocyanopindolol.
ChEMBL 592 11 3 7 5.8 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3cccc(F)c3F)cs2)cc1 10.1021/jm000286i
44312924 164263 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibitory activity against CHO cells expressing human Beta-2 adrenergic receptor with [125I]-iodocyanopindololInhibitory activity against CHO cells expressing human Beta-2 adrenergic receptor with [125I]-iodocyanopindolol
ChEMBL 421 6 3 6 4.2 COc1cc(-c2ccc(CC3NCCc4cc(O)c(O)cc43)cc2)cc(OC)c1OC 10.1016/s0960-894x(00)00459-5
CHEMBL421871 164263 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibitory activity against CHO cells expressing human Beta-2 adrenergic receptor with [125I]-iodocyanopindololInhibitory activity against CHO cells expressing human Beta-2 adrenergic receptor with [125I]-iodocyanopindolol
ChEMBL 421 6 3 6 4.2 COc1cc(-c2ccc(CC3NCCc4cc(O)c(O)cc43)cc2)cc(OC)c1OC 10.1016/s0960-894x(00)00459-5
10054896 113627 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindolol
ChEMBL 639 13 3 9 5.3 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2noc(Cc3ccc(OC(F)(F)F)cc3)n2)cc1 10.1016/s0960-894x(00)00268-7
CHEMBL33292 113627 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindolol
ChEMBL 639 13 3 9 5.3 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2noc(Cc3ccc(OC(F)(F)F)cc3)n2)cc1 10.1016/s0960-894x(00)00268-7
12049920 102146 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity for clone human Beta-2 adrenergic receptor from CHO cell membranes in the presence of I-iodocyanopindololBinding affinity for clone human Beta-2 adrenergic receptor from CHO cell membranes in the presence of I-iodocyanopindolol
ChEMBL 572 12 3 8 4.1 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-n2ncc(Cc3ccc(F)cc3)n2)cc1 10.1016/s0960-894x(00)00422-4
CHEMBL304298 102146 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity for clone human Beta-2 adrenergic receptor from CHO cell membranes in the presence of I-iodocyanopindololBinding affinity for clone human Beta-2 adrenergic receptor from CHO cell membranes in the presence of I-iodocyanopindolol
ChEMBL 572 12 3 8 4.1 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-n2ncc(Cc3ccc(F)cc3)n2)cc1 10.1016/s0960-894x(00)00422-4
46881701 6771 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counter
ChEMBL 477 9 3 8 3.0 Cc1sc2ncn(CC(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)c(=O)c2c1C 10.1016/j.bmcl.2010.01.130
CHEMBL1084145 6771 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counter
ChEMBL 477 9 3 8 3.0 Cc1sc2ncn(CC(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)c(=O)c2c1C 10.1016/j.bmcl.2010.01.130
44338579 162739 0 None - 0 Guinea pig 6.1 pIC50 = 6.1 Binding
Beta-2 adrenergic receptor blocking was assessed from 50% inhibition of the isoproterenol submaximal response on isolated Guinea pig trachea(IT)Beta-2 adrenergic receptor blocking was assessed from 50% inhibition of the isoproterenol submaximal response on isolated Guinea pig trachea(IT)
ChEMBL 364 7 2 5 3.0 COC12CCCCC1c1ccc(F)cc1/C2=N/OCC(O)CNC(C)C 10.1021/jm00122a008
CHEMBL418819 162739 0 None - 0 Guinea pig 6.1 pIC50 = 6.1 Binding
Beta-2 adrenergic receptor blocking was assessed from 50% inhibition of the isoproterenol submaximal response on isolated Guinea pig trachea(IT)Beta-2 adrenergic receptor blocking was assessed from 50% inhibition of the isoproterenol submaximal response on isolated Guinea pig trachea(IT)
ChEMBL 364 7 2 5 3.0 COC12CCCCC1c1ccc(F)cc1/C2=N/OCC(O)CNC(C)C 10.1021/jm00122a008
44338132 109905 0 None - 0 Guinea pig 5.1 pIC50 = 5.1 Binding
Beta-2 adrenergic receptor blocking was assessed from 50% inhibition of the isoproterenol submaximal response on isolated Guinea pig trachea(IT)Beta-2 adrenergic receptor blocking was assessed from 50% inhibition of the isoproterenol submaximal response on isolated Guinea pig trachea(IT)
ChEMBL 404 8 3 6 3.0 CC(C)(C)NCC(O)CO/N=C1/c2ccccc2C2CCCCCC12OCCO 10.1021/jm00122a008
CHEMBL324412 109905 0 None - 0 Guinea pig 5.1 pIC50 = 5.1 Binding
Beta-2 adrenergic receptor blocking was assessed from 50% inhibition of the isoproterenol submaximal response on isolated Guinea pig trachea(IT)Beta-2 adrenergic receptor blocking was assessed from 50% inhibition of the isoproterenol submaximal response on isolated Guinea pig trachea(IT)
ChEMBL 404 8 3 6 3.0 CC(C)(C)NCC(O)CO/N=C1/c2ccccc2C2CCCCCC12OCCO 10.1021/jm00122a008
57393524 70142 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 538 12 3 6 5.8 CCN(Cc1ccncc1)Cc1cccc(-c2ccc(CCNCCc3ccc(O)c4[nH]c(=O)sc34)cc2)c1 10.1016/j.bmcl.2011.10.049
CHEMBL1946766 70142 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from recombinant beta2 adrenoceptor
ChEMBL 538 12 3 6 5.8 CCN(Cc1ccncc1)Cc1cccc(-c2ccc(CCNCCc3ccc(O)c4[nH]c(=O)sc34)cc2)c1 10.1016/j.bmcl.2011.10.049
9799092 47027 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Receptor binding assay(Beta-2 adrenergic receptor) carried out with membranes prepared from human recombinant Sf9 cells expressing the cloned human receptor in the presence of [125I]iodocyanopindololReceptor binding assay(Beta-2 adrenergic receptor) carried out with membranes prepared from human recombinant Sf9 cells expressing the cloned human receptor in the presence of [125I]iodocyanopindolol
ChEMBL 362 9 4 4 3.1 C[C@H](CNc1ccc(CC(=O)O)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0101500
CHEMBL154419 47027 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Receptor binding assay(Beta-2 adrenergic receptor) carried out with membranes prepared from human recombinant Sf9 cells expressing the cloned human receptor in the presence of [125I]iodocyanopindololReceptor binding assay(Beta-2 adrenergic receptor) carried out with membranes prepared from human recombinant Sf9 cells expressing the cloned human receptor in the presence of [125I]iodocyanopindolol
ChEMBL 362 9 4 4 3.1 C[C@H](CNc1ccc(CC(=O)O)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0101500
21435491 69844 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [3H]dihydroalprenolol from beta2-adrenoceptor after 90 mins by liquid scintillation countingDisplacement of [3H]dihydroalprenolol from beta2-adrenoceptor after 90 mins by liquid scintillation counting
ChEMBL 448 15 8 8 1.6 OCc1cc(C(O)CNCCCCCCNCC(O)c2ccc(O)c(CO)c2)ccc1O 10.1016/j.bmcl.2011.11.072
CHEMBL1940683 69844 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [3H]dihydroalprenolol from beta2-adrenoceptor after 90 mins by liquid scintillation countingDisplacement of [3H]dihydroalprenolol from beta2-adrenoceptor after 90 mins by liquid scintillation counting
ChEMBL 448 15 8 8 1.6 OCc1cc(C(O)CNCCCCCCNCC(O)c2ccc(O)c(CO)c2)ccc1O 10.1016/j.bmcl.2011.11.072
54590925 152767 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 μg/well for beta1 and 5 μg/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 μl, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 μM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 μg/well for beta1 and 5 μg/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 μl, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 μM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.
ChEMBL 794 15 6 12 5.9 COc1cc(NC(=O)CCN(C)[C@H]2CC[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3978112 152767 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 μg/well for beta1 and 5 μg/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 μl, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 μM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 μg/well for beta1 and 5 μg/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 μl, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 μM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.
ChEMBL 794 15 6 12 5.9 COc1cc(NC(=O)CCN(C)[C@H]2CC[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
118710950 113250 0 None - 3 Guinea pig 8.1 pIC50 = 8.1 Binding
Agonist activity at adrenergic beta2 receptor in electrically-stimulated Dunkin-Hartley guinea pig tracheal strip assessed as inhibition of contractionAgonist activity at adrenergic beta2 receptor in electrically-stimulated Dunkin-Hartley guinea pig tracheal strip assessed as inhibition of contraction
ChEMBL 402 10 4 6 3.3 CCCCOc1cccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)c1 10.1016/j.bmcl.2014.06.014
CHEMBL3323670 113250 0 None - 3 Guinea pig 8.1 pIC50 = 8.1 Binding
Agonist activity at adrenergic beta2 receptor in electrically-stimulated Dunkin-Hartley guinea pig tracheal strip assessed as inhibition of contractionAgonist activity at adrenergic beta2 receptor in electrically-stimulated Dunkin-Hartley guinea pig tracheal strip assessed as inhibition of contraction
ChEMBL 402 10 4 6 3.3 CCCCOc1cccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)c1 10.1016/j.bmcl.2014.06.014
44335618 4704 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Beta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindolol
ChEMBL 497 12 5 6 3.3 CCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(98)00571-x
CHEMBL104061 4704 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Beta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindolol
ChEMBL 497 12 5 6 3.3 CCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(98)00571-x
44335497 4739 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Beta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindolol
ChEMBL 397 9 3 5 2.7 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccccc1 10.1016/s0960-894x(98)00571-x
CHEMBL104180 4739 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Beta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindolol
ChEMBL 397 9 3 5 2.7 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccccc1 10.1016/s0960-894x(98)00571-x
44335882 4820 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Beta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindolol
ChEMBL 425 11 3 5 2.9 O=S(=O)(CCc1ccccc1)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/s0960-894x(98)00571-x
CHEMBL104551 4820 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Beta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindolol
ChEMBL 425 11 3 5 2.9 O=S(=O)(CCc1ccccc1)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/s0960-894x(98)00571-x
44335560 5228 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Beta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindolol
ChEMBL 469 10 5 6 2.5 CNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(98)00571-x
CHEMBL106746 5228 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Beta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindolol
ChEMBL 469 10 5 6 2.5 CNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(98)00571-x
44301806 100240 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindololBinding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindolol
ChEMBL 607 11 3 8 6.1 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3ccc4ncccc4c3)cs2)cc1 10.1016/s0960-894x(00)00390-5
CHEMBL292598 100240 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindololBinding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindolol
ChEMBL 607 11 3 8 6.1 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3ccc4ncccc4c3)cs2)cc1 10.1016/s0960-894x(00)00390-5
44281343 109867 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindolol
ChEMBL 639 14 3 13 5.2 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2noc(COc3ccc(C4N=NN=N4)cc3)n2)cc1 10.1016/s0960-894x(00)00268-7
CHEMBL32418 109867 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindolol
ChEMBL 639 14 3 13 5.2 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2noc(COc3ccc(C4N=NN=N4)cc3)n2)cc1 10.1016/s0960-894x(00)00268-7
44298281 193051 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
In vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 463 6 1 3 4.9 CN(C(=O)N1CCc2cc(S(=O)(=O)Nc3ccccc3)ccc21)C(C)(C)Cc1ccccc1 10.1016/s0960-894x(99)00277-2
CHEMBL53517 193051 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
In vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 463 6 1 3 4.9 CN(C(=O)N1CCc2cc(S(=O)(=O)Nc3ccccc3)ccc21)C(C)(C)Cc1ccccc1 10.1016/s0960-894x(99)00277-2
105 3392 84 None -10 6 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O nan
2083 3392 84 None -10 6 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O nan
558 3392 84 None -10 6 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O nan
CHEMBL714 3392 84 None -10 6 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O nan
DB01001 3392 84 None -10 6 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O nan
44335663 4707 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Beta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindolol
ChEMBL 560 13 4 7 4.5 O=C(Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1)OCCc1ccccc1 10.1016/s0960-894x(98)00571-x
CHEMBL104076 4707 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Beta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindolol
ChEMBL 560 13 4 7 4.5 O=C(Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1)OCCc1ccccc1 10.1016/s0960-894x(98)00571-x
155552760 173527 0 None -2 2 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at human recombinant beta2 adrenoreceptor expressed in CHOK1 cells incubated for 30 mins by HTRFAntagonist activity at human recombinant beta2 adrenoreceptor expressed in CHOK1 cells incubated for 30 mins by HTRF
ChEMBL 548 24 4 10 -0.2 C=CCc1ccccc1OCC(O)CNCCOCCOCCOCCOCCNC(=O)CS(=O)(=O)O 10.1039/C8MD00412A
CHEMBL4545079 173527 0 None -2 2 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at human recombinant beta2 adrenoreceptor expressed in CHOK1 cells incubated for 30 mins by HTRFAntagonist activity at human recombinant beta2 adrenoreceptor expressed in CHOK1 cells incubated for 30 mins by HTRF
ChEMBL 548 24 4 10 -0.2 C=CCc1ccccc1OCC(O)CNCCOCCOCCOCCOCCNC(=O)CS(=O)(=O)O 10.1039/C8MD00412A
44268266 17809 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandBinding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligand
ChEMBL 317 8 4 5 2.1 C[C@@H](Cc1ccc(O)cc1)NC[C@H](O)COc1ccc(O)cc1 10.1016/s0960-894x(98)00169-3
CHEMBL12633 17809 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandBinding affinity against cloned human beta-2 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligand
ChEMBL 317 8 4 5 2.1 C[C@@H](Cc1ccc(O)cc1)NC[C@H](O)COc1ccc(O)cc1 10.1016/s0960-894x(98)00169-3
40424734 166048 1 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [3H]-CGP-12177 from human beta2-adrenergic receptorDisplacement of [3H]-CGP-12177 from human beta2-adrenergic receptor
ChEMBL 301 8 2 4 2.6 COc1ccc(CCNC[C@H](O)c2ccccc2)cc1OC 10.1039/C7MD00656J
CHEMBL4280606 166048 1 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [3H]-CGP-12177 from human beta2-adrenergic receptorDisplacement of [3H]-CGP-12177 from human beta2-adrenergic receptor
ChEMBL 301 8 2 4 2.6 COc1ccc(CCNC[C@H](O)c2ccccc2)cc1OC 10.1039/C7MD00656J
76336501 105434 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]-cyanopindolol from recombinant human beta-2 adrenergic receptor expressed in CHO cell membranes after 1 hr by scintillation counting analysisDisplacement of [125I]-cyanopindolol from recombinant human beta-2 adrenergic receptor expressed in CHO cell membranes after 1 hr by scintillation counting analysis
ChEMBL 482 6 4 6 4.4 Nc1nc2c(s1)CC[C@H]2C(=O)Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3cccc(Cl)c3)N2)cc1 10.1021/jm4017224
CHEMBL3128198 105434 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]-cyanopindolol from recombinant human beta-2 adrenergic receptor expressed in CHO cell membranes after 1 hr by scintillation counting analysisDisplacement of [125I]-cyanopindolol from recombinant human beta-2 adrenergic receptor expressed in CHO cell membranes after 1 hr by scintillation counting analysis
ChEMBL 482 6 4 6 4.4 Nc1nc2c(s1)CC[C@H]2C(=O)Nc1ccc(C[C@@H]2CC[C@H]([C@H](O)c3cccc(Cl)c3)N2)cc1 10.1021/jm4017224
44461485 106447 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity towards Beta-2 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindololBinding affinity towards Beta-2 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindolol
ChEMBL 564 15 3 9 3.7 CCCCCCn1ncn(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)c1=O 10.1016/s0960-894x(99)00073-6
CHEMBL314893 106447 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity towards Beta-2 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindololBinding affinity towards Beta-2 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindolol
ChEMBL 564 15 3 9 3.7 CCCCCCn1ncn(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)c1=O 10.1016/s0960-894x(99)00073-6
44280795 112072 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity towards Beta-2 adrenergic receptor prepared from CHO cells expressing the cloned human receptor in the presence of [125I]iodocyanopindololBinding affinity towards Beta-2 adrenergic receptor prepared from CHO cells expressing the cloned human receptor in the presence of [125I]iodocyanopindolol
ChEMBL 507 12 3 8 3.8 CCCc1nc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)no1 10.1016/s0960-894x(00)00267-5
CHEMBL33013 112072 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity towards Beta-2 adrenergic receptor prepared from CHO cells expressing the cloned human receptor in the presence of [125I]iodocyanopindololBinding affinity towards Beta-2 adrenergic receptor prepared from CHO cells expressing the cloned human receptor in the presence of [125I]iodocyanopindolol
ChEMBL 507 12 3 8 3.8 CCCc1nc(-c2ccc(S(=O)(=O)Nc3ccc(CCNC[C@H](O)c4cccnc4)cc3)cc2)no1 10.1016/s0960-894x(00)00267-5
155537995 171759 0 None 109 2 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at human recombinant beta2 adrenoreceptor expressed in CHOK1 cells incubated for 30 mins by HTRFAntagonist activity at human recombinant beta2 adrenoreceptor expressed in CHOK1 cells incubated for 30 mins by HTRF
ChEMBL 593 23 5 10 0.2 CC(C)NCC(O)COc1ccccc1CCCSCC(=O)NCCOCCOCCNC(=O)CS(=O)(=O)O 10.1039/C8MD00412A
CHEMBL4475573 171759 0 None 109 2 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at human recombinant beta2 adrenoreceptor expressed in CHOK1 cells incubated for 30 mins by HTRFAntagonist activity at human recombinant beta2 adrenoreceptor expressed in CHOK1 cells incubated for 30 mins by HTRF
ChEMBL 593 23 5 10 0.2 CC(C)NCC(O)COc1ccccc1CCCSCC(=O)NCCOCCOCCNC(=O)CS(=O)(=O)O 10.1039/C8MD00412A
12049922 102255 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity for clone human Beta-2 adrenergic receptor from CHO cell membranes in the presence of I-iodocyanopindololBinding affinity for clone human Beta-2 adrenergic receptor from CHO cell membranes in the presence of I-iodocyanopindolol
ChEMBL 638 13 3 9 4.8 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-n2ncc(Cc3ccc(OC(F)(F)F)cc3)n2)cc1 10.1016/s0960-894x(00)00422-4
CHEMBL304991 102255 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity for clone human Beta-2 adrenergic receptor from CHO cell membranes in the presence of I-iodocyanopindololBinding affinity for clone human Beta-2 adrenergic receptor from CHO cell membranes in the presence of I-iodocyanopindolol
ChEMBL 638 13 3 9 4.8 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-n2ncc(Cc3ccc(OC(F)(F)F)cc3)n2)cc1 10.1016/s0960-894x(00)00422-4
46881617 7846 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counter
ChEMBL 397 9 4 7 2.2 Nc1nc(CC(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cs1 10.1016/j.bmcl.2010.01.130
CHEMBL1090425 7846 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counter
ChEMBL 397 9 4 7 2.2 Nc1nc(CC(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cs1 10.1016/j.bmcl.2010.01.130
12049914 201890 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity for clone human Beta-2 adrenergic receptor from CHO cell membranes in the presence of I-iodocyanopindololBinding affinity for clone human Beta-2 adrenergic receptor from CHO cell membranes in the presence of I-iodocyanopindolol
ChEMBL 558 11 3 8 4.1 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-n2ncc(-c3cccc(F)c3)n2)cc1 10.1016/s0960-894x(00)00422-4
CHEMBL66908 201890 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity for clone human Beta-2 adrenergic receptor from CHO cell membranes in the presence of I-iodocyanopindololBinding affinity for clone human Beta-2 adrenergic receptor from CHO cell membranes in the presence of I-iodocyanopindolol
ChEMBL 558 11 3 8 4.1 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-n2ncc(-c3cccc(F)c3)n2)cc1 10.1016/s0960-894x(00)00422-4
12049923 201967 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity for clone human Beta-2 adrenergic receptor from CHO cell membranes in the presence of I-iodocyanopindololBinding affinity for clone human Beta-2 adrenergic receptor from CHO cell membranes in the presence of I-iodocyanopindolol
ChEMBL 608 12 3 8 4.3 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-n2ncc(Cc3c(F)cc(F)cc3F)n2)cc1 10.1016/s0960-894x(00)00422-4
CHEMBL67404 201967 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity for clone human Beta-2 adrenergic receptor from CHO cell membranes in the presence of I-iodocyanopindololBinding affinity for clone human Beta-2 adrenergic receptor from CHO cell membranes in the presence of I-iodocyanopindolol
ChEMBL 608 12 3 8 4.3 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-n2ncc(Cc3c(F)cc(F)cc3F)n2)cc1 10.1016/s0960-894x(00)00422-4
54673357 145068 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 μg/well for beta1 and 5 μg/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 μl, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 μM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 μg/well for beta1 and 5 μg/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 μl, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 μM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.
ChEMBL 795 17 5 12 6.7 COc1cc(OCCCCN(C)[C@H]2CC[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3915601 145068 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 μg/well for beta1 and 5 μg/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 μl, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 μM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.Adrenergic Receptor Binding Assay: The study of binding to human adrenergic beta1 and beta2 receptors was performed using commercial membranes prepared from Sf9 cells where they are overexpressed (Perkin Elmer). The membrane suspensions (16 μg/well for beta1 and 5 μg/well for beta2) in assay buffer (75 mM Tris/HCl with 12.5 mM MgCl2 and 2 mM EDTA pH=7.4) were incubated with 0.14 or 0.6 nM of 3H-CGP12177 (Amersham) for beta 1 and beta 2 receptors respectively in a final volume of 250 μl, in GFC Multiscreen 96 well plates (Millipore) previously treated with assay buffer containing 0.3% PEI (Sigma). Non specific binding was measured in the presence of 1 μM propanolol. Incubation was maintained for 60 minutes at room temperature and with gentle shaking. The binding reactions were terminated by filtration and washing with 2.5 volumes of Tris/HCl 50 mM pH=7.4.
ChEMBL 795 17 5 12 6.7 COc1cc(OCCCCN(C)[C@H]2CC[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
44307065 201632 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cell
ChEMBL 445 11 3 6 2.6 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2cccnc2)cc1)c1ccc(F)cc1 10.1016/s0960-894x(98)00381-3
CHEMBL64932 201632 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cell
ChEMBL 445 11 3 6 2.6 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2cccnc2)cc1)c1ccc(F)cc1 10.1016/s0960-894x(98)00381-3
44298516 193906 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 467 8 1 5 6.2 O=S(=O)(Nc1ccccc1)c1ccc2c(c1)CCN2c1nc(CCCC2CCCC2)cs1 10.1016/s0960-894x(99)00277-2
CHEMBL55541 193906 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-2 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cells
ChEMBL 467 8 1 5 6.2 O=S(=O)(Nc1ccccc1)c1ccc2c(c1)CCN2c1nc(CCCC2CCCC2)cs1 10.1016/s0960-894x(99)00277-2
44335588 5186 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Beta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindolol
ChEMBL 496 13 4 6 3.9 CCCCC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(98)00571-x
CHEMBL106487 5186 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Beta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-2 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindolol
ChEMBL 496 13 4 6 3.9 CCCCC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(98)00571-x
44461719 204139 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindololBinding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindolol
ChEMBL 641 14 3 6 5.0 O=C1N(CCCC(F)(F)C(F)(F)F)CCN1c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(99)00072-4
CHEMBL83754 204139 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindololBinding affinity towards human Beta-2 adrenergic receptor expressed in CHO cells, using [125I]iodocyanopindolol
ChEMBL 641 14 3 6 5.0 O=C1N(CCCC(F)(F)C(F)(F)F)CCN1c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(99)00072-4
12017013 135745 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.
ChEMBL 588 13 3 8 5.1 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2coc(COc3ccc(F)cc3)n2)cc1 10.1016/s0960-894x(00)00277-8
CHEMBL37335 135745 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.
ChEMBL 588 13 3 8 5.1 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2coc(COc3ccc(F)cc3)n2)cc1 10.1016/s0960-894x(00)00277-8
44301617 197028 0 None - 0 Human 4.1 pIC50 = 4.1 Binding
Binding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindololBinding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindolol
ChEMBL 640 16 3 7 7.7 CCCCCCc1ccc(-c2csc(-c3ccc(S(=O)(=O)Nc4ccc(CCNC[C@H](O)c5cccnc5)cc4)cc3)n2)cc1 10.1016/s0960-894x(00)00390-5
CHEMBL58241 197028 0 None - 0 Human 4.1 pIC50 = 4.1 Binding
Binding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindololBinding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindolol
ChEMBL 640 16 3 7 7.7 CCCCCCc1ccc(-c2csc(-c3ccc(S(=O)(=O)Nc4ccc(CCNC[C@H](O)c5cccnc5)cc4)cc3)n2)cc1 10.1016/s0960-894x(00)00390-5
44281372 99643 0 None - 0 Human 4.1 pIC50 = 4.1 Binding
Binding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindolol
ChEMBL 621 13 3 9 5.5 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2noc(COc3ccc4ccccc4c3)n2)cc1 10.1016/s0960-894x(00)00268-7
CHEMBL287562 99643 0 None - 0 Human 4.1 pIC50 = 4.1 Binding
Binding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindolol
ChEMBL 621 13 3 9 5.5 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2noc(COc3ccc4ccccc4c3)n2)cc1 10.1016/s0960-894x(00)00268-7
44301843 197917 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindololBinding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindolol
ChEMBL 584 13 3 7 5.7 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(CCc3ccccc3)cs2)cc1 10.1016/s0960-894x(00)00390-5
CHEMBL59270 197917 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindololBinding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindolol
ChEMBL 584 13 3 7 5.7 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(CCc3ccccc3)cs2)cc1 10.1016/s0960-894x(00)00390-5
10416656 18407 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cells
ChEMBL 636 16 4 8 7.2 CCCCCCCCc1csc(N2CCc3c(N/C(=N/c4ccc(CCNC[C@H](O)c5cccnc5)cc4)NC#N)cccc32)n1 10.1016/s0960-894x(00)00669-7
CHEMBL127656 18407 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity to the human beta-2 adrenergic receptor assayed using [125I]iodocyanopindolol as radioligand in CHO cells
ChEMBL 636 16 4 8 7.2 CCCCCCCCc1csc(N2CCc3c(N/C(=N/c4ccc(CCNC[C@H](O)c5cccnc5)cc4)NC#N)cccc32)n1 10.1016/s0960-894x(00)00669-7
12049915 102353 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Binding affinity for clone human Beta-2 adrenergic receptor from CHO cell membranes in the presence of I-iodocyanopindololBinding affinity for clone human Beta-2 adrenergic receptor from CHO cell membranes in the presence of I-iodocyanopindolol
ChEMBL 558 11 3 8 4.1 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-n2ncc(-c3ccc(F)cc3)n2)cc1 10.1016/s0960-894x(00)00422-4
CHEMBL305558 102353 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Binding affinity for clone human Beta-2 adrenergic receptor from CHO cell membranes in the presence of I-iodocyanopindololBinding affinity for clone human Beta-2 adrenergic receptor from CHO cell membranes in the presence of I-iodocyanopindolol
ChEMBL 558 11 3 8 4.1 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-n2ncc(-c3ccc(F)cc3)n2)cc1 10.1016/s0960-894x(00)00422-4
44301881 100056 0 None - 0 Human 4.0 pIC50 = 4.0 Binding
Binding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindololBinding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindolol
ChEMBL 612 11 3 8 6.8 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3cc4ccccc4s3)cs2)cc1 10.1016/s0960-894x(00)00390-5
CHEMBL291306 100056 0 None - 0 Human 4.0 pIC50 = 4.0 Binding
Binding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindololBinding affinity against human Beta-2 adrenergic receptor expressed in CHO cells using [125I]iodocyanopindolol
ChEMBL 612 11 3 8 6.8 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3cc4ccccc4s3)cs2)cc1 10.1016/s0960-894x(00)00390-5
44307186 202063 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cell
ChEMBL 455 12 3 6 3.0 CCc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3cccnc3)cc2)cc1 10.1016/s0960-894x(98)00381-3
CHEMBL68021 202063 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cell
ChEMBL 455 12 3 6 3.0 CCc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)COc3cccnc3)cc2)cc1 10.1016/s0960-894x(98)00381-3
12017014 99836 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.
ChEMBL 608 12 3 7 5.4 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2cnc(Cc3cc(F)c(F)c(F)c3)o2)cc1 10.1016/s0960-894x(00)00277-8
CHEMBL289316 99836 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-2 adrenergic receptors in the presence of [125I]iodocyanopindolol.
ChEMBL 608 12 3 7 5.4 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2cnc(Cc3cc(F)c(F)c(F)c3)o2)cc1 10.1016/s0960-894x(00)00277-8
44281344 99369 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Binding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindolol
ChEMBL 628 14 4 10 4.3 CC(=O)Nc1ccc(OCc2nc(-c3ccc(S(=O)(=O)Nc4ccc(CCNC[C@H](O)c5cccnc5)cc4)cc3)no2)cc1 10.1016/s0960-894x(00)00268-7
CHEMBL285704 99369 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Binding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindolol
ChEMBL 628 14 4 10 4.3 CC(=O)Nc1ccc(OCc2nc(-c3ccc(S(=O)(=O)Nc4ccc(CCNC[C@H](O)c5cccnc5)cc4)cc3)no2)cc1 10.1016/s0960-894x(00)00268-7
44281531 100043 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Binding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindolol
ChEMBL 601 13 3 9 5.1 CSc1ccc(Cc2nc(-c3ccc(S(=O)(=O)Nc4ccc(CCNC[C@H](O)c5cccnc5)cc4)cc3)no2)cc1 10.1016/s0960-894x(00)00268-7
CHEMBL291246 100043 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Binding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindolol
ChEMBL 601 13 3 9 5.1 CSc1ccc(Cc2nc(-c3ccc(S(=O)(=O)Nc4ccc(CCNC[C@H](O)c5cccnc5)cc4)cc3)no2)cc1 10.1016/s0960-894x(00)00268-7
155521599 170157 0 None 10 2 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity at human recombinant beta2 adrenoreceptor expressed in CHOK1 cells incubated for 30 mins by HTRFAntagonist activity at human recombinant beta2 adrenoreceptor expressed in CHOK1 cells incubated for 30 mins by HTRF
ChEMBL 1311 40 7 18 5.9 CC(C)NCC(O)COc1ccccc1CCCSCC(=O)NCCOCCOCCNC(=O)CCCCCC1(C)C(/C=C/C=C/C=C2/N(CCCS(=O)(=O)O)c3ccc(S(=O)(=O)O)cc3C2(C)C)=[N+](CCCS(=O)(=O)[O-])c2ccc(S(=O)(=O)O)cc21 10.1039/C8MD00412A
CHEMBL4452249 170157 0 None 10 2 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity at human recombinant beta2 adrenoreceptor expressed in CHOK1 cells incubated for 30 mins by HTRFAntagonist activity at human recombinant beta2 adrenoreceptor expressed in CHOK1 cells incubated for 30 mins by HTRF
ChEMBL 1311 40 7 18 5.9 CC(C)NCC(O)COc1ccccc1CCCSCC(=O)NCCOCCOCCNC(=O)CCCCCC1(C)C(/C=C/C=C/C=C2/N(CCCS(=O)(=O)O)c3ccc(S(=O)(=O)O)cc3C2(C)C)=[N+](CCCS(=O)(=O)[O-])c2ccc(S(=O)(=O)O)cc21 10.1039/C8MD00412A
12043156 167575 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity towards Beta-2 adrenergic receptor prepared from CHO cells expressing the cloned human receptor in the presence of [125I]iodocyanopindololBinding affinity towards Beta-2 adrenergic receptor prepared from CHO cells expressing the cloned human receptor in the presence of [125I]iodocyanopindolol
ChEMBL 575 14 3 8 5.3 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2noc(CCCC3CCCC3)n2)cc1 10.1016/s0960-894x(00)00267-5
CHEMBL433042 167575 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity towards Beta-2 adrenergic receptor prepared from CHO cells expressing the cloned human receptor in the presence of [125I]iodocyanopindololBinding affinity towards Beta-2 adrenergic receptor prepared from CHO cells expressing the cloned human receptor in the presence of [125I]iodocyanopindolol
ChEMBL 575 14 3 8 5.3 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2noc(CCCC3CCCC3)n2)cc1 10.1016/s0960-894x(00)00267-5
10012704 11102 0 None - 2 Guinea pig 6.0 pIC50 = 6.0 Binding
Inhibitory concentration against beta-2-adrenergic receptor in isolated guinea pig tracheal stripsInhibitory concentration against beta-2-adrenergic receptor in isolated guinea pig tracheal strips
ChEMBL 188 5 2 4 0.8 CCO/N=C/C(O)CNC(C)(C)C 10.1021/jm00036a018
CHEMBL1178768 11102 0 None - 2 Guinea pig 6.0 pIC50 = 6.0 Binding
Inhibitory concentration against beta-2-adrenergic receptor in isolated guinea pig tracheal stripsInhibitory concentration against beta-2-adrenergic receptor in isolated guinea pig tracheal strips
ChEMBL 188 5 2 4 0.8 CCO/N=C/C(O)CNC(C)(C)C 10.1021/jm00036a018
CHEMBL39987 11102 0 None - 2 Guinea pig 6.0 pIC50 = 6.0 Binding
Inhibitory concentration against beta-2-adrenergic receptor in isolated guinea pig tracheal stripsInhibitory concentration against beta-2-adrenergic receptor in isolated guinea pig tracheal strips
ChEMBL 188 5 2 4 0.8 CCO/N=C/C(O)CNC(C)(C)C 10.1021/jm00036a018
5806 102690 16 None - 3 Guinea pig 6.0 pIC50 = 6.0 Binding
Inhibitory concentration against beta-2-adrenergic receptor in isolated guinea pig tracheal stripsInhibitory concentration against beta-2-adrenergic receptor in isolated guinea pig tracheal strips
ChEMBL 247 4 2 2 3.0 CC(C)NCC(O)c1ccc(Cl)c(Cl)c1 10.1021/jm00036a018
CHEMBL30816 102690 16 None - 3 Guinea pig 6.0 pIC50 = 6.0 Binding
Inhibitory concentration against beta-2-adrenergic receptor in isolated guinea pig tracheal stripsInhibitory concentration against beta-2-adrenergic receptor in isolated guinea pig tracheal strips
ChEMBL 247 4 2 2 3.0 CC(C)NCC(O)c1ccc(Cl)c(Cl)c1 10.1021/jm00036a018
10371216 99273 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindolol
ChEMBL 591 12 3 8 4.7 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2noc(Cc3ccc(F)c(F)c3)n2)cc1 10.1016/s0960-894x(00)00268-7
CHEMBL285001 99273 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-2 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindolol
ChEMBL 591 12 3 8 4.7 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2noc(Cc3ccc(F)c(F)c3)n2)cc1 10.1016/s0960-894x(00)00268-7
10627736 116482 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity was evaluated on chinese hamster ovary (CHO) cells expressing the cloned human beta-2 adrenergic receptor in the presence of [125I]- iodocyanopindolol.Binding affinity was evaluated on chinese hamster ovary (CHO) cells expressing the cloned human beta-2 adrenergic receptor in the presence of [125I]- iodocyanopindolol.
ChEMBL 624 11 3 7 6.6 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3cccc(C(F)(F)F)c3)cs2)cc1 10.1021/jm000286i
CHEMBL338794 116482 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity was evaluated on chinese hamster ovary (CHO) cells expressing the cloned human beta-2 adrenergic receptor in the presence of [125I]- iodocyanopindolol.Binding affinity was evaluated on chinese hamster ovary (CHO) cells expressing the cloned human beta-2 adrenergic receptor in the presence of [125I]- iodocyanopindolol.
ChEMBL 624 11 3 7 6.6 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3cccc(C(F)(F)F)c3)cs2)cc1 10.1021/jm000286i
105 3392 84 None -10 6 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]CGP1217 from human recombinant adrenergic beta2 receptor transfected in insect Sf9 cells by scintillation countingDisplacement of [3H]CGP1217 from human recombinant adrenergic beta2 receptor transfected in insect Sf9 cells by scintillation counting
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1021/jm801211c
2083 3392 84 None -10 6 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]CGP1217 from human recombinant adrenergic beta2 receptor transfected in insect Sf9 cells by scintillation countingDisplacement of [3H]CGP1217 from human recombinant adrenergic beta2 receptor transfected in insect Sf9 cells by scintillation counting
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1021/jm801211c
558 3392 84 None -10 6 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]CGP1217 from human recombinant adrenergic beta2 receptor transfected in insect Sf9 cells by scintillation countingDisplacement of [3H]CGP1217 from human recombinant adrenergic beta2 receptor transfected in insect Sf9 cells by scintillation counting
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1021/jm801211c
CHEMBL714 3392 84 None -10 6 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]CGP1217 from human recombinant adrenergic beta2 receptor transfected in insect Sf9 cells by scintillation countingDisplacement of [3H]CGP1217 from human recombinant adrenergic beta2 receptor transfected in insect Sf9 cells by scintillation counting
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1021/jm801211c
DB01001 3392 84 None -10 6 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]CGP1217 from human recombinant adrenergic beta2 receptor transfected in insect Sf9 cells by scintillation countingDisplacement of [3H]CGP1217 from human recombinant adrenergic beta2 receptor transfected in insect Sf9 cells by scintillation counting
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1021/jm801211c
44306979 201991 0 None - 0 Human 6.0 pIC50 = 6 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cell
ChEMBL 476 11 4 7 2.7 Nc1ccc(OC[C@@H](O)CNCCc2ccc(NS(=O)(=O)c3ccc(Cl)cc3)cc2)cn1 10.1016/s0960-894x(98)00381-3
CHEMBL67534 201991 0 None - 0 Human 6.0 pIC50 = 6 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-2 adrenergic receptor in membranes from chinese hamster ovary cell
ChEMBL 476 11 4 7 2.7 Nc1ccc(OC[C@@H](O)CNCCc2ccc(NS(=O)(=O)c3ccc(Cl)cc3)cc2)cn1 10.1016/s0960-894x(98)00381-3
44313161 103286 0 None - 0 Human 6.0 pIC50 = 6 Binding
Inhibitory activity against CHO cells expressing human Beta-2 adrenergic receptor with [125I]-iodocyanopindololInhibitory activity against CHO cells expressing human Beta-2 adrenergic receptor with [125I]-iodocyanopindolol
ChEMBL 644 13 6 7 6.5 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2cccc(-c3ccc(OCC4NCCc5cc(O)c(O)cc54)cc3)c2)cc1 10.1016/s0960-894x(00)00459-5
CHEMBL308860 103286 0 None - 0 Human 6.0 pIC50 = 6 Binding
Inhibitory activity against CHO cells expressing human Beta-2 adrenergic receptor with [125I]-iodocyanopindololInhibitory activity against CHO cells expressing human Beta-2 adrenergic receptor with [125I]-iodocyanopindolol
ChEMBL 644 13 6 7 6.5 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2cccc(-c3ccc(OCC4NCCc5cc(O)c(O)cc54)cc3)c2)cc1 10.1016/s0960-894x(00)00459-5
65691 77787 17 None - 1 Human 10.5 pKd = 10.5 Binding
Displacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting methodDisplacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting method
ChEMBL 299 6 2 3 3.5 CC(C)(C)NCC(O)COc1ccccc1-c1ccccc1 10.1021/acsmedchemlett.6b00363
CHEMBL2104145 77787 17 None - 1 Human 10.5 pKd = 10.5 Binding
Displacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting methodDisplacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting method
ChEMBL 299 6 2 3 3.5 CC(C)(C)NCC(O)COc1ccccc1-c1ccccc1 10.1021/acsmedchemlett.6b00363
25271869 158073 2 None 38 2 Human 10.5 pKd = 10.5 Binding
Displacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting methodDisplacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting method
ChEMBL 299 6 2 3 3.5 CC(C)(C)NC[C@@H](O)COc1ccccc1-c1ccccc1 10.1021/acsmedchemlett.6b00363
CHEMBL4092412 158073 2 None 38 2 Human 10.5 pKd = 10.5 Binding
Displacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting methodDisplacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting method
ChEMBL 299 6 2 3 3.5 CC(C)(C)NC[C@@H](O)COc1ccccc1-c1ccccc1 10.1021/acsmedchemlett.6b00363
164612037 184785 0 None -1 20 Human 10.2 pKd = 10.2 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysis
ChEMBL 326 8 4 4 1.8 CCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1021/acs.jmedchem.1c00692
CHEMBL4860528 184785 0 None -1 20 Human 10.2 pKd = 10.2 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysis
ChEMBL 326 8 4 4 1.8 CCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1021/acs.jmedchem.1c00692
168290235 192356 0 None -4 20 Human 10.2 pKd = 10.2 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysis
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5201074 192356 0 None -4 20 Human 10.2 pKd = 10.2 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysis
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222491 192356 0 None -4 20 Human 10.2 pKd = 10.2 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysis
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
168294767 192407 0 None -1 20 Human 10.2 pKd = 10.2 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysis
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5207281 192407 0 None -1 20 Human 10.2 pKd = 10.2 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysis
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222802 192407 0 None -1 20 Human 10.2 pKd = 10.2 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysis
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
168295528 192419 0 None -1 20 Human 10.2 pKd = 10.2 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysis
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5206565 192419 0 None -1 20 Human 10.2 pKd = 10.2 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysis
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222872 192419 0 None -1 20 Human 10.2 pKd = 10.2 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysis
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
165193 3126 60 None 1 43 Human 10.0 pKd = 10 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation counting
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/acs.jmedchem.6b00358
2303 3126 60 None 1 43 Human 10.0 pKd = 10 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation counting
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/acs.jmedchem.6b00358
4946 3126 60 None 1 43 Human 10.0 pKd = 10 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation counting
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/acs.jmedchem.6b00358
564 3126 60 None 1 43 Human 10.0 pKd = 10 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation counting
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/acs.jmedchem.6b00358
62882 3126 60 None 1 43 Human 10.0 pKd = 10 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation counting
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/acs.jmedchem.6b00358
63 3126 60 None 1 43 Human 10.0 pKd = 10 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation counting
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/acs.jmedchem.6b00358
66366 3126 60 None 1 43 Human 10.0 pKd = 10 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation counting
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/acs.jmedchem.6b00358
91536 3126 60 None 1 43 Human 10.0 pKd = 10 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation counting
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/acs.jmedchem.6b00358
CHEMBL27 3126 60 None 1 43 Human 10.0 pKd = 10 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation counting
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/acs.jmedchem.6b00358
CHEMBL452861 3126 60 None 1 43 Human 10.0 pKd = 10 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation counting
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/acs.jmedchem.6b00358
DB00571 3126 60 None 1 43 Human 10.0 pKd = 10 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation counting
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/acs.jmedchem.6b00358
33624 3749 29 None -1 9 Guinea pig 9.8 pKd = 9.8 Binding
In vitro inhibitory activity against beta-2 adrenoceptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenoceptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C 10.1021/jm00156a028
4061 3749 29 None -1 9 Guinea pig 9.8 pKd = 9.8 Binding
In vitro inhibitory activity against beta-2 adrenoceptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenoceptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C 10.1021/jm00156a028
565 3749 29 None -1 9 Guinea pig 9.8 pKd = 9.8 Binding
In vitro inhibitory activity against beta-2 adrenoceptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenoceptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C 10.1021/jm00156a028
CHEMBL499 3749 29 None -1 9 Guinea pig 9.8 pKd = 9.8 Binding
In vitro inhibitory activity against beta-2 adrenoceptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenoceptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C 10.1021/jm00156a028
DB00373 3749 29 None -1 9 Guinea pig 9.8 pKd = 9.8 Binding
In vitro inhibitory activity against beta-2 adrenoceptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenoceptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C 10.1021/jm00156a028
3682 188837 7 None -1 8 Guinea pig 9.7 pKd = 9.7 Binding
Competitive antagonist activity at adrenergic beta2 receptor in precontracted Hartley guinea pig tracheal ring assessed as inhibition of politerol-indiuced relaxant activityCompetitive antagonist activity at adrenergic beta2 receptor in precontracted Hartley guinea pig tracheal ring assessed as inhibition of politerol-indiuced relaxant activity
ChEMBL 277 6 2 3 2.6 Cc1ccc(OCC(O)C(C)NC(C)C)c2c1CCC2 10.1016/j.bmcl.2014.12.077
CHEMBL1256784 188837 7 None -1 8 Guinea pig 9.7 pKd = 9.7 Binding
Competitive antagonist activity at adrenergic beta2 receptor in precontracted Hartley guinea pig tracheal ring assessed as inhibition of politerol-indiuced relaxant activityCompetitive antagonist activity at adrenergic beta2 receptor in precontracted Hartley guinea pig tracheal ring assessed as inhibition of politerol-indiuced relaxant activity
ChEMBL 277 6 2 3 2.6 Cc1ccc(OCC(O)C(C)NC(C)C)c2c1CCC2 10.1016/j.bmcl.2014.12.077
CHEMBL513389 188837 7 None -1 8 Guinea pig 9.7 pKd = 9.7 Binding
Competitive antagonist activity at adrenergic beta2 receptor in precontracted Hartley guinea pig tracheal ring assessed as inhibition of politerol-indiuced relaxant activityCompetitive antagonist activity at adrenergic beta2 receptor in precontracted Hartley guinea pig tracheal ring assessed as inhibition of politerol-indiuced relaxant activity
ChEMBL 277 6 2 3 2.6 Cc1ccc(OCC(O)C(C)NC(C)C)c2c1CCC2 10.1016/j.bmcl.2014.12.077
2585 788 100 None 1 22 Human 9.7 pKd = 9.7 Binding
Displacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysisDisplacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysis
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1021/acs.jmedchem.9b00595
522 788 100 None 1 22 Human 9.7 pKd = 9.7 Binding
Displacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysisDisplacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysis
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1021/acs.jmedchem.9b00595
551 788 100 None 1 22 Human 9.7 pKd = 9.7 Binding
Displacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysisDisplacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysis
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1021/acs.jmedchem.9b00595
CHEMBL723 788 100 None 1 22 Human 9.7 pKd = 9.7 Binding
Displacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysisDisplacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysis
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1021/acs.jmedchem.9b00595
DB01136 788 100 None 1 22 Human 9.7 pKd = 9.7 Binding
Displacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysisDisplacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysis
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1021/acs.jmedchem.9b00595
2687 874 15 None 1 5 Human 9.7 pKd = 9.7 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation counting
ChEMBL 279 5 4 4 1.0 OC(COc1cccc2c1[nH]c(=O)[nH]2)CNC(C)(C)C 10.1021/acs.jmedchem.6b00358
532 874 15 None 1 5 Human 9.7 pKd = 9.7 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation counting
ChEMBL 279 5 4 4 1.0 OC(COc1cccc2c1[nH]c(=O)[nH]2)CNC(C)(C)C 10.1021/acs.jmedchem.6b00358
5387 874 15 None 1 5 Human 9.7 pKd = 9.7 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation counting
ChEMBL 279 5 4 4 1.0 OC(COc1cccc2c1[nH]c(=O)[nH]2)CNC(C)(C)C 10.1021/acs.jmedchem.6b00358
CHEMBL420746 874 15 None 1 5 Human 9.7 pKd = 9.7 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation counting
ChEMBL 279 5 4 4 1.0 OC(COc1cccc2c1[nH]c(=O)[nH]2)CNC(C)(C)C 10.1021/acs.jmedchem.6b00358
33624 3749 29 None -1 9 Guinea pig 9.6 pKd = 9.6 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C 10.1021/jm00361a004
4061 3749 29 None -1 9 Guinea pig 9.6 pKd = 9.6 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C 10.1021/jm00361a004
565 3749 29 None -1 9 Guinea pig 9.6 pKd = 9.6 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C 10.1021/jm00361a004
CHEMBL499 3749 29 None -1 9 Guinea pig 9.6 pKd = 9.6 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C 10.1021/jm00361a004
DB00373 3749 29 None -1 9 Guinea pig 9.6 pKd = 9.6 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C 10.1021/jm00361a004
5311179 1935 18 None 85 3 Human 9.6 pKd = 9.6 Binding
Displacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting methodDisplacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting method
ChEMBL 277 6 2 3 2.6 Cc1c2CCCc2c(cc1)OC[C@H]([C@H](C)NC(C)C)O 10.1021/acsmedchemlett.6b00363
543 1935 18 None 85 3 Human 9.6 pKd = 9.6 Binding
Displacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting methodDisplacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting method
ChEMBL 277 6 2 3 2.6 Cc1c2CCCc2c(cc1)OC[C@H]([C@H](C)NC(C)C)O 10.1021/acsmedchemlett.6b00363
5484725 1935 18 None 85 3 Human 9.6 pKd = 9.6 Binding
Displacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting methodDisplacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting method
ChEMBL 277 6 2 3 2.6 Cc1c2CCCc2c(cc1)OC[C@H]([C@H](C)NC(C)C)O 10.1021/acsmedchemlett.6b00363
CHEMBL1233766 1935 18 None 85 3 Human 9.6 pKd = 9.6 Binding
Displacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting methodDisplacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting method
ChEMBL 277 6 2 3 2.6 Cc1c2CCCc2c(cc1)OC[C@H]([C@H](C)NC(C)C)O 10.1021/acsmedchemlett.6b00363
CHEMBL198059 1935 18 None 85 3 Human 9.6 pKd = 9.6 Binding
Displacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting methodDisplacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting method
ChEMBL 277 6 2 3 2.6 Cc1c2CCCc2c(cc1)OC[C@H]([C@H](C)NC(C)C)O 10.1021/acsmedchemlett.6b00363
11625619 77251 0 None 4 2 Human 9.6 pKd = 9.6 Binding
Kinetic binding affinity to human beta2-adrenoceptorKinetic binding affinity to human beta2-adrenoceptor
ChEMBL 406 6 4 4 3.5 CCc1cc2c(cc1CC)CC(C)(NC[C@H](O)c1ccc(O)c3[nH]c(=O)ccc13)C2 10.1016/j.bmcl.2012.07.096
CHEMBL2088201 77251 0 None 4 2 Human 9.6 pKd = 9.6 Binding
Kinetic binding affinity to human beta2-adrenoceptorKinetic binding affinity to human beta2-adrenoceptor
ChEMBL 406 6 4 4 3.5 CCc1cc2c(cc1CC)CC(C)(NC[C@H](O)c1ccc(O)c3[nH]c(=O)ccc13)C2 10.1016/j.bmcl.2012.07.096
5311179 1935 18 None 85 3 Human 9.5 pKd = 9.5 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation counting
ChEMBL 277 6 2 3 2.6 Cc1c2CCCc2c(cc1)OC[C@H]([C@H](C)NC(C)C)O 10.1021/acs.jmedchem.6b00358
543 1935 18 None 85 3 Human 9.5 pKd = 9.5 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation counting
ChEMBL 277 6 2 3 2.6 Cc1c2CCCc2c(cc1)OC[C@H]([C@H](C)NC(C)C)O 10.1021/acs.jmedchem.6b00358
5484725 1935 18 None 85 3 Human 9.5 pKd = 9.5 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation counting
ChEMBL 277 6 2 3 2.6 Cc1c2CCCc2c(cc1)OC[C@H]([C@H](C)NC(C)C)O 10.1021/acs.jmedchem.6b00358
CHEMBL1233766 1935 18 None 85 3 Human 9.5 pKd = 9.5 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation counting
ChEMBL 277 6 2 3 2.6 Cc1c2CCCc2c(cc1)OC[C@H]([C@H](C)NC(C)C)O 10.1021/acs.jmedchem.6b00358
CHEMBL198059 1935 18 None 85 3 Human 9.5 pKd = 9.5 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation counting
ChEMBL 277 6 2 3 2.6 Cc1c2CCCc2c(cc1)OC[C@H]([C@H](C)NC(C)C)O 10.1021/acs.jmedchem.6b00358
2419 3394 80 None 16 6 Human 9.5 pKd = 9.5 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation counting
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/acs.jmedchem.6b00358
5152 3394 80 None 16 6 Human 9.5 pKd = 9.5 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation counting
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/acs.jmedchem.6b00358
559 3394 80 None 16 6 Human 9.5 pKd = 9.5 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation counting
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/acs.jmedchem.6b00358
CHEMBL1263 3394 80 None 16 6 Human 9.5 pKd = 9.5 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation counting
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/acs.jmedchem.6b00358
DB00938 3394 80 None 16 6 Human 9.5 pKd = 9.5 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation counting
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/acs.jmedchem.6b00358
71707 10095 20 None - 1 Bovine 9.4 pKd = 9.4 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 249 7 2 3 2.3 CC(C)NCC(O)COc1ccccc1C1CC1 10.1021/jm00147a037
CHEMBL1159892 10095 20 None - 1 Bovine 9.4 pKd = 9.4 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 249 7 2 3 2.3 CC(C)NCC(O)COc1ccccc1C1CC1 10.1021/jm00147a037
688570 186268 18 None - 1 Human 9.3 pKd = 9.3 Binding
Binding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nMBinding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nM
ChEMBL 287 6 4 4 2.4 C[C@@H](NCCc1ccc(O)cc1)[C@@H](O)c1ccc(O)cc1 10.1016/j.bmcl.2013.07.052
CHEMBL489553 186268 18 None - 1 Human 9.3 pKd = 9.3 Binding
Binding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nMBinding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nM
ChEMBL 287 6 4 4 2.4 C[C@@H](NCCc1ccc(O)cc1)[C@@H](O)c1ccc(O)cc1 10.1016/j.bmcl.2013.07.052
137 367 47 None -3 12 Human 9.3 pKd = 9.3 Binding
Displacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cells
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1021/jm2008562
2119 367 47 None -3 12 Human 9.3 pKd = 9.3 Binding
Displacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cells
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1021/jm2008562
563 367 47 None -3 12 Human 9.3 pKd = 9.3 Binding
Displacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cells
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1021/jm2008562
66368 367 47 None -3 12 Human 9.3 pKd = 9.3 Binding
Displacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cells
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1021/jm2008562
CHEMBL266195 367 47 None -3 12 Human 9.3 pKd = 9.3 Binding
Displacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cells
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1021/jm2008562
DB00866 367 47 None -3 12 Human 9.3 pKd = 9.3 Binding
Displacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cells
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1021/jm2008562
2176 3065 66 None -2 27 Human 9.3 pKd = 9.3 Binding
Displacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cells
ChEMBL 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C 10.1021/jm2008562
4828 3065 66 None -2 27 Human 9.3 pKd = 9.3 Binding
Displacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cells
ChEMBL 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C 10.1021/jm2008562
91 3065 66 None -2 27 Human 9.3 pKd = 9.3 Binding
Displacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cells
ChEMBL 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C 10.1021/jm2008562
CHEMBL500 3065 66 None -2 27 Human 9.3 pKd = 9.3 Binding
Displacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cells
ChEMBL 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C 10.1021/jm2008562
DB00960 3065 66 None -2 27 Human 9.3 pKd = 9.3 Binding
Displacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cells
ChEMBL 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C 10.1021/jm2008562
165193 3126 60 None 1 43 Human 9.2 pKd = 9.2 Binding
Displacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm2008562
2303 3126 60 None 1 43 Human 9.2 pKd = 9.2 Binding
Displacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm2008562
4946 3126 60 None 1 43 Human 9.2 pKd = 9.2 Binding
Displacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm2008562
564 3126 60 None 1 43 Human 9.2 pKd = 9.2 Binding
Displacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm2008562
62882 3126 60 None 1 43 Human 9.2 pKd = 9.2 Binding
Displacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm2008562
63 3126 60 None 1 43 Human 9.2 pKd = 9.2 Binding
Displacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm2008562
66366 3126 60 None 1 43 Human 9.2 pKd = 9.2 Binding
Displacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm2008562
91536 3126 60 None 1 43 Human 9.2 pKd = 9.2 Binding
Displacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm2008562
CHEMBL27 3126 60 None 1 43 Human 9.2 pKd = 9.2 Binding
Displacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm2008562
CHEMBL452861 3126 60 None 1 43 Human 9.2 pKd = 9.2 Binding
Displacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm2008562
DB00571 3126 60 None 1 43 Human 9.2 pKd = 9.2 Binding
Displacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm2008562
54669764 65146 0 None 37 3 Human 9.2 pKd = 9.2 Binding
Displacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cells
ChEMBL 893 26 4 10 6.8 O=C(CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1)NCCOCCOCCNC[C@H](O)COc1cccc2ccccc12 10.1021/jm2008562
CHEMBL1830491 65146 0 None 37 3 Human 9.2 pKd = 9.2 Binding
Displacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cells
ChEMBL 893 26 4 10 6.8 O=C(CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1)NCCOCCOCCNC[C@H](O)COc1cccc2ccccc12 10.1021/jm2008562
43216 10086 7 None 4 2 Bovine 9.2 pKd = 9.2 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 251 8 2 3 2.4 CCCc1ccccc1OCC(O)CNC(C)C 10.1021/jm00147a037
CHEMBL1159723 10086 7 None 4 2 Bovine 9.2 pKd = 9.2 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 251 8 2 3 2.4 CCCc1ccccc1OCC(O)CNC(C)C 10.1021/jm00147a037
3682 188837 7 None 1 8 Human 9.2 pKd = 9.2 Binding
Binding affinity to human adrenergic beta2 receptorBinding affinity to human adrenergic beta2 receptor
ChEMBL 277 6 2 3 2.6 Cc1ccc(OCC(O)C(C)NC(C)C)c2c1CCC2 10.1016/j.ejmech.2008.12.016
CHEMBL1256784 188837 7 None 1 8 Human 9.2 pKd = 9.2 Binding
Binding affinity to human adrenergic beta2 receptorBinding affinity to human adrenergic beta2 receptor
ChEMBL 277 6 2 3 2.6 Cc1ccc(OCC(O)C(C)NC(C)C)c2c1CCC2 10.1016/j.ejmech.2008.12.016
CHEMBL513389 188837 7 None 1 8 Human 9.2 pKd = 9.2 Binding
Binding affinity to human adrenergic beta2 receptorBinding affinity to human adrenergic beta2 receptor
ChEMBL 277 6 2 3 2.6 Cc1ccc(OCC(O)C(C)NC(C)C)c2c1CCC2 10.1016/j.ejmech.2008.12.016
3682 188837 7 None 1 8 Human 9.2 pKd = 9.2 Binding
Displacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 277 6 2 3 2.6 Cc1ccc(OCC(O)C(C)NC(C)C)c2c1CCC2 10.1021/jm400348g
CHEMBL1256784 188837 7 None 1 8 Human 9.2 pKd = 9.2 Binding
Displacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 277 6 2 3 2.6 Cc1ccc(OCC(O)C(C)NC(C)C)c2c1CCC2 10.1021/jm400348g
CHEMBL513389 188837 7 None 1 8 Human 9.2 pKd = 9.2 Binding
Displacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 277 6 2 3 2.6 Cc1ccc(OCC(O)C(C)NC(C)C)c2c1CCC2 10.1021/jm400348g
132 1244 9 None -1 14 Human 9.2 pKd = 9.2 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation counting
ChEMBL 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 10.1021/acs.jmedchem.6b00358
155346 1244 9 None -1 14 Human 9.2 pKd = 9.2 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation counting
ChEMBL 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 10.1021/acs.jmedchem.6b00358
CHEMBL378501 1244 9 None -1 14 Human 9.2 pKd = 9.2 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation counting
ChEMBL 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 10.1021/acs.jmedchem.6b00358
54756927 65141 0 None 97 3 Human 9.1 pKd = 9.1 Binding
Displacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cells
ChEMBL 833 22 4 8 7.5 O=C(CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1)NCCCCNC[C@H](O)COc1cccc2ccccc12 10.1021/jm2008562
CHEMBL1830486 65141 0 None 97 3 Human 9.1 pKd = 9.1 Binding
Displacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cells
ChEMBL 833 22 4 8 7.5 O=C(CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1)NCCCCNC[C@H](O)COc1cccc2ccccc12 10.1021/jm2008562
137 367 47 None -3 12 Human 9.1 pKd = 9.1 Binding
Binding affinity to N-terminal FLAG-tagged C-terminal His-10-tagged human beta2 adrenoceptor expressed in insect Sf9 cells by surface plasmon resonance analysisBinding affinity to N-terminal FLAG-tagged C-terminal His-10-tagged human beta2 adrenoceptor expressed in insect Sf9 cells by surface plasmon resonance analysis
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1021/ml400312j
2119 367 47 None -3 12 Human 9.1 pKd = 9.1 Binding
Binding affinity to N-terminal FLAG-tagged C-terminal His-10-tagged human beta2 adrenoceptor expressed in insect Sf9 cells by surface plasmon resonance analysisBinding affinity to N-terminal FLAG-tagged C-terminal His-10-tagged human beta2 adrenoceptor expressed in insect Sf9 cells by surface plasmon resonance analysis
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1021/ml400312j
563 367 47 None -3 12 Human 9.1 pKd = 9.1 Binding
Binding affinity to N-terminal FLAG-tagged C-terminal His-10-tagged human beta2 adrenoceptor expressed in insect Sf9 cells by surface plasmon resonance analysisBinding affinity to N-terminal FLAG-tagged C-terminal His-10-tagged human beta2 adrenoceptor expressed in insect Sf9 cells by surface plasmon resonance analysis
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1021/ml400312j
66368 367 47 None -3 12 Human 9.1 pKd = 9.1 Binding
Binding affinity to N-terminal FLAG-tagged C-terminal His-10-tagged human beta2 adrenoceptor expressed in insect Sf9 cells by surface plasmon resonance analysisBinding affinity to N-terminal FLAG-tagged C-terminal His-10-tagged human beta2 adrenoceptor expressed in insect Sf9 cells by surface plasmon resonance analysis
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1021/ml400312j
CHEMBL266195 367 47 None -3 12 Human 9.1 pKd = 9.1 Binding
Binding affinity to N-terminal FLAG-tagged C-terminal His-10-tagged human beta2 adrenoceptor expressed in insect Sf9 cells by surface plasmon resonance analysisBinding affinity to N-terminal FLAG-tagged C-terminal His-10-tagged human beta2 adrenoceptor expressed in insect Sf9 cells by surface plasmon resonance analysis
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1021/ml400312j
DB00866 367 47 None -3 12 Human 9.1 pKd = 9.1 Binding
Binding affinity to N-terminal FLAG-tagged C-terminal His-10-tagged human beta2 adrenoceptor expressed in insect Sf9 cells by surface plasmon resonance analysisBinding affinity to N-terminal FLAG-tagged C-terminal His-10-tagged human beta2 adrenoceptor expressed in insect Sf9 cells by surface plasmon resonance analysis
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1021/ml400312j
165193 3126 60 None 1 43 Human 9.1 pKd = 9.1 Binding
Binding affinity to human adrenergic beta2 receptorBinding affinity to human adrenergic beta2 receptor
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.ejmech.2008.12.016
2303 3126 60 None 1 43 Human 9.1 pKd = 9.1 Binding
Binding affinity to human adrenergic beta2 receptorBinding affinity to human adrenergic beta2 receptor
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.ejmech.2008.12.016
4946 3126 60 None 1 43 Human 9.1 pKd = 9.1 Binding
Binding affinity to human adrenergic beta2 receptorBinding affinity to human adrenergic beta2 receptor
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.ejmech.2008.12.016
564 3126 60 None 1 43 Human 9.1 pKd = 9.1 Binding
Binding affinity to human adrenergic beta2 receptorBinding affinity to human adrenergic beta2 receptor
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.ejmech.2008.12.016
62882 3126 60 None 1 43 Human 9.1 pKd = 9.1 Binding
Binding affinity to human adrenergic beta2 receptorBinding affinity to human adrenergic beta2 receptor
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.ejmech.2008.12.016
63 3126 60 None 1 43 Human 9.1 pKd = 9.1 Binding
Binding affinity to human adrenergic beta2 receptorBinding affinity to human adrenergic beta2 receptor
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.ejmech.2008.12.016
66366 3126 60 None 1 43 Human 9.1 pKd = 9.1 Binding
Binding affinity to human adrenergic beta2 receptorBinding affinity to human adrenergic beta2 receptor
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.ejmech.2008.12.016
91536 3126 60 None 1 43 Human 9.1 pKd = 9.1 Binding
Binding affinity to human adrenergic beta2 receptorBinding affinity to human adrenergic beta2 receptor
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.ejmech.2008.12.016
CHEMBL27 3126 60 None 1 43 Human 9.1 pKd = 9.1 Binding
Binding affinity to human adrenergic beta2 receptorBinding affinity to human adrenergic beta2 receptor
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.ejmech.2008.12.016
CHEMBL452861 3126 60 None 1 43 Human 9.1 pKd = 9.1 Binding
Binding affinity to human adrenergic beta2 receptorBinding affinity to human adrenergic beta2 receptor
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.ejmech.2008.12.016
DB00571 3126 60 None 1 43 Human 9.1 pKd = 9.1 Binding
Binding affinity to human adrenergic beta2 receptorBinding affinity to human adrenergic beta2 receptor
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.ejmech.2008.12.016
165193 3126 60 None -2 43 Bovine 9.1 pKd = 9.1 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00147a037
2303 3126 60 None -2 43 Bovine 9.1 pKd = 9.1 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00147a037
4946 3126 60 None -2 43 Bovine 9.1 pKd = 9.1 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00147a037
564 3126 60 None -2 43 Bovine 9.1 pKd = 9.1 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00147a037
62882 3126 60 None -2 43 Bovine 9.1 pKd = 9.1 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00147a037
63 3126 60 None -2 43 Bovine 9.1 pKd = 9.1 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00147a037
66366 3126 60 None -2 43 Bovine 9.1 pKd = 9.1 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00147a037
91536 3126 60 None -2 43 Bovine 9.1 pKd = 9.1 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00147a037
CHEMBL27 3126 60 None -2 43 Bovine 9.1 pKd = 9.1 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00147a037
CHEMBL452861 3126 60 None -2 43 Bovine 9.1 pKd = 9.1 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00147a037
DB00571 3126 60 None -2 43 Bovine 9.1 pKd = 9.1 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00147a037
204665 10125 9 None 1 2 Human 9.1 pKd = 9.1 Binding
Displacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysisDisplacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysis
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
CHEMBL1160734 10125 9 None 1 2 Human 9.1 pKd = 9.1 Binding
Displacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysisDisplacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysis
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
54757232 65170 0 None 30 3 Human 9.0 pKd = 9.0 Binding
Displacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cells
ChEMBL 883 28 4 10 6.3 C=CCc1ccccc1OC[C@@H](O)CNCCOCCOCCNC(=O)CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1 10.1021/jm2008562
CHEMBL1830618 65170 0 None 30 3 Human 9.0 pKd = 9.0 Binding
Displacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cells
ChEMBL 883 28 4 10 6.3 C=CCc1ccccc1OC[C@@H](O)CNCCOCCOCCNC(=O)CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1 10.1021/jm2008562
165193 3126 60 None -4 43 Guinea pig 9.0 pKd = 9.0 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00156a028
2303 3126 60 None -4 43 Guinea pig 9.0 pKd = 9.0 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00156a028
4946 3126 60 None -4 43 Guinea pig 9.0 pKd = 9.0 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00156a028
564 3126 60 None -4 43 Guinea pig 9.0 pKd = 9.0 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00156a028
62882 3126 60 None -4 43 Guinea pig 9.0 pKd = 9.0 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00156a028
63 3126 60 None -4 43 Guinea pig 9.0 pKd = 9.0 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00156a028
66366 3126 60 None -4 43 Guinea pig 9.0 pKd = 9.0 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00156a028
91536 3126 60 None -4 43 Guinea pig 9.0 pKd = 9.0 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00156a028
CHEMBL27 3126 60 None -4 43 Guinea pig 9.0 pKd = 9.0 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00156a028
CHEMBL452861 3126 60 None -4 43 Guinea pig 9.0 pKd = 9.0 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00156a028
DB00571 3126 60 None -4 43 Guinea pig 9.0 pKd = 9.0 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00156a028
12179890 94184 1 None -3 2 Human 8.9 pKd = 8.9 Binding
Binding affinity to beta2 adrenergic receptorBinding affinity to beta2 adrenergic receptor
ChEMBL 223 6 2 3 1.7 Cc1cccc(OC[C@@H](O)CNC(C)C)c1 10.1021/jm800227h
CHEMBL252319 94184 1 None -3 2 Human 8.9 pKd = 8.9 Binding
Binding affinity to beta2 adrenergic receptorBinding affinity to beta2 adrenergic receptor
ChEMBL 223 6 2 3 1.7 Cc1cccc(OC[C@@H](O)CNC(C)C)c1 10.1021/jm800227h
54757331 65171 0 None 39 3 Human 8.9 pKd = 8.9 Binding
Displacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cells
ChEMBL 883 28 4 10 6.3 C=CCc1ccccc1OCC(O)CNCCOCCOCCNC(=O)CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1 10.1021/jm2008562
CHEMBL1830619 65171 0 None 39 3 Human 8.9 pKd = 8.9 Binding
Displacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cells
ChEMBL 883 28 4 10 6.3 C=CCc1ccccc1OCC(O)CNCCOCCOCCNC(=O)CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1 10.1021/jm2008562
165193 3126 60 None -4 43 Guinea pig 8.9 pKd = 8.9 Binding
Ability to block Beta-2 adrenergic receptor in guinea pig trachea preparationAbility to block Beta-2 adrenergic receptor in guinea pig trachea preparation
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00354a003
2303 3126 60 None -4 43 Guinea pig 8.9 pKd = 8.9 Binding
Ability to block Beta-2 adrenergic receptor in guinea pig trachea preparationAbility to block Beta-2 adrenergic receptor in guinea pig trachea preparation
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00354a003
4946 3126 60 None -4 43 Guinea pig 8.9 pKd = 8.9 Binding
Ability to block Beta-2 adrenergic receptor in guinea pig trachea preparationAbility to block Beta-2 adrenergic receptor in guinea pig trachea preparation
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00354a003
564 3126 60 None -4 43 Guinea pig 8.9 pKd = 8.9 Binding
Ability to block Beta-2 adrenergic receptor in guinea pig trachea preparationAbility to block Beta-2 adrenergic receptor in guinea pig trachea preparation
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00354a003
62882 3126 60 None -4 43 Guinea pig 8.9 pKd = 8.9 Binding
Ability to block Beta-2 adrenergic receptor in guinea pig trachea preparationAbility to block Beta-2 adrenergic receptor in guinea pig trachea preparation
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00354a003
63 3126 60 None -4 43 Guinea pig 8.9 pKd = 8.9 Binding
Ability to block Beta-2 adrenergic receptor in guinea pig trachea preparationAbility to block Beta-2 adrenergic receptor in guinea pig trachea preparation
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00354a003
66366 3126 60 None -4 43 Guinea pig 8.9 pKd = 8.9 Binding
Ability to block Beta-2 adrenergic receptor in guinea pig trachea preparationAbility to block Beta-2 adrenergic receptor in guinea pig trachea preparation
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00354a003
91536 3126 60 None -4 43 Guinea pig 8.9 pKd = 8.9 Binding
Ability to block Beta-2 adrenergic receptor in guinea pig trachea preparationAbility to block Beta-2 adrenergic receptor in guinea pig trachea preparation
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00354a003
CHEMBL27 3126 60 None -4 43 Guinea pig 8.9 pKd = 8.9 Binding
Ability to block Beta-2 adrenergic receptor in guinea pig trachea preparationAbility to block Beta-2 adrenergic receptor in guinea pig trachea preparation
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00354a003
CHEMBL452861 3126 60 None -4 43 Guinea pig 8.9 pKd = 8.9 Binding
Ability to block Beta-2 adrenergic receptor in guinea pig trachea preparationAbility to block Beta-2 adrenergic receptor in guinea pig trachea preparation
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00354a003
DB00571 3126 60 None -4 43 Guinea pig 8.9 pKd = 8.9 Binding
Ability to block Beta-2 adrenergic receptor in guinea pig trachea preparationAbility to block Beta-2 adrenergic receptor in guinea pig trachea preparation
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00354a003
13040879 23636 0 None 1 2 Guinea pig 8.9 pKd = 8.9 Binding
Ability to block Beta-2 adrenergic receptor in guinea pig trachea preparationAbility to block Beta-2 adrenergic receptor in guinea pig trachea preparation
ChEMBL 281 6 2 5 1.6 COC(=O)c1ccccc1OCC(O)CNC(C)(C)C 10.1021/jm00354a003
CHEMBL13365 23636 0 None 1 2 Guinea pig 8.9 pKd = 8.9 Binding
Ability to block Beta-2 adrenergic receptor in guinea pig trachea preparationAbility to block Beta-2 adrenergic receptor in guinea pig trachea preparation
ChEMBL 281 6 2 5 1.6 COC(=O)c1ccccc1OCC(O)CNC(C)(C)C 10.1021/jm00354a003
9904228 98818 0 None 1 2 Guinea pig 8.9 pKd = 8.9 Binding
Ability to block Beta-2 adrenergic receptor in guinea pig trachea preparationAbility to block Beta-2 adrenergic receptor in guinea pig trachea preparation
ChEMBL 295 9 2 5 1.5 COC(=O)CCc1ccccc1OCC(O)CNC(C)C 10.1021/jm00354a003
CHEMBL281967 98818 0 None 1 2 Guinea pig 8.9 pKd = 8.9 Binding
Ability to block Beta-2 adrenergic receptor in guinea pig trachea preparationAbility to block Beta-2 adrenergic receptor in guinea pig trachea preparation
ChEMBL 295 9 2 5 1.5 COC(=O)CCc1ccccc1OCC(O)CNC(C)C 10.1021/jm00354a003
105110 99655 6 None 1 2 Guinea pig 8.9 pKd = 8.9 Binding
In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.
ChEMBL 273 7 2 3 2.8 CC(C)CNCC(O)COc1cccc2ccccc12 10.1021/jm00354a002
CHEMBL287651 99655 6 None 1 2 Guinea pig 8.9 pKd = 8.9 Binding
In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.
ChEMBL 273 7 2 3 2.8 CC(C)CNCC(O)COc1cccc2ccccc12 10.1021/jm00354a002
155569481 175632 0 None 8 2 Human 8.9 pKd = 8.9 Binding
Displacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysisDisplacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysis
ChEMBL 614 23 6 8 2.7 CC(C)NC[C@H](O)COc1ccccc1CCCC(=O)NCCNC(=O)CCCc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
CHEMBL4594173 175632 0 None 8 2 Human 8.9 pKd = 8.9 Binding
Displacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysisDisplacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysis
ChEMBL 614 23 6 8 2.7 CC(C)NC[C@H](O)COc1ccccc1CCCC(=O)NCCNC(=O)CCCc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
11823027 192006 33 None -1 3 Human 8.9 pKd = 8.9 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation counting
ChEMBL 309 5 4 5 0.6 CC(C)(C)NCC(O)COc1cccc2c1CC(O)C(O)C2 10.1021/acs.jmedchem.6b00358
4411 192006 33 None -1 3 Human 8.9 pKd = 8.9 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation counting
ChEMBL 309 5 4 5 0.6 CC(C)(C)NCC(O)COc1cccc2c1CC(O)C(O)C2 10.1021/acs.jmedchem.6b00358
CHEMBL521606 192006 33 None -1 3 Human 8.9 pKd = 8.9 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation counting
ChEMBL 309 5 4 5 0.6 CC(C)(C)NCC(O)COc1cccc2c1CC(O)C(O)C2 10.1021/acs.jmedchem.6b00358
54757026 65144 0 None 74 3 Human 8.9 pKd = 8.9 Binding
Displacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cells
ChEMBL 833 22 4 8 7.5 O=C(CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1)NCCCCNCC(O)COc1cccc2ccccc12 10.1021/jm2008562
CHEMBL1830489 65144 0 None 74 3 Human 8.9 pKd = 8.9 Binding
Displacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cells
ChEMBL 833 22 4 8 7.5 O=C(CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1)NCCCCNCC(O)COc1cccc2ccccc12 10.1021/jm2008562
165193 3126 60 None -4 43 Guinea pig 8.9 pKd = 8.9 Binding
Antagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 minsAntagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 mins
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00208a015
2303 3126 60 None -4 43 Guinea pig 8.9 pKd = 8.9 Binding
Antagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 minsAntagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 mins
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00208a015
4946 3126 60 None -4 43 Guinea pig 8.9 pKd = 8.9 Binding
Antagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 minsAntagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 mins
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00208a015
564 3126 60 None -4 43 Guinea pig 8.9 pKd = 8.9 Binding
Antagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 minsAntagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 mins
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00208a015
62882 3126 60 None -4 43 Guinea pig 8.9 pKd = 8.9 Binding
Antagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 minsAntagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 mins
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00208a015
63 3126 60 None -4 43 Guinea pig 8.9 pKd = 8.9 Binding
Antagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 minsAntagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 mins
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00208a015
66366 3126 60 None -4 43 Guinea pig 8.9 pKd = 8.9 Binding
Antagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 minsAntagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 mins
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00208a015
91536 3126 60 None -4 43 Guinea pig 8.9 pKd = 8.9 Binding
Antagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 minsAntagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 mins
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00208a015
CHEMBL27 3126 60 None -4 43 Guinea pig 8.9 pKd = 8.9 Binding
Antagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 minsAntagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 mins
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00208a015
CHEMBL452861 3126 60 None -4 43 Guinea pig 8.9 pKd = 8.9 Binding
Antagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 minsAntagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 mins
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00208a015
DB00571 3126 60 None -4 43 Guinea pig 8.9 pKd = 8.9 Binding
Antagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 minsAntagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 mins
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00208a015
54758417 65140 0 None 38 3 Human 8.9 pKd = 8.9 Binding
Displacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cells
ChEMBL 805 20 4 8 6.7 O=C(CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1)NCCNC[C@H](O)COc1cccc2ccccc12 10.1021/jm2008562
CHEMBL1830485 65140 0 None 38 3 Human 8.9 pKd = 8.9 Binding
Displacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cells
ChEMBL 805 20 4 8 6.7 O=C(CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1)NCCNC[C@H](O)COc1cccc2ccccc12 10.1021/jm2008562
137 367 47 None -3 12 Human 8.8 pKd = 8.8 Binding
Displacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysisDisplacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysis
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1021/acs.jmedchem.9b00595
2119 367 47 None -3 12 Human 8.8 pKd = 8.8 Binding
Displacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysisDisplacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysis
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1021/acs.jmedchem.9b00595
563 367 47 None -3 12 Human 8.8 pKd = 8.8 Binding
Displacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysisDisplacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysis
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1021/acs.jmedchem.9b00595
66368 367 47 None -3 12 Human 8.8 pKd = 8.8 Binding
Displacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysisDisplacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysis
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1021/acs.jmedchem.9b00595
CHEMBL266195 367 47 None -3 12 Human 8.8 pKd = 8.8 Binding
Displacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysisDisplacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysis
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1021/acs.jmedchem.9b00595
DB00866 367 47 None -3 12 Human 8.8 pKd = 8.8 Binding
Displacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysisDisplacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysis
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1021/acs.jmedchem.9b00595
137 367 47 None -3 12 Human 8.8 pKd = 8.8 Binding
Displacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysisDisplacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysis
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1021/acs.jmedchem.9b00595
2119 367 47 None -3 12 Human 8.8 pKd = 8.8 Binding
Displacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysisDisplacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysis
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1021/acs.jmedchem.9b00595
563 367 47 None -3 12 Human 8.8 pKd = 8.8 Binding
Displacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysisDisplacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysis
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1021/acs.jmedchem.9b00595
66368 367 47 None -3 12 Human 8.8 pKd = 8.8 Binding
Displacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysisDisplacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysis
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1021/acs.jmedchem.9b00595
CHEMBL266195 367 47 None -3 12 Human 8.8 pKd = 8.8 Binding
Displacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysisDisplacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysis
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1021/acs.jmedchem.9b00595
DB00866 367 47 None -3 12 Human 8.8 pKd = 8.8 Binding
Displacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysisDisplacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysis
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1021/acs.jmedchem.9b00595
13040881 98704 0 None 1 2 Guinea pig 8.8 pKd = 8.8 Binding
Ability to block Beta-2 adrenergic receptor in guinea pig trachea preparationAbility to block Beta-2 adrenergic receptor in guinea pig trachea preparation
ChEMBL 295 7 2 5 2.0 CCOC(=O)c1ccccc1OCC(O)CNC(C)(C)C 10.1021/jm00354a003
CHEMBL281294 98704 0 None 1 2 Guinea pig 8.8 pKd = 8.8 Binding
Ability to block Beta-2 adrenergic receptor in guinea pig trachea preparationAbility to block Beta-2 adrenergic receptor in guinea pig trachea preparation
ChEMBL 295 7 2 5 2.0 CCOC(=O)c1ccccc1OCC(O)CNC(C)(C)C 10.1021/jm00354a003
155518547 169712 0 None 29 2 Human 8.7 pKd = 8.7 Binding
Displacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysisDisplacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysis
ChEMBL 558 20 6 7 3.0 CC(C)NC[C@H](O)COc1ccccc1CCCNC(=O)NCCCc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
CHEMBL4446394 169712 0 None 29 2 Human 8.7 pKd = 8.7 Binding
Displacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysisDisplacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysis
ChEMBL 558 20 6 7 3.0 CC(C)NC[C@H](O)COc1ccccc1CCCNC(=O)NCCCc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
26227 91840 5 None - 1 Human 8.0 pKd = 8 Binding
Binding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nMBinding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nM
ChEMBL 265 5 4 4 2.4 CCC(NC1CCCC1)C(O)c1ccc(O)c(O)c1 10.1016/j.bmcl.2013.07.052
CHEMBL2426777 91840 5 None - 1 Human 8.0 pKd = 8 Binding
Binding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nMBinding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nM
ChEMBL 265 5 4 4 2.4 CCC(NC1CCCC1)C(O)c1ccc(O)c(O)c1 10.1016/j.bmcl.2013.07.052
2843596 10081 5 None - 1 Bovine 8.0 pKd = 8.0 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 237 6 2 3 2.0 Cc1cc(C)cc(OCC(O)CNC(C)C)c1 10.1021/jm00147a037
CHEMBL1159714 10081 5 None - 1 Bovine 8.0 pKd = 8.0 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 237 6 2 3 2.0 Cc1cc(C)cc(OCC(O)CNC(C)C)c1 10.1021/jm00147a037
10332812 202224 2 None - 1 Bovine 8.0 pKd = 8.0 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 223 6 2 3 1.7 Cc1ccccc1OCC(O)CNC(C)C 10.1021/jm00147a037
CHEMBL6920 202224 2 None - 1 Bovine 8.0 pKd = 8.0 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 223 6 2 3 1.7 Cc1ccccc1OCC(O)CNC(C)C 10.1021/jm00147a037
54758415 65173 0 None 6 3 Human 8.0 pKd = 8.0 Binding
Displacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cells
ChEMBL 882 26 5 10 6.1 O=C(CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1)NCCOCCOCCNCC(O)COc1cccc2[nH]ccc12 10.1021/jm2008562
CHEMBL1830621 65173 0 None 6 3 Human 8.0 pKd = 8.0 Binding
Displacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cells
ChEMBL 882 26 5 10 6.1 O=C(CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1)NCCOCCOCCNCC(O)COc1cccc2[nH]ccc12 10.1021/jm2008562
1155 1592 45 None 2 5 Human 7.0 pKd = 7 Binding
Binding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nMBinding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nM
ChEMBL 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 10.1016/j.bmcl.2013.07.052
3343 1592 45 None 2 5 Human 7.0 pKd = 7 Binding
Binding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nMBinding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nM
ChEMBL 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 10.1016/j.bmcl.2013.07.052
557 1592 45 None 2 5 Human 7.0 pKd = 7 Binding
Binding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nMBinding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nM
ChEMBL 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 10.1016/j.bmcl.2013.07.052
CHEMBL32800 1592 45 None 2 5 Human 7.0 pKd = 7 Binding
Binding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nMBinding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nM
ChEMBL 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 10.1016/j.bmcl.2013.07.052
DB01288 1592 45 None 2 5 Human 7.0 pKd = 7 Binding
Binding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nMBinding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nM
ChEMBL 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 10.1016/j.bmcl.2013.07.052
56666465 63469 0 None - 1 Human 7.0 pKd = 7 Binding
Binding affinity to human adrenergic beta2 receptor by radioligand binding assayBinding affinity to human adrenergic beta2 receptor by radioligand binding assay
ChEMBL 282 3 4 6 0.4 CC(C)(C)NC[C@H](O)c1ccc2c(c1)CO[B-](O)(O)O2 10.1021/jm200371q
CHEMBL1802359 63469 0 None - 1 Human 7.0 pKd = 7 Binding
Binding affinity to human adrenergic beta2 receptor by radioligand binding assayBinding affinity to human adrenergic beta2 receptor by radioligand binding assay
ChEMBL 282 3 4 6 0.4 CC(C)(C)NC[C@H](O)c1ccc2c(c1)CO[B-](O)(O)O2 10.1021/jm200371q
15578606 107467 2 None -3 2 Guinea pig 7.0 pKd = 7 Binding
In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.
ChEMBL 267 8 2 5 0.9 COC(=O)CCNCC(O)COc1ccccc1C 10.1021/jm00354a002
CHEMBL31938 107467 2 None -3 2 Guinea pig 7.0 pKd = 7 Binding
In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.
ChEMBL 267 8 2 5 0.9 COC(=O)CCNCC(O)COc1ccccc1C 10.1021/jm00354a002
15578577 171993 0 None -1 2 Guinea pig 7.0 pKd = 7 Binding
In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.
ChEMBL 303 8 2 5 1.7 COC(=O)CCNCC(O)COc1cccc2ccccc12 10.1021/jm00354a002
CHEMBL448775 171993 0 None -1 2 Guinea pig 7.0 pKd = 7 Binding
In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.
ChEMBL 303 8 2 5 1.7 COC(=O)CCNCC(O)COc1cccc2ccccc12 10.1021/jm00354a002
3762 14316 24 None - 1 Human 6.0 pKd = 6 Binding
Binding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nMBinding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nM
ChEMBL 239 5 4 4 1.9 CCC(NC(C)C)C(O)c1ccc(O)c(O)c1 10.1016/j.bmcl.2013.07.052
CHEMBL1201153 14316 24 None - 1 Human 6.0 pKd = 6 Binding
Binding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nMBinding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nM
ChEMBL 239 5 4 4 1.9 CCC(NC(C)C)C(O)c1ccc(O)c(O)c1 10.1016/j.bmcl.2013.07.052
CHEMBL1201213 14316 24 None - 1 Human 6.0 pKd = 6 Binding
Binding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nMBinding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nM
ChEMBL 239 5 4 4 1.9 CCC(NC(C)C)C(O)c1ccc(O)c(O)c1 10.1016/j.bmcl.2013.07.052
15578575 99248 2 None -3 2 Guinea pig 6.0 pKd = 6 Binding
In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.
ChEMBL 281 10 2 5 1.4 CCOC(=O)CCCNCC(O)COc1ccccc1 10.1021/jm00354a002
CHEMBL284808 99248 2 None -3 2 Guinea pig 6.0 pKd = 6 Binding
In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.
ChEMBL 281 10 2 5 1.4 CCOC(=O)CCCNCC(O)COc1ccccc1 10.1021/jm00354a002
44279490 104156 0 None -1 2 Guinea pig 6.0 pKd = 6 Binding
In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.
ChEMBL 297 9 2 5 1.8 CCOC(=O)CCNCC(O)COC1=CC=CCC1(C)C 10.1021/jm00354a002
CHEMBL31050 104156 0 None -1 2 Guinea pig 6.0 pKd = 6 Binding
In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.
ChEMBL 297 9 2 5 1.8 CCOC(=O)CCNCC(O)COC1=CC=CCC1(C)C 10.1021/jm00354a002
16737587 159733 0 None -1 2 Human 4.0 pKd = 4 Binding
Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.
ChEMBL 267 8 4 4 2.7 CCCCC[C@@H](C)NC[C@@H](O)c1cc(O)cc(O)c1 nan
CHEMBL4110387 159733 0 None -1 2 Human 4.0 pKd = 4 Binding
Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.
ChEMBL 267 8 4 4 2.7 CCCCC[C@@H](C)NC[C@@H](O)c1cc(O)cc(O)c1 nan
14348818 109273 0 None -12 3 Guinea pig 4.0 pKd = 4 Binding
The compound was tested for beta-adrenergic activity against Beta-2 adrenergic receptor from guinea pig trachea.The compound was tested for beta-adrenergic activity against Beta-2 adrenergic receptor from guinea pig trachea.
ChEMBL 415 7 4 7 2.9 C/C(=N\OCC(O)CNC(C)(C)C)c1cc(Cl)c(NC2=NCCN2)c(Cl)c1 10.1021/jm00115a008
CHEMBL323176 109273 0 None -12 3 Guinea pig 4.0 pKd = 4 Binding
The compound was tested for beta-adrenergic activity against Beta-2 adrenergic receptor from guinea pig trachea.The compound was tested for beta-adrenergic activity against Beta-2 adrenergic receptor from guinea pig trachea.
ChEMBL 415 7 4 7 2.9 C/C(=N\OCC(O)CNC(C)(C)C)c1cc(Cl)c(NC2=NCCN2)c(Cl)c1 10.1021/jm00115a008
71662409 87812 0 None -85 2 Human 6.0 pKd = 6.0 Binding
Displacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 535 14 4 6 3.9 O=C(NCCNCC(O)COc1ccc(OCCOC2CCCC2)cc1)Nc1cccc(Br)c1 10.1021/jm400348g
CHEMBL2348204 87812 0 None -85 2 Human 6.0 pKd = 6.0 Binding
Displacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 535 14 4 6 3.9 O=C(NCCNCC(O)COc1ccc(OCCOC2CCCC2)cc1)Nc1cccc(Br)c1 10.1021/jm400348g
667688 85358 4 None - 1 Human 5.0 pKd = 5.0 Binding
Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.
ChEMBL 303 6 5 5 2.1 C[C@H](Cc1ccc(O)cc1)NC[C@@H](O)c1cc(O)cc(O)c1 nan
CHEMBL229477 85358 4 None - 1 Human 5.0 pKd = 5.0 Binding
Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.
ChEMBL 303 6 5 5 2.1 C[C@H](Cc1ccc(O)cc1)NC[C@@H](O)c1cc(O)cc(O)c1 nan
2369 615 75 None -9 8 Guinea pig 7.0 pKd = 7.0 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
ChEMBL 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C 10.1021/jm00361a004
356 615 75 None -9 8 Guinea pig 7.0 pKd = 7.0 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
ChEMBL 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C 10.1021/jm00361a004
549 615 75 None -9 8 Guinea pig 7.0 pKd = 7.0 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
ChEMBL 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C 10.1021/jm00361a004
CHEMBL423 615 75 None -9 8 Guinea pig 7.0 pKd = 7.0 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
ChEMBL 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C 10.1021/jm00361a004
DB00195 615 75 None -9 8 Guinea pig 7.0 pKd = 7.0 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
ChEMBL 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C 10.1021/jm00361a004
2369 615 75 None -9 8 Guinea pig 7.0 pKd = 7.0 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C 10.1021/jm00156a028
356 615 75 None -9 8 Guinea pig 7.0 pKd = 7.0 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C 10.1021/jm00156a028
549 615 75 None -9 8 Guinea pig 7.0 pKd = 7.0 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C 10.1021/jm00156a028
CHEMBL423 615 75 None -9 8 Guinea pig 7.0 pKd = 7.0 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C 10.1021/jm00156a028
DB00195 615 75 None -9 8 Guinea pig 7.0 pKd = 7.0 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C 10.1021/jm00156a028
16737588 85375 0 None 4 2 Human 5.0 pKd = 5.0 Binding
Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.
ChEMBL 273 6 4 4 2.0 Oc1cc(O)cc([C@@H](O)CNCCc2ccccc2)c1 nan
CHEMBL229620 85375 0 None 4 2 Human 5.0 pKd = 5.0 Binding
Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.
ChEMBL 273 6 4 4 2.0 Oc1cc(O)cc([C@@H](O)CNCCc2ccccc2)c1 nan
13621716 75580 0 None -165 2 Guinea pig 6.0 pKd = 6.0 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 387 11 3 6 3.2 CCOCCNC[C@H](O)COc1ccc(-c2nc(-c3cccs3)c[nH]2)cc1 10.1021/jm00156a028
CHEMBL2052005 75580 0 None -165 2 Guinea pig 6.0 pKd = 6.0 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 387 11 3 6 3.2 CCOCCNC[C@H](O)COc1ccc(-c2nc(-c3cccs3)c[nH]2)cc1 10.1021/jm00156a028
13621710 9194 0 None -478 2 Guinea pig 5.0 pKd = 5.0 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 453 11 3 6 4.0 COc1ccc(CCNCC(O)COc2ccc(-c3nc(C(C)(C)C)c[nH]3)cc2)cc1OC 10.1021/jm00156a028
CHEMBL11097 9194 0 None -478 2 Guinea pig 5.0 pKd = 5.0 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 453 11 3 6 4.0 COc1ccc(CCNCC(O)COc2ccc(-c3nc(C(C)(C)C)c[nH]3)cc2)cc1OC 10.1021/jm00156a028
2258 3104 36 None -1 2 Bovine 6.0 pKd = 6.0 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 225 6 3 4 1.1 O[C@H](COc1ccc(cc1)O)CNC(C)C 10.1021/jm00147a037
42396 3104 36 None -1 2 Bovine 6.0 pKd = 6.0 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 225 6 3 4 1.1 O[C@H](COc1ccc(cc1)O)CNC(C)C 10.1021/jm00147a037
537 3104 36 None -1 2 Bovine 6.0 pKd = 6.0 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 225 6 3 4 1.1 O[C@H](COc1ccc(cc1)O)CNC(C)C 10.1021/jm00147a037
CHEMBL1160714 3104 36 None -1 2 Bovine 6.0 pKd = 6.0 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 225 6 3 4 1.1 O[C@H](COc1ccc(cc1)O)CNC(C)C 10.1021/jm00147a037
DB13777 3104 36 None -1 2 Bovine 6.0 pKd = 6.0 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 225 6 3 4 1.1 O[C@H](COc1ccc(cc1)O)CNC(C)C 10.1021/jm00147a037
105 3392 84 None -5 6 Guinea pig 7.0 pKd = 7.0 Binding
Agonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring at basal tone assessed as bronchorelaxation activityAgonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring at basal tone assessed as bronchorelaxation activity
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1016/j.bmcl.2014.12.077
2083 3392 84 None -5 6 Guinea pig 7.0 pKd = 7.0 Binding
Agonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring at basal tone assessed as bronchorelaxation activityAgonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring at basal tone assessed as bronchorelaxation activity
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1016/j.bmcl.2014.12.077
558 3392 84 None -5 6 Guinea pig 7.0 pKd = 7.0 Binding
Agonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring at basal tone assessed as bronchorelaxation activityAgonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring at basal tone assessed as bronchorelaxation activity
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1016/j.bmcl.2014.12.077
CHEMBL714 3392 84 None -5 6 Guinea pig 7.0 pKd = 7.0 Binding
Agonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring at basal tone assessed as bronchorelaxation activityAgonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring at basal tone assessed as bronchorelaxation activity
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1016/j.bmcl.2014.12.077
DB01001 3392 84 None -5 6 Guinea pig 7.0 pKd = 7.0 Binding
Agonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring at basal tone assessed as bronchorelaxation activityAgonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring at basal tone assessed as bronchorelaxation activity
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1016/j.bmcl.2014.12.077
56597178 87817 0 None -10 2 Human 6.0 pKd = 6.0 Binding
Displacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 473 14 5 7 2.9 O=C(NCCNCC(O)COc1ccc(OCCOC2CCCC2)cc1)Nc1ccccc1O 10.1021/jm400348g
CHEMBL2348209 87817 0 None -10 2 Human 6.0 pKd = 6.0 Binding
Displacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 473 14 5 7 2.9 O=C(NCCNCC(O)COc1ccc(OCCOC2CCCC2)cc1)Nc1ccccc1O 10.1021/jm400348g
3067050 92973 1 None 3 2 Guinea pig 5.0 pKd = 5.0 Binding
Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.
ChEMBL 215 6 2 3 1.7 C=CC(C)(C)OCC(O)CNC(C)(C)C 10.1021/jm00376a011
CHEMBL24586 92973 1 None 3 2 Guinea pig 5.0 pKd = 5.0 Binding
Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.
ChEMBL 215 6 2 3 1.7 C=CC(C)(C)OCC(O)CNC(C)(C)C 10.1021/jm00376a011
45269924 193767 0 None - 1 Guinea pig 7.0 pKd = 7.0 Binding
Binding affinity to adrenergic beta2 receptor in Hartley guinea pig tracheal ringBinding affinity to adrenergic beta2 receptor in Hartley guinea pig tracheal ring
ChEMBL 283 6 5 6 -0.1 CC(C)(C)NC[C@@H](O)c1ccc(OB(O)O)c(CO)c1 10.1016/j.ejmech.2008.12.016
CHEMBL552398 193767 0 None - 1 Guinea pig 7.0 pKd = 7.0 Binding
Binding affinity to adrenergic beta2 receptor in Hartley guinea pig tracheal ringBinding affinity to adrenergic beta2 receptor in Hartley guinea pig tracheal ring
ChEMBL 283 6 5 6 -0.1 CC(C)(C)NC[C@@H](O)c1ccc(OB(O)O)c(CO)c1 10.1016/j.ejmech.2008.12.016
2419 3394 80 None 16 6 Human 6.0 pKd = 6.0 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation counting
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/acs.jmedchem.6b00358
5152 3394 80 None 16 6 Human 6.0 pKd = 6.0 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation counting
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/acs.jmedchem.6b00358
559 3394 80 None 16 6 Human 6.0 pKd = 6.0 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation counting
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/acs.jmedchem.6b00358
CHEMBL1263 3394 80 None 16 6 Human 6.0 pKd = 6.0 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation counting
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/acs.jmedchem.6b00358
DB00938 3394 80 None 16 6 Human 6.0 pKd = 6.0 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation counting
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/acs.jmedchem.6b00358
71662248 87805 0 None -75 2 Human 5.9 pKd = 5.9 Binding
Displacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 475 14 4 6 3.3 O=C(NCCNCC(O)COc1ccc(OCCOC2CCCC2)cc1)Nc1ccccc1F 10.1021/jm400348g
CHEMBL2348197 87805 0 None -75 2 Human 5.9 pKd = 5.9 Binding
Displacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 475 14 4 6 3.3 O=C(NCCNCC(O)COc1ccc(OCCOC2CCCC2)cc1)Nc1ccccc1F 10.1021/jm400348g
105 3392 84 None -5 6 Guinea pig 5.9 pKd = 5.9 Binding
Binding affinity to adrenergic beta2 receptor in Hartley guinea pig tracheal ringBinding affinity to adrenergic beta2 receptor in Hartley guinea pig tracheal ring
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1016/j.ejmech.2008.12.016
2083 3392 84 None -5 6 Guinea pig 5.9 pKd = 5.9 Binding
Binding affinity to adrenergic beta2 receptor in Hartley guinea pig tracheal ringBinding affinity to adrenergic beta2 receptor in Hartley guinea pig tracheal ring
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1016/j.ejmech.2008.12.016
558 3392 84 None -5 6 Guinea pig 5.9 pKd = 5.9 Binding
Binding affinity to adrenergic beta2 receptor in Hartley guinea pig tracheal ringBinding affinity to adrenergic beta2 receptor in Hartley guinea pig tracheal ring
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1016/j.ejmech.2008.12.016
CHEMBL714 3392 84 None -5 6 Guinea pig 5.9 pKd = 5.9 Binding
Binding affinity to adrenergic beta2 receptor in Hartley guinea pig tracheal ringBinding affinity to adrenergic beta2 receptor in Hartley guinea pig tracheal ring
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1016/j.ejmech.2008.12.016
DB01001 3392 84 None -5 6 Guinea pig 5.9 pKd = 5.9 Binding
Binding affinity to adrenergic beta2 receptor in Hartley guinea pig tracheal ringBinding affinity to adrenergic beta2 receptor in Hartley guinea pig tracheal ring
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1016/j.ejmech.2008.12.016
56599100 87823 0 None -12 2 Human 5.9 pKd = 5.9 Binding
Displacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 487 15 4 7 3.2 COc1ccccc1NC(=O)NCCNCC(O)COc1ccc(OCCOC2CCCC2)cc1 10.1021/jm400348g
CHEMBL2348215 87823 0 None -12 2 Human 5.9 pKd = 5.9 Binding
Displacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 487 15 4 7 3.2 COc1ccccc1NC(=O)NCCNCC(O)COc1ccc(OCCOC2CCCC2)cc1 10.1021/jm400348g
2249 509 106 None -6 12 Guinea pig 5.9 pKd = 5.9 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1021/jm00361a004
255 509 106 None -6 12 Guinea pig 5.9 pKd = 5.9 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1021/jm00361a004
548 509 106 None -6 12 Guinea pig 5.9 pKd = 5.9 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1021/jm00361a004
CHEMBL24 509 106 None -6 12 Guinea pig 5.9 pKd = 5.9 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1021/jm00361a004
DB00335 509 106 None -6 12 Guinea pig 5.9 pKd = 5.9 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1021/jm00361a004
2249 509 106 None -6 12 Guinea pig 5.9 pKd = 5.9 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1021/jm00156a028
255 509 106 None -6 12 Guinea pig 5.9 pKd = 5.9 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1021/jm00156a028
548 509 106 None -6 12 Guinea pig 5.9 pKd = 5.9 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1021/jm00156a028
CHEMBL24 509 106 None -6 12 Guinea pig 5.9 pKd = 5.9 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1021/jm00156a028
DB00335 509 106 None -6 12 Guinea pig 5.9 pKd = 5.9 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1021/jm00156a028
12548683 22625 0 None -2 2 Guinea pig 7.9 pKd = 7.9 Binding
Ability to block Beta-2 adrenergic receptor in guinea pig trachea preparationAbility to block Beta-2 adrenergic receptor in guinea pig trachea preparation
ChEMBL 267 7 2 5 1.2 COC(=O)c1ccccc1OCC(O)CNC(C)C 10.1021/jm00354a003
CHEMBL13284 22625 0 None -2 2 Guinea pig 7.9 pKd = 7.9 Binding
Ability to block Beta-2 adrenergic receptor in guinea pig trachea preparationAbility to block Beta-2 adrenergic receptor in guinea pig trachea preparation
ChEMBL 267 7 2 5 1.2 COC(=O)c1ccccc1OCC(O)CNC(C)C 10.1021/jm00354a003
13040886 99261 0 None 1 2 Guinea pig 7.9 pKd = 7.9 Binding
Ability to block Beta-2 adrenergic receptor in guinea pig trachea preparationAbility to block Beta-2 adrenergic receptor in guinea pig trachea preparation
ChEMBL 279 8 2 5 1.7 C=COC(=O)c1ccccc1OCC(O)CNC(C)C 10.1021/jm00354a003
CHEMBL284909 99261 0 None 1 2 Guinea pig 7.9 pKd = 7.9 Binding
Ability to block Beta-2 adrenergic receptor in guinea pig trachea preparationAbility to block Beta-2 adrenergic receptor in guinea pig trachea preparation
ChEMBL 279 8 2 5 1.7 C=COC(=O)c1ccccc1OCC(O)CNC(C)C 10.1021/jm00354a003
5464103 91091 16 None -1 2 Guinea pig 7.9 pKd = 7.9 Binding
Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.
ChEMBL 228 6 2 4 1.5 C/C(=N/OCC(O)CNC(C)(C)C)C1CC1 10.1021/jm00376a011
CHEMBL24045 91091 16 None -1 2 Guinea pig 7.9 pKd = 7.9 Binding
Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.
ChEMBL 228 6 2 4 1.5 C/C(=N/OCC(O)CNC(C)(C)C)C1CC1 10.1021/jm00376a011
6917762 9219 7 None 1 2 Guinea pig 7.9 pKd = 7.9 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor determined as pA2 in guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor determined as pA2 in guinea pig trachea
ChEMBL 228 6 2 4 1.5 C/C(=N\OCC(O)CNC(C)(C)C)C1CC1 10.1021/jm00145a008
CHEMBL111103 9219 7 None 1 2 Guinea pig 7.9 pKd = 7.9 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor determined as pA2 in guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor determined as pA2 in guinea pig trachea
ChEMBL 228 6 2 4 1.5 C/C(=N\OCC(O)CNC(C)(C)C)C1CC1 10.1021/jm00145a008
70695511 77492 1 None -1 2 Guinea pig 7.9 pKd = 7.9 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor determined as pA2 in guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor determined as pA2 in guinea pig trachea
ChEMBL 254 7 2 4 1.9 CC(C)(C)NC[C@H](O)CON=C(C1CC1)C1CC1 10.1021/jm00145a008
CHEMBL2093060 77492 1 None -1 2 Guinea pig 7.9 pKd = 7.9 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor determined as pA2 in guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor determined as pA2 in guinea pig trachea
ChEMBL 254 7 2 4 1.9 CC(C)(C)NC[C@H](O)CON=C(C1CC1)C1CC1 10.1021/jm00145a008
6917762 9219 7 None 1 2 Guinea pig 7.9 pKd = 7.9 Binding
The compound was tested for beta-adrenergic activity against Beta-2 adrenergic receptor from guinea pig trachea.The compound was tested for beta-adrenergic activity against Beta-2 adrenergic receptor from guinea pig trachea.
ChEMBL 228 6 2 4 1.5 C/C(=N\OCC(O)CNC(C)(C)C)C1CC1 10.1021/jm00115a008
CHEMBL111103 9219 7 None 1 2 Guinea pig 7.9 pKd = 7.9 Binding
The compound was tested for beta-adrenergic activity against Beta-2 adrenergic receptor from guinea pig trachea.The compound was tested for beta-adrenergic activity against Beta-2 adrenergic receptor from guinea pig trachea.
ChEMBL 228 6 2 4 1.5 C/C(=N\OCC(O)CNC(C)(C)C)C1CC1 10.1021/jm00115a008
24208809 109937 34 None 5 2 Guinea pig 6.9 pKd = 6.9 Binding
Antagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 minsAntagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 mins
ChEMBL 209 5 2 3 1.7 COc1ccccc1C(O)CNC(C)C 10.1021/jm00208a015
CHEMBL3246226 109937 34 None 5 2 Guinea pig 6.9 pKd = 6.9 Binding
Antagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 minsAntagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 mins
ChEMBL 209 5 2 3 1.7 COc1ccccc1C(O)CNC(C)C 10.1021/jm00208a015
2249 509 106 None -33 12 Human 5.9 pKd = 5.9 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation counting
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1021/acs.jmedchem.6b00358
255 509 106 None -33 12 Human 5.9 pKd = 5.9 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation counting
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1021/acs.jmedchem.6b00358
548 509 106 None -33 12 Human 5.9 pKd = 5.9 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation counting
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1021/acs.jmedchem.6b00358
CHEMBL24 509 106 None -33 12 Human 5.9 pKd = 5.9 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation counting
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1021/acs.jmedchem.6b00358
DB00335 509 106 None -33 12 Human 5.9 pKd = 5.9 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation counting
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1021/acs.jmedchem.6b00358
56599102 87807 0 None -60 2 Human 5.9 pKd = 5.9 Binding
Displacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 475 14 4 6 3.3 O=C(NCCNCC(O)COc1ccc(OCCOC2CCCC2)cc1)Nc1ccc(F)cc1 10.1021/jm400348g
CHEMBL2348199 87807 0 None -60 2 Human 5.9 pKd = 5.9 Binding
Displacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 475 14 4 6 3.3 O=C(NCCNCC(O)COc1ccc(OCCOC2CCCC2)cc1)Nc1ccc(F)cc1 10.1021/jm400348g
71662249 87810 0 None -109 2 Human 5.9 pKd = 5.9 Binding
Displacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 491 14 4 6 3.8 O=C(NCCNCC(O)COc1ccc(OCCOC2CCCC2)cc1)Nc1ccc(Cl)cc1 10.1021/jm400348g
CHEMBL2348202 87810 0 None -109 2 Human 5.9 pKd = 5.9 Binding
Displacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 491 14 4 6 3.8 O=C(NCCNCC(O)COc1ccc(OCCOC2CCCC2)cc1)Nc1ccc(Cl)cc1 10.1021/jm400348g
56598832 87826 0 None -588 3 Human 5.9 pKd = 5.9 Binding
Displacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 527 16 5 7 3.3 O=C(NCCNCC(O)COc1ccc(OCCOCCc2ccc(F)cc2)cc1)Nc1ccc(O)cc1 10.1021/jm400348g
CHEMBL2348218 87826 0 None -588 3 Human 5.9 pKd = 5.9 Binding
Displacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 527 16 5 7 3.3 O=C(NCCNCC(O)COc1ccc(OCCOCCc2ccc(F)cc2)cc1)Nc1ccc(O)cc1 10.1021/jm400348g
13157380 61793 0 None -2041 2 Guinea pig 4.9 pKd = 4.9 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
ChEMBL 493 12 3 7 4.8 COc1ccc(CC(C)NCC(O)COc2ccc(-c3nc(-c4cccs4)c[nH]3)cc2)cc1OC 10.1021/jm00361a004
CHEMBL177765 61793 0 None -2041 2 Guinea pig 4.9 pKd = 4.9 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
ChEMBL 493 12 3 7 4.8 COc1ccc(CC(C)NCC(O)COc2ccc(-c3nc(-c4cccs4)c[nH]3)cc2)cc1OC 10.1021/jm00361a004
11722868 103887 0 None -7 2 Guinea pig 5.9 pKd = 5.9 Binding
Ability to block Beta-2 adrenergic receptor in guinea pig trachea preparationAbility to block Beta-2 adrenergic receptor in guinea pig trachea preparation
ChEMBL 309 8 2 5 1.9 COC(=O)CCc1ccc(OCC(O)CNC(C)(C)C)cc1 10.1021/jm00354a003
CHEMBL31025 103887 0 None -7 2 Guinea pig 5.9 pKd = 5.9 Binding
Ability to block Beta-2 adrenergic receptor in guinea pig trachea preparationAbility to block Beta-2 adrenergic receptor in guinea pig trachea preparation
ChEMBL 309 8 2 5 1.9 COC(=O)CCc1ccc(OCC(O)CNC(C)(C)C)cc1 10.1021/jm00354a003
2249 509 106 None -6 12 Guinea pig 5.9 pKd = 5.9 Binding
Antagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 minsAntagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 mins
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1021/jm00208a015
255 509 106 None -6 12 Guinea pig 5.9 pKd = 5.9 Binding
Antagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 minsAntagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 mins
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1021/jm00208a015
548 509 106 None -6 12 Guinea pig 5.9 pKd = 5.9 Binding
Antagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 minsAntagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 mins
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1021/jm00208a015
CHEMBL24 509 106 None -6 12 Guinea pig 5.9 pKd = 5.9 Binding
Antagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 minsAntagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 mins
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1021/jm00208a015
DB00335 509 106 None -6 12 Guinea pig 5.9 pKd = 5.9 Binding
Antagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 minsAntagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 mins
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1021/jm00208a015
60903220 109939 2 None -1 2 Guinea pig 5.9 pKd = 5.9 Binding
Antagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 minsAntagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 mins
ChEMBL 257 4 2 2 2.5 CC(C)NCC(O)c1cccc(Br)c1 10.1021/jm00208a015
CHEMBL3246229 109939 2 None -1 2 Guinea pig 5.9 pKd = 5.9 Binding
Antagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 minsAntagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 mins
ChEMBL 257 4 2 2 2.5 CC(C)NCC(O)c1cccc(Br)c1 10.1021/jm00208a015
2725073 98675 52 None -10 2 Guinea pig 5.9 pKd = 5.9 Binding
In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.
ChEMBL 167 4 2 3 0.4 NCC(O)COc1ccccc1 10.1021/jm00354a002
CHEMBL281109 98675 52 None -10 2 Guinea pig 5.9 pKd = 5.9 Binding
In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.
ChEMBL 167 4 2 3 0.4 NCC(O)COc1ccccc1 10.1021/jm00354a002
15578573 106865 2 None -25 2 Guinea pig 5.9 pKd = 5.9 Binding
In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.
ChEMBL 267 9 2 5 1.0 CCOC(=O)CCNCC(O)COc1ccccc1 10.1021/jm00354a002
CHEMBL31772 106865 2 None -25 2 Guinea pig 5.9 pKd = 5.9 Binding
In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.
ChEMBL 267 9 2 5 1.0 CCOC(=O)CCNCC(O)COc1ccccc1 10.1021/jm00354a002
13040905 106057 0 None -10 2 Guinea pig 4.9 pKd = 4.9 Binding
Ability to block Beta-2 adrenergic receptor in guinea pig trachea preparationAbility to block Beta-2 adrenergic receptor in guinea pig trachea preparation
ChEMBL 343 10 2 5 2.3 COC(=O)CCc1ccc(OCC(O)CNCc2ccccc2)cc1 10.1021/jm00354a003
CHEMBL31416 106057 0 None -10 2 Guinea pig 4.9 pKd = 4.9 Binding
Ability to block Beta-2 adrenergic receptor in guinea pig trachea preparationAbility to block Beta-2 adrenergic receptor in guinea pig trachea preparation
ChEMBL 343 10 2 5 2.3 COC(=O)CCc1ccc(OCC(O)CNCc2ccccc2)cc1 10.1021/jm00354a003
15578598 99754 2 None -7 2 Guinea pig 4.9 pKd = 4.9 Binding
In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.
ChEMBL 297 10 2 6 1.0 CCOC(=O)CCNCC(O)COc1ccc(OC)cc1 10.1021/jm00354a002
CHEMBL288546 99754 2 None -7 2 Guinea pig 4.9 pKd = 4.9 Binding
In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.
ChEMBL 297 10 2 6 1.0 CCOC(=O)CCNCC(O)COc1ccc(OC)cc1 10.1021/jm00354a002
23844 10089 24 None - 1 Bovine 5.9 pKd = 5.9 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 209 3 3 3 1.8 CC(C)(C)NCC(O)c1ccc(O)cc1 10.1021/jm00147a037
CHEMBL1159887 10089 24 None - 1 Bovine 5.9 pKd = 5.9 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 209 3 3 3 1.8 CC(C)(C)NCC(O)c1ccc(O)cc1 10.1021/jm00147a037
21493193 110904 0 None - 1 Guinea pig 6.9 pKd = 6.9 Binding
Antagonist activity at beta-2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of isoprenaline-induced effectAntagonist activity at beta-2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of isoprenaline-induced effect
ChEMBL 394 12 4 6 2.0 CC(C)NCC(O)COc1cc2c(cc1OCC(O)CNC(C)C)CCCC2 10.1021/jm00214a013
CHEMBL3272439 110904 0 None - 1 Guinea pig 6.9 pKd = 6.9 Binding
Antagonist activity at beta-2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of isoprenaline-induced effectAntagonist activity at beta-2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of isoprenaline-induced effect
ChEMBL 394 12 4 6 2.0 CC(C)NCC(O)COc1cc2c(cc1OCC(O)CNC(C)C)CCCC2 10.1021/jm00214a013
13157365 127274 0 None -239 2 Guinea pig 5.9 pKd = 5.9 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
ChEMBL 465 11 3 6 3.7 COc1ccc(CCNCC(O)COc2ccc(-c3nc(C(F)(F)F)c[nH]3)cc2)cc1OC 10.1021/jm00361a004
CHEMBL366389 127274 0 None -239 2 Guinea pig 5.9 pKd = 5.9 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
ChEMBL 465 11 3 6 3.7 COc1ccc(CCNCC(O)COc2ccc(-c3nc(C(F)(F)F)c[nH]3)cc2)cc1OC 10.1021/jm00361a004
12462216 112159 0 None -2 2 Guinea pig 7.9 pKd = 7.9 Binding
Antagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 minsAntagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 mins
ChEMBL 287 5 2 3 2.5 COc1cc(Br)ccc1C(O)CNC(C)C 10.1021/jm00208a015
CHEMBL3246228 112159 0 None -2 2 Guinea pig 7.9 pKd = 7.9 Binding
Antagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 minsAntagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 mins
ChEMBL 287 5 2 3 2.5 COc1cc(Br)ccc1C(O)CNC(C)C 10.1021/jm00208a015
CHEMBL3303705 112159 0 None -2 2 Guinea pig 7.9 pKd = 7.9 Binding
Antagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 minsAntagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 mins
ChEMBL 287 5 2 3 2.5 COc1cc(Br)ccc1C(O)CNC(C)C 10.1021/jm00208a015
5606 10083 63 None - 1 Bovine 6.9 pKd = 6.9 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 227 3 2 2 2.8 CC(C)(C)NCC(O)c1ccccc1Cl 10.1021/jm00147a037
CHEMBL1159717 10083 63 None - 1 Bovine 6.9 pKd = 6.9 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 227 3 2 2 2.8 CC(C)(C)NCC(O)c1ccccc1Cl 10.1021/jm00147a037
1499 2052 43 None -33 17 Human 6.9 pKd = 6.9 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation counting
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/acs.jmedchem.6b00358
3779 2052 43 None -33 17 Human 6.9 pKd = 6.9 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation counting
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/acs.jmedchem.6b00358
536 2052 43 None -33 17 Human 6.9 pKd = 6.9 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation counting
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/acs.jmedchem.6b00358
CHEMBL434 2052 43 None -33 17 Human 6.9 pKd = 6.9 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation counting
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/acs.jmedchem.6b00358
DB01064 2052 43 None -33 17 Human 6.9 pKd = 6.9 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation counting
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/acs.jmedchem.6b00358
1786 2474 79 None -25 11 Human 6.9 pKd = 6.9 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation counting
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/acs.jmedchem.6b00358
4171 2474 79 None -25 11 Human 6.9 pKd = 6.9 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation counting
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/acs.jmedchem.6b00358
553 2474 79 None -25 11 Human 6.9 pKd = 6.9 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation counting
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/acs.jmedchem.6b00358
CHEMBL13 2474 79 None -25 11 Human 6.9 pKd = 6.9 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation counting
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/acs.jmedchem.6b00358
DB00264 2474 79 None -25 11 Human 6.9 pKd = 6.9 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation counting
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/acs.jmedchem.6b00358
13157406 9324 0 None -144 2 Guinea pig 6.9 pKd = 6.9 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
ChEMBL 357 8 3 5 3.5 CC(C)NCC(O)COc1ccc(-c2nc(-c3cccs3)c[nH]2)cc1 10.1021/jm00361a004
CHEMBL11171 9324 0 None -144 2 Guinea pig 6.9 pKd = 6.9 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
ChEMBL 357 8 3 5 3.5 CC(C)NCC(O)COc1ccc(-c2nc(-c3cccs3)c[nH]2)cc1 10.1021/jm00361a004
6317 18308 36 None - 1 Bovine 5.9 pKd = 5.9 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 224 5 2 4 1.6 CC(C)NCC(O)c1ccc([N+](=O)[O-])cc1 10.1021/jm00147a037
CHEMBL127349 18308 36 None - 1 Bovine 5.9 pKd = 5.9 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 224 5 2 4 1.6 CC(C)NCC(O)c1ccc([N+](=O)[O-])cc1 10.1021/jm00147a037
56599097 87804 0 None -87 2 Human 5.9 pKd = 5.9 Binding
Displacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 487 15 4 7 3.2 COc1ccc(NC(=O)NCCNCC(O)COc2ccc(OCCOC3CCCC3)cc2)cc1 10.1021/jm400348g
CHEMBL2348196 87804 0 None -87 2 Human 5.9 pKd = 5.9 Binding
Displacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 487 15 4 7 3.2 COc1ccc(NC(=O)NCCNCC(O)COc2ccc(OCCOC3CCCC3)cc2)cc1 10.1021/jm400348g
56599231 87813 0 None -81 2 Human 5.9 pKd = 5.9 Binding
Displacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 535 14 4 6 3.9 O=C(NCCNCC(O)COc1ccc(OCCOC2CCCC2)cc1)Nc1ccc(Br)cc1 10.1021/jm400348g
CHEMBL2348205 87813 0 None -81 2 Human 5.9 pKd = 5.9 Binding
Displacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 535 14 4 6 3.9 O=C(NCCNCC(O)COc1ccc(OCCOC2CCCC2)cc1)Nc1ccc(Br)cc1 10.1021/jm400348g
56599232 87815 0 None -81 2 Human 5.9 pKd = 5.9 Binding
Displacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 525 14 4 6 4.2 O=C(NCCNCC(O)COc1ccc(OCCOC2CCCC2)cc1)Nc1cccc(C(F)(F)F)c1 10.1021/jm400348g
CHEMBL2348207 87815 0 None -81 2 Human 5.9 pKd = 5.9 Binding
Displacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 525 14 4 6 4.2 O=C(NCCNCC(O)COc1ccc(OCCOC2CCCC2)cc1)Nc1cccc(C(F)(F)F)c1 10.1021/jm400348g
1155 1592 45 None 2 5 Human 6.9 pKd = 6.9 Binding
Binding affinity to N-terminal FLAG-tagged C-terminal His-10-tagged human beta2 adrenoceptor expressed in insect Sf9 cells by surface plasmon resonance analysisBinding affinity to N-terminal FLAG-tagged C-terminal His-10-tagged human beta2 adrenoceptor expressed in insect Sf9 cells by surface plasmon resonance analysis
ChEMBL 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 10.1021/ml400312j
3343 1592 45 None 2 5 Human 6.9 pKd = 6.9 Binding
Binding affinity to N-terminal FLAG-tagged C-terminal His-10-tagged human beta2 adrenoceptor expressed in insect Sf9 cells by surface plasmon resonance analysisBinding affinity to N-terminal FLAG-tagged C-terminal His-10-tagged human beta2 adrenoceptor expressed in insect Sf9 cells by surface plasmon resonance analysis
ChEMBL 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 10.1021/ml400312j
557 1592 45 None 2 5 Human 6.9 pKd = 6.9 Binding
Binding affinity to N-terminal FLAG-tagged C-terminal His-10-tagged human beta2 adrenoceptor expressed in insect Sf9 cells by surface plasmon resonance analysisBinding affinity to N-terminal FLAG-tagged C-terminal His-10-tagged human beta2 adrenoceptor expressed in insect Sf9 cells by surface plasmon resonance analysis
ChEMBL 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 10.1021/ml400312j
CHEMBL32800 1592 45 None 2 5 Human 6.9 pKd = 6.9 Binding
Binding affinity to N-terminal FLAG-tagged C-terminal His-10-tagged human beta2 adrenoceptor expressed in insect Sf9 cells by surface plasmon resonance analysisBinding affinity to N-terminal FLAG-tagged C-terminal His-10-tagged human beta2 adrenoceptor expressed in insect Sf9 cells by surface plasmon resonance analysis
ChEMBL 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 10.1021/ml400312j
DB01288 1592 45 None 2 5 Human 6.9 pKd = 6.9 Binding
Binding affinity to N-terminal FLAG-tagged C-terminal His-10-tagged human beta2 adrenoceptor expressed in insect Sf9 cells by surface plasmon resonance analysisBinding affinity to N-terminal FLAG-tagged C-terminal His-10-tagged human beta2 adrenoceptor expressed in insect Sf9 cells by surface plasmon resonance analysis
ChEMBL 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 10.1021/ml400312j
165193 3126 60 None -4 43 Guinea pig 7.8 pKd = 7.8 Binding
Competitive antagonist activity at beta-2 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced tracheal relaxationCompetitive antagonist activity at beta-2 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced tracheal relaxation
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00188a019
2303 3126 60 None -4 43 Guinea pig 7.8 pKd = 7.8 Binding
Competitive antagonist activity at beta-2 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced tracheal relaxationCompetitive antagonist activity at beta-2 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced tracheal relaxation
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00188a019
4946 3126 60 None -4 43 Guinea pig 7.8 pKd = 7.8 Binding
Competitive antagonist activity at beta-2 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced tracheal relaxationCompetitive antagonist activity at beta-2 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced tracheal relaxation
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00188a019
564 3126 60 None -4 43 Guinea pig 7.8 pKd = 7.8 Binding
Competitive antagonist activity at beta-2 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced tracheal relaxationCompetitive antagonist activity at beta-2 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced tracheal relaxation
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00188a019
62882 3126 60 None -4 43 Guinea pig 7.8 pKd = 7.8 Binding
Competitive antagonist activity at beta-2 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced tracheal relaxationCompetitive antagonist activity at beta-2 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced tracheal relaxation
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00188a019
63 3126 60 None -4 43 Guinea pig 7.8 pKd = 7.8 Binding
Competitive antagonist activity at beta-2 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced tracheal relaxationCompetitive antagonist activity at beta-2 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced tracheal relaxation
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00188a019
66366 3126 60 None -4 43 Guinea pig 7.8 pKd = 7.8 Binding
Competitive antagonist activity at beta-2 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced tracheal relaxationCompetitive antagonist activity at beta-2 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced tracheal relaxation
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00188a019
91536 3126 60 None -4 43 Guinea pig 7.8 pKd = 7.8 Binding
Competitive antagonist activity at beta-2 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced tracheal relaxationCompetitive antagonist activity at beta-2 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced tracheal relaxation
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00188a019
CHEMBL27 3126 60 None -4 43 Guinea pig 7.8 pKd = 7.8 Binding
Competitive antagonist activity at beta-2 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced tracheal relaxationCompetitive antagonist activity at beta-2 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced tracheal relaxation
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00188a019
CHEMBL452861 3126 60 None -4 43 Guinea pig 7.8 pKd = 7.8 Binding
Competitive antagonist activity at beta-2 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced tracheal relaxationCompetitive antagonist activity at beta-2 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced tracheal relaxation
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00188a019
DB00571 3126 60 None -4 43 Guinea pig 7.8 pKd = 7.8 Binding
Competitive antagonist activity at beta-2 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced tracheal relaxationCompetitive antagonist activity at beta-2 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced tracheal relaxation
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00188a019
105 3392 84 None -10 6 Human 5.9 pKd = 5.9 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation counting
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1021/acs.jmedchem.6b00358
2083 3392 84 None -10 6 Human 5.9 pKd = 5.9 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation counting
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1021/acs.jmedchem.6b00358
558 3392 84 None -10 6 Human 5.9 pKd = 5.9 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation counting
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1021/acs.jmedchem.6b00358
CHEMBL714 3392 84 None -10 6 Human 5.9 pKd = 5.9 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation counting
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1021/acs.jmedchem.6b00358
DB01001 3392 84 None -10 6 Human 5.9 pKd = 5.9 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation counting
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1021/acs.jmedchem.6b00358
66653395 87818 0 None -109 2 Human 5.9 pKd = 5.9 Binding
Displacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 473 14 5 7 2.9 O=C(NCCNCC(O)COc1ccc(OCCOC2CCCC2)cc1)Nc1cccc(O)c1 10.1021/jm400348g
CHEMBL2348210 87818 0 None -109 2 Human 5.9 pKd = 5.9 Binding
Displacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 473 14 5 7 2.9 O=C(NCCNCC(O)COc1ccc(OCCOC2CCCC2)cc1)Nc1cccc(O)c1 10.1021/jm400348g
70517 116526 110 None - 1 Human 3.9 pKd = 3.9 Binding
Binding affinity to N-terminal FLAG-tagged C-terminal His-10-tagged human beta2 adrenoceptor expressed in insect Sf9 cells by surface plasmon resonance analysis in presence of maltose neopentyl glycolBinding affinity to N-terminal FLAG-tagged C-terminal His-10-tagged human beta2 adrenoceptor expressed in insect Sf9 cells by surface plasmon resonance analysis in presence of maltose neopentyl glycol
ChEMBL 163 1 1 3 0.5 c1cc(N2CCNCC2)ccn1 10.1021/ml400312j
CHEMBL339069 116526 110 None - 1 Human 3.9 pKd = 3.9 Binding
Binding affinity to N-terminal FLAG-tagged C-terminal His-10-tagged human beta2 adrenoceptor expressed in insect Sf9 cells by surface plasmon resonance analysis in presence of maltose neopentyl glycolBinding affinity to N-terminal FLAG-tagged C-terminal His-10-tagged human beta2 adrenoceptor expressed in insect Sf9 cells by surface plasmon resonance analysis in presence of maltose neopentyl glycol
ChEMBL 163 1 1 3 0.5 c1cc(N2CCNCC2)ccn1 10.1021/ml400312j
123686 1942 44 None -109 9 Human 6.8 pKd = 6.8 Binding
Displacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 354 9 4 5 1.7 C1=CC=C(C=C1)NC(=O)NCCNCC(COC2=CC=CC=C2C#N)O 10.1021/jm400348g
12581 1942 44 None -109 9 Human 6.8 pKd = 6.8 Binding
Displacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 354 9 4 5 1.7 C1=CC=C(C=C1)NC(=O)NCCNCC(COC2=CC=CC=C2C#N)O 10.1021/jm400348g
CHEMBL11268 1942 44 None -109 9 Human 6.8 pKd = 6.8 Binding
Displacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 354 9 4 5 1.7 C1=CC=C(C=C1)NC(=O)NCCNCC(COC2=CC=CC=C2C#N)O 10.1021/jm400348g
12878481 59659 0 None -169 2 Guinea pig 6.8 pKd = 6.8 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
ChEMBL 341 7 3 4 2.6 OC(CNC1CC1)COc1ccc(-c2nc(C(F)(F)F)c[nH]2)cc1 10.1021/jm00361a004
CHEMBL173424 59659 0 None -169 2 Guinea pig 6.8 pKd = 6.8 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
ChEMBL 341 7 3 4 2.6 OC(CNC1CC1)COc1ccc(-c2nc(C(F)(F)F)c[nH]2)cc1 10.1021/jm00361a004
2685 875 15 None -1096 7 Human 5.8 pKd = 5.8 Binding
Displacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting methodDisplacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting method
ChEMBL 494 11 4 8 2.3 OC(COc1ccc(cc1)c1nc(cn1C)C(F)(F)F)CNCCOc1ccc(c(c1)C(=O)N)O 10.1021/acsmedchemlett.6b00363
541 875 15 None -1096 7 Human 5.8 pKd = 5.8 Binding
Displacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting methodDisplacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting method
ChEMBL 494 11 4 8 2.3 OC(COc1ccc(cc1)c1nc(cn1C)C(F)(F)F)CNCCOc1ccc(c(c1)C(=O)N)O 10.1021/acsmedchemlett.6b00363
CHEMBL280822 875 15 None -1096 7 Human 5.8 pKd = 5.8 Binding
Displacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting methodDisplacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting method
ChEMBL 494 11 4 8 2.3 OC(COc1ccc(cc1)c1nc(cn1C)C(F)(F)F)CNCCOc1ccc(c(c1)C(=O)N)O 10.1021/acsmedchemlett.6b00363
71662410 87814 0 None -12 2 Human 5.8 pKd = 5.8 Binding
Displacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 525 14 4 6 4.2 O=C(NCCNCC(O)COc1ccc(OCCOC2CCCC2)cc1)Nc1ccccc1C(F)(F)F 10.1021/jm400348g
CHEMBL2348206 87814 0 None -12 2 Human 5.8 pKd = 5.8 Binding
Displacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 525 14 4 6 4.2 O=C(NCCNCC(O)COc1ccc(OCCOC2CCCC2)cc1)Nc1ccccc1C(F)(F)F 10.1021/jm400348g
16415941 158506 12 None 2 2 Human 4.8 pKd = 4.8 Binding
Displacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting methodDisplacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting method
ChEMBL 375 3 1 5 4.7 Cc1cc(O)c(CN2CCCC2)c2c1C(=O)/C(=C/c1cc3ccccc3o1)O2 10.1021/acsmedchemlett.6b00363
16415942 158506 12 None 2 2 Human 4.8 pKd = 4.8 Binding
Displacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting methodDisplacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting method
ChEMBL 375 3 1 5 4.7 Cc1cc(O)c(CN2CCCC2)c2c1C(=O)/C(=C/c1cc3ccccc3o1)O2 10.1021/acsmedchemlett.6b00363
CHEMBL4097144 158506 12 None 2 2 Human 4.8 pKd = 4.8 Binding
Displacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting methodDisplacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting method
ChEMBL 375 3 1 5 4.7 Cc1cc(O)c(CN2CCCC2)c2c1C(=O)/C(=C/c1cc3ccccc3o1)O2 10.1021/acsmedchemlett.6b00363
21493193 110904 0 None - 1 Guinea pig 5.8 pKd = 5.8 Binding
Antagonist activity at beta-2 adrenergic receptor in guinea pig right atrium assessed as inhibition of isoprenaline-induced effectAntagonist activity at beta-2 adrenergic receptor in guinea pig right atrium assessed as inhibition of isoprenaline-induced effect
ChEMBL 394 12 4 6 2.0 CC(C)NCC(O)COc1cc2c(cc1OCC(O)CNC(C)C)CCCC2 10.1021/jm00214a013
CHEMBL3272439 110904 0 None - 1 Guinea pig 5.8 pKd = 5.8 Binding
Antagonist activity at beta-2 adrenergic receptor in guinea pig right atrium assessed as inhibition of isoprenaline-induced effectAntagonist activity at beta-2 adrenergic receptor in guinea pig right atrium assessed as inhibition of isoprenaline-induced effect
ChEMBL 394 12 4 6 2.0 CC(C)NCC(O)COc1cc2c(cc1OCC(O)CNC(C)C)CCCC2 10.1021/jm00214a013
13040919 105574 0 None 19 2 Guinea pig 7.8 pKd = 7.8 Binding
Ability to block Beta-2 adrenergic receptor in guinea pig trachea preparationAbility to block Beta-2 adrenergic receptor in guinea pig trachea preparation
ChEMBL 339 9 2 7 1.1 CCOC(=O)C(C)(C)NCC(O)COc1ccccc1C(=O)OC 10.1021/jm00354a003
CHEMBL31335 105574 0 None 19 2 Guinea pig 7.8 pKd = 7.8 Binding
Ability to block Beta-2 adrenergic receptor in guinea pig trachea preparationAbility to block Beta-2 adrenergic receptor in guinea pig trachea preparation
ChEMBL 339 9 2 7 1.1 CCOC(=O)C(C)(C)NCC(O)COc1ccccc1C(=O)OC 10.1021/jm00354a003
12582 935 40 None -11 5 Human 7.8 pKd = 7.8 Binding
Binding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nMBinding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nM
ChEMBL 276 3 3 3 3.0 CC(C)(C)NCC(C1=CC(=C(C(=C1)Cl)N)Cl)O 10.1016/j.bmcl.2013.07.052
2783 935 40 None -11 5 Human 7.8 pKd = 7.8 Binding
Binding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nMBinding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nM
ChEMBL 276 3 3 3 3.0 CC(C)(C)NCC(C1=CC(=C(C(=C1)Cl)N)Cl)O 10.1016/j.bmcl.2013.07.052
CHEMBL49080 935 40 None -11 5 Human 7.8 pKd = 7.8 Binding
Binding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nMBinding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nM
ChEMBL 276 3 3 3 3.0 CC(C)(C)NCC(C1=CC(=C(C(=C1)Cl)N)Cl)O 10.1016/j.bmcl.2013.07.052
DB01407 935 40 None -11 5 Human 7.8 pKd = 7.8 Binding
Binding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nMBinding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nM
ChEMBL 276 3 3 3 3.0 CC(C)(C)NCC(C1=CC(=C(C(=C1)Cl)N)Cl)O 10.1016/j.bmcl.2013.07.052
165193 3126 60 None 1 43 Human 6.8 pKd = 6.8 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation counting
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/acs.jmedchem.6b00358
2303 3126 60 None 1 43 Human 6.8 pKd = 6.8 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation counting
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/acs.jmedchem.6b00358
4946 3126 60 None 1 43 Human 6.8 pKd = 6.8 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation counting
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/acs.jmedchem.6b00358
564 3126 60 None 1 43 Human 6.8 pKd = 6.8 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation counting
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/acs.jmedchem.6b00358
62882 3126 60 None 1 43 Human 6.8 pKd = 6.8 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation counting
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/acs.jmedchem.6b00358
63 3126 60 None 1 43 Human 6.8 pKd = 6.8 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation counting
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/acs.jmedchem.6b00358
66366 3126 60 None 1 43 Human 6.8 pKd = 6.8 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation counting
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/acs.jmedchem.6b00358
91536 3126 60 None 1 43 Human 6.8 pKd = 6.8 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation counting
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/acs.jmedchem.6b00358
CHEMBL27 3126 60 None 1 43 Human 6.8 pKd = 6.8 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation counting
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/acs.jmedchem.6b00358
CHEMBL452861 3126 60 None 1 43 Human 6.8 pKd = 6.8 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation counting
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/acs.jmedchem.6b00358
DB00571 3126 60 None 1 43 Human 6.8 pKd = 6.8 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation counting
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/acs.jmedchem.6b00358
2405 658 71 None -58 4 Human 6.8 pKd = 6.8 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation counting
ChEMBL 325 12 2 5 2.4 OC(COc1ccc(cc1)COCCOC(C)C)CNC(C)C 10.1021/acs.jmedchem.6b00358
380 658 71 None -58 4 Human 6.8 pKd = 6.8 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation counting
ChEMBL 325 12 2 5 2.4 OC(COc1ccc(cc1)COCCOC(C)C)CNC(C)C 10.1021/acs.jmedchem.6b00358
7129 658 71 None -58 4 Human 6.8 pKd = 6.8 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation counting
ChEMBL 325 12 2 5 2.4 OC(COc1ccc(cc1)COCCOC(C)C)CNC(C)C 10.1021/acs.jmedchem.6b00358
CHEMBL645 658 71 None -58 4 Human 6.8 pKd = 6.8 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation counting
ChEMBL 325 12 2 5 2.4 OC(COc1ccc(cc1)COCCOC(C)C)CNC(C)C 10.1021/acs.jmedchem.6b00358
DB00612 658 71 None -58 4 Human 6.8 pKd = 6.8 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation counting
ChEMBL 325 12 2 5 2.4 OC(COc1ccc(cc1)COCCOC(C)C)CNC(C)C 10.1021/acs.jmedchem.6b00358
2685 875 15 None -1096 7 Human 5.8 pKd = 5.8 Binding
Displacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 494 11 4 8 2.3 OC(COc1ccc(cc1)c1nc(cn1C)C(F)(F)F)CNCCOc1ccc(c(c1)C(=O)N)O 10.1021/jm400348g
541 875 15 None -1096 7 Human 5.8 pKd = 5.8 Binding
Displacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 494 11 4 8 2.3 OC(COc1ccc(cc1)c1nc(cn1C)C(F)(F)F)CNCCOc1ccc(c(c1)C(=O)N)O 10.1021/jm400348g
CHEMBL280822 875 15 None -1096 7 Human 5.8 pKd = 5.8 Binding
Displacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 494 11 4 8 2.3 OC(COc1ccc(cc1)c1nc(cn1C)C(F)(F)F)CNCCOc1ccc(c(c1)C(=O)N)O 10.1021/jm400348g
13621706 8955 0 None -154 2 Guinea pig 5.8 pKd = 5.8 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 317 8 3 4 2.9 CC(C)NCC(O)COc1ccc(-c2nc(C(C)C)c[nH]2)cc1 10.1021/jm00156a028
CHEMBL10988 8955 0 None -154 2 Guinea pig 5.8 pKd = 5.8 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 317 8 3 4 2.9 CC(C)NCC(O)COc1ccc(-c2nc(C(C)C)c[nH]2)cc1 10.1021/jm00156a028
13621593 9185 0 None -204 2 Guinea pig 5.8 pKd = 5.8 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 509 11 3 6 4.1 COc1ccc(CCNCC(O)COc2ccc(-c3nc(Br)c[nH]3)cc2Cl)cc1OC 10.1021/jm00156a028
CHEMBL11092 9185 0 None -204 2 Guinea pig 5.8 pKd = 5.8 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 509 11 3 6 4.1 COc1ccc(CCNCC(O)COc2ccc(-c3nc(Br)c[nH]3)cc2Cl)cc1OC 10.1021/jm00156a028
1786 2474 79 None -25 11 Human 4.8 pKd = 4.8 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation counting
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/acs.jmedchem.6b00358
4171 2474 79 None -25 11 Human 4.8 pKd = 4.8 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation counting
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/acs.jmedchem.6b00358
553 2474 79 None -25 11 Human 4.8 pKd = 4.8 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation counting
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/acs.jmedchem.6b00358
CHEMBL13 2474 79 None -25 11 Human 4.8 pKd = 4.8 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation counting
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/acs.jmedchem.6b00358
DB00264 2474 79 None -25 11 Human 4.8 pKd = 4.8 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation counting
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/acs.jmedchem.6b00358
3322591 112270 2 None - 1 Guinea pig 6.8 pKd = 6.8 Binding
Antagonist activity at beta-2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of isoprenaline-induced effectAntagonist activity at beta-2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of isoprenaline-induced effect
ChEMBL 390 12 4 6 2.3 CC(C)NCC(O)COc1cc2ccccc2cc1OCC(O)CNC(C)C 10.1021/jm00214a013
CHEMBL3272440 112270 2 None - 1 Guinea pig 6.8 pKd = 6.8 Binding
Antagonist activity at beta-2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of isoprenaline-induced effectAntagonist activity at beta-2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of isoprenaline-induced effect
ChEMBL 390 12 4 6 2.3 CC(C)NCC(O)COc1cc2ccccc2cc1OCC(O)CNC(C)C 10.1021/jm00214a013
CHEMBL3305652 112270 2 None - 1 Guinea pig 6.8 pKd = 6.8 Binding
Antagonist activity at beta-2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of isoprenaline-induced effectAntagonist activity at beta-2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of isoprenaline-induced effect
ChEMBL 390 12 4 6 2.3 CC(C)NCC(O)COc1cc2ccccc2cc1OCC(O)CNC(C)C 10.1021/jm00214a013
3486 3096 51 None -30 11 Guinea pig 5.8 pKd = 5.8 Binding
Ability to block Beta-2 adrenergic receptor in guinea pig trachea preparationAbility to block Beta-2 adrenergic receptor in guinea pig trachea preparation
ChEMBL 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C 10.1021/jm00354a003
4883 3096 51 None -30 11 Guinea pig 5.8 pKd = 5.8 Binding
Ability to block Beta-2 adrenergic receptor in guinea pig trachea preparationAbility to block Beta-2 adrenergic receptor in guinea pig trachea preparation
ChEMBL 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C 10.1021/jm00354a003
555 3096 51 None -30 11 Guinea pig 5.8 pKd = 5.8 Binding
Ability to block Beta-2 adrenergic receptor in guinea pig trachea preparationAbility to block Beta-2 adrenergic receptor in guinea pig trachea preparation
ChEMBL 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C 10.1021/jm00354a003
CHEMBL6995 3096 51 None -30 11 Guinea pig 5.8 pKd = 5.8 Binding
Ability to block Beta-2 adrenergic receptor in guinea pig trachea preparationAbility to block Beta-2 adrenergic receptor in guinea pig trachea preparation
ChEMBL 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C 10.1021/jm00354a003
DB01297 3096 51 None -30 11 Guinea pig 5.8 pKd = 5.8 Binding
Ability to block Beta-2 adrenergic receptor in guinea pig trachea preparationAbility to block Beta-2 adrenergic receptor in guinea pig trachea preparation
ChEMBL 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C 10.1021/jm00354a003
3527871 112263 1 None - 1 Guinea pig 5.8 pKd = 5.8 Binding
Antagonist activity at beta-2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of isoprenaline-induced effectAntagonist activity at beta-2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of isoprenaline-induced effect
ChEMBL 354 12 4 6 1.5 Cc1cccc(OCC(O)CNC(C)C)c1OCC(O)CNC(C)C 10.1021/jm00214a013
CHEMBL3272435 112263 1 None - 1 Guinea pig 5.8 pKd = 5.8 Binding
Antagonist activity at beta-2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of isoprenaline-induced effectAntagonist activity at beta-2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of isoprenaline-induced effect
ChEMBL 354 12 4 6 1.5 Cc1cccc(OCC(O)CNC(C)C)c1OCC(O)CNC(C)C 10.1021/jm00214a013
CHEMBL3305474 112263 1 None - 1 Guinea pig 5.8 pKd = 5.8 Binding
Antagonist activity at beta-2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of isoprenaline-induced effectAntagonist activity at beta-2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of isoprenaline-induced effect
ChEMBL 354 12 4 6 1.5 Cc1cccc(OCC(O)CNC(C)C)c1OCC(O)CNC(C)C 10.1021/jm00214a013
56599099 87822 0 None -91 2 Human 5.8 pKd = 5.8 Binding
Displacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 471 14 4 6 3.5 Cc1ccc(NC(=O)NCCNCC(O)COc2ccc(OCCOC3CCCC3)cc2)cc1 10.1021/jm400348g
CHEMBL2348214 87822 0 None -91 2 Human 5.8 pKd = 5.8 Binding
Displacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 471 14 4 6 3.5 Cc1ccc(NC(=O)NCCNCC(O)COc2ccc(OCCOC3CCCC3)cc2)cc1 10.1021/jm400348g
13040907 106582 0 None -19 2 Guinea pig 4.8 pKd = 4.8 Binding
Ability to block Beta-2 adrenergic receptor in guinea pig trachea preparationAbility to block Beta-2 adrenergic receptor in guinea pig trachea preparation
ChEMBL 371 12 2 5 2.8 COC(=O)CCc1ccc(OCC(O)CNCCCc2ccccc2)cc1 10.1021/jm00354a003
CHEMBL31583 106582 0 None -19 2 Guinea pig 4.8 pKd = 4.8 Binding
Ability to block Beta-2 adrenergic receptor in guinea pig trachea preparationAbility to block Beta-2 adrenergic receptor in guinea pig trachea preparation
ChEMBL 371 12 2 5 2.8 COC(=O)CCc1ccc(OCC(O)CNCCCc2ccccc2)cc1 10.1021/jm00354a003
15112598 9216 0 None -10 3 Guinea pig 4.8 pKd = 4.8 Binding
The compound was tested for beta-adrenergic activity against Beta-2 adrenergic receptor from guinea pig trachea.The compound was tested for beta-adrenergic activity against Beta-2 adrenergic receptor from guinea pig trachea.
ChEMBL 444 9 3 7 3.3 C/C(=N\OCC(O)CNC(C)(C)C)c1cc(Cl)c(OC(C)C2=NCCN2)c(Cl)c1 10.1021/jm00115a008
CHEMBL111090 9216 0 None -10 3 Guinea pig 4.8 pKd = 4.8 Binding
The compound was tested for beta-adrenergic activity against Beta-2 adrenergic receptor from guinea pig trachea.The compound was tested for beta-adrenergic activity against Beta-2 adrenergic receptor from guinea pig trachea.
ChEMBL 444 9 3 7 3.3 C/C(=N\OCC(O)CNC(C)(C)C)c1cc(Cl)c(OC(C)C2=NCCN2)c(Cl)c1 10.1021/jm00115a008
123133223 147147 0 None - 1 Human 4.8 pKd = 4.8 Binding
Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.
ChEMBL 317 7 4 5 2.4 COc1cccc(C[C@H](C)NC[C@@H](O)c2cc(O)cc(O)c2)c1 nan
CHEMBL3931891 147147 0 None - 1 Human 4.8 pKd = 4.8 Binding
Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.
ChEMBL 317 7 4 5 2.4 COc1cccc(C[C@H](C)NC[C@@H](O)c2cc(O)cc(O)c2)c1 nan
5487795 92831 2 None 79 2 Guinea pig 7.8 pKd = 7.8 Binding
Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.
ChEMBL 284 5 2 4 3.0 CC1C/C(=N/OCC(O)CNC(C)(C)C)CC(C)(C)C1 10.1021/jm00376a011
CHEMBL24500 92831 2 None 79 2 Guinea pig 7.8 pKd = 7.8 Binding
Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.
ChEMBL 284 5 2 4 3.0 CC1C/C(=N/OCC(O)CNC(C)(C)C)CC(C)(C)C1 10.1021/jm00376a011
4930 56856 45 None - 1 Bovine 6.8 pKd = 6.8 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 229 4 2 2 2.9 CC(C)NCC(O)c1ccc2ccccc2c1 10.1021/jm00147a037
CHEMBL16476 56856 45 None - 1 Bovine 6.8 pKd = 6.8 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 229 4 2 2 2.9 CC(C)NCC(O)c1ccc2ccccc2c1 10.1021/jm00147a037
1786 2474 79 None -1 11 Guinea pig 6.8 pKd = 6.8 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm00361a004
4171 2474 79 None -1 11 Guinea pig 6.8 pKd = 6.8 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm00361a004
553 2474 79 None -1 11 Guinea pig 6.8 pKd = 6.8 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm00361a004
CHEMBL13 2474 79 None -1 11 Guinea pig 6.8 pKd = 6.8 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm00361a004
DB00264 2474 79 None -1 11 Guinea pig 6.8 pKd = 6.8 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm00361a004
1786 2474 79 None -1 11 Guinea pig 6.8 pKd = 6.8 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm00156a028
4171 2474 79 None -1 11 Guinea pig 6.8 pKd = 6.8 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm00156a028
553 2474 79 None -1 11 Guinea pig 6.8 pKd = 6.8 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm00156a028
CHEMBL13 2474 79 None -1 11 Guinea pig 6.8 pKd = 6.8 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm00156a028
DB00264 2474 79 None -1 11 Guinea pig 6.8 pKd = 6.8 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm00156a028
13621597 6361 0 None - 1 Guinea pig 4.8 pKd = 4.8 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 441 12 3 7 3.0 COc1ccc(CCNCC(O)COc2ccc(-c3nc(C)c[nH]3)cc2OC)cc1OC 10.1021/jm00156a028
CHEMBL10825 6361 0 None - 1 Guinea pig 4.8 pKd = 4.8 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 441 12 3 7 3.0 COc1ccc(CCNCC(O)COc2ccc(-c3nc(C)c[nH]3)cc2OC)cc1OC 10.1021/jm00156a028
2775690 92565 47 None 15 6 Human 7.8 pKd = 7.8 Binding
Binding affinity to N-terminal FLAG-tagged C-terminal His-10-tagged human beta2 adrenoceptor expressed in insect Sf9 cells by surface plasmon resonance analysisBinding affinity to N-terminal FLAG-tagged C-terminal His-10-tagged human beta2 adrenoceptor expressed in insect Sf9 cells by surface plasmon resonance analysis
ChEMBL 295 1 1 3 3.0 Cc1ccc2nc(C(F)(F)F)cc(N3CCNCC3)c2c1 10.1021/ml400312j
CHEMBL2441619 92565 47 None 15 6 Human 7.8 pKd = 7.8 Binding
Binding affinity to N-terminal FLAG-tagged C-terminal His-10-tagged human beta2 adrenoceptor expressed in insect Sf9 cells by surface plasmon resonance analysisBinding affinity to N-terminal FLAG-tagged C-terminal His-10-tagged human beta2 adrenoceptor expressed in insect Sf9 cells by surface plasmon resonance analysis
ChEMBL 295 1 1 3 3.0 Cc1ccc2nc(C(F)(F)F)cc(N3CCNCC3)c2c1 10.1021/ml400312j
170739 10091 3 None - 1 Bovine 7.8 pKd = 7.8 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 265 8 2 3 2.9 CCC(C)c1cccc(OCC(O)CNC(C)C)c1 10.1021/jm00147a037
CHEMBL1159889 10091 3 None - 1 Bovine 7.8 pKd = 7.8 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 265 8 2 3 2.9 CCC(C)c1cccc(OCC(O)CNC(C)C)c1 10.1021/jm00147a037
1499 2052 43 None -9 17 Guinea pig 7.8 pKd = 7.8 Binding
Agonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring assessed as bronchorelaxation activity against histamine-induced contractionAgonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring assessed as bronchorelaxation activity against histamine-induced contraction
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmcl.2014.12.077
3779 2052 43 None -9 17 Guinea pig 7.8 pKd = 7.8 Binding
Agonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring assessed as bronchorelaxation activity against histamine-induced contractionAgonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring assessed as bronchorelaxation activity against histamine-induced contraction
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmcl.2014.12.077
536 2052 43 None -9 17 Guinea pig 7.8 pKd = 7.8 Binding
Agonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring assessed as bronchorelaxation activity against histamine-induced contractionAgonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring assessed as bronchorelaxation activity against histamine-induced contraction
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmcl.2014.12.077
CHEMBL434 2052 43 None -9 17 Guinea pig 7.8 pKd = 7.8 Binding
Agonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring assessed as bronchorelaxation activity against histamine-induced contractionAgonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring assessed as bronchorelaxation activity against histamine-induced contraction
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmcl.2014.12.077
DB01064 2052 43 None -9 17 Guinea pig 7.8 pKd = 7.8 Binding
Agonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring assessed as bronchorelaxation activity against histamine-induced contractionAgonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring assessed as bronchorelaxation activity against histamine-induced contraction
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmcl.2014.12.077
155774 4021 33 None -5 3 Human 5.8 pKd = 5.8 Binding
Displacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 339 8 4 6 -0.2 OC(COc1ccc(cc1)O)CNCCNC(=O)N1CCOCC1 10.1021/jm400348g
2848 4021 33 None -5 3 Human 5.8 pKd = 5.8 Binding
Displacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 339 8 4 6 -0.2 OC(COc1ccc(cc1)O)CNCCNC(=O)N1CCOCC1 10.1021/jm400348g
538 4021 33 None -5 3 Human 5.8 pKd = 5.8 Binding
Displacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 339 8 4 6 -0.2 OC(COc1ccc(cc1)O)CNCCNC(=O)N1CCOCC1 10.1021/jm400348g
CHEMBL75753 4021 33 None -5 3 Human 5.8 pKd = 5.8 Binding
Displacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 339 8 4 6 -0.2 OC(COc1ccc(cc1)O)CNCCNC(=O)N1CCOCC1 10.1021/jm400348g
DB13781 4021 33 None -5 3 Human 5.8 pKd = 5.8 Binding
Displacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 339 8 4 6 -0.2 OC(COc1ccc(cc1)O)CNCCNC(=O)N1CCOCC1 10.1021/jm400348g
56599233 87816 0 None -87 2 Human 5.8 pKd = 5.8 Binding
Displacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 525 14 4 6 4.2 O=C(NCCNCC(O)COc1ccc(OCCOC2CCCC2)cc1)Nc1ccc(C(F)(F)F)cc1 10.1021/jm400348g
CHEMBL2348208 87816 0 None -87 2 Human 5.8 pKd = 5.8 Binding
Displacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 525 14 4 6 4.2 O=C(NCCNCC(O)COc1ccc(OCCOC2CCCC2)cc1)Nc1ccc(C(F)(F)F)cc1 10.1021/jm400348g
29057685 158275 12 None 1 2 Human 4.8 pKd = 4.8 Binding
Displacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting methodDisplacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting method
ChEMBL 394 4 1 6 3.1 COc1cccc(/C=C2\Oc3c(CN4CCN(C)CC4)c(O)cc(C)c3C2=O)c1 10.1021/acsmedchemlett.6b00363
8056725 158275 12 None 1 2 Human 4.8 pKd = 4.8 Binding
Displacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting methodDisplacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting method
ChEMBL 394 4 1 6 3.1 COc1cccc(/C=C2\Oc3c(CN4CCN(C)CC4)c(O)cc(C)c3C2=O)c1 10.1021/acsmedchemlett.6b00363
CHEMBL4094678 158275 12 None 1 2 Human 4.8 pKd = 4.8 Binding
Displacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting methodDisplacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting method
ChEMBL 394 4 1 6 3.1 COc1cccc(/C=C2\Oc3c(CN4CCN(C)CC4)c(O)cc(C)c3C2=O)c1 10.1021/acsmedchemlett.6b00363
13621620 8885 0 None -1174 2 Guinea pig 4.8 pKd = 4.8 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 425 11 3 6 3.3 COc1ccc(CCNCC(O)COc2ccc(-c3nc(C)c(C)[nH]3)cc2)cc1OC 10.1021/jm00156a028
CHEMBL10983 8885 0 None -1174 2 Guinea pig 4.8 pKd = 4.8 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 425 11 3 6 3.3 COc1ccc(CCNCC(O)COc2ccc(-c3nc(C)c(C)[nH]3)cc2)cc1OC 10.1021/jm00156a028
16736096 141552 0 None 19 2 Human 5.8 pKd = 5.8 Binding
Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.
ChEMBL 337 6 4 4 3.5 C[C@H](Cc1cccc2ccccc12)NC[C@@H](O)c1cc(O)cc(O)c1 nan
CHEMBL388177 141552 0 None 19 2 Human 5.8 pKd = 5.8 Binding
Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.
ChEMBL 337 6 4 4 3.5 C[C@H](Cc1cccc2ccccc12)NC[C@@H](O)c1cc(O)cc(O)c1 nan
16424333 155997 10 None - 1 Human 4.8 pKd = 4.8 Binding
Displacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting methodDisplacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting method
ChEMBL 469 6 1 5 6.1 CCCCN(C)Cc1c(O)cc(C)c2c1O/C(=C\c1cc3cc(Br)ccc3o1)C2=O 10.1021/acsmedchemlett.6b00363
16424334 155997 10 None - 1 Human 4.8 pKd = 4.8 Binding
Displacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting methodDisplacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting method
ChEMBL 469 6 1 5 6.1 CCCCN(C)Cc1c(O)cc(C)c2c1O/C(=C\c1cc3cc(Br)ccc3o1)C2=O 10.1021/acsmedchemlett.6b00363
CHEMBL4068256 155997 10 None - 1 Human 4.8 pKd = 4.8 Binding
Displacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting methodDisplacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting method
ChEMBL 469 6 1 5 6.1 CCCCN(C)Cc1c(O)cc(C)c2c1O/C(=C\c1cc3cc(Br)ccc3o1)C2=O 10.1021/acsmedchemlett.6b00363
13621656 9187 0 None -1348 2 Guinea pig 4.8 pKd = 4.8 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 455 14 3 7 3.2 CCOCc1c[nH]c(-c2ccc(OCC(O)CNCCc3ccc(OC)c(OC)c3)cc2)n1 10.1021/jm00156a028
CHEMBL11093 9187 0 None -1348 2 Guinea pig 4.8 pKd = 4.8 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 455 14 3 7 3.2 CCOCc1c[nH]c(-c2ccc(OCC(O)CNCCc3ccc(OC)c(OC)c3)cc2)n1 10.1021/jm00156a028
57543937 92563 0 None - 1 Human 5.8 pKd = 5.8 Binding
Binding affinity to N-terminal FLAG-tagged C-terminal His-10-tagged human beta2 adrenoceptor expressed in insect Sf9 cells by surface plasmon resonance analysis in presence of maltose neopentyl glycolBinding affinity to N-terminal FLAG-tagged C-terminal His-10-tagged human beta2 adrenoceptor expressed in insect Sf9 cells by surface plasmon resonance analysis in presence of maltose neopentyl glycol
ChEMBL 309 1 0 3 3.3 Cc1ccc2nc(C(F)(F)F)cc(N3CCN(C)CC3)c2c1 10.1021/ml400312j
CHEMBL2441616 92563 0 None - 1 Human 5.8 pKd = 5.8 Binding
Binding affinity to N-terminal FLAG-tagged C-terminal His-10-tagged human beta2 adrenoceptor expressed in insect Sf9 cells by surface plasmon resonance analysis in presence of maltose neopentyl glycolBinding affinity to N-terminal FLAG-tagged C-terminal His-10-tagged human beta2 adrenoceptor expressed in insect Sf9 cells by surface plasmon resonance analysis in presence of maltose neopentyl glycol
ChEMBL 309 1 0 3 3.3 Cc1ccc2nc(C(F)(F)F)cc(N3CCN(C)CC3)c2c1 10.1021/ml400312j
23276420 110903 4 None - 1 Guinea pig 6.7 pKd = 6.7 Binding
Antagonist activity at beta-2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of isoprenaline-induced effectAntagonist activity at beta-2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of isoprenaline-induced effect
ChEMBL 340 12 4 6 1.2 CC(C)NCC(O)COc1ccccc1OCC(O)CNC(C)C 10.1021/jm00214a013
CHEMBL3272434 110903 4 None - 1 Guinea pig 6.7 pKd = 6.7 Binding
Antagonist activity at beta-2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of isoprenaline-induced effectAntagonist activity at beta-2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of isoprenaline-induced effect
ChEMBL 340 12 4 6 1.2 CC(C)NCC(O)COc1ccccc1OCC(O)CNC(C)C 10.1021/jm00214a013
123133224 160153 0 None 9 2 Human 5.7 pKd = 5.7 Binding
Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.
ChEMBL 302 6 5 5 1.9 C[C@H](Cc1cccc(N)c1)NC[C@H](O)c1cc(O)cc(O)c1 nan
CHEMBL4113713 160153 0 None 9 2 Human 5.7 pKd = 5.7 Binding
Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.
ChEMBL 302 6 5 5 1.9 C[C@H](Cc1cccc(N)c1)NC[C@H](O)c1cc(O)cc(O)c1 nan
2687 874 15 None 1 5 Human 7.7 pKd = 7.7 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation counting
ChEMBL 279 5 4 4 1.0 OC(COc1cccc2c1[nH]c(=O)[nH]2)CNC(C)(C)C 10.1021/acs.jmedchem.6b00358
532 874 15 None 1 5 Human 7.7 pKd = 7.7 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation counting
ChEMBL 279 5 4 4 1.0 OC(COc1cccc2c1[nH]c(=O)[nH]2)CNC(C)(C)C 10.1021/acs.jmedchem.6b00358
5387 874 15 None 1 5 Human 7.7 pKd = 7.7 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation counting
ChEMBL 279 5 4 4 1.0 OC(COc1cccc2c1[nH]c(=O)[nH]2)CNC(C)(C)C 10.1021/acs.jmedchem.6b00358
CHEMBL420746 874 15 None 1 5 Human 7.7 pKd = 7.7 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation counting
ChEMBL 279 5 4 4 1.0 OC(COc1cccc2c1[nH]c(=O)[nH]2)CNC(C)(C)C 10.1021/acs.jmedchem.6b00358
9576814 59095 4 None -2 2 Guinea pig 7.7 pKd = 7.7 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor determined as pA2 in guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor determined as pA2 in guinea pig trachea
ChEMBL 228 6 2 4 1.5 C/C(=N\OC[C@H](O)CNC(C)(C)C)C1CC1 10.1021/jm00145a008
CHEMBL171059 59095 4 None -2 2 Guinea pig 7.7 pKd = 7.7 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor determined as pA2 in guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor determined as pA2 in guinea pig trachea
ChEMBL 228 6 2 4 1.5 C/C(=N\OC[C@H](O)CNC(C)(C)C)C1CC1 10.1021/jm00145a008
10016379 10078 0 None - 1 Bovine 5.7 pKd = 5.7 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 277 3 3 3 3.1 CC(C)(C)NCC(O)c1cc(Cl)c(O)c(Cl)c1 10.1021/jm00147a037
CHEMBL1159711 10078 0 None - 1 Bovine 5.7 pKd = 5.7 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 277 3 3 3 3.1 CC(C)(C)NCC(O)c1cc(Cl)c(O)c(Cl)c1 10.1021/jm00147a037
16736091 85291 0 None 66 2 Human 5.7 pKd = 5.7 Binding
Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.
ChEMBL 317 7 4 5 2.4 COc1ccc(C[C@H](C)NC[C@H](O)c2cc(O)cc(O)c2)cc1 nan
CHEMBL228996 85291 0 None 66 2 Human 5.7 pKd = 5.7 Binding
Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.
ChEMBL 317 7 4 5 2.4 COc1ccc(C[C@H](C)NC[C@H](O)c2cc(O)cc(O)c2)cc1 nan
62773144 109938 3 None -1 2 Guinea pig 6.7 pKd = 6.7 Binding
Antagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 minsAntagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 mins
ChEMBL 257 4 2 2 2.5 CC(C)NCC(O)c1ccc(Br)cc1 10.1021/jm00208a015
CHEMBL3246227 109938 3 None -1 2 Guinea pig 6.7 pKd = 6.7 Binding
Antagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 minsAntagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 mins
ChEMBL 257 4 2 2 2.5 CC(C)NCC(O)c1ccc(Br)cc1 10.1021/jm00208a015
15578608 107000 2 None -5 2 Guinea pig 6.7 pKd = 6.7 Binding
In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.
ChEMBL 295 10 2 5 1.7 CCOC(=O)CCCNCC(O)COc1ccccc1C 10.1021/jm00354a002
CHEMBL31857 107000 2 None -5 2 Guinea pig 6.7 pKd = 6.7 Binding
In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.
ChEMBL 295 10 2 5 1.7 CCOC(=O)CCCNCC(O)COc1ccccc1C 10.1021/jm00354a002
15578596 110922 2 None 1 2 Guinea pig 6.7 pKd = 6.7 Binding
In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.
ChEMBL 297 10 2 6 1.0 CCOC(=O)CCNCC(O)COc1cccc(OC)c1 10.1021/jm00354a002
CHEMBL32736 110922 2 None 1 2 Guinea pig 6.7 pKd = 6.7 Binding
In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.
ChEMBL 297 10 2 6 1.0 CCOC(=O)CCNCC(O)COc1cccc(OC)c1 10.1021/jm00354a002
15578590 161490 2 None -5 2 Guinea pig 6.7 pKd = 6.7 Binding
In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.
ChEMBL 301 9 2 5 1.6 CCOC(=O)CCNCC(O)COc1cccc(Cl)c1 10.1021/jm00354a002
CHEMBL416030 161490 2 None -5 2 Guinea pig 6.7 pKd = 6.7 Binding
In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.
ChEMBL 301 9 2 5 1.6 CCOC(=O)CCNCC(O)COc1cccc(Cl)c1 10.1021/jm00354a002
13621761 9263 0 None -10 2 Guinea pig 6.7 pKd = 6.7 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 385 8 3 5 3.9 CC(C)(C)NCC(O)COc1ccc(Cc2nc(-c3cccs3)c[nH]2)cc1 10.1021/jm00156a028
CHEMBL11135 9263 0 None -10 2 Guinea pig 6.7 pKd = 6.7 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 385 8 3 5 3.9 CC(C)(C)NCC(O)COc1ccc(Cc2nc(-c3cccs3)c[nH]2)cc1 10.1021/jm00156a028
13040890 103922 0 None -3 2 Guinea pig 5.7 pKd = 5.7 Binding
Ability to block Beta-2 adrenergic receptor in guinea pig trachea preparationAbility to block Beta-2 adrenergic receptor in guinea pig trachea preparation
ChEMBL 279 8 2 5 1.7 C=COC(=O)c1ccc(OCC(O)CNC(C)C)cc1 10.1021/jm00354a003
CHEMBL31036 103922 0 None -3 2 Guinea pig 5.7 pKd = 5.7 Binding
Ability to block Beta-2 adrenergic receptor in guinea pig trachea preparationAbility to block Beta-2 adrenergic receptor in guinea pig trachea preparation
ChEMBL 279 8 2 5 1.7 C=COC(=O)c1ccc(OCC(O)CNC(C)C)cc1 10.1021/jm00354a003
59373811 109941 5 None -2 2 Guinea pig 5.7 pKd = 5.7 Binding
Antagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 minsAntagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 mins
ChEMBL 193 4 2 2 2.0 Cc1cccc(C(O)CNC(C)C)c1 10.1021/jm00208a015
CHEMBL3246233 109941 5 None -2 2 Guinea pig 5.7 pKd = 5.7 Binding
Antagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 minsAntagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 mins
ChEMBL 193 4 2 2 2.0 Cc1cccc(C(O)CNC(C)C)c1 10.1021/jm00208a015
15578604 106607 1 None 1 2 Guinea pig 5.7 pKd = 5.7 Binding
In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.
ChEMBL 253 7 2 5 0.5 COC(=O)CNCC(O)COc1ccccc1C 10.1021/jm00354a002
CHEMBL31598 106607 1 None 1 2 Guinea pig 5.7 pKd = 5.7 Binding
In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.
ChEMBL 253 7 2 5 0.5 COC(=O)CNCC(O)COc1ccccc1C 10.1021/jm00354a002
13621599 9789 0 None -3981 2 Guinea pig 4.7 pKd = 4.7 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 513 12 3 7 5.0 COc1ccc(CCNCC(O)COc2ccc(-c3nc(-c4cccs4)c[nH]3)cc2Cl)cc1OC 10.1021/jm00156a028
CHEMBL11431 9789 0 None -3981 2 Guinea pig 4.7 pKd = 4.7 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 513 12 3 7 5.0 COc1ccc(CCNCC(O)COc2ccc(-c3nc(-c4cccs4)c[nH]3)cc2Cl)cc1OC 10.1021/jm00156a028
10467512 99413 0 None 2 2 Guinea pig 8.7 pKd = 8.7 Binding
Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.
ChEMBL 254 7 2 4 1.9 CC(C)(C)NCC(O)CON=C(C1CC1)C1CC1 10.1021/jm00376a011
CHEMBL285972 99413 0 None 2 2 Guinea pig 8.7 pKd = 8.7 Binding
Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.
ChEMBL 254 7 2 4 1.9 CC(C)(C)NCC(O)CON=C(C1CC1)C1CC1 10.1021/jm00376a011
10467512 99413 0 None 2 2 Guinea pig 8.7 pKd = 8.7 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor determined as pA2 in guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor determined as pA2 in guinea pig trachea
ChEMBL 254 7 2 4 1.9 CC(C)(C)NCC(O)CON=C(C1CC1)C1CC1 10.1021/jm00145a008
CHEMBL285972 99413 0 None 2 2 Guinea pig 8.7 pKd = 8.7 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor determined as pA2 in guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor determined as pA2 in guinea pig trachea
ChEMBL 254 7 2 4 1.9 CC(C)(C)NCC(O)CON=C(C1CC1)C1CC1 10.1021/jm00145a008
12484297 109216 0 None 15 2 Guinea pig 8.6 pKd = 8.6 Binding
Competitive antagonist activity at beta-2 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced tracheal relaxationCompetitive antagonist activity at beta-2 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced tracheal relaxation
ChEMBL 249 6 3 4 1.3 CC(C)NCC(O)COc1cccc2[nH]cnc12 10.1021/jm00188a019
CHEMBL3228931 109216 0 None 15 2 Guinea pig 8.6 pKd = 8.6 Binding
Competitive antagonist activity at beta-2 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced tracheal relaxationCompetitive antagonist activity at beta-2 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced tracheal relaxation
ChEMBL 249 6 3 4 1.3 CC(C)NCC(O)COc1cccc2[nH]cnc12 10.1021/jm00188a019
54757229 65169 0 None 16 3 Human 8.6 pKd = 8.6 Binding
Displacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cells
ChEMBL 795 22 4 8 6.3 C=CCc1ccccc1OCC(O)CNCCNC(=O)CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1 10.1021/jm2008562
CHEMBL1830617 65169 0 None 16 3 Human 8.6 pKd = 8.6 Binding
Displacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cells
ChEMBL 795 22 4 8 6.3 C=CCc1ccccc1OCC(O)CNCCNC(=O)CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1 10.1021/jm2008562
3682 188837 7 None -1 8 Guinea pig 8.6 pKd = 8.6 Binding
Antagonist activity at adrenergic beta2 receptor in precontracted Hartley guinea pig tracheal ring assessed as inhibition of salbutamol-indiuced relaxant activityAntagonist activity at adrenergic beta2 receptor in precontracted Hartley guinea pig tracheal ring assessed as inhibition of salbutamol-indiuced relaxant activity
ChEMBL 277 6 2 3 2.6 Cc1ccc(OCC(O)C(C)NC(C)C)c2c1CCC2 10.1016/j.bmcl.2014.12.077
CHEMBL1256784 188837 7 None -1 8 Guinea pig 8.6 pKd = 8.6 Binding
Antagonist activity at adrenergic beta2 receptor in precontracted Hartley guinea pig tracheal ring assessed as inhibition of salbutamol-indiuced relaxant activityAntagonist activity at adrenergic beta2 receptor in precontracted Hartley guinea pig tracheal ring assessed as inhibition of salbutamol-indiuced relaxant activity
ChEMBL 277 6 2 3 2.6 Cc1ccc(OCC(O)C(C)NC(C)C)c2c1CCC2 10.1016/j.bmcl.2014.12.077
CHEMBL513389 188837 7 None -1 8 Guinea pig 8.6 pKd = 8.6 Binding
Antagonist activity at adrenergic beta2 receptor in precontracted Hartley guinea pig tracheal ring assessed as inhibition of salbutamol-indiuced relaxant activityAntagonist activity at adrenergic beta2 receptor in precontracted Hartley guinea pig tracheal ring assessed as inhibition of salbutamol-indiuced relaxant activity
ChEMBL 277 6 2 3 2.6 Cc1ccc(OCC(O)C(C)NC(C)C)c2c1CCC2 10.1016/j.bmcl.2014.12.077
1239 1639 46 None 63 4 Human 8.6 pKd = 8.6 Binding
Binding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nMBinding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nM
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2013.07.052
3410 1639 46 None 63 4 Human 8.6 pKd = 8.6 Binding
Binding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nMBinding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nM
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2013.07.052
3465 1639 46 None 63 4 Human 8.6 pKd = 8.6 Binding
Binding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nMBinding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nM
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2013.07.052
CHEMBL1256786 1639 46 None 63 4 Human 8.6 pKd = 8.6 Binding
Binding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nMBinding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nM
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2013.07.052
DB00983 1639 46 None 63 4 Human 8.6 pKd = 8.6 Binding
Binding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nMBinding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nM
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2013.07.052
54756929 65143 0 None 28 3 Human 8.6 pKd = 8.6 Binding
Displacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cells
ChEMBL 805 20 4 8 6.7 O=C(CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1)NCCNCC(O)COc1cccc2ccccc12 10.1021/jm2008562
CHEMBL1830488 65143 0 None 28 3 Human 8.6 pKd = 8.6 Binding
Displacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cells
ChEMBL 805 20 4 8 6.7 O=C(CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1)NCCNCC(O)COc1cccc2ccccc12 10.1021/jm2008562
54757129 65148 0 None 23 3 Human 8.5 pKd = 8.5 Binding
Displacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cells
ChEMBL 795 22 4 8 6.3 C=CCc1ccccc1OC[C@@H](O)CNCCNC(=O)CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1 10.1021/jm2008562
CHEMBL1830493 65148 0 None 23 3 Human 8.5 pKd = 8.5 Binding
Displacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cells
ChEMBL 795 22 4 8 6.3 C=CCc1ccccc1OC[C@@H](O)CNCCNC(=O)CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1 10.1021/jm2008562
10087493 10077 0 None - 1 Bovine 5.7 pKd = 5.7 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 224 3 4 4 1.4 CC(C)(C)NCC(O)c1ccc(O)c(N)c1 10.1021/jm00147a037
CHEMBL1159710 10077 0 None - 1 Bovine 5.7 pKd = 5.7 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 224 3 4 4 1.4 CC(C)(C)NCC(O)c1ccc(O)c(N)c1 10.1021/jm00147a037
66653268 87809 0 None -426 3 Human 5.7 pKd = 5.7 Binding
Displacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 491 14 4 6 3.8 O=C(NCCNCC(O)COc1ccc(OCCOC2CCCC2)cc1)Nc1cccc(Cl)c1 10.1021/jm400348g
CHEMBL2348201 87809 0 None -426 3 Human 5.7 pKd = 5.7 Binding
Displacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 491 14 4 6 3.8 O=C(NCCNCC(O)COc1ccc(OCCOC2CCCC2)cc1)Nc1cccc(Cl)c1 10.1021/jm400348g
3486 3096 51 None -6 11 Bovine 4.7 pKd = 4.7 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C 10.1021/jm00147a037
4883 3096 51 None -6 11 Bovine 4.7 pKd = 4.7 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C 10.1021/jm00147a037
555 3096 51 None -6 11 Bovine 4.7 pKd = 4.7 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C 10.1021/jm00147a037
CHEMBL6995 3096 51 None -6 11 Bovine 4.7 pKd = 4.7 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C 10.1021/jm00147a037
DB01297 3096 51 None -6 11 Bovine 4.7 pKd = 4.7 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C 10.1021/jm00147a037
16736514 142998 0 None 2 2 Human 4.7 pKd = 4.7 Binding
Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.
ChEMBL 273 6 4 4 2.0 Oc1cc(O)cc([C@H](O)CNCCc2ccccc2)c1 nan
CHEMBL389902 142998 0 None 2 2 Human 4.7 pKd = 4.7 Binding
Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.
ChEMBL 273 6 4 4 2.0 Oc1cc(O)cc([C@H](O)CNCCc2ccccc2)c1 nan
13621758 9676 0 None -3 2 Guinea pig 6.7 pKd = 6.7 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 317 7 3 4 2.4 Cc1c[nH]c(Cc2ccc(OCC(O)CNC(C)(C)C)cc2)n1 10.1021/jm00156a028
CHEMBL11362 9676 0 None -3 2 Guinea pig 6.7 pKd = 6.7 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 317 7 3 4 2.4 Cc1c[nH]c(Cc2ccc(OCC(O)CNC(C)(C)C)cc2)n1 10.1021/jm00156a028
13621772 9158 0 None -301 2 Guinea pig 5.7 pKd = 5.7 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 441 14 3 7 2.7 COc1ccc(CCNCC(O)COc2ccc(COCc3ncc[nH]3)cc2)cc1OC 10.1021/jm00156a028
CHEMBL11080 9158 0 None -301 2 Guinea pig 5.7 pKd = 5.7 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 441 14 3 7 2.7 COc1ccc(CCNCC(O)COc2ccc(COCc3ncc[nH]3)cc2)cc1OC 10.1021/jm00156a028
38065 10090 8 None - 1 Bovine 7.7 pKd = 7.7 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 234 6 2 4 1.3 CC(C)NCC(O)COc1ccccc1C#N 10.1021/jm00147a037
CHEMBL1159888 10090 8 None - 1 Bovine 7.7 pKd = 7.7 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 234 6 2 4 1.3 CC(C)NCC(O)COc1ccccc1C#N 10.1021/jm00147a037
13590033 9729 0 None -19 2 Guinea pig 4.7 pKd = 4.7 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 398 11 2 7 2.9 COc1ccc(CCNCC(O)COc2ccc(-c3ncco3)cc2)cc1OC 10.1021/jm00156a028
CHEMBL11401 9729 0 None -19 2 Guinea pig 4.7 pKd = 4.7 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 398 11 2 7 2.9 COc1ccc(CCNCC(O)COc2ccc(-c3ncco3)cc2)cc1OC 10.1021/jm00156a028
10378069 10093 2 None - 1 Bovine 5.7 pKd = 5.7 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 263 8 2 4 1.4 C#CCOc1ccccc1OCC(O)CNC(C)C 10.1021/jm00147a037
CHEMBL1159890 10093 2 None - 1 Bovine 5.7 pKd = 5.7 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 263 8 2 4 1.4 C#CCOc1ccccc1OCC(O)CNC(C)C 10.1021/jm00147a037
21490498 112269 0 None - 1 Guinea pig 6.7 pKd = 6.7 Binding
Antagonist activity at beta-2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of isoprenaline-induced effectAntagonist activity at beta-2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of isoprenaline-induced effect
ChEMBL 354 12 4 6 1.5 Cc1ccc(OCC(O)CNC(C)C)c(OCC(O)CNC(C)C)c1 10.1021/jm00214a013
CHEMBL3272437 112269 0 None - 1 Guinea pig 6.7 pKd = 6.7 Binding
Antagonist activity at beta-2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of isoprenaline-induced effectAntagonist activity at beta-2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of isoprenaline-induced effect
ChEMBL 354 12 4 6 1.5 Cc1ccc(OCC(O)CNC(C)C)c(OCC(O)CNC(C)C)c1 10.1021/jm00214a013
CHEMBL3305647 112269 0 None - 1 Guinea pig 6.7 pKd = 6.7 Binding
Antagonist activity at beta-2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of isoprenaline-induced effectAntagonist activity at beta-2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of isoprenaline-induced effect
ChEMBL 354 12 4 6 1.5 Cc1ccc(OCC(O)CNC(C)C)c(OCC(O)CNC(C)C)c1 10.1021/jm00214a013
13621676 9112 0 None -1122 2 Guinea pig 5.7 pKd = 5.7 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 475 11 3 6 3.4 COc1ccc(CCNCC(O)COc2ccc(-c3nc(Br)c[nH]3)cc2)cc1OC 10.1021/jm00156a028
CHEMBL11051 9112 0 None -1122 2 Guinea pig 5.7 pKd = 5.7 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 475 11 3 6 3.4 COc1ccc(CCNCC(O)COc2ccc(-c3nc(Br)c[nH]3)cc2)cc1OC 10.1021/jm00156a028
29074692 159180 13 None 2 2 Human 4.7 pKd = 4.7 Binding
Displacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting methodDisplacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting method
ChEMBL 339 4 1 5 3.4 COc1cccc(/C=C2\Oc3c(CN(C)C)c(O)cc(C)c3C2=O)c1 10.1021/acsmedchemlett.6b00363
8073977 159180 13 None 2 2 Human 4.7 pKd = 4.7 Binding
Displacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting methodDisplacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting method
ChEMBL 339 4 1 5 3.4 COc1cccc(/C=C2\Oc3c(CN(C)C)c(O)cc(C)c3C2=O)c1 10.1021/acsmedchemlett.6b00363
CHEMBL4104850 159180 13 None 2 2 Human 4.7 pKd = 4.7 Binding
Displacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting methodDisplacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting method
ChEMBL 339 4 1 5 3.4 COc1cccc(/C=C2\Oc3c(CN(C)C)c(O)cc(C)c3C2=O)c1 10.1021/acsmedchemlett.6b00363
12606706 92788 0 None 13 2 Guinea pig 7.7 pKd = 7.7 Binding
Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.
ChEMBL 202 5 2 4 1.1 CC(C)=NOCC(O)CNC(C)(C)C 10.1021/jm00376a011
CHEMBL24480 92788 0 None 13 2 Guinea pig 7.7 pKd = 7.7 Binding
Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.
ChEMBL 202 5 2 4 1.1 CC(C)=NOCC(O)CNC(C)(C)C 10.1021/jm00376a011
CHEMBL555848 92788 0 None 13 2 Guinea pig 7.7 pKd = 7.7 Binding
Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.
ChEMBL 202 5 2 4 1.1 CC(C)=NOCC(O)CNC(C)(C)C 10.1021/jm00376a011
44459891 95704 0 None 7 2 Guinea pig 7.6 pKd = 7.6 Binding
Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.
ChEMBL 217 5 2 3 1.8 CC(C)(C)COCC(O)CNC(C)(C)C 10.1021/jm00376a011
CHEMBL26059 95704 0 None 7 2 Guinea pig 7.6 pKd = 7.6 Binding
Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.
ChEMBL 217 5 2 3 1.8 CC(C)(C)COCC(O)CNC(C)(C)C 10.1021/jm00376a011
105 3392 84 None -10 6 Human 6.7 pKd = 6.7 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation counting
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1021/acs.jmedchem.6b00358
2083 3392 84 None -10 6 Human 6.7 pKd = 6.7 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation counting
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1021/acs.jmedchem.6b00358
558 3392 84 None -10 6 Human 6.7 pKd = 6.7 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation counting
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1021/acs.jmedchem.6b00358
CHEMBL714 3392 84 None -10 6 Human 6.7 pKd = 6.7 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation counting
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1021/acs.jmedchem.6b00358
DB01001 3392 84 None -10 6 Human 6.7 pKd = 6.7 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation counting
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1021/acs.jmedchem.6b00358
702235 52916 93 None -51 4 Human 4.7 pKd = 4.7 Binding
Binding affinity to N-terminal FLAG-tagged C-terminal His-10-tagged human beta2 adrenoceptor expressed in insect Sf9 cells by surface plasmon resonance analysisBinding affinity to N-terminal FLAG-tagged C-terminal His-10-tagged human beta2 adrenoceptor expressed in insect Sf9 cells by surface plasmon resonance analysis
ChEMBL 200 1 2 1 2.6 c1ccc2c(C3CCNCC3)c[nH]c2c1 10.1021/ml400312j
CHEMBL15988 52916 93 None -51 4 Human 4.7 pKd = 4.7 Binding
Binding affinity to N-terminal FLAG-tagged C-terminal His-10-tagged human beta2 adrenoceptor expressed in insect Sf9 cells by surface plasmon resonance analysisBinding affinity to N-terminal FLAG-tagged C-terminal His-10-tagged human beta2 adrenoceptor expressed in insect Sf9 cells by surface plasmon resonance analysis
ChEMBL 200 1 2 1 2.6 c1ccc2c(C3CCNCC3)c[nH]c2c1 10.1021/ml400312j
CHEMBL2011564 52916 93 None -51 4 Human 4.7 pKd = 4.7 Binding
Binding affinity to N-terminal FLAG-tagged C-terminal His-10-tagged human beta2 adrenoceptor expressed in insect Sf9 cells by surface plasmon resonance analysisBinding affinity to N-terminal FLAG-tagged C-terminal His-10-tagged human beta2 adrenoceptor expressed in insect Sf9 cells by surface plasmon resonance analysis
ChEMBL 200 1 2 1 2.6 c1ccc2c(C3CCNCC3)c[nH]c2c1 10.1021/ml400312j
44459922 96352 0 None -4 2 Guinea pig 6.7 pKd = 6.7 Binding
Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.
ChEMBL 230 6 2 4 1.8 C/C(=N/OCC(O)CNC(C)(C)C)C(C)C 10.1021/jm00376a011
CHEMBL26506 96352 0 None -4 2 Guinea pig 6.7 pKd = 6.7 Binding
Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.
ChEMBL 230 6 2 4 1.8 C/C(=N/OCC(O)CNC(C)(C)C)C(C)C 10.1021/jm00376a011
4191179 112264 1 None - 1 Guinea pig 5.6 pKd = 5.6 Binding
Antagonist activity at beta-2 adrenergic receptor in guinea pig right atrium assessed as inhibition of isoprenaline-induced effectAntagonist activity at beta-2 adrenergic receptor in guinea pig right atrium assessed as inhibition of isoprenaline-induced effect
ChEMBL 382 13 4 6 2.3 CC(C)NCC(O)COc1ccc(C(C)C)cc1OCC(O)CNC(C)C 10.1021/jm00214a013
CHEMBL3272438 112264 1 None - 1 Guinea pig 5.6 pKd = 5.6 Binding
Antagonist activity at beta-2 adrenergic receptor in guinea pig right atrium assessed as inhibition of isoprenaline-induced effectAntagonist activity at beta-2 adrenergic receptor in guinea pig right atrium assessed as inhibition of isoprenaline-induced effect
ChEMBL 382 13 4 6 2.3 CC(C)NCC(O)COc1ccc(C(C)C)cc1OCC(O)CNC(C)C 10.1021/jm00214a013
CHEMBL3305475 112264 1 None - 1 Guinea pig 5.6 pKd = 5.6 Binding
Antagonist activity at beta-2 adrenergic receptor in guinea pig right atrium assessed as inhibition of isoprenaline-induced effectAntagonist activity at beta-2 adrenergic receptor in guinea pig right atrium assessed as inhibition of isoprenaline-induced effect
ChEMBL 382 13 4 6 2.3 CC(C)NCC(O)COc1ccc(C(C)C)cc1OCC(O)CNC(C)C 10.1021/jm00214a013
16735494 141508 0 None 3 2 Human 4.6 pKd = 4.6 Binding
Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.
ChEMBL 287 6 4 4 2.4 C[C@H](Cc1ccccc1)NC[C@@H](O)c1cc(O)cc(O)c1 nan
CHEMBL387825 141508 0 None 3 2 Human 4.6 pKd = 4.6 Binding
Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.
ChEMBL 287 6 4 4 2.4 C[C@H](Cc1ccccc1)NC[C@@H](O)c1cc(O)cc(O)c1 nan
20986823 156302 7 None 4 2 Human 4.6 pKd = 4.6 Binding
Displacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting methodDisplacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting method
ChEMBL 243 5 0 3 2.6 CN(C)CCOc1ccc2ccccc2c1C=O 10.1021/acsmedchemlett.6b00363
CHEMBL4071616 156302 7 None 4 2 Human 4.6 pKd = 4.6 Binding
Displacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting methodDisplacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting method
ChEMBL 243 5 0 3 2.6 CN(C)CCOc1ccc2ccccc2c1C=O 10.1021/acsmedchemlett.6b00363
13621770 9244 0 None -7 2 Guinea pig 7.6 pKd = 7.6 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 367 8 3 4 2.5 CC(C)NCC(O)COc1ccc(Cc2nc(Br)c[nH]2)cc1 10.1021/jm00156a028
CHEMBL11125 9244 0 None -7 2 Guinea pig 7.6 pKd = 7.6 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 367 8 3 4 2.5 CC(C)NCC(O)COc1ccc(Cc2nc(Br)c[nH]2)cc1 10.1021/jm00156a028
16735495 85345 0 None 14 2 Human 6.6 pKd = 6.6 Binding
Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.
ChEMBL 337 6 4 4 3.5 C[C@H](Cc1cccc2ccccc12)NC[C@H](O)c1cc(O)cc(O)c1 nan
CHEMBL229401 85345 0 None 14 2 Human 6.6 pKd = 6.6 Binding
Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.
ChEMBL 337 6 4 4 3.5 C[C@H](Cc1cccc2ccccc12)NC[C@H](O)c1cc(O)cc(O)c1 nan
165193 3126 60 None -4 43 Guinea pig 6.6 pKd = 6.6 Binding
Inhibition of beta2-adrenergic receptor in guinea pig tracheal chain assessed as reversal of isoproterenol-induced effect after 15 minsInhibition of beta2-adrenergic receptor in guinea pig tracheal chain assessed as reversal of isoproterenol-induced effect after 15 mins
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00199a012
2303 3126 60 None -4 43 Guinea pig 6.6 pKd = 6.6 Binding
Inhibition of beta2-adrenergic receptor in guinea pig tracheal chain assessed as reversal of isoproterenol-induced effect after 15 minsInhibition of beta2-adrenergic receptor in guinea pig tracheal chain assessed as reversal of isoproterenol-induced effect after 15 mins
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00199a012
4946 3126 60 None -4 43 Guinea pig 6.6 pKd = 6.6 Binding
Inhibition of beta2-adrenergic receptor in guinea pig tracheal chain assessed as reversal of isoproterenol-induced effect after 15 minsInhibition of beta2-adrenergic receptor in guinea pig tracheal chain assessed as reversal of isoproterenol-induced effect after 15 mins
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00199a012
564 3126 60 None -4 43 Guinea pig 6.6 pKd = 6.6 Binding
Inhibition of beta2-adrenergic receptor in guinea pig tracheal chain assessed as reversal of isoproterenol-induced effect after 15 minsInhibition of beta2-adrenergic receptor in guinea pig tracheal chain assessed as reversal of isoproterenol-induced effect after 15 mins
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00199a012
62882 3126 60 None -4 43 Guinea pig 6.6 pKd = 6.6 Binding
Inhibition of beta2-adrenergic receptor in guinea pig tracheal chain assessed as reversal of isoproterenol-induced effect after 15 minsInhibition of beta2-adrenergic receptor in guinea pig tracheal chain assessed as reversal of isoproterenol-induced effect after 15 mins
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00199a012
63 3126 60 None -4 43 Guinea pig 6.6 pKd = 6.6 Binding
Inhibition of beta2-adrenergic receptor in guinea pig tracheal chain assessed as reversal of isoproterenol-induced effect after 15 minsInhibition of beta2-adrenergic receptor in guinea pig tracheal chain assessed as reversal of isoproterenol-induced effect after 15 mins
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00199a012
66366 3126 60 None -4 43 Guinea pig 6.6 pKd = 6.6 Binding
Inhibition of beta2-adrenergic receptor in guinea pig tracheal chain assessed as reversal of isoproterenol-induced effect after 15 minsInhibition of beta2-adrenergic receptor in guinea pig tracheal chain assessed as reversal of isoproterenol-induced effect after 15 mins
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00199a012
91536 3126 60 None -4 43 Guinea pig 6.6 pKd = 6.6 Binding
Inhibition of beta2-adrenergic receptor in guinea pig tracheal chain assessed as reversal of isoproterenol-induced effect after 15 minsInhibition of beta2-adrenergic receptor in guinea pig tracheal chain assessed as reversal of isoproterenol-induced effect after 15 mins
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00199a012
CHEMBL27 3126 60 None -4 43 Guinea pig 6.6 pKd = 6.6 Binding
Inhibition of beta2-adrenergic receptor in guinea pig tracheal chain assessed as reversal of isoproterenol-induced effect after 15 minsInhibition of beta2-adrenergic receptor in guinea pig tracheal chain assessed as reversal of isoproterenol-induced effect after 15 mins
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00199a012
CHEMBL452861 3126 60 None -4 43 Guinea pig 6.6 pKd = 6.6 Binding
Inhibition of beta2-adrenergic receptor in guinea pig tracheal chain assessed as reversal of isoproterenol-induced effect after 15 minsInhibition of beta2-adrenergic receptor in guinea pig tracheal chain assessed as reversal of isoproterenol-induced effect after 15 mins
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00199a012
DB00571 3126 60 None -4 43 Guinea pig 6.6 pKd = 6.6 Binding
Inhibition of beta2-adrenergic receptor in guinea pig tracheal chain assessed as reversal of isoproterenol-induced effect after 15 minsInhibition of beta2-adrenergic receptor in guinea pig tracheal chain assessed as reversal of isoproterenol-induced effect after 15 mins
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00199a012
105 3392 84 None -5 6 Guinea pig 6.6 pKd = 6.6 Binding
Agonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring assessed as bronchorelaxation activity against histamine-induced contractionAgonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring assessed as bronchorelaxation activity against histamine-induced contraction
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1016/j.bmcl.2014.12.077
2083 3392 84 None -5 6 Guinea pig 6.6 pKd = 6.6 Binding
Agonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring assessed as bronchorelaxation activity against histamine-induced contractionAgonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring assessed as bronchorelaxation activity against histamine-induced contraction
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1016/j.bmcl.2014.12.077
558 3392 84 None -5 6 Guinea pig 6.6 pKd = 6.6 Binding
Agonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring assessed as bronchorelaxation activity against histamine-induced contractionAgonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring assessed as bronchorelaxation activity against histamine-induced contraction
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1016/j.bmcl.2014.12.077
CHEMBL714 3392 84 None -5 6 Guinea pig 6.6 pKd = 6.6 Binding
Agonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring assessed as bronchorelaxation activity against histamine-induced contractionAgonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring assessed as bronchorelaxation activity against histamine-induced contraction
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1016/j.bmcl.2014.12.077
DB01001 3392 84 None -5 6 Guinea pig 6.6 pKd = 6.6 Binding
Agonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring assessed as bronchorelaxation activity against histamine-induced contractionAgonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring assessed as bronchorelaxation activity against histamine-induced contraction
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1016/j.bmcl.2014.12.077
13157406 9324 0 None -144 2 Guinea pig 6.6 pKd = 6.6 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 357 8 3 5 3.5 CC(C)NCC(O)COc1ccc(-c2nc(-c3cccs3)c[nH]2)cc1 10.1021/jm00156a028
CHEMBL11171 9324 0 None -144 2 Guinea pig 6.6 pKd = 6.6 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 357 8 3 5 3.5 CC(C)NCC(O)COc1ccc(-c2nc(-c3cccs3)c[nH]2)cc1 10.1021/jm00156a028
1499 2052 43 None -9 17 Guinea pig 7.6 pKd = 7.6 Binding
Agonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring at basal tone assessed as bronchorelaxation activityAgonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring at basal tone assessed as bronchorelaxation activity
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmcl.2014.12.077
3779 2052 43 None -9 17 Guinea pig 7.6 pKd = 7.6 Binding
Agonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring at basal tone assessed as bronchorelaxation activityAgonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring at basal tone assessed as bronchorelaxation activity
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmcl.2014.12.077
536 2052 43 None -9 17 Guinea pig 7.6 pKd = 7.6 Binding
Agonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring at basal tone assessed as bronchorelaxation activityAgonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring at basal tone assessed as bronchorelaxation activity
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmcl.2014.12.077
CHEMBL434 2052 43 None -9 17 Guinea pig 7.6 pKd = 7.6 Binding
Agonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring at basal tone assessed as bronchorelaxation activityAgonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring at basal tone assessed as bronchorelaxation activity
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmcl.2014.12.077
DB01064 2052 43 None -9 17 Guinea pig 7.6 pKd = 7.6 Binding
Agonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring at basal tone assessed as bronchorelaxation activityAgonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring at basal tone assessed as bronchorelaxation activity
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmcl.2014.12.077
13040915 102446 0 None -50 2 Guinea pig 6.6 pKd = 6.6 Binding
Ability to block Beta-2 adrenergic receptor in guinea pig trachea preparationAbility to block Beta-2 adrenergic receptor in guinea pig trachea preparation
ChEMBL 325 10 2 7 0.8 CCOC(=O)CCNCC(O)COc1ccccc1C(=O)OC 10.1021/jm00354a003
CHEMBL30622 102446 0 None -50 2 Guinea pig 6.6 pKd = 6.6 Binding
Ability to block Beta-2 adrenergic receptor in guinea pig trachea preparationAbility to block Beta-2 adrenergic receptor in guinea pig trachea preparation
ChEMBL 325 10 2 7 0.8 CCOC(=O)CCNCC(O)COc1ccccc1C(=O)OC 10.1021/jm00354a003
1499 2052 43 None -33 17 Human 6.6 pKd = 6.6 Binding
Binding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nMBinding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nM
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmcl.2013.07.052
3779 2052 43 None -33 17 Human 6.6 pKd = 6.6 Binding
Binding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nMBinding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nM
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmcl.2013.07.052
536 2052 43 None -33 17 Human 6.6 pKd = 6.6 Binding
Binding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nMBinding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nM
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmcl.2013.07.052
CHEMBL434 2052 43 None -33 17 Human 6.6 pKd = 6.6 Binding
Binding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nMBinding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nM
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmcl.2013.07.052
DB01064 2052 43 None -33 17 Human 6.6 pKd = 6.6 Binding
Binding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nMBinding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nM
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmcl.2013.07.052
15578588 103637 2 None -6 2 Guinea pig 6.6 pKd = 6.6 Binding
In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.
ChEMBL 301 9 2 5 1.6 CCOC(=O)CCNCC(O)COc1ccccc1Cl 10.1021/jm00354a002
CHEMBL30942 103637 2 None -6 2 Guinea pig 6.6 pKd = 6.6 Binding
In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.
ChEMBL 301 9 2 5 1.6 CCOC(=O)CCNCC(O)COc1ccccc1Cl 10.1021/jm00354a002
2598 3707 52 None -6 5 Human 5.6 pKd = 5.6 Binding
Binding affinity to human adrenergic beta2 receptorBinding affinity to human adrenergic beta2 receptor
ChEMBL 225 3 4 4 1.5 OC(c1cc(O)cc(c1)O)CNC(C)(C)C 10.1016/j.ejmech.2008.12.016
5403 3707 52 None -6 5 Human 5.6 pKd = 5.6 Binding
Binding affinity to human adrenergic beta2 receptorBinding affinity to human adrenergic beta2 receptor
ChEMBL 225 3 4 4 1.5 OC(c1cc(O)cc(c1)O)CNC(C)(C)C 10.1016/j.ejmech.2008.12.016
560 3707 52 None -6 5 Human 5.6 pKd = 5.6 Binding
Binding affinity to human adrenergic beta2 receptorBinding affinity to human adrenergic beta2 receptor
ChEMBL 225 3 4 4 1.5 OC(c1cc(O)cc(c1)O)CNC(C)(C)C 10.1016/j.ejmech.2008.12.016
CHEMBL1760 3707 52 None -6 5 Human 5.6 pKd = 5.6 Binding
Binding affinity to human adrenergic beta2 receptorBinding affinity to human adrenergic beta2 receptor
ChEMBL 225 3 4 4 1.5 OC(c1cc(O)cc(c1)O)CNC(C)(C)C 10.1016/j.ejmech.2008.12.016
DB00871 3707 52 None -6 5 Human 5.6 pKd = 5.6 Binding
Binding affinity to human adrenergic beta2 receptorBinding affinity to human adrenergic beta2 receptor
ChEMBL 225 3 4 4 1.5 OC(c1cc(O)cc(c1)O)CNC(C)(C)C 10.1016/j.ejmech.2008.12.016
12462226 112129 1 None 1 2 Guinea pig 5.6 pKd = 5.6 Binding
Antagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 minsAntagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 mins
ChEMBL 223 5 2 3 2.0 COc1ccc(C)cc1C(O)CNC(C)C 10.1021/jm00208a015
CHEMBL3246235 112129 1 None 1 2 Guinea pig 5.6 pKd = 5.6 Binding
Antagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 minsAntagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 mins
ChEMBL 223 5 2 3 2.0 COc1ccc(C)cc1C(O)CNC(C)C 10.1021/jm00208a015
CHEMBL3302805 112129 1 None 1 2 Guinea pig 5.6 pKd = 5.6 Binding
Antagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 minsAntagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 mins
ChEMBL 223 5 2 3 2.0 COc1ccc(C)cc1C(O)CNC(C)C 10.1021/jm00208a015
2598 3707 52 None -6 5 Human 5.6 pKd = 5.6 Binding
Binding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nMBinding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nM
ChEMBL 225 3 4 4 1.5 OC(c1cc(O)cc(c1)O)CNC(C)(C)C 10.1016/j.bmcl.2013.07.052
5403 3707 52 None -6 5 Human 5.6 pKd = 5.6 Binding
Binding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nMBinding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nM
ChEMBL 225 3 4 4 1.5 OC(c1cc(O)cc(c1)O)CNC(C)(C)C 10.1016/j.bmcl.2013.07.052
560 3707 52 None -6 5 Human 5.6 pKd = 5.6 Binding
Binding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nMBinding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nM
ChEMBL 225 3 4 4 1.5 OC(c1cc(O)cc(c1)O)CNC(C)(C)C 10.1016/j.bmcl.2013.07.052
CHEMBL1760 3707 52 None -6 5 Human 5.6 pKd = 5.6 Binding
Binding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nMBinding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nM
ChEMBL 225 3 4 4 1.5 OC(c1cc(O)cc(c1)O)CNC(C)(C)C 10.1016/j.bmcl.2013.07.052
DB00871 3707 52 None -6 5 Human 5.6 pKd = 5.6 Binding
Binding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nMBinding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nM
ChEMBL 225 3 4 4 1.5 OC(c1cc(O)cc(c1)O)CNC(C)(C)C 10.1016/j.bmcl.2013.07.052
15578555 105854 3 None -1 2 Guinea pig 5.6 pKd = 5.6 Binding
In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.
ChEMBL 253 8 2 5 0.6 CCOC(=O)CNCC(O)COc1ccccc1 10.1021/jm00354a002
CHEMBL31392 105854 3 None -1 2 Guinea pig 5.6 pKd = 5.6 Binding
In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.
ChEMBL 253 8 2 5 0.6 CCOC(=O)CNCC(O)COc1ccccc1 10.1021/jm00354a002
15569837 106050 2 None -6 2 Guinea pig 5.6 pKd = 5.6 Binding
In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.
ChEMBL 301 9 2 5 1.6 CCOC(=O)CCNCC(O)COc1ccc(Cl)cc1 10.1021/jm00354a002
CHEMBL31411 106050 2 None -6 2 Guinea pig 5.6 pKd = 5.6 Binding
In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.
ChEMBL 301 9 2 5 1.6 CCOC(=O)CCNCC(O)COc1ccc(Cl)cc1 10.1021/jm00354a002
13157402 167772 0 None -398 2 Guinea pig 5.6 pKd = 5.6 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
ChEMBL 355 8 3 5 3.3 OC(CNC1CC1)COc1ccc(-c2nc(-c3cccs3)c[nH]2)cc1 10.1021/jm00361a004
CHEMBL434360 167772 0 None -398 2 Guinea pig 5.6 pKd = 5.6 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
ChEMBL 355 8 3 5 3.3 OC(CNC1CC1)COc1ccc(-c2nc(-c3cccs3)c[nH]2)cc1 10.1021/jm00361a004
29057664 157568 13 None 1 2 Human 4.6 pKd = 4.6 Binding
Displacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting methodDisplacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting method
ChEMBL 309 3 1 4 3.4 Cc1cc(O)c(CN(C)C)c2c1C(=O)/C(=C/c1ccccc1)O2 10.1021/acsmedchemlett.6b00363
8035384 157568 13 None 1 2 Human 4.6 pKd = 4.6 Binding
Displacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting methodDisplacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting method
ChEMBL 309 3 1 4 3.4 Cc1cc(O)c(CN(C)C)c2c1C(=O)/C(=C/c1ccccc1)O2 10.1021/acsmedchemlett.6b00363
CHEMBL4086982 157568 13 None 1 2 Human 4.6 pKd = 4.6 Binding
Displacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting methodDisplacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting method
ChEMBL 309 3 1 4 3.4 Cc1cc(O)c(CN(C)C)c2c1C(=O)/C(=C/c1ccccc1)O2 10.1021/acsmedchemlett.6b00363
16737369 142524 0 None - 1 Human 5.6 pKd = 5.6 Binding
Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.
ChEMBL 337 6 4 4 3.5 C[C@@H](Cc1cccc2ccccc12)NC[C@@H](O)c1cc(O)cc(O)c1 nan
CHEMBL389519 142524 0 None - 1 Human 5.6 pKd = 5.6 Binding
Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.
ChEMBL 337 6 4 4 3.5 C[C@@H](Cc1cccc2ccccc12)NC[C@@H](O)c1cc(O)cc(O)c1 nan
4606363 112215 3 None - 1 Guinea pig 4.6 pKd = 4.6 Binding
Antagonist activity at beta-2 adrenergic receptor in guinea pig right atrium assessed as inhibition of isoprenaline-induced effectAntagonist activity at beta-2 adrenergic receptor in guinea pig right atrium assessed as inhibition of isoprenaline-induced effect
ChEMBL 382 13 4 6 2.3 CC(C)NCC(O)COc1cccc(C(C)C)c1OCC(O)CNC(C)C 10.1021/jm00214a013
CHEMBL3272436 112215 3 None - 1 Guinea pig 4.6 pKd = 4.6 Binding
Antagonist activity at beta-2 adrenergic receptor in guinea pig right atrium assessed as inhibition of isoprenaline-induced effectAntagonist activity at beta-2 adrenergic receptor in guinea pig right atrium assessed as inhibition of isoprenaline-induced effect
ChEMBL 382 13 4 6 2.3 CC(C)NCC(O)COc1cccc(C(C)C)c1OCC(O)CNC(C)C 10.1021/jm00214a013
CHEMBL3304621 112215 3 None - 1 Guinea pig 4.6 pKd = 4.6 Binding
Antagonist activity at beta-2 adrenergic receptor in guinea pig right atrium assessed as inhibition of isoprenaline-induced effectAntagonist activity at beta-2 adrenergic receptor in guinea pig right atrium assessed as inhibition of isoprenaline-induced effect
ChEMBL 382 13 4 6 2.3 CC(C)NCC(O)COc1cccc(C(C)C)c1OCC(O)CNC(C)C 10.1021/jm00214a013
13621712 75581 0 None -1288 2 Guinea pig 4.6 pKd = 4.6 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 453 11 3 6 4.0 COc1ccc(CCNC[C@H](O)COc2ccc(-c3nc(C(C)(C)C)c[nH]3)cc2)cc1OC 10.1021/jm00156a028
CHEMBL2052006 75581 0 None -1288 2 Guinea pig 4.6 pKd = 4.6 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 453 11 3 6 4.0 COc1ccc(CCNC[C@H](O)COc2ccc(-c3nc(C(C)(C)C)c[nH]3)cc2)cc1OC 10.1021/jm00156a028
2249 509 106 None -33 12 Human 6.6 pKd = 6.6 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation counting
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1021/acs.jmedchem.6b00358
255 509 106 None -33 12 Human 6.6 pKd = 6.6 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation counting
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1021/acs.jmedchem.6b00358
548 509 106 None -33 12 Human 6.6 pKd = 6.6 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation counting
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1021/acs.jmedchem.6b00358
CHEMBL24 509 106 None -33 12 Human 6.6 pKd = 6.6 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation counting
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1021/acs.jmedchem.6b00358
DB00335 509 106 None -33 12 Human 6.6 pKd = 6.6 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation counting
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1021/acs.jmedchem.6b00358
2297435 55302 6 None 10 2 Human 5.6 pKd = 5.6 Binding
Displacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting methodDisplacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting method
ChEMBL 253 7 1 2 3.5 C=CCNCCOc1ccccc1-c1ccccc1 10.1021/acsmedchemlett.6b00363
CHEMBL1621144 55302 6 None 10 2 Human 5.6 pKd = 5.6 Binding
Displacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting methodDisplacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting method
ChEMBL 253 7 1 2 3.5 C=CCNCCOc1ccccc1-c1ccccc1 10.1021/acsmedchemlett.6b00363
56598967 87819 0 None -275 2 Human 5.6 pKd = 5.6 Binding
Displacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 457 14 4 6 3.2 O=C(NCCNCC(O)COc1ccc(OCCOC2CCCC2)cc1)Nc1ccccc1 10.1021/jm400348g
CHEMBL2348211 87819 0 None -275 2 Human 5.6 pKd = 5.6 Binding
Displacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 457 14 4 6 3.2 O=C(NCCNCC(O)COc1ccc(OCCOC2CCCC2)cc1)Nc1ccccc1 10.1021/jm400348g
13157410 127801 0 None -446 2 Guinea pig 4.6 pKd = 4.6 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
ChEMBL 287 7 3 4 1.9 Cc1c[nH]c(-c2ccc(OCC(O)CNC3CC3)cc2)n1 10.1021/jm00361a004
CHEMBL366573 127801 0 None -446 2 Guinea pig 4.6 pKd = 4.6 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
ChEMBL 287 7 3 4 1.9 Cc1c[nH]c(-c2ccc(OCC(O)CNC3CC3)cc2)n1 10.1021/jm00361a004
688469 142383 2 None - 1 Human 4.6 pKd = 4.6 Binding
Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.
ChEMBL 303 6 5 5 2.1 C[C@@H](Cc1ccc(O)cc1)NC[C@@H](O)c1cc(O)cc(O)c1 nan
CHEMBL389390 142383 2 None - 1 Human 4.6 pKd = 4.6 Binding
Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.
ChEMBL 303 6 5 5 2.1 C[C@@H](Cc1ccc(O)cc1)NC[C@@H](O)c1cc(O)cc(O)c1 nan
118725500 116589 0 None - 1 Guinea pig 7.6 pKd = 7.6 Binding
Agonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring assessed as bronchorelaxation activity against histamine-induced contractionAgonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring assessed as bronchorelaxation activity against histamine-induced contraction
ChEMBL 323 5 3 4 1.6 CC(C)C[B-]1(O)OCc2cc([C@@H](O)C[NH2+]C(C)(C)C)ccc2O1 10.1016/j.bmcl.2014.12.077
CHEMBL3393402 116589 0 None - 1 Guinea pig 7.6 pKd = 7.6 Binding
Agonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring assessed as bronchorelaxation activity against histamine-induced contractionAgonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring assessed as bronchorelaxation activity against histamine-induced contraction
ChEMBL 323 5 3 4 1.6 CC(C)C[B-]1(O)OCc2cc([C@@H](O)C[NH2+]C(C)(C)C)ccc2O1 10.1016/j.bmcl.2014.12.077
56599101 87806 0 None -42 2 Human 6.5 pKd = 6.5 Binding
Displacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 475 14 4 6 3.3 O=C(NCCNCC(O)COc1ccc(OCCOC2CCCC2)cc1)Nc1cccc(F)c1 10.1021/jm400348g
CHEMBL2348198 87806 0 None -42 2 Human 6.5 pKd = 6.5 Binding
Displacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 475 14 4 6 3.3 O=C(NCCNCC(O)COc1ccc(OCCOC2CCCC2)cc1)Nc1cccc(F)c1 10.1021/jm400348g
56599229 87808 0 None -37 2 Human 5.5 pKd = 5.5 Binding
Displacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 491 14 4 6 3.8 O=C(NCCNCC(O)COc1ccc(OCCOC2CCCC2)cc1)Nc1ccccc1Cl 10.1021/jm400348g
CHEMBL2348200 87808 0 None -37 2 Human 5.5 pKd = 5.5 Binding
Displacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 491 14 4 6 3.8 O=C(NCCNCC(O)COc1ccc(OCCOC2CCCC2)cc1)Nc1ccccc1Cl 10.1021/jm400348g
16736092 85342 0 None 1 2 Human 4.5 pKd = 4.5 Binding
Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.
ChEMBL 287 6 4 4 2.4 C[C@@H](Cc1ccccc1)NC[C@@H](O)c1cc(O)cc(O)c1 nan
CHEMBL229390 85342 0 None 1 2 Human 4.5 pKd = 4.5 Binding
Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.
ChEMBL 287 6 4 4 2.4 C[C@@H](Cc1ccccc1)NC[C@@H](O)c1cc(O)cc(O)c1 nan
123133227 143604 0 None - 1 Human 4.5 pKd = 4.5 Binding
Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.
ChEMBL 302 6 5 5 1.9 C[C@@H](Cc1cccc(N)c1)NC[C@@H](O)c1cc(O)cc(O)c1 nan
CHEMBL3903905 143604 0 None - 1 Human 4.5 pKd = 4.5 Binding
Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.
ChEMBL 302 6 5 5 1.9 C[C@@H](Cc1cccc(N)c1)NC[C@@H](O)c1cc(O)cc(O)c1 nan
13621595 7498 0 None -575 2 Guinea pig 4.5 pKd = 4.5 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 489 11 3 6 3.7 COc1ccc(CCNCC(O)COc2ccc(-c3nc(C)c[nH]3)cc2Br)cc1OC 10.1021/jm00156a028
CHEMBL10879 7498 0 None -575 2 Guinea pig 4.5 pKd = 4.5 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 489 11 3 6 3.7 COc1ccc(CCNCC(O)COc2ccc(-c3nc(C)c[nH]3)cc2Br)cc1OC 10.1021/jm00156a028
16737411 142657 0 None 8 2 Human 5.5 pKd = 5.5 Binding
Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.
ChEMBL 287 6 4 4 2.4 C[C@H](Cc1ccccc1)NC[C@H](O)c1cc(O)cc(O)c1 nan
CHEMBL389629 142657 0 None 8 2 Human 5.5 pKd = 5.5 Binding
Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.
ChEMBL 287 6 4 4 2.4 C[C@H](Cc1ccccc1)NC[C@H](O)c1cc(O)cc(O)c1 nan
13157374 77597 0 None -1412 2 Guinea pig 4.5 pKd = 4.5 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
ChEMBL 397 11 3 6 2.7 COc1ccc(CCNC[C@H](O)COc2ccc(-c3ncc[nH]3)cc2)cc1OC 10.1021/jm00361a004
CHEMBL2096751 77597 0 None -1412 2 Guinea pig 4.5 pKd = 4.5 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
ChEMBL 397 11 3 6 2.7 COc1ccc(CCNC[C@H](O)COc2ccc(-c3ncc[nH]3)cc2)cc1OC 10.1021/jm00361a004
165193 3126 60 None -4 43 Guinea pig 8.5 pKd = 8.5 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00361a004
2303 3126 60 None -4 43 Guinea pig 8.5 pKd = 8.5 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00361a004
4946 3126 60 None -4 43 Guinea pig 8.5 pKd = 8.5 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00361a004
564 3126 60 None -4 43 Guinea pig 8.5 pKd = 8.5 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00361a004
62882 3126 60 None -4 43 Guinea pig 8.5 pKd = 8.5 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00361a004
63 3126 60 None -4 43 Guinea pig 8.5 pKd = 8.5 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00361a004
66366 3126 60 None -4 43 Guinea pig 8.5 pKd = 8.5 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00361a004
91536 3126 60 None -4 43 Guinea pig 8.5 pKd = 8.5 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00361a004
CHEMBL27 3126 60 None -4 43 Guinea pig 8.5 pKd = 8.5 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00361a004
CHEMBL452861 3126 60 None -4 43 Guinea pig 8.5 pKd = 8.5 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00361a004
DB00571 3126 60 None -4 43 Guinea pig 8.5 pKd = 8.5 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00361a004
12398053 110033 0 None - 1 Guinea pig 8.5 pKd = 8.5 Binding
Inhibition of beta2-adrenergic receptor in guinea pig tracheal chain assessed as reversal of isoproterenol-induced effect after 15 minsInhibition of beta2-adrenergic receptor in guinea pig tracheal chain assessed as reversal of isoproterenol-induced effect after 15 mins
ChEMBL 227 2 2 2 2.6 CC1(C)NC1C(O)c1ccc2ccccc2c1 10.1021/jm00199a012
CHEMBL3251300 110033 0 None - 1 Guinea pig 8.5 pKd = 8.5 Binding
Inhibition of beta2-adrenergic receptor in guinea pig tracheal chain assessed as reversal of isoproterenol-induced effect after 15 minsInhibition of beta2-adrenergic receptor in guinea pig tracheal chain assessed as reversal of isoproterenol-induced effect after 15 mins
ChEMBL 227 2 2 2 2.6 CC1(C)NC1C(O)c1ccc2ccccc2c1 10.1021/jm00199a012
54757126 65147 0 None 57 3 Human 8.5 pKd = 8.5 Binding
Displacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cells
ChEMBL 893 26 4 10 6.8 O=C(CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1)NCCOCCOCCNCC(O)COc1cccc2ccccc12 10.1021/jm2008562
CHEMBL1830492 65147 0 None 57 3 Human 8.5 pKd = 8.5 Binding
Displacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cells
ChEMBL 893 26 4 10 6.8 O=C(CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1)NCCOCCOCCNCC(O)COc1cccc2ccccc12 10.1021/jm2008562
165193 3126 60 None -4 43 Guinea pig 8.5 pKd = 8.5 Binding
Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00376a011
2303 3126 60 None -4 43 Guinea pig 8.5 pKd = 8.5 Binding
Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00376a011
4946 3126 60 None -4 43 Guinea pig 8.5 pKd = 8.5 Binding
Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00376a011
564 3126 60 None -4 43 Guinea pig 8.5 pKd = 8.5 Binding
Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00376a011
62882 3126 60 None -4 43 Guinea pig 8.5 pKd = 8.5 Binding
Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00376a011
63 3126 60 None -4 43 Guinea pig 8.5 pKd = 8.5 Binding
Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00376a011
66366 3126 60 None -4 43 Guinea pig 8.5 pKd = 8.5 Binding
Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00376a011
91536 3126 60 None -4 43 Guinea pig 8.5 pKd = 8.5 Binding
Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00376a011
CHEMBL27 3126 60 None -4 43 Guinea pig 8.5 pKd = 8.5 Binding
Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00376a011
CHEMBL452861 3126 60 None -4 43 Guinea pig 8.5 pKd = 8.5 Binding
Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00376a011
DB00571 3126 60 None -4 43 Guinea pig 8.5 pKd = 8.5 Binding
Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00376a011
165193 3126 60 None -4 43 Guinea pig 8.5 pKd = 8.5 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor determined as pA2 in guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor determined as pA2 in guinea pig trachea
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00145a008
2303 3126 60 None -4 43 Guinea pig 8.5 pKd = 8.5 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor determined as pA2 in guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor determined as pA2 in guinea pig trachea
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00145a008
4946 3126 60 None -4 43 Guinea pig 8.5 pKd = 8.5 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor determined as pA2 in guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor determined as pA2 in guinea pig trachea
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00145a008
564 3126 60 None -4 43 Guinea pig 8.5 pKd = 8.5 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor determined as pA2 in guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor determined as pA2 in guinea pig trachea
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00145a008
62882 3126 60 None -4 43 Guinea pig 8.5 pKd = 8.5 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor determined as pA2 in guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor determined as pA2 in guinea pig trachea
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00145a008
63 3126 60 None -4 43 Guinea pig 8.5 pKd = 8.5 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor determined as pA2 in guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor determined as pA2 in guinea pig trachea
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00145a008
66366 3126 60 None -4 43 Guinea pig 8.5 pKd = 8.5 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor determined as pA2 in guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor determined as pA2 in guinea pig trachea
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00145a008
91536 3126 60 None -4 43 Guinea pig 8.5 pKd = 8.5 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor determined as pA2 in guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor determined as pA2 in guinea pig trachea
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00145a008
CHEMBL27 3126 60 None -4 43 Guinea pig 8.5 pKd = 8.5 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor determined as pA2 in guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor determined as pA2 in guinea pig trachea
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00145a008
CHEMBL452861 3126 60 None -4 43 Guinea pig 8.5 pKd = 8.5 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor determined as pA2 in guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor determined as pA2 in guinea pig trachea
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00145a008
DB00571 3126 60 None -4 43 Guinea pig 8.5 pKd = 8.5 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor determined as pA2 in guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor determined as pA2 in guinea pig trachea
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00145a008
21296271 96474 3 None 1 2 Guinea pig 4.5 pKd = 4.5 Binding
Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.
ChEMBL 241 7 2 3 1.9 CC(C)(C)NCC(O)COC(C1CC1)C1CC1 10.1021/jm00376a011
CHEMBL26607 96474 3 None 1 2 Guinea pig 4.5 pKd = 4.5 Binding
Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.
ChEMBL 241 7 2 3 1.9 CC(C)(C)NCC(O)COC(C1CC1)C1CC1 10.1021/jm00376a011
123133226 160347 0 None - 1 Human 4.5 pKd = 4.5 Binding
Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.
ChEMBL 302 6 5 5 1.9 C[C@H](Cc1cccc(N)c1)NC[C@@H](O)c1cc(O)cc(O)c1 nan
CHEMBL4115254 160347 0 None - 1 Human 4.5 pKd = 4.5 Binding
Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.
ChEMBL 302 6 5 5 1.9 C[C@H](Cc1cccc(N)c1)NC[C@@H](O)c1cc(O)cc(O)c1 nan
192962 109940 12 None -2 2 Guinea pig 6.5 pKd = 6.5 Binding
Antagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 minsAntagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 mins
ChEMBL 193 4 2 2 2.0 Cc1ccc(C(O)CNC(C)C)cc1 10.1021/jm00208a015
CHEMBL3246231 109940 12 None -2 2 Guinea pig 6.5 pKd = 6.5 Binding
Antagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 minsAntagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 mins
ChEMBL 193 4 2 2 2.0 Cc1ccc(C(O)CNC(C)C)cc1 10.1021/jm00208a015
15578594 106567 2 None -1 2 Guinea pig 6.5 pKd = 6.5 Binding
In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.
ChEMBL 281 9 2 5 1.3 CCOC(=O)CCNCC(O)COc1cccc(C)c1 10.1021/jm00354a002
CHEMBL31568 106567 2 None -1 2 Guinea pig 6.5 pKd = 6.5 Binding
In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.
ChEMBL 281 9 2 5 1.3 CCOC(=O)CCNCC(O)COc1cccc(C)c1 10.1021/jm00354a002
10443654 108681 1 None - 1 Bovine 5.5 pKd = 5.5 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 225 5 4 4 0.9 CC(C)NCC(O)c1ccc(O)c(CO)c1 10.1021/jm00147a037
CHEMBL321468 108681 1 None - 1 Bovine 5.5 pKd = 5.5 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 225 5 4 4 0.9 CC(C)NCC(O)c1ccc(O)c(CO)c1 10.1021/jm00147a037
12238214 25252 8 None -19 2 Guinea pig 5.5 pKd = 5.5 Binding
Ability to block Beta-2 adrenergic receptor in guinea pig trachea preparationAbility to block Beta-2 adrenergic receptor in guinea pig trachea preparation
ChEMBL 267 7 2 5 1.2 COC(=O)c1ccc(OCC(O)CNC(C)C)cc1 10.1021/jm00354a003
CHEMBL13504 25252 8 None -19 2 Guinea pig 5.5 pKd = 5.5 Binding
Ability to block Beta-2 adrenergic receptor in guinea pig trachea preparationAbility to block Beta-2 adrenergic receptor in guinea pig trachea preparation
ChEMBL 267 7 2 5 1.2 COC(=O)c1ccc(OCC(O)CNC(C)C)cc1 10.1021/jm00354a003
13040894 99554 0 None -12 2 Guinea pig 5.5 pKd = 5.5 Binding
Ability to block Beta-2 adrenergic receptor in guinea pig trachea preparationAbility to block Beta-2 adrenergic receptor in guinea pig trachea preparation
ChEMBL 309 10 2 5 1.9 COC(=O)CCCc1ccc(OCC(O)CNC(C)C)cc1 10.1021/jm00354a003
CHEMBL286894 99554 0 None -12 2 Guinea pig 5.5 pKd = 5.5 Binding
Ability to block Beta-2 adrenergic receptor in guinea pig trachea preparationAbility to block Beta-2 adrenergic receptor in guinea pig trachea preparation
ChEMBL 309 10 2 5 1.9 COC(=O)CCCc1ccc(OCC(O)CNC(C)C)cc1 10.1021/jm00354a003
13621752 96891 0 None -144 2 Guinea pig 5.5 pKd = 5.5 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 425 12 3 6 2.9 COc1ccc(CCNCC(O)COc2ccc(Cc3nc(C)c[nH]3)cc2)cc1OC 10.1021/jm00156a028
CHEMBL269467 96891 0 None -144 2 Guinea pig 5.5 pKd = 5.5 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 425 12 3 6 2.9 COc1ccc(CCNCC(O)COc2ccc(Cc3nc(C)c[nH]3)cc2)cc1OC 10.1021/jm00156a028
13621642 6113 0 None -2754 2 Guinea pig 4.5 pKd = 4.5 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 453 12 3 7 3.2 COc1ccc(CCNCC(O)COc2ccc(-c3nc(C(C)=O)c(C)[nH]3)cc2)cc1OC 10.1021/jm00156a028
CHEMBL10813 6113 0 None -2754 2 Guinea pig 4.5 pKd = 4.5 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 453 12 3 7 3.2 COc1ccc(CCNCC(O)COc2ccc(-c3nc(C(C)=O)c(C)[nH]3)cc2)cc1OC 10.1021/jm00156a028
16735774 147015 0 None - 1 Human 4.5 pKd = 4.5 Binding
Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.
ChEMBL 267 8 4 4 2.7 CCCCC[C@H](C)NC[C@H](O)c1cc(O)cc(O)c1 nan
CHEMBL3930835 147015 0 None - 1 Human 4.5 pKd = 4.5 Binding
Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.
ChEMBL 267 8 4 4 2.7 CCCCC[C@H](C)NC[C@H](O)c1cc(O)cc(O)c1 nan
12606684 95615 3 None 15 2 Guinea pig 7.5 pKd = 7.5 Binding
Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.
ChEMBL 203 6 2 3 1.4 CC(C)COCC(O)CNC(C)(C)C 10.1021/jm00376a011
CHEMBL1161388 95615 3 None 15 2 Guinea pig 7.5 pKd = 7.5 Binding
Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.
ChEMBL 203 6 2 3 1.4 CC(C)COCC(O)CNC(C)(C)C 10.1021/jm00376a011
CHEMBL26003 95615 3 None 15 2 Guinea pig 7.5 pKd = 7.5 Binding
Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.
ChEMBL 203 6 2 3 1.4 CC(C)COCC(O)CNC(C)(C)C 10.1021/jm00376a011
23276420 110903 4 None - 1 Guinea pig 6.5 pKd = 6.5 Binding
Antagonist activity at beta-2 adrenergic receptor in guinea pig right atrium assessed as inhibition of isoprenaline-induced effectAntagonist activity at beta-2 adrenergic receptor in guinea pig right atrium assessed as inhibition of isoprenaline-induced effect
ChEMBL 340 12 4 6 1.2 CC(C)NCC(O)COc1ccccc1OCC(O)CNC(C)C 10.1021/jm00214a013
CHEMBL3272434 110903 4 None - 1 Guinea pig 6.5 pKd = 6.5 Binding
Antagonist activity at beta-2 adrenergic receptor in guinea pig right atrium assessed as inhibition of isoprenaline-induced effectAntagonist activity at beta-2 adrenergic receptor in guinea pig right atrium assessed as inhibition of isoprenaline-induced effect
ChEMBL 340 12 4 6 1.2 CC(C)NCC(O)COc1ccccc1OCC(O)CNC(C)C 10.1021/jm00214a013
12521601 128111 0 None -20 2 Guinea pig 7.5 pKd = 7.5 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
ChEMBL 371 7 3 5 3.9 CC(C)(C)NCC(O)COc1ccc(-c2nc(-c3cccs3)c[nH]2)cc1 10.1021/jm00361a004
CHEMBL366769 128111 0 None -20 2 Guinea pig 7.5 pKd = 7.5 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
ChEMBL 371 7 3 5 3.9 CC(C)(C)NCC(O)COc1ccc(-c2nc(-c3cccs3)c[nH]2)cc1 10.1021/jm00361a004
1499 2052 43 None -8 17 Bovine 6.5 pKd = 6.5 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm00147a037
3779 2052 43 None -8 17 Bovine 6.5 pKd = 6.5 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm00147a037
536 2052 43 None -8 17 Bovine 6.5 pKd = 6.5 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm00147a037
CHEMBL434 2052 43 None -8 17 Bovine 6.5 pKd = 6.5 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm00147a037
DB01064 2052 43 None -8 17 Bovine 6.5 pKd = 6.5 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm00147a037
2405 658 71 None -58 4 Human 4.5 pKd = 4.5 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation counting
ChEMBL 325 12 2 5 2.4 OC(COc1ccc(cc1)COCCOC(C)C)CNC(C)C 10.1021/acs.jmedchem.6b00358
380 658 71 None -58 4 Human 4.5 pKd = 4.5 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation counting
ChEMBL 325 12 2 5 2.4 OC(COc1ccc(cc1)COCCOC(C)C)CNC(C)C 10.1021/acs.jmedchem.6b00358
7129 658 71 None -58 4 Human 4.5 pKd = 4.5 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation counting
ChEMBL 325 12 2 5 2.4 OC(COc1ccc(cc1)COCCOC(C)C)CNC(C)C 10.1021/acs.jmedchem.6b00358
CHEMBL645 658 71 None -58 4 Human 4.5 pKd = 4.5 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation counting
ChEMBL 325 12 2 5 2.4 OC(COc1ccc(cc1)COCCOC(C)C)CNC(C)C 10.1021/acs.jmedchem.6b00358
DB00612 658 71 None -58 4 Human 4.5 pKd = 4.5 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation counting
ChEMBL 325 12 2 5 2.4 OC(COc1ccc(cc1)COCCOC(C)C)CNC(C)C 10.1021/acs.jmedchem.6b00358
4191179 112264 1 None - 1 Guinea pig 6.5 pKd = 6.5 Binding
Antagonist activity at beta-2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of isoprenaline-induced effectAntagonist activity at beta-2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of isoprenaline-induced effect
ChEMBL 382 13 4 6 2.3 CC(C)NCC(O)COc1ccc(C(C)C)cc1OCC(O)CNC(C)C 10.1021/jm00214a013
CHEMBL3272438 112264 1 None - 1 Guinea pig 6.5 pKd = 6.5 Binding
Antagonist activity at beta-2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of isoprenaline-induced effectAntagonist activity at beta-2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of isoprenaline-induced effect
ChEMBL 382 13 4 6 2.3 CC(C)NCC(O)COc1ccc(C(C)C)cc1OCC(O)CNC(C)C 10.1021/jm00214a013
CHEMBL3305475 112264 1 None - 1 Guinea pig 6.5 pKd = 6.5 Binding
Antagonist activity at beta-2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of isoprenaline-induced effectAntagonist activity at beta-2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of isoprenaline-induced effect
ChEMBL 382 13 4 6 2.3 CC(C)NCC(O)COc1ccc(C(C)C)cc1OCC(O)CNC(C)C 10.1021/jm00214a013
3527871 112263 1 None - 1 Guinea pig 5.5 pKd = 5.5 Binding
Antagonist activity at beta-2 adrenergic receptor in guinea pig right atrium assessed as inhibition of isoprenaline-induced effectAntagonist activity at beta-2 adrenergic receptor in guinea pig right atrium assessed as inhibition of isoprenaline-induced effect
ChEMBL 354 12 4 6 1.5 Cc1cccc(OCC(O)CNC(C)C)c1OCC(O)CNC(C)C 10.1021/jm00214a013
CHEMBL3272435 112263 1 None - 1 Guinea pig 5.5 pKd = 5.5 Binding
Antagonist activity at beta-2 adrenergic receptor in guinea pig right atrium assessed as inhibition of isoprenaline-induced effectAntagonist activity at beta-2 adrenergic receptor in guinea pig right atrium assessed as inhibition of isoprenaline-induced effect
ChEMBL 354 12 4 6 1.5 Cc1cccc(OCC(O)CNC(C)C)c1OCC(O)CNC(C)C 10.1021/jm00214a013
CHEMBL3305474 112263 1 None - 1 Guinea pig 5.5 pKd = 5.5 Binding
Antagonist activity at beta-2 adrenergic receptor in guinea pig right atrium assessed as inhibition of isoprenaline-induced effectAntagonist activity at beta-2 adrenergic receptor in guinea pig right atrium assessed as inhibition of isoprenaline-induced effect
ChEMBL 354 12 4 6 1.5 Cc1cccc(OCC(O)CNC(C)C)c1OCC(O)CNC(C)C 10.1021/jm00214a013
13621721 161566 0 None -2630 2 Guinea pig 4.5 pKd = 4.5 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 420 10 3 6 3.8 OC(CNCCc1ccncc1)COc1ccc(-c2nc(-c3cccs3)c[nH]2)cc1 10.1021/jm00156a028
CHEMBL416151 161566 0 None -2630 2 Guinea pig 4.5 pKd = 4.5 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 420 10 3 6 3.8 OC(CNCCc1ccncc1)COc1ccc(-c2nc(-c3cccs3)c[nH]2)cc1 10.1021/jm00156a028
16735272 85371 0 None 46 2 Human 6.5 pKd = 6.5 Binding
Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.
ChEMBL 337 6 4 4 3.5 C[C@@H](Cc1cccc2ccccc12)NC[C@H](O)c1cc(O)cc(O)c1 nan
CHEMBL229614 85371 0 None 46 2 Human 6.5 pKd = 6.5 Binding
Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.
ChEMBL 337 6 4 4 3.5 C[C@@H](Cc1cccc2ccccc12)NC[C@H](O)c1cc(O)cc(O)c1 nan
13621686 9739 0 None -575 2 Guinea pig 5.5 pKd = 5.5 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 469 13 3 8 2.8 CCOC(=O)c1c[nH]c(-c2ccc(OCC(O)CNCCc3ccc(OC)c(OC)c3)cc2)n1 10.1021/jm00156a028
CHEMBL11406 9739 0 None -575 2 Guinea pig 5.5 pKd = 5.5 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 469 13 3 8 2.8 CCOC(=O)c1c[nH]c(-c2ccc(OCC(O)CNCCc3ccc(OC)c(OC)c3)cc2)n1 10.1021/jm00156a028
13621774 98015 0 None -208 2 Guinea pig 5.5 pKd = 5.5 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 427 13 3 7 2.6 COc1ccc(CCNCC(O)COc2ccc(OCc3ncc[nH]3)cc2)cc1OC 10.1021/jm00156a028
CHEMBL275934 98015 0 None -208 2 Guinea pig 5.5 pKd = 5.5 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 427 13 3 7 2.6 COc1ccc(CCNCC(O)COc2ccc(OCc3ncc[nH]3)cc2)cc1OC 10.1021/jm00156a028
13157371 59711 0 None -3235 2 Guinea pig 4.5 pKd = 4.5 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
ChEMBL 397 11 3 6 2.7 COc1ccc(CCNCC(O)COc2ccc(-c3ncc[nH]3)cc2)cc1OC 10.1021/jm00361a004
CHEMBL173629 59711 0 None -3235 2 Guinea pig 4.5 pKd = 4.5 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
ChEMBL 397 11 3 6 2.7 COc1ccc(CCNCC(O)COc2ccc(-c3ncc[nH]3)cc2)cc1OC 10.1021/jm00361a004
688468 141788 7 None 190 2 Human 6.5 pKd = 6.5 Binding
Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.
ChEMBL 303 6 5 5 2.1 C[C@H](Cc1ccc(O)cc1)NC[C@H](O)c1cc(O)cc(O)c1 nan
CHEMBL388570 141788 7 None 190 2 Human 6.5 pKd = 6.5 Binding
Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.
ChEMBL 303 6 5 5 2.1 C[C@H](Cc1ccc(O)cc1)NC[C@H](O)c1cc(O)cc(O)c1 nan
1534386 92568 39 None - 1 Human 6.5 pKd = 6.5 Binding
Binding affinity to N-terminal FLAG-tagged C-terminal His-10-tagged human beta2 adrenoceptor expressed in insect Sf9 cells by surface plasmon resonance analysis in presence of maltose neopentyl glycolBinding affinity to N-terminal FLAG-tagged C-terminal His-10-tagged human beta2 adrenoceptor expressed in insect Sf9 cells by surface plasmon resonance analysis in presence of maltose neopentyl glycol
ChEMBL 213 1 1 3 1.6 c1ccc2c(N3CCNCC3)ccnc2c1 10.1021/ml400312j
CHEMBL2441621 92568 39 None - 1 Human 6.5 pKd = 6.5 Binding
Binding affinity to N-terminal FLAG-tagged C-terminal His-10-tagged human beta2 adrenoceptor expressed in insect Sf9 cells by surface plasmon resonance analysis in presence of maltose neopentyl glycolBinding affinity to N-terminal FLAG-tagged C-terminal His-10-tagged human beta2 adrenoceptor expressed in insect Sf9 cells by surface plasmon resonance analysis in presence of maltose neopentyl glycol
ChEMBL 213 1 1 3 1.6 c1ccc2c(N3CCNCC3)ccnc2c1 10.1021/ml400312j
2799984 92567 75 None - 1 Human 5.5 pKd = 5.5 Binding
Binding affinity to N-terminal FLAG-tagged C-terminal His-10-tagged human beta2 adrenoceptor expressed in insect Sf9 cells by surface plasmon resonance analysisBinding affinity to N-terminal FLAG-tagged C-terminal His-10-tagged human beta2 adrenoceptor expressed in insect Sf9 cells by surface plasmon resonance analysis
ChEMBL 231 1 1 3 1.8 Clc1cncc(Cl)c1N1CCNCC1 10.1021/ml400312j
CHEMBL2441620 92567 75 None - 1 Human 5.5 pKd = 5.5 Binding
Binding affinity to N-terminal FLAG-tagged C-terminal His-10-tagged human beta2 adrenoceptor expressed in insect Sf9 cells by surface plasmon resonance analysisBinding affinity to N-terminal FLAG-tagged C-terminal His-10-tagged human beta2 adrenoceptor expressed in insect Sf9 cells by surface plasmon resonance analysis
ChEMBL 231 1 1 3 1.8 Clc1cncc(Cl)c1N1CCNCC1 10.1021/ml400312j
3322591 112270 2 None - 1 Guinea pig 5.5 pKd = 5.5 Binding
Antagonist activity at beta-2 adrenergic receptor in guinea pig right atrium assessed as inhibition of isoprenaline-induced effectAntagonist activity at beta-2 adrenergic receptor in guinea pig right atrium assessed as inhibition of isoprenaline-induced effect
ChEMBL 390 12 4 6 2.3 CC(C)NCC(O)COc1cc2ccccc2cc1OCC(O)CNC(C)C 10.1021/jm00214a013
CHEMBL3272440 112270 2 None - 1 Guinea pig 5.5 pKd = 5.5 Binding
Antagonist activity at beta-2 adrenergic receptor in guinea pig right atrium assessed as inhibition of isoprenaline-induced effectAntagonist activity at beta-2 adrenergic receptor in guinea pig right atrium assessed as inhibition of isoprenaline-induced effect
ChEMBL 390 12 4 6 2.3 CC(C)NCC(O)COc1cc2ccccc2cc1OCC(O)CNC(C)C 10.1021/jm00214a013
CHEMBL3305652 112270 2 None - 1 Guinea pig 5.5 pKd = 5.5 Binding
Antagonist activity at beta-2 adrenergic receptor in guinea pig right atrium assessed as inhibition of isoprenaline-induced effectAntagonist activity at beta-2 adrenergic receptor in guinea pig right atrium assessed as inhibition of isoprenaline-induced effect
ChEMBL 390 12 4 6 2.3 CC(C)NCC(O)COc1cc2ccccc2cc1OCC(O)CNC(C)C 10.1021/jm00214a013
56597179 87827 0 None -501 2 Human 5.5 pKd = 5.5 Binding
Displacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 473 14 5 7 2.9 O=C(NCCNCC(O)COc1ccc(OCCOC2CCCC2)cc1)Nc1ccc(O)cc1 10.1021/jm400348g
CHEMBL2348219 87827 0 None -501 2 Human 5.5 pKd = 5.5 Binding
Displacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 473 14 5 7 2.9 O=C(NCCNCC(O)COc1ccc(OCCOC2CCCC2)cc1)Nc1ccc(O)cc1 10.1021/jm400348g
12582 935 40 None -2 5 Bovine 7.4 pKd = 7.4 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 276 3 3 3 3.0 CC(C)(C)NCC(C1=CC(=C(C(=C1)Cl)N)Cl)O 10.1021/jm00147a037
2783 935 40 None -2 5 Bovine 7.4 pKd = 7.4 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 276 3 3 3 3.0 CC(C)(C)NCC(C1=CC(=C(C(=C1)Cl)N)Cl)O 10.1021/jm00147a037
CHEMBL49080 935 40 None -2 5 Bovine 7.4 pKd = 7.4 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 276 3 3 3 3.0 CC(C)(C)NCC(C1=CC(=C(C(=C1)Cl)N)Cl)O 10.1021/jm00147a037
DB01407 935 40 None -2 5 Bovine 7.4 pKd = 7.4 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 276 3 3 3 3.0 CC(C)(C)NCC(C1=CC(=C(C(=C1)Cl)N)Cl)O 10.1021/jm00147a037
13157382 61916 0 None -3981 2 Guinea pig 4.4 pKd = 4.4 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
ChEMBL 507 12 3 7 5.2 COc1ccc(CC(C)(C)NCC(O)COc2ccc(-c3nc(-c4cccs4)c[nH]3)cc2)cc1OC 10.1021/jm00361a004
CHEMBL177860 61916 0 None -3981 2 Guinea pig 4.4 pKd = 4.4 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
ChEMBL 507 12 3 7 5.2 COc1ccc(CC(C)(C)NCC(O)COc2ccc(-c3nc(-c4cccs4)c[nH]3)cc2)cc1OC 10.1021/jm00361a004
688467 85357 2 None 14 2 Human 5.4 pKd = 5.4 Binding
Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.
ChEMBL 303 6 5 5 2.1 C[C@@H](Cc1ccc(O)cc1)NC[C@H](O)c1cc(O)cc(O)c1 nan
CHEMBL229476 85357 2 None 14 2 Human 5.4 pKd = 5.4 Binding
Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.
ChEMBL 303 6 5 5 2.1 C[C@@H](Cc1ccc(O)cc1)NC[C@H](O)c1cc(O)cc(O)c1 nan
12484287 109215 0 None 2 2 Guinea pig 6.4 pKd = 6.4 Binding
Competitive antagonist activity at beta-2 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced tracheal relaxationCompetitive antagonist activity at beta-2 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced tracheal relaxation
ChEMBL 249 6 3 4 1.3 CC(C)NCC(O)COc1ccc2[nH]cnc2c1 10.1021/jm00188a019
CHEMBL3228930 109215 0 None 2 2 Guinea pig 6.4 pKd = 6.4 Binding
Competitive antagonist activity at beta-2 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced tracheal relaxationCompetitive antagonist activity at beta-2 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced tracheal relaxation
ChEMBL 249 6 3 4 1.3 CC(C)NCC(O)COc1ccc2[nH]cnc2c1 10.1021/jm00188a019
2184756 55591 3 None 12 2 Human 5.4 pKd = 5.4 Binding
Displacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting methodDisplacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting method
ChEMBL 285 8 0 3 3.3 CN(C)CCOCCOc1ccccc1-c1ccccc1 10.1021/acsmedchemlett.6b00363
CHEMBL1623548 55591 3 None 12 2 Human 5.4 pKd = 5.4 Binding
Displacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting methodDisplacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting method
ChEMBL 285 8 0 3 3.3 CN(C)CCOCCOc1ccccc1-c1ccccc1 10.1021/acsmedchemlett.6b00363
13621602 9721 0 None -1096 2 Guinea pig 5.4 pKd = 5.4 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 493 12 3 7 4.7 COc1ccc(CCNCC(O)COc2ccc(-c3nc(-c4cccs4)c[nH]3)cc2C)cc1OC 10.1021/jm00156a028
CHEMBL11396 9721 0 None -1096 2 Guinea pig 5.4 pKd = 5.4 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 493 12 3 7 4.7 COc1ccc(CCNCC(O)COc2ccc(-c3nc(-c4cccs4)c[nH]3)cc2C)cc1OC 10.1021/jm00156a028
13621653 75579 0 None -2238 2 Guinea pig 4.4 pKd = 4.4 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 441 13 3 7 2.8 COCc1c[nH]c(-c2ccc(OC[C@@H](O)CNCCc3ccc(OC)c(OC)c3)cc2)n1 10.1021/jm00156a028
CHEMBL2052004 75579 0 None -2238 2 Guinea pig 4.4 pKd = 4.4 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 441 13 3 7 2.8 COCc1c[nH]c(-c2ccc(OC[C@@H](O)CNCCc3ccc(OC)c(OC)c3)cc2)n1 10.1021/jm00156a028
678605 155901 3 None - 1 Human 4.4 pKd = 4.4 Binding
Displacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting methodDisplacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting method
ChEMBL 267 3 1 2 3.8 C[n+]1c(/C=C/Nc2ccccc2)sc2ccccc21 10.1021/acsmedchemlett.6b00363
678606 155901 3 None - 1 Human 4.4 pKd = 4.4 Binding
Displacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting methodDisplacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting method
ChEMBL 267 3 1 2 3.8 C[n+]1c(/C=C/Nc2ccccc2)sc2ccccc21 10.1021/acsmedchemlett.6b00363
CHEMBL4067230 155901 3 None - 1 Human 4.4 pKd = 4.4 Binding
Displacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting methodDisplacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting method
ChEMBL 267 3 1 2 3.8 C[n+]1c(/C=C/Nc2ccccc2)sc2ccccc21 10.1021/acsmedchemlett.6b00363
2775690 92565 47 None 15 6 Human 7.4 pKd = 7.4 Binding
Binding affinity to N-terminal FLAG-tagged C-terminal His-10-tagged human beta2 adrenoceptor expressed in insect Sf9 cells by surface plasmon resonance analysis in presence of maltose neopentyl glycolBinding affinity to N-terminal FLAG-tagged C-terminal His-10-tagged human beta2 adrenoceptor expressed in insect Sf9 cells by surface plasmon resonance analysis in presence of maltose neopentyl glycol
ChEMBL 295 1 1 3 3.0 Cc1ccc2nc(C(F)(F)F)cc(N3CCNCC3)c2c1 10.1021/ml400312j
CHEMBL2441619 92565 47 None 15 6 Human 7.4 pKd = 7.4 Binding
Binding affinity to N-terminal FLAG-tagged C-terminal His-10-tagged human beta2 adrenoceptor expressed in insect Sf9 cells by surface plasmon resonance analysis in presence of maltose neopentyl glycolBinding affinity to N-terminal FLAG-tagged C-terminal His-10-tagged human beta2 adrenoceptor expressed in insect Sf9 cells by surface plasmon resonance analysis in presence of maltose neopentyl glycol
ChEMBL 295 1 1 3 3.0 Cc1ccc2nc(C(F)(F)F)cc(N3CCNCC3)c2c1 10.1021/ml400312j
13040883 98705 0 None 1 2 Guinea pig 7.4 pKd = 7.4 Binding
Ability to block Beta-2 adrenergic receptor in guinea pig trachea preparationAbility to block Beta-2 adrenergic receptor in guinea pig trachea preparation
ChEMBL 297 8 3 6 0.6 COC(=O)c1ccccc1OCC(O)CNC(C)(C)CO 10.1021/jm00354a003
CHEMBL281298 98705 0 None 1 2 Guinea pig 7.4 pKd = 7.4 Binding
Ability to block Beta-2 adrenergic receptor in guinea pig trachea preparationAbility to block Beta-2 adrenergic receptor in guinea pig trachea preparation
ChEMBL 297 8 3 6 0.6 COC(=O)c1ccccc1OCC(O)CNC(C)(C)CO 10.1021/jm00354a003
15578592 99028 2 None -1 2 Guinea pig 7.4 pKd = 7.4 Binding
In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.
ChEMBL 281 9 2 5 1.3 CCOC(=O)CCNCC(O)COc1ccccc1C 10.1021/jm00354a002
CHEMBL283289 99028 2 None -1 2 Guinea pig 7.4 pKd = 7.4 Binding
In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.
ChEMBL 281 9 2 5 1.3 CCOC(=O)CCNCC(O)COc1ccccc1C 10.1021/jm00354a002
235055 106926 8 None -3 2 Guinea pig 7.4 pKd = 7.4 Binding
In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.
ChEMBL 223 7 2 3 1.7 CC(C)CNCC(O)COc1ccccc1 10.1021/jm00354a002
CHEMBL31811 106926 8 None -3 2 Guinea pig 7.4 pKd = 7.4 Binding
In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.
ChEMBL 223 7 2 3 1.7 CC(C)CNCC(O)COc1ccccc1 10.1021/jm00354a002
15578610 111649 0 None -2 2 Guinea pig 7.4 pKd = 7.4 Binding
In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.
ChEMBL 309 11 2 5 2.1 CCOC(=O)CCCCNCC(O)COc1ccccc1C 10.1021/jm00354a002
CHEMBL32902 111649 0 None -2 2 Guinea pig 7.4 pKd = 7.4 Binding
In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.
ChEMBL 309 11 2 5 2.1 CCOC(=O)CCCCNCC(O)COc1ccccc1C 10.1021/jm00354a002
12398051 110032 0 None 43 2 Guinea pig 6.4 pKd = 6.4 Binding
Inhibition of beta2-adrenergic receptor in guinea pig tracheal chain assessed as reversal of isoproterenol-induced effect after 15 minsInhibition of beta2-adrenergic receptor in guinea pig tracheal chain assessed as reversal of isoproterenol-induced effect after 15 mins
ChEMBL 245 2 2 2 2.8 CC1(C)NC1C(O)c1ccc(Cl)c(Cl)c1 10.1021/jm00199a012
CHEMBL3251299 110032 0 None 43 2 Guinea pig 6.4 pKd = 6.4 Binding
Inhibition of beta2-adrenergic receptor in guinea pig tracheal chain assessed as reversal of isoproterenol-induced effect after 15 minsInhibition of beta2-adrenergic receptor in guinea pig tracheal chain assessed as reversal of isoproterenol-induced effect after 15 mins
ChEMBL 245 2 2 2 2.8 CC1(C)NC1C(O)c1ccc(Cl)c(Cl)c1 10.1021/jm00199a012
12462222 112131 0 None -39 2 Guinea pig 6.4 pKd = 6.4 Binding
Antagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 minsAntagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 mins
ChEMBL 223 5 2 3 2.0 COc1cc(C)ccc1C(O)CNC(C)C 10.1021/jm00208a015
CHEMBL3246232 112131 0 None -39 2 Guinea pig 6.4 pKd = 6.4 Binding
Antagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 minsAntagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 mins
ChEMBL 223 5 2 3 2.0 COc1cc(C)ccc1C(O)CNC(C)C 10.1021/jm00208a015
CHEMBL3302868 112131 0 None -39 2 Guinea pig 6.4 pKd = 6.4 Binding
Antagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 minsAntagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 mins
ChEMBL 223 5 2 3 2.0 COc1cc(C)ccc1C(O)CNC(C)C 10.1021/jm00208a015
2598 3707 52 None 6 5 Bovine 5.4 pKd = 5.4 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 225 3 4 4 1.5 OC(c1cc(O)cc(c1)O)CNC(C)(C)C 10.1021/jm00147a037
5403 3707 52 None 6 5 Bovine 5.4 pKd = 5.4 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 225 3 4 4 1.5 OC(c1cc(O)cc(c1)O)CNC(C)(C)C 10.1021/jm00147a037
560 3707 52 None 6 5 Bovine 5.4 pKd = 5.4 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 225 3 4 4 1.5 OC(c1cc(O)cc(c1)O)CNC(C)(C)C 10.1021/jm00147a037
CHEMBL1760 3707 52 None 6 5 Bovine 5.4 pKd = 5.4 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 225 3 4 4 1.5 OC(c1cc(O)cc(c1)O)CNC(C)(C)C 10.1021/jm00147a037
DB00871 3707 52 None 6 5 Bovine 5.4 pKd = 5.4 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 225 3 4 4 1.5 OC(c1cc(O)cc(c1)O)CNC(C)(C)C 10.1021/jm00147a037
1960 2805 64 None -549 26 Human 5.4 pKd = 5.4 Binding
Binding affinity to human adrenergic beta2 receptorBinding affinity to human adrenergic beta2 receptor
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1016/j.ejmech.2008.12.016
439260 2805 64 None -549 26 Human 5.4 pKd = 5.4 Binding
Binding affinity to human adrenergic beta2 receptorBinding affinity to human adrenergic beta2 receptor
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1016/j.ejmech.2008.12.016
505 2805 64 None -549 26 Human 5.4 pKd = 5.4 Binding
Binding affinity to human adrenergic beta2 receptorBinding affinity to human adrenergic beta2 receptor
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1016/j.ejmech.2008.12.016
CHEMBL1437 2805 64 None -549 26 Human 5.4 pKd = 5.4 Binding
Binding affinity to human adrenergic beta2 receptorBinding affinity to human adrenergic beta2 receptor
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1016/j.ejmech.2008.12.016
DB00368 2805 64 None -549 26 Human 5.4 pKd = 5.4 Binding
Binding affinity to human adrenergic beta2 receptorBinding affinity to human adrenergic beta2 receptor
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1016/j.ejmech.2008.12.016
12941056 101733 0 None -10 2 Guinea pig 5.4 pKd = 5.4 Binding
Ability to block Beta-2 adrenergic receptor in guinea pig trachea preparationAbility to block Beta-2 adrenergic receptor in guinea pig trachea preparation
ChEMBL 281 8 2 5 1.1 COC(=O)Cc1ccc(OCC(O)CNC(C)C)cc1 10.1021/jm00354a003
CHEMBL30292 101733 0 None -10 2 Guinea pig 5.4 pKd = 5.4 Binding
Ability to block Beta-2 adrenergic receptor in guinea pig trachea preparationAbility to block Beta-2 adrenergic receptor in guinea pig trachea preparation
ChEMBL 281 8 2 5 1.1 COC(=O)Cc1ccc(OCC(O)CNC(C)C)cc1 10.1021/jm00354a003
559935 103307 7 None -12 2 Guinea pig 5.4 pKd = 5.4 Binding
Ability to block Beta-2 adrenergic receptor in guinea pig trachea preparationAbility to block Beta-2 adrenergic receptor in guinea pig trachea preparation
ChEMBL 281 6 2 5 1.6 COC(=O)c1ccc(OCC(O)CNC(C)(C)C)cc1 10.1021/jm00354a003
CHEMBL30899 103307 7 None -12 2 Guinea pig 5.4 pKd = 5.4 Binding
Ability to block Beta-2 adrenergic receptor in guinea pig trachea preparationAbility to block Beta-2 adrenergic receptor in guinea pig trachea preparation
ChEMBL 281 6 2 5 1.6 COC(=O)c1ccc(OCC(O)CNC(C)(C)C)cc1 10.1021/jm00354a003
1960 2805 64 None -549 26 Human 5.4 pKd = 5.4 Binding
Binding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nMBinding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nM
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1016/j.bmcl.2013.07.052
439260 2805 64 None -549 26 Human 5.4 pKd = 5.4 Binding
Binding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nMBinding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nM
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1016/j.bmcl.2013.07.052
505 2805 64 None -549 26 Human 5.4 pKd = 5.4 Binding
Binding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nMBinding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nM
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1016/j.bmcl.2013.07.052
CHEMBL1437 2805 64 None -549 26 Human 5.4 pKd = 5.4 Binding
Binding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nMBinding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nM
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1016/j.bmcl.2013.07.052
DB00368 2805 64 None -549 26 Human 5.4 pKd = 5.4 Binding
Binding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nMBinding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nM
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1016/j.bmcl.2013.07.052
13621764 161459 0 None -1288 2 Guinea pig 5.4 pKd = 5.4 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 507 14 3 7 4.5 COc1ccc(CCNCC(O)COc2ccc(CCc3nc(-c4cccs4)c[nH]3)cc2)cc1OC 10.1021/jm00156a028
CHEMBL415970 161459 0 None -1288 2 Guinea pig 5.4 pKd = 5.4 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 507 14 3 7 4.5 COc1ccc(CCNCC(O)COc2ccc(CCc3nc(-c4cccs4)c[nH]3)cc2)cc1OC 10.1021/jm00156a028
13621690 9777 0 None -1318 2 Guinea pig 4.4 pKd = 4.4 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 440 12 4 7 1.8 COc1ccc(CCNCC(O)COc2ccc(-c3nc(C(N)=O)c[nH]3)cc2)cc1OC 10.1021/jm00156a028
CHEMBL11427 9777 0 None -1318 2 Guinea pig 4.4 pKd = 4.4 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 440 12 4 7 1.8 COc1ccc(CCNCC(O)COc2ccc(-c3nc(C(N)=O)c[nH]3)cc2)cc1OC 10.1021/jm00156a028
12606686 92413 3 None 31 2 Guinea pig 6.4 pKd = 6.4 Binding
Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.
ChEMBL 189 5 2 3 1.2 CC(C)OCC(O)CNC(C)(C)C 10.1021/jm00376a011
CHEMBL1161385 92413 3 None 31 2 Guinea pig 6.4 pKd = 6.4 Binding
Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.
ChEMBL 189 5 2 3 1.2 CC(C)OCC(O)CNC(C)(C)C 10.1021/jm00376a011
CHEMBL24391 92413 3 None 31 2 Guinea pig 6.4 pKd = 6.4 Binding
Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.
ChEMBL 189 5 2 3 1.2 CC(C)OCC(O)CNC(C)(C)C 10.1021/jm00376a011
23843 8354 19 None - 1 Bovine 5.4 pKd = 5.4 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 195 4 3 3 1.4 CC(C)NCC(O)c1ccc(O)cc1 10.1021/jm00147a037
CHEMBL109378 8354 19 None - 1 Bovine 5.4 pKd = 5.4 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 195 4 3 3 1.4 CC(C)NCC(O)c1ccc(O)cc1 10.1021/jm00147a037
18047 201915 18 None -4 5 Bovine 7.4 pKd = 7.4 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 223 6 2 3 1.7 Cc1cccc(OCC(O)CNC(C)C)c1 10.1021/jm00147a037
CHEMBL67096 201915 18 None -4 5 Bovine 7.4 pKd = 7.4 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 223 6 2 3 1.7 Cc1cccc(OCC(O)CNC(C)C)c1 10.1021/jm00147a037
13621671 168851 1 None -234 2 Guinea pig 5.4 pKd = 5.4 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 496 13 3 8 2.5 COc1ccc(CCNCC(O)COc2ccc(-c3nc(CN4CCOCC4)c[nH]3)cc2)cc1OC 10.1021/jm00156a028
CHEMBL442522 168851 1 None -234 2 Guinea pig 5.4 pKd = 5.4 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 496 13 3 8 2.5 COc1ccc(CCNCC(O)COc2ccc(-c3nc(CN4CCOCC4)c[nH]3)cc2)cc1OC 10.1021/jm00156a028
4606363 112215 3 None - 1 Guinea pig 5.4 pKd = 5.4 Binding
Antagonist activity at beta-2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of isoprenaline-induced effectAntagonist activity at beta-2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of isoprenaline-induced effect
ChEMBL 382 13 4 6 2.3 CC(C)NCC(O)COc1cccc(C(C)C)c1OCC(O)CNC(C)C 10.1021/jm00214a013
CHEMBL3272436 112215 3 None - 1 Guinea pig 5.4 pKd = 5.4 Binding
Antagonist activity at beta-2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of isoprenaline-induced effectAntagonist activity at beta-2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of isoprenaline-induced effect
ChEMBL 382 13 4 6 2.3 CC(C)NCC(O)COc1cccc(C(C)C)c1OCC(O)CNC(C)C 10.1021/jm00214a013
CHEMBL3304621 112215 3 None - 1 Guinea pig 5.4 pKd = 5.4 Binding
Antagonist activity at beta-2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of isoprenaline-induced effectAntagonist activity at beta-2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of isoprenaline-induced effect
ChEMBL 382 13 4 6 2.3 CC(C)NCC(O)COc1cccc(C(C)C)c1OCC(O)CNC(C)C 10.1021/jm00214a013
3486 3096 51 None -30 11 Guinea pig 5.4 pKd = 5.4 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
ChEMBL 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C 10.1021/jm00361a004
4883 3096 51 None -30 11 Guinea pig 5.4 pKd = 5.4 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
ChEMBL 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C 10.1021/jm00361a004
555 3096 51 None -30 11 Guinea pig 5.4 pKd = 5.4 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
ChEMBL 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C 10.1021/jm00361a004
CHEMBL6995 3096 51 None -30 11 Guinea pig 5.4 pKd = 5.4 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
ChEMBL 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C 10.1021/jm00361a004
DB01297 3096 51 None -30 11 Guinea pig 5.4 pKd = 5.4 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
ChEMBL 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C 10.1021/jm00361a004
13157407 59954 0 None -245 2 Guinea pig 4.3 pKd = 4.3 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
ChEMBL 419 10 3 5 4.4 OC(CNCCc1ccccc1)COc1ccc(-c2nc(-c3cccs3)c[nH]2)cc1 10.1021/jm00361a004
CHEMBL174259 59954 0 None -245 2 Guinea pig 4.3 pKd = 4.3 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
ChEMBL 419 10 3 5 4.4 OC(CNCCc1ccccc1)COc1ccc(-c2nc(-c3cccs3)c[nH]2)cc1 10.1021/jm00361a004
54758320 65172 0 None 6 3 Human 7.3 pKd = 7.3 Binding
Displacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cells
ChEMBL 794 20 5 8 6.1 O=C(CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1)NCCNCC(O)COc1cccc2[nH]ccc12 10.1021/jm2008562
CHEMBL1830620 65172 0 None 6 3 Human 7.3 pKd = 7.3 Binding
Displacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cells
ChEMBL 794 20 5 8 6.1 O=C(CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1)NCCNCC(O)COc1cccc2[nH]ccc12 10.1021/jm2008562
44459541 95684 0 None 1 2 Guinea pig 7.3 pKd = 7.3 Binding
Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.
ChEMBL 242 7 2 4 1.9 C/C(CC1CC1)=N/OCC(O)CNC(C)(C)C 10.1021/jm00376a011
CHEMBL26049 95684 0 None 1 2 Guinea pig 7.3 pKd = 7.3 Binding
Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.
ChEMBL 242 7 2 4 1.9 C/C(CC1CC1)=N/OCC(O)CNC(C)(C)C 10.1021/jm00376a011
6917762 9219 7 None 1 2 Guinea pig 7.3 pKd = 7.3 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor determined as pA2 in guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor determined as pA2 in guinea pig trachea
ChEMBL 228 6 2 4 1.5 C/C(=N\OCC(O)CNC(C)(C)C)C1CC1 10.1021/jm00145a008
CHEMBL111103 9219 7 None 1 2 Guinea pig 7.3 pKd = 7.3 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor determined as pA2 in guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor determined as pA2 in guinea pig trachea
ChEMBL 228 6 2 4 1.5 C/C(=N\OCC(O)CNC(C)(C)C)C1CC1 10.1021/jm00145a008
161394 119455 13 None - 1 Bovine 6.3 pKd = 6.3 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 252 4 4 4 0.9 CC(C)(C)NCC(O)c1ccc(O)c(C(N)=O)c1 10.1021/jm00147a037
CHEMBL349845 119455 13 None - 1 Bovine 6.3 pKd = 6.3 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 252 4 4 4 0.9 CC(C)(C)NCC(O)c1ccc(O)c(C(N)=O)c1 10.1021/jm00147a037
135079 10387 1 None -9772 2 Guinea pig 4.3 pKd = 4.3 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
ChEMBL 479 12 3 7 4.4 COc1ccc(CCNCC(O)COc2ccc(-c3nc(-c4cccs4)c[nH]3)cc2)cc1OC 10.1021/jm00361a004
CHEMBL11671 10387 1 None -9772 2 Guinea pig 4.3 pKd = 4.3 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
ChEMBL 479 12 3 7 4.4 COc1ccc(CCNCC(O)COc2ccc(-c3nc(-c4cccs4)c[nH]3)cc2)cc1OC 10.1021/jm00361a004
16735257 85290 0 None 151 2 Human 6.3 pKd = 6.3 Binding
Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.
ChEMBL 317 7 4 5 2.4 COc1ccc(C[C@@H](C)NC[C@H](O)c2cc(O)cc(O)c2)cc1 nan
CHEMBL228992 85290 0 None 151 2 Human 6.3 pKd = 6.3 Binding
Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.
ChEMBL 317 7 4 5 2.4 COc1ccc(C[C@@H](C)NC[C@H](O)c2cc(O)cc(O)c2)cc1 nan
1720 2901 35 None -2 2 Human 5.3 pKd = 5.3 Binding
Binding affinity to human adrenergic beta2 receptorBinding affinity to human adrenergic beta2 receptor
ChEMBL 211 4 4 4 1.1 OC(c1cc(O)cc(c1)O)CNC(C)C 10.1016/j.ejmech.2008.12.016
4086 2901 35 None -2 2 Human 5.3 pKd = 5.3 Binding
Binding affinity to human adrenergic beta2 receptorBinding affinity to human adrenergic beta2 receptor
ChEMBL 211 4 4 4 1.1 OC(c1cc(O)cc(c1)O)CNC(C)C 10.1016/j.ejmech.2008.12.016
7250 2901 35 None -2 2 Human 5.3 pKd = 5.3 Binding
Binding affinity to human adrenergic beta2 receptorBinding affinity to human adrenergic beta2 receptor
ChEMBL 211 4 4 4 1.1 OC(c1cc(O)cc(c1)O)CNC(C)C 10.1016/j.ejmech.2008.12.016
CHEMBL776 2901 35 None -2 2 Human 5.3 pKd = 5.3 Binding
Binding affinity to human adrenergic beta2 receptorBinding affinity to human adrenergic beta2 receptor
ChEMBL 211 4 4 4 1.1 OC(c1cc(O)cc(c1)O)CNC(C)C 10.1016/j.ejmech.2008.12.016
DB00816 2901 35 None -2 2 Human 5.3 pKd = 5.3 Binding
Binding affinity to human adrenergic beta2 receptorBinding affinity to human adrenergic beta2 receptor
ChEMBL 211 4 4 4 1.1 OC(c1cc(O)cc(c1)O)CNC(C)C 10.1016/j.ejmech.2008.12.016
5473526 157786 2 None 2 2 Human 5.3 pKd = 5.3 Binding
Displacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting methodDisplacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting method
ChEMBL 286 2 0 1 4.6 C[n+]1c(/C=C/c2ccccc2Cl)sc2ccccc21 10.1021/acsmedchemlett.6b00363
CHEMBL4089434 157786 2 None 2 2 Human 5.3 pKd = 5.3 Binding
Displacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting methodDisplacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting method
ChEMBL 286 2 0 1 4.6 C[n+]1c(/C=C/c2ccccc2Cl)sc2ccccc21 10.1021/acsmedchemlett.6b00363
118725500 116589 0 None - 1 Guinea pig 8.3 pKd = 8.3 Binding
Agonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring at basal tone assessed as bronchorelaxation activityAgonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring at basal tone assessed as bronchorelaxation activity
ChEMBL 323 5 3 4 1.6 CC(C)C[B-]1(O)OCc2cc([C@@H](O)C[NH2+]C(C)(C)C)ccc2O1 10.1016/j.bmcl.2014.12.077
CHEMBL3393402 116589 0 None - 1 Guinea pig 8.3 pKd = 8.3 Binding
Agonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring at basal tone assessed as bronchorelaxation activityAgonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring at basal tone assessed as bronchorelaxation activity
ChEMBL 323 5 3 4 1.6 CC(C)C[B-]1(O)OCc2cc([C@@H](O)C[NH2+]C(C)(C)C)ccc2O1 10.1016/j.bmcl.2014.12.077
54757027 65145 0 None 24 3 Human 8.2 pKd = 8.2 Binding
Displacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cells
ChEMBL 889 26 4 8 9.1 O=C(CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1)NCCCCCCCCNCC(O)COc1cccc2ccccc12 10.1021/jm2008562
CHEMBL1830490 65145 0 None 24 3 Human 8.2 pKd = 8.2 Binding
Displacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cells
ChEMBL 889 26 4 8 9.1 O=C(CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1)NCCCCCCCCNCC(O)COc1cccc2ccccc12 10.1021/jm2008562
1499 2052 43 None -33 17 Human 7.3 pKd = 7.3 Binding
Binding affinity to human adrenergic beta2 receptorBinding affinity to human adrenergic beta2 receptor
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.ejmech.2008.12.016
3779 2052 43 None -33 17 Human 7.3 pKd = 7.3 Binding
Binding affinity to human adrenergic beta2 receptorBinding affinity to human adrenergic beta2 receptor
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.ejmech.2008.12.016
536 2052 43 None -33 17 Human 7.3 pKd = 7.3 Binding
Binding affinity to human adrenergic beta2 receptorBinding affinity to human adrenergic beta2 receptor
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.ejmech.2008.12.016
CHEMBL434 2052 43 None -33 17 Human 7.3 pKd = 7.3 Binding
Binding affinity to human adrenergic beta2 receptorBinding affinity to human adrenergic beta2 receptor
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.ejmech.2008.12.016
DB01064 2052 43 None -33 17 Human 7.3 pKd = 7.3 Binding
Binding affinity to human adrenergic beta2 receptorBinding affinity to human adrenergic beta2 receptor
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.ejmech.2008.12.016
10060160 10094 3 None - 1 Bovine 7.3 pKd = 7.3 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 239 7 3 4 0.9 CC(C)NCC(O)COc1ccccc1CO 10.1021/jm00147a037
CHEMBL1159891 10094 3 None - 1 Bovine 7.3 pKd = 7.3 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 239 7 3 4 0.9 CC(C)NCC(O)COc1ccccc1CO 10.1021/jm00147a037
15578563 99598 0 None -1 2 Guinea pig 7.3 pKd = 7.3 Binding
In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.
ChEMBL 317 9 2 5 2.1 CCOC(=O)CCNCC(O)COc1cccc2ccccc12 10.1021/jm00354a002
CHEMBL287242 99598 0 None -1 2 Guinea pig 7.3 pKd = 7.3 Binding
In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.
ChEMBL 317 9 2 5 2.1 CCOC(=O)CCNCC(O)COc1cccc2ccccc12 10.1021/jm00354a002
1720 2901 35 None -2 2 Human 6.3 pKd = 6.3 Binding
Binding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nMBinding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nM
ChEMBL 211 4 4 4 1.1 OC(c1cc(O)cc(c1)O)CNC(C)C 10.1016/j.bmcl.2013.07.052
4086 2901 35 None -2 2 Human 6.3 pKd = 6.3 Binding
Binding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nMBinding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nM
ChEMBL 211 4 4 4 1.1 OC(c1cc(O)cc(c1)O)CNC(C)C 10.1016/j.bmcl.2013.07.052
7250 2901 35 None -2 2 Human 6.3 pKd = 6.3 Binding
Binding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nMBinding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nM
ChEMBL 211 4 4 4 1.1 OC(c1cc(O)cc(c1)O)CNC(C)C 10.1016/j.bmcl.2013.07.052
CHEMBL776 2901 35 None -2 2 Human 6.3 pKd = 6.3 Binding
Binding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nMBinding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nM
ChEMBL 211 4 4 4 1.1 OC(c1cc(O)cc(c1)O)CNC(C)C 10.1016/j.bmcl.2013.07.052
DB00816 2901 35 None -2 2 Human 6.3 pKd = 6.3 Binding
Binding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nMBinding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nM
ChEMBL 211 4 4 4 1.1 OC(c1cc(O)cc(c1)O)CNC(C)C 10.1016/j.bmcl.2013.07.052
159899 107056 28 None -1 2 Guinea pig 6.3 pKd = 6.3 Binding
In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.
ChEMBL 217 4 2 3 1.5 NCC(O)COc1cccc2ccccc12 10.1021/jm00354a002
CHEMBL31888 107056 28 None -1 2 Guinea pig 6.3 pKd = 6.3 Binding
In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.
ChEMBL 217 4 2 3 1.5 NCC(O)COc1cccc2ccccc12 10.1021/jm00354a002
44459632 95993 0 None 2 2 Guinea pig 5.3 pKd = 5.3 Binding
Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.
ChEMBL 230 7 3 4 1.1 CC(NOCC(O)CNC(C)(C)C)C1CC1 10.1021/jm00376a011
CHEMBL26224 95993 0 None 2 2 Guinea pig 5.3 pKd = 5.3 Binding
Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.
ChEMBL 230 7 3 4 1.1 CC(NOCC(O)CNC(C)(C)C)C1CC1 10.1021/jm00376a011
9816183 100068 5 None 5 2 Human 7.3 pKd = 7.3 Binding
Compound was tested for its binding affinity to human Beta-2 adrenergic receptor by using the radioligand [3H]CGP-12177Compound was tested for its binding affinity to human Beta-2 adrenergic receptor by using the radioligand [3H]CGP-12177
ChEMBL 240 3 4 6 1.0 CNCC(O)c1ccc(O)c2nc(O)sc12 10.1016/s0960-894x(99)00205-x
CHEMBL29141 100068 5 None 5 2 Human 7.3 pKd = 7.3 Binding
Compound was tested for its binding affinity to human Beta-2 adrenergic receptor by using the radioligand [3H]CGP-12177Compound was tested for its binding affinity to human Beta-2 adrenergic receptor by using the radioligand [3H]CGP-12177
ChEMBL 240 3 4 6 1.0 CNCC(O)c1ccc(O)c2nc(O)sc12 10.1016/s0960-894x(99)00205-x
5311116 2293 6 None -1258 3 Human 5.3 pKd = 5.3 Binding
Displacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 484 15 5 8 2.2 N#Cc1cc(OCCOCC2CC2)ccc1OCC(CNCCNC(=O)Nc1ccc(cc1)O)O 10.1021/jm400348g
544 2293 6 None -1258 3 Human 5.3 pKd = 5.3 Binding
Displacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 484 15 5 8 2.2 N#Cc1cc(OCCOCC2CC2)ccc1OCC(CNCCNC(=O)Nc1ccc(cc1)O)O 10.1021/jm400348g
CHEMBL207802 2293 6 None -1258 3 Human 5.3 pKd = 5.3 Binding
Displacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 484 15 5 8 2.2 N#Cc1cc(OCCOCC2CC2)ccc1OCC(CNCCNC(=O)Nc1ccc(cc1)O)O 10.1021/jm400348g
10353067 10084 2 None - 1 Bovine 5.3 pKd = 5.3 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 210 4 4 4 1.0 CC(C)NCC(O)c1ccc(O)c(N)c1 10.1021/jm00147a037
CHEMBL1159719 10084 2 None - 1 Bovine 5.3 pKd = 5.3 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 210 4 4 4 1.0 CC(C)NCC(O)c1ccc(O)c(N)c1 10.1021/jm00147a037
105 3392 84 None -1 6 Bovine 6.3 pKd = 6.3 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1021/jm00147a037
2083 3392 84 None -1 6 Bovine 6.3 pKd = 6.3 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1021/jm00147a037
558 3392 84 None -1 6 Bovine 6.3 pKd = 6.3 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1021/jm00147a037
CHEMBL714 3392 84 None -1 6 Bovine 6.3 pKd = 6.3 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1021/jm00147a037
DB01001 3392 84 None -1 6 Bovine 6.3 pKd = 6.3 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1021/jm00147a037
10105627 10079 0 None - 1 Bovine 6.3 pKd = 6.3 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 238 4 4 4 1.9 CNc1cc(C(O)CNC(C)(C)C)ccc1O 10.1021/jm00147a037
CHEMBL1159712 10079 0 None - 1 Bovine 6.3 pKd = 6.3 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 238 4 4 4 1.9 CNc1cc(C(O)CNC(C)(C)C)ccc1O 10.1021/jm00147a037
123133222 159488 0 None 6 2 Human 5.3 pKd = 5.3 Binding
Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.
ChEMBL 317 7 4 5 2.4 COc1cccc(C[C@@H](C)NC[C@@H](O)c2cc(O)cc(O)c2)c1 nan
CHEMBL4108239 159488 0 None 6 2 Human 5.3 pKd = 5.3 Binding
Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.
ChEMBL 317 7 4 5 2.4 COc1cccc(C[C@@H](C)NC[C@@H](O)c2cc(O)cc(O)c2)c1 nan
13621631 9584 0 None -169 2 Guinea pig 5.3 pKd = 5.3 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 489 11 3 6 3.7 COc1ccc(CCNCC(O)COc2ccc(-c3nc(Br)c(C)[nH]3)cc2)cc1OC 10.1021/jm00156a028
CHEMBL11307 9584 0 None -169 2 Guinea pig 5.3 pKd = 5.3 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 489 11 3 6 3.7 COc1ccc(CCNCC(O)COc2ccc(-c3nc(Br)c(C)[nH]3)cc2)cc1OC 10.1021/jm00156a028
13621638 9756 0 None -2137 2 Guinea pig 4.3 pKd = 4.3 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 455 13 3 7 3.1 COCc1[nH]c(-c2ccc(OCC(O)CNCCc3ccc(OC)c(OC)c3)cc2)nc1C 10.1021/jm00156a028
CHEMBL11414 9756 0 None -2137 2 Guinea pig 4.3 pKd = 4.3 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 455 13 3 7 3.1 COCc1[nH]c(-c2ccc(OCC(O)CNCCc3ccc(OC)c(OC)c3)cc2)nc1C 10.1021/jm00156a028
71662246 87820 0 None -11 2 Human 6.3 pKd = 6.3 Binding
Displacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 471 14 4 6 3.5 Cc1ccccc1NC(=O)NCCNCC(O)COc1ccc(OCCOC2CCCC2)cc1 10.1021/jm400348g
CHEMBL2348212 87820 0 None -11 2 Human 6.3 pKd = 6.3 Binding
Displacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 471 14 4 6 3.5 Cc1ccccc1NC(=O)NCCNCC(O)COc1ccc(OCCOC2CCCC2)cc1 10.1021/jm400348g
3123920 2774 79 None -31622 6 Bovine 4.3 pKd = 4.3 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 209 6 2 3 1.4 OC(COc1ccccc1)CNC(C)C 10.1021/jm00147a037
546 2774 79 None -31622 6 Bovine 4.3 pKd = 4.3 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 209 6 2 3 1.4 OC(COc1ccccc1)CNC(C)C 10.1021/jm00147a037
CHEMBL7154 2774 79 None -31622 6 Bovine 4.3 pKd = 4.3 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 209 6 2 3 1.4 OC(COc1ccccc1)CNC(C)C 10.1021/jm00147a037
13302060 12711 0 None -112 2 Guinea pig 4.3 pKd = 4.3 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 411 11 2 7 2.7 COc1ccc(CCNCC(O)COc2ccc(-c3nccn3C)cc2)cc1OC 10.1021/jm00156a028
CHEMBL1188509 12711 0 None -112 2 Guinea pig 4.3 pKd = 4.3 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 411 11 2 7 2.7 COc1ccc(CCNCC(O)COc2ccc(-c3nccn3C)cc2)cc1OC 10.1021/jm00156a028
CHEMBL536552 12711 0 None -112 2 Guinea pig 4.3 pKd = 4.3 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 411 11 2 7 2.7 COc1ccc(CCNCC(O)COc2ccc(-c3nccn3C)cc2)cc1OC 10.1021/jm00156a028
29072430 158911 12 None 6 2 Human 5.3 pKd = 5.3 Binding
Displacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting methodDisplacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting method
ChEMBL 365 4 1 5 3.9 COc1cccc(/C=C2\Oc3c(CN4CCCC4)c(O)cc(C)c3C2=O)c1 10.1021/acsmedchemlett.6b00363
8071397 158911 12 None 6 2 Human 5.3 pKd = 5.3 Binding
Displacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting methodDisplacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting method
ChEMBL 365 4 1 5 3.9 COc1cccc(/C=C2\Oc3c(CN4CCCC4)c(O)cc(C)c3C2=O)c1 10.1021/acsmedchemlett.6b00363
CHEMBL4101524 158911 12 None 6 2 Human 5.3 pKd = 5.3 Binding
Displacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting methodDisplacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting method
ChEMBL 365 4 1 5 3.9 COc1cccc(/C=C2\Oc3c(CN4CCCC4)c(O)cc(C)c3C2=O)c1 10.1021/acsmedchemlett.6b00363
13621722 96859 5 None -229 2 Guinea pig 5.3 pKd = 5.3 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 275 7 3 4 1.8 CC(C)NCC(O)COc1ccc(-c2ncc[nH]2)cc1 10.1021/jm00156a028
CHEMBL269219 96859 5 None -229 2 Guinea pig 5.3 pKd = 5.3 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 275 7 3 4 1.8 CC(C)NCC(O)COc1ccc(-c2ncc[nH]2)cc1 10.1021/jm00156a028
12521605 165775 0 None -9 2 Guinea pig 6.3 pKd = 6.3 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
ChEMBL 303 6 3 4 2.5 Cc1c[nH]c(-c2ccc(OCC(O)CNC(C)(C)C)cc2)n1 10.1021/jm00361a004
CHEMBL427297 165775 0 None -9 2 Guinea pig 6.3 pKd = 6.3 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
ChEMBL 303 6 3 4 2.5 Cc1c[nH]c(-c2ccc(OCC(O)CNC(C)(C)C)cc2)n1 10.1021/jm00361a004
13621715 5050 0 None -436 2 Guinea pig 5.3 pKd = 5.3 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 387 11 3 6 3.2 CCOCCNCC(O)COc1ccc(-c2nc(-c3cccs3)c[nH]2)cc1 10.1021/jm00156a028
CHEMBL10574 5050 0 None -436 2 Guinea pig 5.3 pKd = 5.3 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 387 11 3 6 3.2 CCOCCNCC(O)COc1ccc(-c2nc(-c3cccs3)c[nH]2)cc1 10.1021/jm00156a028
16735276 145437 0 None -1 2 Human 4.3 pKd = 4.3 Binding
Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.
ChEMBL 267 8 4 4 2.7 CCCCC[C@H](C)NC[C@@H](O)c1cc(O)cc(O)c1 nan
CHEMBL3918348 145437 0 None -1 2 Human 4.3 pKd = 4.3 Binding
Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.
ChEMBL 267 8 4 4 2.7 CCCCC[C@H](C)NC[C@@H](O)c1cc(O)cc(O)c1 nan
13157364 77598 0 None -30 2 Guinea pig 7.2 pKd = 7.2 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
ChEMBL 341 7 3 4 2.6 O[C@@H](CNC1CC1)COc1ccc(-c2nc(C(F)(F)F)c[nH]2)cc1 10.1021/jm00361a004
CHEMBL2096752 77598 0 None -30 2 Guinea pig 7.2 pKd = 7.2 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
ChEMBL 341 7 3 4 2.6 O[C@@H](CNC1CC1)COc1ccc(-c2nc(C(F)(F)F)c[nH]2)cc1 10.1021/jm00361a004
217246 10080 38 None - 1 Bovine 7.2 pKd = 7.2 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 262 4 3 3 2.6 CC(C)NCC(O)c1cc(Cl)c(N)c(Cl)c1 10.1021/jm00147a037
CHEMBL1159713 10080 38 None - 1 Bovine 7.2 pKd = 7.2 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 262 4 3 3 2.6 CC(C)NCC(O)c1cc(Cl)c(N)c(Cl)c1 10.1021/jm00147a037
2464 3570 52 None 2 6 Bovine 6.2 pKd = 6.2 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C 10.1021/jm00147a037
5253 3570 52 None 2 6 Bovine 6.2 pKd = 6.2 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C 10.1021/jm00147a037
7297 3570 52 None 2 6 Bovine 6.2 pKd = 6.2 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C 10.1021/jm00147a037
CHEMBL471 3570 52 None 2 6 Bovine 6.2 pKd = 6.2 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C 10.1021/jm00147a037
DB00489 3570 52 None 2 6 Bovine 6.2 pKd = 6.2 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C 10.1021/jm00147a037
44274623 96355 3 None -7 2 Guinea pig 6.2 pKd = 6.2 Binding
Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.
ChEMBL 201 6 2 3 1.2 CC(C)(C)NCC(O)COCC1CC1 10.1021/jm00376a011
CHEMBL26507 96355 3 None -7 2 Guinea pig 6.2 pKd = 6.2 Binding
Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.
ChEMBL 201 6 2 3 1.2 CC(C)(C)NCC(O)COCC1CC1 10.1021/jm00376a011
13621626 9427 0 None -741 2 Guinea pig 5.2 pKd = 5.2 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 445 11 3 6 3.6 COc1ccc(CCNCC(O)COc2ccc(-c3nc(C)c(Cl)[nH]3)cc2)cc1OC 10.1021/jm00156a028
CHEMBL11224 9427 0 None -741 2 Guinea pig 5.2 pKd = 5.2 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 445 11 3 6 3.6 COc1ccc(CCNCC(O)COc2ccc(-c3nc(C)c(Cl)[nH]3)cc2)cc1OC 10.1021/jm00156a028
44279657 103884 1 None -2 2 Guinea pig 8.2 pKd = 8.2 Binding
In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.
ChEMBL 237 7 2 3 2.0 Cc1ccccc1OCC(O)CNCC(C)C 10.1021/jm00354a002
CHEMBL31021 103884 1 None -2 2 Guinea pig 8.2 pKd = 8.2 Binding
In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.
ChEMBL 237 7 2 3 2.0 Cc1ccccc1OCC(O)CNCC(C)C 10.1021/jm00354a002
6917762 9219 7 None 1 2 Guinea pig 8.2 pKd = 8.2 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor determined as pA2 in guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor determined as pA2 in guinea pig trachea
ChEMBL 228 6 2 4 1.5 C/C(=N\OCC(O)CNC(C)(C)C)C1CC1 10.1021/jm00145a008
CHEMBL111103 9219 7 None 1 2 Guinea pig 8.2 pKd = 8.2 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor determined as pA2 in guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor determined as pA2 in guinea pig trachea
ChEMBL 228 6 2 4 1.5 C/C(=N\OCC(O)CNC(C)(C)C)C1CC1 10.1021/jm00145a008
25104 10082 19 None -467 2 Bovine 6.2 pKd = 6.2 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 225 3 4 4 1.5 CC(C)(C)NCC(O)c1ccc(O)c(O)c1 10.1021/jm00147a037
CHEMBL1159715 10082 19 None -467 2 Bovine 6.2 pKd = 6.2 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 225 3 4 4 1.5 CC(C)(C)NCC(O)c1ccc(O)c(O)c1 10.1021/jm00147a037
21490498 112269 0 None - 1 Guinea pig 6.2 pKd = 6.2 Binding
Antagonist activity at beta-2 adrenergic receptor in guinea pig right atrium assessed as inhibition of isoprenaline-induced effectAntagonist activity at beta-2 adrenergic receptor in guinea pig right atrium assessed as inhibition of isoprenaline-induced effect
ChEMBL 354 12 4 6 1.5 Cc1ccc(OCC(O)CNC(C)C)c(OCC(O)CNC(C)C)c1 10.1021/jm00214a013
CHEMBL3272437 112269 0 None - 1 Guinea pig 6.2 pKd = 6.2 Binding
Antagonist activity at beta-2 adrenergic receptor in guinea pig right atrium assessed as inhibition of isoprenaline-induced effectAntagonist activity at beta-2 adrenergic receptor in guinea pig right atrium assessed as inhibition of isoprenaline-induced effect
ChEMBL 354 12 4 6 1.5 Cc1ccc(OCC(O)CNC(C)C)c(OCC(O)CNC(C)C)c1 10.1021/jm00214a013
CHEMBL3305647 112269 0 None - 1 Guinea pig 6.2 pKd = 6.2 Binding
Antagonist activity at beta-2 adrenergic receptor in guinea pig right atrium assessed as inhibition of isoprenaline-induced effectAntagonist activity at beta-2 adrenergic receptor in guinea pig right atrium assessed as inhibition of isoprenaline-induced effect
ChEMBL 354 12 4 6 1.5 Cc1ccc(OCC(O)CNC(C)C)c(OCC(O)CNC(C)C)c1 10.1021/jm00214a013
123133225 144264 0 None 5 2 Human 5.2 pKd = 5.2 Binding
Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.
ChEMBL 302 6 5 5 1.9 C[C@@H](Cc1cccc(N)c1)NC[C@H](O)c1cc(O)cc(O)c1 nan
CHEMBL3909417 144264 0 None 5 2 Human 5.2 pKd = 5.2 Binding
Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.
ChEMBL 302 6 5 5 1.9 C[C@@H](Cc1cccc(N)c1)NC[C@H](O)c1cc(O)cc(O)c1 nan
328583 110031 1 None 676 2 Guinea pig 7.2 pKd = 7.2 Binding
Inhibition of beta2-adrenergic receptor in guinea pig tracheal chain assessed as reversal of isoproterenol-induced effect after 15 minsInhibition of beta2-adrenergic receptor in guinea pig tracheal chain assessed as reversal of isoproterenol-induced effect after 15 mins
ChEMBL 177 2 2 2 1.5 CC1(C)NC1C(O)c1ccccc1 10.1021/jm00199a012
CHEMBL3251298 110031 1 None 676 2 Guinea pig 7.2 pKd = 7.2 Binding
Inhibition of beta2-adrenergic receptor in guinea pig tracheal chain assessed as reversal of isoproterenol-induced effect after 15 minsInhibition of beta2-adrenergic receptor in guinea pig tracheal chain assessed as reversal of isoproterenol-induced effect after 15 mins
ChEMBL 177 2 2 2 1.5 CC1(C)NC1C(O)c1ccccc1 10.1021/jm00199a012
12521588 60047 0 None -10 2 Guinea pig 6.2 pKd = 6.2 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
ChEMBL 289 6 3 4 2.2 CC(C)(C)NCC(O)COc1ccc(-c2ncc[nH]2)cc1 10.1021/jm00361a004
CHEMBL174783 60047 0 None -10 2 Guinea pig 6.2 pKd = 6.2 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
ChEMBL 289 6 3 4 2.2 CC(C)(C)NCC(O)COc1ccc(-c2ncc[nH]2)cc1 10.1021/jm00361a004
13621665 98032 0 None -1412 2 Guinea pig 4.2 pKd = 4.2 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 455 14 3 7 2.9 COCCc1c[nH]c(-c2ccc(OCC(O)CNCCc3ccc(OC)c(OC)c3)cc2)n1 10.1021/jm00156a028
CHEMBL276029 98032 0 None -1412 2 Guinea pig 4.2 pKd = 4.2 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 455 14 3 7 2.9 COCCc1c[nH]c(-c2ccc(OCC(O)CNCCc3ccc(OC)c(OC)c3)cc2)n1 10.1021/jm00156a028
13040888 106372 0 None 1 2 Guinea pig 7.2 pKd = 7.2 Binding
Ability to block Beta-2 adrenergic receptor in guinea pig trachea preparationAbility to block Beta-2 adrenergic receptor in guinea pig trachea preparation
ChEMBL 279 8 2 5 1.7 C=COC(=O)c1cccc(OCC(O)CNC(C)C)c1 10.1021/jm00354a003
CHEMBL31450 106372 0 None 1 2 Guinea pig 7.2 pKd = 7.2 Binding
Ability to block Beta-2 adrenergic receptor in guinea pig trachea preparationAbility to block Beta-2 adrenergic receptor in guinea pig trachea preparation
ChEMBL 279 8 2 5 1.7 C=COC(=O)c1cccc(OCC(O)CNC(C)C)c1 10.1021/jm00354a003
1028 287 69 None -89 30 Human 6.2 pKd = 6.2 Binding
Binding affinity to human adrenergic beta2 receptorBinding affinity to human adrenergic beta2 receptor
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1016/j.ejmech.2008.12.016
139148732 287 69 None -89 30 Human 6.2 pKd = 6.2 Binding
Binding affinity to human adrenergic beta2 receptorBinding affinity to human adrenergic beta2 receptor
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1016/j.ejmech.2008.12.016
479 287 69 None -89 30 Human 6.2 pKd = 6.2 Binding
Binding affinity to human adrenergic beta2 receptorBinding affinity to human adrenergic beta2 receptor
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1016/j.ejmech.2008.12.016
5816 287 69 None -89 30 Human 6.2 pKd = 6.2 Binding
Binding affinity to human adrenergic beta2 receptorBinding affinity to human adrenergic beta2 receptor
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1016/j.ejmech.2008.12.016
CHEMBL679 287 69 None -89 30 Human 6.2 pKd = 6.2 Binding
Binding affinity to human adrenergic beta2 receptorBinding affinity to human adrenergic beta2 receptor
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1016/j.ejmech.2008.12.016
DB00668 287 69 None -89 30 Human 6.2 pKd = 6.2 Binding
Binding affinity to human adrenergic beta2 receptorBinding affinity to human adrenergic beta2 receptor
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1016/j.ejmech.2008.12.016
5311179 1935 18 None 85 3 Human 6.2 pKd = 6.2 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation counting
ChEMBL 277 6 2 3 2.6 Cc1c2CCCc2c(cc1)OC[C@H]([C@H](C)NC(C)C)O 10.1021/acs.jmedchem.6b00358
543 1935 18 None 85 3 Human 6.2 pKd = 6.2 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation counting
ChEMBL 277 6 2 3 2.6 Cc1c2CCCc2c(cc1)OC[C@H]([C@H](C)NC(C)C)O 10.1021/acs.jmedchem.6b00358
5484725 1935 18 None 85 3 Human 6.2 pKd = 6.2 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation counting
ChEMBL 277 6 2 3 2.6 Cc1c2CCCc2c(cc1)OC[C@H]([C@H](C)NC(C)C)O 10.1021/acs.jmedchem.6b00358
CHEMBL1233766 1935 18 None 85 3 Human 6.2 pKd = 6.2 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation counting
ChEMBL 277 6 2 3 2.6 Cc1c2CCCc2c(cc1)OC[C@H]([C@H](C)NC(C)C)O 10.1021/acs.jmedchem.6b00358
CHEMBL198059 1935 18 None 85 3 Human 6.2 pKd = 6.2 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation counting
ChEMBL 277 6 2 3 2.6 Cc1c2CCCc2c(cc1)OC[C@H]([C@H](C)NC(C)C)O 10.1021/acs.jmedchem.6b00358
1028 287 69 None -89 30 Human 6.2 pKd = 6.2 Binding
Binding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nMBinding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nM
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1016/j.bmcl.2013.07.052
139148732 287 69 None -89 30 Human 6.2 pKd = 6.2 Binding
Binding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nMBinding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nM
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1016/j.bmcl.2013.07.052
479 287 69 None -89 30 Human 6.2 pKd = 6.2 Binding
Binding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nMBinding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nM
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1016/j.bmcl.2013.07.052
5816 287 69 None -89 30 Human 6.2 pKd = 6.2 Binding
Binding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nMBinding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nM
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1016/j.bmcl.2013.07.052
CHEMBL679 287 69 None -89 30 Human 6.2 pKd = 6.2 Binding
Binding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nMBinding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nM
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1016/j.bmcl.2013.07.052
DB00668 287 69 None -89 30 Human 6.2 pKd = 6.2 Binding
Binding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nMBinding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nM
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1016/j.bmcl.2013.07.052
15578602 98899 2 None 1 2 Guinea pig 6.2 pKd = 6.2 Binding
In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.
ChEMBL 267 8 2 5 0.9 CCOC(=O)CNCC(O)COc1ccccc1C 10.1021/jm00354a002
CHEMBL282537 98899 2 None 1 2 Guinea pig 6.2 pKd = 6.2 Binding
In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.
ChEMBL 267 8 2 5 0.9 CCOC(=O)CNCC(O)COc1ccccc1C 10.1021/jm00354a002
15578561 104367 0 None 1 2 Guinea pig 6.2 pKd = 6.2 Binding
In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.
ChEMBL 274 7 3 4 0.7 NC(=O)CNCC(O)COc1cccc2ccccc12 10.1021/jm00354a002
CHEMBL31099 104367 0 None 1 2 Guinea pig 6.2 pKd = 6.2 Binding
In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.
ChEMBL 274 7 3 4 0.7 NC(=O)CNCC(O)COc1cccc2ccccc12 10.1021/jm00354a002
15578559 106635 0 None 1 2 Guinea pig 6.2 pKd = 6.2 Binding
In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.
ChEMBL 303 8 2 5 1.7 CCOC(=O)CNCC(O)COc1cccc2ccccc12 10.1021/jm00354a002
CHEMBL31611 106635 0 None 1 2 Guinea pig 6.2 pKd = 6.2 Binding
In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.
ChEMBL 303 8 2 5 1.7 CCOC(=O)CNCC(O)COc1cccc2ccccc12 10.1021/jm00354a002
1054 1549 49 None -6 3 Guinea pig 5.2 pKd = 5.2 Binding
Ability to block Beta-2 adrenergic receptor in guinea pig trachea preparationAbility to block Beta-2 adrenergic receptor in guinea pig trachea preparation
ChEMBL 295 9 2 5 1.5 COC(=O)CCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm00354a003
59768 1549 49 None -6 3 Guinea pig 5.2 pKd = 5.2 Binding
Ability to block Beta-2 adrenergic receptor in guinea pig trachea preparationAbility to block Beta-2 adrenergic receptor in guinea pig trachea preparation
ChEMBL 295 9 2 5 1.5 COC(=O)CCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm00354a003
7178 1549 49 None -6 3 Guinea pig 5.2 pKd = 5.2 Binding
Ability to block Beta-2 adrenergic receptor in guinea pig trachea preparationAbility to block Beta-2 adrenergic receptor in guinea pig trachea preparation
ChEMBL 295 9 2 5 1.5 COC(=O)CCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm00354a003
CHEMBL768 1549 49 None -6 3 Guinea pig 5.2 pKd = 5.2 Binding
Ability to block Beta-2 adrenergic receptor in guinea pig trachea preparationAbility to block Beta-2 adrenergic receptor in guinea pig trachea preparation
ChEMBL 295 9 2 5 1.5 COC(=O)CCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm00354a003
DB00187 1549 49 None -6 3 Guinea pig 5.2 pKd = 5.2 Binding
Ability to block Beta-2 adrenergic receptor in guinea pig trachea preparationAbility to block Beta-2 adrenergic receptor in guinea pig trachea preparation
ChEMBL 295 9 2 5 1.5 COC(=O)CCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm00354a003
157736 98496 8 None -31 2 Guinea pig 5.2 pKd = 5.2 Binding
Ability to block Beta-2 adrenergic receptor in guinea pig trachea preparationAbility to block Beta-2 adrenergic receptor in guinea pig trachea preparation
ChEMBL 309 10 2 5 1.9 CCOC(=O)CCc1ccc(OCC(O)CNC(C)C)cc1 10.1021/jm00354a003
CHEMBL279777 98496 8 None -31 2 Guinea pig 5.2 pKd = 5.2 Binding
Ability to block Beta-2 adrenergic receptor in guinea pig trachea preparationAbility to block Beta-2 adrenergic receptor in guinea pig trachea preparation
ChEMBL 309 10 2 5 1.9 CCOC(=O)CCc1ccc(OCC(O)CNC(C)C)cc1 10.1021/jm00354a003
13040902 104395 0 None -1 2 Guinea pig 5.2 pKd = 5.2 Binding
Ability to block Beta-2 adrenergic receptor in guinea pig trachea preparationAbility to block Beta-2 adrenergic receptor in guinea pig trachea preparation
ChEMBL 323 11 2 5 2.3 CCCOC(=O)CCc1ccc(OCC(O)CNC(C)C)cc1 10.1021/jm00354a003
CHEMBL31117 104395 0 None -1 2 Guinea pig 5.2 pKd = 5.2 Binding
Ability to block Beta-2 adrenergic receptor in guinea pig trachea preparationAbility to block Beta-2 adrenergic receptor in guinea pig trachea preparation
ChEMBL 323 11 2 5 2.3 CCCOC(=O)CCc1ccc(OCC(O)CNC(C)C)cc1 10.1021/jm00354a003
13040909 106675 0 None -19 2 Guinea pig 5.2 pKd = 5.2 Binding
Ability to block Beta-2 adrenergic receptor in guinea pig trachea preparationAbility to block Beta-2 adrenergic receptor in guinea pig trachea preparation
ChEMBL 417 13 2 7 2.4 COC(=O)CCc1ccc(OCC(O)CNCCc2ccc(OC)c(OC)c2)cc1 10.1021/jm00354a003
CHEMBL31638 106675 0 None -19 2 Guinea pig 5.2 pKd = 5.2 Binding
Ability to block Beta-2 adrenergic receptor in guinea pig trachea preparationAbility to block Beta-2 adrenergic receptor in guinea pig trachea preparation
ChEMBL 417 13 2 7 2.4 COC(=O)CCc1ccc(OCC(O)CNCCc2ccc(OC)c(OC)c2)cc1 10.1021/jm00354a003
3486 3096 51 None -30 11 Guinea pig 5.2 pKd = 5.2 Binding
Antagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 minsAntagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 mins
ChEMBL 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C 10.1021/jm00208a015
4883 3096 51 None -30 11 Guinea pig 5.2 pKd = 5.2 Binding
Antagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 minsAntagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 mins
ChEMBL 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C 10.1021/jm00208a015
555 3096 51 None -30 11 Guinea pig 5.2 pKd = 5.2 Binding
Antagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 minsAntagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 mins
ChEMBL 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C 10.1021/jm00208a015
CHEMBL6995 3096 51 None -30 11 Guinea pig 5.2 pKd = 5.2 Binding
Antagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 minsAntagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 mins
ChEMBL 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C 10.1021/jm00208a015
DB01297 3096 51 None -30 11 Guinea pig 5.2 pKd = 5.2 Binding
Antagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 minsAntagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 mins
ChEMBL 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C 10.1021/jm00208a015
13621700 201340 0 None -3630 2 Guinea pig 4.2 pKd = 4.2 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 439 12 3 7 2.9 COc1ccc(CCNC[C@H](O)COc2ccc(-c3nc(C(C)=O)c[nH]3)cc2)cc1OC 10.1021/jm00156a028
CHEMBL63421 201340 0 None -3630 2 Guinea pig 4.2 pKd = 4.2 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 439 12 3 7 2.9 COc1ccc(CCNC[C@H](O)COc2ccc(-c3nc(C(C)=O)c[nH]3)cc2)cc1OC 10.1021/jm00156a028
328583 110031 1 None 676 2 Guinea pig 7.2 pKd = 7.2 Binding
Inhibition of beta2-adrenergic receptor in guinea pig tracheal chain assessed as reversal of isoproterenol-induced effect after 15 minsInhibition of beta2-adrenergic receptor in guinea pig tracheal chain assessed as reversal of isoproterenol-induced effect after 15 mins
ChEMBL 177 2 2 2 1.5 CC1(C)NC1C(O)c1ccccc1 10.1021/jm00199a012
CHEMBL3251298 110031 1 None 676 2 Guinea pig 7.2 pKd = 7.2 Binding
Inhibition of beta2-adrenergic receptor in guinea pig tracheal chain assessed as reversal of isoproterenol-induced effect after 15 minsInhibition of beta2-adrenergic receptor in guinea pig tracheal chain assessed as reversal of isoproterenol-induced effect after 15 mins
ChEMBL 177 2 2 2 1.5 CC1(C)NC1C(O)c1ccccc1 10.1021/jm00199a012
13157386 62832 1 None -138 2 Guinea pig 7.2 pKd = 7.2 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 479 12 3 7 4.4 COc1ccc(CCNC[C@H](O)COc2ccc(-c3nc(-c4cccs4)c[nH]3)cc2)cc1OC 10.1021/jm00156a028
CHEMBL1788320 62832 1 None -138 2 Guinea pig 7.2 pKd = 7.2 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 479 12 3 7 4.4 COc1ccc(CCNC[C@H](O)COc2ccc(-c3nc(-c4cccs4)c[nH]3)cc2)cc1OC 10.1021/jm00156a028
CHEMBL1789879 62832 1 None -138 2 Guinea pig 7.2 pKd = 7.2 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 479 12 3 7 4.4 COc1ccc(CCNC[C@H](O)COc2ccc(-c3nc(-c4cccs4)c[nH]3)cc2)cc1OC 10.1021/jm00156a028
44383643 165071 1 None 15 2 Guinea pig 5.2 pKd = 5.2 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor determined as pA2 in guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor determined as pA2 in guinea pig trachea
ChEMBL 238 7 1 3 3.0 CC(C)(C)NCCCON=C(C1CC1)C1CC1 10.1021/jm00145a008
CHEMBL424369 165071 1 None 15 2 Guinea pig 5.2 pKd = 5.2 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor determined as pA2 in guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor determined as pA2 in guinea pig trachea
ChEMBL 238 7 1 3 3.0 CC(C)(C)NCCCON=C(C1CC1)C1CC1 10.1021/jm00145a008
13621720 97837 0 None -407 2 Guinea pig 5.2 pKd = 5.2 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 357 9 3 5 3.5 CCCNCC(O)COc1ccc(-c2nc(-c3cccs3)c[nH]2)cc1 10.1021/jm00156a028
CHEMBL274830 97837 0 None -407 2 Guinea pig 5.2 pKd = 5.2 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 357 9 3 5 3.5 CCCNCC(O)COc1ccc(-c2nc(-c3cccs3)c[nH]2)cc1 10.1021/jm00156a028
681 1432 65 None -707 39 Human 4.2 pKd = 4.2 Binding
Binding affinity to human adrenergic beta2 receptorBinding affinity to human adrenergic beta2 receptor
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.ejmech.2008.12.016
940 1432 65 None -707 39 Human 4.2 pKd = 4.2 Binding
Binding affinity to human adrenergic beta2 receptorBinding affinity to human adrenergic beta2 receptor
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.ejmech.2008.12.016
947 1432 65 None -707 39 Human 4.2 pKd = 4.2 Binding
Binding affinity to human adrenergic beta2 receptorBinding affinity to human adrenergic beta2 receptor
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.ejmech.2008.12.016
CHEMBL59 1432 65 None -707 39 Human 4.2 pKd = 4.2 Binding
Binding affinity to human adrenergic beta2 receptorBinding affinity to human adrenergic beta2 receptor
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.ejmech.2008.12.016
DB00988 1432 65 None -707 39 Human 4.2 pKd = 4.2 Binding
Binding affinity to human adrenergic beta2 receptorBinding affinity to human adrenergic beta2 receptor
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.ejmech.2008.12.016
72705086 92564 0 None - 1 Human 4.2 pKd = 4.2 Binding
Binding affinity to N-terminal FLAG-tagged C-terminal His-10-tagged human beta2 adrenoceptor expressed in insect Sf9 cells by surface plasmon resonance analysis in presence of maltose neopentyl glycolBinding affinity to N-terminal FLAG-tagged C-terminal His-10-tagged human beta2 adrenoceptor expressed in insect Sf9 cells by surface plasmon resonance analysis in presence of maltose neopentyl glycol
ChEMBL 330 1 0 2 4.8 Cc1ccc2nc(C(F)(F)F)cc(N3CCC(F)(F)CC3)c2c1 10.1021/ml400312j
CHEMBL2441617 92564 0 None - 1 Human 4.2 pKd = 4.2 Binding
Binding affinity to N-terminal FLAG-tagged C-terminal His-10-tagged human beta2 adrenoceptor expressed in insect Sf9 cells by surface plasmon resonance analysis in presence of maltose neopentyl glycolBinding affinity to N-terminal FLAG-tagged C-terminal His-10-tagged human beta2 adrenoceptor expressed in insect Sf9 cells by surface plasmon resonance analysis in presence of maltose neopentyl glycol
ChEMBL 330 1 0 2 4.8 Cc1ccc2nc(C(F)(F)F)cc(N3CCC(F)(F)CC3)c2c1 10.1021/ml400312j
54756928 65142 0 None 28 3 Human 8.2 pKd = 8.2 Binding
Displacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cells
ChEMBL 889 26 4 8 9.1 O=C(CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1)NCCCCCCCCNC[C@H](O)COc1cccc2ccccc12 10.1021/jm2008562
CHEMBL1830487 65142 0 None 28 3 Human 8.2 pKd = 8.2 Binding
Displacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cells
ChEMBL 889 26 4 8 9.1 O=C(CCCCCNC(=O)COc1ccc(/C=C/c2ccc3n2[B-](F)(F)[N+]2=C(c4cccs4)C=CC2=C3)cc1)NCCCCCCCCNC[C@H](O)COc1cccc2ccccc12 10.1021/jm2008562
15578565 106505 0 None -2 2 Guinea pig 8.1 pKd = 8.1 Binding
In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.
ChEMBL 309 9 2 5 2.1 CCOC(=O)CC(C)(C)NCC(O)COc1ccccc1C 10.1021/jm00354a002
CHEMBL31529 106505 0 None -2 2 Guinea pig 8.1 pKd = 8.1 Binding
In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.In vitro ability to block beta-2 adrenergic receptor in guinea pig trachea.
ChEMBL 309 9 2 5 2.1 CCOC(=O)CC(C)(C)NCC(O)COc1ccccc1C 10.1021/jm00354a002
11823027 192006 33 None -1 3 Human 7.2 pKd = 7.2 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation counting
ChEMBL 309 5 4 5 0.6 CC(C)(C)NCC(O)COc1cccc2c1CC(O)C(O)C2 10.1021/acs.jmedchem.6b00358
4411 192006 33 None -1 3 Human 7.2 pKd = 7.2 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation counting
ChEMBL 309 5 4 5 0.6 CC(C)(C)NCC(O)COc1cccc2c1CC(O)C(O)C2 10.1021/acs.jmedchem.6b00358
CHEMBL521606 192006 33 None -1 3 Human 7.2 pKd = 7.2 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation counting
ChEMBL 309 5 4 5 0.6 CC(C)(C)NCC(O)COc1cccc2c1CC(O)C(O)C2 10.1021/acs.jmedchem.6b00358
702318 87096 67 None 19 2 Human 7.1 pKd = 7.1 Binding
Binding affinity to N-terminal FLAG-tagged C-terminal His-10-tagged human beta2 adrenoceptor expressed in insect Sf9 cells by surface plasmon resonance analysis in presence of maltose neopentyl glycolBinding affinity to N-terminal FLAG-tagged C-terminal His-10-tagged human beta2 adrenoceptor expressed in insect Sf9 cells by surface plasmon resonance analysis in presence of maltose neopentyl glycol
ChEMBL 227 1 1 3 2.0 Cc1cc(N2CCNCC2)c2ccccc2n1 10.1021/ml400312j
CHEMBL2335165 87096 67 None 19 2 Human 7.1 pKd = 7.1 Binding
Binding affinity to N-terminal FLAG-tagged C-terminal His-10-tagged human beta2 adrenoceptor expressed in insect Sf9 cells by surface plasmon resonance analysis in presence of maltose neopentyl glycolBinding affinity to N-terminal FLAG-tagged C-terminal His-10-tagged human beta2 adrenoceptor expressed in insect Sf9 cells by surface plasmon resonance analysis in presence of maltose neopentyl glycol
ChEMBL 227 1 1 3 2.0 Cc1cc(N2CCNCC2)c2ccccc2n1 10.1021/ml400312j
1499 2052 43 None -33 17 Human 6.1 pKd = 6.1 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation counting
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/acs.jmedchem.6b00358
3779 2052 43 None -33 17 Human 6.1 pKd = 6.1 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation counting
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/acs.jmedchem.6b00358
536 2052 43 None -33 17 Human 6.1 pKd = 6.1 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation counting
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/acs.jmedchem.6b00358
CHEMBL434 2052 43 None -33 17 Human 6.1 pKd = 6.1 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation counting
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/acs.jmedchem.6b00358
DB01064 2052 43 None -33 17 Human 6.1 pKd = 6.1 Binding
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation countingDisplacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation counting
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/acs.jmedchem.6b00358
13157386 62832 1 None -138 2 Guinea pig 5.1 pKd = 5.1 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
ChEMBL 479 12 3 7 4.4 COc1ccc(CCNC[C@H](O)COc2ccc(-c3nc(-c4cccs4)c[nH]3)cc2)cc1OC 10.1021/jm00361a004
CHEMBL1788320 62832 1 None -138 2 Guinea pig 5.1 pKd = 5.1 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
ChEMBL 479 12 3 7 4.4 COc1ccc(CCNC[C@H](O)COc2ccc(-c3nc(-c4cccs4)c[nH]3)cc2)cc1OC 10.1021/jm00361a004
CHEMBL1789879 62832 1 None -138 2 Guinea pig 5.1 pKd = 5.1 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
ChEMBL 479 12 3 7 4.4 COc1ccc(CCNC[C@H](O)COc2ccc(-c3nc(-c4cccs4)c[nH]3)cc2)cc1OC 10.1021/jm00361a004
135079 10387 1 None -9772 2 Guinea pig 5.1 pKd = 5.1 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 479 12 3 7 4.4 COc1ccc(CCNCC(O)COc2ccc(-c3nc(-c4cccs4)c[nH]3)cc2)cc1OC 10.1021/jm00156a028
CHEMBL11671 10387 1 None -9772 2 Guinea pig 5.1 pKd = 5.1 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 479 12 3 7 4.4 COc1ccc(CCNCC(O)COc2ccc(-c3nc(-c4cccs4)c[nH]3)cc2)cc1OC 10.1021/jm00156a028
13621723 9844 0 None -1698 2 Guinea pig 4.1 pKd = 4.1 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 395 10 5 5 2.2 O=C(NCCNCC(O)COc1ccc(-c2ncc[nH]2)cc1)Nc1ccccc1 10.1021/jm00156a028
CHEMBL11467 9844 0 None -1698 2 Guinea pig 4.1 pKd = 4.1 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 395 10 5 5 2.2 O=C(NCCNCC(O)COc1ccc(-c2ncc[nH]2)cc1)Nc1ccccc1 10.1021/jm00156a028
738389 88743 94 None - 1 Human 7.1 pKd = 7.1 Binding
Binding affinity to N-terminal FLAG-tagged C-terminal His-10-tagged human beta2 adrenoceptor expressed in insect Sf9 cells by surface plasmon resonance analysis in presence of maltose neopentyl glycolBinding affinity to N-terminal FLAG-tagged C-terminal His-10-tagged human beta2 adrenoceptor expressed in insect Sf9 cells by surface plasmon resonance analysis in presence of maltose neopentyl glycol
ChEMBL 247 1 1 3 2.3 Clc1ccc2c(N3CCNCC3)ccnc2c1 10.1021/ml400312j
CHEMBL236696 88743 94 None - 1 Human 7.1 pKd = 7.1 Binding
Binding affinity to N-terminal FLAG-tagged C-terminal His-10-tagged human beta2 adrenoceptor expressed in insect Sf9 cells by surface plasmon resonance analysis in presence of maltose neopentyl glycolBinding affinity to N-terminal FLAG-tagged C-terminal His-10-tagged human beta2 adrenoceptor expressed in insect Sf9 cells by surface plasmon resonance analysis in presence of maltose neopentyl glycol
ChEMBL 247 1 1 3 2.3 Clc1ccc2c(N3CCNCC3)ccnc2c1 10.1021/ml400312j
13040884 23563 0 None -15 2 Guinea pig 7.1 pKd = 7.1 Binding
Ability to block Beta-2 adrenergic receptor in guinea pig trachea preparationAbility to block Beta-2 adrenergic receptor in guinea pig trachea preparation
ChEMBL 389 11 2 7 2.1 COC(=O)c1ccccc1OCC(O)CNCCc1ccc(OC)c(OC)c1 10.1021/jm00354a003
CHEMBL13358 23563 0 None -15 2 Guinea pig 7.1 pKd = 7.1 Binding
Ability to block Beta-2 adrenergic receptor in guinea pig trachea preparationAbility to block Beta-2 adrenergic receptor in guinea pig trachea preparation
ChEMBL 389 11 2 7 2.1 COC(=O)c1ccccc1OCC(O)CNCCc1ccc(OC)c(OC)c1 10.1021/jm00354a003
3464 3111 29 None 1659 2 Human 7.1 pKd = 7.1 Binding
Binding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nMBinding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nM
ChEMBL 290 5 4 4 2.0 CCC(C(c1ccc(c2c1ccc(=O)[nH]2)O)O)NC(C)C 10.1016/j.bmcl.2013.07.052
4916 3111 29 None 1659 2 Human 7.1 pKd = 7.1 Binding
Binding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nMBinding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nM
ChEMBL 290 5 4 4 2.0 CCC(C(c1ccc(c2c1ccc(=O)[nH]2)O)O)NC(C)C 10.1016/j.bmcl.2013.07.052
CHEMBL160519 3111 29 None 1659 2 Human 7.1 pKd = 7.1 Binding
Binding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nMBinding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nM
ChEMBL 290 5 4 4 2.0 CCC(C(c1ccc(c2c1ccc(=O)[nH]2)O)O)NC(C)C 10.1016/j.bmcl.2013.07.052
DB01366 3111 29 None 1659 2 Human 7.1 pKd = 7.1 Binding
Binding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nMBinding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nM
ChEMBL 290 5 4 4 2.0 CCC(C(c1ccc(c2c1ccc(=O)[nH]2)O)O)NC(C)C 10.1016/j.bmcl.2013.07.052
13040896 101725 1 None -15 2 Guinea pig 6.1 pKd = 6.1 Binding
Ability to block Beta-2 adrenergic receptor in guinea pig trachea preparationAbility to block Beta-2 adrenergic receptor in guinea pig trachea preparation
ChEMBL 293 8 2 5 1.6 COC(=O)/C=C/c1ccc(OCC(O)CNC(C)C)cc1 10.1021/jm00354a003
CHEMBL30289 101725 1 None -15 2 Guinea pig 6.1 pKd = 6.1 Binding
Ability to block Beta-2 adrenergic receptor in guinea pig trachea preparationAbility to block Beta-2 adrenergic receptor in guinea pig trachea preparation
ChEMBL 293 8 2 5 1.6 COC(=O)/C=C/c1ccc(OCC(O)CNC(C)C)cc1 10.1021/jm00354a003
12238216 106626 0 None -2 2 Guinea pig 6.1 pKd = 6.1 Binding
Ability to block Beta-2 adrenergic receptor in guinea pig trachea preparationAbility to block Beta-2 adrenergic receptor in guinea pig trachea preparation
ChEMBL 281 8 2 5 1.6 CCOC(=O)c1ccc(OCC(O)CNC(C)C)cc1 10.1021/jm00354a003
CHEMBL31608 106626 0 None -2 2 Guinea pig 6.1 pKd = 6.1 Binding
Ability to block Beta-2 adrenergic receptor in guinea pig trachea preparationAbility to block Beta-2 adrenergic receptor in guinea pig trachea preparation
ChEMBL 281 8 2 5 1.6 CCOC(=O)c1ccc(OCC(O)CNC(C)C)cc1 10.1021/jm00354a003
56599230 87811 0 None -10 2 Human 6.1 pKd = 6.1 Binding
Displacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 535 14 4 6 3.9 O=C(NCCNCC(O)COc1ccc(OCCOC2CCCC2)cc1)Nc1ccccc1Br 10.1021/jm400348g
CHEMBL2348203 87811 0 None -10 2 Human 6.1 pKd = 6.1 Binding
Displacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 535 14 4 6 3.9 O=C(NCCNCC(O)COc1ccc(OCCOC2CCCC2)cc1)Nc1ccccc1Br 10.1021/jm400348g
16737412 85341 0 None 3 2 Human 5.1 pKd = 5.1 Binding
Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.
ChEMBL 287 6 4 4 2.4 C[C@@H](Cc1ccccc1)NC[C@H](O)c1cc(O)cc(O)c1 nan
CHEMBL229388 85341 0 None 3 2 Human 5.1 pKd = 5.1 Binding
Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.
ChEMBL 287 6 4 4 2.4 C[C@@H](Cc1ccccc1)NC[C@H](O)c1cc(O)cc(O)c1 nan
14348818 109273 0 None -12 3 Guinea pig 4.1 pKd = 4.1 Binding
The compound was tested for beta-adrenergic activity against Beta-2 adrenergic receptor from guinea pig trachea.The compound was tested for beta-adrenergic activity against Beta-2 adrenergic receptor from guinea pig trachea.
ChEMBL 415 7 4 7 2.9 C/C(=N\OCC(O)CNC(C)(C)C)c1cc(Cl)c(NC2=NCCN2)c(Cl)c1 10.1021/jm00115a008
CHEMBL323176 109273 0 None -12 3 Guinea pig 4.1 pKd = 4.1 Binding
The compound was tested for beta-adrenergic activity against Beta-2 adrenergic receptor from guinea pig trachea.The compound was tested for beta-adrenergic activity against Beta-2 adrenergic receptor from guinea pig trachea.
ChEMBL 415 7 4 7 2.9 C/C(=N\OCC(O)CNC(C)(C)C)c1cc(Cl)c(NC2=NCCN2)c(Cl)c1 10.1021/jm00115a008
44459582 93112 0 None 13 2 Guinea pig 8.1 pKd = 8.1 Binding
Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.
ChEMBL 312 8 2 5 2.5 CC(C)(C)NCC(O)CO/N=C(/CC(=O)C(C)(C)C)C1CC1 10.1021/jm00376a011
CHEMBL24644 93112 0 None 13 2 Guinea pig 8.1 pKd = 8.1 Binding
Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.
ChEMBL 312 8 2 5 2.5 CC(C)(C)NCC(O)CO/N=C(/CC(=O)C(C)(C)C)C1CC1 10.1021/jm00376a011
12878477 103046 0 None -10 2 Guinea pig 8.1 pKd = 8.1 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
ChEMBL 357 6 3 4 3.2 CC(C)(C)NC[C@H](O)COc1ccc(-c2nc(C(F)(F)F)c[nH]2)cc1 10.1021/jm00361a004
CHEMBL3085291 103046 0 None -10 2 Guinea pig 8.1 pKd = 8.1 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
ChEMBL 357 6 3 4 3.2 CC(C)(C)NC[C@H](O)COc1ccc(-c2nc(C(F)(F)F)c[nH]2)cc1 10.1021/jm00361a004
54579961 62717 1 None 3 2 Guinea pig 8.1 pKd = 8.1 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor determined as pA2 in guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor determined as pA2 in guinea pig trachea
ChEMBL 254 7 2 4 1.9 CC(C)(C)NC[C@@H](O)CON=C(C1CC1)C1CC1 10.1021/jm00145a008
CHEMBL1788274 62717 1 None 3 2 Guinea pig 8.1 pKd = 8.1 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor determined as pA2 in guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor determined as pA2 in guinea pig trachea
ChEMBL 254 7 2 4 1.9 CC(C)(C)NC[C@@H](O)CON=C(C1CC1)C1CC1 10.1021/jm00145a008
11460205 92562 9 None - 1 Human 5.1 pKd = 5.1 Binding
Binding affinity to N-terminal FLAG-tagged C-terminal His-10-tagged human beta2 adrenoceptor expressed in insect Sf9 cells by surface plasmon resonance analysis in presence of maltose neopentyl glycolBinding affinity to N-terminal FLAG-tagged C-terminal His-10-tagged human beta2 adrenoceptor expressed in insect Sf9 cells by surface plasmon resonance analysis in presence of maltose neopentyl glycol
ChEMBL 281 1 1 3 2.7 FC(F)(F)c1ccc2c(N3CCNCC3)ccnc2c1 10.1021/ml400312j
CHEMBL2441615 92562 9 None - 1 Human 5.1 pKd = 5.1 Binding
Binding affinity to N-terminal FLAG-tagged C-terminal His-10-tagged human beta2 adrenoceptor expressed in insect Sf9 cells by surface plasmon resonance analysis in presence of maltose neopentyl glycolBinding affinity to N-terminal FLAG-tagged C-terminal His-10-tagged human beta2 adrenoceptor expressed in insect Sf9 cells by surface plasmon resonance analysis in presence of maltose neopentyl glycol
ChEMBL 281 1 1 3 2.7 FC(F)(F)c1ccc2c(N3CCNCC3)ccnc2c1 10.1021/ml400312j
44459890 99534 0 None -8 2 Guinea pig 7.1 pKd = 7.1 Binding
Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.
ChEMBL 214 6 2 4 1.1 CC(C)(C)NCC(O)CO/N=C\C1CC1 10.1021/jm00376a011
CHEMBL286783 99534 0 None -8 2 Guinea pig 7.1 pKd = 7.1 Binding
Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.
ChEMBL 214 6 2 4 1.1 CC(C)(C)NCC(O)CO/N=C\C1CC1 10.1021/jm00376a011
738389 88743 94 None - 1 Human 7.1 pKd = 7.1 Binding
Binding affinity to N-terminal FLAG-tagged C-terminal His-10-tagged human beta2 adrenoceptor expressed in insect Sf9 cells by surface plasmon resonance analysisBinding affinity to N-terminal FLAG-tagged C-terminal His-10-tagged human beta2 adrenoceptor expressed in insect Sf9 cells by surface plasmon resonance analysis
ChEMBL 247 1 1 3 2.3 Clc1ccc2c(N3CCNCC3)ccnc2c1 10.1021/ml400312j
CHEMBL236696 88743 94 None - 1 Human 7.1 pKd = 7.1 Binding
Binding affinity to N-terminal FLAG-tagged C-terminal His-10-tagged human beta2 adrenoceptor expressed in insect Sf9 cells by surface plasmon resonance analysisBinding affinity to N-terminal FLAG-tagged C-terminal His-10-tagged human beta2 adrenoceptor expressed in insect Sf9 cells by surface plasmon resonance analysis
ChEMBL 247 1 1 3 2.3 Clc1ccc2c(N3CCNCC3)ccnc2c1 10.1021/ml400312j
123686 1942 44 None -891 9 Guinea pig 6.1 pKd = 6.1 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 354 9 4 5 1.7 C1=CC=C(C=C1)NC(=O)NCCNCC(COC2=CC=CC=C2C#N)O 10.1021/jm00156a028
12581 1942 44 None -891 9 Guinea pig 6.1 pKd = 6.1 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 354 9 4 5 1.7 C1=CC=C(C=C1)NC(=O)NCCNCC(COC2=CC=CC=C2C#N)O 10.1021/jm00156a028
CHEMBL11268 1942 44 None -891 9 Guinea pig 6.1 pKd = 6.1 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 354 9 4 5 1.7 C1=CC=C(C=C1)NC(=O)NCCNCC(COC2=CC=CC=C2C#N)O 10.1021/jm00156a028
2777813 67118 58 None - 1 Human 7.1 pKd = 7.1 Binding
Binding affinity to N-terminal FLAG-tagged C-terminal His-10-tagged human beta2 adrenoceptor expressed in insect Sf9 cells by surface plasmon resonance analysis in presence of maltose neopentyl glycolBinding affinity to N-terminal FLAG-tagged C-terminal His-10-tagged human beta2 adrenoceptor expressed in insect Sf9 cells by surface plasmon resonance analysis in presence of maltose neopentyl glycol
ChEMBL 281 1 1 3 2.7 FC(F)(F)c1cc(N2CCNCC2)c2ccccc2n1 10.1021/ml400312j
CHEMBL1892158 67118 58 None - 1 Human 7.1 pKd = 7.1 Binding
Binding affinity to N-terminal FLAG-tagged C-terminal His-10-tagged human beta2 adrenoceptor expressed in insect Sf9 cells by surface plasmon resonance analysis in presence of maltose neopentyl glycolBinding affinity to N-terminal FLAG-tagged C-terminal His-10-tagged human beta2 adrenoceptor expressed in insect Sf9 cells by surface plasmon resonance analysis in presence of maltose neopentyl glycol
ChEMBL 281 1 1 3 2.7 FC(F)(F)c1cc(N2CCNCC2)c2ccccc2n1 10.1021/ml400312j
13621796 9342 0 None -1659 2 Guinea pig 5.1 pKd = 5.1 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 480 12 3 8 3.8 COc1ccc(CCNCC(O)COc2ccc(-c3nc(-c4cccs4)c[nH]3)cn2)cc1OC 10.1021/jm00156a028
CHEMBL11178 9342 0 None -1659 2 Guinea pig 5.1 pKd = 5.1 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 480 12 3 8 3.8 COc1ccc(CCNCC(O)COc2ccc(-c3nc(-c4cccs4)c[nH]3)cn2)cc1OC 10.1021/jm00156a028
56599098 87821 0 None -95 2 Human 6.1 pKd = 6.1 Binding
Displacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 471 14 4 6 3.5 Cc1cccc(NC(=O)NCCNCC(O)COc2ccc(OCCOC3CCCC3)cc2)c1 10.1021/jm400348g
CHEMBL2348213 87821 0 None -95 2 Human 6.1 pKd = 6.1 Binding
Displacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 471 14 4 6 3.5 Cc1cccc(NC(=O)NCCNCC(O)COc2ccc(OCCOC3CCCC3)cc2)c1 10.1021/jm400348g
13157405 77596 0 None -141 2 Guinea pig 6.1 pKd = 6.1 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
ChEMBL 355 8 3 5 3.3 O[C@@H](CNC1CC1)COc1ccc(-c2nc(-c3cccs3)c[nH]2)cc1 10.1021/jm00361a004
CHEMBL2096750 77596 0 None -141 2 Guinea pig 6.1 pKd = 6.1 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
ChEMBL 355 8 3 5 3.3 O[C@@H](CNC1CC1)COc1ccc(-c2nc(-c3cccs3)c[nH]2)cc1 10.1021/jm00361a004
3869259 156899 3 None 3 2 Human 6.1 pKd = 6.1 Binding
Displacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting methodDisplacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting method
ChEMBL 419 4 0 5 5.5 CCOC(=O)c1cc(/C=C/c2sc3ccccc3[n+]2C)c2sc3ccccc3n12 10.1021/acsmedchemlett.6b00363
45052940 156899 3 None 3 2 Human 6.1 pKd = 6.1 Binding
Displacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting methodDisplacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting method
ChEMBL 419 4 0 5 5.5 CCOC(=O)c1cc(/C=C/c2sc3ccccc3[n+]2C)c2sc3ccccc3n12 10.1021/acsmedchemlett.6b00363
5942882 156899 3 None 3 2 Human 6.1 pKd = 6.1 Binding
Displacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting methodDisplacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting method
ChEMBL 419 4 0 5 5.5 CCOC(=O)c1cc(/C=C/c2sc3ccccc3[n+]2C)c2sc3ccccc3n12 10.1021/acsmedchemlett.6b00363
CHEMBL4079127 156899 3 None 3 2 Human 6.1 pKd = 6.1 Binding
Displacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting methodDisplacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting method
ChEMBL 419 4 0 5 5.5 CCOC(=O)c1cc(/C=C/c2sc3ccccc3[n+]2C)c2sc3ccccc3n12 10.1021/acsmedchemlett.6b00363
71662247 87824 0 None -51 2 Human 6.1 pKd = 6.1 Binding
Displacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 487 15 4 7 3.2 COc1cccc(NC(=O)NCCNCC(O)COc2ccc(OCCOC3CCCC3)cc2)c1 10.1021/jm400348g
CHEMBL2348216 87824 0 None -51 2 Human 6.1 pKd = 6.1 Binding
Displacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 487 15 4 7 3.2 COc1cccc(NC(=O)NCCNCC(O)COc2ccc(OCCOC3CCCC3)cc2)c1 10.1021/jm400348g
44383465 120230 1 None 2 2 Guinea pig 8.0 pKd = 8.0 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor determined as pA2 in guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor determined as pA2 in guinea pig trachea
ChEMBL 228 6 2 4 1.5 C/C(=N\OC[C@@H](O)CNC(C)(C)C)C1CC1 10.1021/jm00145a008
CHEMBL355100 120230 1 None 2 2 Guinea pig 8.0 pKd = 8.0 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor determined as pA2 in guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor determined as pA2 in guinea pig trachea
ChEMBL 228 6 2 4 1.5 C/C(=N\OC[C@@H](O)CNC(C)(C)C)C1CC1 10.1021/jm00145a008
19136 110883 22 None - 1 Bovine 6.0 pKd = 6.0 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 195 4 3 3 1.4 CC(C)NCC(O)c1cccc(O)c1 10.1021/jm00147a037
CHEMBL327122 110883 22 None - 1 Bovine 6.0 pKd = 6.0 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 195 4 3 3 1.4 CC(C)NCC(O)c1cccc(O)c1 10.1021/jm00147a037
13621680 161561 0 None -446 2 Guinea pig 6.0 pKd = 6.0 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 431 11 3 6 3.3 COc1ccc(CCNCC(O)COc2ccc(-c3nc(Cl)c[nH]3)cc2)cc1OC 10.1021/jm00156a028
CHEMBL416150 161561 0 None -446 2 Guinea pig 6.0 pKd = 6.0 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
ChEMBL 431 11 3 6 3.3 COc1ccc(CCNCC(O)COc2ccc(-c3nc(Cl)c[nH]3)cc2)cc1OC 10.1021/jm00156a028
1720 2901 35 None 2 2 Bovine 5.0 pKd = 5.0 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 211 4 4 4 1.1 OC(c1cc(O)cc(c1)O)CNC(C)C 10.1021/jm00147a037
4086 2901 35 None 2 2 Bovine 5.0 pKd = 5.0 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 211 4 4 4 1.1 OC(c1cc(O)cc(c1)O)CNC(C)C 10.1021/jm00147a037
7250 2901 35 None 2 2 Bovine 5.0 pKd = 5.0 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 211 4 4 4 1.1 OC(c1cc(O)cc(c1)O)CNC(C)C 10.1021/jm00147a037
CHEMBL776 2901 35 None 2 2 Bovine 5.0 pKd = 5.0 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 211 4 4 4 1.1 OC(c1cc(O)cc(c1)O)CNC(C)C 10.1021/jm00147a037
DB00816 2901 35 None 2 2 Bovine 5.0 pKd = 5.0 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
ChEMBL 211 4 4 4 1.1 OC(c1cc(O)cc(c1)O)CNC(C)C 10.1021/jm00147a037
702318 87096 67 None 19 2 Human 7.0 pKd = 7.0 Binding
Binding affinity to N-terminal FLAG-tagged C-terminal His-10-tagged human beta2 adrenoceptor expressed in insect Sf9 cells by surface plasmon resonance analysisBinding affinity to N-terminal FLAG-tagged C-terminal His-10-tagged human beta2 adrenoceptor expressed in insect Sf9 cells by surface plasmon resonance analysis
ChEMBL 227 1 1 3 2.0 Cc1cc(N2CCNCC2)c2ccccc2n1 10.1021/ml400312j
CHEMBL2335165 87096 67 None 19 2 Human 7.0 pKd = 7.0 Binding
Binding affinity to N-terminal FLAG-tagged C-terminal His-10-tagged human beta2 adrenoceptor expressed in insect Sf9 cells by surface plasmon resonance analysisBinding affinity to N-terminal FLAG-tagged C-terminal His-10-tagged human beta2 adrenoceptor expressed in insect Sf9 cells by surface plasmon resonance analysis
ChEMBL 227 1 1 3 2.0 Cc1cc(N2CCNCC2)c2ccccc2n1 10.1021/ml400312j
12462220 112104 2 None 1 2 Guinea pig 6.0 pKd = 6.0 Binding
Antagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 minsAntagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 mins
ChEMBL 287 5 2 3 2.5 COc1ccc(Br)cc1C(O)CNC(C)C 10.1021/jm00208a015
CHEMBL3246230 112104 2 None 1 2 Guinea pig 6.0 pKd = 6.0 Binding
Antagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 minsAntagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 mins
ChEMBL 287 5 2 3 2.5 COc1ccc(Br)cc1C(O)CNC(C)C 10.1021/jm00208a015
CHEMBL3302368 112104 2 None 1 2 Guinea pig 6.0 pKd = 6.0 Binding
Antagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 minsAntagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 mins
ChEMBL 287 5 2 3 2.5 COc1ccc(Br)cc1C(O)CNC(C)C 10.1021/jm00208a015
16735274 159476 0 None 1 2 Human 5.0 pKd = 5.0 Binding
Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.
ChEMBL 267 8 4 4 2.7 CCCCC[C@@H](C)NC[C@H](O)c1cc(O)cc(O)c1 nan
CHEMBL4108123 159476 0 None 1 2 Human 5.0 pKd = 5.0 Binding
Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.Beta2-AR Binding Assay: HEK 293 cells stability transfected with cDNA encoding human beta2-AR (provided by Dr. Brian Kobilka, Stanford Medical Center, Palo Alto, Calif.) were grown in Dulbecco's Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS), 0.05% penicillin-streptomycin, and 400 μg/ml G418 as previously described (Pauwels et al., Biochem. Pharmacol. 42: 1683-1689, 1991). The cells were scraped from the 150x25 mm plates and centrifuged at 500xg for 5 minutes. The pellet was homogenized in 50 mM Tris-HCl, pH 7.7, with a Polytron, centrifuged at 27,000xg, and resuspended in the same buffer. The latter process was repeated, and the pellet was resuspended in 25 mM Tris-HCl containing 120 mM NaCl, 5.4 mM KCl, 1.8 mM CaCl2, 0.8 mM MgCl2, and 5 mM glucose, pH 7.4. The binding assays contained 0.3 nM [3H]CGP-12177 in a volume of 1.0 ml. Nonspecific binding was determined by 1 uM propranolol.
ChEMBL 267 8 4 4 2.7 CCCCC[C@@H](C)NC[C@H](O)c1cc(O)cc(O)c1 nan
2892936 95461 5 None 15 2 Guinea pig 7.0 pKd = 7.0 Binding
Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.
ChEMBL 271 5 2 3 3.0 CC1CC(OCC(O)CNC(C)(C)C)CC(C)(C)C1 10.1021/jm00376a011
CHEMBL25929 95461 5 None 15 2 Guinea pig 7.0 pKd = 7.0 Binding
Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.
ChEMBL 271 5 2 3 3.0 CC1CC(OCC(O)CNC(C)(C)C)CC(C)(C)C1 10.1021/jm00376a011
44274622 99318 0 None 3 2 Guinea pig 6.0 pKd = 6.0 Binding
Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.
ChEMBL 215 6 2 3 1.6 CC(OCC(O)CNC(C)(C)C)C1CC1 10.1021/jm00376a011
CHEMBL285309 99318 0 None 3 2 Guinea pig 6.0 pKd = 6.0 Binding
Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.Beta-2 adrenergic receptor blocking activity in trachea of guinea pig.
ChEMBL 215 6 2 3 1.6 CC(OCC(O)CNC(C)(C)C)C1CC1 10.1021/jm00376a011
9849699 72902 9 None 1 2 Human 10.9 pKi = 10.9 Binding
Displacement of [125I]Iodocyanopindolol from human adrenergic beta2 receptor expressed in insect sf9 cells by scintillation countingDisplacement of [125I]Iodocyanopindolol from human adrenergic beta2 receptor expressed in insect sf9 cells by scintillation counting
ChEMBL 524 11 4 6 5.0 CC(C)(Cc1ccc(Oc2ccc(C(N)=O)cn2)cc1)NC[C@H](O)COc1cccc2[nH]c3ccccc3c12 10.1021/ml200071k
CHEMBL2012520 72902 9 None 1 2 Human 10.9 pKi = 10.9 Binding
Displacement of [125I]Iodocyanopindolol from human adrenergic beta2 receptor expressed in insect sf9 cells by scintillation countingDisplacement of [125I]Iodocyanopindolol from human adrenergic beta2 receptor expressed in insect sf9 cells by scintillation counting
ChEMBL 524 11 4 6 5.0 CC(C)(Cc1ccc(Oc2ccc(C(N)=O)cn2)cc1)NC[C@H](O)COc1cccc2[nH]c3ccccc3c12 10.1021/ml200071k
CHEMBL2012521 72902 9 None 1 2 Human 10.9 pKi = 10.9 Binding
Displacement of [125I]Iodocyanopindolol from human adrenergic beta2 receptor expressed in insect sf9 cells by scintillation countingDisplacement of [125I]Iodocyanopindolol from human adrenergic beta2 receptor expressed in insect sf9 cells by scintillation counting
ChEMBL 524 11 4 6 5.0 CC(C)(Cc1ccc(Oc2ccc(C(N)=O)cn2)cc1)NC[C@H](O)COc1cccc2[nH]c3ccccc3c12 10.1021/ml200071k
CHEMBL2012522 72902 9 None 1 2 Human 10.9 pKi = 10.9 Binding
Displacement of [125I]Iodocyanopindolol from human adrenergic beta2 receptor expressed in insect sf9 cells by scintillation countingDisplacement of [125I]Iodocyanopindolol from human adrenergic beta2 receptor expressed in insect sf9 cells by scintillation counting
ChEMBL 524 11 4 6 5.0 CC(C)(Cc1ccc(Oc2ccc(C(N)=O)cn2)cc1)NC[C@H](O)COc1cccc2[nH]c3ccccc3c12 10.1021/ml200071k
164620727 185494 0 None 7 2 Human 10.9 pKi = 10.9 Binding
Displacement of 125I-cyanopindolol from human adrenergic beta2 receptorDisplacement of 125I-cyanopindolol from human adrenergic beta2 receptor
ChEMBL 821 16 6 9 6.8 O=C(N[C@@H](c1ccccc1)c1ccc(-c2cccc(OCc3ccc(C(=O)NCCCNC[C@H](O)c4ccc(O)c5[nH]c(=O)ccc45)cc3)c2)cc1)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2021.127975
CHEMBL4871517 185494 0 None 7 2 Human 10.9 pKi = 10.9 Binding
Displacement of 125I-cyanopindolol from human adrenergic beta2 receptorDisplacement of 125I-cyanopindolol from human adrenergic beta2 receptor
ChEMBL 821 16 6 9 6.8 O=C(N[C@@H](c1ccccc1)c1ccc(-c2cccc(OCc3ccc(C(=O)NCCCNC[C@H](O)c4ccc(O)c5[nH]c(=O)ccc45)cc3)c2)cc1)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2021.127975
71113309 184989 0 None 19 2 Human 10.8 pKi = 10.8 Binding
Displacement of 125I-cyanopindolol from human adrenergic beta2 receptorDisplacement of 125I-cyanopindolol from human adrenergic beta2 receptor
ChEMBL 654 15 5 8 5.4 O=C(NC(c1ccccc1)c1cccc(OCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)c1)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2021.127975
CHEMBL4863525 184989 0 None 19 2 Human 10.8 pKi = 10.8 Binding
Displacement of 125I-cyanopindolol from human adrenergic beta2 receptorDisplacement of 125I-cyanopindolol from human adrenergic beta2 receptor
ChEMBL 654 15 5 8 5.4 O=C(NC(c1ccccc1)c1cccc(OCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)c1)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2021.127975
168280960 190244 0 None 6 2 Human 10.7 pKi = 10.7 Binding
Displacement of 125I-cyanopindolol from human beta2 adrenoceptor expressed in CHO-K1 cell membrane measured after 1 hr by Cheng-prusoff equation analysisDisplacement of 125I-cyanopindolol from human beta2 adrenoceptor expressed in CHO-K1 cell membrane measured after 1 hr by Cheng-prusoff equation analysis
ChEMBL 760 16 5 10 6.0 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2ccc(C(=O)OCCCCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
CHEMBL5184455 190244 0 None 6 2 Human 10.7 pKi = 10.7 Binding
Displacement of 125I-cyanopindolol from human beta2 adrenoceptor expressed in CHO-K1 cell membrane measured after 1 hr by Cheng-prusoff equation analysisDisplacement of 125I-cyanopindolol from human beta2 adrenoceptor expressed in CHO-K1 cell membrane measured after 1 hr by Cheng-prusoff equation analysis
ChEMBL 760 16 5 10 6.0 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2ccc(C(=O)OCCCCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
164627621 185734 0 None 15 2 Human 10.6 pKi = 10.6 Binding
Displacement of 125I-cyanopindolol from human adrenergic beta2 receptorDisplacement of 125I-cyanopindolol from human adrenergic beta2 receptor
ChEMBL 640 14 5 8 5.0 O=C(NC(c1ccccc1)c1cccc(OCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)c1)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2021.127975
CHEMBL4874819 185734 0 None 15 2 Human 10.6 pKi = 10.6 Binding
Displacement of 125I-cyanopindolol from human adrenergic beta2 receptorDisplacement of 125I-cyanopindolol from human adrenergic beta2 receptor
ChEMBL 640 14 5 8 5.0 O=C(NC(c1ccccc1)c1cccc(OCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)c1)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2021.127975
90213810 190659 0 None 2 2 Human 10.6 pKi = 10.6 Binding
Displacement of 125I-cyanopindolol from human beta2 adrenoceptor expressed in CHO-K1 cell membrane measured after 1 hr by Cheng-prusoff equation analysisDisplacement of 125I-cyanopindolol from human beta2 adrenoceptor expressed in CHO-K1 cell membrane measured after 1 hr by Cheng-prusoff equation analysis
ChEMBL 750 16 5 11 5.6 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2ccc(C(=O)OCCCCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)o2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
CHEMBL5190387 190659 0 None 2 2 Human 10.6 pKi = 10.6 Binding
Displacement of 125I-cyanopindolol from human beta2 adrenoceptor expressed in CHO-K1 cell membrane measured after 1 hr by Cheng-prusoff equation analysisDisplacement of 125I-cyanopindolol from human beta2 adrenoceptor expressed in CHO-K1 cell membrane measured after 1 hr by Cheng-prusoff equation analysis
ChEMBL 750 16 5 11 5.6 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2ccc(C(=O)OCCCCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)o2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
168287036 190900 0 None 3 2 Human 10.6 pKi = 10.6 Binding
Displacement of 125I-cyanopindolol from human beta2 adrenoceptor expressed in CHO-K1 cell membrane measured after 1 hr by Cheng-prusoff equation analysisDisplacement of 125I-cyanopindolol from human beta2 adrenoceptor expressed in CHO-K1 cell membrane measured after 1 hr by Cheng-prusoff equation analysis
ChEMBL 760 16 5 10 6.0 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2cccc(C(=O)OCCCCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
CHEMBL5193853 190900 0 None 3 2 Human 10.6 pKi = 10.6 Binding
Displacement of 125I-cyanopindolol from human beta2 adrenoceptor expressed in CHO-K1 cell membrane measured after 1 hr by Cheng-prusoff equation analysisDisplacement of 125I-cyanopindolol from human beta2 adrenoceptor expressed in CHO-K1 cell membrane measured after 1 hr by Cheng-prusoff equation analysis
ChEMBL 760 16 5 10 6.0 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2cccc(C(=O)OCCCCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
168290830 191348 0 None 7 2 Human 10.6 pKi = 10.6 Binding
Displacement of 125I-cyanopindolol from human beta2 adrenoceptor expressed in CHO-K1 cell membrane measured after 1 hr by Cheng-prusoff equation analysisDisplacement of 125I-cyanopindolol from human beta2 adrenoceptor expressed in CHO-K1 cell membrane measured after 1 hr by Cheng-prusoff equation analysis
ChEMBL 790 17 5 11 6.0 COc1cc(C(=O)OCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1COc1cccc([C@@H](NC(=O)O[C@H]2CN3CCC2CC3)c2ccccc2)c1 10.1021/acs.jmedchem.2c00609
CHEMBL5200887 191348 0 None 7 2 Human 10.6 pKi = 10.6 Binding
Displacement of 125I-cyanopindolol from human beta2 adrenoceptor expressed in CHO-K1 cell membrane measured after 1 hr by Cheng-prusoff equation analysisDisplacement of 125I-cyanopindolol from human beta2 adrenoceptor expressed in CHO-K1 cell membrane measured after 1 hr by Cheng-prusoff equation analysis
ChEMBL 790 17 5 11 6.0 COc1cc(C(=O)OCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1COc1cccc([C@@H](NC(=O)O[C@H]2CN3CCC2CC3)c2ccccc2)c1 10.1021/acs.jmedchem.2c00609
487 779 65 None 4 6 Human 10.5 pKi = 10.5 Binding
Displacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assay
ChEMBL 298 6 3 3 3.1 OC(COc1cccc2c1c1ccccc1[nH]2)CNC(C)C 10.1021/acs.jmedchem.9b00349
569 779 65 None 4 6 Human 10.5 pKi = 10.5 Binding
Displacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assay
ChEMBL 298 6 3 3 3.1 OC(COc1cccc2c1c1ccccc1[nH]2)CNC(C)C 10.1021/acs.jmedchem.9b00349
71739 779 65 None 4 6 Human 10.5 pKi = 10.5 Binding
Displacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assay
ChEMBL 298 6 3 3 3.1 OC(COc1cccc2c1c1ccccc1[nH]2)CNC(C)C 10.1021/acs.jmedchem.9b00349
CHEMBL324665 779 65 None 4 6 Human 10.5 pKi = 10.5 Binding
Displacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assay
ChEMBL 298 6 3 3 3.1 OC(COc1cccc2c1c1ccccc1[nH]2)CNC(C)C 10.1021/acs.jmedchem.9b00349
185395 139303 37 None 6 3 Human 10.5 pKi = 10.5 Binding
Displacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assay
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNC[C@H](O)COc1cccc2[nH]c3ccccc3c12 10.1021/acs.jmedchem.9b00349
CHEMBL3799125 139303 37 None 6 3 Human 10.5 pKi = 10.5 Binding
Displacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assay
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNC[C@H](O)COc1cccc2[nH]c3ccccc3c12 10.1021/acs.jmedchem.9b00349
185395 139303 37 None 6 3 Human 10.5 pKi = 10.5 Binding
Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cellsDisplacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNC[C@H](O)COc1cccc2[nH]c3ccccc3c12 10.1016/j.bmc.2016.04.028
CHEMBL3799125 139303 37 None 6 3 Human 10.5 pKi = 10.5 Binding
Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cellsDisplacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNC[C@H](O)COc1cccc2[nH]c3ccccc3c12 10.1016/j.bmc.2016.04.028
164617537 184620 0 None 100 2 Human 10.4 pKi = 10.4 Binding
Displacement of 125I-cyanopindolol from human adrenergic beta2 receptorDisplacement of 125I-cyanopindolol from human adrenergic beta2 receptor
ChEMBL 654 15 5 8 5.4 O=C(N[C@H](c1ccccc1)c1cccc(OCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)c1)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2021.127975
CHEMBL4857743 184620 0 None 100 2 Human 10.4 pKi = 10.4 Binding
Displacement of 125I-cyanopindolol from human adrenergic beta2 receptorDisplacement of 125I-cyanopindolol from human adrenergic beta2 receptor
ChEMBL 654 15 5 8 5.4 O=C(N[C@H](c1ccccc1)c1cccc(OCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)c1)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2021.127975
71093373 191816 0 None 7 2 Human 10.4 pKi = 10.4 Binding
Displacement of 125I-cyanopindolol from human beta2 adrenoceptor expressed in CHO-K1 cell membrane measured after 1 hr by Cheng-prusoff equation analysisDisplacement of 125I-cyanopindolol from human beta2 adrenoceptor expressed in CHO-K1 cell membrane measured after 1 hr by Cheng-prusoff equation analysis
ChEMBL 760 16 5 10 6.0 O=C(NC(c1ccccc1)c1cccc(OCc2ccc(C(=O)OCCCCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
CHEMBL5208201 191816 0 None 7 2 Human 10.4 pKi = 10.4 Binding
Displacement of 125I-cyanopindolol from human beta2 adrenoceptor expressed in CHO-K1 cell membrane measured after 1 hr by Cheng-prusoff equation analysisDisplacement of 125I-cyanopindolol from human beta2 adrenoceptor expressed in CHO-K1 cell membrane measured after 1 hr by Cheng-prusoff equation analysis
ChEMBL 760 16 5 10 6.0 O=C(NC(c1ccccc1)c1cccc(OCc2ccc(C(=O)OCCCCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
164621790 185200 0 None 5 2 Human 10.3 pKi = 10.3 Binding
Displacement of 125I-cyanopindolol from human adrenergic beta2 receptorDisplacement of 125I-cyanopindolol from human adrenergic beta2 receptor
ChEMBL 849 17 5 9 7.6 CCN(CCCNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12)C(=O)c1ccc(COc2cccc(-c3ccc([C@@H](NC(=O)O[C@H]4CN5CCC4CC5)c4ccccc4)cc3)c2)cc1 10.1016/j.bmcl.2021.127975
CHEMBL4866806 185200 0 None 5 2 Human 10.3 pKi = 10.3 Binding
Displacement of 125I-cyanopindolol from human adrenergic beta2 receptorDisplacement of 125I-cyanopindolol from human adrenergic beta2 receptor
ChEMBL 849 17 5 9 7.6 CCN(CCCNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12)C(=O)c1ccc(COc2cccc(-c3ccc([C@@H](NC(=O)O[C@H]4CN5CCC4CC5)c4ccccc4)cc3)c2)cc1 10.1016/j.bmcl.2021.127975
168279881 190258 0 None 15 2 Human 10.3 pKi = 10.3 Binding
Displacement of 125I-cyanopindolol from human beta2 adrenoceptor expressed in CHO-K1 cell membrane measured after 1 hr by Cheng-prusoff equation analysisDisplacement of 125I-cyanopindolol from human beta2 adrenoceptor expressed in CHO-K1 cell membrane measured after 1 hr by Cheng-prusoff equation analysis
ChEMBL 760 16 5 10 6.0 O=C(N[C@H](c1ccccc1)c1cccc(OCc2ccc(C(=O)OCCCCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
CHEMBL5184598 190258 0 None 15 2 Human 10.3 pKi = 10.3 Binding
Displacement of 125I-cyanopindolol from human beta2 adrenoceptor expressed in CHO-K1 cell membrane measured after 1 hr by Cheng-prusoff equation analysisDisplacement of 125I-cyanopindolol from human beta2 adrenoceptor expressed in CHO-K1 cell membrane measured after 1 hr by Cheng-prusoff equation analysis
ChEMBL 760 16 5 10 6.0 O=C(N[C@H](c1ccccc1)c1cccc(OCc2ccc(C(=O)OCCCCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
168296356 191877 0 None 3 2 Human 10.3 pKi = 10.3 Binding
Displacement of 125I-cyanopindolol from human beta2 adrenoceptor expressed in CHO-K1 cell membrane measured after 1 hr by Cheng-prusoff equation analysisDisplacement of 125I-cyanopindolol from human beta2 adrenoceptor expressed in CHO-K1 cell membrane measured after 1 hr by Cheng-prusoff equation analysis
ChEMBL 751 16 5 12 5.0 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2nc(C(=O)OCCCCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)co2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
CHEMBL5208957 191877 0 None 3 2 Human 10.3 pKi = 10.3 Binding
Displacement of 125I-cyanopindolol from human beta2 adrenoceptor expressed in CHO-K1 cell membrane measured after 1 hr by Cheng-prusoff equation analysisDisplacement of 125I-cyanopindolol from human beta2 adrenoceptor expressed in CHO-K1 cell membrane measured after 1 hr by Cheng-prusoff equation analysis
ChEMBL 751 16 5 12 5.0 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2nc(C(=O)OCCCCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)co2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
155525244 170418 0 None 15 2 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranesDisplacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranes
ChEMBL 516 17 3 8 4.5 COc1cc(CCNC[C@H](O)COc2cccc3ccccc23)ccc1OCCCSSCCN 10.1016/j.bmc.2019.05.034
CHEMBL4456301 170418 0 None 15 2 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranesDisplacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranes
ChEMBL 516 17 3 8 4.5 COc1cc(CCNC[C@H](O)COc2cccc3ccccc23)ccc1OCCCSSCCN 10.1016/j.bmc.2019.05.034
164616287 184403 0 None 3 2 Human 10.0 pKi = 10 Binding
Displacement of 125I-cyanopindolol from human adrenergic beta2 receptorDisplacement of 125I-cyanopindolol from human adrenergic beta2 receptor
ChEMBL 668 16 5 8 5.8 O=C(NC(c1ccccc1)c1cccc(OCCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)c1)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2021.127975
CHEMBL4854418 184403 0 None 3 2 Human 10.0 pKi = 10 Binding
Displacement of 125I-cyanopindolol from human adrenergic beta2 receptorDisplacement of 125I-cyanopindolol from human adrenergic beta2 receptor
ChEMBL 668 16 5 8 5.8 O=C(NC(c1ccccc1)c1cccc(OCCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)c1)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2021.127975
164622948 185512 0 None 1 2 Human 10.0 pKi = 10 Binding
Displacement of 125I-cyanopindolol from human adrenergic beta2 receptorDisplacement of 125I-cyanopindolol from human adrenergic beta2 receptor
ChEMBL 911 18 5 9 8.7 O=C(N[C@@H](c1ccccc1)c1ccc(-c2cccc(OCc3ccc(C(=O)N(CCCNC[C@H](O)c4ccc(O)c5[nH]c(=O)ccc45)Cc4ccccc4)cc3)c2)cc1)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2021.127975
CHEMBL4871702 185512 0 None 1 2 Human 10.0 pKi = 10 Binding
Displacement of 125I-cyanopindolol from human adrenergic beta2 receptorDisplacement of 125I-cyanopindolol from human adrenergic beta2 receptor
ChEMBL 911 18 5 9 8.7 O=C(N[C@@H](c1ccccc1)c1ccc(-c2cccc(OCc3ccc(C(=O)N(CCCNC[C@H](O)c4ccc(O)c5[nH]c(=O)ccc45)Cc4ccccc4)cc3)c2)cc1)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2021.127975
46889812 6363 0 None 10 3 Human 10.0 pKi = 10 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cells
ChEMBL 415 7 2 4 4.4 OC(COc1cccc2[nH]c3ccccc3c12)CN1CCC(Cc2cccnc2)CC1 10.1016/j.bmcl.2010.04.009
CHEMBL1082501 6363 0 None 10 3 Human 10.0 pKi = 10 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cells
ChEMBL 415 7 2 4 4.4 OC(COc1cccc2[nH]c3ccccc3c12)CN1CCC(Cc2cccnc2)CC1 10.1016/j.bmcl.2010.04.009
6603756 122376 3 None 2 2 Human 10.0 pKi = 10 Binding
Inhibition of I-iodocyanopindolol binding to human beta 2 adrenergic receptorsInhibition of I-iodocyanopindolol binding to human beta 2 adrenergic receptors
ChEMBL 279 5 4 5 1.4 CC(C)(C)NC[C@H](O)COc1cccc2[nH]c(O)nc12 10.1021/jm000544b
CHEMBL36060 122376 3 None 2 2 Human 10.0 pKi = 10 Binding
Inhibition of I-iodocyanopindolol binding to human beta 2 adrenergic receptorsInhibition of I-iodocyanopindolol binding to human beta 2 adrenergic receptors
ChEMBL 279 5 4 5 1.4 CC(C)(C)NC[C@H](O)COc1cccc2[nH]c(O)nc12 10.1021/jm000544b
487 779 65 None 4 6 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]DHA from human beta2 adrenoceptor by liquid scintillation counterDisplacement of [3H]DHA from human beta2 adrenoceptor by liquid scintillation counter
ChEMBL 298 6 3 3 3.1 OC(COc1cccc2c1c1ccccc1[nH]2)CNC(C)C 10.1016/j.bmcl.2008.09.046
569 779 65 None 4 6 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]DHA from human beta2 adrenoceptor by liquid scintillation counterDisplacement of [3H]DHA from human beta2 adrenoceptor by liquid scintillation counter
ChEMBL 298 6 3 3 3.1 OC(COc1cccc2c1c1ccccc1[nH]2)CNC(C)C 10.1016/j.bmcl.2008.09.046
71739 779 65 None 4 6 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]DHA from human beta2 adrenoceptor by liquid scintillation counterDisplacement of [3H]DHA from human beta2 adrenoceptor by liquid scintillation counter
ChEMBL 298 6 3 3 3.1 OC(COc1cccc2c1c1ccccc1[nH]2)CNC(C)C 10.1016/j.bmcl.2008.09.046
CHEMBL324665 779 65 None 4 6 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]DHA from human beta2 adrenoceptor by liquid scintillation counterDisplacement of [3H]DHA from human beta2 adrenoceptor by liquid scintillation counter
ChEMBL 298 6 3 3 3.1 OC(COc1cccc2c1c1ccccc1[nH]2)CNC(C)C 10.1016/j.bmcl.2008.09.046
3682 188837 7 None 1 8 Human 9.9 pKi = 9.9 Binding
Displacement of [3H](-)-CGP12177 from human adrenergic beta2 receptorDisplacement of [3H](-)-CGP12177 from human adrenergic beta2 receptor
ChEMBL 277 6 2 3 2.6 Cc1ccc(OCC(O)C(C)NC(C)C)c2c1CCC2 10.1021/jm2006782
CHEMBL1256784 188837 7 None 1 8 Human 9.9 pKi = 9.9 Binding
Displacement of [3H](-)-CGP12177 from human adrenergic beta2 receptorDisplacement of [3H](-)-CGP12177 from human adrenergic beta2 receptor
ChEMBL 277 6 2 3 2.6 Cc1ccc(OCC(O)C(C)NC(C)C)c2c1CCC2 10.1021/jm2006782
CHEMBL513389 188837 7 None 1 8 Human 9.9 pKi = 9.9 Binding
Displacement of [3H](-)-CGP12177 from human adrenergic beta2 receptorDisplacement of [3H](-)-CGP12177 from human adrenergic beta2 receptor
ChEMBL 277 6 2 3 2.6 Cc1ccc(OCC(O)C(C)NC(C)C)c2c1CCC2 10.1021/jm2006782
23968266 188807 0 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]DHA from human beta2 adrenoceptor by liquid scintillation counterDisplacement of [3H]DHA from human beta2 adrenoceptor by liquid scintillation counter
ChEMBL 313 5 2 4 3.7 CC(C)(C)NCC(O)COc1cccc2oc3ccccc3c12 10.1016/j.bmcl.2008.09.046
CHEMBL513104 188807 0 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]DHA from human beta2 adrenoceptor by liquid scintillation counterDisplacement of [3H]DHA from human beta2 adrenoceptor by liquid scintillation counter
ChEMBL 313 5 2 4 3.7 CC(C)(C)NCC(O)COc1cccc2oc3ccccc3c12 10.1016/j.bmcl.2008.09.046
164627100 185967 0 None 25 2 Human 9.8 pKi = 9.8 Binding
Displacement of 125I-cyanopindolol from human adrenergic beta2 receptorDisplacement of 125I-cyanopindolol from human adrenergic beta2 receptor
ChEMBL 739 13 6 9 5.8 COc1cc(C(=O)NCCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.bmcl.2021.127975
CHEMBL4878138 185967 0 None 25 2 Human 9.8 pKi = 9.8 Binding
Displacement of 125I-cyanopindolol from human adrenergic beta2 receptorDisplacement of 125I-cyanopindolol from human adrenergic beta2 receptor
ChEMBL 739 13 6 9 5.8 COc1cc(C(=O)NCCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.bmcl.2021.127975
3682 188837 7 None 1 8 Human 9.8 pKi = 9.8 Binding
Binding affinity to human adrenergic beta2 receptor by radioligand displacement assayBinding affinity to human adrenergic beta2 receptor by radioligand displacement assay
ChEMBL 277 6 2 3 2.6 Cc1ccc(OCC(O)C(C)NC(C)C)c2c1CCC2 10.1016/j.ejmech.2013.01.044
CHEMBL1256784 188837 7 None 1 8 Human 9.8 pKi = 9.8 Binding
Binding affinity to human adrenergic beta2 receptor by radioligand displacement assayBinding affinity to human adrenergic beta2 receptor by radioligand displacement assay
ChEMBL 277 6 2 3 2.6 Cc1ccc(OCC(O)C(C)NC(C)C)c2c1CCC2 10.1016/j.ejmech.2013.01.044
CHEMBL513389 188837 7 None 1 8 Human 9.8 pKi = 9.8 Binding
Binding affinity to human adrenergic beta2 receptor by radioligand displacement assayBinding affinity to human adrenergic beta2 receptor by radioligand displacement assay
ChEMBL 277 6 2 3 2.6 Cc1ccc(OCC(O)C(C)NC(C)C)c2c1CCC2 10.1016/j.ejmech.2013.01.044
155548437 173189 0 None 3 2 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranesDisplacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranes
ChEMBL 502 16 3 8 4.1 COc1cc(CCNC[C@H](O)COc2cccc3ccccc23)ccc1OCCSSCCN 10.1016/j.bmc.2019.05.034
CHEMBL4537221 173189 0 None 3 2 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranesDisplacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranes
ChEMBL 502 16 3 8 4.1 COc1cc(CCNC[C@H](O)COc2cccc3ccccc23)ccc1OCCSSCCN 10.1016/j.bmc.2019.05.034
2585 788 100 None 1 22 Human 9.8 pKi = 9.8 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
522 788 100 None 1 22 Human 9.8 pKi = 9.8 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
551 788 100 None 1 22 Human 9.8 pKi = 9.8 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
CHEMBL723 788 100 None 1 22 Human 9.8 pKi = 9.8 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
DB01136 788 100 None 1 22 Human 9.8 pKi = 9.8 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
2419 3394 80 None 16 6 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cellsDisplacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmc.2016.04.028
5152 3394 80 None 16 6 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cellsDisplacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmc.2016.04.028
559 3394 80 None 16 6 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cellsDisplacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmc.2016.04.028
CHEMBL1263 3394 80 None 16 6 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cellsDisplacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmc.2016.04.028
DB00938 3394 80 None 16 6 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cellsDisplacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmc.2016.04.028
71113213 183857 0 None 1 2 Human 9.7 pKi = 9.7 Binding
Displacement of 125I-cyanopindolol from human adrenergic beta2 receptorDisplacement of 125I-cyanopindolol from human adrenergic beta2 receptor
ChEMBL 696 18 5 8 6.6 O=C(NC(c1ccccc1)c1cccc(OCCCCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)c1)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2021.127975
CHEMBL4846536 183857 0 None 1 2 Human 9.7 pKi = 9.7 Binding
Displacement of 125I-cyanopindolol from human adrenergic beta2 receptorDisplacement of 125I-cyanopindolol from human adrenergic beta2 receptor
ChEMBL 696 18 5 8 6.6 O=C(NC(c1ccccc1)c1cccc(OCCCCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)c1)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2021.127975
164617389 184278 0 None -1 2 Human 9.7 pKi = 9.7 Binding
Displacement of 125I-cyanopindolol from human adrenergic beta2 receptorDisplacement of 125I-cyanopindolol from human adrenergic beta2 receptor
ChEMBL 682 17 5 8 6.2 O=C(NC(c1ccccc1)c1cccc(OCCCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)c1)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2021.127975
CHEMBL4852629 184278 0 None -1 2 Human 9.7 pKi = 9.7 Binding
Displacement of 125I-cyanopindolol from human adrenergic beta2 receptorDisplacement of 125I-cyanopindolol from human adrenergic beta2 receptor
ChEMBL 682 17 5 8 6.2 O=C(NC(c1ccccc1)c1cccc(OCCCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)c1)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2021.127975
46889811 6362 0 None 16 3 Human 9.7 pKi = 9.7 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cells
ChEMBL 444 8 2 4 5.0 COc1ccc(CC2CCN(CC(O)COc3cccc4[nH]c5ccccc5c34)CC2)cc1 10.1016/j.bmcl.2010.04.009
CHEMBL1082500 6362 0 None 16 3 Human 9.7 pKi = 9.7 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cells
ChEMBL 444 8 2 4 5.0 COc1ccc(CC2CCN(CC(O)COc3cccc4[nH]c5ccccc5c34)CC2)cc1 10.1016/j.bmcl.2010.04.009
46889852 6439 0 None 79 3 Human 9.7 pKi = 9.7 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cells
ChEMBL 428 7 2 4 4.7 O=C(c1ccccc1)C1CCN(CC(O)COc2cccc3[nH]c4ccccc4c23)CC1 10.1016/j.bmcl.2010.04.009
CHEMBL1082827 6439 0 None 79 3 Human 9.7 pKi = 9.7 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cells
ChEMBL 428 7 2 4 4.7 O=C(c1ccccc1)C1CCN(CC(O)COc2cccc3[nH]c4ccccc4c23)CC1 10.1016/j.bmcl.2010.04.009
46889853 6440 0 None 64 3 Human 9.7 pKi = 9.7 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cells
ChEMBL 458 8 2 5 4.7 COc1ccc(C(=O)C2CCN(CC(O)COc3cccc4[nH]c5ccccc5c34)CC2)cc1 10.1016/j.bmcl.2010.04.009
CHEMBL1082828 6440 0 None 64 3 Human 9.7 pKi = 9.7 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cells
ChEMBL 458 8 2 5 4.7 COc1ccc(C(=O)C2CCN(CC(O)COc3cccc4[nH]c5ccccc5c34)CC2)cc1 10.1016/j.bmcl.2010.04.009
33624 3749 29 None 1 9 Human 9.7 pKi = 9.7 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C nan
4061 3749 29 None 1 9 Human 9.7 pKi = 9.7 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C nan
565 3749 29 None 1 9 Human 9.7 pKi = 9.7 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C nan
CHEMBL499 3749 29 None 1 9 Human 9.7 pKi = 9.7 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C nan
DB00373 3749 29 None 1 9 Human 9.7 pKi = 9.7 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C nan
33624 3749 29 None 1 9 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]-CGP12177 from human beta2 ADR expressed in HEK293T cell membrane after 90 mins by scintillation countingDisplacement of [3H]-CGP12177 from human beta2 ADR expressed in HEK293T cell membrane after 90 mins by scintillation counting
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C 10.1021/acs.jmedchem.8b00625
4061 3749 29 None 1 9 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]-CGP12177 from human beta2 ADR expressed in HEK293T cell membrane after 90 mins by scintillation countingDisplacement of [3H]-CGP12177 from human beta2 ADR expressed in HEK293T cell membrane after 90 mins by scintillation counting
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C 10.1021/acs.jmedchem.8b00625
565 3749 29 None 1 9 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]-CGP12177 from human beta2 ADR expressed in HEK293T cell membrane after 90 mins by scintillation countingDisplacement of [3H]-CGP12177 from human beta2 ADR expressed in HEK293T cell membrane after 90 mins by scintillation counting
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C 10.1021/acs.jmedchem.8b00625
CHEMBL499 3749 29 None 1 9 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]-CGP12177 from human beta2 ADR expressed in HEK293T cell membrane after 90 mins by scintillation countingDisplacement of [3H]-CGP12177 from human beta2 ADR expressed in HEK293T cell membrane after 90 mins by scintillation counting
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C 10.1021/acs.jmedchem.8b00625
DB00373 3749 29 None 1 9 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]-CGP12177 from human beta2 ADR expressed in HEK293T cell membrane after 90 mins by scintillation countingDisplacement of [3H]-CGP12177 from human beta2 ADR expressed in HEK293T cell membrane after 90 mins by scintillation counting
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C 10.1021/acs.jmedchem.8b00625
165193 3126 60 None 1 43 Human 9.6 pKi = 9.6 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
2303 3126 60 None 1 43 Human 9.6 pKi = 9.6 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
4946 3126 60 None 1 43 Human 9.6 pKi = 9.6 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
564 3126 60 None 1 43 Human 9.6 pKi = 9.6 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
62882 3126 60 None 1 43 Human 9.6 pKi = 9.6 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
63 3126 60 None 1 43 Human 9.6 pKi = 9.6 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
66366 3126 60 None 1 43 Human 9.6 pKi = 9.6 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
91536 3126 60 None 1 43 Human 9.6 pKi = 9.6 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
CHEMBL27 3126 60 None 1 43 Human 9.6 pKi = 9.6 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
CHEMBL452861 3126 60 None 1 43 Human 9.6 pKi = 9.6 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
DB00571 3126 60 None 1 43 Human 9.6 pKi = 9.6 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
2419 3394 80 None 16 6 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/acs.jmedchem.9b00349
5152 3394 80 None 16 6 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/acs.jmedchem.9b00349
559 3394 80 None 16 6 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/acs.jmedchem.9b00349
CHEMBL1263 3394 80 None 16 6 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/acs.jmedchem.9b00349
DB00938 3394 80 None 16 6 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/acs.jmedchem.9b00349
127045853 139250 0 None 20 6 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cellsDisplacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells
ChEMBL 492 12 4 7 3.6 COc1cc(CCNC[C@H](O)c2ccc(O)c3c2OCC(=O)N3)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
CHEMBL3798748 139250 0 None 20 6 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cellsDisplacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells
ChEMBL 492 12 4 7 3.6 COc1cc(CCNC[C@H](O)c2ccc(O)c3c2OCC(=O)N3)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
164615119 184380 0 None -1 2 Human 9.6 pKi = 9.6 Binding
Displacement of 125I-cyanopindolol from human adrenergic beta2 receptorDisplacement of 125I-cyanopindolol from human adrenergic beta2 receptor
ChEMBL 688 13 5 8 5.6 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)c1)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2021.127975
CHEMBL4854091 184380 0 None -1 2 Human 9.6 pKi = 9.6 Binding
Displacement of 125I-cyanopindolol from human adrenergic beta2 receptorDisplacement of 125I-cyanopindolol from human adrenergic beta2 receptor
ChEMBL 688 13 5 8 5.6 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)c1)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2021.127975
71113107 185988 0 None 39 2 Human 9.6 pKi = 9.6 Binding
Displacement of 125I-cyanopindolol from human adrenergic beta2 receptorDisplacement of 125I-cyanopindolol from human adrenergic beta2 receptor
ChEMBL 696 18 5 8 6.6 O=C(NC(c1ccccc1)c1ccc(OCCCCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2021.127975
CHEMBL4878395 185988 0 None 39 2 Human 9.6 pKi = 9.6 Binding
Displacement of 125I-cyanopindolol from human adrenergic beta2 receptorDisplacement of 125I-cyanopindolol from human adrenergic beta2 receptor
ChEMBL 696 18 5 8 6.6 O=C(NC(c1ccccc1)c1ccc(OCCCCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2021.127975
164615119 184380 0 None -1 2 Human 9.6 pKi = 9.6 Binding
Displacement of 125I-cyanopindolol from human beta2 adrenoceptor expressed in CHO-K1 cell membrane measured after 1 hr by Cheng-prusoff equation analysisDisplacement of 125I-cyanopindolol from human beta2 adrenoceptor expressed in CHO-K1 cell membrane measured after 1 hr by Cheng-prusoff equation analysis
ChEMBL 688 13 5 8 5.6 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
CHEMBL4854091 184380 0 None -1 2 Human 9.6 pKi = 9.6 Binding
Displacement of 125I-cyanopindolol from human beta2 adrenoceptor expressed in CHO-K1 cell membrane measured after 1 hr by Cheng-prusoff equation analysisDisplacement of 125I-cyanopindolol from human beta2 adrenoceptor expressed in CHO-K1 cell membrane measured after 1 hr by Cheng-prusoff equation analysis
ChEMBL 688 13 5 8 5.6 O=C(N[C@@H](c1ccccc1)c1cccc(OCc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)c1)O[C@H]1CN2CCC1CC2 10.1021/acs.jmedchem.2c00609
46889854 7212 0 None 104 3 Human 9.5 pKi = 9.5 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cells
ChEMBL 446 7 2 4 4.8 O=C(c1ccc(F)cc1)C1CCN(CC(O)COc2cccc3[nH]c4ccccc4c23)CC1 10.1016/j.bmcl.2010.04.009
CHEMBL1086077 7212 0 None 104 3 Human 9.5 pKi = 9.5 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cells
ChEMBL 446 7 2 4 4.8 O=C(c1ccc(F)cc1)C1CCN(CC(O)COc2cccc3[nH]c4ccccc4c23)CC1 10.1016/j.bmcl.2010.04.009
49864442 15459 0 None 27 2 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptorDisplacement of [3H]CGP12177 from human beta2 adrenoceptor
ChEMBL 373 8 4 6 2.4 CN(CCCNC[C@H](O)c1ccc(O)c2[nH]c(=O)sc12)c1ccccc1 10.1016/j.bmcl.2010.06.136
CHEMBL1221804 15459 0 None 27 2 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptorDisplacement of [3H]CGP12177 from human beta2 adrenoceptor
ChEMBL 373 8 4 6 2.4 CN(CCCNC[C@H](O)c1ccc(O)c2[nH]c(=O)sc12)c1ccccc1 10.1016/j.bmcl.2010.06.136
3858663 176284 9 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of radioligand from human adrenergic beta2 receptorDisplacement of radioligand from human adrenergic beta2 receptor
ChEMBL 455 8 2 4 4.6 Cc1c[nH]c2cccc(OCC(O)CN3CCN(C(c4ccccc4)c4ccccc4)CC3)c12 10.1021/jm200371q
CHEMBL461463 176284 9 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of radioligand from human adrenergic beta2 receptorDisplacement of radioligand from human adrenergic beta2 receptor
ChEMBL 455 8 2 4 4.6 Cc1c[nH]c2cccc(OCC(O)CN3CCN(C(c4ccccc4)c4ccccc4)CC3)c12 10.1021/jm200371q
10051943 16134 0 None 588 3 Human 9.5 pKi = 9.5 Binding
Binding affinity for human Beta-2 adrenergic receptor expressed in CHO cells by radioligand competition binding assays using [125I]iodocyanopindolol (ICYP)Binding affinity for human Beta-2 adrenergic receptor expressed in CHO cells by radioligand competition binding assays using [125I]iodocyanopindolol (ICYP)
ChEMBL 507 2 3 3 3.7 Oc1cc2c(cc1O)C(Cc1cc(I)cc(I)c1)NCC2 10.1021/jm960208o
CHEMBL122757 16134 0 None 588 3 Human 9.5 pKi = 9.5 Binding
Binding affinity for human Beta-2 adrenergic receptor expressed in CHO cells by radioligand competition binding assays using [125I]iodocyanopindolol (ICYP)Binding affinity for human Beta-2 adrenergic receptor expressed in CHO cells by radioligand competition binding assays using [125I]iodocyanopindolol (ICYP)
ChEMBL 507 2 3 3 3.7 Oc1cc2c(cc1O)C(Cc1cc(I)cc(I)c1)NCC2 10.1021/jm960208o
3858663 176284 9 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]DHA from human beta2 adrenoceptor by liquid scintillation counterDisplacement of [3H]DHA from human beta2 adrenoceptor by liquid scintillation counter
ChEMBL 455 8 2 4 4.6 Cc1c[nH]c2cccc(OCC(O)CN3CCN(C(c4ccccc4)c4ccccc4)CC3)c12 10.1016/j.bmcl.2008.09.046
CHEMBL461463 176284 9 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]DHA from human beta2 adrenoceptor by liquid scintillation counterDisplacement of [3H]DHA from human beta2 adrenoceptor by liquid scintillation counter
ChEMBL 455 8 2 4 4.6 Cc1c[nH]c2cccc(OCC(O)CN3CCN(C(c4ccccc4)c4ccccc4)CC3)c12 10.1016/j.bmcl.2008.09.046
165193 3126 60 None 1 43 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranesDisplacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranes
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmc.2019.05.034
2303 3126 60 None 1 43 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranesDisplacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranes
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmc.2019.05.034
4946 3126 60 None 1 43 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranesDisplacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranes
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmc.2019.05.034
564 3126 60 None 1 43 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranesDisplacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranes
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmc.2019.05.034
62882 3126 60 None 1 43 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranesDisplacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranes
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmc.2019.05.034
63 3126 60 None 1 43 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranesDisplacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranes
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmc.2019.05.034
66366 3126 60 None 1 43 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranesDisplacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranes
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmc.2019.05.034
91536 3126 60 None 1 43 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranesDisplacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranes
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmc.2019.05.034
CHEMBL27 3126 60 None 1 43 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranesDisplacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranes
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmc.2019.05.034
CHEMBL452861 3126 60 None 1 43 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranesDisplacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranes
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmc.2019.05.034
DB00571 3126 60 None 1 43 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranesDisplacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranes
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmc.2019.05.034
2176 3065 66 None -2 27 Human 9.4 pKi = 9.4 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C nan
4828 3065 66 None -2 27 Human 9.4 pKi = 9.4 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C nan
91 3065 66 None -2 27 Human 9.4 pKi = 9.4 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C nan
CHEMBL500 3065 66 None -2 27 Human 9.4 pKi = 9.4 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C nan
DB00960 3065 66 None -2 27 Human 9.4 pKi = 9.4 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C nan
155559960 174312 0 None 10 2 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysisDisplacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysis
ChEMBL 586 22 6 7 3.8 CC(C)NC[C@H](O)COc1ccccc1CCCCNC(=O)NCCCCc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
CHEMBL4564189 174312 0 None 10 2 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysisDisplacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysis
ChEMBL 586 22 6 7 3.8 CC(C)NC[C@H](O)COc1ccccc1CCCCNC(=O)NCCCCc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
2419 3394 80 None 16 6 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]cyanopindolol from human recombinant beta2 adrenergic receptor expressed in CHO cells by filtration assayDisplacement of [125I]cyanopindolol from human recombinant beta2 adrenergic receptor expressed in CHO cells by filtration assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/jm100068m
5152 3394 80 None 16 6 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]cyanopindolol from human recombinant beta2 adrenergic receptor expressed in CHO cells by filtration assayDisplacement of [125I]cyanopindolol from human recombinant beta2 adrenergic receptor expressed in CHO cells by filtration assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/jm100068m
559 3394 80 None 16 6 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]cyanopindolol from human recombinant beta2 adrenergic receptor expressed in CHO cells by filtration assayDisplacement of [125I]cyanopindolol from human recombinant beta2 adrenergic receptor expressed in CHO cells by filtration assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/jm100068m
CHEMBL1263 3394 80 None 16 6 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]cyanopindolol from human recombinant beta2 adrenergic receptor expressed in CHO cells by filtration assayDisplacement of [125I]cyanopindolol from human recombinant beta2 adrenergic receptor expressed in CHO cells by filtration assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/jm100068m
DB00938 3394 80 None 16 6 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]cyanopindolol from human recombinant beta2 adrenergic receptor expressed in CHO cells by filtration assayDisplacement of [125I]cyanopindolol from human recombinant beta2 adrenergic receptor expressed in CHO cells by filtration assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/jm100068m
2176 3065 66 None -2 27 Human 9.4 pKi = 9.4 Binding
Binding affinity at human adrenergic beta2 receptorBinding affinity at human adrenergic beta2 receptor
ChEMBL 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C 10.1016/j.bmcl.2007.07.086
4828 3065 66 None -2 27 Human 9.4 pKi = 9.4 Binding
Binding affinity at human adrenergic beta2 receptorBinding affinity at human adrenergic beta2 receptor
ChEMBL 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C 10.1016/j.bmcl.2007.07.086
91 3065 66 None -2 27 Human 9.4 pKi = 9.4 Binding
Binding affinity at human adrenergic beta2 receptorBinding affinity at human adrenergic beta2 receptor
ChEMBL 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C 10.1016/j.bmcl.2007.07.086
CHEMBL500 3065 66 None -2 27 Human 9.4 pKi = 9.4 Binding
Binding affinity at human adrenergic beta2 receptorBinding affinity at human adrenergic beta2 receptor
ChEMBL 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C 10.1016/j.bmcl.2007.07.086
DB00960 3065 66 None -2 27 Human 9.4 pKi = 9.4 Binding
Binding affinity at human adrenergic beta2 receptorBinding affinity at human adrenergic beta2 receptor
ChEMBL 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C 10.1016/j.bmcl.2007.07.086
118710940 113238 0 None 1 3 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assay
ChEMBL 398 7 4 5 3.7 O=c1[nH]c2c(O)ccc([C@@H](O)CN[C@@H]3CCC[C@@H]3CCc3ccccc3)c2s1 10.1016/j.bmcl.2014.06.014
CHEMBL3323658 113238 0 None 1 3 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assay
ChEMBL 398 7 4 5 3.7 O=c1[nH]c2c(O)ccc([C@@H](O)CN[C@@H]3CCC[C@@H]3CCc3ccccc3)c2s1 10.1016/j.bmcl.2014.06.014
11617407 15433 0 None 4 2 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptorDisplacement of [3H]CGP12177 from human beta2 adrenoceptor
ChEMBL 358 6 4 5 2.9 CC(C)(Cc1ccccc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)sc12 10.1016/j.bmcl.2010.06.136
CHEMBL1221590 15433 0 None 4 2 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptorDisplacement of [3H]CGP12177 from human beta2 adrenoceptor
ChEMBL 358 6 4 5 2.9 CC(C)(Cc1ccccc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)sc12 10.1016/j.bmcl.2010.06.136
155539613 172268 0 None 2 2 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysisDisplacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysis
ChEMBL 677 24 5 13 2.9 CC(C)NC[C@H](O)COc1ccccc1CCCn1cc(CNCc2cn(CCCc3ccccc3OC[C@@H](O)CNC(C)C)nn2)nn1 10.1021/acs.jmedchem.9b00595
CHEMBL4514723 172268 0 None 2 2 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysisDisplacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysis
ChEMBL 677 24 5 13 2.9 CC(C)NC[C@H](O)COc1ccccc1CCCn1cc(CNCc2cn(CCCc3ccccc3OC[C@@H](O)CNC(C)C)nn2)nn1 10.1021/acs.jmedchem.9b00595
165193 3126 60 None 1 43 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]-CGP-12177 from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-CGP-12177 from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmc.2013.11.030
2303 3126 60 None 1 43 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]-CGP-12177 from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-CGP-12177 from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmc.2013.11.030
4946 3126 60 None 1 43 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]-CGP-12177 from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-CGP-12177 from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmc.2013.11.030
564 3126 60 None 1 43 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]-CGP-12177 from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-CGP-12177 from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmc.2013.11.030
62882 3126 60 None 1 43 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]-CGP-12177 from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-CGP-12177 from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmc.2013.11.030
63 3126 60 None 1 43 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]-CGP-12177 from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-CGP-12177 from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmc.2013.11.030
66366 3126 60 None 1 43 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]-CGP-12177 from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-CGP-12177 from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmc.2013.11.030
91536 3126 60 None 1 43 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]-CGP-12177 from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-CGP-12177 from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmc.2013.11.030
CHEMBL27 3126 60 None 1 43 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]-CGP-12177 from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-CGP-12177 from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmc.2013.11.030
CHEMBL452861 3126 60 None 1 43 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]-CGP-12177 from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-CGP-12177 from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmc.2013.11.030
DB00571 3126 60 None 1 43 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]-CGP-12177 from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-CGP-12177 from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmc.2013.11.030
102262219 139516 0 None 12 6 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cellsDisplacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells
ChEMBL 488 12 4 6 4.1 COc1cc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
CHEMBL3800400 139516 0 None 12 6 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cellsDisplacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells
ChEMBL 488 12 4 6 4.1 COc1cc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
46889810 7320 0 None 28 3 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cells
ChEMBL 414 7 2 3 5.0 OC(COc1cccc2[nH]c3ccccc3c12)CN1CCC(Cc2ccccc2)CC1 10.1016/j.bmcl.2010.04.009
CHEMBL1086542 7320 0 None 28 3 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cells
ChEMBL 414 7 2 3 5.0 OC(COc1cccc2[nH]c3ccccc3c12)CN1CCC(Cc2ccccc2)CC1 10.1016/j.bmcl.2010.04.009
137 367 47 None -3 12 Human 9.3 pKi = 9.3 Binding
Displacement of [3H](-)CGP 12177 from human recombinant beta2 adrenoceptor after 120 mins by scintillation counting methodDisplacement of [3H](-)CGP 12177 from human recombinant beta2 adrenoceptor after 120 mins by scintillation counting method
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1039/C8MD00412A
2119 367 47 None -3 12 Human 9.3 pKi = 9.3 Binding
Displacement of [3H](-)CGP 12177 from human recombinant beta2 adrenoceptor after 120 mins by scintillation counting methodDisplacement of [3H](-)CGP 12177 from human recombinant beta2 adrenoceptor after 120 mins by scintillation counting method
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1039/C8MD00412A
563 367 47 None -3 12 Human 9.3 pKi = 9.3 Binding
Displacement of [3H](-)CGP 12177 from human recombinant beta2 adrenoceptor after 120 mins by scintillation counting methodDisplacement of [3H](-)CGP 12177 from human recombinant beta2 adrenoceptor after 120 mins by scintillation counting method
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1039/C8MD00412A
66368 367 47 None -3 12 Human 9.3 pKi = 9.3 Binding
Displacement of [3H](-)CGP 12177 from human recombinant beta2 adrenoceptor after 120 mins by scintillation counting methodDisplacement of [3H](-)CGP 12177 from human recombinant beta2 adrenoceptor after 120 mins by scintillation counting method
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1039/C8MD00412A
CHEMBL266195 367 47 None -3 12 Human 9.3 pKi = 9.3 Binding
Displacement of [3H](-)CGP 12177 from human recombinant beta2 adrenoceptor after 120 mins by scintillation counting methodDisplacement of [3H](-)CGP 12177 from human recombinant beta2 adrenoceptor after 120 mins by scintillation counting method
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1039/C8MD00412A
DB00866 367 47 None -3 12 Human 9.3 pKi = 9.3 Binding
Displacement of [3H](-)CGP 12177 from human recombinant beta2 adrenoceptor after 120 mins by scintillation counting methodDisplacement of [3H](-)CGP 12177 from human recombinant beta2 adrenoceptor after 120 mins by scintillation counting method
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1039/C8MD00412A
49864395 15446 0 None 1 2 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptorDisplacement of [3H]CGP12177 from human beta2 adrenoceptor
ChEMBL 400 7 4 6 3.1 O=c1[nH]c2c(O)ccc([C@@H](O)CN[C@@H]3CCC[C@H]3OCc3ccccc3)c2s1 10.1016/j.bmcl.2010.06.136
CHEMBL1221680 15446 0 None 1 2 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptorDisplacement of [3H]CGP12177 from human beta2 adrenoceptor
ChEMBL 400 7 4 6 3.1 O=c1[nH]c2c(O)ccc([C@@H](O)CN[C@@H]3CCC[C@H]3OCc3ccccc3)c2s1 10.1016/j.bmcl.2010.06.136
3682 188837 7 None 1 8 Human 9.3 pKi = 9.3 Binding
Displacement of radiolabeled ICI 118551 from human adrenergic beta2 receptorDisplacement of radiolabeled ICI 118551 from human adrenergic beta2 receptor
ChEMBL 277 6 2 3 2.6 Cc1ccc(OCC(O)C(C)NC(C)C)c2c1CCC2 10.1021/jm8007618
CHEMBL1256784 188837 7 None 1 8 Human 9.3 pKi = 9.3 Binding
Displacement of radiolabeled ICI 118551 from human adrenergic beta2 receptorDisplacement of radiolabeled ICI 118551 from human adrenergic beta2 receptor
ChEMBL 277 6 2 3 2.6 Cc1ccc(OCC(O)C(C)NC(C)C)c2c1CCC2 10.1021/jm8007618
CHEMBL513389 188837 7 None 1 8 Human 9.3 pKi = 9.3 Binding
Displacement of radiolabeled ICI 118551 from human adrenergic beta2 receptorDisplacement of radiolabeled ICI 118551 from human adrenergic beta2 receptor
ChEMBL 277 6 2 3 2.6 Cc1ccc(OCC(O)C(C)NC(C)C)c2c1CCC2 10.1021/jm8007618
164613832 183946 0 None -3 2 Human 9.3 pKi = 9.3 Binding
Displacement of 125I-cyanopindolol from human adrenergic beta2 receptorDisplacement of 125I-cyanopindolol from human adrenergic beta2 receptor
ChEMBL 654 15 5 8 5.4 O=C(N[C@@H](c1ccccc1)c1cccc(OCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)c1)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2021.127975
CHEMBL4847910 183946 0 None -3 2 Human 9.3 pKi = 9.3 Binding
Displacement of 125I-cyanopindolol from human adrenergic beta2 receptorDisplacement of 125I-cyanopindolol from human adrenergic beta2 receptor
ChEMBL 654 15 5 8 5.4 O=C(N[C@@H](c1ccccc1)c1cccc(OCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)c1)O[C@H]1CN2CCC1CC2 10.1016/j.bmcl.2021.127975
165193 3126 60 None 1 43 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]CGP12177 from human recombinant beta2 adrenergic receptor expressed in CHO cells after 60 minsDisplacement of [3H]CGP12177 from human recombinant beta2 adrenergic receptor expressed in CHO cells after 60 mins
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmcl.2013.01.025
2303 3126 60 None 1 43 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]CGP12177 from human recombinant beta2 adrenergic receptor expressed in CHO cells after 60 minsDisplacement of [3H]CGP12177 from human recombinant beta2 adrenergic receptor expressed in CHO cells after 60 mins
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmcl.2013.01.025
4946 3126 60 None 1 43 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]CGP12177 from human recombinant beta2 adrenergic receptor expressed in CHO cells after 60 minsDisplacement of [3H]CGP12177 from human recombinant beta2 adrenergic receptor expressed in CHO cells after 60 mins
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmcl.2013.01.025
564 3126 60 None 1 43 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]CGP12177 from human recombinant beta2 adrenergic receptor expressed in CHO cells after 60 minsDisplacement of [3H]CGP12177 from human recombinant beta2 adrenergic receptor expressed in CHO cells after 60 mins
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmcl.2013.01.025
62882 3126 60 None 1 43 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]CGP12177 from human recombinant beta2 adrenergic receptor expressed in CHO cells after 60 minsDisplacement of [3H]CGP12177 from human recombinant beta2 adrenergic receptor expressed in CHO cells after 60 mins
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmcl.2013.01.025
63 3126 60 None 1 43 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]CGP12177 from human recombinant beta2 adrenergic receptor expressed in CHO cells after 60 minsDisplacement of [3H]CGP12177 from human recombinant beta2 adrenergic receptor expressed in CHO cells after 60 mins
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmcl.2013.01.025
66366 3126 60 None 1 43 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]CGP12177 from human recombinant beta2 adrenergic receptor expressed in CHO cells after 60 minsDisplacement of [3H]CGP12177 from human recombinant beta2 adrenergic receptor expressed in CHO cells after 60 mins
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmcl.2013.01.025
91536 3126 60 None 1 43 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]CGP12177 from human recombinant beta2 adrenergic receptor expressed in CHO cells after 60 minsDisplacement of [3H]CGP12177 from human recombinant beta2 adrenergic receptor expressed in CHO cells after 60 mins
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmcl.2013.01.025
CHEMBL27 3126 60 None 1 43 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]CGP12177 from human recombinant beta2 adrenergic receptor expressed in CHO cells after 60 minsDisplacement of [3H]CGP12177 from human recombinant beta2 adrenergic receptor expressed in CHO cells after 60 mins
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmcl.2013.01.025
CHEMBL452861 3126 60 None 1 43 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]CGP12177 from human recombinant beta2 adrenergic receptor expressed in CHO cells after 60 minsDisplacement of [3H]CGP12177 from human recombinant beta2 adrenergic receptor expressed in CHO cells after 60 mins
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmcl.2013.01.025
DB00571 3126 60 None 1 43 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]CGP12177 from human recombinant beta2 adrenergic receptor expressed in CHO cells after 60 minsDisplacement of [3H]CGP12177 from human recombinant beta2 adrenergic receptor expressed in CHO cells after 60 mins
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmcl.2013.01.025
39468 2270 33 None 3 7 Human 9.3 pKi = 9.3 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 291 5 2 4 2.3 O[C@H](COc1cccc2c1CCCC2=O)CNC(C)(C)C nan
431 2270 33 None 3 7 Human 9.3 pKi = 9.3 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 291 5 2 4 2.3 O[C@H](COc1cccc2c1CCCC2=O)CNC(C)(C)C nan
570 2270 33 None 3 7 Human 9.3 pKi = 9.3 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 291 5 2 4 2.3 O[C@H](COc1cccc2c1CCCC2=O)CNC(C)(C)C nan
CHEMBL1201237 2270 33 None 3 7 Human 9.3 pKi = 9.3 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 291 5 2 4 2.3 O[C@H](COc1cccc2c1CCCC2=O)CNC(C)(C)C nan
DB01210 2270 33 None 3 7 Human 9.3 pKi = 9.3 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 291 5 2 4 2.3 O[C@H](COc1cccc2c1CCCC2=O)CNC(C)(C)C nan
11625619 77251 0 None 4 2 Human 9.2 pKi = 9.2 Binding
Binding affinity to human beta2-adrenoceptor by radioligand binding assayBinding affinity to human beta2-adrenoceptor by radioligand binding assay
ChEMBL 406 6 4 4 3.5 CCc1cc2c(cc1CC)CC(C)(NC[C@H](O)c1ccc(O)c3[nH]c(=O)ccc13)C2 10.1016/j.bmcl.2012.07.096
CHEMBL2088201 77251 0 None 4 2 Human 9.2 pKi = 9.2 Binding
Binding affinity to human beta2-adrenoceptor by radioligand binding assayBinding affinity to human beta2-adrenoceptor by radioligand binding assay
ChEMBL 406 6 4 4 3.5 CCc1cc2c(cc1CC)CC(C)(NC[C@H](O)c1ccc(O)c3[nH]c(=O)ccc13)C2 10.1016/j.bmcl.2012.07.096
118710936 113234 0 None 29 3 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assay
ChEMBL 362 5 4 5 3.3 O=c1[nH]c2c(O)ccc([C@@H](O)CN[C@H]3CCC[C@@H]3C3CCCC3)c2s1 10.1016/j.bmcl.2014.06.014
CHEMBL3323654 113234 0 None 29 3 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assay
ChEMBL 362 5 4 5 3.3 O=c1[nH]c2c(O)ccc([C@@H](O)CN[C@H]3CCC[C@@H]3C3CCCC3)c2s1 10.1016/j.bmcl.2014.06.014
49864396 15448 0 None 25 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptorDisplacement of [3H]CGP12177 from human beta2 adrenoceptor
ChEMBL 362 5 4 5 3.3 O=c1[nH]c2c(O)ccc([C@@H](O)CN[C@@H]3CCC[C@@H]3C3CCCC3)c2s1 10.1016/j.bmcl.2010.06.136
CHEMBL1221682 15448 0 None 25 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptorDisplacement of [3H]CGP12177 from human beta2 adrenoceptor
ChEMBL 362 5 4 5 3.3 O=c1[nH]c2c(O)ccc([C@@H](O)CN[C@@H]3CCC[C@@H]3C3CCCC3)c2s1 10.1016/j.bmcl.2010.06.136
44391257 65761 0 None -1 2 Human 9.2 pKi = 9.2 Binding
Binding affinity for human beta-2 adrenergic receptor by displacing [125I]iodocyanopindolol expressed in hamster CHO cellsBinding affinity for human beta-2 adrenergic receptor by displacing [125I]iodocyanopindolol expressed in hamster CHO cells
ChEMBL 411 9 4 6 2.3 CC(COc1ccc2c(c1)NC(=O)CO2)NCC(O)COc1cccc2[nH]ccc12 10.1016/j.bmcl.2004.11.030
CHEMBL183921 65761 0 None -1 2 Human 9.2 pKi = 9.2 Binding
Binding affinity for human beta-2 adrenergic receptor by displacing [125I]iodocyanopindolol expressed in hamster CHO cellsBinding affinity for human beta-2 adrenergic receptor by displacing [125I]iodocyanopindolol expressed in hamster CHO cells
ChEMBL 411 9 4 6 2.3 CC(COc1ccc2c(c1)NC(=O)CO2)NCC(O)COc1cccc2[nH]ccc12 10.1016/j.bmcl.2004.11.030
44391257 65761 0 None -1 2 Human 9.2 pKi = 9.2 Binding
Negative logarithm causing 50% receptor occupancy against beta-2 adrenergic receptorNegative logarithm causing 50% receptor occupancy against beta-2 adrenergic receptor
ChEMBL 411 9 4 6 2.3 CC(COc1ccc2c(c1)NC(=O)CO2)NCC(O)COc1cccc2[nH]ccc12 10.1021/jm058225d
CHEMBL183921 65761 0 None -1 2 Human 9.2 pKi = 9.2 Binding
Negative logarithm causing 50% receptor occupancy against beta-2 adrenergic receptorNegative logarithm causing 50% receptor occupancy against beta-2 adrenergic receptor
ChEMBL 411 9 4 6 2.3 CC(COc1ccc2c(c1)NC(=O)CO2)NCC(O)COc1cccc2[nH]ccc12 10.1021/jm058225d
155569481 175632 0 None 8 2 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysisDisplacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysis
ChEMBL 614 23 6 8 2.7 CC(C)NC[C@H](O)COc1ccccc1CCCC(=O)NCCNC(=O)CCCc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
CHEMBL4594173 175632 0 None 8 2 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysisDisplacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysis
ChEMBL 614 23 6 8 2.7 CC(C)NC[C@H](O)COc1ccccc1CCCC(=O)NCCNC(=O)CCCc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
165193 3126 60 None 1 43 Human 9.1 pKi = 9.1 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
2303 3126 60 None 1 43 Human 9.1 pKi = 9.1 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
4946 3126 60 None 1 43 Human 9.1 pKi = 9.1 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
564 3126 60 None 1 43 Human 9.1 pKi = 9.1 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
62882 3126 60 None 1 43 Human 9.1 pKi = 9.1 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
63 3126 60 None 1 43 Human 9.1 pKi = 9.1 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
66366 3126 60 None 1 43 Human 9.1 pKi = 9.1 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
91536 3126 60 None 1 43 Human 9.1 pKi = 9.1 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
CHEMBL27 3126 60 None 1 43 Human 9.1 pKi = 9.1 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
CHEMBL452861 3126 60 None 1 43 Human 9.1 pKi = 9.1 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
DB00571 3126 60 None 1 43 Human 9.1 pKi = 9.1 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
155544582 172798 0 None 5 2 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysisDisplacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysis
ChEMBL 528 21 4 6 5.3 CC(C)NC[C@H](O)COc1ccccc1CCCCCCCCc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
CHEMBL4527821 172798 0 None 5 2 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysisDisplacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysis
ChEMBL 528 21 4 6 5.3 CC(C)NC[C@H](O)COc1ccccc1CCCCCCCCc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
49864396 15448 0 None 25 3 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assay
ChEMBL 362 5 4 5 3.3 O=c1[nH]c2c(O)ccc([C@@H](O)CN[C@@H]3CCC[C@@H]3C3CCCC3)c2s1 10.1016/j.bmcl.2014.06.014
CHEMBL1221682 15448 0 None 25 3 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assay
ChEMBL 362 5 4 5 3.3 O=c1[nH]c2c(O)ccc([C@@H](O)CN[C@@H]3CCC[C@@H]3C3CCCC3)c2s1 10.1016/j.bmcl.2014.06.014
118710935 113233 0 None 9 3 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assay
ChEMBL 362 5 4 5 3.3 O=c1[nH]c2c(O)ccc([C@@H](O)CN[C@H]3CCC[C@H]3C3CCCC3)c2s1 10.1016/j.bmcl.2014.06.014
CHEMBL3323653 113233 0 None 9 3 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assay
ChEMBL 362 5 4 5 3.3 O=c1[nH]c2c(O)ccc([C@@H](O)CN[C@H]3CCC[C@H]3C3CCCC3)c2s1 10.1016/j.bmcl.2014.06.014
49864397 15449 0 None 8 2 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptorDisplacement of [3H]CGP12177 from human beta2 adrenoceptor
ChEMBL 362 5 4 5 3.3 O=c1[nH]c2c(O)ccc([C@@H](O)CN[C@@H]3CCC[C@H]3C3CCCC3)c2s1 10.1016/j.bmcl.2010.06.136
CHEMBL1221683 15449 0 None 8 2 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptorDisplacement of [3H]CGP12177 from human beta2 adrenoceptor
ChEMBL 362 5 4 5 3.3 O=c1[nH]c2c(O)ccc([C@@H](O)CN[C@@H]3CCC[C@H]3C3CCCC3)c2s1 10.1016/j.bmcl.2010.06.136
185394 139145 34 None 3 5 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assay
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNC[C@@H](O)COc1cccc2[nH]c3ccccc3c12 10.1021/acs.jmedchem.9b00349
CHEMBL3798017 139145 34 None 3 5 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assay
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNC[C@@H](O)COc1cccc2[nH]c3ccccc3c12 10.1021/acs.jmedchem.9b00349
185394 139145 34 None 3 5 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cellsDisplacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNC[C@@H](O)COc1cccc2[nH]c3ccccc3c12 10.1016/j.bmc.2016.04.028
CHEMBL3798017 139145 34 None 3 5 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cellsDisplacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNC[C@@H](O)COc1cccc2[nH]c3ccccc3c12 10.1016/j.bmc.2016.04.028
155528927 170820 0 None 3 2 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysisDisplacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysis
ChEMBL 649 22 5 13 2.1 CC(C)NC[C@H](O)COc1ccccc1CCn1cc(CNCc2cn(CCc3ccccc3OC[C@@H](O)CNC(C)C)nn2)nn1 10.1021/acs.jmedchem.9b00595
CHEMBL4462252 170820 0 None 3 2 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysisDisplacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysis
ChEMBL 649 22 5 13 2.1 CC(C)NC[C@H](O)COc1ccccc1CCn1cc(CNCc2cn(CCc3ccccc3OC[C@@H](O)CNC(C)C)nn2)nn1 10.1021/acs.jmedchem.9b00595
204665 10125 9 None 1 2 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysisDisplacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysis
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
CHEMBL1160734 10125 9 None 1 2 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysisDisplacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysis
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
155536373 171600 0 None 6 2 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysisDisplacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysis
ChEMBL 500 19 4 6 4.5 CC(C)NC[C@H](O)COc1ccccc1CCCCCCc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
CHEMBL4473518 171600 0 None 6 2 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysisDisplacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysis
ChEMBL 500 19 4 6 4.5 CC(C)NC[C@H](O)COc1ccccc1CCCCCCc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
2419 3394 80 None 16 6 Human 9.0 pKi = 9 Binding
Binding affinity for human beta-2 adrenergic receptorBinding affinity for human beta-2 adrenergic receptor
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2004.06.086
5152 3394 80 None 16 6 Human 9.0 pKi = 9 Binding
Binding affinity for human beta-2 adrenergic receptorBinding affinity for human beta-2 adrenergic receptor
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2004.06.086
559 3394 80 None 16 6 Human 9.0 pKi = 9 Binding
Binding affinity for human beta-2 adrenergic receptorBinding affinity for human beta-2 adrenergic receptor
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2004.06.086
CHEMBL1263 3394 80 None 16 6 Human 9.0 pKi = 9 Binding
Binding affinity for human beta-2 adrenergic receptorBinding affinity for human beta-2 adrenergic receptor
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2004.06.086
DB00938 3394 80 None 16 6 Human 9.0 pKi = 9 Binding
Binding affinity for human beta-2 adrenergic receptorBinding affinity for human beta-2 adrenergic receptor
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2004.06.086
137 367 47 None -3 12 Human 9.0 pKi = 9 Binding
Displacement of [3H]-CGP12177 from human recombinant beta2 adrenoceptor expressed in CHOK1 cells after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human recombinant beta2 adrenoceptor expressed in CHOK1 cells after 1.5 hrs by scintillation counting analysis
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1021/ml400312j
2119 367 47 None -3 12 Human 9.0 pKi = 9 Binding
Displacement of [3H]-CGP12177 from human recombinant beta2 adrenoceptor expressed in CHOK1 cells after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human recombinant beta2 adrenoceptor expressed in CHOK1 cells after 1.5 hrs by scintillation counting analysis
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1021/ml400312j
563 367 47 None -3 12 Human 9.0 pKi = 9 Binding
Displacement of [3H]-CGP12177 from human recombinant beta2 adrenoceptor expressed in CHOK1 cells after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human recombinant beta2 adrenoceptor expressed in CHOK1 cells after 1.5 hrs by scintillation counting analysis
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1021/ml400312j
66368 367 47 None -3 12 Human 9.0 pKi = 9 Binding
Displacement of [3H]-CGP12177 from human recombinant beta2 adrenoceptor expressed in CHOK1 cells after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human recombinant beta2 adrenoceptor expressed in CHOK1 cells after 1.5 hrs by scintillation counting analysis
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1021/ml400312j
CHEMBL266195 367 47 None -3 12 Human 9.0 pKi = 9 Binding
Displacement of [3H]-CGP12177 from human recombinant beta2 adrenoceptor expressed in CHOK1 cells after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human recombinant beta2 adrenoceptor expressed in CHOK1 cells after 1.5 hrs by scintillation counting analysis
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1021/ml400312j
DB00866 367 47 None -3 12 Human 9.0 pKi = 9 Binding
Displacement of [3H]-CGP12177 from human recombinant beta2 adrenoceptor expressed in CHOK1 cells after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human recombinant beta2 adrenoceptor expressed in CHOK1 cells after 1.5 hrs by scintillation counting analysis
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1021/ml400312j
3682 188837 7 None 1 8 Human 9.0 pKi = 9 Binding
Displacement of [3H]CGP1217 from human recombinant adrenergic beta2 receptor transfected in insect Sf9 cells by scintillation countingDisplacement of [3H]CGP1217 from human recombinant adrenergic beta2 receptor transfected in insect Sf9 cells by scintillation counting
ChEMBL 277 6 2 3 2.6 Cc1ccc(OCC(O)C(C)NC(C)C)c2c1CCC2 10.1021/jm801211c
CHEMBL1256784 188837 7 None 1 8 Human 9.0 pKi = 9 Binding
Displacement of [3H]CGP1217 from human recombinant adrenergic beta2 receptor transfected in insect Sf9 cells by scintillation countingDisplacement of [3H]CGP1217 from human recombinant adrenergic beta2 receptor transfected in insect Sf9 cells by scintillation counting
ChEMBL 277 6 2 3 2.6 Cc1ccc(OCC(O)C(C)NC(C)C)c2c1CCC2 10.1021/jm801211c
CHEMBL513389 188837 7 None 1 8 Human 9.0 pKi = 9 Binding
Displacement of [3H]CGP1217 from human recombinant adrenergic beta2 receptor transfected in insect Sf9 cells by scintillation countingDisplacement of [3H]CGP1217 from human recombinant adrenergic beta2 receptor transfected in insect Sf9 cells by scintillation counting
ChEMBL 277 6 2 3 2.6 Cc1ccc(OCC(O)C(C)NC(C)C)c2c1CCC2 10.1021/jm801211c
49864333 15422 0 None 1 2 Human 9.0 pKi = 9 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptorDisplacement of [3H]CGP12177 from human beta2 adrenoceptor
ChEMBL 336 5 4 5 2.9 C[C@@H](NC[C@H](O)c1ccc(O)c2[nH]c(=O)sc12)C1CCCCC1 10.1016/j.bmcl.2010.06.136
CHEMBL1221541 15422 0 None 1 2 Human 9.0 pKi = 9 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptorDisplacement of [3H]CGP12177 from human beta2 adrenoceptor
ChEMBL 336 5 4 5 2.9 C[C@@H](NC[C@H](O)c1ccc(O)c2[nH]c(=O)sc12)C1CCCCC1 10.1016/j.bmcl.2010.06.136
90645347 112008 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assayDisplacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assay
ChEMBL 578 12 6 7 5.6 CC(C)(N)COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1-c1ccccc1 10.1016/j.bmcl.2014.04.095
CHEMBL3298987 112008 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assayDisplacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assay
ChEMBL 578 12 6 7 5.6 CC(C)(N)COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1-c1ccccc1 10.1016/j.bmcl.2014.04.095
127 3066 45 None -2 15 Human 9.0 pKi = 9.0 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 248 6 3 3 1.9 O[C@H](COc1cccc2c1cc[nH]2)CNC(C)C nan
688095 3066 45 None -2 15 Human 9.0 pKi = 9.0 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 248 6 3 3 1.9 O[C@H](COc1cccc2c1cc[nH]2)CNC(C)C nan
CHEMBL117405 3066 45 None -2 15 Human 9.0 pKi = 9.0 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 248 6 3 3 1.9 O[C@H](COc1cccc2c1cc[nH]2)CNC(C)C nan
155529870 170929 0 None 30 2 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranesDisplacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranes
ChEMBL 516 17 3 8 4.5 COc1cc(CCNC[C@@H](O)COc2cccc3ccccc23)ccc1OCCCSSCCN 10.1016/j.bmc.2019.05.034
CHEMBL4463925 170929 0 None 30 2 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranesDisplacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranes
ChEMBL 516 17 3 8 4.5 COc1cc(CCNC[C@@H](O)COc2cccc3ccccc23)ccc1OCCCSSCCN 10.1016/j.bmc.2019.05.034
155515551 169398 0 None 1 2 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysisDisplacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysis
ChEMBL 584 25 4 6 6.8 CC(C)NC[C@H](O)COc1ccccc1CCCCCCCCCCCCc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
CHEMBL4441975 169398 0 None 1 2 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysisDisplacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysis
ChEMBL 584 25 4 6 6.8 CC(C)NC[C@H](O)COc1ccccc1CCCCCCCCCCCCc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
155518547 169712 0 None 29 2 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysisDisplacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysis
ChEMBL 558 20 6 7 3.0 CC(C)NC[C@H](O)COc1ccccc1CCCNC(=O)NCCCc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
CHEMBL4446394 169712 0 None 29 2 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysisDisplacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysis
ChEMBL 558 20 6 7 3.0 CC(C)NC[C@H](O)COc1ccccc1CCCNC(=O)NCCCc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
4080436 6626 3 None 10 3 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cells
ChEMBL 279 6 1 4 1.9 CC(C)c1ccccc1OCC(O)CN1CCOCC1 10.1016/j.bmcl.2010.04.009
CHEMBL1083668 6626 3 None 10 3 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cells
ChEMBL 279 6 1 4 1.9 CC(C)c1ccccc1OCC(O)CN1CCOCC1 10.1016/j.bmcl.2010.04.009
49864358 15432 0 None 1 2 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptorDisplacement of [3H]CGP12177 from human beta2 adrenoceptor
ChEMBL 344 7 4 5 2.6 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCCc3ccccc3)c2s1 10.1016/j.bmcl.2010.06.136
CHEMBL1221589 15432 0 None 1 2 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptorDisplacement of [3H]CGP12177 from human beta2 adrenoceptor
ChEMBL 344 7 4 5 2.6 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCCc3ccccc3)c2s1 10.1016/j.bmcl.2010.06.136
137 367 47 None -3 12 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysisDisplacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysis
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1021/acs.jmedchem.9b00595
2119 367 47 None -3 12 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysisDisplacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysis
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1021/acs.jmedchem.9b00595
563 367 47 None -3 12 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysisDisplacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysis
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1021/acs.jmedchem.9b00595
66368 367 47 None -3 12 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysisDisplacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysis
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1021/acs.jmedchem.9b00595
CHEMBL266195 367 47 None -3 12 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysisDisplacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysis
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1021/acs.jmedchem.9b00595
DB00866 367 47 None -3 12 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysisDisplacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysis
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1021/acs.jmedchem.9b00595
137 367 47 None -3 12 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysisDisplacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysis
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1021/acs.jmedchem.9b00595
2119 367 47 None -3 12 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysisDisplacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysis
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1021/acs.jmedchem.9b00595
563 367 47 None -3 12 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysisDisplacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysis
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1021/acs.jmedchem.9b00595
66368 367 47 None -3 12 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysisDisplacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysis
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1021/acs.jmedchem.9b00595
CHEMBL266195 367 47 None -3 12 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysisDisplacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysis
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1021/acs.jmedchem.9b00595
DB00866 367 47 None -3 12 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysisDisplacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysis
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1021/acs.jmedchem.9b00595
10239722 111953 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assayDisplacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assay
ChEMBL 550 11 6 7 5.0 COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1-c1ccc(CN)cc1 10.1016/j.bmcl.2014.04.095
CHEMBL3298326 111953 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assayDisplacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assay
ChEMBL 550 11 6 7 5.0 COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1-c1ccc(CN)cc1 10.1016/j.bmcl.2014.04.095
118710948 113248 0 None 5 3 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assay
ChEMBL 386 9 4 5 3.5 CCCCc1cccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)c1 10.1016/j.bmcl.2014.06.014
CHEMBL3323668 113248 0 None 5 3 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assay
ChEMBL 386 9 4 5 3.5 CCCCc1cccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)c1 10.1016/j.bmcl.2014.06.014
2419 3394 80 None 16 6 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]-CYP from human beta2-adrenergic receptor expressed in COS-7 cells by gamma countingDisplacement of [125I]-CYP from human beta2-adrenergic receptor expressed in COS-7 cells by gamma counting
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmc.2009.11.062
5152 3394 80 None 16 6 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]-CYP from human beta2-adrenergic receptor expressed in COS-7 cells by gamma countingDisplacement of [125I]-CYP from human beta2-adrenergic receptor expressed in COS-7 cells by gamma counting
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmc.2009.11.062
559 3394 80 None 16 6 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]-CYP from human beta2-adrenergic receptor expressed in COS-7 cells by gamma countingDisplacement of [125I]-CYP from human beta2-adrenergic receptor expressed in COS-7 cells by gamma counting
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmc.2009.11.062
CHEMBL1263 3394 80 None 16 6 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]-CYP from human beta2-adrenergic receptor expressed in COS-7 cells by gamma countingDisplacement of [125I]-CYP from human beta2-adrenergic receptor expressed in COS-7 cells by gamma counting
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmc.2009.11.062
DB00938 3394 80 None 16 6 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]-CYP from human beta2-adrenergic receptor expressed in COS-7 cells by gamma countingDisplacement of [125I]-CYP from human beta2-adrenergic receptor expressed in COS-7 cells by gamma counting
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmc.2009.11.062
9917280 14356 0 None 39810 2 Human 8.8 pKi = 8.8 Binding
Binding affinity for human Beta-2 adrenergic receptor expressed in CHO cells by radioligand competition binding assays using [125I]iodocyanopindolol (ICYP)Binding affinity for human Beta-2 adrenergic receptor expressed in CHO cells by radioligand competition binding assays using [125I]iodocyanopindolol (ICYP)
ChEMBL 633 2 3 3 4.3 Oc1cc2c(cc1O)C(Cc1cc(I)c(I)c(I)c1)NCC2 10.1021/jm960208o
CHEMBL120278 14356 0 None 39810 2 Human 8.8 pKi = 8.8 Binding
Binding affinity for human Beta-2 adrenergic receptor expressed in CHO cells by radioligand competition binding assays using [125I]iodocyanopindolol (ICYP)Binding affinity for human Beta-2 adrenergic receptor expressed in CHO cells by radioligand competition binding assays using [125I]iodocyanopindolol (ICYP)
ChEMBL 633 2 3 3 4.3 Oc1cc2c(cc1O)C(Cc1cc(I)c(I)c(I)c1)NCC2 10.1021/jm960208o
155510718 168937 0 None 1 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysisDisplacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysis
ChEMBL 556 23 4 6 6.1 CC(C)NC[C@H](O)COc1ccccc1CCCCCCCCCCc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
CHEMBL4434772 168937 0 None 1 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysisDisplacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysis
ChEMBL 556 23 4 6 6.1 CC(C)NC[C@H](O)COc1ccccc1CCCCCCCCCCc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
10414389 16305 0 None 120 2 Human 8.8 pKi = 8.8 Binding
Binding affinity for human Beta-2 adrenergic receptor expressed in CHO cells by radioligand competition binding assays using [125I]iodocyanopindolol (ICYP)Binding affinity for human Beta-2 adrenergic receptor expressed in CHO cells by radioligand competition binding assays using [125I]iodocyanopindolol (ICYP)
ChEMBL 522 2 4 4 3.3 Nc1c(I)cc(CC2NCCc3cc(O)c(O)cc32)cc1I 10.1021/jm960208o
CHEMBL123596 16305 0 None 120 2 Human 8.8 pKi = 8.8 Binding
Binding affinity for human Beta-2 adrenergic receptor expressed in CHO cells by radioligand competition binding assays using [125I]iodocyanopindolol (ICYP)Binding affinity for human Beta-2 adrenergic receptor expressed in CHO cells by radioligand competition binding assays using [125I]iodocyanopindolol (ICYP)
ChEMBL 522 2 4 4 3.3 Nc1c(I)cc(CC2NCCc3cc(O)c(O)cc32)cc1I 10.1021/jm960208o
44391257 65761 0 None -1 2 Human 8.8 pKi = 8.8 Binding
Binding affinity for human beta-2 adrenergic receptor by displacing [125I]iodocyanopindolol expressed in hamster CHO cellsBinding affinity for human beta-2 adrenergic receptor by displacing [125I]iodocyanopindolol expressed in hamster CHO cells
ChEMBL 411 9 4 6 2.3 CC(COc1ccc2c(c1)NC(=O)CO2)NCC(O)COc1cccc2[nH]ccc12 10.1016/j.bmcl.2004.11.030
CHEMBL183921 65761 0 None -1 2 Human 8.8 pKi = 8.8 Binding
Binding affinity for human beta-2 adrenergic receptor by displacing [125I]iodocyanopindolol expressed in hamster CHO cellsBinding affinity for human beta-2 adrenergic receptor by displacing [125I]iodocyanopindolol expressed in hamster CHO cells
ChEMBL 411 9 4 6 2.3 CC(COc1ccc2c(c1)NC(=O)CO2)NCC(O)COc1cccc2[nH]ccc12 10.1016/j.bmcl.2004.11.030
11592062 111952 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assayDisplacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assay
ChEMBL 550 11 6 7 5.0 COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1-c1cccc(CN)c1 10.1016/j.bmcl.2014.04.095
CHEMBL3298325 111952 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assayDisplacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assay
ChEMBL 550 11 6 7 5.0 COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1-c1cccc(CN)c1 10.1016/j.bmcl.2014.04.095
118710950 113250 0 None 2 3 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assay
ChEMBL 402 10 4 6 3.3 CCCCOc1cccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)c1 10.1016/j.bmcl.2014.06.014
CHEMBL3323670 113250 0 None 2 3 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assay
ChEMBL 402 10 4 6 3.3 CCCCOc1cccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)c1 10.1016/j.bmcl.2014.06.014
165193 3126 60 None 1 43 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-CGP12177 from human beta2 ADR expressed in HEK293T cell membrane after 90 mins by scintillation countingDisplacement of [3H]-CGP12177 from human beta2 ADR expressed in HEK293T cell membrane after 90 mins by scintillation counting
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/acs.jmedchem.8b00625
2303 3126 60 None 1 43 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-CGP12177 from human beta2 ADR expressed in HEK293T cell membrane after 90 mins by scintillation countingDisplacement of [3H]-CGP12177 from human beta2 ADR expressed in HEK293T cell membrane after 90 mins by scintillation counting
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/acs.jmedchem.8b00625
4946 3126 60 None 1 43 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-CGP12177 from human beta2 ADR expressed in HEK293T cell membrane after 90 mins by scintillation countingDisplacement of [3H]-CGP12177 from human beta2 ADR expressed in HEK293T cell membrane after 90 mins by scintillation counting
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/acs.jmedchem.8b00625
564 3126 60 None 1 43 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-CGP12177 from human beta2 ADR expressed in HEK293T cell membrane after 90 mins by scintillation countingDisplacement of [3H]-CGP12177 from human beta2 ADR expressed in HEK293T cell membrane after 90 mins by scintillation counting
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/acs.jmedchem.8b00625
62882 3126 60 None 1 43 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-CGP12177 from human beta2 ADR expressed in HEK293T cell membrane after 90 mins by scintillation countingDisplacement of [3H]-CGP12177 from human beta2 ADR expressed in HEK293T cell membrane after 90 mins by scintillation counting
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/acs.jmedchem.8b00625
63 3126 60 None 1 43 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-CGP12177 from human beta2 ADR expressed in HEK293T cell membrane after 90 mins by scintillation countingDisplacement of [3H]-CGP12177 from human beta2 ADR expressed in HEK293T cell membrane after 90 mins by scintillation counting
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/acs.jmedchem.8b00625
66366 3126 60 None 1 43 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-CGP12177 from human beta2 ADR expressed in HEK293T cell membrane after 90 mins by scintillation countingDisplacement of [3H]-CGP12177 from human beta2 ADR expressed in HEK293T cell membrane after 90 mins by scintillation counting
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/acs.jmedchem.8b00625
91536 3126 60 None 1 43 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-CGP12177 from human beta2 ADR expressed in HEK293T cell membrane after 90 mins by scintillation countingDisplacement of [3H]-CGP12177 from human beta2 ADR expressed in HEK293T cell membrane after 90 mins by scintillation counting
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/acs.jmedchem.8b00625
CHEMBL27 3126 60 None 1 43 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-CGP12177 from human beta2 ADR expressed in HEK293T cell membrane after 90 mins by scintillation countingDisplacement of [3H]-CGP12177 from human beta2 ADR expressed in HEK293T cell membrane after 90 mins by scintillation counting
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/acs.jmedchem.8b00625
CHEMBL452861 3126 60 None 1 43 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-CGP12177 from human beta2 ADR expressed in HEK293T cell membrane after 90 mins by scintillation countingDisplacement of [3H]-CGP12177 from human beta2 ADR expressed in HEK293T cell membrane after 90 mins by scintillation counting
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/acs.jmedchem.8b00625
DB00571 3126 60 None 1 43 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-CGP12177 from human beta2 ADR expressed in HEK293T cell membrane after 90 mins by scintillation countingDisplacement of [3H]-CGP12177 from human beta2 ADR expressed in HEK293T cell membrane after 90 mins by scintillation counting
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/acs.jmedchem.8b00625
49864356 15430 0 None 2 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptorDisplacement of [3H]CGP12177 from human beta2 adrenoceptor
ChEMBL 330 6 4 5 2.2 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3ccccc3)c2s1 10.1016/j.bmcl.2010.06.136
CHEMBL1221587 15430 0 None 2 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptorDisplacement of [3H]CGP12177 from human beta2 adrenoceptor
ChEMBL 330 6 4 5 2.2 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3ccccc3)c2s1 10.1016/j.bmcl.2010.06.136
49864379 15441 0 None 8 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptorDisplacement of [3H]CGP12177 from human beta2 adrenoceptor
ChEMBL 358 8 4 5 2.9 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCCCc3ccccc3)c2s1 10.1016/j.bmcl.2010.06.136
CHEMBL1221636 15441 0 None 8 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptorDisplacement of [3H]CGP12177 from human beta2 adrenoceptor
ChEMBL 358 8 4 5 2.9 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCCCc3ccccc3)c2s1 10.1016/j.bmcl.2010.06.136
49864335 15424 0 None 4 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptorDisplacement of [3H]CGP12177 from human beta2 adrenoceptor
ChEMBL 338 5 4 5 3.1 CC(C)(C)CC(C)(C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)sc12 10.1016/j.bmcl.2010.06.136
CHEMBL1221543 15424 0 None 4 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptorDisplacement of [3H]CGP12177 from human beta2 adrenoceptor
ChEMBL 338 5 4 5 3.1 CC(C)(C)CC(C)(C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)sc12 10.1016/j.bmcl.2010.06.136
10577317 15322 0 None 2691 2 Human 8.7 pKi = 8.7 Binding
Binding affinity for human Beta-2 adrenergic receptor expressed in CHO cells by radioligand competition binding assays using [125I]iodocyanopindolol (ICYP)Binding affinity for human Beta-2 adrenergic receptor expressed in CHO cells by radioligand competition binding assays using [125I]iodocyanopindolol (ICYP)
ChEMBL 500 4 4 4 4.4 O=C(Nc1ccc(CC2NCCc3cc(O)c(O)cc32)cc1I)c1ccccc1 10.1021/jm960208o
CHEMBL121704 15322 0 None 2691 2 Human 8.7 pKi = 8.7 Binding
Binding affinity for human Beta-2 adrenergic receptor expressed in CHO cells by radioligand competition binding assays using [125I]iodocyanopindolol (ICYP)Binding affinity for human Beta-2 adrenergic receptor expressed in CHO cells by radioligand competition binding assays using [125I]iodocyanopindolol (ICYP)
ChEMBL 500 4 4 4 4.4 O=C(Nc1ccc(CC2NCCc3cc(O)c(O)cc32)cc1I)c1ccccc1 10.1021/jm960208o
52941476 17488 0 None 6 3 Human 8.0 pKi = 8 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 488 9 2 7 4.9 CCc1cccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)c1 10.1016/j.bmcl.2010.08.039
CHEMBL1258484 17488 0 None 6 3 Human 8.0 pKi = 8 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 488 9 2 7 4.9 CCc1cccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)c1 10.1016/j.bmcl.2010.08.039
52948805 17558 0 None 6 3 Human 8.0 pKi = 8 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 502 9 2 7 5.5 CC(C)c1ccccc1OCC(O)CNC1CCN(c2ncnc3scc(-c4ccccc4)c23)CC1 10.1016/j.bmcl.2010.08.039
CHEMBL1258704 17558 0 None 6 3 Human 8.0 pKi = 8 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 502 9 2 7 5.5 CC(C)c1ccccc1OCC(O)CNC1CCN(c2ncnc3scc(-c4ccccc4)c23)CC1 10.1016/j.bmcl.2010.08.039
9858463 93687 0 None 19 2 Human 8.0 pKi = 8 Binding
Displacement of [125I]iodocyanopindolol from human adrenergic beta-2 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human adrenergic beta-2 receptor expressed in CHO cells
ChEMBL 325 8 2 6 2.4 O[C@@H](CNCCOc1ccc(-c2cocn2)cc1)c1cccnc1 10.1016/j.bmcl.2007.06.072
CHEMBL249336 93687 0 None 19 2 Human 8.0 pKi = 8 Binding
Displacement of [125I]iodocyanopindolol from human adrenergic beta-2 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human adrenergic beta-2 receptor expressed in CHO cells
ChEMBL 325 8 2 6 2.4 O[C@@H](CNCCOc1ccc(-c2cocn2)cc1)c1cccnc1 10.1016/j.bmcl.2007.06.072
10291064 94031 0 None 14 2 Human 8.0 pKi = 8 Binding
Displacement of [125I]iodocyanopindolol from human adrenergic beta-2 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human adrenergic beta-2 receptor expressed in CHO cells
ChEMBL 341 8 2 6 2.9 O[C@@H](CNCCOc1ccc(-c2cscn2)cc1)c1cccnc1 10.1016/j.bmcl.2007.06.072
CHEMBL251392 94031 0 None 14 2 Human 8.0 pKi = 8 Binding
Displacement of [125I]iodocyanopindolol from human adrenergic beta-2 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human adrenergic beta-2 receptor expressed in CHO cells
ChEMBL 341 8 2 6 2.9 O[C@@H](CNCCOc1ccc(-c2cscn2)cc1)c1cccnc1 10.1016/j.bmcl.2007.06.072
10438748 58213 0 None -13 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]-dihydroalprenolol from human beta2-adrenoceptor expressed in HEK cells after 4 hrsDisplacement of [3H]-dihydroalprenolol from human beta2-adrenoceptor expressed in HEK cells after 4 hrs
ChEMBL 612 14 5 7 6.2 O=C(Nc1ccccc1-c1ccccc1)OC1CCN(CCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1016/j.bmcl.2011.01.043
CHEMBL1683932 58213 0 None -13 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]-dihydroalprenolol from human beta2-adrenoceptor expressed in HEK cells after 4 hrsDisplacement of [3H]-dihydroalprenolol from human beta2-adrenoceptor expressed in HEK cells after 4 hrs
ChEMBL 612 14 5 7 6.2 O=C(Nc1ccccc1-c1ccccc1)OC1CCN(CCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1016/j.bmcl.2011.01.043
90645346 111990 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assayDisplacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assay
ChEMBL 578 13 6 7 4.7 O=C(NCCOc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1)c1ccccc1 10.1016/j.bmcl.2014.04.095
CHEMBL3298762 111990 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assayDisplacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assay
ChEMBL 578 13 6 7 4.7 O=C(NCCOc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1)c1ccccc1 10.1016/j.bmcl.2014.04.095
11180293 112003 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assayDisplacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assay
ChEMBL 543 12 6 8 3.1 O=c1ccc2c([C@@H](O)CNCCc3ccc(Nc4ccc(OCCN5CCNCC5)cc4)cc3)ccc(O)c2[nH]1 10.1016/j.bmcl.2014.04.095
CHEMBL3298897 112003 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assayDisplacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assay
ChEMBL 543 12 6 8 3.1 O=c1ccc2c([C@@H](O)CNCCc3ccc(Nc4ccc(OCCN5CCNCC5)cc4)cc3)ccc(O)c2[nH]1 10.1016/j.bmcl.2014.04.095
155566405 175354 0 None 3 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H](-)CGP 12177 from human recombinant beta2 adrenoceptor after 120 mins by scintillation counting methodDisplacement of [3H](-)CGP 12177 from human recombinant beta2 adrenoceptor after 120 mins by scintillation counting method
ChEMBL 426 21 3 8 0.8 C=CCc1ccccc1OCC(O)CNCCOCCOCCOCCOCCN 10.1039/C8MD00412A
CHEMBL4587648 175354 0 None 3 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H](-)CGP 12177 from human recombinant beta2 adrenoceptor after 120 mins by scintillation counting methodDisplacement of [3H](-)CGP 12177 from human recombinant beta2 adrenoceptor after 120 mins by scintillation counting method
ChEMBL 426 21 3 8 0.8 C=CCc1ccccc1OCC(O)CNCCOCCOCCOCCOCCN 10.1039/C8MD00412A
52947060 17386 0 None -1 3 Human 7.0 pKi = 7 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 474 8 2 7 4.7 Cc1c(-c2ccccc2)sc2ncnc(N3CCC(NCC(O)COc4ccccc4)CC3)c12 10.1016/j.bmcl.2010.08.039
CHEMBL1258144 17386 0 None -1 3 Human 7.0 pKi = 7 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 474 8 2 7 4.7 Cc1c(-c2ccccc2)sc2ncnc(N3CCC(NCC(O)COc4ccccc4)CC3)c12 10.1016/j.bmcl.2010.08.039
59119410 111760 0 None 158 2 Human 7.0 pKi = 7 Binding
Displacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assay
ChEMBL 436 11 5 6 4.3 CC(C)Oc1ccc(Nc2ccc(CCNCC(O)c3ccc(O)c(CO)c3)cc2)cc1 10.1016/j.bmcl.2014.04.069
CHEMBL3290993 111760 0 None 158 2 Human 7.0 pKi = 7 Binding
Displacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assay
ChEMBL 436 11 5 6 4.3 CC(C)Oc1ccc(Nc2ccc(CCNCC(O)c3ccc(O)c(CO)c3)cc2)cc1 10.1016/j.bmcl.2014.04.069
73056757 103784 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 303 7 4 5 2.0 COc1ccc(CCNC[C@H](O)c2cc(O)cc(O)c2)cc1 10.1016/j.bmc.2013.11.030
CHEMBL3099657 103784 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 303 7 4 5 2.0 COc1ccc(CCNC[C@H](O)c2cc(O)cc(O)c2)cc1 10.1016/j.bmc.2013.11.030
4418 33985 80 None -23 7 Dog 6.0 pKi = 6 Binding
Beta-2 adrenergic receptor binding affinity by measuring the displacement of [3H]DHA binding in rat lungBeta-2 adrenergic receptor binding affinity by measuring the displacement of [3H]DHA binding in rat lung
ChEMBL 392 7 1 5 3.4 COc1ccccc1N1CCN(CC(O)COc2cccc3ccccc23)CC1 10.1016/s0960-894x(00)00016-0
CHEMBL142635 33985 80 None -23 7 Dog 6.0 pKi = 6 Binding
Beta-2 adrenergic receptor binding affinity by measuring the displacement of [3H]DHA binding in rat lungBeta-2 adrenergic receptor binding affinity by measuring the displacement of [3H]DHA binding in rat lung
ChEMBL 392 7 1 5 3.4 COc1ccccc1N1CCN(CC(O)COc2cccc3ccccc23)CC1 10.1016/s0960-894x(00)00016-0
44391270 63633 0 None -630 2 Human 6.0 pKi = 6 Binding
Binding affinity for human beta-2 adrenergic receptor by displacing [125I]iodocyanopindolol expressed in hamster CHO cellsBinding affinity for human beta-2 adrenergic receptor by displacing [125I]iodocyanopindolol expressed in hamster CHO cells
ChEMBL 381 9 3 5 2.9 O=C1COc2ccc(OCCNCCCOc3cccc4[nH]ccc34)cc2N1 10.1016/j.bmcl.2004.11.030
CHEMBL180700 63633 0 None -630 2 Human 6.0 pKi = 6 Binding
Binding affinity for human beta-2 adrenergic receptor by displacing [125I]iodocyanopindolol expressed in hamster CHO cellsBinding affinity for human beta-2 adrenergic receptor by displacing [125I]iodocyanopindolol expressed in hamster CHO cells
ChEMBL 381 9 3 5 2.9 O=C1COc2ccc(OCCNCCCOc3cccc4[nH]ccc34)cc2N1 10.1016/j.bmcl.2004.11.030
2685 875 15 None -1096 7 Human 6.0 pKi = 6 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranesDisplacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranes
ChEMBL 494 11 4 8 2.3 OC(COc1ccc(cc1)c1nc(cn1C)C(F)(F)F)CNCCOc1ccc(c(c1)C(=O)N)O 10.1016/j.bmc.2019.05.034
541 875 15 None -1096 7 Human 6.0 pKi = 6 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranesDisplacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranes
ChEMBL 494 11 4 8 2.3 OC(COc1ccc(cc1)c1nc(cn1C)C(F)(F)F)CNCCOc1ccc(c(c1)C(=O)N)O 10.1016/j.bmc.2019.05.034
CHEMBL280822 875 15 None -1096 7 Human 6.0 pKi = 6 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranesDisplacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranes
ChEMBL 494 11 4 8 2.3 OC(COc1ccc(cc1)c1nc(cn1C)C(F)(F)F)CNCCOc1ccc(c(c1)C(=O)N)O 10.1016/j.bmc.2019.05.034
44391270 63633 0 None -630 2 Human 6.0 pKi = 6 Binding
Negative logarithm causing 50% receptor occupancy against beta-2 adrenergic receptorNegative logarithm causing 50% receptor occupancy against beta-2 adrenergic receptor
ChEMBL 381 9 3 5 2.9 O=C1COc2ccc(OCCNCCCOc3cccc4[nH]ccc34)cc2N1 10.1021/jm058225d
CHEMBL180700 63633 0 None -630 2 Human 6.0 pKi = 6 Binding
Negative logarithm causing 50% receptor occupancy against beta-2 adrenergic receptorNegative logarithm causing 50% receptor occupancy against beta-2 adrenergic receptor
ChEMBL 381 9 3 5 2.9 O=C1COc2ccc(OCCNCCCOc3cccc4[nH]ccc34)cc2N1 10.1021/jm058225d
44424580 85373 0 None -1 2 Human 4.0 pKi = 4 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 253 7 4 4 2.3 CCCC[C@@H](C)NC[C@@H](O)c1cc(O)cc(O)c1 10.1021/jm070030d
CHEMBL229616 85373 0 None -1 2 Human 4.0 pKi = 4 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 253 7 4 4 2.3 CCCC[C@@H](C)NC[C@@H](O)c1cc(O)cc(O)c1 10.1021/jm070030d
119570 3098 90 None -1202 40 Human 4.0 pKi = 4 Binding
Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cellsDisplacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1016/j.bmc.2016.04.028
2233 3098 90 None -1202 40 Human 4.0 pKi = 4 Binding
Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cellsDisplacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1016/j.bmc.2016.04.028
953 3098 90 None -1202 40 Human 4.0 pKi = 4 Binding
Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cellsDisplacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1016/j.bmc.2016.04.028
CHEMBL301265 3098 90 None -1202 40 Human 4.0 pKi = 4 Binding
Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cellsDisplacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1016/j.bmc.2016.04.028
DB00413 3098 90 None -1202 40 Human 4.0 pKi = 4 Binding
Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cellsDisplacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1016/j.bmc.2016.04.028
2 3198 19 None -6606 29 Human 4.0 pKi = 4 Binding
Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cellsDisplacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.bmc.2016.04.028
54562 3198 19 None -6606 29 Human 4.0 pKi = 4 Binding
Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cellsDisplacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.bmc.2016.04.028
CHEMBL240773 3198 19 None -6606 29 Human 4.0 pKi = 4 Binding
Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cellsDisplacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.bmc.2016.04.028
2249 509 106 None -33 12 Human 5.0 pKi = 5 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C nan
255 509 106 None -33 12 Human 5.0 pKi = 5 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C nan
548 509 106 None -33 12 Human 5.0 pKi = 5 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C nan
CHEMBL24 509 106 None -33 12 Human 5.0 pKi = 5 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C nan
DB00335 509 106 None -33 12 Human 5.0 pKi = 5 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C nan
73056757 103784 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 303 7 4 5 2.0 COc1ccc(CCNC[C@H](O)c2cc(O)cc(O)c2)cc1 10.1016/j.bmc.2013.11.030
CHEMBL3099657 103784 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 303 7 4 5 2.0 COc1ccc(CCNC[C@H](O)c2cc(O)cc(O)c2)cc1 10.1016/j.bmc.2013.11.030
10231679 93866 0 None -5 3 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]iodocyanopindolol from human cloned adrenergic beta-2 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human cloned adrenergic beta-2 receptor expressed in CHO cells
ChEMBL 572 14 4 7 4.4 CS(=O)(=O)Nc1cc(C[C@H](O)CN[C@H](Cc2ccccc2)c2ccc(OC(F)F)c(OC(F)F)c2)ccc1O 10.1016/j.bmcl.2007.05.030
CHEMBL250553 93866 0 None -5 3 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]iodocyanopindolol from human cloned adrenergic beta-2 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human cloned adrenergic beta-2 receptor expressed in CHO cells
ChEMBL 572 14 4 7 4.4 CS(=O)(=O)Nc1cc(C[C@H](O)CN[C@H](Cc2ccccc2)c2ccc(OC(F)F)c(OC(F)F)c2)ccc1O 10.1016/j.bmcl.2007.05.030
667688 85358 4 None - 1 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 303 6 5 5 2.1 C[C@H](Cc1ccc(O)cc1)NC[C@@H](O)c1cc(O)cc(O)c1 10.1021/jm070030d
CHEMBL229477 85358 4 None - 1 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 303 6 5 5 2.1 C[C@H](Cc1ccc(O)cc1)NC[C@@H](O)c1cc(O)cc(O)c1 10.1021/jm070030d
667688 85358 4 None - 1 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 303 6 5 5 2.1 C[C@H](Cc1ccc(O)cc1)NC[C@@H](O)c1cc(O)cc(O)c1 10.1021/jm070030d
CHEMBL229477 85358 4 None - 1 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 303 6 5 5 2.1 C[C@H](Cc1ccc(O)cc1)NC[C@@H](O)c1cc(O)cc(O)c1 10.1021/jm070030d
667688 85358 4 None - 1 Human 5.0 pKi = 5.0 Binding
Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.
ChEMBL 303 6 5 5 2.1 C[C@H](Cc1ccc(O)cc1)NC[C@@H](O)c1cc(O)cc(O)c1 nan
CHEMBL229477 85358 4 None - 1 Human 5.0 pKi = 5.0 Binding
Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.
ChEMBL 303 6 5 5 2.1 C[C@H](Cc1ccc(O)cc1)NC[C@@H](O)c1cc(O)cc(O)c1 nan
145965875 163505 0 None - 1 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-DHA from Nb80-fused beta2 adrenergic receptor (unknown origin) expressed in Sf9 cell membranes after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-DHA from Nb80-fused beta2 adrenergic receptor (unknown origin) expressed in Sf9 cell membranes after 2 hrs by microbeta scintillation counting method
ChEMBL 390 8 1 3 5.0 COc1ccc2c(c1)c(CCNCCCc1cccc(C(F)(F)F)c1)cn2C 10.1021/acs.jmedchem.7b01558
CHEMBL4209269 163505 0 None - 1 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-DHA from Nb80-fused beta2 adrenergic receptor (unknown origin) expressed in Sf9 cell membranes after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-DHA from Nb80-fused beta2 adrenergic receptor (unknown origin) expressed in Sf9 cell membranes after 2 hrs by microbeta scintillation counting method
ChEMBL 390 8 1 3 5.0 COc1ccc2c(c1)c(CCNCCCc1cccc(C(F)(F)F)c1)cn2C 10.1021/acs.jmedchem.7b01558
36811 1421 34 None -51 7 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 301 7 4 4 3.0 CC(CCc1ccc(cc1)O)NCCc1ccc(c(c1)O)O nan
535 1421 34 None -51 7 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 301 7 4 4 3.0 CC(CCc1ccc(cc1)O)NCCc1ccc(c(c1)O)O nan
937 1421 34 None -51 7 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 301 7 4 4 3.0 CC(CCc1ccc(cc1)O)NCCc1ccc(c(c1)O)O nan
CHEMBL926 1421 34 None -51 7 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 301 7 4 4 3.0 CC(CCc1ccc(cc1)O)NCCc1ccc(c(c1)O)O nan
DB00841 1421 34 None -51 7 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 301 7 4 4 3.0 CC(CCc1ccc(cc1)O)NCCc1ccc(c(c1)O)O nan
16737588 85375 0 None 4 2 Human 5.0 pKi = 5.0 Binding
Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.
ChEMBL 273 6 4 4 2.0 Oc1cc(O)cc([C@@H](O)CNCCc2ccccc2)c1 nan
CHEMBL229620 85375 0 None 4 2 Human 5.0 pKi = 5.0 Binding
Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.
ChEMBL 273 6 4 4 2.0 Oc1cc(O)cc([C@@H](O)CNCCc2ccccc2)c1 nan
16737588 85375 0 None 4 2 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 273 6 4 4 2.0 Oc1cc(O)cc([C@@H](O)CNCCc2ccccc2)c1 10.1021/jm070030d
CHEMBL229620 85375 0 None 4 2 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 273 6 4 4 2.0 Oc1cc(O)cc([C@@H](O)CNCCc2ccccc2)c1 10.1021/jm070030d
16737588 85375 0 None 4 2 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 273 6 4 4 2.0 Oc1cc(O)cc([C@@H](O)CNCCc2ccccc2)c1 10.1021/jm070030d
CHEMBL229620 85375 0 None 4 2 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 273 6 4 4 2.0 Oc1cc(O)cc([C@@H](O)CNCCc2ccccc2)c1 10.1021/jm070030d
10140996 154367 0 None -134 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]iodocyanopindolol from human cloned adrenergic beta-2 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human cloned adrenergic beta-2 receptor expressed in CHO cells
ChEMBL 486 11 5 7 3.0 COc1ccc([C@@H](Cc2ccccc2)NC[C@@H](O)Cc2ccc(O)c(NS(C)(=O)=O)c2)cc1O 10.1016/j.bmcl.2007.05.030
CHEMBL400947 154367 0 None -134 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]iodocyanopindolol from human cloned adrenergic beta-2 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human cloned adrenergic beta-2 receptor expressed in CHO cells
ChEMBL 486 11 5 7 3.0 COc1ccc([C@@H](Cc2ccccc2)NC[C@@H](O)Cc2ccc(O)c(NS(C)(=O)=O)c2)cc1O 10.1016/j.bmcl.2007.05.030
1531 2226 64 None -1 15 Human 8.0 pKi = 8.0 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O nan
3869 2226 64 None -1 15 Human 8.0 pKi = 8.0 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O nan
7207 2226 64 None -1 15 Human 8.0 pKi = 8.0 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O nan
CHEMBL429 2226 64 None -1 15 Human 8.0 pKi = 8.0 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O nan
DB00598 2226 64 None -1 15 Human 8.0 pKi = 8.0 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O nan
24936885 17286 0 None -1 3 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 504 9 3 8 4.6 CCc1cc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)ccc1O 10.1016/j.bmcl.2010.08.039
CHEMBL1257797 17286 0 None -1 3 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 504 9 3 8 4.6 CCc1cc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)ccc1O 10.1016/j.bmcl.2010.08.039
52949488 17349 0 None 1 3 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 490 9 2 8 4.4 COc1ccccc1OCC(O)CNC1CCN(c2ncnc3scc(-c4ccccc4)c23)CC1 10.1016/j.bmcl.2010.08.039
CHEMBL1258023 17349 0 None 1 3 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 490 9 2 8 4.4 COc1ccccc1OCC(O)CNC1CCN(c2ncnc3scc(-c4ccccc4)c23)CC1 10.1016/j.bmcl.2010.08.039
44393971 65884 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity for human beta-2 adrenergic receptorBinding affinity for human beta-2 adrenergic receptor
ChEMBL 432 10 4 5 3.4 O=CNc1cc([C@@H](O)CNCCc2ccc(OC3Cc4ccccc4C3)cc2)ccc1O 10.1016/j.bmcl.2004.06.086
CHEMBL184538 65884 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity for human beta-2 adrenergic receptorBinding affinity for human beta-2 adrenergic receptor
ChEMBL 432 10 4 5 3.4 O=CNc1cc([C@@H](O)CNCCc2ccc(OC3Cc4ccccc4C3)cc2)ccc1O 10.1016/j.bmcl.2004.06.086
9806791 15365 0 None 1621 2 Human 7.9 pKi = 7.9 Binding
Binding affinity for human Beta-2 adrenergic receptor expressed in CHO cells by radioligand competition binding assays using [125I]iodocyanopindolol (ICYP)Binding affinity for human Beta-2 adrenergic receptor expressed in CHO cells by radioligand competition binding assays using [125I]iodocyanopindolol (ICYP)
ChEMBL 523 2 4 4 3.4 Oc1cc2c(cc1O)C(Cc1cc(I)c(O)c(I)c1)NCC2 10.1021/jm960208o
CHEMBL121964 15365 0 None 1621 2 Human 7.9 pKi = 7.9 Binding
Binding affinity for human Beta-2 adrenergic receptor expressed in CHO cells by radioligand competition binding assays using [125I]iodocyanopindolol (ICYP)Binding affinity for human Beta-2 adrenergic receptor expressed in CHO cells by radioligand competition binding assays using [125I]iodocyanopindolol (ICYP)
ChEMBL 523 2 4 4 3.4 Oc1cc2c(cc1O)C(Cc1cc(I)c(O)c(I)c1)NCC2 10.1021/jm960208o
155521390 170010 0 None 22 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysisDisplacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysis
ChEMBL 586 21 6 8 2.0 CC(C)NC[C@H](O)COc1ccccc1CCC(=O)NCCNC(=O)CCc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
CHEMBL4450606 170010 0 None 22 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysisDisplacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysis
ChEMBL 586 21 6 8 2.0 CC(C)NC[C@H](O)COc1ccccc1CCC(=O)NCCNC(=O)CCc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
49864394 15445 0 None 6 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptorDisplacement of [3H]CGP12177 from human beta2 adrenoceptor
ChEMBL 322 4 4 5 2.6 O=c1[nH]c2c(O)ccc([C@@H](O)CNC3CCCCCC3)c2s1 10.1016/j.bmcl.2010.06.136
CHEMBL1221679 15445 0 None 6 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptorDisplacement of [3H]CGP12177 from human beta2 adrenoceptor
ChEMBL 322 4 4 5 2.6 O=c1[nH]c2c(O)ccc([C@@H](O)CNC3CCCCCC3)c2s1 10.1016/j.bmcl.2010.06.136
10512270 164796 9 None 5 2 Dog 7.0 pKi = 7.0 Binding
Binding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranes
ChEMBL 201 3 4 4 0.5 CNC[C@H](O)c1ccc(O)c(O)c1F 10.1021/jm990599h
CHEMBL42370 164796 9 None 5 2 Dog 7.0 pKi = 7.0 Binding
Binding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranes
ChEMBL 201 3 4 4 0.5 CNC[C@H](O)c1ccc(O)c(O)c1F 10.1021/jm990599h
1499 2052 43 None -8 17 Bovine 7.0 pKi = 7.0 Binding
Compound was evaluated for beta adrenergic binding affinity towards beta-2 receptor of bovine lungCompound was evaluated for beta adrenergic binding affinity towards beta-2 receptor of bovine lung
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm00084a006
3779 2052 43 None -8 17 Bovine 7.0 pKi = 7.0 Binding
Compound was evaluated for beta adrenergic binding affinity towards beta-2 receptor of bovine lungCompound was evaluated for beta adrenergic binding affinity towards beta-2 receptor of bovine lung
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm00084a006
536 2052 43 None -8 17 Bovine 7.0 pKi = 7.0 Binding
Compound was evaluated for beta adrenergic binding affinity towards beta-2 receptor of bovine lungCompound was evaluated for beta adrenergic binding affinity towards beta-2 receptor of bovine lung
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm00084a006
CHEMBL434 2052 43 None -8 17 Bovine 7.0 pKi = 7.0 Binding
Compound was evaluated for beta adrenergic binding affinity towards beta-2 receptor of bovine lungCompound was evaluated for beta adrenergic binding affinity towards beta-2 receptor of bovine lung
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm00084a006
DB01064 2052 43 None -8 17 Bovine 7.0 pKi = 7.0 Binding
Compound was evaluated for beta adrenergic binding affinity towards beta-2 receptor of bovine lungCompound was evaluated for beta adrenergic binding affinity towards beta-2 receptor of bovine lung
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm00084a006
3654892 6920 5 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cells
ChEMBL 515 9 1 6 3.9 Cc1ccc(C(C)C)c(OCC(O)CN2CCN(CCN3C(=O)c4cccc5cccc(c45)C3=O)CC2)c1 10.1016/j.bmcl.2010.04.009
CHEMBL1084773 6920 5 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cells
ChEMBL 515 9 1 6 3.9 Cc1ccc(C(C)C)c(OCC(O)CN2CCN(CCN3C(=O)c4cccc5cccc(c45)C3=O)CC2)c1 10.1016/j.bmcl.2010.04.009
1499 2052 43 None -8 17 Bovine 7.0 pKi = 7.0 Binding
Tested for binding affinity against beta-2 adrenergic receptor in bovine lung using [3H]DHA as radioligandTested for binding affinity against beta-2 adrenergic receptor in bovine lung using [3H]DHA as radioligand
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm00073a006
3779 2052 43 None -8 17 Bovine 7.0 pKi = 7.0 Binding
Tested for binding affinity against beta-2 adrenergic receptor in bovine lung using [3H]DHA as radioligandTested for binding affinity against beta-2 adrenergic receptor in bovine lung using [3H]DHA as radioligand
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm00073a006
536 2052 43 None -8 17 Bovine 7.0 pKi = 7.0 Binding
Tested for binding affinity against beta-2 adrenergic receptor in bovine lung using [3H]DHA as radioligandTested for binding affinity against beta-2 adrenergic receptor in bovine lung using [3H]DHA as radioligand
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm00073a006
CHEMBL434 2052 43 None -8 17 Bovine 7.0 pKi = 7.0 Binding
Tested for binding affinity against beta-2 adrenergic receptor in bovine lung using [3H]DHA as radioligandTested for binding affinity against beta-2 adrenergic receptor in bovine lung using [3H]DHA as radioligand
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm00073a006
DB01064 2052 43 None -8 17 Bovine 7.0 pKi = 7.0 Binding
Tested for binding affinity against beta-2 adrenergic receptor in bovine lung using [3H]DHA as radioligandTested for binding affinity against beta-2 adrenergic receptor in bovine lung using [3H]DHA as radioligand
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm00073a006
10472143 118759 0 None -2454 17 Human 6.0 pKi = 6.0 Binding
Binding affinity towards Beta-2 adrenergic receptorBinding affinity towards Beta-2 adrenergic receptor
ChEMBL 335 1 1 2 3.0 C[C@H]1C[C@H](C)N1C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)CC2N(C)C1 10.1021/jm020153s
CHEMBL343755 118759 0 None -2454 17 Human 6.0 pKi = 6.0 Binding
Binding affinity towards Beta-2 adrenergic receptorBinding affinity towards Beta-2 adrenergic receptor
ChEMBL 335 1 1 2 3.0 C[C@H]1C[C@H](C)N1C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)CC2N(C)C1 10.1021/jm020153s
1028 287 69 None -30 30 Dog 6.0 pKi = 6.0 Binding
Binding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranes
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm990599h
139148732 287 69 None -30 30 Dog 6.0 pKi = 6.0 Binding
Binding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranes
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm990599h
479 287 69 None -30 30 Dog 6.0 pKi = 6.0 Binding
Binding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranes
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm990599h
5816 287 69 None -30 30 Dog 6.0 pKi = 6.0 Binding
Binding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranes
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm990599h
CHEMBL679 287 69 None -30 30 Dog 6.0 pKi = 6.0 Binding
Binding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranes
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm990599h
DB00668 287 69 None -30 30 Dog 6.0 pKi = 6.0 Binding
Binding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranes
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm990599h
1960 2805 64 None -338 26 Dog 5.0 pKi = 5.0 Binding
Binding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranes
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm990599h
439260 2805 64 None -338 26 Dog 5.0 pKi = 5.0 Binding
Binding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranes
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm990599h
505 2805 64 None -338 26 Dog 5.0 pKi = 5.0 Binding
Binding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranes
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm990599h
CHEMBL1437 2805 64 None -338 26 Dog 5.0 pKi = 5.0 Binding
Binding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranes
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm990599h
DB00368 2805 64 None -338 26 Dog 5.0 pKi = 5.0 Binding
Binding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranes
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm990599h
44287337 150614 0 None 2 3 Human 7.0 pKi = 7.0 Binding
Ability to bind to human Beta-2 adrenergic receptor using membranes of stably transfected CHO cellsAbility to bind to human Beta-2 adrenergic receptor using membranes of stably transfected CHO cells
ChEMBL 378 9 4 5 2.5 C[C@H](Cc1ccc(OCC(=O)NO)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1016/S0960-894X(97)00266-7
CHEMBL39596 150614 0 None 2 3 Human 7.0 pKi = 7.0 Binding
Ability to bind to human Beta-2 adrenergic receptor using membranes of stably transfected CHO cellsAbility to bind to human Beta-2 adrenergic receptor using membranes of stably transfected CHO cells
ChEMBL 378 9 4 5 2.5 C[C@H](Cc1ccc(OCC(=O)NO)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1016/S0960-894X(97)00266-7
46221398 8601 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]cyanopindolol from human recombinant beta2 adrenergic receptor expressed in CHO cells by filtration assayDisplacement of [125I]cyanopindolol from human recombinant beta2 adrenergic receptor expressed in CHO cells by filtration assay
ChEMBL 448 10 4 4 4.7 CCCCc1cc2c(cc1CCCC)CC(NC[C@H](O)c1ccc(O)c3[nH]c(=O)ccc13)C2 10.1021/jm100068m
CHEMBL1095779 8601 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]cyanopindolol from human recombinant beta2 adrenergic receptor expressed in CHO cells by filtration assayDisplacement of [125I]cyanopindolol from human recombinant beta2 adrenergic receptor expressed in CHO cells by filtration assay
ChEMBL 448 10 4 4 4.7 CCCCc1cc2c(cc1CCCC)CC(NC[C@H](O)c1ccc(O)c3[nH]c(=O)ccc13)C2 10.1021/jm100068m
15221055 202700 0 None 5 2 Human 4.9 pKi = 4.9 Binding
Compound was tested for its binding affinity against beta2 adrenergic receptor in CHO cell membrane using [125I]iodocyanopindolol as the radioligand.Compound was tested for its binding affinity against beta2 adrenergic receptor in CHO cell membrane using [125I]iodocyanopindolol as the radioligand.
ChEMBL 368 9 3 5 3.1 C[C@H](Cc1ncc(CCC(=O)O)s1)NCC(O)c1cccc(Cl)c1 10.1016/0960-894X(96)00417-9
CHEMBL72060 202700 0 None 5 2 Human 4.9 pKi = 4.9 Binding
Compound was tested for its binding affinity against beta2 adrenergic receptor in CHO cell membrane using [125I]iodocyanopindolol as the radioligand.Compound was tested for its binding affinity against beta2 adrenergic receptor in CHO cell membrane using [125I]iodocyanopindolol as the radioligand.
ChEMBL 368 9 3 5 3.1 C[C@H](Cc1ncc(CCC(=O)O)s1)NCC(O)c1cccc(Cl)c1 10.1016/0960-894X(96)00417-9
10484263 58220 0 None -15 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-dihydroalprenolol from human beta2-adrenoceptor expressed in HEK cells after 4 hrsDisplacement of [3H]-dihydroalprenolol from human beta2-adrenoceptor expressed in HEK cells after 4 hrs
ChEMBL 639 16 6 6 6.5 O=C(Nc1ccccc1-c1ccccc1)NC1CCN(CCCCCCCCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1016/j.bmcl.2011.01.043
CHEMBL1683940 58220 0 None -15 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-dihydroalprenolol from human beta2-adrenoceptor expressed in HEK cells after 4 hrsDisplacement of [3H]-dihydroalprenolol from human beta2-adrenoceptor expressed in HEK cells after 4 hrs
ChEMBL 639 16 6 6 6.5 O=C(Nc1ccccc1-c1ccccc1)NC1CCN(CCCCCCCCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1016/j.bmcl.2011.01.043
73057083 103785 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 303 7 4 5 2.0 COc1ccc(CCNC[C@@H](O)c2cc(O)cc(O)c2)cc1 10.1016/j.bmc.2013.11.030
CHEMBL3099658 103785 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 303 7 4 5 2.0 COc1ccc(CCNC[C@@H](O)c2cc(O)cc(O)c2)cc1 10.1016/j.bmc.2013.11.030
73057083 103785 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 303 7 4 5 2.0 COc1ccc(CCNC[C@@H](O)c2cc(O)cc(O)c2)cc1 10.1016/j.bmc.2013.11.030
CHEMBL3099658 103785 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 303 7 4 5 2.0 COc1ccc(CCNC[C@@H](O)c2cc(O)cc(O)c2)cc1 10.1016/j.bmc.2013.11.030
10553602 126618 0 None - 1 Human 4.9 pKi = 4.9 Binding
Inhibition of I-iodocyanopindolol binding to human beta 2 adrenergic receptorsInhibition of I-iodocyanopindolol binding to human beta 2 adrenergic receptors
ChEMBL 506 10 6 8 0.9 CS(=O)(=O)Nc1cc([C@@H](O)CNC2CCN(c3ccc(C(=O)NCC(=O)O)cc3)CC2)ccc1O 10.1021/jm000544b
CHEMBL36568 126618 0 None - 1 Human 4.9 pKi = 4.9 Binding
Inhibition of I-iodocyanopindolol binding to human beta 2 adrenergic receptorsInhibition of I-iodocyanopindolol binding to human beta 2 adrenergic receptors
ChEMBL 506 10 6 8 0.9 CS(=O)(=O)Nc1cc([C@@H](O)CNC2CCN(c3ccc(C(=O)NCC(=O)O)cc3)CC2)ccc1O 10.1021/jm000544b
52943969 17598 0 None -1 3 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 517 9 3 8 4.3 CC(=O)Nc1cccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)c1 10.1016/j.bmcl.2010.08.039
CHEMBL1258825 17598 0 None -1 3 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 517 9 3 8 4.3 CC(=O)Nc1cccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)c1 10.1016/j.bmcl.2010.08.039
14485405 202483 0 None - 1 Mouse 5.9 pKi = 5.9 Binding
Ki value was determined by accumulation of c-AMP in S-49 mouse lymphoma cells (Beta2).Ki value was determined by accumulation of c-AMP in S-49 mouse lymphoma cells (Beta2).
ChEMBL 441 13 4 5 3.9 CC(=O)Nc1ccc(OCC(O)CNC(C)CCCCC(=O)Nc2ccc(C)cc2)cc1 10.1021/jm00163a036
CHEMBL70809 202483 0 None - 1 Mouse 5.9 pKi = 5.9 Binding
Ki value was determined by accumulation of c-AMP in S-49 mouse lymphoma cells (Beta2).Ki value was determined by accumulation of c-AMP in S-49 mouse lymphoma cells (Beta2).
ChEMBL 441 13 4 5 3.9 CC(=O)Nc1ccc(OCC(O)CNC(C)CCCCC(=O)Nc2ccc(C)cc2)cc1 10.1021/jm00163a036
15054189 193901 0 None -91 3 Human 5.9 pKi = 5.9 Binding
Binding affinity towards Beta-2 adrenergic receptor in human peripheral mononuclear leukocyte membranes using [125I]pindololBinding affinity towards Beta-2 adrenergic receptor in human peripheral mononuclear leukocyte membranes using [125I]pindolol
ChEMBL 433 6 2 6 2.4 COc1ccccc1N1CCN(CCCn2c(=O)[nH]c3c([nH]c4ccccc43)c2=O)CC1 10.1021/jm00110a014
CHEMBL55528 193901 0 None -91 3 Human 5.9 pKi = 5.9 Binding
Binding affinity towards Beta-2 adrenergic receptor in human peripheral mononuclear leukocyte membranes using [125I]pindololBinding affinity towards Beta-2 adrenergic receptor in human peripheral mononuclear leukocyte membranes using [125I]pindolol
ChEMBL 433 6 2 6 2.4 COc1ccccc1N1CCN(CCCn2c(=O)[nH]c3c([nH]c4ccccc43)c2=O)CC1 10.1021/jm00110a014
46221397 8600 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]cyanopindolol from human recombinant beta2 adrenergic receptor expressed in CHO cells by filtration assayDisplacement of [125I]cyanopindolol from human recombinant beta2 adrenergic receptor expressed in CHO cells by filtration assay
ChEMBL 420 8 4 4 3.9 CCCc1cc2c(cc1CCC)CC(NC[C@H](O)c1ccc(O)c3[nH]c(=O)ccc13)C2 10.1021/jm100068m
CHEMBL1095778 8600 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]cyanopindolol from human recombinant beta2 adrenergic receptor expressed in CHO cells by filtration assayDisplacement of [125I]cyanopindolol from human recombinant beta2 adrenergic receptor expressed in CHO cells by filtration assay
ChEMBL 420 8 4 4 3.9 CCCc1cc2c(cc1CCC)CC(NC[C@H](O)c1ccc(O)c3[nH]c(=O)ccc13)C2 10.1021/jm100068m
118710945 113243 0 None 2 3 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assay
ChEMBL 398 6 4 5 3.8 CCc1cccc([C@H]2CCC[C@H]2NC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)c1 10.1016/j.bmcl.2014.06.014
CHEMBL3323663 113243 0 None 2 3 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assay
ChEMBL 398 6 4 5 3.8 CCc1cccc([C@H]2CCC[C@H]2NC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)c1 10.1016/j.bmcl.2014.06.014
44328703 10118 0 None 1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assay
ChEMBL 241 6 4 5 0.8 CC(C)NC[C@H](O)COc1ccc(O)c(O)c1 10.1021/acs.jmedchem.9b00349
CHEMBL1160694 10118 0 None 1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assay
ChEMBL 241 6 4 5 0.8 CC(C)NC[C@H](O)COc1ccc(O)c(O)c1 10.1021/acs.jmedchem.9b00349
10173878 111954 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assayDisplacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assay
ChEMBL 459 10 5 6 4.2 CCOc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 10.1016/j.bmcl.2014.04.095
CHEMBL3298327 111954 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assayDisplacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assay
ChEMBL 459 10 5 6 4.2 CCOc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 10.1016/j.bmcl.2014.04.095
56677231 63293 0 None 234 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 367 7 4 5 3.5 COc1ccc(C[C@H](C)NC[C@H](O)c2cc(O)cc(O)c2)c2ccccc12 10.1016/j.bmc.2013.11.030
CHEMBL1800934 63293 0 None 234 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 367 7 4 5 3.5 COc1ccc(C[C@H](C)NC[C@H](O)c2cc(O)cc(O)c2)c2ccccc12 10.1016/j.bmc.2013.11.030
56677231 63293 0 None 234 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 367 7 4 5 3.5 COc1ccc(C[C@H](C)NC[C@H](O)c2cc(O)cc(O)c2)c2ccccc12 10.1016/j.bmc.2013.11.030
CHEMBL1800934 63293 0 None 234 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 367 7 4 5 3.5 COc1ccc(C[C@H](C)NC[C@H](O)c2cc(O)cc(O)c2)c2ccccc12 10.1016/j.bmc.2013.11.030
12353620 202631 1 None 66 2 Bovine 6.9 pKi = 6.9 Binding
Compound was evaluated for beta adrenergic binding affinity towards beta-2 receptor of bovine lungCompound was evaluated for beta adrenergic binding affinity towards beta-2 receptor of bovine lung
ChEMBL 195 0 4 4 0.4 N[C@@H]1CCc2c(ccc(O)c2O)[C@H]1O 10.1021/jm00084a006
CHEMBL7160 202631 1 None 66 2 Bovine 6.9 pKi = 6.9 Binding
Compound was evaluated for beta adrenergic binding affinity towards beta-2 receptor of bovine lungCompound was evaluated for beta adrenergic binding affinity towards beta-2 receptor of bovine lung
ChEMBL 195 0 4 4 0.4 N[C@@H]1CCc2c(ccc(O)c2O)[C@H]1O 10.1021/jm00084a006
46889643 6557 0 None -4 3 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cells
ChEMBL 483 7 2 5 4.1 O=C1c2cccc3cccc(c23)C(=O)N1CC1CCN(CC(O)COc2cccc3[nH]ccc23)CC1 10.1016/j.bmcl.2010.04.009
CHEMBL1083368 6557 0 None -4 3 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cells
ChEMBL 483 7 2 5 4.1 O=C1c2cccc3cccc(c23)C(=O)N1CC1CCN(CC(O)COc2cccc3[nH]ccc23)CC1 10.1016/j.bmcl.2010.04.009
10132882 94060 0 None -1 2 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]iodocyanopindolol from human adrenergic beta-2 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human adrenergic beta-2 receptor expressed in CHO cells
ChEMBL 355 8 2 6 3.2 Cc1nc(-c2ccc(OCCNC[C@H](O)c3cccnc3)cc2)cs1 10.1016/j.bmcl.2007.06.072
CHEMBL251599 94060 0 None -1 2 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]iodocyanopindolol from human adrenergic beta-2 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human adrenergic beta-2 receptor expressed in CHO cells
ChEMBL 355 8 2 6 3.2 Cc1nc(-c2ccc(OCCNC[C@H](O)c3cccnc3)cc2)cs1 10.1016/j.bmcl.2007.06.072
44444195 94087 0 None -10 3 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]iodocyanopindolol from human cloned adrenergic beta-2 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human cloned adrenergic beta-2 receptor expressed in CHO cells
ChEMBL 548 13 4 7 4.3 COc1ccc([C@H](CCc2ccc(Cl)cc2)NC[C@H](O)Cc2ccc(O)c(NS(C)(=O)=O)c2)cc1OC 10.1016/j.bmcl.2007.05.030
CHEMBL251764 94087 0 None -10 3 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]iodocyanopindolol from human cloned adrenergic beta-2 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human cloned adrenergic beta-2 receptor expressed in CHO cells
ChEMBL 548 13 4 7 4.3 COc1ccc([C@H](CCc2ccc(Cl)cc2)NC[C@H](O)Cc2ccc(O)c(NS(C)(=O)=O)c2)cc1OC 10.1016/j.bmcl.2007.05.030
155534529 171387 0 None 2 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assay
ChEMBL 467 14 4 7 3.7 COc1cc(CCNC[C@@H](O)COc2ccc(O)c(O)c2)ccc1OCCCc1ccccc1 10.1021/acs.jmedchem.9b00349
CHEMBL4470694 171387 0 None 2 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assay
ChEMBL 467 14 4 7 3.7 COc1cc(CCNC[C@@H](O)COc2ccc(O)c(O)c2)ccc1OCCCc1ccccc1 10.1021/acs.jmedchem.9b00349
6603820 95317 13 None -128 13 Human 5.9 pKi = 5.9 Binding
Binding affinity against Beta-2 adrenergic receptorBinding affinity against Beta-2 adrenergic receptor
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1021/jm00018a002
CHEMBL25856 95317 13 None -128 13 Human 5.9 pKi = 5.9 Binding
Binding affinity against Beta-2 adrenergic receptorBinding affinity against Beta-2 adrenergic receptor
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1021/jm00018a002
53319789 58221 0 None 1 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-dihydroalprenolol from human beta2-adrenoceptor expressed in HEK cells after 4 hrsDisplacement of [3H]-dihydroalprenolol from human beta2-adrenoceptor expressed in HEK cells after 4 hrs
ChEMBL 667 16 5 6 7.1 O=C(Nc1ccccc1-c1ccccc1)O[C@H]1C[N+]2(CCCCCCCCCNCC(O)c3ccc(O)c4[nH]c(=O)ccc34)CCC1CC2 10.1016/j.bmcl.2011.01.043
CHEMBL1683941 58221 0 None 1 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-dihydroalprenolol from human beta2-adrenoceptor expressed in HEK cells after 4 hrsDisplacement of [3H]-dihydroalprenolol from human beta2-adrenoceptor expressed in HEK cells after 4 hrs
ChEMBL 667 16 5 6 7.1 O=C(Nc1ccccc1-c1ccccc1)O[C@H]1C[N+]2(CCCCCCCCCNCC(O)c3ccc(O)c4[nH]c(=O)ccc34)CCC1CC2 10.1016/j.bmcl.2011.01.043
15221053 202880 0 None 2 3 Human 5.9 pKi = 5.9 Binding
Compound was tested for its binding affinity against beta2 adrenergic receptor in CHO cell membrane using [125I]iodocyanopindolol as the radioligand.Compound was tested for its binding affinity against beta2 adrenergic receptor in CHO cell membrane using [125I]iodocyanopindolol as the radioligand.
ChEMBL 364 11 3 6 2.1 C[C@H](Cc1ncc(CCC(=O)O)s1)NC[C@H](O)COc1ccccc1 10.1016/0960-894X(96)00417-9
CHEMBL73220 202880 0 None 2 3 Human 5.9 pKi = 5.9 Binding
Compound was tested for its binding affinity against beta2 adrenergic receptor in CHO cell membrane using [125I]iodocyanopindolol as the radioligand.Compound was tested for its binding affinity against beta2 adrenergic receptor in CHO cell membrane using [125I]iodocyanopindolol as the radioligand.
ChEMBL 364 11 3 6 2.1 C[C@H](Cc1ncc(CCC(=O)O)s1)NC[C@H](O)COc1ccccc1 10.1016/0960-894X(96)00417-9
10287658 111750 0 None 25 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assay
ChEMBL 408 10 5 6 3.5 COc1ccc(Nc2ccc(CCNCC(O)c3ccc(O)c(CO)c3)cc2)cc1 10.1016/j.bmcl.2014.04.069
CHEMBL3290984 111750 0 None 25 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assay
ChEMBL 408 10 5 6 3.5 COc1ccc(Nc2ccc(CCNCC(O)c3ccc(O)c(CO)c3)cc2)cc1 10.1016/j.bmcl.2014.04.069
90644141 111762 0 None 6 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assay
ChEMBL 396 9 5 5 3.6 OCc1cc(C(O)CNCCc2ccc(Nc3ccc(F)cc3)cc2)ccc1O 10.1016/j.bmcl.2014.04.069
CHEMBL3290995 111762 0 None 6 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assay
ChEMBL 396 9 5 5 3.6 OCc1cc(C(O)CNCCc2ccc(Nc3ccc(F)cc3)cc2)ccc1O 10.1016/j.bmcl.2014.04.069
90644145 111739 0 None - 1 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assay
ChEMBL 446 9 4 5 4.1 OCc1cc(C(O)CNCCc2ccc(N3CCC(c4ccccc4)CC3)cc2)ccc1O 10.1016/j.bmcl.2014.04.069
CHEMBL3290974 111739 0 None - 1 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assay
ChEMBL 446 9 4 5 4.1 OCc1cc(C(O)CNCCc2ccc(N3CCC(c4ccccc4)CC3)cc2)ccc1O 10.1016/j.bmcl.2014.04.069
1155 1592 45 None 2 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-CGP12177 from human recombinant beta2 adrenoceptor expressed in HEK293 cells after 1 hr by scintillation counting analysisDisplacement of [3H]-CGP12177 from human recombinant beta2 adrenoceptor expressed in HEK293 cells after 1 hr by scintillation counting analysis
ChEMBL 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 10.1021/ml400312j
3343 1592 45 None 2 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-CGP12177 from human recombinant beta2 adrenoceptor expressed in HEK293 cells after 1 hr by scintillation counting analysisDisplacement of [3H]-CGP12177 from human recombinant beta2 adrenoceptor expressed in HEK293 cells after 1 hr by scintillation counting analysis
ChEMBL 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 10.1021/ml400312j
557 1592 45 None 2 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-CGP12177 from human recombinant beta2 adrenoceptor expressed in HEK293 cells after 1 hr by scintillation counting analysisDisplacement of [3H]-CGP12177 from human recombinant beta2 adrenoceptor expressed in HEK293 cells after 1 hr by scintillation counting analysis
ChEMBL 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 10.1021/ml400312j
CHEMBL32800 1592 45 None 2 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-CGP12177 from human recombinant beta2 adrenoceptor expressed in HEK293 cells after 1 hr by scintillation counting analysisDisplacement of [3H]-CGP12177 from human recombinant beta2 adrenoceptor expressed in HEK293 cells after 1 hr by scintillation counting analysis
ChEMBL 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 10.1021/ml400312j
DB01288 1592 45 None 2 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-CGP12177 from human recombinant beta2 adrenoceptor expressed in HEK293 cells after 1 hr by scintillation counting analysisDisplacement of [3H]-CGP12177 from human recombinant beta2 adrenoceptor expressed in HEK293 cells after 1 hr by scintillation counting analysis
ChEMBL 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 10.1021/ml400312j
10081581 11080 0 None -2 2 Bovine 5.9 pKi = 5.9 Binding
Binding affinity against beta-2-adrenergic receptor in bovine lungBinding affinity against beta-2-adrenergic receptor in bovine lung
ChEMBL 202 6 2 4 1.1 CC/C=N/OCC(O)CNC(C)(C)C 10.1021/jm00036a018
CHEMBL1178704 11080 0 None -2 2 Bovine 5.9 pKi = 5.9 Binding
Binding affinity against beta-2-adrenergic receptor in bovine lungBinding affinity against beta-2-adrenergic receptor in bovine lung
ChEMBL 202 6 2 4 1.1 CC/C=N/OCC(O)CNC(C)(C)C 10.1021/jm00036a018
CHEMBL38033 11080 0 None -2 2 Bovine 5.9 pKi = 5.9 Binding
Binding affinity against beta-2-adrenergic receptor in bovine lungBinding affinity against beta-2-adrenergic receptor in bovine lung
ChEMBL 202 6 2 4 1.1 CC/C=N/OCC(O)CNC(C)(C)C 10.1021/jm00036a018
46889642 6862 0 None 3 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cells
ChEMBL 483 7 2 5 4.1 O=C1c2cccc3cccc(c23)C(=O)N1CC1CCN(CC(O)COc2ccc3[nH]ccc3c2)CC1 10.1016/j.bmcl.2010.04.009
CHEMBL1084527 6862 0 None 3 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cells
ChEMBL 483 7 2 5 4.1 O=C1c2cccc3cccc(c23)C(=O)N1CC1CCN(CC(O)COc2ccc3[nH]ccc3c2)CC1 10.1016/j.bmcl.2010.04.009
53380559 63295 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]CGP-12177 from human beta2-adrenergic receptor expressed in HEK 293 cellsDisplacement of [3H]CGP-12177 from human beta2-adrenergic receptor expressed in HEK 293 cells
ChEMBL 317 7 5 5 2.4 CC[C@H](Cc1ccc(O)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2009.11.062
CHEMBL1800936 63295 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]CGP-12177 from human beta2-adrenergic receptor expressed in HEK 293 cellsDisplacement of [3H]CGP-12177 from human beta2-adrenergic receptor expressed in HEK 293 cells
ChEMBL 317 7 5 5 2.4 CC[C@H](Cc1ccc(O)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2009.11.062
145990586 166279 0 None 1 11 Human 7.9 pKi = 7.9 Binding
Binding affinity to andrenergic beta2 receptor (unknown origin) assessed as inhibition of radioligand binding by radioligand competition binding assayBinding affinity to andrenergic beta2 receptor (unknown origin) assessed as inhibition of radioligand binding by radioligand competition binding assay
ChEMBL 297 2 2 4 2.6 COc1cc2c3c(c1OC)-c1ccccc1[C@@H](O)[C@@H]3NCC2 10.1039/C7MD00656J
CHEMBL4285281 166279 0 None 1 11 Human 7.9 pKi = 7.9 Binding
Binding affinity to andrenergic beta2 receptor (unknown origin) assessed as inhibition of radioligand binding by radioligand competition binding assayBinding affinity to andrenergic beta2 receptor (unknown origin) assessed as inhibition of radioligand binding by radioligand competition binding assay
ChEMBL 297 2 2 4 2.6 COc1cc2c3c(c1OC)-c1ccccc1[C@@H](O)[C@@H]3NCC2 10.1039/C7MD00656J
46889700 6982 0 None 18 3 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cells
ChEMBL 472 7 1 5 4.5 CC(C)c1ccccc1OCC(O)CN1CCC(N2C(=O)c3cccc4cccc(c34)C2=O)CC1 10.1016/j.bmcl.2010.04.009
CHEMBL1085013 6982 0 None 18 3 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cells
ChEMBL 472 7 1 5 4.5 CC(C)c1ccccc1OCC(O)CN1CCC(N2C(=O)c3cccc4cccc(c34)C2=O)CC1 10.1016/j.bmcl.2010.04.009
10326800 58218 1 None -70 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-dihydroalprenolol from human beta2-adrenoceptor expressed in HEK cells after 4 hrsDisplacement of [3H]-dihydroalprenolol from human beta2-adrenoceptor expressed in HEK cells after 4 hrs
ChEMBL 640 16 5 7 7.0 O=C(Nc1ccccc1-c1ccccc1)OC1CCN(CCCCCCCCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1016/j.bmcl.2011.01.043
CHEMBL1683938 58218 1 None -70 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-dihydroalprenolol from human beta2-adrenoceptor expressed in HEK cells after 4 hrsDisplacement of [3H]-dihydroalprenolol from human beta2-adrenoceptor expressed in HEK cells after 4 hrs
ChEMBL 640 16 5 7 7.0 O=C(Nc1ccccc1-c1ccccc1)OC1CCN(CCCCCCCCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1016/j.bmcl.2011.01.043
127045854 139021 0 None 13 6 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cellsDisplacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells
ChEMBL 492 12 4 7 3.6 COc1cc(CCNC[C@@H](O)c2ccc(O)c3c2OCC(=O)N3)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
CHEMBL3797205 139021 0 None 13 6 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cellsDisplacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells
ChEMBL 492 12 4 7 3.6 COc1cc(CCNC[C@@H](O)c2ccc(O)c3c2OCC(=O)N3)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
53380558 63302 2 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 367 7 4 5 3.5 COc1ccc(C[C@@H](C)NC[C@H](O)c2cc(O)cc(O)c2)c2ccccc12 10.1016/j.bmc.2013.11.030
CHEMBL1800963 63302 2 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 367 7 4 5 3.5 COc1ccc(C[C@@H](C)NC[C@H](O)c2cc(O)cc(O)c2)c2ccccc12 10.1016/j.bmc.2013.11.030
53380558 63302 2 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 367 7 4 5 3.5 COc1ccc(C[C@@H](C)NC[C@H](O)c2cc(O)cc(O)c2)c2ccccc12 10.1016/j.bmc.2013.11.030
CHEMBL1800963 63302 2 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 367 7 4 5 3.5 COc1ccc(C[C@@H](C)NC[C@H](O)c2cc(O)cc(O)c2)c2ccccc12 10.1016/j.bmc.2013.11.030
44423640 141511 0 None 4 3 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]CYP from human adrenergic beta 2 receptor transfected in CHO cells in presence of 100 uM GTPDisplacement of [125I]CYP from human adrenergic beta 2 receptor transfected in CHO cells in presence of 100 uM GTP
ChEMBL 398 9 3 6 2.2 C[C@H](Cc1ccc(OCC(=O)O)cc1)NC[C@H](O)c1cc(Br)no1 10.1016/j.bmc.2007.01.056
CHEMBL387851 141511 0 None 4 3 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]CYP from human adrenergic beta 2 receptor transfected in CHO cells in presence of 100 uM GTPDisplacement of [125I]CYP from human adrenergic beta 2 receptor transfected in CHO cells in presence of 100 uM GTP
ChEMBL 398 9 3 6 2.2 C[C@H](Cc1ccc(OCC(=O)O)cc1)NC[C@H](O)c1cc(Br)no1 10.1016/j.bmc.2007.01.056
129896798 182075 32 None -1 3 Human 5.9 pKi = 5.9 Binding
Binding affinity to beta2 adrenoceptor (unknown origin)Binding affinity to beta2 adrenoceptor (unknown origin)
ChEMBL 366 7 2 3 4.5 Cc1ccc(CN(CC(O)COc2cccc3[nH]ccc23)C(C)(C)C)cc1 10.1021/acs.jmedchem.0c01450
CHEMBL4789047 182075 32 None -1 3 Human 5.9 pKi = 5.9 Binding
Binding affinity to beta2 adrenoceptor (unknown origin)Binding affinity to beta2 adrenoceptor (unknown origin)
ChEMBL 366 7 2 3 4.5 Cc1ccc(CN(CC(O)COc2cccc3[nH]ccc23)C(C)(C)C)cc1 10.1021/acs.jmedchem.0c01450
155524756 170427 0 None -1 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranesDisplacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranes
ChEMBL 510 19 3 9 3.2 COCCc1ccc(OC[C@H](O)CNCCc2ccc(OCCSSCCN)c(OC)c2)cc1 10.1016/j.bmc.2019.05.034
CHEMBL4456505 170427 0 None -1 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranesDisplacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranes
ChEMBL 510 19 3 9 3.2 COCCc1ccc(OC[C@H](O)CNCCc2ccc(OCCSSCCN)c(OC)c2)cc1 10.1016/j.bmc.2019.05.034
52941603 17102 0 None 1 3 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 573 9 2 9 3.8 O=C(c1cccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)c1)N1CCOCC1 10.1016/j.bmcl.2010.08.039
CHEMBL1257204 17102 0 None 1 3 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 573 9 2 9 3.8 O=C(c1cccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)c1)N1CCOCC1 10.1016/j.bmcl.2010.08.039
46889701 6983 0 None 1 3 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cells
ChEMBL 500 9 2 6 4.0 C=CCc1ccccc1OCC(O)CN1CCC(CN2C(=O)c3cccc4cc(O)cc(c34)C2=O)CC1 10.1016/j.bmcl.2010.04.009
CHEMBL1085014 6983 0 None 1 3 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cells
ChEMBL 500 9 2 6 4.0 C=CCc1ccccc1OCC(O)CN1CCC(CN2C(=O)c3cccc4cc(O)cc(c34)C2=O)CC1 10.1016/j.bmcl.2010.04.009
3486 3096 51 None -5 11 Mouse 4.9 pKi = 4.9 Binding
Ki value was determined by accumulation of c-AMP in S-49 mouse lymphoma cells (Beta2).Ki value was determined by accumulation of c-AMP in S-49 mouse lymphoma cells (Beta2).
ChEMBL 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C 10.1021/jm00163a036
4883 3096 51 None -5 11 Mouse 4.9 pKi = 4.9 Binding
Ki value was determined by accumulation of c-AMP in S-49 mouse lymphoma cells (Beta2).Ki value was determined by accumulation of c-AMP in S-49 mouse lymphoma cells (Beta2).
ChEMBL 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C 10.1021/jm00163a036
555 3096 51 None -5 11 Mouse 4.9 pKi = 4.9 Binding
Ki value was determined by accumulation of c-AMP in S-49 mouse lymphoma cells (Beta2).Ki value was determined by accumulation of c-AMP in S-49 mouse lymphoma cells (Beta2).
ChEMBL 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C 10.1021/jm00163a036
CHEMBL6995 3096 51 None -5 11 Mouse 4.9 pKi = 4.9 Binding
Ki value was determined by accumulation of c-AMP in S-49 mouse lymphoma cells (Beta2).Ki value was determined by accumulation of c-AMP in S-49 mouse lymphoma cells (Beta2).
ChEMBL 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C 10.1021/jm00163a036
DB01297 3096 51 None -5 11 Mouse 4.9 pKi = 4.9 Binding
Ki value was determined by accumulation of c-AMP in S-49 mouse lymphoma cells (Beta2).Ki value was determined by accumulation of c-AMP in S-49 mouse lymphoma cells (Beta2).
ChEMBL 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C 10.1021/jm00163a036
443372 10123 23 None 1 3 Golden hamster 6.9 pKi = 6.9 Binding
Displacement of [125I](-)-iodopindolol from adrenergic beta2 receptor in Syrian hamster DDT1 MF2 cellsDisplacement of [125I](-)-iodopindolol from adrenergic beta2 receptor in Syrian hamster DDT1 MF2 cells
ChEMBL 211 4 4 4 1.1 CC(C)NC[C@H](O)c1ccc(O)c(O)c1 10.1021/jm800613s
CHEMBL1160723 10123 23 None 1 3 Golden hamster 6.9 pKi = 6.9 Binding
Displacement of [125I](-)-iodopindolol from adrenergic beta2 receptor in Syrian hamster DDT1 MF2 cellsDisplacement of [125I](-)-iodopindolol from adrenergic beta2 receptor in Syrian hamster DDT1 MF2 cells
ChEMBL 211 4 4 4 1.1 CC(C)NC[C@H](O)c1ccc(O)c(O)c1 10.1021/jm800613s
CHEMBL2062275 10123 23 None 1 3 Golden hamster 6.9 pKi = 6.9 Binding
Displacement of [125I](-)-iodopindolol from adrenergic beta2 receptor in Syrian hamster DDT1 MF2 cellsDisplacement of [125I](-)-iodopindolol from adrenergic beta2 receptor in Syrian hamster DDT1 MF2 cells
ChEMBL 211 4 4 4 1.1 CC(C)NC[C@H](O)c1ccc(O)c(O)c1 10.1021/jm800613s
2810 67245 50 None 1 2 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 213 4 2 2 2.4 CC(C)NCC(O)c1ccccc1Cl nan
CHEMBL1902627 67245 50 None 1 2 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 213 4 2 2 2.4 CC(C)NCC(O)c1ccccc1Cl nan
52943968 17597 0 None -3 3 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 518 9 4 8 3.8 NC(=O)Nc1cccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)c1 10.1016/j.bmcl.2010.08.039
CHEMBL1258824 17597 0 None -3 3 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 518 9 4 8 3.8 NC(=O)Nc1cccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)c1 10.1016/j.bmcl.2010.08.039
11776640 13420 0 None -2 3 Guinea pig 5.9 pKi = 5.9 Binding
Binding affinity against Beta-2 adrenergic receptor was measured using [125I]CYP as radioligandBinding affinity against Beta-2 adrenergic receptor was measured using [125I]CYP as radioligand
ChEMBL 245 3 1 5 1.1 CCCc1cnc2c(N3CCNCC3)nccn12 10.1021/jm00099a012
CHEMBL1193824 13420 0 None -2 3 Guinea pig 5.9 pKi = 5.9 Binding
Binding affinity against Beta-2 adrenergic receptor was measured using [125I]CYP as radioligandBinding affinity against Beta-2 adrenergic receptor was measured using [125I]CYP as radioligand
ChEMBL 245 3 1 5 1.1 CCCc1cnc2c(N3CCNCC3)nccn12 10.1021/jm00099a012
CHEMBL545293 13420 0 None -2 3 Guinea pig 5.9 pKi = 5.9 Binding
Binding affinity against Beta-2 adrenergic receptor was measured using [125I]CYP as radioligandBinding affinity against Beta-2 adrenergic receptor was measured using [125I]CYP as radioligand
ChEMBL 245 3 1 5 1.1 CCCc1cnc2c(N3CCNCC3)nccn12 10.1021/jm00099a012
44312269 202724 0 None -2 3 Human 4.9 pKi = 4.9 Binding
Compound was tested for its binding affinity against beta2 adrenergic receptor in CHO cell membrane using [125I]iodocyanopindolol as the radioligand.Compound was tested for its binding affinity against beta2 adrenergic receptor in CHO cell membrane using [125I]iodocyanopindolol as the radioligand.
ChEMBL 382 10 3 5 3.5 C[C@H](Cc1ncc(CCCC(=O)O)s1)NCC(O)c1cccc(Cl)c1 10.1016/0960-894X(96)00417-9
CHEMBL72168 202724 0 None -2 3 Human 4.9 pKi = 4.9 Binding
Compound was tested for its binding affinity against beta2 adrenergic receptor in CHO cell membrane using [125I]iodocyanopindolol as the radioligand.Compound was tested for its binding affinity against beta2 adrenergic receptor in CHO cell membrane using [125I]iodocyanopindolol as the radioligand.
ChEMBL 382 10 3 5 3.5 C[C@H](Cc1ncc(CCCC(=O)O)s1)NCC(O)c1cccc(Cl)c1 10.1016/0960-894X(96)00417-9
44112 120764 41 None -1 7 Human 7.9 pKi = 7.9 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 380 7 2 4 4.5 Cc1cc2c(OCC(CNC(C)(C)C)OC(=O)c3ccccc3)cccc2[nH]1 nan
CHEMBL357995 120764 41 None -1 7 Human 7.9 pKi = 7.9 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 380 7 2 4 4.5 Cc1cc2c(OCC(CNC(C)(C)C)OC(=O)c3ccccc3)cccc2[nH]1 nan
24936626 17212 0 None -1 3 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 506 9 4 9 3.6 OCc1cc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)ccc1O 10.1016/j.bmcl.2010.08.039
CHEMBL1257555 17212 0 None -1 3 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 506 9 4 9 3.6 OCc1cc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)ccc1O 10.1016/j.bmcl.2010.08.039
52946537 17526 0 None 2 3 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 384 7 2 7 2.7 OC(CNC1CCN(c2ncnc3ccsc23)CC1)COc1ccccc1 10.1016/j.bmcl.2010.08.039
CHEMBL1258599 17526 0 None 2 3 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 384 7 2 7 2.7 OC(CNC1CCN(c2ncnc3ccsc23)CC1)COc1ccccc1 10.1016/j.bmcl.2010.08.039
5806 102690 16 None -2 3 Bovine 6.9 pKi = 6.9 Binding
Binding affinity against beta-2-adrenergic receptor in bovine lungBinding affinity against beta-2-adrenergic receptor in bovine lung
ChEMBL 247 4 2 2 3.0 CC(C)NCC(O)c1ccc(Cl)c(Cl)c1 10.1021/jm00036a018
CHEMBL30816 102690 16 None -2 3 Bovine 6.9 pKi = 6.9 Binding
Binding affinity against beta-2-adrenergic receptor in bovine lungBinding affinity against beta-2-adrenergic receptor in bovine lung
ChEMBL 247 4 2 2 3.0 CC(C)NCC(O)c1ccc(Cl)c(Cl)c1 10.1021/jm00036a018
44331346 206638 0 None 46 2 Human 6.9 pKi = 6.9 Binding
Binding affinity of compound against Beta-2 adrenergic receptor was determinedBinding affinity of compound against Beta-2 adrenergic receptor was determined
ChEMBL 638 17 5 8 4.2 CCCCCCCCC(=O)Nc1ccc(S(=O)(=O)N2CCC(CNC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)CC2)cc1 10.1016/s0960-894x(02)00608-x
CHEMBL99599 206638 0 None 46 2 Human 6.9 pKi = 6.9 Binding
Binding affinity of compound against Beta-2 adrenergic receptor was determinedBinding affinity of compound against Beta-2 adrenergic receptor was determined
ChEMBL 638 17 5 8 4.2 CCCCCCCCC(=O)Nc1ccc(S(=O)(=O)N2CCC(CNC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)CC2)cc1 10.1016/s0960-894x(02)00608-x
172745 99648 7 None 2 6 Dog 6.9 pKi = 6.9 Binding
Binding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranes
ChEMBL 187 2 4 4 0.2 NCC(O)c1ccc(O)c(O)c1F 10.1021/jm990599h
CHEMBL287587 99648 7 None 2 6 Dog 6.9 pKi = 6.9 Binding
Binding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranes
ChEMBL 187 2 4 4 0.2 NCC(O)c1ccc(O)c(O)c1F 10.1021/jm990599h
10012704 11102 0 None -1 2 Bovine 5.9 pKi = 5.9 Binding
Binding affinity against beta-2-adrenergic receptor in bovine lungBinding affinity against beta-2-adrenergic receptor in bovine lung
ChEMBL 188 5 2 4 0.8 CCO/N=C/C(O)CNC(C)(C)C 10.1021/jm00036a018
CHEMBL1178768 11102 0 None -1 2 Bovine 5.9 pKi = 5.9 Binding
Binding affinity against beta-2-adrenergic receptor in bovine lungBinding affinity against beta-2-adrenergic receptor in bovine lung
ChEMBL 188 5 2 4 0.8 CCO/N=C/C(O)CNC(C)(C)C 10.1021/jm00036a018
CHEMBL39987 11102 0 None -1 2 Bovine 5.9 pKi = 5.9 Binding
Binding affinity against beta-2-adrenergic receptor in bovine lungBinding affinity against beta-2-adrenergic receptor in bovine lung
ChEMBL 188 5 2 4 0.8 CCO/N=C/C(O)CNC(C)(C)C 10.1021/jm00036a018
155564274 174839 0 None -19 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranesDisplacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranes
ChEMBL 643 19 4 11 3.7 Cn1cc(C(F)(F)F)nc1-c1ccc(OC[C@@H](O)CNCCOc2ccc(OCCCSSCCN)c(C(N)=O)c2)cc1 10.1016/j.bmc.2019.05.034
CHEMBL4576034 174839 0 None -19 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranesDisplacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranes
ChEMBL 643 19 4 11 3.7 Cn1cc(C(F)(F)F)nc1-c1ccc(OC[C@@H](O)CNCCOc2ccc(OCCCSSCCN)c(C(N)=O)c2)cc1 10.1016/j.bmc.2019.05.034
14485412 102448 0 None - 1 Mouse 6.8 pKi = 6.8 Binding
Ki value was determined by accumulation of c-AMP in S-49 mouse lymphoma cells (Beta2).Ki value was determined by accumulation of c-AMP in S-49 mouse lymphoma cells (Beta2).
ChEMBL 495 13 4 5 4.6 CC(=O)Nc1ccc(OC[C@@H](O)CN[C@H](C)CCCCC(=O)Nc2ccc(C(F)(F)F)cc2)cc1 10.1021/jm00163a036
CHEMBL306237 102448 0 None - 1 Mouse 6.8 pKi = 6.8 Binding
Ki value was determined by accumulation of c-AMP in S-49 mouse lymphoma cells (Beta2).Ki value was determined by accumulation of c-AMP in S-49 mouse lymphoma cells (Beta2).
ChEMBL 495 13 4 5 4.6 CC(=O)Nc1ccc(OC[C@@H](O)CN[C@H](C)CCCCC(=O)Nc2ccc(C(F)(F)F)cc2)cc1 10.1021/jm00163a036
118710944 113242 0 None 2 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assay
ChEMBL 384 5 4 5 3.6 Cc1ccc([C@H]2CCC[C@H]2NC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)cc1 10.1016/j.bmcl.2014.06.014
CHEMBL3323662 113242 0 None 2 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assay
ChEMBL 384 5 4 5 3.6 Cc1ccc([C@H]2CCC[C@H]2NC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)cc1 10.1016/j.bmcl.2014.06.014
12828570 4990 0 None 1 2 Bovine 4.8 pKi = 4.8 Binding
Tested for binding affinity against beta-2 adrenergic receptor in bovine lung using [3H]DHA as radioligandTested for binding affinity against beta-2 adrenergic receptor in bovine lung using [3H]DHA as radioligand
ChEMBL 237 3 3 4 1.7 CC(C)NCC1OCCc2c1ccc(O)c2O 10.1021/jm00073a006
CHEMBL105434 4990 0 None 1 2 Bovine 4.8 pKi = 4.8 Binding
Tested for binding affinity against beta-2 adrenergic receptor in bovine lung using [3H]DHA as radioligandTested for binding affinity against beta-2 adrenergic receptor in bovine lung using [3H]DHA as radioligand
ChEMBL 237 3 3 4 1.7 CC(C)NCC1OCCc2c1ccc(O)c2O 10.1021/jm00073a006
118710943 113241 0 None 5 3 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assay
ChEMBL 384 5 4 5 3.6 Cc1cccc([C@H]2CCC[C@H]2NC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)c1 10.1016/j.bmcl.2014.06.014
CHEMBL3323661 113241 0 None 5 3 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assay
ChEMBL 384 5 4 5 3.6 Cc1cccc([C@H]2CCC[C@H]2NC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)c1 10.1016/j.bmcl.2014.06.014
155527302 170651 0 None 1 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H](-)CGP 12177 from human recombinant beta2 adrenoceptor after 120 mins by scintillation counting methodDisplacement of [3H](-)CGP 12177 from human recombinant beta2 adrenoceptor after 120 mins by scintillation counting method
ChEMBL 355 12 2 6 2.3 COC(=O)CSCCCc1ccccc1OCC(O)CNC(C)C 10.1039/C8MD00412A
CHEMBL4459696 170651 0 None 1 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H](-)CGP 12177 from human recombinant beta2 adrenoceptor after 120 mins by scintillation counting methodDisplacement of [3H](-)CGP 12177 from human recombinant beta2 adrenoceptor after 120 mins by scintillation counting method
ChEMBL 355 12 2 6 2.3 COC(=O)CSCCCc1ccccc1OCC(O)CNC(C)C 10.1039/C8MD00412A
155515823 169445 0 None 5 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysisDisplacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysis
ChEMBL 621 20 5 13 1.7 CC(C)NC[C@H](O)COc1ccccc1Cn1cc(CNCc2cn(Cc3ccccc3OC[C@@H](O)CNC(C)C)nn2)nn1 10.1021/acs.jmedchem.9b00595
CHEMBL4442559 169445 0 None 5 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysisDisplacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysis
ChEMBL 621 20 5 13 1.7 CC(C)NC[C@H](O)COc1ccccc1Cn1cc(CNCc2cn(Cc3ccccc3OC[C@@H](O)CNC(C)C)nn2)nn1 10.1021/acs.jmedchem.9b00595
44423645 84971 0 None 4 3 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]CYP from human adrenergic beta 2 receptor transfected in CHO cells in presence of 100 uM GTPDisplacement of [125I]CYP from human adrenergic beta 2 receptor transfected in CHO cells in presence of 100 uM GTP
ChEMBL 396 10 2 5 3.9 CCCCOc1ccc(C[C@@H](C)NC[C@H](O)c2cc(Br)no2)cc1 10.1016/j.bmc.2007.01.056
CHEMBL226349 84971 0 None 4 3 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]CYP from human adrenergic beta 2 receptor transfected in CHO cells in presence of 100 uM GTPDisplacement of [125I]CYP from human adrenergic beta 2 receptor transfected in CHO cells in presence of 100 uM GTP
ChEMBL 396 10 2 5 3.9 CCCCOc1ccc(C[C@@H](C)NC[C@H](O)c2cc(Br)no2)cc1 10.1016/j.bmc.2007.01.056
319 1292 39 None -16 9 Human 7.8 pKi = 7.8 Binding
Binding affinity to human beta2-adrenoceptor by radioligand binding assayBinding affinity to human beta2-adrenoceptor by radioligand binding assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2012.07.096
321 1292 39 None -16 9 Human 7.8 pKi = 7.8 Binding
Binding affinity to human beta2-adrenoceptor by radioligand binding assayBinding affinity to human beta2-adrenoceptor by radioligand binding assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2012.07.096
444031 1292 39 None -16 9 Human 7.8 pKi = 7.8 Binding
Binding affinity to human beta2-adrenoceptor by radioligand binding assayBinding affinity to human beta2-adrenoceptor by radioligand binding assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2012.07.096
784 1292 39 None -16 9 Human 7.8 pKi = 7.8 Binding
Binding affinity to human beta2-adrenoceptor by radioligand binding assayBinding affinity to human beta2-adrenoceptor by radioligand binding assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2012.07.096
CHEMBL1346 1292 39 None -16 9 Human 7.8 pKi = 7.8 Binding
Binding affinity to human beta2-adrenoceptor by radioligand binding assayBinding affinity to human beta2-adrenoceptor by radioligand binding assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2012.07.096
DB00496 1292 39 None -16 9 Human 7.8 pKi = 7.8 Binding
Binding affinity to human beta2-adrenoceptor by radioligand binding assayBinding affinity to human beta2-adrenoceptor by radioligand binding assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2012.07.096
44312421 162774 0 None 2 3 Human 6.8 pKi = 6.8 Binding
Compound was tested for its binding affinity against beta2 adrenergic receptor in CHO cell membrane using [125I]iodocyanopindolol as the radioligand.Compound was tested for its binding affinity against beta2 adrenergic receptor in CHO cell membrane using [125I]iodocyanopindolol as the radioligand.
ChEMBL 392 13 3 6 2.9 C[C@H](Cc1ncc(CCCCC(=O)O)s1)NC[C@H](O)COc1ccccc1 10.1016/0960-894X(96)00417-9
CHEMBL419085 162774 0 None 2 3 Human 6.8 pKi = 6.8 Binding
Compound was tested for its binding affinity against beta2 adrenergic receptor in CHO cell membrane using [125I]iodocyanopindolol as the radioligand.Compound was tested for its binding affinity against beta2 adrenergic receptor in CHO cell membrane using [125I]iodocyanopindolol as the radioligand.
ChEMBL 392 13 3 6 2.9 C[C@H](Cc1ncc(CCCCC(=O)O)s1)NC[C@H](O)COc1ccccc1 10.1016/0960-894X(96)00417-9
2770390 6629 10 None 1 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cells
ChEMBL 499 10 1 6 3.2 C=CCc1ccccc1OCC(O)CN1CCN(CCN2C(=O)c3cccc4cccc(c34)C2=O)CC1 10.1016/j.bmcl.2010.04.009
CHEMBL1083672 6629 10 None 1 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cells
ChEMBL 499 10 1 6 3.2 C=CCc1ccccc1OCC(O)CN1CCN(CCN2C(=O)c3cccc4cccc(c34)C2=O)CC1 10.1016/j.bmcl.2010.04.009
172745 99648 7 None -10 6 Rat 5.8 pKi = 5.8 Binding
Binding affinity against adrenergic beta 2 receptor versus 1 nM [3H]dihydroalprenolol in rat cerebral cerebellar membranesBinding affinity against adrenergic beta 2 receptor versus 1 nM [3H]dihydroalprenolol in rat cerebral cerebellar membranes
ChEMBL 187 2 4 4 0.2 NCC(O)c1ccc(O)c(O)c1F 10.1021/jm00076a024
CHEMBL287587 99648 7 None -10 6 Rat 5.8 pKi = 5.8 Binding
Binding affinity against adrenergic beta 2 receptor versus 1 nM [3H]dihydroalprenolol in rat cerebral cerebellar membranesBinding affinity against adrenergic beta 2 receptor versus 1 nM [3H]dihydroalprenolol in rat cerebral cerebellar membranes
ChEMBL 187 2 4 4 0.2 NCC(O)c1ccc(O)c(O)c1F 10.1021/jm00076a024
10117815 93535 0 None -60 2 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]iodocyanopindolol from human cloned adrenergic beta-2 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human cloned adrenergic beta-2 receptor expressed in CHO cells
ChEMBL 500 12 4 7 3.3 COc1ccc([C@@H](Cc2ccccc2)NC[C@H](O)Cc2ccc(O)c(NS(C)(=O)=O)c2)cc1OC 10.1016/j.bmcl.2007.05.030
CHEMBL248548 93535 0 None -60 2 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]iodocyanopindolol from human cloned adrenergic beta-2 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human cloned adrenergic beta-2 receptor expressed in CHO cells
ChEMBL 500 12 4 7 3.3 COc1ccc([C@@H](Cc2ccccc2)NC[C@H](O)Cc2ccc(O)c(NS(C)(=O)=O)c2)cc1OC 10.1016/j.bmcl.2007.05.030
49864439 15456 0 None 4 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptorDisplacement of [3H]CGP12177 from human beta2 adrenoceptor
ChEMBL 390 5 4 5 4.1 O=c1[nH]c2c(O)ccc([C@@H](O)CNC3CCCCC3C3CCCCC3)c2s1 10.1016/j.bmcl.2010.06.136
CHEMBL1221801 15456 0 None 4 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptorDisplacement of [3H]CGP12177 from human beta2 adrenoceptor
ChEMBL 390 5 4 5 4.1 O=c1[nH]c2c(O)ccc([C@@H](O)CNC3CCCCC3C3CCCCC3)c2s1 10.1016/j.bmcl.2010.06.136
104903 56035 14 None -5 6 Human 4.8 pKi = 4.8 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 624 6 0 8 5.5 C[C@@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)C3=CC[C@]2(C)[C@H]1C(=O)CN1CCN(c2cc(N3CCCC3)nc(N3CCCC3)n2)CC1 nan
CHEMBL1630578 56035 14 None -5 6 Human 4.8 pKi = 4.8 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 624 6 0 8 5.5 C[C@@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)C3=CC[C@]2(C)[C@H]1C(=O)CN1CCN(c2cc(N3CCCC3)nc(N3CCCC3)n2)CC1 nan
44310900 202656 0 None - 1 Mouse 4.8 pKi = 4.8 Binding
Ki value was determined by accumulation of c-AMP in S-49 mouse lymphoma cells (Beta2).Ki value was determined by accumulation of c-AMP in S-49 mouse lymphoma cells (Beta2).
ChEMBL 441 13 4 5 3.9 CC(=O)Nc1ccc(OC[C@@H](O)CN[C@@H](C)CCCCC(=O)Nc2ccc(C)cc2)cc1 10.1021/jm00163a036
CHEMBL71734 202656 0 None - 1 Mouse 4.8 pKi = 4.8 Binding
Ki value was determined by accumulation of c-AMP in S-49 mouse lymphoma cells (Beta2).Ki value was determined by accumulation of c-AMP in S-49 mouse lymphoma cells (Beta2).
ChEMBL 441 13 4 5 3.9 CC(=O)Nc1ccc(OC[C@@H](O)CN[C@@H](C)CCCCC(=O)Nc2ccc(C)cc2)cc1 10.1021/jm00163a036
10310047 111758 0 None 199 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assay
ChEMBL 422 11 5 6 3.9 CCOc1ccc(Nc2ccc(CCNCC(O)c3ccc(O)c(CO)c3)cc2)cc1 10.1016/j.bmcl.2014.04.069
CHEMBL3290991 111758 0 None 199 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assay
ChEMBL 422 11 5 6 3.9 CCOc1ccc(Nc2ccc(CCNCC(O)c3ccc(O)c(CO)c3)cc2)cc1 10.1016/j.bmcl.2014.04.069
6603724 154780 3 None -1 3 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]prazosin from human adrenergic beta2 receptor expressed in CHO cell membraneDisplacement of [3H]prazosin from human adrenergic beta2 receptor expressed in CHO cell membrane
ChEMBL 187 2 4 4 0.2 NC[C@H](O)c1cc(O)c(O)cc1F 10.1016/j.bmc.2009.10.015
CHEMBL40317 154780 3 None -1 3 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]prazosin from human adrenergic beta2 receptor expressed in CHO cell membraneDisplacement of [3H]prazosin from human adrenergic beta2 receptor expressed in CHO cell membrane
ChEMBL 187 2 4 4 0.2 NC[C@H](O)c1cc(O)c(O)cc1F 10.1016/j.bmc.2009.10.015
9512 3566 35 None -3 2 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]cyanopindolol from human cloned beta-2 adrenergic receptor expressed in Sf9 cellsDisplacement of [125I]cyanopindolol from human cloned beta-2 adrenergic receptor expressed in Sf9 cells
ChEMBL 410 9 4 4 4.4 Clc1cccc(c1)[C@H](CNCCNc1cccc(c1)c1cccc(c1)C(=O)O)O 10.1021/jm0509445
9887812 3566 35 None -3 2 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]cyanopindolol from human cloned beta-2 adrenergic receptor expressed in Sf9 cellsDisplacement of [125I]cyanopindolol from human cloned beta-2 adrenergic receptor expressed in Sf9 cells
ChEMBL 410 9 4 4 4.4 Clc1cccc(c1)[C@H](CNCCNc1cccc(c1)c1cccc(c1)C(=O)O)O 10.1021/jm0509445
CHEMBL208427 3566 35 None -3 2 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]cyanopindolol from human cloned beta-2 adrenergic receptor expressed in Sf9 cellsDisplacement of [125I]cyanopindolol from human cloned beta-2 adrenergic receptor expressed in Sf9 cells
ChEMBL 410 9 4 4 4.4 Clc1cccc(c1)[C@H](CNCCNc1cccc(c1)c1cccc(c1)C(=O)O)O 10.1021/jm0509445
DB06190 3566 35 None -3 2 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]cyanopindolol from human cloned beta-2 adrenergic receptor expressed in Sf9 cellsDisplacement of [125I]cyanopindolol from human cloned beta-2 adrenergic receptor expressed in Sf9 cells
ChEMBL 410 9 4 4 4.4 Clc1cccc(c1)[C@H](CNCCNc1cccc(c1)c1cccc(c1)C(=O)O)O 10.1021/jm0509445
90644140 111761 0 None 25 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assay
ChEMBL 394 9 6 6 3.2 OCc1cc(C(O)CNCCc2ccc(Nc3ccc(O)cc3)cc2)ccc1O 10.1016/j.bmcl.2014.04.069
CHEMBL3290994 111761 0 None 25 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assay
ChEMBL 394 9 6 6 3.2 OCc1cc(C(O)CNCCc2ccc(Nc3ccc(O)cc3)cc2)ccc1O 10.1016/j.bmcl.2014.04.069
24865727 192501 0 None -1000 11 Human 5.8 pKi = 5.8 Binding
Displacement of radioligand from human cloned adrenergic beta2 receptorDisplacement of radioligand from human cloned adrenergic beta2 receptor
ChEMBL 479 7 0 5 4.4 Cc1ccc2c(OCCN3CCC(Cc4cccc(N5CCCS5(=O)=O)c4)CC3)cccc2n1 10.1021/jm8001444
CHEMBL522708 192501 0 None -1000 11 Human 5.8 pKi = 5.8 Binding
Displacement of radioligand from human cloned adrenergic beta2 receptorDisplacement of radioligand from human cloned adrenergic beta2 receptor
ChEMBL 479 7 0 5 4.4 Cc1ccc2c(OCCN3CCC(Cc4cccc(N5CCCS5(=O)=O)c4)CC3)cccc2n1 10.1021/jm8001444
16735259 85207 0 None - 1 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 317 7 4 5 2.4 COc1ccc(C[C@H](C)NC[C@@H](O)c2cc(O)cc(O)c2)cc1 10.1021/jm070030d
CHEMBL228417 85207 0 None - 1 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 317 7 4 5 2.4 COc1ccc(C[C@H](C)NC[C@@H](O)c2cc(O)cc(O)c2)cc1 10.1021/jm070030d
90644146 111740 0 None 5 2 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assay
ChEMBL 460 10 4 5 4.2 OCc1cc(C(O)CNCCc2ccc(N3CCC(Cc4ccccc4)CC3)cc2)ccc1O 10.1016/j.bmcl.2014.04.069
CHEMBL3290975 111740 0 None 5 2 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assay
ChEMBL 460 10 4 5 4.2 OCc1cc(C(O)CNCCc2ccc(N3CCC(Cc4ccccc4)CC3)cc2)ccc1O 10.1016/j.bmcl.2014.04.069
123133223 147147 0 None - 1 Human 4.8 pKi = 4.8 Binding
Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.
ChEMBL 317 7 4 5 2.4 COc1cccc(C[C@H](C)NC[C@@H](O)c2cc(O)cc(O)c2)c1 nan
CHEMBL3931891 147147 0 None - 1 Human 4.8 pKi = 4.8 Binding
Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.
ChEMBL 317 7 4 5 2.4 COc1cccc(C[C@H](C)NC[C@@H](O)c2cc(O)cc(O)c2)c1 nan
16735259 85207 0 None - 1 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 317 7 4 5 2.4 COc1ccc(C[C@H](C)NC[C@@H](O)c2cc(O)cc(O)c2)cc1 10.1021/jm070030d
CHEMBL228417 85207 0 None - 1 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 317 7 4 5 2.4 COc1ccc(C[C@H](C)NC[C@@H](O)c2cc(O)cc(O)c2)cc1 10.1021/jm070030d
155537995 171759 0 None 109 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H](-)CGP 12177 from human recombinant beta2 adrenoceptor after 120 mins by scintillation counting methodDisplacement of [3H](-)CGP 12177 from human recombinant beta2 adrenoceptor after 120 mins by scintillation counting method
ChEMBL 593 23 5 10 0.2 CC(C)NCC(O)COc1ccccc1CCCSCC(=O)NCCOCCOCCNC(=O)CS(=O)(=O)O 10.1039/C8MD00412A
CHEMBL4475573 171759 0 None 109 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H](-)CGP 12177 from human recombinant beta2 adrenoceptor after 120 mins by scintillation counting methodDisplacement of [3H](-)CGP 12177 from human recombinant beta2 adrenoceptor after 120 mins by scintillation counting method
ChEMBL 593 23 5 10 0.2 CC(C)NCC(O)COc1ccccc1CCCSCC(=O)NCCOCCOCCNC(=O)CS(=O)(=O)O 10.1039/C8MD00412A
44396568 66934 0 None -9 3 Human 6.8 pKi = 6.8 Binding
Binding inhibition constant was determined by inhibition of [125I]iodocyanopindolol binding to Beta-2 adrenergic receptorBinding inhibition constant was determined by inhibition of [125I]iodocyanopindolol binding to Beta-2 adrenergic receptor
ChEMBL 529 12 5 7 3.7 C[C@H](Cc1c[nH]c2c(OCC(=O)O)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2004.10.035
CHEMBL188196 66934 0 None -9 3 Human 6.8 pKi = 6.8 Binding
Binding inhibition constant was determined by inhibition of [125I]iodocyanopindolol binding to Beta-2 adrenergic receptorBinding inhibition constant was determined by inhibition of [125I]iodocyanopindolol binding to Beta-2 adrenergic receptor
ChEMBL 529 12 5 7 3.7 C[C@H](Cc1c[nH]c2c(OCC(=O)O)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2004.10.035
3931 2208 42 None 3 2 Human 6.8 pKi = 6.8 Binding
Inhibition of I-iodocyanopindolol binding to human beta 2 adrenergic receptorsInhibition of I-iodocyanopindolol binding to human beta 2 adrenergic receptors
ChEMBL 584 17 6 7 4.5 CCCCCCNC(=O)Nc1ccc(cc1)S(=O)(=O)Nc1ccc(cc1)CCNC[C@@H](COc1ccc(cc1)O)O 10.1021/jm000544b
9829836 2208 42 None 3 2 Human 6.8 pKi = 6.8 Binding
Inhibition of I-iodocyanopindolol binding to human beta 2 adrenergic receptorsInhibition of I-iodocyanopindolol binding to human beta 2 adrenergic receptors
ChEMBL 584 17 6 7 4.5 CCCCCCNC(=O)Nc1ccc(cc1)S(=O)(=O)Nc1ccc(cc1)CCNC[C@@H](COc1ccc(cc1)O)O 10.1021/jm000544b
CHEMBL12998 2208 42 None 3 2 Human 6.8 pKi = 6.8 Binding
Inhibition of I-iodocyanopindolol binding to human beta 2 adrenergic receptorsInhibition of I-iodocyanopindolol binding to human beta 2 adrenergic receptors
ChEMBL 584 17 6 7 4.5 CCCCCCNC(=O)Nc1ccc(cc1)S(=O)(=O)Nc1ccc(cc1)CCNC[C@@H](COc1ccc(cc1)O)O 10.1021/jm000544b
9821129 202725 0 None -2 3 Human 5.8 pKi = 5.8 Binding
Compound was tested for its binding affinity against beta2 adrenergic receptor in CHO cell membrane using [125I]iodocyanopindolol as the radioligand.Compound was tested for its binding affinity against beta2 adrenergic receptor in CHO cell membrane using [125I]iodocyanopindolol as the radioligand.
ChEMBL 378 12 3 6 2.5 C[C@H](Cc1ncc(CCCC(=O)O)s1)NC[C@H](O)COc1ccccc1 10.1016/0960-894X(96)00417-9
CHEMBL72169 202725 0 None -2 3 Human 5.8 pKi = 5.8 Binding
Compound was tested for its binding affinity against beta2 adrenergic receptor in CHO cell membrane using [125I]iodocyanopindolol as the radioligand.Compound was tested for its binding affinity against beta2 adrenergic receptor in CHO cell membrane using [125I]iodocyanopindolol as the radioligand.
ChEMBL 378 12 3 6 2.5 C[C@H](Cc1ncc(CCCC(=O)O)s1)NC[C@H](O)COc1ccccc1 10.1016/0960-894X(96)00417-9
24937137 17561 0 None 3 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 430 8 4 9 1.9 OCc1cc(OCC(O)CNC2CCN(c3ncnc4ccsc34)CC2)ccc1O 10.1016/j.bmcl.2010.08.039
CHEMBL1258707 17561 0 None 3 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 430 8 4 9 1.9 OCc1cc(OCC(O)CNC2CCN(c3ncnc4ccsc34)CC2)ccc1O 10.1016/j.bmcl.2010.08.039
1499 2052 43 None -33 17 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C nan
3779 2052 43 None -33 17 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C nan
536 2052 43 None -33 17 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C nan
CHEMBL434 2052 43 None -33 17 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C nan
DB01064 2052 43 None -33 17 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C nan
46889770 6628 0 None 5 3 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cells
ChEMBL 306 7 2 4 2.2 CC(C)c1ccccc1OCC(O)CNC1CCN(C)CC1 10.1016/j.bmcl.2010.04.009
CHEMBL1083670 6628 0 None 5 3 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cells
ChEMBL 306 7 2 4 2.2 CC(C)c1ccccc1OCC(O)CNC1CCN(C)CC1 10.1016/j.bmcl.2010.04.009
46889730 7035 0 None 42 3 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cells
ChEMBL 436 8 1 5 3.6 CC(C)c1ccccc1OCC(O)CN1CCC(CN2C(=O)c3ccccc3C2=O)CC1 10.1016/j.bmcl.2010.04.009
CHEMBL1085270 7035 0 None 42 3 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cells
ChEMBL 436 8 1 5 3.6 CC(C)c1ccccc1OCC(O)CN1CCC(CN2C(=O)c3ccccc3C2=O)CC1 10.1016/j.bmcl.2010.04.009
44286983 141166 0 None 3 3 Human 6.8 pKi = 6.8 Binding
Ability to bind to human Beta-2 adrenergic receptor using membranes of stably transfected CHO cellsAbility to bind to human Beta-2 adrenergic receptor using membranes of stably transfected CHO cells
ChEMBL 362 9 3 4 2.5 C[C@H](Cc1ccc(OCC(N)=O)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1016/S0960-894X(97)00266-7
CHEMBL38569 141166 0 None 3 3 Human 6.8 pKi = 6.8 Binding
Ability to bind to human Beta-2 adrenergic receptor using membranes of stably transfected CHO cellsAbility to bind to human Beta-2 adrenergic receptor using membranes of stably transfected CHO cells
ChEMBL 362 9 3 4 2.5 C[C@H](Cc1ccc(OCC(N)=O)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1016/S0960-894X(97)00266-7
155521528 170027 0 None 1 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assay
ChEMBL 376 8 3 4 4.0 COc1ccccc1OCCNC[C@@H](O)c1cccc2[nH]c3ccccc3c12 10.1021/acs.jmedchem.9b00349
CHEMBL4450756 170027 0 None 1 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assay
ChEMBL 376 8 3 4 4.0 COc1ccccc1OCCNC[C@@H](O)c1cccc2[nH]c3ccccc3c12 10.1021/acs.jmedchem.9b00349
131268 112390 24 None -112 3 Guinea pig 5.8 pKi = 5.8 Binding
Binding affinity against Beta-2 adrenergic receptor was measured using [125I]CYP as radioligandBinding affinity against Beta-2 adrenergic receptor was measured using [125I]CYP as radioligand
ChEMBL 203 1 1 5 0.1 c1cn2ccnc2c(N2CCNCC2)n1 10.1021/jm00099a012
CHEMBL331036 112390 24 None -112 3 Guinea pig 5.8 pKi = 5.8 Binding
Binding affinity against Beta-2 adrenergic receptor was measured using [125I]CYP as radioligandBinding affinity against Beta-2 adrenergic receptor was measured using [125I]CYP as radioligand
ChEMBL 203 1 1 5 0.1 c1cn2ccnc2c(N2CCNCC2)n1 10.1021/jm00099a012
44287321 99987 0 None -1 2 Human 4.8 pKi = 4.8 Binding
Ability to bind to human Beta-2 adrenergic receptor using membranes of stably transfected CHO cellsAbility to bind to human Beta-2 adrenergic receptor using membranes of stably transfected CHO cells
ChEMBL 407 10 4 5 2.5 C[C@H](Cc1ccc(OC(C(=O)O)C(=O)O)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1016/S0960-894X(97)00266-7
CHEMBL290752 99987 0 None -1 2 Human 4.8 pKi = 4.8 Binding
Ability to bind to human Beta-2 adrenergic receptor using membranes of stably transfected CHO cellsAbility to bind to human Beta-2 adrenergic receptor using membranes of stably transfected CHO cells
ChEMBL 407 10 4 5 2.5 C[C@H](Cc1ccc(OC(C(=O)O)C(=O)O)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1016/S0960-894X(97)00266-7
9928332 96719 4 None -870 10 Dog 5.8 pKi = 5.8 Binding
Compound was evaluated for its binding affinity to beta-2 receptor in rat brain using [3H]- DHA radioligand assayCompound was evaluated for its binding affinity to beta-2 receptor in rat brain using [3H]- DHA radioligand assay
ChEMBL 349 6 0 3 5.0 COc1cccc2c1CCC[C@H]2CN(C)CCc1ccc2ccoc2c1 10.1016/0960-894X(95)00398-D
CHEMBL268258 96719 4 None -870 10 Dog 5.8 pKi = 5.8 Binding
Compound was evaluated for its binding affinity to beta-2 receptor in rat brain using [3H]- DHA radioligand assayCompound was evaluated for its binding affinity to beta-2 receptor in rat brain using [3H]- DHA radioligand assay
ChEMBL 349 6 0 3 5.0 COc1cccc2c1CCC[C@H]2CN(C)CCc1ccc2ccoc2c1 10.1016/0960-894X(95)00398-D
11625333 77250 0 None 2 2 Human 6.8 pKi = 6.8 Binding
Binding affinity to human beta2-adrenoceptor by radioligand binding assayBinding affinity to human beta2-adrenoceptor by radioligand binding assay
ChEMBL 392 4 4 4 3.3 Cc1c(C)c(C)c2c(c1C)CC(NC[C@H](O)c1ccc(O)c3[nH]c(=O)ccc13)C2 10.1016/j.bmcl.2012.07.096
CHEMBL2088200 77250 0 None 2 2 Human 6.8 pKi = 6.8 Binding
Binding affinity to human beta2-adrenoceptor by radioligand binding assayBinding affinity to human beta2-adrenoceptor by radioligand binding assay
ChEMBL 392 4 4 4 3.3 Cc1c(C)c(C)c2c(c1C)CC(NC[C@H](O)c1ccc(O)c3[nH]c(=O)ccc13)C2 10.1016/j.bmcl.2012.07.096
24936491 17323 0 None -2 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 494 8 3 8 4.2 Oc1ccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccc(F)cc5)c34)CC2)cc1 10.1016/j.bmcl.2010.08.039
CHEMBL1257916 17323 0 None -2 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 494 8 3 8 4.2 Oc1ccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccc(F)cc5)c34)CC2)cc1 10.1016/j.bmcl.2010.08.039
1786 2474 79 None -25 11 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O nan
4171 2474 79 None -25 11 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O nan
553 2474 79 None -25 11 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O nan
CHEMBL13 2474 79 None -25 11 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O nan
DB00264 2474 79 None -25 11 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O nan
44350012 17825 0 None -11 3 Guinea pig 4.8 pKi = 4.8 Binding
Binding affinity against Beta-2 adrenergic receptor was measured using [125I]CYP as radioligandBinding affinity against Beta-2 adrenergic receptor was measured using [125I]CYP as radioligand
ChEMBL 363 4 3 7 0.4 CC1CN=C2C(N3CCNCC3)=NC=CN21.O=C(O)C/C=C\CC(=O)O 10.1021/jm00099a012
CHEMBL126394 17825 0 None -11 3 Guinea pig 4.8 pKi = 4.8 Binding
Binding affinity against Beta-2 adrenergic receptor was measured using [125I]CYP as radioligandBinding affinity against Beta-2 adrenergic receptor was measured using [125I]CYP as radioligand
ChEMBL 363 4 3 7 0.4 CC1CN=C2C(N3CCNCC3)=NC=CN21.O=C(O)C/C=C\CC(=O)O 10.1021/jm00099a012
16736096 141552 0 None 19 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 337 6 4 4 3.5 C[C@H](Cc1cccc2ccccc12)NC[C@@H](O)c1cc(O)cc(O)c1 10.1021/jm070030d
CHEMBL388177 141552 0 None 19 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 337 6 4 4 3.5 C[C@H](Cc1cccc2ccccc12)NC[C@@H](O)c1cc(O)cc(O)c1 10.1021/jm070030d
16736096 141552 0 None 19 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 337 6 4 4 3.5 C[C@H](Cc1cccc2ccccc12)NC[C@@H](O)c1cc(O)cc(O)c1 10.1021/jm070030d
CHEMBL388177 141552 0 None 19 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 337 6 4 4 3.5 C[C@H](Cc1cccc2ccccc12)NC[C@@H](O)c1cc(O)cc(O)c1 10.1021/jm070030d
16736096 141552 0 None 19 2 Human 5.8 pKi = 5.8 Binding
Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.
ChEMBL 337 6 4 4 3.5 C[C@H](Cc1cccc2ccccc12)NC[C@@H](O)c1cc(O)cc(O)c1 nan
CHEMBL388177 141552 0 None 19 2 Human 5.8 pKi = 5.8 Binding
Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.
ChEMBL 337 6 4 4 3.5 C[C@H](Cc1cccc2ccccc12)NC[C@@H](O)c1cc(O)cc(O)c1 nan
24937269 17450 0 None 2 3 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 490 9 3 8 3.8 OCc1cccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)c1 10.1016/j.bmcl.2010.08.039
CHEMBL1258371 17450 0 None 2 3 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 490 9 3 8 3.8 OCc1cccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)c1 10.1016/j.bmcl.2010.08.039
127046950 139502 0 None 3 6 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assay
ChEMBL 437 12 4 6 4.0 COc1cc(CCNC[C@H](O)c2ccc(O)c(O)c2)ccc1OCCCc1ccccc1 10.1021/acs.jmedchem.9b00349
CHEMBL3800303 139502 0 None 3 6 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assay
ChEMBL 437 12 4 6 4.0 COc1cc(CCNC[C@H](O)c2ccc(O)c(O)c2)ccc1OCCCc1ccccc1 10.1021/acs.jmedchem.9b00349
127046950 139502 0 None 3 6 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cellsDisplacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells
ChEMBL 437 12 4 6 4.0 COc1cc(CCNC[C@H](O)c2ccc(O)c(O)c2)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
CHEMBL3800303 139502 0 None 3 6 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cellsDisplacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells
ChEMBL 437 12 4 6 4.0 COc1cc(CCNC[C@H](O)c2ccc(O)c(O)c2)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
203685 30526 8 None 3 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysisDisplacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysis
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OC[C@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
CHEMBL1395661 30526 8 None 3 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysisDisplacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysis
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OC[C@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
49864461 15461 0 None 1 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptorDisplacement of [3H]CGP12177 from human beta2 adrenoceptor
ChEMBL 381 12 4 6 2.8 CCCCN(CCCC)CCNC[C@H](O)c1ccc(O)c2[nH]c(=O)sc12 10.1016/j.bmcl.2010.06.136
CHEMBL1221862 15461 0 None 1 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptorDisplacement of [3H]CGP12177 from human beta2 adrenoceptor
ChEMBL 381 12 4 6 2.8 CCCCN(CCCC)CCNC[C@H](O)c1ccc(O)c2[nH]c(=O)sc12 10.1016/j.bmcl.2010.06.136
10283146 106776 0 None 1 2 Human 6.8 pKi = 6.8 Binding
Binding affinity of compound against Beta-2 adrenergic receptor was determinedBinding affinity of compound against Beta-2 adrenergic receptor was determined
ChEMBL 656 12 5 9 3.1 CS(=O)(=O)Nc1cc([C@@H](O)CNCC2CCN(S(=O)(=O)c3ccc(-n4cc(CC(=O)O)c5ccccc54)cc3)CC2)ccc1O 10.1016/s0960-894x(02)00608-x
CHEMBL317003 106776 0 None 1 2 Human 6.8 pKi = 6.8 Binding
Binding affinity of compound against Beta-2 adrenergic receptor was determinedBinding affinity of compound against Beta-2 adrenergic receptor was determined
ChEMBL 656 12 5 9 3.1 CS(=O)(=O)Nc1cc([C@@H](O)CNCC2CCN(S(=O)(=O)c3ccc(-n4cc(CC(=O)O)c5ccccc54)cc3)CC2)ccc1O 10.1016/s0960-894x(02)00608-x
10455 3218 34 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]CGP1217 from human recombinant adrenergic beta2 receptor transfected in insect Sf9 cells by scintillation countingDisplacement of [3H]CGP1217 from human recombinant adrenergic beta2 receptor transfected in insect Sf9 cells by scintillation counting
ChEMBL 301 7 4 4 2.7 CC(NCC(c1ccc(cc1)O)O)CCc1ccc(cc1)O 10.1021/jm801211c
56052 3218 34 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]CGP1217 from human recombinant adrenergic beta2 receptor transfected in insect Sf9 cells by scintillation countingDisplacement of [3H]CGP1217 from human recombinant adrenergic beta2 receptor transfected in insect Sf9 cells by scintillation counting
ChEMBL 301 7 4 4 2.7 CC(NCC(c1ccc(cc1)O)O)CCc1ccc(cc1)O 10.1021/jm801211c
CHEMBL509336 3218 34 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]CGP1217 from human recombinant adrenergic beta2 receptor transfected in insect Sf9 cells by scintillation countingDisplacement of [3H]CGP1217 from human recombinant adrenergic beta2 receptor transfected in insect Sf9 cells by scintillation counting
ChEMBL 301 7 4 4 2.7 CC(NCC(c1ccc(cc1)O)O)CCc1ccc(cc1)O 10.1021/jm801211c
DB11541 3218 34 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]CGP1217 from human recombinant adrenergic beta2 receptor transfected in insect Sf9 cells by scintillation countingDisplacement of [3H]CGP1217 from human recombinant adrenergic beta2 receptor transfected in insect Sf9 cells by scintillation counting
ChEMBL 301 7 4 4 2.7 CC(NCC(c1ccc(cc1)O)O)CCc1ccc(cc1)O 10.1021/jm801211c
155515982 169432 0 None -7079 17 Human 5.8 pKi = 5.8 Binding
Displacement of [3H] CGP12177 from beta2 adrenergic receptor (unknown origin)Displacement of [3H] CGP12177 from beta2 adrenergic receptor (unknown origin)
ChEMBL 473 10 2 5 4.1 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2)c2ccccc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4442460 169432 0 None -7079 17 Human 5.8 pKi = 5.8 Binding
Displacement of [3H] CGP12177 from beta2 adrenergic receptor (unknown origin)Displacement of [3H] CGP12177 from beta2 adrenergic receptor (unknown origin)
ChEMBL 473 10 2 5 4.1 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2)c2ccccc2)CC1 10.1021/acs.jmedchem.9b01085
105 3392 84 None -10 6 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]cyanopindolol from human recombinant beta2 adrenergic receptor expressed in CHO cells by filtration assayDisplacement of [125I]cyanopindolol from human recombinant beta2 adrenergic receptor expressed in CHO cells by filtration assay
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1021/jm100068m
2083 3392 84 None -10 6 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]cyanopindolol from human recombinant beta2 adrenergic receptor expressed in CHO cells by filtration assayDisplacement of [125I]cyanopindolol from human recombinant beta2 adrenergic receptor expressed in CHO cells by filtration assay
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1021/jm100068m
558 3392 84 None -10 6 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]cyanopindolol from human recombinant beta2 adrenergic receptor expressed in CHO cells by filtration assayDisplacement of [125I]cyanopindolol from human recombinant beta2 adrenergic receptor expressed in CHO cells by filtration assay
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1021/jm100068m
CHEMBL714 3392 84 None -10 6 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]cyanopindolol from human recombinant beta2 adrenergic receptor expressed in CHO cells by filtration assayDisplacement of [125I]cyanopindolol from human recombinant beta2 adrenergic receptor expressed in CHO cells by filtration assay
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1021/jm100068m
DB01001 3392 84 None -10 6 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]cyanopindolol from human recombinant beta2 adrenergic receptor expressed in CHO cells by filtration assayDisplacement of [125I]cyanopindolol from human recombinant beta2 adrenergic receptor expressed in CHO cells by filtration assay
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1021/jm100068m
667688 85358 4 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 303 6 5 5 2.1 C[C@H](Cc1ccc(O)cc1)NC[C@@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2013.11.030
CHEMBL229477 85358 4 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 303 6 5 5 2.1 C[C@H](Cc1ccc(O)cc1)NC[C@@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2013.11.030
688467 85357 2 None 14 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 303 6 5 5 2.1 C[C@@H](Cc1ccc(O)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2013.11.030
CHEMBL229476 85357 2 None 14 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 303 6 5 5 2.1 C[C@@H](Cc1ccc(O)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2013.11.030
688467 85357 2 None 14 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 303 6 5 5 2.1 C[C@@H](Cc1ccc(O)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2013.11.030
CHEMBL229476 85357 2 None 14 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 303 6 5 5 2.1 C[C@@H](Cc1ccc(O)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2013.11.030
2419 3394 80 None 16 6 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-CYP from human beta2-adrenergic receptor Y308A mutant expressed in COS-7 cells by gamma countingDisplacement of [125I]-CYP from human beta2-adrenergic receptor Y308A mutant expressed in COS-7 cells by gamma counting
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmc.2009.11.062
5152 3394 80 None 16 6 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-CYP from human beta2-adrenergic receptor Y308A mutant expressed in COS-7 cells by gamma countingDisplacement of [125I]-CYP from human beta2-adrenergic receptor Y308A mutant expressed in COS-7 cells by gamma counting
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmc.2009.11.062
559 3394 80 None 16 6 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-CYP from human beta2-adrenergic receptor Y308A mutant expressed in COS-7 cells by gamma countingDisplacement of [125I]-CYP from human beta2-adrenergic receptor Y308A mutant expressed in COS-7 cells by gamma counting
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmc.2009.11.062
CHEMBL1263 3394 80 None 16 6 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-CYP from human beta2-adrenergic receptor Y308A mutant expressed in COS-7 cells by gamma countingDisplacement of [125I]-CYP from human beta2-adrenergic receptor Y308A mutant expressed in COS-7 cells by gamma counting
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmc.2009.11.062
DB00938 3394 80 None 16 6 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-CYP from human beta2-adrenergic receptor Y308A mutant expressed in COS-7 cells by gamma countingDisplacement of [125I]-CYP from human beta2-adrenergic receptor Y308A mutant expressed in COS-7 cells by gamma counting
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmc.2009.11.062
15711869 13214 0 None -3548 6 Dog 4.7 pKi = 4.7 Binding
Compound was tested in vitro for binding affinity for beta receptorCompound was tested in vitro for binding affinity for beta receptor
ChEMBL 333 2 2 3 3.5 NC[C@@H]1O[C@H](c2ccccc2)Cc2c1ccc(Br)c2O 10.1021/jm00114a002
CHEMBL1192194 13214 0 None -3548 6 Dog 4.7 pKi = 4.7 Binding
Compound was tested in vitro for binding affinity for beta receptorCompound was tested in vitro for binding affinity for beta receptor
ChEMBL 333 2 2 3 3.5 NC[C@@H]1O[C@H](c2ccccc2)Cc2c1ccc(Br)c2O 10.1021/jm00114a002
CHEMBL543390 13214 0 None -3548 6 Dog 4.7 pKi = 4.7 Binding
Compound was tested in vitro for binding affinity for beta receptorCompound was tested in vitro for binding affinity for beta receptor
ChEMBL 333 2 2 3 3.5 NC[C@@H]1O[C@H](c2ccccc2)Cc2c1ccc(Br)c2O 10.1021/jm00114a002
16736094 85343 0 None 9 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 302 6 5 5 1.9 C[C@H](Cc1ccc(N)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1021/jm070030d
CHEMBL229391 85343 0 None 9 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 302 6 5 5 1.9 C[C@H](Cc1ccc(N)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1021/jm070030d
16736094 85343 0 None 9 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 302 6 5 5 1.9 C[C@H](Cc1ccc(N)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1021/jm070030d
CHEMBL229391 85343 0 None 9 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 302 6 5 5 1.9 C[C@H](Cc1ccc(N)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1021/jm070030d
123133224 160153 0 None 9 2 Human 5.7 pKi = 5.7 Binding
Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.
ChEMBL 302 6 5 5 1.9 C[C@H](Cc1cccc(N)c1)NC[C@H](O)c1cc(O)cc(O)c1 nan
CHEMBL4113713 160153 0 None 9 2 Human 5.7 pKi = 5.7 Binding
Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.
ChEMBL 302 6 5 5 1.9 C[C@H](Cc1cccc(N)c1)NC[C@H](O)c1cc(O)cc(O)c1 nan
3157 1437 69 None -97 12 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 nan
7170 1437 69 None -97 12 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 nan
954 1437 69 None -97 12 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 nan
CHEMBL707 1437 69 None -97 12 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 nan
DB00590 1437 69 None -97 12 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 nan
52947562 17490 0 None -2 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 384 7 2 7 2.7 OC(CNC1CCN(c2ncnc3sccc23)CC1)COc1ccccc1 10.1016/j.bmcl.2010.08.039
CHEMBL1258486 17490 0 None -2 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 384 7 2 7 2.7 OC(CNC1CCN(c2ncnc3sccc23)CC1)COc1ccccc1 10.1016/j.bmcl.2010.08.039
1043 1545 13 None -20892 29 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
149 1545 13 None -20892 29 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
8223 1545 13 None -20892 29 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
CHEMBL442 1545 13 None -20892 29 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
DB00696 1545 13 None -20892 29 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
52948056 17322 0 None 1 3 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 478 8 2 7 4.5 OC(CNC1CCN(c2ncnc3scc(-c4ccc(F)cc4)c23)CC1)COc1ccccc1 10.1016/j.bmcl.2010.08.039
CHEMBL1257915 17322 0 None 1 3 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 478 8 2 7 4.5 OC(CNC1CCN(c2ncnc3scc(-c4ccc(F)cc4)c23)CC1)COc1ccccc1 10.1016/j.bmcl.2010.08.039
10406968 113245 0 None 1 3 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assay
ChEMBL 372 8 4 5 3.1 CCCc1ccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)cc1 10.1016/j.bmcl.2014.06.014
CHEMBL3323665 113245 0 None 1 3 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assay
ChEMBL 372 8 4 5 3.1 CCCc1ccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)cc1 10.1016/j.bmcl.2014.06.014
53318455 58212 0 None 1 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-dihydroalprenolol from human beta2-adrenoceptor expressed in HEK cells after 4 hrsDisplacement of [3H]-dihydroalprenolol from human beta2-adrenoceptor expressed in HEK cells after 4 hrs
ChEMBL 556 10 5 7 4.6 O=C(Nc1ccccc1-c1ccccc1)OC1CCN(CCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1016/j.bmcl.2011.01.043
CHEMBL1683931 58212 0 None 1 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-dihydroalprenolol from human beta2-adrenoceptor expressed in HEK cells after 4 hrsDisplacement of [3H]-dihydroalprenolol from human beta2-adrenoceptor expressed in HEK cells after 4 hrs
ChEMBL 556 10 5 7 4.6 O=C(Nc1ccccc1-c1ccccc1)OC1CCN(CCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1016/j.bmcl.2011.01.043
70691181 77248 0 None 13 2 Human 7.7 pKi = 7.7 Binding
Binding affinity to human beta2-adrenoceptor by radioligand binding assayBinding affinity to human beta2-adrenoceptor by radioligand binding assay
ChEMBL 392 7 4 4 3.4 CCCCc1ccc2c(c1)CC(NC[C@H](O)c1ccc(O)c3[nH]c(=O)ccc13)C2 10.1016/j.bmcl.2012.07.096
CHEMBL2088199 77248 0 None 13 2 Human 7.7 pKi = 7.7 Binding
Binding affinity to human beta2-adrenoceptor by radioligand binding assayBinding affinity to human beta2-adrenoceptor by radioligand binding assay
ChEMBL 392 7 4 4 3.4 CCCCc1ccc2c(c1)CC(NC[C@H](O)c1ccc(O)c3[nH]c(=O)ccc13)C2 10.1016/j.bmcl.2012.07.096
49864357 15431 0 None 45 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptorDisplacement of [3H]CGP12177 from human beta2 adrenoceptor
ChEMBL 397 6 4 7 3.1 Cc1onc(-c2ccccc2)c1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)sc12 10.1016/j.bmcl.2010.06.136
CHEMBL1221588 15431 0 None 45 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptorDisplacement of [3H]CGP12177 from human beta2 adrenoceptor
ChEMBL 397 6 4 7 3.1 Cc1onc(-c2ccccc2)c1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)sc12 10.1016/j.bmcl.2010.06.136
44391257 65761 0 None -1 2 Human 7.7 pKi = 7.7 Binding
Binding affinity for human beta-2 adrenergic receptor by displacing [125I]iodocyanopindolol expressed in hamster CHO cellsBinding affinity for human beta-2 adrenergic receptor by displacing [125I]iodocyanopindolol expressed in hamster CHO cells
ChEMBL 411 9 4 6 2.3 CC(COc1ccc2c(c1)NC(=O)CO2)NCC(O)COc1cccc2[nH]ccc12 10.1016/j.bmcl.2004.11.030
CHEMBL183921 65761 0 None -1 2 Human 7.7 pKi = 7.7 Binding
Binding affinity for human beta-2 adrenergic receptor by displacing [125I]iodocyanopindolol expressed in hamster CHO cellsBinding affinity for human beta-2 adrenergic receptor by displacing [125I]iodocyanopindolol expressed in hamster CHO cells
ChEMBL 411 9 4 6 2.3 CC(COc1ccc2c(c1)NC(=O)CO2)NCC(O)COc1cccc2[nH]ccc12 10.1016/j.bmcl.2004.11.030
90645345 111974 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assayDisplacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assay
ChEMBL 574 12 6 8 4.7 CC(C)(C)OC(=O)NCCOc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 10.1016/j.bmcl.2014.04.095
CHEMBL3298692 111974 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assayDisplacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assay
ChEMBL 574 12 6 8 4.7 CC(C)(C)OC(=O)NCCOc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 10.1016/j.bmcl.2014.04.095
56943485 111998 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assayDisplacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assay
ChEMBL 544 12 5 8 3.6 O=c1ccc2c([C@@H](O)CNCCc3ccc(Nc4ccc(OCCN5CCOCC5)cc4)cc3)ccc(O)c2[nH]1 10.1016/j.bmcl.2014.04.095
CHEMBL3298831 111998 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assayDisplacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assay
ChEMBL 544 12 5 8 3.6 O=c1ccc2c([C@@H](O)CNCCc3ccc(Nc4ccc(OCCN5CCOCC5)cc4)cc3)ccc(O)c2[nH]1 10.1016/j.bmcl.2014.04.095
1499 2052 43 None -33 17 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-CGP-12177 from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-CGP-12177 from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2013.11.030
3779 2052 43 None -33 17 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-CGP-12177 from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-CGP-12177 from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2013.11.030
536 2052 43 None -33 17 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-CGP-12177 from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-CGP-12177 from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2013.11.030
CHEMBL434 2052 43 None -33 17 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-CGP-12177 from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-CGP-12177 from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2013.11.030
DB01064 2052 43 None -33 17 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-CGP-12177 from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-CGP-12177 from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2013.11.030
15711850 13113 0 None -354 5 Dog 4.7 pKi = 4.7 Binding
Compound was tested in vitro for binding affinity for beta receptorCompound was tested in vitro for binding affinity for beta receptor
ChEMBL 275 2 2 3 3.2 Cc1ccc2c(c1O)C[C@@H](C1CCCCC1)O[C@H]2CN 10.1021/jm00114a002
CHEMBL1191350 13113 0 None -354 5 Dog 4.7 pKi = 4.7 Binding
Compound was tested in vitro for binding affinity for beta receptorCompound was tested in vitro for binding affinity for beta receptor
ChEMBL 275 2 2 3 3.2 Cc1ccc2c(c1O)C[C@@H](C1CCCCC1)O[C@H]2CN 10.1021/jm00114a002
CHEMBL542436 13113 0 None -354 5 Dog 4.7 pKi = 4.7 Binding
Compound was tested in vitro for binding affinity for beta receptorCompound was tested in vitro for binding affinity for beta receptor
ChEMBL 275 2 2 3 3.2 Cc1ccc2c(c1O)C[C@@H](C1CCCCC1)O[C@H]2CN 10.1021/jm00114a002
16736091 85291 0 None 66 2 Human 5.7 pKi = 5.7 Binding
Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.
ChEMBL 317 7 4 5 2.4 COc1ccc(C[C@H](C)NC[C@H](O)c2cc(O)cc(O)c2)cc1 nan
CHEMBL228996 85291 0 None 66 2 Human 5.7 pKi = 5.7 Binding
Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.
ChEMBL 317 7 4 5 2.4 COc1ccc(C[C@H](C)NC[C@H](O)c2cc(O)cc(O)c2)cc1 nan
16736091 85291 0 None 66 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 317 7 4 5 2.4 COc1ccc(C[C@H](C)NC[C@H](O)c2cc(O)cc(O)c2)cc1 10.1021/jm070030d
CHEMBL228996 85291 0 None 66 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 317 7 4 5 2.4 COc1ccc(C[C@H](C)NC[C@H](O)c2cc(O)cc(O)c2)cc1 10.1021/jm070030d
16736091 85291 0 None 66 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 317 7 4 5 2.4 COc1ccc(C[C@H](C)NC[C@H](O)c2cc(O)cc(O)c2)cc1 10.1021/jm070030d
CHEMBL228996 85291 0 None 66 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 317 7 4 5 2.4 COc1ccc(C[C@H](C)NC[C@H](O)c2cc(O)cc(O)c2)cc1 10.1021/jm070030d
6603724 154780 3 None -1 3 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]prazosin from human adrenergic beta2 receptor D192G, F193V mutant expressed in CHO cell membraneDisplacement of [3H]prazosin from human adrenergic beta2 receptor D192G, F193V mutant expressed in CHO cell membrane
ChEMBL 187 2 4 4 0.2 NC[C@H](O)c1cc(O)c(O)cc1F 10.1016/j.bmc.2009.10.015
CHEMBL40317 154780 3 None -1 3 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]prazosin from human adrenergic beta2 receptor D192G, F193V mutant expressed in CHO cell membraneDisplacement of [3H]prazosin from human adrenergic beta2 receptor D192G, F193V mutant expressed in CHO cell membrane
ChEMBL 187 2 4 4 0.2 NC[C@H](O)c1cc(O)c(O)cc1F 10.1016/j.bmc.2009.10.015
1028 287 69 None -89 30 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O nan
139148732 287 69 None -89 30 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O nan
479 287 69 None -89 30 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O nan
5816 287 69 None -89 30 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O nan
CHEMBL679 287 69 None -89 30 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O nan
DB00668 287 69 None -89 30 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O nan
10375227 11098 0 None -2 2 Bovine 5.7 pKi = 5.7 Binding
Binding affinity against beta-2-adrenergic receptor in bovine lungBinding affinity against beta-2-adrenergic receptor in bovine lung
ChEMBL 188 5 2 4 0.8 C/C=N/OCC(O)CNC(C)(C)C 10.1021/jm00036a018
CHEMBL1178761 11098 0 None -2 2 Bovine 5.7 pKi = 5.7 Binding
Binding affinity against beta-2-adrenergic receptor in bovine lungBinding affinity against beta-2-adrenergic receptor in bovine lung
ChEMBL 188 5 2 4 0.8 C/C=N/OCC(O)CNC(C)(C)C 10.1021/jm00036a018
CHEMBL39873 11098 0 None -2 2 Bovine 5.7 pKi = 5.7 Binding
Binding affinity against beta-2-adrenergic receptor in bovine lungBinding affinity against beta-2-adrenergic receptor in bovine lung
ChEMBL 188 5 2 4 0.8 C/C=N/OCC(O)CNC(C)(C)C 10.1021/jm00036a018
10287730 3467 36 None -2511 12 Human 5.7 pKi = 5.7 Binding
Binding affinity for human beta-2 adrenergic receptor Binding affinity for human beta-2 adrenergic receptor
ChEMBL 412 6 0 5 4.3 Cc1ccc2c(n1)cccc2OCCN1CCN(CC1)Cc1cccc2c1nccc2 10.1021/jm049039v
77 3467 36 None -2511 12 Human 5.7 pKi = 5.7 Binding
Binding affinity for human beta-2 adrenergic receptor Binding affinity for human beta-2 adrenergic receptor
ChEMBL 412 6 0 5 4.3 Cc1ccc2c(n1)cccc2OCCN1CCN(CC1)Cc1cccc2c1nccc2 10.1021/jm049039v
CHEMBL425190 3467 36 None -2511 12 Human 5.7 pKi = 5.7 Binding
Binding affinity for human beta-2 adrenergic receptor Binding affinity for human beta-2 adrenergic receptor
ChEMBL 412 6 0 5 4.3 Cc1ccc2c(n1)cccc2OCCN1CCN(CC1)Cc1cccc2c1nccc2 10.1021/jm049039v
2967101 67308 5 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]dihydroalprenolol from human ADRB2 expressed in HEK293T cells after 1 hr by liquid scintillation counterDisplacement of [3H]dihydroalprenolol from human ADRB2 expressed in HEK293T cells after 1 hr by liquid scintillation counter
ChEMBL 263 6 2 3 2.6 Cc1ccc(C)c(OCC(O)CNC2CCCC2)c1 10.1021/jm300280e
CHEMBL1907082 67308 5 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]dihydroalprenolol from human ADRB2 expressed in HEK293T cells after 1 hr by liquid scintillation counterDisplacement of [3H]dihydroalprenolol from human ADRB2 expressed in HEK293T cells after 1 hr by liquid scintillation counter
ChEMBL 263 6 2 3 2.6 Cc1ccc(C)c(OCC(O)CNC2CCCC2)c1 10.1021/jm300280e
118710937 113235 0 None 19 3 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assay
ChEMBL 376 5 4 5 3.7 O=c1[nH]c2c(O)ccc([C@@H](O)CN[C@@H]3CCC[C@@H]3C3CCCCC3)c2s1 10.1016/j.bmcl.2014.06.014
CHEMBL3323655 113235 0 None 19 3 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assay
ChEMBL 376 5 4 5 3.7 O=c1[nH]c2c(O)ccc([C@@H](O)CN[C@@H]3CCC[C@@H]3C3CCCCC3)c2s1 10.1016/j.bmcl.2014.06.014
9871887 102712 0 None 6 4 Human 8.7 pKi = 8.7 Binding
Binding Affinity against human beta-2 adrenergic receptor expressed in Chinese hamster ovary(CHO) cells was measured by using [125I]ICYP radioligandBinding Affinity against human beta-2 adrenergic receptor expressed in Chinese hamster ovary(CHO) cells was measured by using [125I]ICYP radioligand
ChEMBL 537 3 3 4 3.7 COc1c(I)cc(CC2NCCc3cc(O)c(O)cc32)cc1I 10.1021/jm990012z
CHEMBL308351 102712 0 None 6 4 Human 8.7 pKi = 8.7 Binding
Binding Affinity against human beta-2 adrenergic receptor expressed in Chinese hamster ovary(CHO) cells was measured by using [125I]ICYP radioligandBinding Affinity against human beta-2 adrenergic receptor expressed in Chinese hamster ovary(CHO) cells was measured by using [125I]ICYP radioligand
ChEMBL 537 3 3 4 3.7 COc1c(I)cc(CC2NCCc3cc(O)c(O)cc32)cc1I 10.1021/jm990012z
9871887 102712 0 None 6 4 Human 8.7 pKi = 8.7 Binding
Binding affinity for human Beta-2 adrenergic receptor expressed in CHO cells by radioligand competition binding assays using [125I]iodocyanopindolol (ICYP)Binding affinity for human Beta-2 adrenergic receptor expressed in CHO cells by radioligand competition binding assays using [125I]iodocyanopindolol (ICYP)
ChEMBL 537 3 3 4 3.7 COc1c(I)cc(CC2NCCc3cc(O)c(O)cc32)cc1I 10.1021/jm960208o
CHEMBL308351 102712 0 None 6 4 Human 8.7 pKi = 8.7 Binding
Binding affinity for human Beta-2 adrenergic receptor expressed in CHO cells by radioligand competition binding assays using [125I]iodocyanopindolol (ICYP)Binding affinity for human Beta-2 adrenergic receptor expressed in CHO cells by radioligand competition binding assays using [125I]iodocyanopindolol (ICYP)
ChEMBL 537 3 3 4 3.7 COc1c(I)cc(CC2NCCc3cc(O)c(O)cc32)cc1I 10.1021/jm960208o
46889769 6627 0 None 109 3 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cells
ChEMBL 304 8 2 4 1.8 C=CCc1ccccc1OCC(O)CNC1CCN(C)CC1 10.1016/j.bmcl.2010.04.009
CHEMBL1083669 6627 0 None 109 3 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cells
ChEMBL 304 8 2 4 1.8 C=CCc1ccccc1OCC(O)CNC1CCN(C)CC1 10.1016/j.bmcl.2010.04.009
2419 3394 80 None 16 6 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-dihydroalprenolol from human beta2-adrenoceptor expressed in HEK cells after 4 hrsDisplacement of [3H]-dihydroalprenolol from human beta2-adrenoceptor expressed in HEK cells after 4 hrs
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.01.043
5152 3394 80 None 16 6 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-dihydroalprenolol from human beta2-adrenoceptor expressed in HEK cells after 4 hrsDisplacement of [3H]-dihydroalprenolol from human beta2-adrenoceptor expressed in HEK cells after 4 hrs
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.01.043
559 3394 80 None 16 6 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-dihydroalprenolol from human beta2-adrenoceptor expressed in HEK cells after 4 hrsDisplacement of [3H]-dihydroalprenolol from human beta2-adrenoceptor expressed in HEK cells after 4 hrs
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.01.043
CHEMBL1263 3394 80 None 16 6 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-dihydroalprenolol from human beta2-adrenoceptor expressed in HEK cells after 4 hrsDisplacement of [3H]-dihydroalprenolol from human beta2-adrenoceptor expressed in HEK cells after 4 hrs
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.01.043
DB00938 3394 80 None 16 6 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-dihydroalprenolol from human beta2-adrenoceptor expressed in HEK cells after 4 hrsDisplacement of [3H]-dihydroalprenolol from human beta2-adrenoceptor expressed in HEK cells after 4 hrs
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.01.043
1499 2052 43 None -33 17 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2013.11.030
3779 2052 43 None -33 17 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2013.11.030
536 2052 43 None -33 17 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2013.11.030
CHEMBL434 2052 43 None -33 17 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2013.11.030
DB01064 2052 43 None -33 17 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2013.11.030
11647002 15447 0 None 22 3 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assay
ChEMBL 400 7 4 6 3.1 O=c1[nH]c2c(O)ccc([C@@H](O)CN[C@H]3CCC[C@@H]3OCc3ccccc3)c2s1 10.1016/j.bmcl.2014.06.014
CHEMBL1221681 15447 0 None 22 3 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assay
ChEMBL 400 7 4 6 3.1 O=c1[nH]c2c(O)ccc([C@@H](O)CN[C@H]3CCC[C@@H]3OCc3ccccc3)c2s1 10.1016/j.bmcl.2014.06.014
44391257 65761 0 None -1 2 Human 8.6 pKi = 8.6 Binding
Binding affinity for human beta-2 adrenergic receptor by displacing [125I]iodocyanopindolol expressed in hamster CHO cellsBinding affinity for human beta-2 adrenergic receptor by displacing [125I]iodocyanopindolol expressed in hamster CHO cells
ChEMBL 411 9 4 6 2.3 CC(COc1ccc2c(c1)NC(=O)CO2)NCC(O)COc1cccc2[nH]ccc12 10.1016/j.bmcl.2004.11.030
CHEMBL183921 65761 0 None -1 2 Human 8.6 pKi = 8.6 Binding
Binding affinity for human beta-2 adrenergic receptor by displacing [125I]iodocyanopindolol expressed in hamster CHO cellsBinding affinity for human beta-2 adrenergic receptor by displacing [125I]iodocyanopindolol expressed in hamster CHO cells
ChEMBL 411 9 4 6 2.3 CC(COc1ccc2c(c1)NC(=O)CO2)NCC(O)COc1cccc2[nH]ccc12 10.1016/j.bmcl.2004.11.030
2419 3394 80 None 16 6 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2014.04.069
5152 3394 80 None 16 6 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2014.04.069
559 3394 80 None 16 6 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2014.04.069
CHEMBL1263 3394 80 None 16 6 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2014.04.069
DB00938 3394 80 None 16 6 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2014.04.069
2419 3394 80 None 16 6 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assayDisplacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2014.04.095
5152 3394 80 None 16 6 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assayDisplacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2014.04.095
559 3394 80 None 16 6 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assayDisplacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2014.04.095
CHEMBL1263 3394 80 None 16 6 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assayDisplacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2014.04.095
DB00938 3394 80 None 16 6 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assayDisplacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2014.04.095
1239 1639 46 None 63 4 Human 8.6 pKi = 8.6 Binding
Binding affinity for human beta-2 adrenergic receptorBinding affinity for human beta-2 adrenergic receptor
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2004.06.086
3410 1639 46 None 63 4 Human 8.6 pKi = 8.6 Binding
Binding affinity for human beta-2 adrenergic receptorBinding affinity for human beta-2 adrenergic receptor
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2004.06.086
3465 1639 46 None 63 4 Human 8.6 pKi = 8.6 Binding
Binding affinity for human beta-2 adrenergic receptorBinding affinity for human beta-2 adrenergic receptor
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2004.06.086
CHEMBL1256786 1639 46 None 63 4 Human 8.6 pKi = 8.6 Binding
Binding affinity for human beta-2 adrenergic receptorBinding affinity for human beta-2 adrenergic receptor
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2004.06.086
DB00983 1639 46 None 63 4 Human 8.6 pKi = 8.6 Binding
Binding affinity for human beta-2 adrenergic receptorBinding affinity for human beta-2 adrenergic receptor
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2004.06.086
1239 1639 46 None 63 4 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.06.014
3410 1639 46 None 63 4 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.06.014
3465 1639 46 None 63 4 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.06.014
CHEMBL1256786 1639 46 None 63 4 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.06.014
DB00983 1639 46 None 63 4 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.06.014
1239 1639 46 None 63 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptorDisplacement of [3H]CGP12177 from human beta2 adrenoceptor
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2010.06.136
3410 1639 46 None 63 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptorDisplacement of [3H]CGP12177 from human beta2 adrenoceptor
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2010.06.136
3465 1639 46 None 63 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptorDisplacement of [3H]CGP12177 from human beta2 adrenoceptor
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2010.06.136
CHEMBL1256786 1639 46 None 63 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptorDisplacement of [3H]CGP12177 from human beta2 adrenoceptor
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2010.06.136
DB00983 1639 46 None 63 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptorDisplacement of [3H]CGP12177 from human beta2 adrenoceptor
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2010.06.136
9984829 34903 0 None 1 2 Dog 8.6 pKi = 8.6 Binding
Beta-2 adrenergic receptor binding affinity by measuring the displacement of [3H]DHA binding in rat lungBeta-2 adrenergic receptor binding affinity by measuring the displacement of [3H]DHA binding in rat lung
ChEMBL 542 11 2 8 3.5 COc1ccccc1N1CCN(CCCN2C(=O)CSc3c(OCC(O)CNC(C)(C)C)cccc32)CC1 10.1016/s0960-894x(00)00016-0
CHEMBL143463 34903 0 None 1 2 Dog 8.6 pKi = 8.6 Binding
Beta-2 adrenergic receptor binding affinity by measuring the displacement of [3H]DHA binding in rat lungBeta-2 adrenergic receptor binding affinity by measuring the displacement of [3H]DHA binding in rat lung
ChEMBL 542 11 2 8 3.5 COc1ccccc1N1CCN(CCCN2C(=O)CSc3c(OCC(O)CNC(C)(C)C)cccc32)CC1 10.1016/s0960-894x(00)00016-0
49864380 15442 0 None -1 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptorDisplacement of [3H]CGP12177 from human beta2 adrenoceptor
ChEMBL 380 5 4 5 3.8 C[C@@H](NC[C@H](O)c1ccc(O)c2[nH]c(=O)sc12)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.06.136
CHEMBL1221637 15442 0 None -1 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptorDisplacement of [3H]CGP12177 from human beta2 adrenoceptor
ChEMBL 380 5 4 5 3.8 C[C@@H](NC[C@H](O)c1ccc(O)c2[nH]c(=O)sc12)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.06.136
127047859 139508 0 None 1 6 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cellsDisplacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells
ChEMBL 476 12 3 6 4.1 COc1cc(CCNCCc2ccc(O)c3c2OCC(=O)N3)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
CHEMBL3800341 139508 0 None 1 6 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cellsDisplacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells
ChEMBL 476 12 3 6 4.1 COc1cc(CCNCCc2ccc(O)c3c2OCC(=O)N3)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
44423643 141512 0 None 8 3 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]CYP from human adrenergic beta 2 receptor transfected in CHO cells in presence of 100 uM GTPDisplacement of [125I]CYP from human adrenergic beta 2 receptor transfected in CHO cells in presence of 100 uM GTP
ChEMBL 426 10 2 7 2.6 CCOC(=O)COc1ccc(C[C@@H](C)NC[C@H](O)c2cc(Br)no2)cc1 10.1016/j.bmc.2007.01.056
CHEMBL387852 141512 0 None 8 3 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]CYP from human adrenergic beta 2 receptor transfected in CHO cells in presence of 100 uM GTPDisplacement of [125I]CYP from human adrenergic beta 2 receptor transfected in CHO cells in presence of 100 uM GTP
ChEMBL 426 10 2 7 2.6 CCOC(=O)COc1ccc(C[C@@H](C)NC[C@H](O)c2cc(Br)no2)cc1 10.1016/j.bmc.2007.01.056
155526570 170586 0 None 999 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H](-)CGP 12177 from human recombinant beta2 adrenoceptor after 120 mins by scintillation counting methodDisplacement of [3H](-)CGP 12177 from human recombinant beta2 adrenoceptor after 120 mins by scintillation counting method
ChEMBL 471 20 4 8 1.2 CC(C)NCC(O)COc1ccccc1CCCSCC(=O)NCCOCCOCCN 10.1039/C8MD00412A
CHEMBL4458797 170586 0 None 999 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H](-)CGP 12177 from human recombinant beta2 adrenoceptor after 120 mins by scintillation counting methodDisplacement of [3H](-)CGP 12177 from human recombinant beta2 adrenoceptor after 120 mins by scintillation counting method
ChEMBL 471 20 4 8 1.2 CC(C)NCC(O)COc1ccccc1CCCSCC(=O)NCCOCCOCCN 10.1039/C8MD00412A
44396798 168815 0 None -18 3 Human 7.7 pKi = 7.7 Binding
Binding inhibition constant was determined by inhibition of [125I]iodocyanopindolol binding to Beta-2 adrenergic receptorBinding inhibition constant was determined by inhibition of [125I]iodocyanopindolol binding to Beta-2 adrenergic receptor
ChEMBL 542 10 5 7 3.2 C[C@H](Cc1c[nH]c2c(S(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccc(N)c2)c1 10.1016/j.bmcl.2004.09.054
CHEMBL442225 168815 0 None -18 3 Human 7.7 pKi = 7.7 Binding
Binding inhibition constant was determined by inhibition of [125I]iodocyanopindolol binding to Beta-2 adrenergic receptorBinding inhibition constant was determined by inhibition of [125I]iodocyanopindolol binding to Beta-2 adrenergic receptor
ChEMBL 542 10 5 7 3.2 C[C@H](Cc1c[nH]c2c(S(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccc(N)c2)c1 10.1016/j.bmcl.2004.09.054
24936882 17385 0 None 3 3 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 512 9 4 10 3.6 OCc1cc(OCC(O)CNC2CCN(c3ncnc4scc(-c5cccs5)c34)CC2)ccc1O 10.1016/j.bmcl.2010.08.039
CHEMBL1258143 17385 0 None 3 3 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 512 9 4 10 3.6 OCc1cc(OCC(O)CNC2CCN(c3ncnc4scc(-c5cccs5)c34)CC2)ccc1O 10.1016/j.bmcl.2010.08.039
155561031 174413 0 None 1 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranesDisplacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranes
ChEMBL 524 20 3 9 3.6 COCCc1ccc(OC[C@@H](O)CNCCc2ccc(OCCCSSCCN)c(OC)c2)cc1 10.1016/j.bmc.2019.05.034
CHEMBL4566666 174413 0 None 1 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranesDisplacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranes
ChEMBL 524 20 3 9 3.6 COCCc1ccc(OC[C@@H](O)CNCCc2ccc(OCCCSSCCN)c(OC)c2)cc1 10.1016/j.bmc.2019.05.034
4183 1986 62 None 2 3 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assay
ChEMBL 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O 10.1016/j.bmcl.2014.06.014
6918554 1986 62 None 2 3 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assay
ChEMBL 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O 10.1016/j.bmcl.2014.06.014
7455 1986 62 None 2 3 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assay
ChEMBL 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O 10.1016/j.bmcl.2014.06.014
CHEMBL1095777 1986 62 None 2 3 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assay
ChEMBL 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O 10.1016/j.bmcl.2014.06.014
DB05039 1986 62 None 2 3 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assay
ChEMBL 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O 10.1016/j.bmcl.2014.06.014
4183 1986 62 None 2 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptorDisplacement of [3H]CGP12177 from human beta2 adrenoceptor
ChEMBL 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O 10.1016/j.bmcl.2010.06.136
6918554 1986 62 None 2 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptorDisplacement of [3H]CGP12177 from human beta2 adrenoceptor
ChEMBL 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O 10.1016/j.bmcl.2010.06.136
7455 1986 62 None 2 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptorDisplacement of [3H]CGP12177 from human beta2 adrenoceptor
ChEMBL 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O 10.1016/j.bmcl.2010.06.136
CHEMBL1095777 1986 62 None 2 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptorDisplacement of [3H]CGP12177 from human beta2 adrenoceptor
ChEMBL 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O 10.1016/j.bmcl.2010.06.136
DB05039 1986 62 None 2 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptorDisplacement of [3H]CGP12177 from human beta2 adrenoceptor
ChEMBL 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O 10.1016/j.bmcl.2010.06.136
44444188 94046 0 None 1 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]iodocyanopindolol from human cloned adrenergic beta-2 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human cloned adrenergic beta-2 receptor expressed in CHO cells
ChEMBL 484 12 4 6 3.6 COc1cccc([C@H](CCc2ccccc2)NC[C@H](O)Cc2ccc(O)c(NS(C)(=O)=O)c2)c1 10.1016/j.bmcl.2007.05.030
CHEMBL251554 94046 0 None 1 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]iodocyanopindolol from human cloned adrenergic beta-2 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human cloned adrenergic beta-2 receptor expressed in CHO cells
ChEMBL 484 12 4 6 3.6 COc1cccc([C@H](CCc2ccccc2)NC[C@H](O)Cc2ccc(O)c(NS(C)(=O)=O)c2)c1 10.1016/j.bmcl.2007.05.030
155516656 169549 0 None -40 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranesDisplacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranes
ChEMBL 629 18 4 11 3.3 Cn1cc(C(F)(F)F)nc1-c1ccc(OC[C@@H](O)CNCCOc2ccc(OCCSSCCN)c(C(N)=O)c2)cc1 10.1016/j.bmc.2019.05.034
CHEMBL4443911 169549 0 None -40 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranesDisplacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranes
ChEMBL 629 18 4 11 3.3 Cn1cc(C(F)(F)F)nc1-c1ccc(OC[C@@H](O)CNCCOc2ccc(OCCSSCCN)c(C(N)=O)c2)cc1 10.1016/j.bmc.2019.05.034
10083242 13707 0 None -5 3 Guinea pig 5.7 pKi = 5.7 Binding
Binding affinity against Beta-2 adrenergic receptor was measured using [125I]CYP as radioligandBinding affinity against Beta-2 adrenergic receptor was measured using [125I]CYP as radioligand
ChEMBL 245 2 1 5 1.3 CC(C)c1cnc2c(N3CCNCC3)nccn12 10.1021/jm00099a012
CHEMBL1195814 13707 0 None -5 3 Guinea pig 5.7 pKi = 5.7 Binding
Binding affinity against Beta-2 adrenergic receptor was measured using [125I]CYP as radioligandBinding affinity against Beta-2 adrenergic receptor was measured using [125I]CYP as radioligand
ChEMBL 245 2 1 5 1.3 CC(C)c1cnc2c(N3CCNCC3)nccn12 10.1021/jm00099a012
CHEMBL555391 13707 0 None -5 3 Guinea pig 5.7 pKi = 5.7 Binding
Binding affinity against Beta-2 adrenergic receptor was measured using [125I]CYP as radioligandBinding affinity against Beta-2 adrenergic receptor was measured using [125I]CYP as radioligand
ChEMBL 245 2 1 5 1.3 CC(C)c1cnc2c(N3CCNCC3)nccn12 10.1021/jm00099a012
73056758 103787 0 None - 1 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]-CGP-12177 from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-CGP-12177 from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 331 8 4 5 2.8 CC[C@@H](Cc1ccc(OC)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2013.11.030
CHEMBL3099660 103787 0 None - 1 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]-CGP-12177 from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-CGP-12177 from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 331 8 4 5 2.8 CC[C@@H](Cc1ccc(OC)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2013.11.030
12475776 163548 7 None - 1 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]-DHA from Nb80-fused beta2 adrenergic receptor (unknown origin) expressed in Sf9 cell membranes after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-DHA from Nb80-fused beta2 adrenergic receptor (unknown origin) expressed in Sf9 cell membranes after 2 hrs by microbeta scintillation counting method
ChEMBL 204 3 1 3 1.7 COc1ccc2c(c1)c(CCN)cn2C 10.1021/acs.jmedchem.7b01558
CHEMBL4209786 163548 7 None - 1 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]-DHA from Nb80-fused beta2 adrenergic receptor (unknown origin) expressed in Sf9 cell membranes after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-DHA from Nb80-fused beta2 adrenergic receptor (unknown origin) expressed in Sf9 cell membranes after 2 hrs by microbeta scintillation counting method
ChEMBL 204 3 1 3 1.7 COc1ccc2c(c1)c(CCN)cn2C 10.1021/acs.jmedchem.7b01558
16736514 142998 0 None 2 2 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 273 6 4 4 2.0 Oc1cc(O)cc([C@H](O)CNCCc2ccccc2)c1 10.1021/jm070030d
CHEMBL389902 142998 0 None 2 2 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 273 6 4 4 2.0 Oc1cc(O)cc([C@H](O)CNCCc2ccccc2)c1 10.1021/jm070030d
16736514 142998 0 None 2 2 Human 4.7 pKi = 4.7 Binding
Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.
ChEMBL 273 6 4 4 2.0 Oc1cc(O)cc([C@H](O)CNCCc2ccccc2)c1 nan
CHEMBL389902 142998 0 None 2 2 Human 4.7 pKi = 4.7 Binding
Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.
ChEMBL 273 6 4 4 2.0 Oc1cc(O)cc([C@H](O)CNCCc2ccccc2)c1 nan
16736514 142998 0 None 2 2 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 273 6 4 4 2.0 Oc1cc(O)cc([C@H](O)CNCCc2ccccc2)c1 10.1021/jm070030d
CHEMBL389902 142998 0 None 2 2 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 273 6 4 4 2.0 Oc1cc(O)cc([C@H](O)CNCCc2ccccc2)c1 10.1021/jm070030d
1599 2299 47 None -131 16 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 nan
3955 2299 47 None -131 16 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 nan
7215 2299 47 None -131 16 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 nan
CHEMBL841 2299 47 None -131 16 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 nan
DB00836 2299 47 None -131 16 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 nan
9967732 93717 0 None 19 2 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]iodocyanopindolol from human adrenergic beta-2 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human adrenergic beta-2 receptor expressed in CHO cells
ChEMBL 339 8 2 6 2.7 Cc1nc(-c2ccc(OCCNC[C@H](O)c3cccnc3)cc2)co1 10.1016/j.bmcl.2007.06.072
CHEMBL249534 93717 0 None 19 2 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]iodocyanopindolol from human adrenergic beta-2 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human adrenergic beta-2 receptor expressed in CHO cells
ChEMBL 339 8 2 6 2.7 Cc1nc(-c2ccc(OCCNC[C@H](O)c3cccnc3)cc2)co1 10.1016/j.bmcl.2007.06.072
146025802 169000 0 None -1 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assay
ChEMBL 349 10 4 7 1.5 COc1ccccc1OCCNC[C@H](O)COc1ccc(O)c(O)c1 10.1021/acs.jmedchem.9b00349
CHEMBL4435895 169000 0 None -1 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assay
ChEMBL 349 10 4 7 1.5 COc1ccccc1OCCNC[C@H](O)COc1ccc(O)c(O)c1 10.1021/acs.jmedchem.9b00349
10348864 58216 0 None -147 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-dihydroalprenolol from human beta2-adrenoceptor expressed in HEK cells after 4 hrsDisplacement of [3H]-dihydroalprenolol from human beta2-adrenoceptor expressed in HEK cells after 4 hrs
ChEMBL 616 18 5 7 6.7 O=CNc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)ccc1O 10.1016/j.bmcl.2011.01.043
CHEMBL1683935 58216 0 None -147 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-dihydroalprenolol from human beta2-adrenoceptor expressed in HEK cells after 4 hrsDisplacement of [3H]-dihydroalprenolol from human beta2-adrenoceptor expressed in HEK cells after 4 hrs
ChEMBL 616 18 5 7 6.7 O=CNc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)ccc1O 10.1016/j.bmcl.2011.01.043
9894801 120212 0 None 4 2 Human 5.7 pKi = 5.7 Binding
Inhibition of 125 I-Iodocyanopindolol binding to Beta-2 adrenergic receptorInhibition of 125 I-Iodocyanopindolol binding to Beta-2 adrenergic receptor
ChEMBL 592 11 5 10 1.7 CS(=O)(=O)Nc1cc([C@@H](O)CNC2CCN(c3ccc(CC4SC(=O)N(CC(=O)O)C4=O)cc3)CC2)ccc1O 10.1016/s0960-894x(01)00147-0
CHEMBL354906 120212 0 None 4 2 Human 5.7 pKi = 5.7 Binding
Inhibition of 125 I-Iodocyanopindolol binding to Beta-2 adrenergic receptorInhibition of 125 I-Iodocyanopindolol binding to Beta-2 adrenergic receptor
ChEMBL 592 11 5 10 1.7 CS(=O)(=O)Nc1cc([C@@H](O)CNC2CCN(c3ccc(CC4SC(=O)N(CC(=O)O)C4=O)cc3)CC2)ccc1O 10.1016/s0960-894x(01)00147-0
14485416 164108 0 None - 1 Mouse 5.7 pKi = 5.7 Binding
Ki value was determined by accumulation of c-AMP in S-49 mouse lymphoma cells (Beta2).Ki value was determined by accumulation of c-AMP in S-49 mouse lymphoma cells (Beta2).
ChEMBL 495 13 4 5 4.6 CC(=O)Nc1ccc(OC[C@H](O)CN[C@H](C)CCCCC(=O)Nc2ccc(C(F)(F)F)cc2)cc1 10.1021/jm00163a036
CHEMBL421682 164108 0 None - 1 Mouse 5.7 pKi = 5.7 Binding
Ki value was determined by accumulation of c-AMP in S-49 mouse lymphoma cells (Beta2).Ki value was determined by accumulation of c-AMP in S-49 mouse lymphoma cells (Beta2).
ChEMBL 495 13 4 5 4.6 CC(=O)Nc1ccc(OC[C@H](O)CN[C@H](C)CCCCC(=O)Nc2ccc(C(F)(F)F)cc2)cc1 10.1021/jm00163a036
46221395 8429 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]cyanopindolol from human recombinant beta2 adrenergic receptor expressed in CHO cells by filtration assayDisplacement of [125I]cyanopindolol from human recombinant beta2 adrenergic receptor expressed in CHO cells by filtration assay
ChEMBL 336 4 4 4 2.0 O=c1ccc2c([C@@H](O)CNC3Cc4ccccc4C3)ccc(O)c2[nH]1 10.1021/jm100068m
CHEMBL1094323 8429 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]cyanopindolol from human recombinant beta2 adrenergic receptor expressed in CHO cells by filtration assayDisplacement of [125I]cyanopindolol from human recombinant beta2 adrenergic receptor expressed in CHO cells by filtration assay
ChEMBL 336 4 4 4 2.0 O=c1ccc2c([C@@H](O)CNC3Cc4ccccc4C3)ccc(O)c2[nH]1 10.1021/jm100068m
10431900 63294 0 None 10 2 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-CYP from human beta2-adrenergic receptor expressed in COS-7 cells by gamma countingDisplacement of [125I]-CYP from human beta2-adrenergic receptor expressed in COS-7 cells by gamma counting
ChEMBL 413 16 4 4 5.3 OCc1cc(C(O)CNCCCCCCCCCCCc2ccccc2)ccc1O 10.1016/j.bmc.2009.11.062
CHEMBL1800935 63294 0 None 10 2 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-CYP from human beta2-adrenergic receptor expressed in COS-7 cells by gamma countingDisplacement of [125I]-CYP from human beta2-adrenergic receptor expressed in COS-7 cells by gamma counting
ChEMBL 413 16 4 4 5.3 OCc1cc(C(O)CNCCCCCCCCCCCc2ccccc2)ccc1O 10.1016/j.bmc.2009.11.062
1786 2474 79 None -25 11 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranesDisplacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranes
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1016/j.bmc.2019.05.034
4171 2474 79 None -25 11 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranesDisplacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranes
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1016/j.bmc.2019.05.034
553 2474 79 None -25 11 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranesDisplacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranes
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1016/j.bmc.2019.05.034
CHEMBL13 2474 79 None -25 11 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranesDisplacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranes
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1016/j.bmc.2019.05.034
DB00264 2474 79 None -25 11 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranesDisplacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranes
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1016/j.bmc.2019.05.034
155521165 169980 0 None -14 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranesDisplacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranes
ChEMBL 600 17 3 10 4.4 COc1cc(CCNC[C@H](O)COc2ccc(-c3nc(C(F)(F)F)cn3C)cc2)ccc1OCCSSCCN 10.1016/j.bmc.2019.05.034
CHEMBL4450085 169980 0 None -14 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranesDisplacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranes
ChEMBL 600 17 3 10 4.4 COc1cc(CCNC[C@H](O)COc2ccc(-c3nc(C(F)(F)F)cn3C)cc2)ccc1OCCSSCCN 10.1016/j.bmc.2019.05.034
71612644 132829 0 None -2 2 Human 4.7 pKi = 4.7 Binding
Inhibition Assay: Human recombinant adrenergic β2 receptors expressed in CHO cells are used in modified Tris-HCl buffer pH 7.4. A 50 aliquot is incubated with 0.2 nM [3H]CGP-12177 for 60 minutes at 25° C. Non-specific binding is estimated in the presence of 10 μM ICI-118551. Receptors are filtered and washed, the filters are then counted to determine [3H]CGP-12177 specifically bound. Compounds are screened at 10 μM.Inhibition Assay: Human recombinant adrenergic β2 receptors expressed in CHO cells are used in modified Tris-HCl buffer pH 7.4. A 50 aliquot is incubated with 0.2 nM [3H]CGP-12177 for 60 minutes at 25° C. Non-specific binding is estimated in the presence of 10 μM ICI-118551. Receptors are filtered and washed, the filters are then counted to determine [3H]CGP-12177 specifically bound. Compounds are screened at 10 μM.
ChEMBL 303 7 2 5 0.5 N#CC1CCCN1C(=O)CNCC(O)COc1ccccc1 nan
CHEMBL3704833 132829 0 None -2 2 Human 4.7 pKi = 4.7 Binding
Inhibition Assay: Human recombinant adrenergic β2 receptors expressed in CHO cells are used in modified Tris-HCl buffer pH 7.4. A 50 aliquot is incubated with 0.2 nM [3H]CGP-12177 for 60 minutes at 25° C. Non-specific binding is estimated in the presence of 10 μM ICI-118551. Receptors are filtered and washed, the filters are then counted to determine [3H]CGP-12177 specifically bound. Compounds are screened at 10 μM.Inhibition Assay: Human recombinant adrenergic β2 receptors expressed in CHO cells are used in modified Tris-HCl buffer pH 7.4. A 50 aliquot is incubated with 0.2 nM [3H]CGP-12177 for 60 minutes at 25° C. Non-specific binding is estimated in the presence of 10 μM ICI-118551. Receptors are filtered and washed, the filters are then counted to determine [3H]CGP-12177 specifically bound. Compounds are screened at 10 μM.
ChEMBL 303 7 2 5 0.5 N#CC1CCCN1C(=O)CNCC(O)COc1ccccc1 nan
44396659 67012 0 None -6 3 Human 6.7 pKi = 6.7 Binding
Binding inhibition constant was determined by inhibition of [125I]iodocyanopindolol binding to Beta-2 adrenergic receptorBinding inhibition constant was determined by inhibition of [125I]iodocyanopindolol binding to Beta-2 adrenergic receptor
ChEMBL 535 11 4 8 3.2 CS(=O)(=O)Oc1cccc2c(CCNC[C@H](O)c3cccc(NS(=O)(=O)c4cccs4)c3)c[nH]c12 10.1016/j.bmcl.2004.09.054
CHEMBL188622 67012 0 None -6 3 Human 6.7 pKi = 6.7 Binding
Binding inhibition constant was determined by inhibition of [125I]iodocyanopindolol binding to Beta-2 adrenergic receptorBinding inhibition constant was determined by inhibition of [125I]iodocyanopindolol binding to Beta-2 adrenergic receptor
ChEMBL 535 11 4 8 3.2 CS(=O)(=O)Oc1cccc2c(CCNC[C@H](O)c3cccc(NS(=O)(=O)c4cccs4)c3)c[nH]c12 10.1016/j.bmcl.2004.09.054
24936627 17489 0 None 4 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 444 8 4 9 2.2 Cc1csc2ncnc(N3CCC(NCC(O)COc4ccc(O)c(CO)c4)CC3)c12 10.1016/j.bmcl.2010.08.039
CHEMBL1258485 17489 0 None 4 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 444 8 4 9 2.2 Cc1csc2ncnc(N3CCC(NCC(O)COc4ccc(O)c(CO)c4)CC3)c12 10.1016/j.bmcl.2010.08.039
9908924 141111 0 None -2 3 Human 5.7 pKi = 5.7 Binding
Ability to bind to human Beta-2 adrenergic receptor using membranes of stably transfected CHO cellsAbility to bind to human Beta-2 adrenergic receptor using membranes of stably transfected CHO cells
ChEMBL 399 9 3 5 2.8 C[C@H](Cc1ccc(OCS(=O)(=O)O)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1016/S0960-894X(97)00266-7
CHEMBL38538 141111 0 None -2 3 Human 5.7 pKi = 5.7 Binding
Ability to bind to human Beta-2 adrenergic receptor using membranes of stably transfected CHO cellsAbility to bind to human Beta-2 adrenergic receptor using membranes of stably transfected CHO cells
ChEMBL 399 9 3 5 2.8 C[C@H](Cc1ccc(OCS(=O)(=O)O)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1016/S0960-894X(97)00266-7
44581972 175017 0 None -75 10 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]iodocyanopindolol from adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from adrenergic beta2 receptor expressed in CHO cells
ChEMBL 499 6 2 6 4.3 O=C(Nc1cccc(Cn2ncc(N3CCNCC3)c(Cl)c2=O)c1)c1ccc(-c2ccccc2)cc1 10.1021/jm800962k
CHEMBL458001 175017 0 None -75 10 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]iodocyanopindolol from adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from adrenergic beta2 receptor expressed in CHO cells
ChEMBL 499 6 2 6 4.3 O=C(Nc1cccc(Cn2ncc(N3CCNCC3)c(Cl)c2=O)c1)c1ccc(-c2ccccc2)cc1 10.1021/jm800962k
16735494 141508 0 None 3 2 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 287 6 4 4 2.4 C[C@H](Cc1ccccc1)NC[C@@H](O)c1cc(O)cc(O)c1 10.1021/jm070030d
CHEMBL387825 141508 0 None 3 2 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 287 6 4 4 2.4 C[C@H](Cc1ccccc1)NC[C@@H](O)c1cc(O)cc(O)c1 10.1021/jm070030d
25023953 186790 0 None - 1 Golden hamster 5.6 pKi = 5.6 Binding
Displacement of [125I](-)-iodopindolol from adrenergic beta2 receptor in Syrian hamster DDT1 MF2 cellsDisplacement of [125I](-)-iodopindolol from adrenergic beta2 receptor in Syrian hamster DDT1 MF2 cells
ChEMBL 577 17 8 15 -1.5 O=CNc1cc(C(O)CNCCOCCOCCNc2ncnc3c2ncn3[C@@H]2O[C@H](CO)[C@@H](O)[C@H]2O)ccc1O 10.1021/jm800613s
CHEMBL493489 186790 0 None - 1 Golden hamster 5.6 pKi = 5.6 Binding
Displacement of [125I](-)-iodopindolol from adrenergic beta2 receptor in Syrian hamster DDT1 MF2 cellsDisplacement of [125I](-)-iodopindolol from adrenergic beta2 receptor in Syrian hamster DDT1 MF2 cells
ChEMBL 577 17 8 15 -1.5 O=CNc1cc(C(O)CNCCOCCOCCNc2ncnc3c2ncn3[C@@H]2O[C@H](CO)[C@@H](O)[C@H]2O)ccc1O 10.1021/jm800613s
131645 31922 7 None -1 2 Dog 7.6 pKi = 7.6 Binding
Beta-2 adrenergic receptor binding affinity by measuring the displacement of [3H]DHA binding in rat lungBeta-2 adrenergic receptor binding affinity by measuring the displacement of [3H]DHA binding in rat lung
ChEMBL 310 5 3 5 1.9 CC(C)(C)NCC(O)COc1cccc2c1SCC(=O)N2 10.1016/s0960-894x(00)00016-0
CHEMBL140908 31922 7 None -1 2 Dog 7.6 pKi = 7.6 Binding
Beta-2 adrenergic receptor binding affinity by measuring the displacement of [3H]DHA binding in rat lungBeta-2 adrenergic receptor binding affinity by measuring the displacement of [3H]DHA binding in rat lung
ChEMBL 310 5 3 5 1.9 CC(C)(C)NCC(O)COc1cccc2c1SCC(=O)N2 10.1016/s0960-894x(00)00016-0
1239 1639 46 None 63 4 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]cyanopindolol from human recombinant beta2 adrenergic receptor expressed in CHO cells by filtration assayDisplacement of [125I]cyanopindolol from human recombinant beta2 adrenergic receptor expressed in CHO cells by filtration assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1021/jm100068m
3410 1639 46 None 63 4 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]cyanopindolol from human recombinant beta2 adrenergic receptor expressed in CHO cells by filtration assayDisplacement of [125I]cyanopindolol from human recombinant beta2 adrenergic receptor expressed in CHO cells by filtration assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1021/jm100068m
3465 1639 46 None 63 4 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]cyanopindolol from human recombinant beta2 adrenergic receptor expressed in CHO cells by filtration assayDisplacement of [125I]cyanopindolol from human recombinant beta2 adrenergic receptor expressed in CHO cells by filtration assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1021/jm100068m
CHEMBL1256786 1639 46 None 63 4 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]cyanopindolol from human recombinant beta2 adrenergic receptor expressed in CHO cells by filtration assayDisplacement of [125I]cyanopindolol from human recombinant beta2 adrenergic receptor expressed in CHO cells by filtration assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1021/jm100068m
DB00983 1639 46 None 63 4 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]cyanopindolol from human recombinant beta2 adrenergic receptor expressed in CHO cells by filtration assayDisplacement of [125I]cyanopindolol from human recombinant beta2 adrenergic receptor expressed in CHO cells by filtration assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1021/jm100068m
127046948 139527 0 None 13 6 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cellsDisplacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells
ChEMBL 488 12 4 6 4.1 COc1cc(CCNC[C@@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
CHEMBL3800468 139527 0 None 13 6 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cellsDisplacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells
ChEMBL 488 12 4 6 4.1 COc1cc(CCNC[C@@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
4292932 169646 1 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]DHA from human beta2 adrenoceptor by liquid scintillation counterDisplacement of [3H]DHA from human beta2 adrenoceptor by liquid scintillation counter
ChEMBL 319 7 4 4 1.3 CC(C)(C)NCC(O)COc1cccc2[nH]cc(CC(N)=O)c12 10.1016/j.bmcl.2008.09.046
CHEMBL444553 169646 1 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]DHA from human beta2 adrenoceptor by liquid scintillation counterDisplacement of [3H]DHA from human beta2 adrenoceptor by liquid scintillation counter
ChEMBL 319 7 4 4 1.3 CC(C)(C)NCC(O)COc1cccc2[nH]cc(CC(N)=O)c12 10.1016/j.bmcl.2008.09.046
24321330 6743 0 None 1 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cells
ChEMBL 486 8 1 5 4.7 CC(C)c1ccccc1OCC(O)CN1CCC(CN2C(=O)c3cccc4cccc(c34)C2=O)CC1 10.1016/j.bmcl.2010.04.009
CHEMBL1083996 6743 0 None 1 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cells
ChEMBL 486 8 1 5 4.7 CC(C)c1ccccc1OCC(O)CN1CCC(CN2C(=O)c3cccc4cccc(c34)C2=O)CC1 10.1016/j.bmcl.2010.04.009
10082076 13733 0 None -9 3 Guinea pig 5.6 pKi = 5.6 Binding
Binding affinity against Beta-2 adrenergic receptor was measured using [125I]CYP as radioligandBinding affinity against Beta-2 adrenergic receptor was measured using [125I]CYP as radioligand
ChEMBL 217 1 1 5 0.4 Cc1cnc2c(N3CCNCC3)nccn12 10.1021/jm00099a012
CHEMBL1195953 13733 0 None -9 3 Guinea pig 5.6 pKi = 5.6 Binding
Binding affinity against Beta-2 adrenergic receptor was measured using [125I]CYP as radioligandBinding affinity against Beta-2 adrenergic receptor was measured using [125I]CYP as radioligand
ChEMBL 217 1 1 5 0.4 Cc1cnc2c(N3CCNCC3)nccn12 10.1021/jm00099a012
CHEMBL555637 13733 0 None -9 3 Guinea pig 5.6 pKi = 5.6 Binding
Binding affinity against Beta-2 adrenergic receptor was measured using [125I]CYP as radioligandBinding affinity against Beta-2 adrenergic receptor was measured using [125I]CYP as radioligand
ChEMBL 217 1 1 5 0.4 Cc1cnc2c(N3CCNCC3)nccn12 10.1021/jm00099a012
16735494 141508 0 None 3 2 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 287 6 4 4 2.4 C[C@H](Cc1ccccc1)NC[C@@H](O)c1cc(O)cc(O)c1 10.1021/jm070030d
CHEMBL387825 141508 0 None 3 2 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 287 6 4 4 2.4 C[C@H](Cc1ccccc1)NC[C@@H](O)c1cc(O)cc(O)c1 10.1021/jm070030d
16735494 141508 0 None 3 2 Human 4.6 pKi = 4.6 Binding
Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.
ChEMBL 287 6 4 4 2.4 C[C@H](Cc1ccccc1)NC[C@@H](O)c1cc(O)cc(O)c1 nan
CHEMBL387825 141508 0 None 3 2 Human 4.6 pKi = 4.6 Binding
Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.
ChEMBL 287 6 4 4 2.4 C[C@H](Cc1ccccc1)NC[C@@H](O)c1cc(O)cc(O)c1 nan
164451 102689 11 None -7 3 Human 5.6 pKi = 5.6 Binding
Compound was tested for its binding affinity against beta2 adrenergic receptor in CHO cell membrane using [125I]iodocyanopindolol as the radioligand.Compound was tested for its binding affinity against beta2 adrenergic receptor in CHO cell membrane using [125I]iodocyanopindolol as the radioligand.
ChEMBL 361 12 3 6 1.6 O=C(O)COc1ccc(OCCNC[C@H](O)COc2ccccc2)cc1 10.1016/0960-894X(96)00417-9
CHEMBL308150 102689 11 None -7 3 Human 5.6 pKi = 5.6 Binding
Compound was tested for its binding affinity against beta2 adrenergic receptor in CHO cell membrane using [125I]iodocyanopindolol as the radioligand.Compound was tested for its binding affinity against beta2 adrenergic receptor in CHO cell membrane using [125I]iodocyanopindolol as the radioligand.
ChEMBL 361 12 3 6 1.6 O=C(O)COc1ccc(OCCNC[C@H](O)COc2ccccc2)cc1 10.1016/0960-894X(96)00417-9
16735495 85345 0 None 14 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 337 6 4 4 3.5 C[C@H](Cc1cccc2ccccc12)NC[C@H](O)c1cc(O)cc(O)c1 10.1021/jm070030d
CHEMBL229401 85345 0 None 14 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 337 6 4 4 3.5 C[C@H](Cc1cccc2ccccc12)NC[C@H](O)c1cc(O)cc(O)c1 10.1021/jm070030d
1836 2544 56 None -53 15 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 nan
3340 2544 56 None -53 15 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 nan
5281040 2544 56 None -53 15 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 nan
CHEMBL787 2544 56 None -53 15 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 nan
DB00471 2544 56 None -53 15 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 nan
44581973 175018 0 None -1122 10 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]iodocyanopindolol from adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from adrenergic beta2 receptor expressed in CHO cells
ChEMBL 513 6 2 6 4.6 Cc1ccc(Cn2ncc(N3CCNCC3)c(Cl)c2=O)cc1NC(=O)c1ccc(-c2ccccc2)cc1 10.1021/jm800962k
CHEMBL458002 175018 0 None -1122 10 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]iodocyanopindolol from adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from adrenergic beta2 receptor expressed in CHO cells
ChEMBL 513 6 2 6 4.6 Cc1ccc(Cn2ncc(N3CCNCC3)c(Cl)c2=O)cc1NC(=O)c1ccc(-c2ccccc2)cc1 10.1021/jm800962k
10207208 153621 0 None -2 3 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]iodocyanopindolol from human cloned adrenergic beta-2 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human cloned adrenergic beta-2 receptor expressed in CHO cells
ChEMBL 500 12 4 7 3.3 COc1ccc([C@H](Cc2ccccc2)NC[C@@H](O)Cc2ccc(O)c(NS(C)(=O)=O)c2)cc1OC 10.1016/j.bmcl.2007.05.030
CHEMBL398557 153621 0 None -2 3 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]iodocyanopindolol from human cloned adrenergic beta-2 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human cloned adrenergic beta-2 receptor expressed in CHO cells
ChEMBL 500 12 4 7 3.3 COc1ccc([C@H](Cc2ccccc2)NC[C@@H](O)Cc2ccc(O)c(NS(C)(=O)=O)c2)cc1OC 10.1016/j.bmcl.2007.05.030
49864332 15421 0 None 6 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptorDisplacement of [3H]CGP12177 from human beta2 adrenoceptor
ChEMBL 310 7 4 5 2.4 CCC(CC)CNC[C@H](O)c1ccc(O)c2[nH]c(=O)sc12 10.1016/j.bmcl.2010.06.136
CHEMBL1221540 15421 0 None 6 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptorDisplacement of [3H]CGP12177 from human beta2 adrenoceptor
ChEMBL 310 7 4 5 2.4 CCC(CC)CNC[C@H](O)c1ccc(O)c2[nH]c(=O)sc12 10.1016/j.bmcl.2010.06.136
16735495 85345 0 None 14 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 337 6 4 4 3.5 C[C@H](Cc1cccc2ccccc12)NC[C@H](O)c1cc(O)cc(O)c1 10.1021/jm070030d
CHEMBL229401 85345 0 None 14 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 337 6 4 4 3.5 C[C@H](Cc1cccc2ccccc12)NC[C@H](O)c1cc(O)cc(O)c1 10.1021/jm070030d
10488284 100701 6 None - 1 Dog 4.6 pKi = 4.6 Binding
Binding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranes
ChEMBL 201 3 4 4 0.5 CNC[C@@H](O)c1ccc(O)c(O)c1F 10.1021/jm990599h
CHEMBL295651 100701 6 None - 1 Dog 4.6 pKi = 4.6 Binding
Binding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranes
ChEMBL 201 3 4 4 0.5 CNC[C@@H](O)c1ccc(O)c(O)c1F 10.1021/jm990599h
16735495 85345 0 None 14 2 Human 6.6 pKi = 6.6 Binding
Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.
ChEMBL 337 6 4 4 3.5 C[C@H](Cc1cccc2ccccc12)NC[C@H](O)c1cc(O)cc(O)c1 nan
CHEMBL229401 85345 0 None 14 2 Human 6.6 pKi = 6.6 Binding
Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.
ChEMBL 337 6 4 4 3.5 C[C@H](Cc1cccc2ccccc12)NC[C@H](O)c1cc(O)cc(O)c1 nan
155286375 184789 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to beta2 adrenoceptor (unknown origin)Binding affinity to beta2 adrenoceptor (unknown origin)
ChEMBL 299 3 4 4 2.1 Oc1ccc2c(c1O)CC[C@@H](NCC1CC(F)(F)C1)[C@@H]2O 10.1021/acs.jmedchem.0c01195
CHEMBL4860571 184789 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to beta2 adrenoceptor (unknown origin)Binding affinity to beta2 adrenoceptor (unknown origin)
ChEMBL 299 3 4 4 2.1 Oc1ccc2c(c1O)CC[C@@H](NCC1CC(F)(F)C1)[C@@H]2O 10.1021/acs.jmedchem.0c01195
155314047 185356 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to beta2 adrenoceptor (unknown origin)Binding affinity to beta2 adrenoceptor (unknown origin)
ChEMBL 263 2 4 4 2.0 Oc1ccc2c(c1O)CC[C@@H](NC1CCCC1)[C@@H]2O 10.1021/acs.jmedchem.0c01195
CHEMBL4869517 185356 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to beta2 adrenoceptor (unknown origin)Binding affinity to beta2 adrenoceptor (unknown origin)
ChEMBL 263 2 4 4 2.0 Oc1ccc2c(c1O)CC[C@@H](NC1CCCC1)[C@@H]2O 10.1021/acs.jmedchem.0c01195
44396596 122771 0 None -1 3 Human 7.6 pKi = 7.6 Binding
Binding inhibition constant was determined by inhibition of [125I]iodocyanopindolol binding to Beta-2 adrenergic receptorBinding inhibition constant was determined by inhibition of [125I]iodocyanopindolol binding to Beta-2 adrenergic receptor
ChEMBL 485 10 4 6 4.3 COc1cccc2c(C[C@@H](C)NC[C@H](O)c3cccc(NS(=O)(=O)c4cccs4)c3)c[nH]c12 10.1016/j.bmcl.2004.10.035
CHEMBL361505 122771 0 None -1 3 Human 7.6 pKi = 7.6 Binding
Binding inhibition constant was determined by inhibition of [125I]iodocyanopindolol binding to Beta-2 adrenergic receptorBinding inhibition constant was determined by inhibition of [125I]iodocyanopindolol binding to Beta-2 adrenergic receptor
ChEMBL 485 10 4 6 4.3 COc1cccc2c(C[C@@H](C)NC[C@H](O)c3cccc(NS(=O)(=O)c4cccs4)c3)c[nH]c12 10.1016/j.bmcl.2004.10.035
24937014 17211 0 None 2 3 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 506 9 4 9 3.6 OCc1cc(O)ccc1OCC(O)CNC1CCN(c2ncnc3scc(-c4ccccc4)c23)CC1 10.1016/j.bmcl.2010.08.039
CHEMBL1257554 17211 0 None 2 3 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 506 9 4 9 3.6 OCc1cc(O)ccc1OCC(O)CNC1CCN(c2ncnc3scc(-c4ccccc4)c23)CC1 10.1016/j.bmcl.2010.08.039
52944986 17416 0 None -1 3 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 478 8 2 7 4.5 OC(CNC1CCN(c2ncnc3scc(-c4ccccc4)c23)CC1)COc1ccccc1F 10.1016/j.bmcl.2010.08.039
CHEMBL1258257 17416 0 None -1 3 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 478 8 2 7 4.5 OC(CNC1CCN(c2ncnc3scc(-c4ccccc4)c23)CC1)COc1ccccc1F 10.1016/j.bmcl.2010.08.039
49864334 15423 0 None 1 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptorDisplacement of [3H]CGP12177 from human beta2 adrenoceptor
ChEMBL 336 5 4 5 2.9 C[C@H](NC[C@H](O)c1ccc(O)c2[nH]c(=O)sc12)C1CCCCC1 10.1016/j.bmcl.2010.06.136
CHEMBL1221542 15423 0 None 1 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptorDisplacement of [3H]CGP12177 from human beta2 adrenoceptor
ChEMBL 336 5 4 5 2.9 C[C@H](NC[C@H](O)c1ccc(O)c2[nH]c(=O)sc12)C1CCCCC1 10.1016/j.bmcl.2010.06.136
166177238 191404 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of 125I-cyanopindolol from human beta2 adrenoceptor expressed in CHO-K1 cell membrane measured after 1 hr by Cheng-prusoff equation analysisDisplacement of 125I-cyanopindolol from human beta2 adrenoceptor expressed in CHO-K1 cell membrane measured after 1 hr by Cheng-prusoff equation analysis
ChEMBL 292 7 5 5 0.6 O=c1ccc2c([C@@H](O)CNCCCCO)ccc(O)c2[nH]1 10.1021/acs.jmedchem.2c00609
CHEMBL5201712 191404 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of 125I-cyanopindolol from human beta2 adrenoceptor expressed in CHO-K1 cell membrane measured after 1 hr by Cheng-prusoff equation analysisDisplacement of 125I-cyanopindolol from human beta2 adrenoceptor expressed in CHO-K1 cell membrane measured after 1 hr by Cheng-prusoff equation analysis
ChEMBL 292 7 5 5 0.6 O=c1ccc2c([C@@H](O)CNCCCCO)ccc(O)c2[nH]1 10.1021/acs.jmedchem.2c00609
56943515 111939 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assayDisplacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assay
ChEMBL 478 13 6 7 3.7 CC(C)(N)COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c(NC=O)c3)cc2)cc1 10.1016/j.bmcl.2014.04.095
CHEMBL3298213 111939 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assayDisplacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assay
ChEMBL 478 13 6 7 3.7 CC(C)(N)COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c(NC=O)c3)cc2)cc1 10.1016/j.bmcl.2014.04.095
10082625 13666 0 None -1 3 Guinea pig 6.6 pKi = 6.6 Binding
Binding affinity against Beta-2 adrenergic receptor was measured using [125I]CYP as radioligandBinding affinity against Beta-2 adrenergic receptor was measured using [125I]CYP as radioligand
ChEMBL 231 1 1 5 0.8 Cc1cn2c(C)cnc2c(N2CCNCC2)n1 10.1021/jm00099a012
CHEMBL1195526 13666 0 None -1 3 Guinea pig 6.6 pKi = 6.6 Binding
Binding affinity against Beta-2 adrenergic receptor was measured using [125I]CYP as radioligandBinding affinity against Beta-2 adrenergic receptor was measured using [125I]CYP as radioligand
ChEMBL 231 1 1 5 0.8 Cc1cn2c(C)cnc2c(N2CCNCC2)n1 10.1021/jm00099a012
CHEMBL554785 13666 0 None -1 3 Guinea pig 6.6 pKi = 6.6 Binding
Binding affinity against Beta-2 adrenergic receptor was measured using [125I]CYP as radioligandBinding affinity against Beta-2 adrenergic receptor was measured using [125I]CYP as radioligand
ChEMBL 231 1 1 5 0.8 Cc1cn2c(C)cnc2c(N2CCNCC2)n1 10.1021/jm00099a012
73056756 103790 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 345 9 4 5 3.1 CCC[C@H](Cc1ccc(OC)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2013.11.030
CHEMBL3099663 103790 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 345 9 4 5 3.1 CCC[C@H](Cc1ccc(OC)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2013.11.030
2405 658 71 None -58 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranesDisplacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranes
ChEMBL 325 12 2 5 2.4 OC(COc1ccc(cc1)COCCOC(C)C)CNC(C)C 10.1016/j.bmc.2019.05.034
380 658 71 None -58 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranesDisplacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranes
ChEMBL 325 12 2 5 2.4 OC(COc1ccc(cc1)COCCOC(C)C)CNC(C)C 10.1016/j.bmc.2019.05.034
7129 658 71 None -58 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranesDisplacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranes
ChEMBL 325 12 2 5 2.4 OC(COc1ccc(cc1)COCCOC(C)C)CNC(C)C 10.1016/j.bmc.2019.05.034
CHEMBL645 658 71 None -58 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranesDisplacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranes
ChEMBL 325 12 2 5 2.4 OC(COc1ccc(cc1)COCCOC(C)C)CNC(C)C 10.1016/j.bmc.2019.05.034
DB00612 658 71 None -58 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranesDisplacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranes
ChEMBL 325 12 2 5 2.4 OC(COc1ccc(cc1)COCCOC(C)C)CNC(C)C 10.1016/j.bmc.2019.05.034
73056756 103790 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 345 9 4 5 3.1 CCC[C@H](Cc1ccc(OC)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2013.11.030
CHEMBL3099663 103790 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 345 9 4 5 3.1 CCC[C@H](Cc1ccc(OC)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2013.11.030
145965875 163505 0 None - 1 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]-DHA from Nb69-fused beta2 adrenergic receptor (unknown origin) expressed in Sf9 cell membranes after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-DHA from Nb69-fused beta2 adrenergic receptor (unknown origin) expressed in Sf9 cell membranes after 2 hrs by microbeta scintillation counting method
ChEMBL 390 8 1 3 5.0 COc1ccc2c(c1)c(CCNCCCc1cccc(C(F)(F)F)c1)cn2C 10.1021/acs.jmedchem.7b01558
CHEMBL4209269 163505 0 None - 1 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]-DHA from Nb69-fused beta2 adrenergic receptor (unknown origin) expressed in Sf9 cell membranes after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-DHA from Nb69-fused beta2 adrenergic receptor (unknown origin) expressed in Sf9 cell membranes after 2 hrs by microbeta scintillation counting method
ChEMBL 390 8 1 3 5.0 COc1ccc2c(c1)c(CCNCCCc1cccc(C(F)(F)F)c1)cn2C 10.1021/acs.jmedchem.7b01558
59119466 111763 0 None 39 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assay
ChEMBL 436 10 5 7 3.3 COC(=O)c1ccc(Nc2ccc(CCNCC(O)c3ccc(O)c(CO)c3)cc2)cc1 10.1016/j.bmcl.2014.04.069
CHEMBL3290996 111763 0 None 39 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assay
ChEMBL 436 10 5 7 3.3 COC(=O)c1ccc(Nc2ccc(CCNCC(O)c3ccc(O)c(CO)c3)cc2)cc1 10.1016/j.bmcl.2014.04.069
16737369 142524 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 337 6 4 4 3.5 C[C@@H](Cc1cccc2ccccc12)NC[C@@H](O)c1cc(O)cc(O)c1 10.1021/jm070030d
CHEMBL389519 142524 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 337 6 4 4 3.5 C[C@@H](Cc1cccc2ccccc12)NC[C@@H](O)c1cc(O)cc(O)c1 10.1021/jm070030d
761003 76588 48 None - 1 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]dihydroalprenolol from human ADRB2 expressed in HEK293T cells after 1 hr by liquid scintillation counterDisplacement of [3H]dihydroalprenolol from human ADRB2 expressed in HEK293T cells after 1 hr by liquid scintillation counter
ChEMBL 205 2 2 3 1.6 Cc1nc2c(CN(C)C)c(O)ccc2[nH]1 10.1021/jm300280e
CHEMBL2070835 76588 48 None - 1 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]dihydroalprenolol from human ADRB2 expressed in HEK293T cells after 1 hr by liquid scintillation counterDisplacement of [3H]dihydroalprenolol from human ADRB2 expressed in HEK293T cells after 1 hr by liquid scintillation counter
ChEMBL 205 2 2 3 1.6 Cc1nc2c(CN(C)C)c(O)ccc2[nH]1 10.1021/jm300280e
16737369 142524 0 None - 1 Human 5.6 pKi = 5.6 Binding
Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.
ChEMBL 337 6 4 4 3.5 C[C@@H](Cc1cccc2ccccc12)NC[C@@H](O)c1cc(O)cc(O)c1 nan
CHEMBL389519 142524 0 None - 1 Human 5.6 pKi = 5.6 Binding
Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.
ChEMBL 337 6 4 4 3.5 C[C@@H](Cc1cccc2ccccc12)NC[C@@H](O)c1cc(O)cc(O)c1 nan
16737369 142524 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 337 6 4 4 3.5 C[C@@H](Cc1cccc2ccccc12)NC[C@@H](O)c1cc(O)cc(O)c1 10.1021/jm070030d
CHEMBL389519 142524 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 337 6 4 4 3.5 C[C@@H](Cc1cccc2ccccc12)NC[C@@H](O)c1cc(O)cc(O)c1 10.1021/jm070030d
24936883 17134 0 None 2 2 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 506 9 4 9 3.6 OCc1ccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)cc1O 10.1016/j.bmcl.2010.08.039
CHEMBL1257324 17134 0 None 2 2 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 506 9 4 9 3.6 OCc1ccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)cc1O 10.1016/j.bmcl.2010.08.039
44444193 153269 0 None 1 3 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]iodocyanopindolol from human cloned adrenergic beta-2 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human cloned adrenergic beta-2 receptor expressed in CHO cells
ChEMBL 548 13 4 7 4.3 COc1ccc([C@H](CCc2cccc(Cl)c2)NC[C@H](O)Cc2ccc(O)c(NS(C)(=O)=O)c2)cc1OC 10.1016/j.bmcl.2007.05.030
CHEMBL398241 153269 0 None 1 3 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]iodocyanopindolol from human cloned adrenergic beta-2 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human cloned adrenergic beta-2 receptor expressed in CHO cells
ChEMBL 548 13 4 7 4.3 COc1ccc([C@H](CCc2cccc(Cl)c2)NC[C@H](O)Cc2ccc(O)c(NS(C)(=O)=O)c2)cc1OC 10.1016/j.bmcl.2007.05.030
155521599 170157 0 None 10 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H](-)CGP 12177 from human recombinant beta2 adrenoceptor after 120 mins by scintillation counting methodDisplacement of [3H](-)CGP 12177 from human recombinant beta2 adrenoceptor after 120 mins by scintillation counting method
ChEMBL 1311 40 7 18 5.9 CC(C)NCC(O)COc1ccccc1CCCSCC(=O)NCCOCCOCCNC(=O)CCCCCC1(C)C(/C=C/C=C/C=C2/N(CCCS(=O)(=O)O)c3ccc(S(=O)(=O)O)cc3C2(C)C)=[N+](CCCS(=O)(=O)[O-])c2ccc(S(=O)(=O)O)cc21 10.1039/C8MD00412A
CHEMBL4452249 170157 0 None 10 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H](-)CGP 12177 from human recombinant beta2 adrenoceptor after 120 mins by scintillation counting methodDisplacement of [3H](-)CGP 12177 from human recombinant beta2 adrenoceptor after 120 mins by scintillation counting method
ChEMBL 1311 40 7 18 5.9 CC(C)NCC(O)COc1ccccc1CCCSCC(=O)NCCOCCOCCNC(=O)CCCCCC1(C)C(/C=C/C=C/C=C2/N(CCCS(=O)(=O)O)c3ccc(S(=O)(=O)O)cc3C2(C)C)=[N+](CCCS(=O)(=O)[O-])c2ccc(S(=O)(=O)O)cc21 10.1039/C8MD00412A
16736091 85291 0 None 66 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 317 7 4 5 2.4 COc1ccc(C[C@H](C)NC[C@H](O)c2cc(O)cc(O)c2)cc1 10.1016/j.bmc.2013.11.030
CHEMBL228996 85291 0 None 66 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 317 7 4 5 2.4 COc1ccc(C[C@H](C)NC[C@H](O)c2cc(O)cc(O)c2)cc1 10.1016/j.bmc.2013.11.030
155511898 169021 0 None 12 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assay
ChEMBL 360 8 2 3 4.5 COc1ccccc1OCCNCCc1cccc2[nH]c3ccccc3c12 10.1021/acs.jmedchem.9b00349
CHEMBL4436343 169021 0 None 12 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assay
ChEMBL 360 8 2 3 4.5 COc1ccccc1OCCNCCc1cccc2[nH]c3ccccc3c12 10.1021/acs.jmedchem.9b00349
1239 1639 46 None 63 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cellsDisplacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmc.2016.04.028
3410 1639 46 None 63 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cellsDisplacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmc.2016.04.028
3465 1639 46 None 63 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cellsDisplacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmc.2016.04.028
CHEMBL1256786 1639 46 None 63 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cellsDisplacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmc.2016.04.028
DB00983 1639 46 None 63 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cellsDisplacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmc.2016.04.028
16736091 85291 0 None 66 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 317 7 4 5 2.4 COc1ccc(C[C@H](C)NC[C@H](O)c2cc(O)cc(O)c2)cc1 10.1016/j.bmc.2013.11.030
CHEMBL228996 85291 0 None 66 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 317 7 4 5 2.4 COc1ccc(C[C@H](C)NC[C@H](O)c2cc(O)cc(O)c2)cc1 10.1016/j.bmc.2013.11.030
49864355 15429 0 None 1 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptorDisplacement of [3H]CGP12177 from human beta2 adrenoceptor
ChEMBL 374 5 4 5 3.1 O=c1[nH]c2c(O)ccc([C@@H](O)CNCC34CC5CC(CC(C5)C3)C4)c2s1 10.1016/j.bmcl.2010.06.136
CHEMBL1221586 15429 0 None 1 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptorDisplacement of [3H]CGP12177 from human beta2 adrenoceptor
ChEMBL 374 5 4 5 3.1 O=c1[nH]c2c(O)ccc([C@@H](O)CNCC34CC5CC(CC(C5)C3)C4)c2s1 10.1016/j.bmcl.2010.06.136
44286965 159850 0 None 4 3 Human 6.6 pKi = 6.6 Binding
Ability to bind to human Beta-2 adrenergic receptor using membranes of stably transfected CHO cellsAbility to bind to human Beta-2 adrenergic receptor using membranes of stably transfected CHO cells
ChEMBL 349 9 3 4 3.0 C[C@H](Cc1ccc(OCCO)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1016/S0960-894X(97)00266-7
CHEMBL41113 159850 0 None 4 3 Human 6.6 pKi = 6.6 Binding
Ability to bind to human Beta-2 adrenergic receptor using membranes of stably transfected CHO cellsAbility to bind to human Beta-2 adrenergic receptor using membranes of stably transfected CHO cells
ChEMBL 349 9 3 4 3.0 C[C@H](Cc1ccc(OCCO)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1016/S0960-894X(97)00266-7
10420352 168164 10 None 6 4 Dog 6.6 pKi = 6.6 Binding
Binding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranes
ChEMBL 201 3 4 4 0.5 CNCC(O)c1ccc(O)c(O)c1F 10.1021/jm990599h
CHEMBL43711 168164 10 None 6 4 Dog 6.6 pKi = 6.6 Binding
Binding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranes
ChEMBL 201 3 4 4 0.5 CNCC(O)c1ccc(O)c(O)c1F 10.1021/jm990599h
24936488 17452 0 None -1 3 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 414 7 3 8 2.7 Cc1csc2ncnc(N3CCC(NCC(O)COc4ccc(O)cc4)CC3)c12 10.1016/j.bmcl.2010.08.039
CHEMBL1258373 17452 0 None -1 3 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 414 7 3 8 2.7 Cc1csc2ncnc(N3CCC(NCC(O)COc4ccc(O)cc4)CC3)c12 10.1016/j.bmcl.2010.08.039
16717791 77247 0 None 1 2 Human 6.6 pKi = 6.6 Binding
Binding affinity to human beta2-adrenoceptor by radioligand binding assayBinding affinity to human beta2-adrenoceptor by radioligand binding assay
ChEMBL 376 6 3 3 3.7 CCc1cc2c(cc1CC)CC(NCCc1ccc(O)c3[nH]c(=O)ccc13)C2 10.1016/j.bmcl.2012.07.096
CHEMBL2088198 77247 0 None 1 2 Human 6.6 pKi = 6.6 Binding
Binding affinity to human beta2-adrenoceptor by radioligand binding assayBinding affinity to human beta2-adrenoceptor by radioligand binding assay
ChEMBL 376 6 3 3 3.7 CCc1cc2c(cc1CC)CC(NCCc1ccc(O)c3[nH]c(=O)ccc13)C2 10.1016/j.bmcl.2012.07.096
118710946 113244 0 None 1 2 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assay
ChEMBL 414 7 4 6 3.7 CCOc1cccc([C@H]2CCC[C@H]2NC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)c1 10.1016/j.bmcl.2014.06.014
CHEMBL3323664 113244 0 None 1 2 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assay
ChEMBL 414 7 4 6 3.7 CCOc1cccc([C@H]2CCC[C@H]2NC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)c1 10.1016/j.bmcl.2014.06.014
73056757 103784 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-CGP-12177 from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-CGP-12177 from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 303 7 4 5 2.0 COc1ccc(CCNC[C@H](O)c2cc(O)cc(O)c2)cc1 10.1016/j.bmc.2013.11.030
CHEMBL3099657 103784 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-CGP-12177 from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-CGP-12177 from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 303 7 4 5 2.0 COc1ccc(CCNC[C@H](O)c2cc(O)cc(O)c2)cc1 10.1016/j.bmc.2013.11.030
145972154 164126 0 None - 1 Human 3.6 pKi = 3.6 Binding
Displacement of [3H]-DHA from Nb69-fused beta2 adrenergic receptor (unknown origin) expressed in Sf9 cell membranes after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-DHA from Nb69-fused beta2 adrenergic receptor (unknown origin) expressed in Sf9 cell membranes after 2 hrs by microbeta scintillation counting method
ChEMBL 303 5 1 3 4.3 Cc1ccccc1C(C)NCc1ccc(-c2ncccn2)cc1 10.1021/acs.jmedchem.7b01558
CHEMBL4217119 164126 0 None - 1 Human 3.6 pKi = 3.6 Binding
Displacement of [3H]-DHA from Nb69-fused beta2 adrenergic receptor (unknown origin) expressed in Sf9 cell membranes after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-DHA from Nb69-fused beta2 adrenergic receptor (unknown origin) expressed in Sf9 cell membranes after 2 hrs by microbeta scintillation counting method
ChEMBL 303 5 1 3 4.3 Cc1ccccc1C(C)NCc1ccc(-c2ncccn2)cc1 10.1021/acs.jmedchem.7b01558
24937390 17418 0 None 1 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 490 8 3 8 4.4 Cc1c(-c2ccccc2)sc2ncnc(N3CCC(NCC(O)COc4ccc(O)cc4)CC3)c12 10.1016/j.bmcl.2010.08.039
CHEMBL1258259 17418 0 None 1 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 490 8 3 8 4.4 Cc1c(-c2ccccc2)sc2ncnc(N3CCC(NCC(O)COc4ccc(O)cc4)CC3)c12 10.1016/j.bmcl.2010.08.039
44444170 153358 0 None -2 2 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]iodocyanopindolol from human cloned adrenergic beta-2 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human cloned adrenergic beta-2 receptor expressed in CHO cells
ChEMBL 470 11 4 6 3.2 COc1cccc([C@@H](Cc2ccccc2)NC[C@H](O)Cc2ccc(O)c(NS(C)(=O)=O)c2)c1 10.1016/j.bmcl.2007.05.030
CHEMBL398320 153358 0 None -2 2 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]iodocyanopindolol from human cloned adrenergic beta-2 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human cloned adrenergic beta-2 receptor expressed in CHO cells
ChEMBL 470 11 4 6 3.2 COc1cccc([C@@H](Cc2ccccc2)NC[C@H](O)Cc2ccc(O)c(NS(C)(=O)=O)c2)c1 10.1016/j.bmcl.2007.05.030
1960 2805 64 None -338 26 Dog 4.6 pKi = 4.6 Binding
Binding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranes
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm990599h
439260 2805 64 None -338 26 Dog 4.6 pKi = 4.6 Binding
Binding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranes
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm990599h
505 2805 64 None -338 26 Dog 4.6 pKi = 4.6 Binding
Binding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranes
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm990599h
CHEMBL1437 2805 64 None -338 26 Dog 4.6 pKi = 4.6 Binding
Binding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranes
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm990599h
DB00368 2805 64 None -338 26 Dog 4.6 pKi = 4.6 Binding
Binding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranes
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm990599h
10773922 156940 0 None 1 2 Dog 4.6 pKi = 4.6 Binding
Binding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranes
ChEMBL 187 2 4 4 0.2 NC[C@@H](O)c1ccc(O)c(O)c1F 10.1021/jm990599h
CHEMBL40796 156940 0 None 1 2 Dog 4.6 pKi = 4.6 Binding
Binding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranes
ChEMBL 187 2 4 4 0.2 NC[C@@H](O)c1ccc(O)c(O)c1F 10.1021/jm990599h
688469 142383 2 None - 1 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 303 6 5 5 2.1 C[C@@H](Cc1ccc(O)cc1)NC[C@@H](O)c1cc(O)cc(O)c1 10.1021/jm070030d
CHEMBL389390 142383 2 None - 1 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 303 6 5 5 2.1 C[C@@H](Cc1ccc(O)cc1)NC[C@@H](O)c1cc(O)cc(O)c1 10.1021/jm070030d
688469 142383 2 None - 1 Human 4.6 pKi = 4.6 Binding
Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.
ChEMBL 303 6 5 5 2.1 C[C@@H](Cc1ccc(O)cc1)NC[C@@H](O)c1cc(O)cc(O)c1 nan
CHEMBL389390 142383 2 None - 1 Human 4.6 pKi = 4.6 Binding
Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.
ChEMBL 303 6 5 5 2.1 C[C@@H](Cc1ccc(O)cc1)NC[C@@H](O)c1cc(O)cc(O)c1 nan
688469 142383 2 None - 1 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 303 6 5 5 2.1 C[C@@H](Cc1ccc(O)cc1)NC[C@@H](O)c1cc(O)cc(O)c1 10.1021/jm070030d
CHEMBL389390 142383 2 None - 1 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 303 6 5 5 2.1 C[C@@H](Cc1ccc(O)cc1)NC[C@@H](O)c1cc(O)cc(O)c1 10.1021/jm070030d
12582 935 40 None -11 5 Human 7.6 pKi = 7.6 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 276 3 3 3 3.0 CC(C)(C)NCC(C1=CC(=C(C(=C1)Cl)N)Cl)O nan
2783 935 40 None -11 5 Human 7.6 pKi = 7.6 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 276 3 3 3 3.0 CC(C)(C)NCC(C1=CC(=C(C(=C1)Cl)N)Cl)O nan
CHEMBL49080 935 40 None -11 5 Human 7.6 pKi = 7.6 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 276 3 3 3 3.0 CC(C)(C)NCC(C1=CC(=C(C(=C1)Cl)N)Cl)O nan
DB01407 935 40 None -11 5 Human 7.6 pKi = 7.6 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 276 3 3 3 3.0 CC(C)(C)NCC(C1=CC(=C(C(=C1)Cl)N)Cl)O nan
24936492 17352 0 None 2 3 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 482 8 3 9 4.1 Oc1ccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5cccs5)c34)CC2)cc1 10.1016/j.bmcl.2010.08.039
CHEMBL1258026 17352 0 None 2 3 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 482 8 3 9 4.1 Oc1ccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5cccs5)c34)CC2)cc1 10.1016/j.bmcl.2010.08.039
10465942 13419 0 None -1 3 Guinea pig 6.6 pKi = 6.6 Binding
Binding affinity against Beta-2 adrenergic receptor was measured using [125I]CYP as radioligandBinding affinity against Beta-2 adrenergic receptor was measured using [125I]CYP as radioligand
ChEMBL 217 1 1 5 0.4 Cc1cn2ccnc2c(N2CCNCC2)n1 10.1021/jm00099a012
CHEMBL1193821 13419 0 None -1 3 Guinea pig 6.6 pKi = 6.6 Binding
Binding affinity against Beta-2 adrenergic receptor was measured using [125I]CYP as radioligandBinding affinity against Beta-2 adrenergic receptor was measured using [125I]CYP as radioligand
ChEMBL 217 1 1 5 0.4 Cc1cn2ccnc2c(N2CCNCC2)n1 10.1021/jm00099a012
CHEMBL545289 13419 0 None -1 3 Guinea pig 6.6 pKi = 6.6 Binding
Binding affinity against Beta-2 adrenergic receptor was measured using [125I]CYP as radioligandBinding affinity against Beta-2 adrenergic receptor was measured using [125I]CYP as radioligand
ChEMBL 217 1 1 5 0.4 Cc1cn2ccnc2c(N2CCNCC2)n1 10.1021/jm00099a012
44444187 94018 0 None -9 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]iodocyanopindolol from human cloned adrenergic beta-2 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human cloned adrenergic beta-2 receptor expressed in CHO cells
ChEMBL 484 12 4 6 3.6 COc1ccc([C@H](CCc2ccccc2)NC[C@H](O)Cc2ccc(O)c(NS(C)(=O)=O)c2)cc1 10.1016/j.bmcl.2007.05.030
CHEMBL251347 94018 0 None -9 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]iodocyanopindolol from human cloned adrenergic beta-2 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human cloned adrenergic beta-2 receptor expressed in CHO cells
ChEMBL 484 12 4 6 3.6 COc1ccc([C@H](CCc2ccccc2)NC[C@H](O)Cc2ccc(O)c(NS(C)(=O)=O)c2)cc1 10.1016/j.bmcl.2007.05.030
53380558 63302 2 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]CGP-12177 from human beta2-adrenergic receptor expressed in HEK 293 cellsDisplacement of [3H]CGP-12177 from human beta2-adrenergic receptor expressed in HEK 293 cells
ChEMBL 367 7 4 5 3.5 COc1ccc(C[C@@H](C)NC[C@H](O)c2cc(O)cc(O)c2)c2ccccc12 10.1016/j.bmc.2009.11.062
CHEMBL1800963 63302 2 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]CGP-12177 from human beta2-adrenergic receptor expressed in HEK 293 cellsDisplacement of [3H]CGP-12177 from human beta2-adrenergic receptor expressed in HEK 293 cells
ChEMBL 367 7 4 5 3.5 COc1ccc(C[C@@H](C)NC[C@H](O)c2cc(O)cc(O)c2)c2ccccc12 10.1016/j.bmc.2009.11.062
6603724 154780 3 None -1 3 Dog 4.6 pKi = 4.6 Binding
Binding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranes
ChEMBL 187 2 4 4 0.2 NC[C@H](O)c1cc(O)c(O)cc1F 10.1021/jm990599h
CHEMBL40317 154780 3 None -1 3 Dog 4.6 pKi = 4.6 Binding
Binding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranes
ChEMBL 187 2 4 4 0.2 NC[C@H](O)c1cc(O)c(O)cc1F 10.1021/jm990599h
145946829 166997 0 None -4 2 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]-CGP12177 from human beta2 ADR expressed in HEK293T cell membrane after 90 mins by scintillation countingDisplacement of [3H]-CGP12177 from human beta2 ADR expressed in HEK293T cell membrane after 90 mins by scintillation counting
ChEMBL 380 11 3 6 1.0 CNCC(O)COc1ccc(S(=O)(=O)NCCOc2ccccc2)cc1 10.1021/acs.jmedchem.8b00625
CHEMBL4170519 166997 0 None -4 2 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]-CGP12177 from human beta2 ADR expressed in HEK293T cell membrane after 90 mins by scintillation countingDisplacement of [3H]-CGP12177 from human beta2 ADR expressed in HEK293T cell membrane after 90 mins by scintillation counting
ChEMBL 380 11 3 6 1.0 CNCC(O)COc1ccc(S(=O)(=O)NCCOc2ccccc2)cc1 10.1021/acs.jmedchem.8b00625
CHEMBL4300598 166997 0 None -4 2 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]-CGP12177 from human beta2 ADR expressed in HEK293T cell membrane after 90 mins by scintillation countingDisplacement of [3H]-CGP12177 from human beta2 ADR expressed in HEK293T cell membrane after 90 mins by scintillation counting
ChEMBL 380 11 3 6 1.0 CNCC(O)COc1ccc(S(=O)(=O)NCCOc2ccccc2)cc1 10.1021/acs.jmedchem.8b00625
567 715 10 None -4 5 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]CYP from human adrenergic beta 2 receptor transfected in CHO cells in presence of 100 uM GTPDisplacement of [125I]CYP from human adrenergic beta 2 receptor transfected in CHO cells in presence of 100 uM GTP
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1016/j.bmc.2007.01.056
9841972 715 10 None -4 5 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]CYP from human adrenergic beta 2 receptor transfected in CHO cells in presence of 100 uM GTPDisplacement of [125I]CYP from human adrenergic beta 2 receptor transfected in CHO cells in presence of 100 uM GTP
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1016/j.bmc.2007.01.056
CHEMBL284782 715 10 None -4 5 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]CYP from human adrenergic beta 2 receptor transfected in CHO cells in presence of 100 uM GTPDisplacement of [125I]CYP from human adrenergic beta 2 receptor transfected in CHO cells in presence of 100 uM GTP
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1016/j.bmc.2007.01.056
14485414 202601 0 None - 1 Mouse 5.5 pKi = 5.5 Binding
Ki value was determined by accumulation of c-AMP in S-49 mouse lymphoma cells (Beta2).Ki value was determined by accumulation of c-AMP in S-49 mouse lymphoma cells (Beta2).
ChEMBL 495 13 4 5 4.6 CC(=O)Nc1ccc(OC[C@@H](O)CN[C@@H](C)CCCCC(=O)Nc2ccc(C(F)(F)F)cc2)cc1 10.1021/jm00163a036
CHEMBL71432 202601 0 None - 1 Mouse 5.5 pKi = 5.5 Binding
Ki value was determined by accumulation of c-AMP in S-49 mouse lymphoma cells (Beta2).Ki value was determined by accumulation of c-AMP in S-49 mouse lymphoma cells (Beta2).
ChEMBL 495 13 4 5 4.6 CC(=O)Nc1ccc(OC[C@@H](O)CN[C@@H](C)CCCCC(=O)Nc2ccc(C(F)(F)F)cc2)cc1 10.1021/jm00163a036
16736092 85342 0 None 1 2 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 287 6 4 4 2.4 C[C@@H](Cc1ccccc1)NC[C@@H](O)c1cc(O)cc(O)c1 10.1021/jm070030d
CHEMBL229390 85342 0 None 1 2 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 287 6 4 4 2.4 C[C@@H](Cc1ccccc1)NC[C@@H](O)c1cc(O)cc(O)c1 10.1021/jm070030d
16736092 85342 0 None 1 2 Human 4.5 pKi = 4.5 Binding
Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.
ChEMBL 287 6 4 4 2.4 C[C@@H](Cc1ccccc1)NC[C@@H](O)c1cc(O)cc(O)c1 nan
CHEMBL229390 85342 0 None 1 2 Human 4.5 pKi = 4.5 Binding
Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.
ChEMBL 287 6 4 4 2.4 C[C@@H](Cc1ccccc1)NC[C@@H](O)c1cc(O)cc(O)c1 nan
16735259 85207 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 317 7 4 5 2.4 COc1ccc(C[C@H](C)NC[C@@H](O)c2cc(O)cc(O)c2)cc1 10.1016/j.bmc.2013.11.030
CHEMBL228417 85207 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 317 7 4 5 2.4 COc1ccc(C[C@H](C)NC[C@@H](O)c2cc(O)cc(O)c2)cc1 10.1016/j.bmc.2013.11.030
16735259 85207 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 317 7 4 5 2.4 COc1ccc(C[C@H](C)NC[C@@H](O)c2cc(O)cc(O)c2)cc1 10.1016/j.bmc.2013.11.030
CHEMBL228417 85207 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 317 7 4 5 2.4 COc1ccc(C[C@H](C)NC[C@@H](O)c2cc(O)cc(O)c2)cc1 10.1016/j.bmc.2013.11.030
123133227 143604 0 None - 1 Human 4.5 pKi = 4.5 Binding
Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.
ChEMBL 302 6 5 5 1.9 C[C@@H](Cc1cccc(N)c1)NC[C@@H](O)c1cc(O)cc(O)c1 nan
CHEMBL3903905 143604 0 None - 1 Human 4.5 pKi = 4.5 Binding
Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.
ChEMBL 302 6 5 5 1.9 C[C@@H](Cc1cccc(N)c1)NC[C@@H](O)c1cc(O)cc(O)c1 nan
16735492 85344 0 None - 1 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 302 6 5 5 1.9 C[C@@H](Cc1ccc(N)cc1)NC[C@@H](O)c1cc(O)cc(O)c1 10.1021/jm070030d
CHEMBL229400 85344 0 None - 1 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 302 6 5 5 1.9 C[C@@H](Cc1ccc(N)cc1)NC[C@@H](O)c1cc(O)cc(O)c1 10.1021/jm070030d
13864389 4982 2 None -8 2 Bovine 4.5 pKi = 4.5 Binding
Tested for binding affinity against beta-2 adrenergic receptor in bovine lung using [3H]DHA as radioligandTested for binding affinity against beta-2 adrenergic receptor in bovine lung using [3H]DHA as radioligand
ChEMBL 195 1 3 4 0.7 NCC1OCCc2cc(O)c(O)cc21 10.1021/jm00073a006
CHEMBL105383 4982 2 None -8 2 Bovine 4.5 pKi = 4.5 Binding
Tested for binding affinity against beta-2 adrenergic receptor in bovine lung using [3H]DHA as radioligandTested for binding affinity against beta-2 adrenergic receptor in bovine lung using [3H]DHA as radioligand
ChEMBL 195 1 3 4 0.7 NCC1OCCc2cc(O)c(O)cc21 10.1021/jm00073a006
16736092 85342 0 None 1 2 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 287 6 4 4 2.4 C[C@@H](Cc1ccccc1)NC[C@@H](O)c1cc(O)cc(O)c1 10.1021/jm070030d
CHEMBL229390 85342 0 None 1 2 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 287 6 4 4 2.4 C[C@@H](Cc1ccccc1)NC[C@@H](O)c1cc(O)cc(O)c1 10.1021/jm070030d
16735492 85344 0 None - 1 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 302 6 5 5 1.9 C[C@@H](Cc1ccc(N)cc1)NC[C@@H](O)c1cc(O)cc(O)c1 10.1021/jm070030d
CHEMBL229400 85344 0 None - 1 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 302 6 5 5 1.9 C[C@@H](Cc1ccc(N)cc1)NC[C@@H](O)c1cc(O)cc(O)c1 10.1021/jm070030d
1588 2284 24 None -50 44 Human 7.5 pKi = 7.5 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
28864 2284 24 None -50 44 Human 7.5 pKi = 7.5 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
43 2284 24 None -50 44 Human 7.5 pKi = 7.5 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
CHEMBL157138 2284 24 None -50 44 Human 7.5 pKi = 7.5 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
DB00589 2284 24 None -50 44 Human 7.5 pKi = 7.5 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
1862 161 14 None -28 7 Rat 4.5 pKi = 4.5 Binding
Binding affinity against adrenergic beta 2 receptor versus 1 nM [3H]dihydroalprenolol in rat cerebral cerebellar membranesBinding affinity against adrenergic beta 2 receptor versus 1 nM [3H]dihydroalprenolol in rat cerebral cerebellar membranes
ChEMBL 187 2 4 4 0.2 NCC(c1cc(O)c(cc1F)O)O 10.1021/jm00076a024
510 161 14 None -28 7 Rat 4.5 pKi = 4.5 Binding
Binding affinity against adrenergic beta 2 receptor versus 1 nM [3H]dihydroalprenolol in rat cerebral cerebellar membranesBinding affinity against adrenergic beta 2 receptor versus 1 nM [3H]dihydroalprenolol in rat cerebral cerebellar membranes
ChEMBL 187 2 4 4 0.2 NCC(c1cc(O)c(cc1F)O)O 10.1021/jm00076a024
CHEMBL281232 161 14 None -28 7 Rat 4.5 pKi = 4.5 Binding
Binding affinity against adrenergic beta 2 receptor versus 1 nM [3H]dihydroalprenolol in rat cerebral cerebellar membranesBinding affinity against adrenergic beta 2 receptor versus 1 nM [3H]dihydroalprenolol in rat cerebral cerebellar membranes
ChEMBL 187 2 4 4 0.2 NCC(c1cc(O)c(cc1F)O)O 10.1021/jm00076a024
73056755 103788 0 None - 1 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 345 8 4 5 3.0 COc1ccc(C[C@H](NC[C@H](O)c2cc(O)cc(O)c2)C(C)C)cc1 10.1016/j.bmc.2013.11.030
CHEMBL3099661 103788 0 None - 1 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 345 8 4 5 3.0 COc1ccc(C[C@H](NC[C@H](O)c2cc(O)cc(O)c2)C(C)C)cc1 10.1016/j.bmc.2013.11.030
73056755 103788 0 None - 1 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 345 8 4 5 3.0 COc1ccc(C[C@H](NC[C@H](O)c2cc(O)cc(O)c2)C(C)C)cc1 10.1016/j.bmc.2013.11.030
CHEMBL3099661 103788 0 None - 1 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 345 8 4 5 3.0 COc1ccc(C[C@H](NC[C@H](O)c2cc(O)cc(O)c2)C(C)C)cc1 10.1016/j.bmc.2013.11.030
56663519 63299 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 317 7 5 5 2.4 CC[C@@H](Cc1ccc(O)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2013.11.030
CHEMBL1800960 63299 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 317 7 5 5 2.4 CC[C@@H](Cc1ccc(O)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2013.11.030
16737411 142657 0 None 8 2 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 287 6 4 4 2.4 C[C@H](Cc1ccccc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1021/jm070030d
CHEMBL389629 142657 0 None 8 2 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 287 6 4 4 2.4 C[C@H](Cc1ccccc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1021/jm070030d
16737411 142657 0 None 8 2 Human 5.5 pKi = 5.5 Binding
Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.
ChEMBL 287 6 4 4 2.4 C[C@H](Cc1ccccc1)NC[C@H](O)c1cc(O)cc(O)c1 nan
CHEMBL389629 142657 0 None 8 2 Human 5.5 pKi = 5.5 Binding
Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.
ChEMBL 287 6 4 4 2.4 C[C@H](Cc1ccccc1)NC[C@H](O)c1cc(O)cc(O)c1 nan
56663519 63299 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 317 7 5 5 2.4 CC[C@@H](Cc1ccc(O)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2013.11.030
CHEMBL1800960 63299 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 317 7 5 5 2.4 CC[C@@H](Cc1ccc(O)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2013.11.030
16737411 142657 0 None 8 2 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 287 6 4 4 2.4 C[C@H](Cc1ccccc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1021/jm070030d
CHEMBL389629 142657 0 None 8 2 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 287 6 4 4 2.4 C[C@H](Cc1ccccc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1021/jm070030d
2464 3570 52 None -7 6 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C nan
5253 3570 52 None -7 6 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C nan
7297 3570 52 None -7 6 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C nan
CHEMBL471 3570 52 None -7 6 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C nan
DB00489 3570 52 None -7 6 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C nan
46889670 6919 0 None 2 3 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cells
ChEMBL 533 7 2 5 5.2 O=C1c2cccc3cccc(c23)C(=O)N1CC1CCN(CC(O)COc2cccc3[nH]c4ccccc4c23)CC1 10.1016/j.bmcl.2010.04.009
CHEMBL1084772 6919 0 None 2 3 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cells
ChEMBL 533 7 2 5 5.2 O=C1c2cccc3cccc(c23)C(=O)N1CC1CCN(CC(O)COc2cccc3[nH]c4ccccc4c23)CC1 10.1016/j.bmcl.2010.04.009
49864460 15460 0 None -1 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptorDisplacement of [3H]CGP12177 from human beta2 adrenoceptor
ChEMBL 396 7 4 6 3.4 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCSc3ccc(Cl)cc3)c2s1 10.1016/j.bmcl.2010.06.136
CHEMBL1221861 15460 0 None -1 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptorDisplacement of [3H]CGP12177 from human beta2 adrenoceptor
ChEMBL 396 7 4 6 3.4 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCSc3ccc(Cl)cc3)c2s1 10.1016/j.bmcl.2010.06.136
9892481 69875 11 None 3162 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assay
ChEMBL 435 12 6 6 3.0 O=CNc1cc([C@@H](O)CNCCc2ccc(NC[C@H](O)c3ccccc3)cc2)ccc1O 10.1016/j.bmcl.2014.04.069
CHEMBL1940832 69875 11 None 3162 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assay
ChEMBL 435 12 6 6 3.0 O=CNc1cc([C@@H](O)CNCCc2ccc(NC[C@H](O)c3ccccc3)cc2)ccc1O 10.1016/j.bmcl.2014.04.069
9892481 69875 11 None 3162 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assayDisplacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assay
ChEMBL 435 12 6 6 3.0 O=CNc1cc([C@@H](O)CNCCc2ccc(NC[C@H](O)c3ccccc3)cc2)ccc1O 10.1016/j.bmcl.2014.04.095
CHEMBL1940832 69875 11 None 3162 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assayDisplacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assay
ChEMBL 435 12 6 6 3.0 O=CNc1cc([C@@H](O)CNCCc2ccc(NC[C@H](O)c3ccccc3)cc2)ccc1O 10.1016/j.bmcl.2014.04.095
90645344 111951 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assayDisplacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assay
ChEMBL 550 11 6 7 5.0 COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1-c1ccccc1CN 10.1016/j.bmcl.2014.04.095
CHEMBL3298324 111951 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assayDisplacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assay
ChEMBL 550 11 6 7 5.0 COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1-c1ccccc1CN 10.1016/j.bmcl.2014.04.095
63952 8487 37 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]cyanopindolol from human recombinant beta2 adrenergic receptor expressed in CHO cells by filtration assayDisplacement of [125I]cyanopindolol from human recombinant beta2 adrenergic receptor expressed in CHO cells by filtration assay
ChEMBL 368 7 4 5 2.5 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1 10.1021/jm100068m
86306667 8487 37 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]cyanopindolol from human recombinant beta2 adrenergic receptor expressed in CHO cells by filtration assayDisplacement of [125I]cyanopindolol from human recombinant beta2 adrenergic receptor expressed in CHO cells by filtration assay
ChEMBL 368 7 4 5 2.5 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1 10.1021/jm100068m
CHEMBL1094785 8487 37 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]cyanopindolol from human recombinant beta2 adrenergic receptor expressed in CHO cells by filtration assayDisplacement of [125I]cyanopindolol from human recombinant beta2 adrenergic receptor expressed in CHO cells by filtration assay
ChEMBL 368 7 4 5 2.5 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1 10.1021/jm100068m
14823035 141019 2 None 52 3 Human 8.5 pKi = 8.5 Binding
Ability to bind to human Beta-2 adrenergic receptor using membranes of stably transfected CHO cellsAbility to bind to human Beta-2 adrenergic receptor using membranes of stably transfected CHO cells
ChEMBL 377 9 2 5 3.1 COC(=O)COc1ccc(C[C@@H](C)NC[C@H](O)c2cccc(Cl)c2)cc1 10.1016/S0960-894X(97)00266-7
CHEMBL38486 141019 2 None 52 3 Human 8.5 pKi = 8.5 Binding
Ability to bind to human Beta-2 adrenergic receptor using membranes of stably transfected CHO cellsAbility to bind to human Beta-2 adrenergic receptor using membranes of stably transfected CHO cells
ChEMBL 377 9 2 5 3.1 COC(=O)COc1ccc(C[C@@H](C)NC[C@H](O)c2cccc(Cl)c2)cc1 10.1016/S0960-894X(97)00266-7
2419 3394 80 None 16 6 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2014.06.014
5152 3394 80 None 16 6 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2014.06.014
559 3394 80 None 16 6 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2014.06.014
CHEMBL1263 3394 80 None 16 6 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2014.06.014
DB00938 3394 80 None 16 6 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2014.06.014
68807656 113246 0 None 1 3 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assay
ChEMBL 372 8 4 5 3.1 CCCc1cccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)c1 10.1016/j.bmcl.2014.06.014
CHEMBL3323666 113246 0 None 1 3 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assay
ChEMBL 372 8 4 5 3.1 CCCc1cccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)c1 10.1016/j.bmcl.2014.06.014
155552089 173437 0 None 10 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H](-)CGP 12177 from human recombinant beta2 adrenoceptor after 120 mins by scintillation counting methodDisplacement of [3H](-)CGP 12177 from human recombinant beta2 adrenoceptor after 120 mins by scintillation counting method
ChEMBL 571 21 4 9 2.8 CC(C)NCC(O)COc1ccccc1CCCSCC(=O)NCCOCCOCCNC(=O)OC(C)(C)C 10.1039/C8MD00412A
CHEMBL4542960 173437 0 None 10 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H](-)CGP 12177 from human recombinant beta2 adrenoceptor after 120 mins by scintillation counting methodDisplacement of [3H](-)CGP 12177 from human recombinant beta2 adrenoceptor after 120 mins by scintillation counting method
ChEMBL 571 21 4 9 2.8 CC(C)NCC(O)COc1ccccc1CCCSCC(=O)NCCOCCOCCNC(=O)OC(C)(C)C 10.1039/C8MD00412A
2419 3394 80 None 16 6 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptorDisplacement of [3H]CGP12177 from human beta2 adrenoceptor
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2010.06.136
5152 3394 80 None 16 6 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptorDisplacement of [3H]CGP12177 from human beta2 adrenoceptor
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2010.06.136
559 3394 80 None 16 6 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptorDisplacement of [3H]CGP12177 from human beta2 adrenoceptor
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2010.06.136
CHEMBL1263 3394 80 None 16 6 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptorDisplacement of [3H]CGP12177 from human beta2 adrenoceptor
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2010.06.136
DB00938 3394 80 None 16 6 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptorDisplacement of [3H]CGP12177 from human beta2 adrenoceptor
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2010.06.136
10456417 65766 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity for human beta-2 adrenergic receptorBinding affinity for human beta-2 adrenergic receptor
ChEMBL 450 14 4 6 3.7 O=CNc1cc([C@@H](O)CNCCc2cccc(OCCCOc3ccccc3)c2)ccc1O 10.1016/j.bmcl.2004.06.086
CHEMBL183948 65766 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity for human beta-2 adrenergic receptorBinding affinity for human beta-2 adrenergic receptor
ChEMBL 450 14 4 6 3.7 O=CNc1cc([C@@H](O)CNCCc2cccc(OCCCOc3ccccc3)c2)ccc1O 10.1016/j.bmcl.2004.06.086
146025801 170054 0 None 1 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assay
ChEMBL 376 8 3 4 4.0 COc1ccccc1OCCNC[C@H](O)c1cccc2[nH]c3ccccc3c12 10.1021/acs.jmedchem.9b00349
CHEMBL4451135 170054 0 None 1 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assay
ChEMBL 376 8 3 4 4.0 COc1ccccc1OCCNC[C@H](O)c1cccc2[nH]c3ccccc3c12 10.1021/acs.jmedchem.9b00349
9986442 58214 0 None -10 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-dihydroalprenolol from human beta2-adrenoceptor expressed in HEK cells after 4 hrsDisplacement of [3H]-dihydroalprenolol from human beta2-adrenoceptor expressed in HEK cells after 4 hrs
ChEMBL 626 15 5 7 6.6 O=C(Nc1ccccc1-c1ccccc1)OC1CCN(CCCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1016/j.bmcl.2011.01.043
CHEMBL1683933 58214 0 None -10 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-dihydroalprenolol from human beta2-adrenoceptor expressed in HEK cells after 4 hrsDisplacement of [3H]-dihydroalprenolol from human beta2-adrenoceptor expressed in HEK cells after 4 hrs
ChEMBL 626 15 5 7 6.6 O=C(Nc1ccccc1-c1ccccc1)OC1CCN(CCCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1016/j.bmcl.2011.01.043
155529446 170876 0 None 8 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranesDisplacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranes
ChEMBL 502 16 3 8 4.1 COc1cc(CCNC[C@@H](O)COc2cccc3ccccc23)ccc1OCCSSCCN 10.1016/j.bmc.2019.05.034
CHEMBL4463246 170876 0 None 8 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranesDisplacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranes
ChEMBL 502 16 3 8 4.1 COc1cc(CCNC[C@@H](O)COc2cccc3ccccc23)ccc1OCCSSCCN 10.1016/j.bmc.2019.05.034
155563970 174778 0 None 5 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysisDisplacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysis
ChEMBL 530 18 6 7 2.2 CC(C)NC[C@H](O)COc1ccccc1CCNC(=O)NCCc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
CHEMBL4574652 174778 0 None 5 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysisDisplacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysis
ChEMBL 530 18 6 7 2.2 CC(C)NC[C@H](O)COc1ccccc1CCNC(=O)NCCc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
9874175 58215 1 None -34 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-dihydroalprenolol from human beta2-adrenoceptor expressed in HEK cells after 4 hrsDisplacement of [3H]-dihydroalprenolol from human beta2-adrenoceptor expressed in HEK cells after 4 hrs
ChEMBL 640 16 5 7 7.0 O=C(Nc1ccccc1-c1ccccc1)OC1CCN(CCCCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1016/j.bmcl.2011.01.043
CHEMBL1683934 58215 1 None -34 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-dihydroalprenolol from human beta2-adrenoceptor expressed in HEK cells after 4 hrsDisplacement of [3H]-dihydroalprenolol from human beta2-adrenoceptor expressed in HEK cells after 4 hrs
ChEMBL 640 16 5 7 7.0 O=C(Nc1ccccc1-c1ccccc1)OC1CCN(CCCCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1016/j.bmcl.2011.01.043
165193 3126 60 None 1 43 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmc.2013.11.030
2303 3126 60 None 1 43 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmc.2013.11.030
4946 3126 60 None 1 43 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmc.2013.11.030
564 3126 60 None 1 43 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmc.2013.11.030
62882 3126 60 None 1 43 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmc.2013.11.030
63 3126 60 None 1 43 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmc.2013.11.030
66366 3126 60 None 1 43 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmc.2013.11.030
91536 3126 60 None 1 43 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmc.2013.11.030
CHEMBL27 3126 60 None 1 43 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmc.2013.11.030
CHEMBL452861 3126 60 None 1 43 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmc.2013.11.030
DB00571 3126 60 None 1 43 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmc.2013.11.030
155531982 171114 0 None 6 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H](-)CGP 12177 from human recombinant beta2 adrenoceptor after 120 mins by scintillation counting methodDisplacement of [3H](-)CGP 12177 from human recombinant beta2 adrenoceptor after 120 mins by scintillation counting method
ChEMBL 526 22 3 9 2.3 C=CCc1ccccc1OCC(O)CNCCOCCOCCOCCOCCNC(=O)OC(C)(C)C 10.1039/C8MD00412A
CHEMBL4466532 171114 0 None 6 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H](-)CGP 12177 from human recombinant beta2 adrenoceptor after 120 mins by scintillation counting methodDisplacement of [3H](-)CGP 12177 from human recombinant beta2 adrenoceptor after 120 mins by scintillation counting method
ChEMBL 526 22 3 9 2.3 C=CCc1ccccc1OCC(O)CNCCOCCOCCOCCOCCNC(=O)OC(C)(C)C 10.1039/C8MD00412A
9860739 147717 1 None -1 3 Human 8.4 pKi = 8.4 Binding
Binding affinity at human adrenergic beta2 receptorBinding affinity at human adrenergic beta2 receptor
ChEMBL 288 6 3 3 2.8 O[C@@H](CNC1CCCCC1)COc1cccc2[nH]ccc12 10.1016/j.bmcl.2007.07.086
CHEMBL393648 147717 1 None -1 3 Human 8.4 pKi = 8.4 Binding
Binding affinity at human adrenergic beta2 receptorBinding affinity at human adrenergic beta2 receptor
ChEMBL 288 6 3 3 2.8 O[C@@H](CNC1CCCCC1)COc1cccc2[nH]ccc12 10.1016/j.bmcl.2007.07.086
49864415 15454 0 None 117 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptorDisplacement of [3H]CGP12177 from human beta2 adrenoceptor
ChEMBL 362 4 4 5 3.1 CC1(C)[C@@H]2CC[C@@]1(C)[C@@H](NC[C@H](O)c1ccc(O)c3[nH]c(=O)sc13)C2 10.1016/j.bmcl.2010.06.136
CHEMBL1221735 15454 0 None 117 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptorDisplacement of [3H]CGP12177 from human beta2 adrenoceptor
ChEMBL 362 4 4 5 3.1 CC1(C)[C@@H]2CC[C@@]1(C)[C@@H](NC[C@H](O)c1ccc(O)c3[nH]c(=O)sc13)C2 10.1016/j.bmcl.2010.06.136
118710949 113249 0 None 3 3 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assay
ChEMBL 402 10 4 6 3.3 CCCCOc1ccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)cc1 10.1016/j.bmcl.2014.06.014
CHEMBL3323669 113249 0 None 3 3 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assay
ChEMBL 402 10 4 6 3.3 CCCCOc1ccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)cc1 10.1016/j.bmcl.2014.06.014
688468 141788 7 None 190 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 303 6 5 5 2.1 C[C@H](Cc1ccc(O)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2013.11.030
CHEMBL388570 141788 7 None 190 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 303 6 5 5 2.1 C[C@H](Cc1ccc(O)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2013.11.030
52949489 17350 0 None 1 3 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 490 9 2 8 4.4 COc1cccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)c1 10.1016/j.bmcl.2010.08.039
CHEMBL1258024 17350 0 None 1 3 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 490 9 2 8 4.4 COc1cccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)c1 10.1016/j.bmcl.2010.08.039
52947443 17417 0 None -1 3 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 478 8 2 7 4.5 OC(CNC1CCN(c2ncnc3scc(-c4ccccc4)c23)CC1)COc1cccc(F)c1 10.1016/j.bmcl.2010.08.039
CHEMBL1258258 17417 0 None -1 3 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 478 8 2 7 4.5 OC(CNC1CCN(c2ncnc3scc(-c4ccccc4)c23)CC1)COc1cccc(F)c1 10.1016/j.bmcl.2010.08.039
9924779 93991 0 None 8 2 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]iodocyanopindolol from human adrenergic beta-2 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human adrenergic beta-2 receptor expressed in CHO cells
ChEMBL 355 9 3 7 1.9 OCc1nc(-c2ccc(OCCNC[C@H](O)c3cccnc3)cc2)co1 10.1016/j.bmcl.2007.06.072
CHEMBL251180 93991 0 None 8 2 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]iodocyanopindolol from human adrenergic beta-2 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human adrenergic beta-2 receptor expressed in CHO cells
ChEMBL 355 9 3 7 1.9 OCc1nc(-c2ccc(OCCNC[C@H](O)c3cccnc3)cc2)co1 10.1016/j.bmcl.2007.06.072
49864378 15440 0 None 1 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptorDisplacement of [3H]CGP12177 from human beta2 adrenoceptor
ChEMBL 356 4 4 5 3.0 O=c1[nH]c2c(O)ccc([C@@H](O)CN[C@H]3CCCc4ccccc43)c2s1 10.1016/j.bmcl.2010.06.136
CHEMBL1221635 15440 0 None 1 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptorDisplacement of [3H]CGP12177 from human beta2 adrenoceptor
ChEMBL 356 4 4 5 3.0 O=c1[nH]c2c(O)ccc([C@@H](O)CN[C@H]3CCCc4ccccc43)c2s1 10.1016/j.bmcl.2010.06.136
4276762 6861 11 None 1 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cells
ChEMBL 530 8 1 6 4.9 COc1ccc(OCC(O)CN2CCC(CN3C(=O)c4cccc5cccc(c45)C3=O)CC2)c(C(C)(C)C)c1 10.1016/j.bmcl.2010.04.009
CHEMBL1084526 6861 11 None 1 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cells
ChEMBL 530 8 1 6 4.9 COc1ccc(OCC(O)CN2CCC(CN3C(=O)c4cccc5cccc(c45)C3=O)CC2)c(C(C)(C)C)c1 10.1016/j.bmcl.2010.04.009
145946991 167039 0 None -1 2 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]-CGP12177 from human beta2 ADR expressed in HEK293T cell membrane after 90 mins by scintillation countingDisplacement of [3H]-CGP12177 from human beta2 ADR expressed in HEK293T cell membrane after 90 mins by scintillation counting
ChEMBL 330 9 3 5 1.0 CNCC(O)COc1ccc(S(=O)(=O)NC(C)C(C)C)cc1 10.1021/acs.jmedchem.8b00625
CHEMBL4163665 167039 0 None -1 2 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]-CGP12177 from human beta2 ADR expressed in HEK293T cell membrane after 90 mins by scintillation countingDisplacement of [3H]-CGP12177 from human beta2 ADR expressed in HEK293T cell membrane after 90 mins by scintillation counting
ChEMBL 330 9 3 5 1.0 CNCC(O)COc1ccc(S(=O)(=O)NC(C)C(C)C)cc1 10.1021/acs.jmedchem.8b00625
CHEMBL4301131 167039 0 None -1 2 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]-CGP12177 from human beta2 ADR expressed in HEK293T cell membrane after 90 mins by scintillation countingDisplacement of [3H]-CGP12177 from human beta2 ADR expressed in HEK293T cell membrane after 90 mins by scintillation counting
ChEMBL 330 9 3 5 1.0 CNCC(O)COc1ccc(S(=O)(=O)NC(C)C(C)C)cc1 10.1021/acs.jmedchem.8b00625
123133226 160347 0 None - 1 Human 4.5 pKi = 4.5 Binding
Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.
ChEMBL 302 6 5 5 1.9 C[C@H](Cc1cccc(N)c1)NC[C@@H](O)c1cc(O)cc(O)c1 nan
CHEMBL4115254 160347 0 None - 1 Human 4.5 pKi = 4.5 Binding
Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.
ChEMBL 302 6 5 5 1.9 C[C@H](Cc1cccc(N)c1)NC[C@@H](O)c1cc(O)cc(O)c1 nan
16735493 85352 0 None - 1 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 302 6 5 5 1.9 C[C@H](Cc1ccc(N)cc1)NC[C@@H](O)c1cc(O)cc(O)c1 10.1021/jm070030d
CHEMBL229443 85352 0 None - 1 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 302 6 5 5 1.9 C[C@H](Cc1ccc(N)cc1)NC[C@@H](O)c1cc(O)cc(O)c1 10.1021/jm070030d
16735493 85352 0 None - 1 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 302 6 5 5 1.9 C[C@H](Cc1ccc(N)cc1)NC[C@@H](O)c1cc(O)cc(O)c1 10.1021/jm070030d
CHEMBL229443 85352 0 None - 1 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 302 6 5 5 1.9 C[C@H](Cc1ccc(N)cc1)NC[C@@H](O)c1cc(O)cc(O)c1 10.1021/jm070030d
1239 1639 46 None 63 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.04.069
3410 1639 46 None 63 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.04.069
3465 1639 46 None 63 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.04.069
CHEMBL1256786 1639 46 None 63 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.04.069
DB00983 1639 46 None 63 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.04.069
1239 1639 46 None 63 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assayDisplacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.04.095
3410 1639 46 None 63 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assayDisplacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.04.095
3465 1639 46 None 63 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assayDisplacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.04.095
CHEMBL1256786 1639 46 None 63 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assayDisplacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.04.095
DB00983 1639 46 None 63 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assayDisplacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.04.095
56943517 111999 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assayDisplacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assay
ChEMBL 621 13 5 9 2.8 CS(=O)(=O)N1CCN(CCOc2ccc(Nc3ccc(CCNC[C@H](O)c4ccc(O)c5[nH]c(=O)ccc45)cc3)cc2)CC1 10.1016/j.bmcl.2014.04.095
CHEMBL3298832 111999 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assayDisplacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assay
ChEMBL 621 13 5 9 2.8 CS(=O)(=O)N1CCN(CCOc2ccc(Nc3ccc(CCNC[C@H](O)c4ccc(O)c5[nH]c(=O)ccc45)cc3)cc2)CC1 10.1016/j.bmcl.2014.04.095
10227108 94055 0 None -6 2 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]iodocyanopindolol from human cloned adrenergic beta-2 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human cloned adrenergic beta-2 receptor expressed in CHO cells
ChEMBL 470 11 4 6 3.2 COc1ccc([C@@H](Cc2ccccc2)NC[C@H](O)Cc2ccc(O)c(NS(C)(=O)=O)c2)cc1 10.1016/j.bmcl.2007.05.030
CHEMBL251580 94055 0 None -6 2 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]iodocyanopindolol from human cloned adrenergic beta-2 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human cloned adrenergic beta-2 receptor expressed in CHO cells
ChEMBL 470 11 4 6 3.2 COc1ccc([C@@H](Cc2ccccc2)NC[C@H](O)Cc2ccc(O)c(NS(C)(=O)=O)c2)cc1 10.1016/j.bmcl.2007.05.030
25023952 192678 0 None - 1 Golden hamster 6.5 pKi = 6.5 Binding
Displacement of [125I](-)-iodopindolol from adrenergic beta2 receptor in Syrian hamster DDT1 MF2 cellsDisplacement of [125I](-)-iodopindolol from adrenergic beta2 receptor in Syrian hamster DDT1 MF2 cells
ChEMBL 545 15 8 13 0.0 O=CNc1cc(C(O)CNCCCCCCNc2ncnc3c2ncn3[C@@H]2O[C@H](CO)[C@@H](O)[C@H]2O)ccc1O 10.1021/jm800613s
CHEMBL524037 192678 0 None - 1 Golden hamster 6.5 pKi = 6.5 Binding
Displacement of [125I](-)-iodopindolol from adrenergic beta2 receptor in Syrian hamster DDT1 MF2 cellsDisplacement of [125I](-)-iodopindolol from adrenergic beta2 receptor in Syrian hamster DDT1 MF2 cells
ChEMBL 545 15 8 13 0.0 O=CNc1cc(C(O)CNCCCCCCNc2ncnc3c2ncn3[C@@H]2O[C@H](CO)[C@@H](O)[C@H]2O)ccc1O 10.1021/jm800613s
44424579 85372 0 None - 1 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 253 7 4 4 2.3 CCCC[C@H](C)NC[C@H](O)c1cc(O)cc(O)c1 10.1021/jm070030d
CHEMBL229615 85372 0 None - 1 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 253 7 4 4 2.3 CCCC[C@H](C)NC[C@H](O)c1cc(O)cc(O)c1 10.1021/jm070030d
16735774 147015 0 None - 1 Human 4.5 pKi = 4.5 Binding
Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.
ChEMBL 267 8 4 4 2.7 CCCCC[C@H](C)NC[C@H](O)c1cc(O)cc(O)c1 nan
CHEMBL3930835 147015 0 None - 1 Human 4.5 pKi = 4.5 Binding
Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.
ChEMBL 267 8 4 4 2.7 CCCCC[C@H](C)NC[C@H](O)c1cc(O)cc(O)c1 nan
90644153 111748 0 None 19 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assay
ChEMBL 470 11 5 6 5.3 OCc1cc(C(O)CNCCc2ccc(Nc3ccc(Oc4ccccc4)cc3)cc2)ccc1O 10.1016/j.bmcl.2014.04.069
CHEMBL3290982 111748 0 None 19 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assay
ChEMBL 470 11 5 6 5.3 OCc1cc(C(O)CNCCc2ccc(Nc3ccc(Oc4ccccc4)cc3)cc2)ccc1O 10.1016/j.bmcl.2014.04.069
59119467 111749 0 None 39 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assay
ChEMBL 428 9 5 5 4.6 OCc1cc(C(O)CNCCc2ccc(Nc3ccc4ccccc4c3)cc2)ccc1O 10.1016/j.bmcl.2014.04.069
CHEMBL3290983 111749 0 None 39 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assay
ChEMBL 428 9 5 5 4.6 OCc1cc(C(O)CNCCc2ccc(Nc3ccc4ccccc4c3)cc2)ccc1O 10.1016/j.bmcl.2014.04.069
59119417 111753 0 None 39 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assay
ChEMBL 454 10 5 5 5.2 OCc1cc(C(O)CNCCc2ccc(Nc3ccc(-c4ccccc4)cc3)cc2)ccc1O 10.1016/j.bmcl.2014.04.069
CHEMBL3290987 111753 0 None 39 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assay
ChEMBL 454 10 5 5 5.2 OCc1cc(C(O)CNCCc2ccc(Nc3ccc(-c4ccccc4)cc3)cc2)ccc1O 10.1016/j.bmcl.2014.04.069
10310564 111754 0 None 39 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assay
ChEMBL 454 10 5 5 5.2 OCc1cc(C(O)CNCCc2ccc(Nc3cccc(-c4ccccc4)c3)cc2)ccc1O 10.1016/j.bmcl.2014.04.069
CHEMBL3290988 111754 0 None 39 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assay
ChEMBL 454 10 5 5 5.2 OCc1cc(C(O)CNCCc2ccc(Nc3cccc(-c4ccccc4)c3)cc2)ccc1O 10.1016/j.bmcl.2014.04.069
145946294 166933 0 None -3 2 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]-CGP12177 from human beta2 ADR expressed in HEK293T cell membrane after 90 mins by scintillation countingDisplacement of [3H]-CGP12177 from human beta2 ADR expressed in HEK293T cell membrane after 90 mins by scintillation counting
ChEMBL 302 8 3 5 0.3 CNCC(O)COc1ccc(S(=O)(=O)NC(C)C)cc1 10.1021/acs.jmedchem.8b00625
CHEMBL4174345 166933 0 None -3 2 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]-CGP12177 from human beta2 ADR expressed in HEK293T cell membrane after 90 mins by scintillation countingDisplacement of [3H]-CGP12177 from human beta2 ADR expressed in HEK293T cell membrane after 90 mins by scintillation counting
ChEMBL 302 8 3 5 0.3 CNCC(O)COc1ccc(S(=O)(=O)NC(C)C)cc1 10.1021/acs.jmedchem.8b00625
CHEMBL4299816 166933 0 None -3 2 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]-CGP12177 from human beta2 ADR expressed in HEK293T cell membrane after 90 mins by scintillation countingDisplacement of [3H]-CGP12177 from human beta2 ADR expressed in HEK293T cell membrane after 90 mins by scintillation counting
ChEMBL 302 8 3 5 0.3 CNCC(O)COc1ccc(S(=O)(=O)NC(C)C)cc1 10.1021/acs.jmedchem.8b00625
44424579 85372 0 None - 1 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 253 7 4 4 2.3 CCCC[C@H](C)NC[C@H](O)c1cc(O)cc(O)c1 10.1021/jm070030d
CHEMBL229615 85372 0 None - 1 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 253 7 4 4 2.3 CCCC[C@H](C)NC[C@H](O)c1cc(O)cc(O)c1 10.1021/jm070030d
90644142 111736 0 None - 1 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assay
ChEMBL 365 7 4 4 2.5 OCc1cc(C(O)CNCCc2ccc(Br)cc2)ccc1O 10.1016/j.bmcl.2014.04.069
CHEMBL3290971 111736 0 None - 1 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assay
ChEMBL 365 7 4 4 2.5 OCc1cc(C(O)CNCCc2ccc(Br)cc2)ccc1O 10.1016/j.bmcl.2014.04.069
90644149 111743 0 None - 1 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assay
ChEMBL 447 9 4 6 3.1 OCc1cc(C(O)CNCCc2ccc(N3CCN(c4ccccc4)CC3)cc2)ccc1O 10.1016/j.bmcl.2014.04.069
CHEMBL3290978 111743 0 None - 1 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assay
ChEMBL 447 9 4 6 3.1 OCc1cc(C(O)CNCCc2ccc(N3CCN(c4ccccc4)CC3)cc2)ccc1O 10.1016/j.bmcl.2014.04.069
12353629 202216 0 None 1 3 Human 7.5 pKi = 7.5 Binding
Binding affinity to beta2 adrenoceptor (unknown origin)Binding affinity to beta2 adrenoceptor (unknown origin)
ChEMBL 237 2 4 4 1.4 CC(C)N[C@@H]1CCc2c(ccc(O)c2O)[C@H]1O 10.1021/acs.jmedchem.0c01195
CHEMBL6913 202216 0 None 1 3 Human 7.5 pKi = 7.5 Binding
Binding affinity to beta2 adrenoceptor (unknown origin)Binding affinity to beta2 adrenoceptor (unknown origin)
ChEMBL 237 2 4 4 1.4 CC(C)N[C@@H]1CCc2c(ccc(O)c2O)[C@H]1O 10.1021/acs.jmedchem.0c01195
118710951 113251 0 None -1 2 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assay
ChEMBL 358 6 4 5 2.8 Cc1ccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)cc1C 10.1016/j.bmcl.2014.06.014
CHEMBL3323671 113251 0 None -1 2 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assay
ChEMBL 358 6 4 5 2.8 Cc1ccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)cc1C 10.1016/j.bmcl.2014.06.014
56677231 63293 0 None 234 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]CGP-12177 from human beta2-adrenergic receptor expressed in HEK 293 cellsDisplacement of [3H]CGP-12177 from human beta2-adrenergic receptor expressed in HEK 293 cells
ChEMBL 367 7 4 5 3.5 COc1ccc(C[C@H](C)NC[C@H](O)c2cc(O)cc(O)c2)c2ccccc12 10.1016/j.bmc.2009.11.062
CHEMBL1800934 63293 0 None 234 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]CGP-12177 from human beta2-adrenergic receptor expressed in HEK 293 cellsDisplacement of [3H]CGP-12177 from human beta2-adrenergic receptor expressed in HEK 293 cells
ChEMBL 367 7 4 5 3.5 COc1ccc(C[C@H](C)NC[C@H](O)c2cc(O)cc(O)c2)c2ccccc12 10.1016/j.bmc.2009.11.062
3086576 176371 29 None 40 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]CGP1217 from human recombinant adrenergic beta2 receptor transfected in insect Sf9 cells by scintillation countingDisplacement of [3H]CGP1217 from human recombinant adrenergic beta2 receptor transfected in insect Sf9 cells by scintillation counting
ChEMBL 261 2 3 4 1.1 CC(C)N[C@@H]1CCn2c(=O)[nH]c3cccc(c32)[C@H]1O 10.1021/jm801211c
CHEMBL462313 176371 29 None 40 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]CGP1217 from human recombinant adrenergic beta2 receptor transfected in insect Sf9 cells by scintillation countingDisplacement of [3H]CGP1217 from human recombinant adrenergic beta2 receptor transfected in insect Sf9 cells by scintillation counting
ChEMBL 261 2 3 4 1.1 CC(C)N[C@@H]1CCn2c(=O)[nH]c3cccc(c32)[C@H]1O 10.1021/jm801211c
CHEMBL513390 176371 29 None 40 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]CGP1217 from human recombinant adrenergic beta2 receptor transfected in insect Sf9 cells by scintillation countingDisplacement of [3H]CGP1217 from human recombinant adrenergic beta2 receptor transfected in insect Sf9 cells by scintillation counting
ChEMBL 261 2 3 4 1.1 CC(C)N[C@@H]1CCn2c(=O)[nH]c3cccc(c32)[C@H]1O 10.1021/jm801211c
155536406 171581 0 None -1 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranesDisplacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranes
ChEMBL 524 20 3 9 3.6 COCCc1ccc(OC[C@H](O)CNCCc2ccc(OCCCSSCCN)c(OC)c2)cc1 10.1016/j.bmc.2019.05.034
CHEMBL4473272 171581 0 None -1 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranesDisplacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranes
ChEMBL 524 20 3 9 3.6 COCCc1ccc(OC[C@H](O)CNCCc2ccc(OCCCSSCCN)c(OC)c2)cc1 10.1016/j.bmc.2019.05.034
10059780 12835 0 None -6 3 Guinea pig 5.5 pKi = 5.5 Binding
Binding affinity against Beta-2 adrenergic receptor was measured using [125I]CYP as radioligandBinding affinity against Beta-2 adrenergic receptor was measured using [125I]CYP as radioligand
ChEMBL 231 2 1 5 0.7 CCc1cnc2c(N3CCNCC3)nccn12 10.1021/jm00099a012
CHEMBL1189347 12835 0 None -6 3 Guinea pig 5.5 pKi = 5.5 Binding
Binding affinity against Beta-2 adrenergic receptor was measured using [125I]CYP as radioligandBinding affinity against Beta-2 adrenergic receptor was measured using [125I]CYP as radioligand
ChEMBL 231 2 1 5 0.7 CCc1cnc2c(N3CCNCC3)nccn12 10.1021/jm00099a012
CHEMBL538537 12835 0 None -6 3 Guinea pig 5.5 pKi = 5.5 Binding
Binding affinity against Beta-2 adrenergic receptor was measured using [125I]CYP as radioligandBinding affinity against Beta-2 adrenergic receptor was measured using [125I]CYP as radioligand
ChEMBL 231 2 1 5 0.7 CCc1cnc2c(N3CCNCC3)nccn12 10.1021/jm00099a012
4143663 6799 12 None -2 3 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cells
ChEMBL 514 10 1 6 4.3 C=CCc1ccc(OCC(O)CN2CCC(CN3C(=O)c4cccc5cccc(c45)C3=O)CC2)c(OC)c1 10.1016/j.bmcl.2010.04.009
CHEMBL1084274 6799 12 None -2 3 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cells
ChEMBL 514 10 1 6 4.3 C=CCc1ccc(OCC(O)CN2CCC(CN3C(=O)c4cccc5cccc(c45)C3=O)CC2)c(OC)c1 10.1016/j.bmcl.2010.04.009
1239 1639 46 None 63 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-dihydroalprenolol from human beta2-adrenoceptor expressed in HEK cells after 4 hrsDisplacement of [3H]-dihydroalprenolol from human beta2-adrenoceptor expressed in HEK cells after 4 hrs
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2011.01.043
3410 1639 46 None 63 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-dihydroalprenolol from human beta2-adrenoceptor expressed in HEK cells after 4 hrsDisplacement of [3H]-dihydroalprenolol from human beta2-adrenoceptor expressed in HEK cells after 4 hrs
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2011.01.043
3465 1639 46 None 63 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-dihydroalprenolol from human beta2-adrenoceptor expressed in HEK cells after 4 hrsDisplacement of [3H]-dihydroalprenolol from human beta2-adrenoceptor expressed in HEK cells after 4 hrs
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2011.01.043
CHEMBL1256786 1639 46 None 63 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-dihydroalprenolol from human beta2-adrenoceptor expressed in HEK cells after 4 hrsDisplacement of [3H]-dihydroalprenolol from human beta2-adrenoceptor expressed in HEK cells after 4 hrs
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2011.01.043
DB00983 1639 46 None 63 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-dihydroalprenolol from human beta2-adrenoceptor expressed in HEK cells after 4 hrsDisplacement of [3H]-dihydroalprenolol from human beta2-adrenoceptor expressed in HEK cells after 4 hrs
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2011.01.043
3464 3111 29 None 1659 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cellsDisplacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells
ChEMBL 290 5 4 4 2.0 CCC(C(c1ccc(c2c1ccc(=O)[nH]2)O)O)NC(C)C 10.1016/j.bmc.2016.04.028
4916 3111 29 None 1659 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cellsDisplacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells
ChEMBL 290 5 4 4 2.0 CCC(C(c1ccc(c2c1ccc(=O)[nH]2)O)O)NC(C)C 10.1016/j.bmc.2016.04.028
CHEMBL160519 3111 29 None 1659 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cellsDisplacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells
ChEMBL 290 5 4 4 2.0 CCC(C(c1ccc(c2c1ccc(=O)[nH]2)O)O)NC(C)C 10.1016/j.bmc.2016.04.028
DB01366 3111 29 None 1659 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cellsDisplacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells
ChEMBL 290 5 4 4 2.0 CCC(C(c1ccc(c2c1ccc(=O)[nH]2)O)O)NC(C)C 10.1016/j.bmc.2016.04.028
1960 2805 64 None -549 26 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cellsDisplacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1016/j.bmc.2016.04.028
439260 2805 64 None -549 26 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cellsDisplacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1016/j.bmc.2016.04.028
505 2805 64 None -549 26 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cellsDisplacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1016/j.bmc.2016.04.028
CHEMBL1437 2805 64 None -549 26 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cellsDisplacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1016/j.bmc.2016.04.028
DB00368 2805 64 None -549 26 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cellsDisplacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1016/j.bmc.2016.04.028
18525747 162983 34 None - 1 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]-DHA from Nb80-fused beta2 adrenergic receptor (unknown origin) expressed in Sf9 cell membranes after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-DHA from Nb80-fused beta2 adrenergic receptor (unknown origin) expressed in Sf9 cell membranes after 2 hrs by microbeta scintillation counting method
ChEMBL 204 3 1 3 2.5 CNCc1ccc(-c2nccs2)cc1 10.1021/acs.jmedchem.7b01558
CHEMBL4202934 162983 34 None - 1 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]-DHA from Nb80-fused beta2 adrenergic receptor (unknown origin) expressed in Sf9 cell membranes after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-DHA from Nb80-fused beta2 adrenergic receptor (unknown origin) expressed in Sf9 cell membranes after 2 hrs by microbeta scintillation counting method
ChEMBL 204 3 1 3 2.5 CNCc1ccc(-c2nccs2)cc1 10.1021/acs.jmedchem.7b01558
688469 142383 2 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 303 6 5 5 2.1 C[C@@H](Cc1ccc(O)cc1)NC[C@@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2013.11.030
CHEMBL389390 142383 2 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 303 6 5 5 2.1 C[C@@H](Cc1ccc(O)cc1)NC[C@@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2013.11.030
16735272 85371 0 None 46 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 337 6 4 4 3.5 C[C@@H](Cc1cccc2ccccc12)NC[C@H](O)c1cc(O)cc(O)c1 10.1021/jm070030d
CHEMBL229614 85371 0 None 46 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 337 6 4 4 3.5 C[C@@H](Cc1cccc2ccccc12)NC[C@H](O)c1cc(O)cc(O)c1 10.1021/jm070030d
97803 163952 87 None - 1 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]-DHA from Nb80-fused beta2 adrenergic receptor (unknown origin) expressed in Sf9 cell membranes after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-DHA from Nb80-fused beta2 adrenergic receptor (unknown origin) expressed in Sf9 cell membranes after 2 hrs by microbeta scintillation counting method
ChEMBL 155 1 1 1 2.4 CC(N)c1ccc(Cl)cc1 10.1021/acs.jmedchem.7b01558
CHEMBL4214761 163952 87 None - 1 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]-DHA from Nb80-fused beta2 adrenergic receptor (unknown origin) expressed in Sf9 cell membranes after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-DHA from Nb80-fused beta2 adrenergic receptor (unknown origin) expressed in Sf9 cell membranes after 2 hrs by microbeta scintillation counting method
ChEMBL 155 1 1 1 2.4 CC(N)c1ccc(Cl)cc1 10.1021/acs.jmedchem.7b01558
16735272 85371 0 None 46 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 337 6 4 4 3.5 C[C@@H](Cc1cccc2ccccc12)NC[C@H](O)c1cc(O)cc(O)c1 10.1021/jm070030d
CHEMBL229614 85371 0 None 46 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 337 6 4 4 3.5 C[C@@H](Cc1cccc2ccccc12)NC[C@H](O)c1cc(O)cc(O)c1 10.1021/jm070030d
10008017 99397 5 None - 1 Human 5.5 pKi = 5.5 Binding
Inhibition of I-iodocyanopindolol binding to human beta 2 adrenergic receptorsInhibition of I-iodocyanopindolol binding to human beta 2 adrenergic receptors
ChEMBL 562 12 6 8 2.3 CC(C)C[C@H](NC(=O)c1ccc(N2CCC(NC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)CC2)cc1)C(=O)O 10.1021/jm000544b
CHEMBL285881 99397 5 None - 1 Human 5.5 pKi = 5.5 Binding
Inhibition of I-iodocyanopindolol binding to human beta 2 adrenergic receptorsInhibition of I-iodocyanopindolol binding to human beta 2 adrenergic receptors
ChEMBL 562 12 6 8 2.3 CC(C)C[C@H](NC(=O)c1ccc(N2CCC(NC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)CC2)cc1)C(=O)O 10.1021/jm000544b
16735272 85371 0 None 46 2 Human 6.5 pKi = 6.5 Binding
Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.
ChEMBL 337 6 4 4 3.5 C[C@@H](Cc1cccc2ccccc12)NC[C@H](O)c1cc(O)cc(O)c1 nan
CHEMBL229614 85371 0 None 46 2 Human 6.5 pKi = 6.5 Binding
Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.
ChEMBL 337 6 4 4 3.5 C[C@@H](Cc1cccc2ccccc12)NC[C@H](O)c1cc(O)cc(O)c1 nan
73056759 103789 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 345 8 4 5 3.0 COc1ccc(C[C@@H](NC[C@H](O)c2cc(O)cc(O)c2)C(C)C)cc1 10.1016/j.bmc.2013.11.030
CHEMBL3099662 103789 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 345 8 4 5 3.0 COc1ccc(C[C@@H](NC[C@H](O)c2cc(O)cc(O)c2)C(C)C)cc1 10.1016/j.bmc.2013.11.030
46221603 8456 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]cyanopindolol from human recombinant beta2 adrenergic receptor expressed in CHO cells by filtration assayDisplacement of [125I]cyanopindolol from human recombinant beta2 adrenergic receptor expressed in CHO cells by filtration assay
ChEMBL 396 6 4 6 2.0 COc1cc2c(cc1OC)CC(NC[C@H](O)c1ccc(O)c3[nH]c(=O)ccc13)C2 10.1021/jm100068m
CHEMBL1094486 8456 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]cyanopindolol from human recombinant beta2 adrenergic receptor expressed in CHO cells by filtration assayDisplacement of [125I]cyanopindolol from human recombinant beta2 adrenergic receptor expressed in CHO cells by filtration assay
ChEMBL 396 6 4 6 2.0 COc1cc2c(cc1OC)CC(NC[C@H](O)c1ccc(O)c3[nH]c(=O)ccc13)C2 10.1021/jm100068m
73056759 103789 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 345 8 4 5 3.0 COc1ccc(C[C@@H](NC[C@H](O)c2cc(O)cc(O)c2)C(C)C)cc1 10.1016/j.bmc.2013.11.030
CHEMBL3099662 103789 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 345 8 4 5 3.0 COc1ccc(C[C@@H](NC[C@H](O)c2cc(O)cc(O)c2)C(C)C)cc1 10.1016/j.bmc.2013.11.030
688468 141788 7 None 190 2 Human 6.5 pKi = 6.5 Binding
Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.
ChEMBL 303 6 5 5 2.1 C[C@H](Cc1ccc(O)cc1)NC[C@H](O)c1cc(O)cc(O)c1 nan
CHEMBL388570 141788 7 None 190 2 Human 6.5 pKi = 6.5 Binding
Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.
ChEMBL 303 6 5 5 2.1 C[C@H](Cc1ccc(O)cc1)NC[C@H](O)c1cc(O)cc(O)c1 nan
688468 141788 7 None 190 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 303 6 5 5 2.1 C[C@H](Cc1ccc(O)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1021/jm070030d
CHEMBL388570 141788 7 None 190 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 303 6 5 5 2.1 C[C@H](Cc1ccc(O)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1021/jm070030d
44393827 66249 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity for human beta-2 adrenergic receptorBinding affinity for human beta-2 adrenergic receptor
ChEMBL 392 10 4 5 3.6 O=CNc1cc([C@@H](O)CNCCc2ccc(Oc3ccccc3)cc2)ccc1O 10.1016/j.bmcl.2004.06.086
CHEMBL185262 66249 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity for human beta-2 adrenergic receptorBinding affinity for human beta-2 adrenergic receptor
ChEMBL 392 10 4 5 3.6 O=CNc1cc([C@@H](O)CNCCc2ccc(Oc3ccccc3)cc2)ccc1O 10.1016/j.bmcl.2004.06.086
73056754 103786 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 331 8 4 5 2.8 CC[C@H](Cc1ccc(OC)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2013.11.030
CHEMBL3099659 103786 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 331 8 4 5 2.8 CC[C@H](Cc1ccc(OC)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2013.11.030
73056754 103786 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 331 8 4 5 2.8 CC[C@H](Cc1ccc(OC)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2013.11.030
CHEMBL3099659 103786 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 331 8 4 5 2.8 CC[C@H](Cc1ccc(OC)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2013.11.030
10162297 153361 0 None -3 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]iodocyanopindolol from human cloned adrenergic beta-2 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human cloned adrenergic beta-2 receptor expressed in CHO cells
ChEMBL 470 11 4 6 3.2 COc1cccc([C@@H](Cc2ccccc2)NC[C@@H](O)Cc2ccc(O)c(NS(C)(=O)=O)c2)c1 10.1016/j.bmcl.2007.05.030
CHEMBL398322 153361 0 None -3 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]iodocyanopindolol from human cloned adrenergic beta-2 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human cloned adrenergic beta-2 receptor expressed in CHO cells
ChEMBL 470 11 4 6 3.2 COc1cccc([C@@H](Cc2ccccc2)NC[C@@H](O)Cc2ccc(O)c(NS(C)(=O)=O)c2)c1 10.1016/j.bmcl.2007.05.030
688468 141788 7 None 190 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 303 6 5 5 2.1 C[C@H](Cc1ccc(O)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1021/jm070030d
CHEMBL388570 141788 7 None 190 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 303 6 5 5 2.1 C[C@H](Cc1ccc(O)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1021/jm070030d
10464801 11094 0 None -3 2 Bovine 5.5 pKi = 5.5 Binding
Binding affinity against beta-2-adrenergic receptor in bovine lungBinding affinity against beta-2-adrenergic receptor in bovine lung
ChEMBL 174 6 2 4 0.4 CCO/N=C/C(O)CNC(C)C 10.1021/jm00036a018
CHEMBL1178754 11094 0 None -3 2 Bovine 5.5 pKi = 5.5 Binding
Binding affinity against beta-2-adrenergic receptor in bovine lungBinding affinity against beta-2-adrenergic receptor in bovine lung
ChEMBL 174 6 2 4 0.4 CCO/N=C/C(O)CNC(C)C 10.1021/jm00036a018
CHEMBL39682 11094 0 None -3 2 Bovine 5.5 pKi = 5.5 Binding
Binding affinity against beta-2-adrenergic receptor in bovine lungBinding affinity against beta-2-adrenergic receptor in bovine lung
ChEMBL 174 6 2 4 0.4 CCO/N=C/C(O)CNC(C)C 10.1021/jm00036a018
14925759 157482 6 None -12302 13 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]CGP12177 from human recombinant beta2 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by beta counting methodDisplacement of [3H]CGP12177 from human recombinant beta2 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by beta counting method
ChEMBL 349 5 0 3 3.2 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4085780 157482 6 None -12302 13 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]CGP12177 from human recombinant beta2 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by beta counting methodDisplacement of [3H]CGP12177 from human recombinant beta2 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by beta counting method
ChEMBL 349 5 0 3 3.2 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
2291 3123 52 None -3 12 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O nan
2561 3123 52 None -3 12 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O nan
4932 3123 52 None -3 12 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O nan
CHEMBL631 3123 52 None -3 12 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O nan
DB01182 3123 52 None -3 12 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O nan
53326837 58222 0 None -7 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-dihydroalprenolol from human beta2-adrenoceptor expressed in HEK cells after 4 hrsDisplacement of [3H]-dihydroalprenolol from human beta2-adrenoceptor expressed in HEK cells after 4 hrs
ChEMBL 722 17 5 10 5.3 C[N+]1(CCCCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)[C@@H]2C[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)C[C@@H]1[C@H]1O[C@H]12 10.1016/j.bmcl.2011.01.043
CHEMBL1683942 58222 0 None -7 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-dihydroalprenolol from human beta2-adrenoceptor expressed in HEK cells after 4 hrsDisplacement of [3H]-dihydroalprenolol from human beta2-adrenoceptor expressed in HEK cells after 4 hrs
ChEMBL 722 17 5 10 5.3 C[N+]1(CCCCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)[C@@H]2C[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)C[C@@H]1[C@H]1O[C@H]12 10.1016/j.bmcl.2011.01.043
1028 287 69 None -89 30 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cellsDisplacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1016/j.bmc.2016.04.028
139148732 287 69 None -89 30 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cellsDisplacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1016/j.bmc.2016.04.028
479 287 69 None -89 30 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cellsDisplacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1016/j.bmc.2016.04.028
5816 287 69 None -89 30 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cellsDisplacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1016/j.bmc.2016.04.028
CHEMBL679 287 69 None -89 30 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cellsDisplacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1016/j.bmc.2016.04.028
DB00668 287 69 None -89 30 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cellsDisplacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1016/j.bmc.2016.04.028
10602703 119799 0 None - 1 Human 5.4 pKi = 5.4 Binding
Inhibition of I-iodocyanopindolol binding to human beta 2 adrenergic receptorsInhibition of I-iodocyanopindolol binding to human beta 2 adrenergic receptors
ChEMBL 548 11 6 8 1.9 CC(C)[C@H](NC(=O)c1ccc(N2CCC(NC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)CC2)cc1)C(=O)O 10.1021/jm000544b
CHEMBL35282 119799 0 None - 1 Human 5.4 pKi = 5.4 Binding
Inhibition of I-iodocyanopindolol binding to human beta 2 adrenergic receptorsInhibition of I-iodocyanopindolol binding to human beta 2 adrenergic receptors
ChEMBL 548 11 6 8 1.9 CC(C)[C@H](NC(=O)c1ccc(N2CCC(NC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)CC2)cc1)C(=O)O 10.1021/jm000544b
360400 96804 2 None 1 2 Bovine 4.4 pKi = 4.4 Binding
Compound was evaluated for beta adrenergic binding affinity towards beta-2 receptor of bovine lungCompound was evaluated for beta adrenergic binding affinity towards beta-2 receptor of bovine lung
ChEMBL 237 2 2 4 1.9 CC(C)N1CCOC(c2ccc(O)c(O)c2)C1 10.1021/jm00084a006
CHEMBL268881 96804 2 None 1 2 Bovine 4.4 pKi = 4.4 Binding
Compound was evaluated for beta adrenergic binding affinity towards beta-2 receptor of bovine lungCompound was evaluated for beta adrenergic binding affinity towards beta-2 receptor of bovine lung
ChEMBL 237 2 2 4 1.9 CC(C)N1CCOC(c2ccc(O)c(O)c2)C1 10.1021/jm00084a006
49864413 15452 0 None 2 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptorDisplacement of [3H]CGP12177 from human beta2 adrenoceptor
ChEMBL 414 7 4 6 3.4 O=c1[nH]c2c(O)ccc([C@@H](O)CN[C@H]3CCCC[C@@H]3OCc3ccccc3)c2s1 10.1016/j.bmcl.2010.06.136
CHEMBL1221733 15452 0 None 2 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptorDisplacement of [3H]CGP12177 from human beta2 adrenoceptor
ChEMBL 414 7 4 6 3.4 O=c1[nH]c2c(O)ccc([C@@H](O)CN[C@H]3CCCC[C@@H]3OCc3ccccc3)c2s1 10.1016/j.bmcl.2010.06.136
12475776 163548 7 None - 1 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]-DHA from Nb69-fused beta2 adrenergic receptor (unknown origin) expressed in Sf9 cell membranes after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-DHA from Nb69-fused beta2 adrenergic receptor (unknown origin) expressed in Sf9 cell membranes after 2 hrs by microbeta scintillation counting method
ChEMBL 204 3 1 3 1.7 COc1ccc2c(c1)c(CCN)cn2C 10.1021/acs.jmedchem.7b01558
CHEMBL4209786 163548 7 None - 1 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]-DHA from Nb69-fused beta2 adrenergic receptor (unknown origin) expressed in Sf9 cell membranes after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-DHA from Nb69-fused beta2 adrenergic receptor (unknown origin) expressed in Sf9 cell membranes after 2 hrs by microbeta scintillation counting method
ChEMBL 204 3 1 3 1.7 COc1ccc2c(c1)c(CCN)cn2C 10.1021/acs.jmedchem.7b01558
18525747 162983 34 None - 1 Human 3.4 pKi = 3.4 Binding
Displacement of [3H]-DHA from Nb69-fused beta2 adrenergic receptor (unknown origin) expressed in Sf9 cell membranes after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-DHA from Nb69-fused beta2 adrenergic receptor (unknown origin) expressed in Sf9 cell membranes after 2 hrs by microbeta scintillation counting method
ChEMBL 204 3 1 3 2.5 CNCc1ccc(-c2nccs2)cc1 10.1021/acs.jmedchem.7b01558
CHEMBL4202934 162983 34 None - 1 Human 3.4 pKi = 3.4 Binding
Displacement of [3H]-DHA from Nb69-fused beta2 adrenergic receptor (unknown origin) expressed in Sf9 cell membranes after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-DHA from Nb69-fused beta2 adrenergic receptor (unknown origin) expressed in Sf9 cell membranes after 2 hrs by microbeta scintillation counting method
ChEMBL 204 3 1 3 2.5 CNCc1ccc(-c2nccs2)cc1 10.1021/acs.jmedchem.7b01558
688467 85357 2 None 14 2 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 303 6 5 5 2.1 C[C@@H](Cc1ccc(O)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1021/jm070030d
CHEMBL229476 85357 2 None 14 2 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 303 6 5 5 2.1 C[C@@H](Cc1ccc(O)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1021/jm070030d
688467 85357 2 None 14 2 Human 5.4 pKi = 5.4 Binding
Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.
ChEMBL 303 6 5 5 2.1 C[C@@H](Cc1ccc(O)cc1)NC[C@H](O)c1cc(O)cc(O)c1 nan
CHEMBL229476 85357 2 None 14 2 Human 5.4 pKi = 5.4 Binding
Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.
ChEMBL 303 6 5 5 2.1 C[C@@H](Cc1ccc(O)cc1)NC[C@H](O)c1cc(O)cc(O)c1 nan
46889771 6901 0 None 6 3 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cells
ChEMBL 549 7 3 6 4.9 O=C1c2cccc3cc(O)cc(c23)C(=O)N1CC1CCN(CC(O)COc2cccc3[nH]c4ccccc4c23)CC1 10.1016/j.bmcl.2010.04.009
CHEMBL1084706 6901 0 None 6 3 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cells
ChEMBL 549 7 3 6 4.9 O=C1c2cccc3cc(O)cc(c23)C(=O)N1CC1CCN(CC(O)COc2cccc3[nH]c4ccccc4c23)CC1 10.1016/j.bmcl.2010.04.009
9946573 154203 0 None 10 2 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]iodocyanopindolol from human adrenergic beta-2 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human adrenergic beta-2 receptor expressed in CHO cells
ChEMBL 353 9 2 6 3.0 CCc1nc(-c2ccc(OCCNC[C@H](O)c3cccnc3)cc2)co1 10.1016/j.bmcl.2007.06.072
CHEMBL400049 154203 0 None 10 2 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]iodocyanopindolol from human adrenergic beta-2 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human adrenergic beta-2 receptor expressed in CHO cells
ChEMBL 353 9 2 6 3.0 CCc1nc(-c2ccc(OCCNC[C@H](O)c3cccnc3)cc2)co1 10.1016/j.bmcl.2007.06.072
52946430 17628 0 None -1 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 517 9 3 8 3.7 CNC(=O)c1cccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)c1 10.1016/j.bmcl.2010.08.039
CHEMBL1258940 17628 0 None -1 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 517 9 3 8 3.7 CNC(=O)c1cccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)c1 10.1016/j.bmcl.2010.08.039
247704 288 26 None -3 5 Dog 5.4 pKi = 5.4 Binding
Binding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranes
ChEMBL 183 3 4 4 0.4 CNC[C@H](c1ccc(c(c1)O)O)O 10.1021/jm990599h
4450 288 26 None -3 5 Dog 5.4 pKi = 5.4 Binding
Binding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranes
ChEMBL 183 3 4 4 0.4 CNC[C@H](c1ccc(c(c1)O)O)O 10.1021/jm990599h
CHEMBL42280 288 26 None -3 5 Dog 5.4 pKi = 5.4 Binding
Binding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranes
ChEMBL 183 3 4 4 0.4 CNC[C@H](c1ccc(c(c1)O)O)O 10.1021/jm990599h
13720717 77483 0 None 3 2 Guinea pig 6.4 pKi = 6.4 Binding
Binding affinity against Beta-2 adrenergic receptor in guinea pig lung membranesBinding affinity against Beta-2 adrenergic receptor in guinea pig lung membranes
ChEMBL 363 5 3 6 2.7 COc1cc(C[C@H]2NCCc3cc(O)c(O)c(F)c32)cc(OC)c1OC 10.1021/jm00081a007
CHEMBL2092996 77483 0 None 3 2 Guinea pig 6.4 pKi = 6.4 Binding
Binding affinity against Beta-2 adrenergic receptor in guinea pig lung membranesBinding affinity against Beta-2 adrenergic receptor in guinea pig lung membranes
ChEMBL 363 5 3 6 2.7 COc1cc(C[C@H]2NCCc3cc(O)c(O)c(F)c32)cc(OC)c1OC 10.1021/jm00081a007
688467 85357 2 None 14 2 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 303 6 5 5 2.1 C[C@@H](Cc1ccc(O)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1021/jm070030d
CHEMBL229476 85357 2 None 14 2 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 303 6 5 5 2.1 C[C@@H](Cc1ccc(O)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1021/jm070030d
693141 115671 37 None - 1 Human 3.4 pKi = 3.4 Binding
Displacement of [3H]-DHA from Nb69-fused beta2 adrenergic receptor (unknown origin) expressed in Sf9 cell membranes after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-DHA from Nb69-fused beta2 adrenergic receptor (unknown origin) expressed in Sf9 cell membranes after 2 hrs by microbeta scintillation counting method
ChEMBL 177 2 1 2 2.6 CNCc1cc2ccccc2s1 10.1021/acs.jmedchem.7b01558
CHEMBL3358195 115671 37 None - 1 Human 3.4 pKi = 3.4 Binding
Displacement of [3H]-DHA from Nb69-fused beta2 adrenergic receptor (unknown origin) expressed in Sf9 cell membranes after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-DHA from Nb69-fused beta2 adrenergic receptor (unknown origin) expressed in Sf9 cell membranes after 2 hrs by microbeta scintillation counting method
ChEMBL 177 2 1 2 2.6 CNCc1cc2ccccc2s1 10.1021/acs.jmedchem.7b01558
46889728 6624 0 None 5 3 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cells
ChEMBL 516 9 1 6 4.7 COc1cc2c3c(cccc3c1)C(=O)N(CC1CCN(CC(O)COc3ccccc3C(C)C)CC1)C2=O 10.1016/j.bmcl.2010.04.009
CHEMBL1083666 6624 0 None 5 3 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cells
ChEMBL 516 9 1 6 4.7 COc1cc2c3c(cccc3c1)C(=O)N(CC1CCN(CC(O)COc3ccccc3C(C)C)CC1)C2=O 10.1016/j.bmcl.2010.04.009
44444179 93695 0 None 3 3 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]iodocyanopindolol from human cloned adrenergic beta-2 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human cloned adrenergic beta-2 receptor expressed in CHO cells
ChEMBL 508 10 4 5 4.5 CS(=O)(=O)Nc1cc(C[C@H](O)CN[C@H](Cc2ccccc2)c2ccc(Cl)c(Cl)c2)ccc1O 10.1016/j.bmcl.2007.05.030
CHEMBL249359 93695 0 None 3 3 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]iodocyanopindolol from human cloned adrenergic beta-2 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human cloned adrenergic beta-2 receptor expressed in CHO cells
ChEMBL 508 10 4 5 4.5 CS(=O)(=O)Nc1cc(C[C@H](O)CN[C@H](Cc2ccccc2)c2ccc(Cl)c(Cl)c2)ccc1O 10.1016/j.bmcl.2007.05.030
155545790 172903 0 None 12 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysisDisplacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysis
ChEMBL 593 18 5 13 1.6 CC(C)NC[C@H](O)COc1ccccc1-n1cc(CNCc2cn(-c3ccccc3OC[C@@H](O)CNC(C)C)nn2)nn1 10.1021/acs.jmedchem.9b00595
CHEMBL4530266 172903 0 None 12 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysisDisplacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysis
ChEMBL 593 18 5 13 1.6 CC(C)NC[C@H](O)COc1ccccc1-n1cc(CNCc2cn(-c3ccccc3OC[C@@H](O)CNC(C)C)nn2)nn1 10.1021/acs.jmedchem.9b00595
155527582 170642 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assay
ChEMBL 333 10 3 6 2.5 COc1ccccc1OCCNCCCOc1ccc(O)c(O)c1 10.1021/acs.jmedchem.9b00349
CHEMBL4459541 170642 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assay
ChEMBL 333 10 3 6 2.5 COc1ccccc1OCCNCCCOc1ccc(O)c(O)c1 10.1021/acs.jmedchem.9b00349
10774431 158642 8 None - 1 Dog 4.4 pKi = 4.4 Binding
Binding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranes
ChEMBL 201 3 4 4 0.5 CNC[C@H](O)c1cc(O)c(O)cc1F 10.1021/jm990599h
CHEMBL40986 158642 8 None - 1 Dog 4.4 pKi = 4.4 Binding
Binding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranes
ChEMBL 201 3 4 4 0.5 CNC[C@H](O)c1cc(O)c(O)cc1F 10.1021/jm990599h
123600 2275 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cells in presence of 100 uM boric acidDisplacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cells in presence of 100 uM boric acid
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)[C@H](CNC(C)(C)C)O 10.1016/j.bmc.2011.11.054
1575 2275 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cells in presence of 100 uM boric acidDisplacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cells in presence of 100 uM boric acid
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)[C@H](CNC(C)(C)C)O 10.1016/j.bmc.2011.11.054
9816 2275 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cells in presence of 100 uM boric acidDisplacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cells in presence of 100 uM boric acid
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)[C@H](CNC(C)(C)C)O 10.1016/j.bmc.2011.11.054
CHEMBL1002 2275 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cells in presence of 100 uM boric acidDisplacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cells in presence of 100 uM boric acid
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)[C@H](CNC(C)(C)C)O 10.1016/j.bmc.2011.11.054
DB13139 2275 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cells in presence of 100 uM boric acidDisplacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cells in presence of 100 uM boric acid
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)[C@H](CNC(C)(C)C)O 10.1016/j.bmc.2011.11.054
123600 2275 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cells in presence of 100 uM boric acidDisplacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cells in presence of 100 uM boric acid
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)[C@H](CNC(C)(C)C)O 10.1016/j.bmc.2011.11.054
1575 2275 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cells in presence of 100 uM boric acidDisplacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cells in presence of 100 uM boric acid
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)[C@H](CNC(C)(C)C)O 10.1016/j.bmc.2011.11.054
9816 2275 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cells in presence of 100 uM boric acidDisplacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cells in presence of 100 uM boric acid
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)[C@H](CNC(C)(C)C)O 10.1016/j.bmc.2011.11.054
CHEMBL1002 2275 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cells in presence of 100 uM boric acidDisplacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cells in presence of 100 uM boric acid
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)[C@H](CNC(C)(C)C)O 10.1016/j.bmc.2011.11.054
DB13139 2275 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cells in presence of 100 uM boric acidDisplacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cells in presence of 100 uM boric acid
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)[C@H](CNC(C)(C)C)O 10.1016/j.bmc.2011.11.054
9866060 77245 0 None -1 2 Human 6.4 pKi = 6.4 Binding
Binding affinity to human beta2-adrenoceptor by radioligand binding assayBinding affinity to human beta2-adrenoceptor by radioligand binding assay
ChEMBL 406 6 4 4 3.5 CCc1cc2c(cc1CC)CC(NCC(O)c1ccc(O)c3[nH]c(=O)c(C)cc13)C2 10.1016/j.bmcl.2012.07.096
CHEMBL2088196 77245 0 None -1 2 Human 6.4 pKi = 6.4 Binding
Binding affinity to human beta2-adrenoceptor by radioligand binding assayBinding affinity to human beta2-adrenoceptor by radioligand binding assay
ChEMBL 406 6 4 4 3.5 CCc1cc2c(cc1CC)CC(NCC(O)c1ccc(O)c3[nH]c(=O)c(C)cc13)C2 10.1016/j.bmcl.2012.07.096
10527469 155712 1 None -8317 16 Human 5.4 pKi = 5.4 Binding
Binding affinity against adrenergic receptor subtype Beta-2 adrenergic receptor using [3H]DHA as radioligandBinding affinity against adrenergic receptor subtype Beta-2 adrenergic receptor using [3H]DHA as radioligand
ChEMBL 448 4 1 7 3.0 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(sc5cccnc54)c3=O)C[C@@H]21 10.1021/jm970364a
CHEMBL40650 155712 1 None -8317 16 Human 5.4 pKi = 5.4 Binding
Binding affinity against adrenergic receptor subtype Beta-2 adrenergic receptor using [3H]DHA as radioligandBinding affinity against adrenergic receptor subtype Beta-2 adrenergic receptor using [3H]DHA as radioligand
ChEMBL 448 4 1 7 3.0 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(sc5cccnc54)c3=O)C[C@@H]21 10.1021/jm970364a
6603724 154780 3 None -1 3 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]prazosin from human adrenergic beta2 receptor T164I mutant expressed in CHO cell membraneDisplacement of [3H]prazosin from human adrenergic beta2 receptor T164I mutant expressed in CHO cell membrane
ChEMBL 187 2 4 4 0.2 NC[C@H](O)c1cc(O)c(O)cc1F 10.1016/j.bmc.2009.10.015
CHEMBL40317 154780 3 None -1 3 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]prazosin from human adrenergic beta2 receptor T164I mutant expressed in CHO cell membraneDisplacement of [3H]prazosin from human adrenergic beta2 receptor T164I mutant expressed in CHO cell membrane
ChEMBL 187 2 4 4 0.2 NC[C@H](O)c1cc(O)c(O)cc1F 10.1016/j.bmc.2009.10.015
70686652 76408 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cellsDisplacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cells
ChEMBL 283 3 4 5 -0.1 CC(C)(C)NC[C@H](O)c1ccc2c(c1)C[OH+][B-](O)(O)O2 10.1016/j.bmc.2011.11.054
CHEMBL2068576 76408 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cellsDisplacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cells
ChEMBL 283 3 4 5 -0.1 CC(C)(C)NC[C@H](O)c1ccc2c(c1)C[OH+][B-](O)(O)O2 10.1016/j.bmc.2011.11.054
70686652 76408 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cellsDisplacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cells
ChEMBL 283 3 4 5 -0.1 CC(C)(C)NC[C@H](O)c1ccc2c(c1)C[OH+][B-](O)(O)O2 10.1016/j.bmc.2011.11.054
CHEMBL2068576 76408 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cellsDisplacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cells
ChEMBL 283 3 4 5 -0.1 CC(C)(C)NC[C@H](O)c1ccc2c(c1)C[OH+][B-](O)(O)O2 10.1016/j.bmc.2011.11.054
53380559 63295 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 317 7 5 5 2.4 CC[C@H](Cc1ccc(O)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2013.11.030
CHEMBL1800936 63295 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 317 7 5 5 2.4 CC[C@H](Cc1ccc(O)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2013.11.030
53380559 63295 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 317 7 5 5 2.4 CC[C@H](Cc1ccc(O)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2013.11.030
CHEMBL1800936 63295 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 317 7 5 5 2.4 CC[C@H](Cc1ccc(O)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2013.11.030
44444185 154208 0 None -43 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]iodocyanopindolol from human cloned adrenergic beta-2 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human cloned adrenergic beta-2 receptor expressed in CHO cells
ChEMBL 514 13 4 7 3.6 COc1ccc([C@H](CCc2ccccc2)NC[C@H](O)Cc2ccc(O)c(NS(C)(=O)=O)c2)cc1OC 10.1016/j.bmcl.2007.05.030
CHEMBL400067 154208 0 None -43 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]iodocyanopindolol from human cloned adrenergic beta-2 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human cloned adrenergic beta-2 receptor expressed in CHO cells
ChEMBL 514 13 4 7 3.6 COc1ccc([C@H](CCc2ccccc2)NC[C@H](O)Cc2ccc(O)c(NS(C)(=O)=O)c2)cc1OC 10.1016/j.bmcl.2007.05.030
14485410 202388 0 None - 1 Mouse 6.4 pKi = 6.4 Binding
Ki value was determined by accumulation of c-AMP in S-49 mouse lymphoma cells (Beta2).Ki value was determined by accumulation of c-AMP in S-49 mouse lymphoma cells (Beta2).
ChEMBL 495 13 4 5 4.6 CC(=O)Nc1ccc(OCC(O)CNC(C)CCCCC(=O)Nc2ccc(C(F)(F)F)cc2)cc1 10.1021/jm00163a036
CHEMBL70217 202388 0 None - 1 Mouse 6.4 pKi = 6.4 Binding
Ki value was determined by accumulation of c-AMP in S-49 mouse lymphoma cells (Beta2).Ki value was determined by accumulation of c-AMP in S-49 mouse lymphoma cells (Beta2).
ChEMBL 495 13 4 5 4.6 CC(=O)Nc1ccc(OCC(O)CNC(C)CCCCC(=O)Nc2ccc(C(F)(F)F)cc2)cc1 10.1021/jm00163a036
145974110 163912 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-DHA from Nb69-fused beta2 adrenergic receptor (unknown origin) expressed in Sf9 cell membranes after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-DHA from Nb69-fused beta2 adrenergic receptor (unknown origin) expressed in Sf9 cell membranes after 2 hrs by microbeta scintillation counting method
ChEMBL 356 8 1 3 4.6 COc1ccc2c(c1)c(CCNCCCc1ccc(Cl)cc1)cn2C 10.1021/acs.jmedchem.7b01558
CHEMBL4214185 163912 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-DHA from Nb69-fused beta2 adrenergic receptor (unknown origin) expressed in Sf9 cell membranes after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-DHA from Nb69-fused beta2 adrenergic receptor (unknown origin) expressed in Sf9 cell membranes after 2 hrs by microbeta scintillation counting method
ChEMBL 356 8 1 3 4.6 COc1ccc2c(c1)c(CCNCCCc1ccc(Cl)cc1)cn2C 10.1021/acs.jmedchem.7b01558
14485432 202809 0 None - 1 Mouse 4.4 pKi = 4.4 Binding
Ki value was determined by accumulation of c-AMP in S-49 mouse lymphoma cells (Beta2).Ki value was determined by accumulation of c-AMP in S-49 mouse lymphoma cells (Beta2).
ChEMBL 488 12 3 4 5.8 C[C@@H](CCCCC(=O)Nc1ccc(C(F)(F)F)cc1)NC[C@H](O)COc1cccc2ccccc12 10.1021/jm00163a036
CHEMBL72707 202809 0 None - 1 Mouse 4.4 pKi = 4.4 Binding
Ki value was determined by accumulation of c-AMP in S-49 mouse lymphoma cells (Beta2).Ki value was determined by accumulation of c-AMP in S-49 mouse lymphoma cells (Beta2).
ChEMBL 488 12 3 4 5.8 C[C@@H](CCCCC(=O)Nc1ccc(C(F)(F)F)cc1)NC[C@H](O)COc1cccc2ccccc12 10.1021/jm00163a036
145978746 163133 0 None - 1 Human 3.4 pKi = 3.4 Binding
Displacement of [3H]-DHA from Nb69-fused beta2 adrenergic receptor (unknown origin) expressed in Sf9 cell membranes after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-DHA from Nb69-fused beta2 adrenergic receptor (unknown origin) expressed in Sf9 cell membranes after 2 hrs by microbeta scintillation counting method
ChEMBL 300 5 1 3 4.2 CC(CC(F)(F)F)NCc1ccc(-c2nccs2)cc1 10.1021/acs.jmedchem.7b01558
CHEMBL4204907 163133 0 None - 1 Human 3.4 pKi = 3.4 Binding
Displacement of [3H]-DHA from Nb69-fused beta2 adrenergic receptor (unknown origin) expressed in Sf9 cell membranes after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-DHA from Nb69-fused beta2 adrenergic receptor (unknown origin) expressed in Sf9 cell membranes after 2 hrs by microbeta scintillation counting method
ChEMBL 300 5 1 3 4.2 CC(CC(F)(F)F)NCc1ccc(-c2nccs2)cc1 10.1021/acs.jmedchem.7b01558
44286964 162832 0 None 1 2 Human 4.4 pKi = 4.4 Binding
Ability to bind to human Beta-2 adrenergic receptor using membranes of stably transfected CHO cellsAbility to bind to human Beta-2 adrenergic receptor using membranes of stably transfected CHO cells
ChEMBL 399 9 4 4 3.1 C[C@H](Cc1ccc(OCP(=O)(O)O)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1016/S0960-894X(97)00266-7
CHEMBL41948 162832 0 None 1 2 Human 4.4 pKi = 4.4 Binding
Ability to bind to human Beta-2 adrenergic receptor using membranes of stably transfected CHO cellsAbility to bind to human Beta-2 adrenergic receptor using membranes of stably transfected CHO cells
ChEMBL 399 9 4 4 3.1 C[C@H](Cc1ccc(OCP(=O)(O)O)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1016/S0960-894X(97)00266-7
6603724 154780 3 None -1 3 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]prazosin from human adrenergic beta2 receptor V117C mutant expressed in CHO cell membraneDisplacement of [3H]prazosin from human adrenergic beta2 receptor V117C mutant expressed in CHO cell membrane
ChEMBL 187 2 4 4 0.2 NC[C@H](O)c1cc(O)c(O)cc1F 10.1016/j.bmc.2009.10.015
CHEMBL40317 154780 3 None -1 3 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]prazosin from human adrenergic beta2 receptor V117C mutant expressed in CHO cell membraneDisplacement of [3H]prazosin from human adrenergic beta2 receptor V117C mutant expressed in CHO cell membrane
ChEMBL 187 2 4 4 0.2 NC[C@H](O)c1cc(O)c(O)cc1F 10.1016/j.bmc.2009.10.015
145947253 167079 0 None -1 2 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]-CGP12177 from human beta2 ADR expressed in HEK293T cell membrane after 90 mins by scintillation countingDisplacement of [3H]-CGP12177 from human beta2 ADR expressed in HEK293T cell membrane after 90 mins by scintillation counting
ChEMBL 364 10 3 5 1.2 CNCC(O)COc1ccc(S(=O)(=O)NCCc2ccccc2)cc1 10.1021/acs.jmedchem.8b00625
CHEMBL4162590 167079 0 None -1 2 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]-CGP12177 from human beta2 ADR expressed in HEK293T cell membrane after 90 mins by scintillation countingDisplacement of [3H]-CGP12177 from human beta2 ADR expressed in HEK293T cell membrane after 90 mins by scintillation counting
ChEMBL 364 10 3 5 1.2 CNCC(O)COc1ccc(S(=O)(=O)NCCc2ccccc2)cc1 10.1021/acs.jmedchem.8b00625
CHEMBL4301724 167079 0 None -1 2 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]-CGP12177 from human beta2 ADR expressed in HEK293T cell membrane after 90 mins by scintillation countingDisplacement of [3H]-CGP12177 from human beta2 ADR expressed in HEK293T cell membrane after 90 mins by scintillation counting
ChEMBL 364 10 3 5 1.2 CNCC(O)COc1ccc(S(=O)(=O)NCCc2ccccc2)cc1 10.1021/acs.jmedchem.8b00625
90644148 111742 0 None - 1 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assay
ChEMBL 474 10 4 6 3.9 O=C(c1ccccc1)C1CCN(c2ccc(CCNCC(O)c3ccc(O)c(CO)c3)cc2)CC1 10.1016/j.bmcl.2014.04.069
CHEMBL3290977 111742 0 None - 1 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assay
ChEMBL 474 10 4 6 3.9 O=C(c1ccccc1)C1CCN(c2ccc(CCNCC(O)c3ccc(O)c(CO)c3)cc2)CC1 10.1016/j.bmcl.2014.04.069
2867500 55215 8 None - 1 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]dihydroalprenolol from human ADRB2 expressed in HEK293T cells after 1 hr by liquid scintillation counterDisplacement of [3H]dihydroalprenolol from human ADRB2 expressed in HEK293T cells after 1 hr by liquid scintillation counter
ChEMBL 336 8 2 5 1.5 Cc1ccc(C(C)C)c(OCC(O)CN2CCN(CCO)CC2)c1 10.1021/jm300280e
CHEMBL1620339 55215 8 None - 1 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]dihydroalprenolol from human ADRB2 expressed in HEK293T cells after 1 hr by liquid scintillation counterDisplacement of [3H]dihydroalprenolol from human ADRB2 expressed in HEK293T cells after 1 hr by liquid scintillation counter
ChEMBL 336 8 2 5 1.5 Cc1ccc(C(C)C)c(OCC(O)CN2CCN(CCO)CC2)c1 10.1021/jm300280e
1070880 55429 8 None - 1 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]dihydroalprenolol from human ADRB2 expressed in HEK293T cells after 1 hr by liquid scintillation counterDisplacement of [3H]dihydroalprenolol from human ADRB2 expressed in HEK293T cells after 1 hr by liquid scintillation counter
ChEMBL 355 6 1 5 4.7 CC(=O)c1c(CSc2ccccc2)oc2ccc(O)c(CN(C)C)c12 10.1021/jm300280e
28434923 55429 8 None - 1 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]dihydroalprenolol from human ADRB2 expressed in HEK293T cells after 1 hr by liquid scintillation counterDisplacement of [3H]dihydroalprenolol from human ADRB2 expressed in HEK293T cells after 1 hr by liquid scintillation counter
ChEMBL 355 6 1 5 4.7 CC(=O)c1c(CSc2ccccc2)oc2ccc(O)c(CN(C)C)c12 10.1021/jm300280e
CHEMBL1622248 55429 8 None - 1 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]dihydroalprenolol from human ADRB2 expressed in HEK293T cells after 1 hr by liquid scintillation counterDisplacement of [3H]dihydroalprenolol from human ADRB2 expressed in HEK293T cells after 1 hr by liquid scintillation counter
ChEMBL 355 6 1 5 4.7 CC(=O)c1c(CSc2ccccc2)oc2ccc(O)c(CN(C)C)c12 10.1021/jm300280e
183812 204015 21 None 977 2 Human 8.4 pKi = 8.4 Binding
Binding affinity to human beta2-adrenoceptor by radioligand binding assayBinding affinity to human beta2-adrenoceptor by radioligand binding assay
ChEMBL 464 13 3 8 2.9 O=S(=O)(CCCOCCc1ccccc1)CCNCCc1ccc(O)c2nc(O)sc12 10.1016/j.bmcl.2012.07.096
CHEMBL82663 204015 21 None 977 2 Human 8.4 pKi = 8.4 Binding
Binding affinity to human beta2-adrenoceptor by radioligand binding assayBinding affinity to human beta2-adrenoceptor by radioligand binding assay
ChEMBL 464 13 3 8 2.9 O=S(=O)(CCCOCCc1ccccc1)CCNCCc1ccc(O)c2nc(O)sc12 10.1016/j.bmcl.2012.07.096
52943362 17351 0 None 2 3 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 466 8 2 8 4.4 OC(CNC1CCN(c2ncnc3scc(-c4cccs4)c23)CC1)COc1ccccc1 10.1016/j.bmcl.2010.08.039
CHEMBL1258025 17351 0 None 2 3 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 466 8 2 8 4.4 OC(CNC1CCN(c2ncnc3scc(-c4cccs4)c23)CC1)COc1ccccc1 10.1016/j.bmcl.2010.08.039
688468 141788 7 None 190 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 303 6 5 5 2.1 C[C@H](Cc1ccc(O)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2013.11.030
CHEMBL388570 141788 7 None 190 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 303 6 5 5 2.1 C[C@H](Cc1ccc(O)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2013.11.030
49864416 15455 0 None 30 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptorDisplacement of [3H]CGP12177 from human beta2 adrenoceptor
ChEMBL 376 5 4 5 3.7 O=c1[nH]c2c(O)ccc([C@@H](O)CNC3CCCC3C3CCCCC3)c2s1 10.1016/j.bmcl.2010.06.136
CHEMBL1221736 15455 0 None 30 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptorDisplacement of [3H]CGP12177 from human beta2 adrenoceptor
ChEMBL 376 5 4 5 3.7 O=c1[nH]c2c(O)ccc([C@@H](O)CNC3CCCC3C3CCCCC3)c2s1 10.1016/j.bmcl.2010.06.136
16735257 85290 0 None 151 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 317 7 4 5 2.4 COc1ccc(C[C@@H](C)NC[C@H](O)c2cc(O)cc(O)c2)cc1 10.1016/j.bmc.2013.11.030
CHEMBL228992 85290 0 None 151 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 317 7 4 5 2.4 COc1ccc(C[C@@H](C)NC[C@H](O)c2cc(O)cc(O)c2)cc1 10.1016/j.bmc.2013.11.030
16735257 85290 0 None 151 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 317 7 4 5 2.4 COc1ccc(C[C@@H](C)NC[C@H](O)c2cc(O)cc(O)c2)cc1 10.1016/j.bmc.2013.11.030
CHEMBL228992 85290 0 None 151 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 317 7 4 5 2.4 COc1ccc(C[C@@H](C)NC[C@H](O)c2cc(O)cc(O)c2)cc1 10.1016/j.bmc.2013.11.030
118710939 113237 0 None 14 3 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assay
ChEMBL 336 5 4 5 2.7 CC(C)[C@H]1CCC[C@H]1NC[C@H](O)c1ccc(O)c2[nH]c(=O)sc12 10.1016/j.bmcl.2014.06.014
CHEMBL3323657 113237 0 None 14 3 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assay
ChEMBL 336 5 4 5 2.7 CC(C)[C@H]1CCC[C@H]1NC[C@H](O)c1ccc(O)c2[nH]c(=O)sc12 10.1016/j.bmcl.2014.06.014
49864441 15458 0 None 4 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptorDisplacement of [3H]CGP12177 from human beta2 adrenoceptor
ChEMBL 346 7 4 6 2.0 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCOc3ccccc3)c2s1 10.1016/j.bmcl.2010.06.136
CHEMBL1221803 15458 0 None 4 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptorDisplacement of [3H]CGP12177 from human beta2 adrenoceptor
ChEMBL 346 7 4 6 2.0 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCOc3ccccc3)c2s1 10.1016/j.bmcl.2010.06.136
24937389 17251 0 None -4 3 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 520 10 3 9 4.2 COCc1cc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)ccc1O 10.1016/j.bmcl.2010.08.039
CHEMBL1257675 17251 0 None -4 3 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 520 10 3 9 4.2 COCc1cc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)ccc1O 10.1016/j.bmcl.2010.08.039
46889699 6555 0 None 26 3 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cells
ChEMBL 470 8 1 5 4.1 C=CCc1ccccc1OCC(O)CN1CCC(N2C(=O)c3cccc4cccc(c34)C2=O)CC1 10.1016/j.bmcl.2010.04.009
CHEMBL1083364 6555 0 None 26 3 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cells
ChEMBL 470 8 1 5 4.1 C=CCc1ccccc1OCC(O)CN1CCC(N2C(=O)c3cccc4cccc(c34)C2=O)CC1 10.1016/j.bmcl.2010.04.009
49864414 15453 0 None 37 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptorDisplacement of [3H]CGP12177 from human beta2 adrenoceptor
ChEMBL 362 4 4 5 3.1 CC1(C)[C@@H]2CC[C@]1(C)[C@@H](NC[C@H](O)c1ccc(O)c3[nH]c(=O)sc13)C2 10.1016/j.bmcl.2010.06.136
CHEMBL1221734 15453 0 None 37 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptorDisplacement of [3H]CGP12177 from human beta2 adrenoceptor
ChEMBL 362 4 4 5 3.1 CC1(C)[C@@H]2CC[C@]1(C)[C@@H](NC[C@H](O)c1ccc(O)c3[nH]c(=O)sc13)C2 10.1016/j.bmcl.2010.06.136
44361723 33791 0 None - 1 Dog 5.4 pKi = 5.4 Binding
Beta-2 adrenergic receptor binding affinity by measuring the displacement of [3H]DHA binding in rat lungBeta-2 adrenergic receptor binding affinity by measuring the displacement of [3H]DHA binding in rat lung
ChEMBL 429 7 2 7 2.3 COc1ccccc1N1CCN(CC(O)COc2ccc3c(c2)NC(=O)CS3)CC1 10.1016/s0960-894x(00)00016-0
CHEMBL142474 33791 0 None - 1 Dog 5.4 pKi = 5.4 Binding
Beta-2 adrenergic receptor binding affinity by measuring the displacement of [3H]DHA binding in rat lungBeta-2 adrenergic receptor binding affinity by measuring the displacement of [3H]DHA binding in rat lung
ChEMBL 429 7 2 7 2.3 COc1ccccc1N1CCN(CC(O)COc2ccc3c(c2)NC(=O)CS3)CC1 10.1016/s0960-894x(00)00016-0
11299620 96822 2 None -74131 6 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cellsDisplacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells
ChEMBL 247 5 1 2 3.4 CCCN(CCC)[C@H]1CCc2c(O)cccc2C1 10.1016/j.bmc.2016.04.028
CHEMBL269004 96822 2 None -74131 6 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cellsDisplacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells
ChEMBL 247 5 1 2 3.4 CCCN(CCC)[C@H]1CCc2c(O)cccc2C1 10.1016/j.bmc.2016.04.028
53379897 63300 0 None 40 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]CGP-12177 from human beta2-adrenergic receptor expressed in HEK 293 cellsDisplacement of [3H]CGP-12177 from human beta2-adrenergic receptor expressed in HEK 293 cells
ChEMBL 337 6 4 4 3.5 C[C@H](Cc1ccc2ccccc2c1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2009.11.062
CHEMBL1800961 63300 0 None 40 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]CGP-12177 from human beta2-adrenergic receptor expressed in HEK 293 cellsDisplacement of [3H]CGP-12177 from human beta2-adrenergic receptor expressed in HEK 293 cells
ChEMBL 337 6 4 4 3.5 C[C@H](Cc1ccc2ccccc2c1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2009.11.062
14485423 202658 0 None - 1 Mouse 4.4 pKi = 4.4 Binding
Ki value was determined by accumulation of c-AMP in S-49 mouse lymphoma cells (Beta2).Ki value was determined by accumulation of c-AMP in S-49 mouse lymphoma cells (Beta2).
ChEMBL 434 12 3 4 5.1 Cc1ccc(NC(=O)CCCC[C@H](C)NC[C@H](O)COc2cccc3ccccc23)cc1 10.1021/jm00163a036
CHEMBL71765 202658 0 None - 1 Mouse 4.4 pKi = 4.4 Binding
Ki value was determined by accumulation of c-AMP in S-49 mouse lymphoma cells (Beta2).Ki value was determined by accumulation of c-AMP in S-49 mouse lymphoma cells (Beta2).
ChEMBL 434 12 3 4 5.1 Cc1ccc(NC(=O)CCCC[C@H](C)NC[C@H](O)COc2cccc3ccccc23)cc1 10.1021/jm00163a036
52943932 17559 0 None 1 3 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 485 8 2 8 4.2 N#Cc1cccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)c1 10.1016/j.bmcl.2010.08.039
CHEMBL1258705 17559 0 None 1 3 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 485 8 2 8 4.2 N#Cc1cccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)c1 10.1016/j.bmcl.2010.08.039
73056754 103786 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-CGP-12177 from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-CGP-12177 from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 331 8 4 5 2.8 CC[C@H](Cc1ccc(OC)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2013.11.030
CHEMBL3099659 103786 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-CGP-12177 from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-CGP-12177 from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 331 8 4 5 2.8 CC[C@H](Cc1ccc(OC)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2013.11.030
155513731 169215 0 None 2 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assay
ChEMBL 241 6 4 5 0.8 CC(C)NC[C@@H](O)COc1ccc(O)c(O)c1 10.1021/acs.jmedchem.9b00349
CHEMBL4439238 169215 0 None 2 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assay
ChEMBL 241 6 4 5 0.8 CC(C)NC[C@@H](O)COc1ccc(O)c(O)c1 10.1021/acs.jmedchem.9b00349
1960 2805 64 None -30 26 Rat 5.4 pKi = 5.4 Binding
Binding affinity against adrenergic beta 2 receptor versus 1 nM [3H]dihydroalprenolol in rat cerebral cerebellar membranesBinding affinity against adrenergic beta 2 receptor versus 1 nM [3H]dihydroalprenolol in rat cerebral cerebellar membranes
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00076a024
439260 2805 64 None -30 26 Rat 5.4 pKi = 5.4 Binding
Binding affinity against adrenergic beta 2 receptor versus 1 nM [3H]dihydroalprenolol in rat cerebral cerebellar membranesBinding affinity against adrenergic beta 2 receptor versus 1 nM [3H]dihydroalprenolol in rat cerebral cerebellar membranes
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00076a024
505 2805 64 None -30 26 Rat 5.4 pKi = 5.4 Binding
Binding affinity against adrenergic beta 2 receptor versus 1 nM [3H]dihydroalprenolol in rat cerebral cerebellar membranesBinding affinity against adrenergic beta 2 receptor versus 1 nM [3H]dihydroalprenolol in rat cerebral cerebellar membranes
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00076a024
CHEMBL1437 2805 64 None -30 26 Rat 5.4 pKi = 5.4 Binding
Binding affinity against adrenergic beta 2 receptor versus 1 nM [3H]dihydroalprenolol in rat cerebral cerebellar membranesBinding affinity against adrenergic beta 2 receptor versus 1 nM [3H]dihydroalprenolol in rat cerebral cerebellar membranes
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00076a024
DB00368 2805 64 None -30 26 Rat 5.4 pKi = 5.4 Binding
Binding affinity against adrenergic beta 2 receptor versus 1 nM [3H]dihydroalprenolol in rat cerebral cerebellar membranesBinding affinity against adrenergic beta 2 receptor versus 1 nM [3H]dihydroalprenolol in rat cerebral cerebellar membranes
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00076a024
9958539 102618 0 None 1 3 Human 6.4 pKi = 6.4 Binding
Binding Affinity against human Beta-2 adrenergic receptor expressed in Chinese hamster ovary(CHO) cells was measured by using [125I]ICYP radioligandBinding Affinity against human Beta-2 adrenergic receptor expressed in Chinese hamster ovary(CHO) cells was measured by using [125I]ICYP radioligand
ChEMBL 527 3 2 5 3.4 COc1c(I)cc(CC2NCCc3nc(N)sc32)cc1I 10.1021/jm990012z
CHEMBL307647 102618 0 None 1 3 Human 6.4 pKi = 6.4 Binding
Binding Affinity against human Beta-2 adrenergic receptor expressed in Chinese hamster ovary(CHO) cells was measured by using [125I]ICYP radioligandBinding Affinity against human Beta-2 adrenergic receptor expressed in Chinese hamster ovary(CHO) cells was measured by using [125I]ICYP radioligand
ChEMBL 527 3 2 5 3.4 COc1c(I)cc(CC2NCCc3nc(N)sc32)cc1I 10.1021/jm990012z
44287268 158459 0 None -2 2 Human 4.4 pKi = 4.4 Binding
Ability to bind to human Beta-2 adrenergic receptor using membranes of stably transfected CHO cellsAbility to bind to human Beta-2 adrenergic receptor using membranes of stably transfected CHO cells
ChEMBL 441 11 3 5 4.5 CC(C)OP(=O)(O)COc1ccc(C[C@@H](C)NC[C@H](O)c2cccc(Cl)c2)cc1 10.1016/S0960-894X(97)00266-7
CHEMBL40966 158459 0 None -2 2 Human 4.4 pKi = 4.4 Binding
Ability to bind to human Beta-2 adrenergic receptor using membranes of stably transfected CHO cellsAbility to bind to human Beta-2 adrenergic receptor using membranes of stably transfected CHO cells
ChEMBL 441 11 3 5 4.5 CC(C)OP(=O)(O)COc1ccc(C[C@@H](C)NC[C@H](O)c2cccc(Cl)c2)cc1 10.1016/S0960-894X(97)00266-7
73056758 103787 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 331 8 4 5 2.8 CC[C@@H](Cc1ccc(OC)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2013.11.030
CHEMBL3099660 103787 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 331 8 4 5 2.8 CC[C@@H](Cc1ccc(OC)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2013.11.030
5581 101175 10 None -1 7 Human 7.4 pKi = 7.4 Binding
Binding Affinity against human beta-2 adrenergic receptor expressed in Chinese hamster ovary(CHO) cells was measured by using [125I]ICYP radioligandBinding Affinity against human beta-2 adrenergic receptor expressed in Chinese hamster ovary(CHO) cells was measured by using [125I]ICYP radioligand
ChEMBL 345 5 3 6 2.6 COc1cc(CC2NCCc3cc(O)c(O)cc32)cc(OC)c1OC 10.1021/jm990012z
CHEMBL299175 101175 10 None -1 7 Human 7.4 pKi = 7.4 Binding
Binding Affinity against human beta-2 adrenergic receptor expressed in Chinese hamster ovary(CHO) cells was measured by using [125I]ICYP radioligandBinding Affinity against human beta-2 adrenergic receptor expressed in Chinese hamster ovary(CHO) cells was measured by using [125I]ICYP radioligand
ChEMBL 345 5 3 6 2.6 COc1cc(CC2NCCc3cc(O)c(O)cc32)cc(OC)c1OC 10.1021/jm990012z
5581 101175 10 None -1 7 Human 7.4 pKi = 7.4 Binding
Binding affinity for human Beta-2 adrenergic receptor expressed in CHO cells by radioligand competition binding assays using [125I]iodocyanopindolol (ICYP)Binding affinity for human Beta-2 adrenergic receptor expressed in CHO cells by radioligand competition binding assays using [125I]iodocyanopindolol (ICYP)
ChEMBL 345 5 3 6 2.6 COc1cc(CC2NCCc3cc(O)c(O)cc32)cc(OC)c1OC 10.1021/jm960208o
CHEMBL299175 101175 10 None -1 7 Human 7.4 pKi = 7.4 Binding
Binding affinity for human Beta-2 adrenergic receptor expressed in CHO cells by radioligand competition binding assays using [125I]iodocyanopindolol (ICYP)Binding affinity for human Beta-2 adrenergic receptor expressed in CHO cells by radioligand competition binding assays using [125I]iodocyanopindolol (ICYP)
ChEMBL 345 5 3 6 2.6 COc1cc(CC2NCCc3cc(O)c(O)cc32)cc(OC)c1OC 10.1021/jm960208o
73056758 103787 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 331 8 4 5 2.8 CC[C@@H](Cc1ccc(OC)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2013.11.030
CHEMBL3099660 103787 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 331 8 4 5 2.8 CC[C@@H](Cc1ccc(OC)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2013.11.030
25023951 176369 0 None - 1 Golden hamster 5.4 pKi = 5.4 Binding
Displacement of [125I](-)-iodopindolol from adrenergic beta2 receptor in Syrian hamster DDT1 MF2 cellsDisplacement of [125I](-)-iodopindolol from adrenergic beta2 receptor in Syrian hamster DDT1 MF2 cells
ChEMBL 489 11 8 13 -0.8 Nc1cc(C(O)CNCCCCNc2ncnc3c2ncn3[C@@H]2O[C@H](CO)[C@@H](O)[C@H]2O)ccc1O 10.1021/jm800613s
CHEMBL462274 176369 0 None - 1 Golden hamster 5.4 pKi = 5.4 Binding
Displacement of [125I](-)-iodopindolol from adrenergic beta2 receptor in Syrian hamster DDT1 MF2 cellsDisplacement of [125I](-)-iodopindolol from adrenergic beta2 receptor in Syrian hamster DDT1 MF2 cells
ChEMBL 489 11 8 13 -0.8 Nc1cc(C(O)CNCCCCNc2ncnc3c2ncn3[C@@H]2O[C@H](CO)[C@@H](O)[C@H]2O)ccc1O 10.1021/jm800613s
693141 115671 37 None - 1 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]-DHA from Nb80-fused beta2 adrenergic receptor (unknown origin) expressed in Sf9 cell membranes after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-DHA from Nb80-fused beta2 adrenergic receptor (unknown origin) expressed in Sf9 cell membranes after 2 hrs by microbeta scintillation counting method
ChEMBL 177 2 1 2 2.6 CNCc1cc2ccccc2s1 10.1021/acs.jmedchem.7b01558
CHEMBL3358195 115671 37 None - 1 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]-DHA from Nb80-fused beta2 adrenergic receptor (unknown origin) expressed in Sf9 cell membranes after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-DHA from Nb80-fused beta2 adrenergic receptor (unknown origin) expressed in Sf9 cell membranes after 2 hrs by microbeta scintillation counting method
ChEMBL 177 2 1 2 2.6 CNCc1cc2ccccc2s1 10.1021/acs.jmedchem.7b01558
14485419 102251 0 None - 1 Mouse 4.4 pKi = 4.4 Binding
Ki value was determined by accumulation of c-AMP in S-49 mouse lymphoma cells (Beta2).Ki value was determined by accumulation of c-AMP in S-49 mouse lymphoma cells (Beta2).
ChEMBL 434 12 3 4 5.1 Cc1ccc(NC(=O)CCCCC(C)NCC(O)COc2cccc3ccccc23)cc1 10.1021/jm00163a036
CHEMBL304961 102251 0 None - 1 Mouse 4.4 pKi = 4.4 Binding
Ki value was determined by accumulation of c-AMP in S-49 mouse lymphoma cells (Beta2).Ki value was determined by accumulation of c-AMP in S-49 mouse lymphoma cells (Beta2).
ChEMBL 434 12 3 4 5.1 Cc1ccc(NC(=O)CCCCC(C)NCC(O)COc2cccc3ccccc23)cc1 10.1021/jm00163a036
10834286 113949 0 None 19 2 Human 5.4 pKi = 5.4 Binding
Binding affinity for human Beta-2 adrenergic receptor expressed in CHO cells by radioligand competition binding assays using [125I]iodocyanopindolol (ICYP)Binding affinity for human Beta-2 adrenergic receptor expressed in CHO cells by radioligand competition binding assays using [125I]iodocyanopindolol (ICYP)
ChEMBL 391 2 3 3 4.6 Oc1cc2c(cc1O)C(Cc1cc(C(F)(F)F)cc(C(F)(F)F)c1)NCC2 10.1021/jm960208o
CHEMBL333438 113949 0 None 19 2 Human 5.4 pKi = 5.4 Binding
Binding affinity for human Beta-2 adrenergic receptor expressed in CHO cells by radioligand competition binding assays using [125I]iodocyanopindolol (ICYP)Binding affinity for human Beta-2 adrenergic receptor expressed in CHO cells by radioligand competition binding assays using [125I]iodocyanopindolol (ICYP)
ChEMBL 391 2 3 3 4.6 Oc1cc2c(cc1O)C(Cc1cc(C(F)(F)F)cc(C(F)(F)F)c1)NCC2 10.1021/jm960208o
10236758 115259 3 None -44668 13 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]CGP12177 from human recombinant beta2 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by beta counting methodDisplacement of [3H]CGP12177 from human recombinant beta2 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by beta counting method
ChEMBL 328 7 0 2 4.3 CCCCC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL3354065 115259 3 None -44668 13 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]CGP12177 from human recombinant beta2 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by beta counting methodDisplacement of [3H]CGP12177 from human recombinant beta2 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by beta counting method
ChEMBL 328 7 0 2 4.3 CCCCC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.8b00265
145972154 164126 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-DHA from Nb80-fused beta2 adrenergic receptor (unknown origin) expressed in Sf9 cell membranes after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-DHA from Nb80-fused beta2 adrenergic receptor (unknown origin) expressed in Sf9 cell membranes after 2 hrs by microbeta scintillation counting method
ChEMBL 303 5 1 3 4.3 Cc1ccccc1C(C)NCc1ccc(-c2ncccn2)cc1 10.1021/acs.jmedchem.7b01558
CHEMBL4217119 164126 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-DHA from Nb80-fused beta2 adrenergic receptor (unknown origin) expressed in Sf9 cell membranes after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-DHA from Nb80-fused beta2 adrenergic receptor (unknown origin) expressed in Sf9 cell membranes after 2 hrs by microbeta scintillation counting method
ChEMBL 303 5 1 3 4.3 Cc1ccccc1C(C)NCc1ccc(-c2ncccn2)cc1 10.1021/acs.jmedchem.7b01558
13720716 62709 0 None 1 2 Guinea pig 7.4 pKi = 7.4 Binding
Binding affinity against Beta-2 adrenergic receptor in guinea pig lung membranesBinding affinity against Beta-2 adrenergic receptor in guinea pig lung membranes
ChEMBL 363 5 3 6 2.7 COc1cc(C[C@@H]2NCCc3cc(O)c(O)c(F)c32)cc(OC)c1OC 10.1021/jm00081a007
CHEMBL1788251 62709 0 None 1 2 Guinea pig 7.4 pKi = 7.4 Binding
Binding affinity against Beta-2 adrenergic receptor in guinea pig lung membranesBinding affinity against Beta-2 adrenergic receptor in guinea pig lung membranes
ChEMBL 363 5 3 6 2.7 COc1cc(C[C@@H]2NCCc3cc(O)c(O)c(F)c32)cc(OC)c1OC 10.1021/jm00081a007
52946357 17525 0 None 1 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 430 8 4 9 1.9 OCc1cc(OCC(O)CNC2CCN(c3ncnc4sccc34)CC2)ccc1O 10.1016/j.bmcl.2010.08.039
CHEMBL1258598 17525 0 None 1 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 430 8 4 9 1.9 OCc1cc(OCC(O)CNC2CCN(c3ncnc4sccc34)CC2)ccc1O 10.1016/j.bmcl.2010.08.039
70684846 77246 9 None 4 2 Human 7.4 pKi = 7.4 Binding
Binding affinity to human beta2-adrenoceptor by radioligand binding assayBinding affinity to human beta2-adrenoceptor by radioligand binding assay
ChEMBL 394 6 4 4 3.2 CCc1cc2c(cc1CC)CC(NC[C@H](O)c1ccc(O)c3c1CCC(=O)N3)C2 10.1016/j.bmcl.2012.07.096
CHEMBL2088197 77246 9 None 4 2 Human 7.4 pKi = 7.4 Binding
Binding affinity to human beta2-adrenoceptor by radioligand binding assayBinding affinity to human beta2-adrenoceptor by radioligand binding assay
ChEMBL 394 6 4 4 3.2 CCc1cc2c(cc1CC)CC(NC[C@H](O)c1ccc(O)c3c1CCC(=O)N3)C2 10.1016/j.bmcl.2012.07.096
155552185 173479 0 None -8128 16 Human 5.4 pKi = 5.4 Binding
Displacement of [3H] CGP12177 from beta2 adrenergic receptor (unknown origin)Displacement of [3H] CGP12177 from beta2 adrenergic receptor (unknown origin)
ChEMBL 491 10 2 5 4.3 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccc(F)cc2)c2ccccc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4544086 173479 0 None -8128 16 Human 5.4 pKi = 5.4 Binding
Displacement of [3H] CGP12177 from beta2 adrenergic receptor (unknown origin)Displacement of [3H] CGP12177 from beta2 adrenergic receptor (unknown origin)
ChEMBL 491 10 2 5 4.3 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccc(F)cc2)c2ccccc2)CC1 10.1021/acs.jmedchem.9b01085
44423646 84800 0 None 4 3 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]CYP from human adrenergic beta 2 receptor transfected in CHO cells in presence of 100 uM GTPDisplacement of [125I]CYP from human adrenergic beta 2 receptor transfected in CHO cells in presence of 100 uM GTP
ChEMBL 396 10 2 5 3.9 CCCCOc1ccc(C[C@@H](C)NC[C@@H](O)c2cc(Br)no2)cc1 10.1016/j.bmc.2007.01.056
CHEMBL225775 84800 0 None 4 3 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]CYP from human adrenergic beta 2 receptor transfected in CHO cells in presence of 100 uM GTPDisplacement of [125I]CYP from human adrenergic beta 2 receptor transfected in CHO cells in presence of 100 uM GTP
ChEMBL 396 10 2 5 3.9 CCCCOc1ccc(C[C@@H](C)NC[C@@H](O)c2cc(Br)no2)cc1 10.1016/j.bmc.2007.01.056
10103956 11081 0 None -2 2 Bovine 5.3 pKi = 5.3 Binding
Binding affinity against beta-2-adrenergic receptor in bovine lungBinding affinity against beta-2-adrenergic receptor in bovine lung
ChEMBL 188 7 2 4 0.8 CC/C=N/OCC(O)CNC(C)C 10.1021/jm00036a018
CHEMBL1178707 11081 0 None -2 2 Bovine 5.3 pKi = 5.3 Binding
Binding affinity against beta-2-adrenergic receptor in bovine lungBinding affinity against beta-2-adrenergic receptor in bovine lung
ChEMBL 188 7 2 4 0.8 CC/C=N/OCC(O)CNC(C)C 10.1021/jm00036a018
CHEMBL38114 11081 0 None -2 2 Bovine 5.3 pKi = 5.3 Binding
Binding affinity against beta-2-adrenergic receptor in bovine lungBinding affinity against beta-2-adrenergic receptor in bovine lung
ChEMBL 188 7 2 4 0.8 CC/C=N/OCC(O)CNC(C)C 10.1021/jm00036a018
14485430 202437 0 None - 1 Mouse 4.3 pKi = 4.3 Binding
Ki value was determined by accumulation of c-AMP in S-49 mouse lymphoma cells (Beta2).Ki value was determined by accumulation of c-AMP in S-49 mouse lymphoma cells (Beta2).
ChEMBL 488 12 3 4 5.8 C[C@H](CCCCC(=O)Nc1ccc(C(F)(F)F)cc1)NC[C@H](O)COc1cccc2ccccc12 10.1021/jm00163a036
CHEMBL70539 202437 0 None - 1 Mouse 4.3 pKi = 4.3 Binding
Ki value was determined by accumulation of c-AMP in S-49 mouse lymphoma cells (Beta2).Ki value was determined by accumulation of c-AMP in S-49 mouse lymphoma cells (Beta2).
ChEMBL 488 12 3 4 5.8 C[C@H](CCCCC(=O)Nc1ccc(C(F)(F)F)cc1)NC[C@H](O)COc1cccc2ccccc12 10.1021/jm00163a036
443372 10123 23 None -1 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assay
ChEMBL 211 4 4 4 1.1 CC(C)NC[C@H](O)c1ccc(O)c(O)c1 10.1021/acs.jmedchem.9b00349
CHEMBL1160723 10123 23 None -1 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assay
ChEMBL 211 4 4 4 1.1 CC(C)NC[C@H](O)c1ccc(O)c(O)c1 10.1021/acs.jmedchem.9b00349
CHEMBL2062275 10123 23 None -1 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assay
ChEMBL 211 4 4 4 1.1 CC(C)NC[C@H](O)c1ccc(O)c(O)c1 10.1021/acs.jmedchem.9b00349
1499 2052 43 None -33 17 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cellsDisplacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2016.04.028
3779 2052 43 None -33 17 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cellsDisplacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2016.04.028
536 2052 43 None -33 17 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cellsDisplacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2016.04.028
CHEMBL434 2052 43 None -33 17 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cellsDisplacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2016.04.028
DB01064 2052 43 None -33 17 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cellsDisplacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2016.04.028
10947658 28475 0 None -4168 17 Human 5.3 pKi = 5.3 Binding
Binding affinity against Beta-2 adrenergic receptorBinding affinity against Beta-2 adrenergic receptor
ChEMBL 335 1 1 2 3.0 C[C@H]1C[C@@H](C)N1C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)CC2N(C)C1 10.1021/jm020153s
CHEMBL137781 28475 0 None -4168 17 Human 5.3 pKi = 5.3 Binding
Binding affinity against Beta-2 adrenergic receptorBinding affinity against Beta-2 adrenergic receptor
ChEMBL 335 1 1 2 3.0 C[C@H]1C[C@@H](C)N1C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)CC2N(C)C1 10.1021/jm020153s
155537285 171707 0 None 5 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysisDisplacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysis
ChEMBL 558 19 6 8 1.2 CC(C)NC[C@H](O)COc1ccccc1CC(=O)NCCNC(=O)Cc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
CHEMBL4474813 171707 0 None 5 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysisDisplacement of [3H]DHA from beta2 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysis
ChEMBL 558 19 6 8 1.2 CC(C)NC[C@H](O)COc1ccccc1CC(=O)NCCNC(=O)Cc1ccccc1OC[C@@H](O)CNC(C)C 10.1021/acs.jmedchem.9b00595
123600 2275 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cells in presence of 100 uM phenylboronic acidDisplacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cells in presence of 100 uM phenylboronic acid
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)[C@H](CNC(C)(C)C)O 10.1016/j.bmc.2011.11.054
1575 2275 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cells in presence of 100 uM phenylboronic acidDisplacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cells in presence of 100 uM phenylboronic acid
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)[C@H](CNC(C)(C)C)O 10.1016/j.bmc.2011.11.054
9816 2275 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cells in presence of 100 uM phenylboronic acidDisplacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cells in presence of 100 uM phenylboronic acid
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)[C@H](CNC(C)(C)C)O 10.1016/j.bmc.2011.11.054
CHEMBL1002 2275 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cells in presence of 100 uM phenylboronic acidDisplacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cells in presence of 100 uM phenylboronic acid
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)[C@H](CNC(C)(C)C)O 10.1016/j.bmc.2011.11.054
DB13139 2275 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cells in presence of 100 uM phenylboronic acidDisplacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cells in presence of 100 uM phenylboronic acid
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)[C@H](CNC(C)(C)C)O 10.1016/j.bmc.2011.11.054
123600 2275 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cells in presence of 100 uM phenylboronic acidDisplacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cells in presence of 100 uM phenylboronic acid
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)[C@H](CNC(C)(C)C)O 10.1016/j.bmc.2011.11.054
1575 2275 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cells in presence of 100 uM phenylboronic acidDisplacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cells in presence of 100 uM phenylboronic acid
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)[C@H](CNC(C)(C)C)O 10.1016/j.bmc.2011.11.054
9816 2275 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cells in presence of 100 uM phenylboronic acidDisplacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cells in presence of 100 uM phenylboronic acid
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)[C@H](CNC(C)(C)C)O 10.1016/j.bmc.2011.11.054
CHEMBL1002 2275 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cells in presence of 100 uM phenylboronic acidDisplacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cells in presence of 100 uM phenylboronic acid
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)[C@H](CNC(C)(C)C)O 10.1016/j.bmc.2011.11.054
DB13139 2275 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cells in presence of 100 uM phenylboronic acidDisplacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cells in presence of 100 uM phenylboronic acid
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)[C@H](CNC(C)(C)C)O 10.1016/j.bmc.2011.11.054
127046951 139359 0 None 11 6 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cellsDisplacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells
ChEMBL 437 12 4 6 4.0 COc1cc(CCNC[C@@H](O)c2ccc(O)c(O)c2)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
CHEMBL3799427 139359 0 None 11 6 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cellsDisplacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells
ChEMBL 437 12 4 6 4.0 COc1cc(CCNC[C@@H](O)c2ccc(O)c(O)c2)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
16735257 85290 0 None 151 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 317 7 4 5 2.4 COc1ccc(C[C@@H](C)NC[C@H](O)c2cc(O)cc(O)c2)cc1 10.1021/jm070030d
CHEMBL228992 85290 0 None 151 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 317 7 4 5 2.4 COc1ccc(C[C@@H](C)NC[C@H](O)c2cc(O)cc(O)c2)cc1 10.1021/jm070030d
2977358 55877 3 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of radioligand from human adrenergic beta2 receptorDisplacement of radioligand from human adrenergic beta2 receptor
ChEMBL 271 7 2 3 2.7 CC(O)CNCCOc1ccccc1-c1ccccc1 10.1021/jm200371q
CHEMBL1626224 55877 3 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of radioligand from human adrenergic beta2 receptorDisplacement of radioligand from human adrenergic beta2 receptor
ChEMBL 271 7 2 3 2.7 CC(O)CNCCOc1ccccc1-c1ccccc1 10.1021/jm200371q
16735257 85290 0 None 151 2 Human 6.3 pKi = 6.3 Binding
Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.
ChEMBL 317 7 4 5 2.4 COc1ccc(C[C@@H](C)NC[C@H](O)c2cc(O)cc(O)c2)cc1 nan
CHEMBL228992 85290 0 None 151 2 Human 6.3 pKi = 6.3 Binding
Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.
ChEMBL 317 7 4 5 2.4 COc1ccc(C[C@@H](C)NC[C@H](O)c2cc(O)cc(O)c2)cc1 nan
73057082 103791 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 345 9 4 5 3.1 CCC[C@@H](Cc1ccc(OC)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2013.11.030
CHEMBL3099664 103791 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 345 9 4 5 3.1 CCC[C@@H](Cc1ccc(OC)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2013.11.030
73057082 103791 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 345 9 4 5 3.1 CCC[C@@H](Cc1ccc(OC)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2013.11.030
CHEMBL3099664 103791 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 345 9 4 5 3.1 CCC[C@@H](Cc1ccc(OC)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2013.11.030
16735257 85290 0 None 151 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 317 7 4 5 2.4 COc1ccc(C[C@@H](C)NC[C@H](O)c2cc(O)cc(O)c2)cc1 10.1021/jm070030d
CHEMBL228992 85290 0 None 151 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 317 7 4 5 2.4 COc1ccc(C[C@@H](C)NC[C@H](O)c2cc(O)cc(O)c2)cc1 10.1021/jm070030d
11432806 65851 0 None -12 3 Human 7.3 pKi = 7.3 Binding
Binding inhibition constant was determined by inhibition of [125I]iodocyanopindolol binding to Beta-2 adrenergic receptorBinding inhibition constant was determined by inhibition of [125I]iodocyanopindolol binding to Beta-2 adrenergic receptor
ChEMBL 549 11 4 8 3.6 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2004.09.054
11432806 65851 0 None -12 3 Human 7.3 pKi = 7.3 Binding
Binding inhibition constant was determined by inhibition of [125I]iodocyanopindolol binding to Beta-2 adrenergic receptorBinding inhibition constant was determined by inhibition of [125I]iodocyanopindolol binding to Beta-2 adrenergic receptor
ChEMBL 549 11 4 8 3.6 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2004.10.035
CHEMBL184407 65851 0 None -12 3 Human 7.3 pKi = 7.3 Binding
Binding inhibition constant was determined by inhibition of [125I]iodocyanopindolol binding to Beta-2 adrenergic receptorBinding inhibition constant was determined by inhibition of [125I]iodocyanopindolol binding to Beta-2 adrenergic receptor
ChEMBL 549 11 4 8 3.6 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2004.09.054
CHEMBL184407 65851 0 None -12 3 Human 7.3 pKi = 7.3 Binding
Binding inhibition constant was determined by inhibition of [125I]iodocyanopindolol binding to Beta-2 adrenergic receptorBinding inhibition constant was determined by inhibition of [125I]iodocyanopindolol binding to Beta-2 adrenergic receptor
ChEMBL 549 11 4 8 3.6 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2004.10.035
49864381 15443 0 None -1 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptorDisplacement of [3H]CGP12177 from human beta2 adrenoceptor
ChEMBL 380 5 4 5 3.8 C[C@H](NC[C@H](O)c1ccc(O)c2[nH]c(=O)sc12)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.06.136
CHEMBL1221638 15443 0 None -1 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptorDisplacement of [3H]CGP12177 from human beta2 adrenoceptor
ChEMBL 380 5 4 5 3.8 C[C@H](NC[C@H](O)c1ccc(O)c2[nH]c(=O)sc12)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.06.136
5581 101175 10 None 1 7 Guinea pig 7.3 pKi = 7.3 Binding
Binding affinity against Beta-2 adrenergic receptor in guinea pig lung membranesBinding affinity against Beta-2 adrenergic receptor in guinea pig lung membranes
ChEMBL 345 5 3 6 2.6 COc1cc(CC2NCCc3cc(O)c(O)cc32)cc(OC)c1OC 10.1021/jm00081a007
CHEMBL299175 101175 10 None 1 7 Guinea pig 7.3 pKi = 7.3 Binding
Binding affinity against Beta-2 adrenergic receptor in guinea pig lung membranesBinding affinity against Beta-2 adrenergic receptor in guinea pig lung membranes
ChEMBL 345 5 3 6 2.6 COc1cc(CC2NCCc3cc(O)c(O)cc32)cc(OC)c1OC 10.1021/jm00081a007
10651147 110181 0 None - 1 Human 6.3 pKi = 6.3 Binding
Inhibition of I-iodocyanopindolol binding to human beta 2 adrenergic receptorsInhibition of I-iodocyanopindolol binding to human beta 2 adrenergic receptors
ChEMBL 596 12 6 8 2.5 CS(=O)(=O)Nc1cc([C@@H](O)CNC2CCN(c3ccc(C(=O)N[C@@H](Cc4ccccc4)C(=O)O)cc3)CC2)ccc1O 10.1021/jm000544b
CHEMBL32599 110181 0 None - 1 Human 6.3 pKi = 6.3 Binding
Inhibition of I-iodocyanopindolol binding to human beta 2 adrenergic receptorsInhibition of I-iodocyanopindolol binding to human beta 2 adrenergic receptors
ChEMBL 596 12 6 8 2.5 CS(=O)(=O)Nc1cc([C@@H](O)CNC2CCN(c3ccc(C(=O)N[C@@H](Cc4ccccc4)C(=O)O)cc3)CC2)ccc1O 10.1021/jm000544b
44361776 35348 0 None - 1 Dog 5.3 pKi = 5.3 Binding
Beta-2 adrenergic receptor binding affinity by measuring the displacement of [3H]DHA binding in rat lungBeta-2 adrenergic receptor binding affinity by measuring the displacement of [3H]DHA binding in rat lung
ChEMBL 417 6 2 6 2.4 O=C1CSc2cc(OCC(O)CN3CCN(c4ccc(F)cc4)CC3)ccc2N1 10.1016/s0960-894x(00)00016-0
CHEMBL143944 35348 0 None - 1 Dog 5.3 pKi = 5.3 Binding
Beta-2 adrenergic receptor binding affinity by measuring the displacement of [3H]DHA binding in rat lungBeta-2 adrenergic receptor binding affinity by measuring the displacement of [3H]DHA binding in rat lung
ChEMBL 417 6 2 6 2.4 O=C1CSc2cc(OCC(O)CN3CCN(c4ccc(F)cc4)CC3)ccc2N1 10.1016/s0960-894x(00)00016-0
10292413 93830 0 None 7 2 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]iodocyanopindolol from human adrenergic beta-2 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human adrenergic beta-2 receptor expressed in CHO cells
ChEMBL 367 9 2 6 3.6 CC(C)c1nc(-c2ccc(OCCNC[C@H](O)c3cccnc3)cc2)co1 10.1016/j.bmcl.2007.06.072
CHEMBL250352 93830 0 None 7 2 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]iodocyanopindolol from human adrenergic beta-2 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human adrenergic beta-2 receptor expressed in CHO cells
ChEMBL 367 9 2 6 3.6 CC(C)c1nc(-c2ccc(OCCNC[C@H](O)c3cccnc3)cc2)co1 10.1016/j.bmcl.2007.06.072
12828562 109205 0 None -3 2 Bovine 5.3 pKi = 5.3 Binding
Tested for binding affinity against beta-2 adrenergic receptor in bovine lung using [3H]DHA as radioligandTested for binding affinity against beta-2 adrenergic receptor in bovine lung using [3H]DHA as radioligand
ChEMBL 237 3 3 4 1.7 CC(C)NCC1OCCc2cc(O)c(O)cc21 10.1021/jm00073a006
CHEMBL322842 109205 0 None -3 2 Bovine 5.3 pKi = 5.3 Binding
Tested for binding affinity against beta-2 adrenergic receptor in bovine lung using [3H]DHA as radioligandTested for binding affinity against beta-2 adrenergic receptor in bovine lung using [3H]DHA as radioligand
ChEMBL 237 3 3 4 1.7 CC(C)NCC1OCCc2cc(O)c(O)cc21 10.1021/jm00073a006
13864381 206593 3 None -48 4 Bovine 4.3 pKi = 4.3 Binding
Tested for binding affinity against beta-2 adrenergic receptor in bovine lung using [3H]DHA as radioligandTested for binding affinity against beta-2 adrenergic receptor in bovine lung using [3H]DHA as radioligand
ChEMBL 195 1 3 4 0.7 NCC1OCCc2c1ccc(O)c2O 10.1021/jm00073a006
CHEMBL542683 206593 3 None -48 4 Bovine 4.3 pKi = 4.3 Binding
Tested for binding affinity against beta-2 adrenergic receptor in bovine lung using [3H]DHA as radioligandTested for binding affinity against beta-2 adrenergic receptor in bovine lung using [3H]DHA as radioligand
ChEMBL 195 1 3 4 0.7 NCC1OCCc2c1ccc(O)c2O 10.1021/jm00073a006
CHEMBL99361 206593 3 None -48 4 Bovine 4.3 pKi = 4.3 Binding
Tested for binding affinity against beta-2 adrenergic receptor in bovine lung using [3H]DHA as radioligandTested for binding affinity against beta-2 adrenergic receptor in bovine lung using [3H]DHA as radioligand
ChEMBL 195 1 3 4 0.7 NCC1OCCc2c1ccc(O)c2O 10.1021/jm00073a006
9816183 100068 5 None 5 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptorDisplacement of [3H]CGP12177 from human beta2 adrenoceptor
ChEMBL 240 3 4 6 1.0 CNCC(O)c1ccc(O)c2nc(O)sc12 10.1016/j.bmcl.2010.06.136
CHEMBL29141 100068 5 None 5 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptorDisplacement of [3H]CGP12177 from human beta2 adrenoceptor
ChEMBL 240 3 4 6 1.0 CNCC(O)c1ccc(O)c2nc(O)sc12 10.1016/j.bmcl.2010.06.136
56943518 111956 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assayDisplacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assay
ChEMBL 488 12 6 7 3.6 NCCCOc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 10.1016/j.bmcl.2014.04.095
CHEMBL3298329 111956 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assayDisplacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assay
ChEMBL 488 12 6 7 3.6 NCCCOc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 10.1016/j.bmcl.2014.04.095
56943545 111957 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assayDisplacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assay
ChEMBL 502 13 6 7 4.0 NCCCCOc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 10.1016/j.bmcl.2014.04.095
CHEMBL3298330 111957 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assayDisplacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assay
ChEMBL 502 13 6 7 4.0 NCCCCOc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 10.1016/j.bmcl.2014.04.095
15461453 172232 0 None 4 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assay
ChEMBL 390 10 2 4 4.8 COc1ccccc1OCCNCCCOc1cccc2[nH]c3ccccc3c12 10.1021/acs.jmedchem.9b00349
CHEMBL4513932 172232 0 None 4 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assay
ChEMBL 390 10 2 4 4.8 COc1ccccc1OCCNCCCOc1cccc2[nH]c3ccccc3c12 10.1021/acs.jmedchem.9b00349
118710941 113239 0 None 5 3 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assay
ChEMBL 370 5 4 5 3.3 O=c1[nH]c2c(O)ccc([C@@H](O)CN[C@@H]3CCC[C@@H]3c3ccccc3)c2s1 10.1016/j.bmcl.2014.06.014
CHEMBL3323659 113239 0 None 5 3 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assay
ChEMBL 370 5 4 5 3.3 O=c1[nH]c2c(O)ccc([C@@H](O)CN[C@@H]3CCC[C@@H]3c3ccccc3)c2s1 10.1016/j.bmcl.2014.06.014
44393865 123569 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity for human beta-2 adrenergic receptorBinding affinity for human beta-2 adrenergic receptor
ChEMBL 434 13 4 5 3.8 O=CNc1cc([C@@H](O)CNCCc2ccc(OCCCc3ccccc3)cc2)ccc1O 10.1016/j.bmcl.2004.06.086
CHEMBL363329 123569 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity for human beta-2 adrenergic receptorBinding affinity for human beta-2 adrenergic receptor
ChEMBL 434 13 4 5 3.8 O=CNc1cc([C@@H](O)CNCCc2ccc(OCCCc3ccccc3)cc2)ccc1O 10.1016/j.bmcl.2004.06.086
46889729 6984 0 None 3 3 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cells
ChEMBL 434 9 1 5 3.2 C=CCc1ccccc1OCC(O)CN1CCC(CN2C(=O)c3ccccc3C2=O)CC1 10.1016/j.bmcl.2010.04.009
CHEMBL1085016 6984 0 None 3 3 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cells
ChEMBL 434 9 1 5 3.2 C=CCc1ccccc1OCC(O)CN1CCC(CN2C(=O)c3ccccc3C2=O)CC1 10.1016/j.bmcl.2010.04.009
10273469 93806 0 None -3 2 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]iodocyanopindolol from human adrenergic beta-2 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human adrenergic beta-2 receptor expressed in CHO cells
ChEMBL 417 9 2 6 4.6 O[C@@H](CNCCOc1ccc(-c2csc(-c3ccccc3)n2)cc1)c1cccnc1 10.1016/j.bmcl.2007.06.072
CHEMBL250144 93806 0 None -3 2 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]iodocyanopindolol from human adrenergic beta-2 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human adrenergic beta-2 receptor expressed in CHO cells
ChEMBL 417 9 2 6 4.6 O[C@@H](CNCCOc1ccc(-c2csc(-c3ccccc3)n2)cc1)c1cccnc1 10.1016/j.bmcl.2007.06.072
1960 2805 64 None -338 26 Dog 5.3 pKi = 5.3 Binding
Binding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranes
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm990599h
439260 2805 64 None -338 26 Dog 5.3 pKi = 5.3 Binding
Binding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranes
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm990599h
505 2805 64 None -338 26 Dog 5.3 pKi = 5.3 Binding
Binding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranes
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm990599h
CHEMBL1437 2805 64 None -338 26 Dog 5.3 pKi = 5.3 Binding
Binding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranes
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm990599h
DB00368 2805 64 None -338 26 Dog 5.3 pKi = 5.3 Binding
Binding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranes
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm990599h
681 1432 65 None -93 39 Dog 4.3 pKi = 4.3 Binding
Binding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranes
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm990599h
940 1432 65 None -93 39 Dog 4.3 pKi = 4.3 Binding
Binding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranes
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm990599h
947 1432 65 None -93 39 Dog 4.3 pKi = 4.3 Binding
Binding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranes
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm990599h
CHEMBL59 1432 65 None -93 39 Dog 4.3 pKi = 4.3 Binding
Binding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranes
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm990599h
DB00988 1432 65 None -93 39 Dog 4.3 pKi = 4.3 Binding
Binding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranes
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm990599h
541604 164776 10 None -72 4 Dog 4.3 pKi = 4.3 Binding
Binding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranes
ChEMBL 201 3 4 4 0.5 CNCC(O)c1cc(O)c(O)cc1F 10.1021/jm990599h
CHEMBL42359 164776 10 None -72 4 Dog 4.3 pKi = 4.3 Binding
Binding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranes
ChEMBL 201 3 4 4 0.5 CNCC(O)c1cc(O)c(O)cc1F 10.1021/jm990599h
44423641 84959 0 None 12 2 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]CYP from human adrenergic beta 2 receptor transfected in CHO cells in presence of 100 uM GTPDisplacement of [125I]CYP from human adrenergic beta 2 receptor transfected in CHO cells in presence of 100 uM GTP
ChEMBL 398 9 3 6 2.2 C[C@H](Cc1ccc(OCC(=O)O)cc1)NC[C@@H](O)c1cc(Br)no1 10.1016/j.bmc.2007.01.056
CHEMBL226293 84959 0 None 12 2 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]CYP from human adrenergic beta 2 receptor transfected in CHO cells in presence of 100 uM GTPDisplacement of [125I]CYP from human adrenergic beta 2 receptor transfected in CHO cells in presence of 100 uM GTP
ChEMBL 398 9 3 6 2.2 C[C@H](Cc1ccc(OCC(=O)O)cc1)NC[C@@H](O)c1cc(Br)no1 10.1016/j.bmc.2007.01.056
1499 2052 43 None -33 17 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cellsDisplacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cells
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2011.11.054
3779 2052 43 None -33 17 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cellsDisplacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cells
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2011.11.054
536 2052 43 None -33 17 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cellsDisplacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cells
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2011.11.054
CHEMBL434 2052 43 None -33 17 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cellsDisplacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cells
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2011.11.054
DB01064 2052 43 None -33 17 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cellsDisplacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cells
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2011.11.054
1499 2052 43 None -33 17 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cellsDisplacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cells
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2011.11.054
3779 2052 43 None -33 17 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cellsDisplacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cells
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2011.11.054
536 2052 43 None -33 17 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cellsDisplacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cells
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2011.11.054
CHEMBL434 2052 43 None -33 17 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cellsDisplacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cells
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2011.11.054
DB01064 2052 43 None -33 17 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cellsDisplacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cells
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2011.11.054
24865725 187491 0 None -1000 12 Human 6.3 pKi = 6.3 Binding
Displacement of radioligand from human cloned adrenergic beta2 receptorDisplacement of radioligand from human cloned adrenergic beta2 receptor
ChEMBL 453 8 1 5 4.2 Cc1ccc2c(OCCN3CCC(Cc4cccc(NS(C)(=O)=O)c4)CC3)cccc2n1 10.1021/jm8001444
CHEMBL497963 187491 0 None -1000 12 Human 6.3 pKi = 6.3 Binding
Displacement of radioligand from human cloned adrenergic beta2 receptorDisplacement of radioligand from human cloned adrenergic beta2 receptor
ChEMBL 453 8 1 5 4.2 Cc1ccc2c(OCCN3CCC(Cc4cccc(NS(C)(=O)=O)c4)CC3)cccc2n1 10.1021/jm8001444
145946710 166985 0 None 2 2 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-CGP12177 from human beta2 ADR expressed in HEK293T cell membrane after 90 mins by scintillation countingDisplacement of [3H]-CGP12177 from human beta2 ADR expressed in HEK293T cell membrane after 90 mins by scintillation counting
ChEMBL 316 7 3 5 0.7 CNCC(O)COc1ccc(S(=O)(=O)NC(C)(C)C)cc1 10.1021/acs.jmedchem.8b00625
CHEMBL4161638 166985 0 None 2 2 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-CGP12177 from human beta2 ADR expressed in HEK293T cell membrane after 90 mins by scintillation countingDisplacement of [3H]-CGP12177 from human beta2 ADR expressed in HEK293T cell membrane after 90 mins by scintillation counting
ChEMBL 316 7 3 5 0.7 CNCC(O)COc1ccc(S(=O)(=O)NC(C)(C)C)cc1 10.1021/acs.jmedchem.8b00625
CHEMBL4300393 166985 0 None 2 2 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-CGP12177 from human beta2 ADR expressed in HEK293T cell membrane after 90 mins by scintillation countingDisplacement of [3H]-CGP12177 from human beta2 ADR expressed in HEK293T cell membrane after 90 mins by scintillation counting
ChEMBL 316 7 3 5 0.7 CNCC(O)COc1ccc(S(=O)(=O)NC(C)(C)C)cc1 10.1021/acs.jmedchem.8b00625
155536080 171538 0 None -34 10 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-CGP12177 from human recombinant adrenergic Beta2 receptor expressed in Flp-In HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-CGP12177 from human recombinant adrenergic Beta2 receptor expressed in Flp-In HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 219 2 1 2 2.9 CC[C@H]1c2cc(OC)ccc2CC[C@@]1(C)N 10.1021/acsmedchemlett.9b00225
CHEMBL4472703 171538 0 None -34 10 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-CGP12177 from human recombinant adrenergic Beta2 receptor expressed in Flp-In HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-CGP12177 from human recombinant adrenergic Beta2 receptor expressed in Flp-In HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 219 2 1 2 2.9 CC[C@H]1c2cc(OC)ccc2CC[C@@]1(C)N 10.1021/acsmedchemlett.9b00225
44396532 66408 0 None -1 3 Human 7.3 pKi = 7.3 Binding
Binding inhibition constant was determined by inhibition of [125I]iodocyanopindolol binding to Beta-2 adrenergic receptorBinding inhibition constant was determined by inhibition of [125I]iodocyanopindolol binding to Beta-2 adrenergic receptor
ChEMBL 455 9 4 5 4.3 C[C@H](Cc1c[nH]c2ccccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2004.10.035
CHEMBL185836 66408 0 None -1 3 Human 7.3 pKi = 7.3 Binding
Binding inhibition constant was determined by inhibition of [125I]iodocyanopindolol binding to Beta-2 adrenergic receptorBinding inhibition constant was determined by inhibition of [125I]iodocyanopindolol binding to Beta-2 adrenergic receptor
ChEMBL 455 9 4 5 4.3 C[C@H](Cc1c[nH]c2ccccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2004.10.035
155512746 169094 0 None -19 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranesDisplacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranes
ChEMBL 568 22 3 10 3.9 COc1cc(CCNC[C@H](O)COc2ccc(COCCOC(C)C)cc2)ccc1OCCSSCCN 10.1016/j.bmc.2019.05.034
CHEMBL4437569 169094 0 None -19 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranesDisplacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranes
ChEMBL 568 22 3 10 3.9 COc1cc(CCNC[C@H](O)COc2ccc(COCCOC(C)C)cc2)ccc1OCCSSCCN 10.1016/j.bmc.2019.05.034
10140092 94056 0 None -9 3 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]iodocyanopindolol from human cloned adrenergic beta-2 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human cloned adrenergic beta-2 receptor expressed in CHO cells
ChEMBL 470 11 4 6 3.2 COc1ccc([C@@H](Cc2ccccc2)NC[C@@H](O)Cc2ccc(O)c(NS(C)(=O)=O)c2)cc1 10.1016/j.bmcl.2007.05.030
CHEMBL251581 94056 0 None -9 3 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]iodocyanopindolol from human cloned adrenergic beta-2 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human cloned adrenergic beta-2 receptor expressed in CHO cells
ChEMBL 470 11 4 6 3.2 COc1ccc([C@@H](Cc2ccccc2)NC[C@@H](O)Cc2ccc(O)c(NS(C)(=O)=O)c2)cc1 10.1016/j.bmcl.2007.05.030
42629372 63301 0 None 52 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]CGP-12177 from human beta2-adrenergic receptor expressed in HEK 293 cellsDisplacement of [3H]CGP-12177 from human beta2-adrenergic receptor expressed in HEK 293 cells
ChEMBL 337 6 4 4 3.5 C[C@@H](Cc1ccc2ccccc2c1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2009.11.062
CHEMBL1800962 63301 0 None 52 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]CGP-12177 from human beta2-adrenergic receptor expressed in HEK 293 cellsDisplacement of [3H]CGP-12177 from human beta2-adrenergic receptor expressed in HEK 293 cells
ChEMBL 337 6 4 4 3.5 C[C@@H](Cc1ccc2ccccc2c1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2009.11.062
105 3392 84 None -10 6 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]CGP1217 from human recombinant adrenergic beta2 receptor transfected in insect Sf9 cells by scintillation countingDisplacement of [3H]CGP1217 from human recombinant adrenergic beta2 receptor transfected in insect Sf9 cells by scintillation counting
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1021/jm801211c
2083 3392 84 None -10 6 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]CGP1217 from human recombinant adrenergic beta2 receptor transfected in insect Sf9 cells by scintillation countingDisplacement of [3H]CGP1217 from human recombinant adrenergic beta2 receptor transfected in insect Sf9 cells by scintillation counting
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1021/jm801211c
558 3392 84 None -10 6 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]CGP1217 from human recombinant adrenergic beta2 receptor transfected in insect Sf9 cells by scintillation countingDisplacement of [3H]CGP1217 from human recombinant adrenergic beta2 receptor transfected in insect Sf9 cells by scintillation counting
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1021/jm801211c
CHEMBL714 3392 84 None -10 6 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]CGP1217 from human recombinant adrenergic beta2 receptor transfected in insect Sf9 cells by scintillation countingDisplacement of [3H]CGP1217 from human recombinant adrenergic beta2 receptor transfected in insect Sf9 cells by scintillation counting
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1021/jm801211c
DB01001 3392 84 None -10 6 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]CGP1217 from human recombinant adrenergic beta2 receptor transfected in insect Sf9 cells by scintillation countingDisplacement of [3H]CGP1217 from human recombinant adrenergic beta2 receptor transfected in insect Sf9 cells by scintillation counting
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1021/jm801211c
155514341 169279 0 None 3 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H](-)CGP 12177 from human recombinant beta2 adrenoceptor after 120 mins by scintillation counting methodDisplacement of [3H](-)CGP 12177 from human recombinant beta2 adrenoceptor after 120 mins by scintillation counting method
ChEMBL 640 26 6 11 -0.3 C=CCc1ccccc1OCC(O)CNCCOCCOCCOCCOCCNC(=O)C1C(C(=O)O)C(C(=O)O)C1C(=O)O 10.1039/C8MD00412A
CHEMBL4440189 169279 0 None 3 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H](-)CGP 12177 from human recombinant beta2 adrenoceptor after 120 mins by scintillation counting methodDisplacement of [3H](-)CGP 12177 from human recombinant beta2 adrenoceptor after 120 mins by scintillation counting method
ChEMBL 640 26 6 11 -0.3 C=CCc1ccccc1OCC(O)CNCCOCCOCCOCCOCCNC(=O)C1C(C(=O)O)C(C(=O)O)C1C(=O)O 10.1039/C8MD00412A
9866061 77244 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity to human beta2-adrenoceptor by radioligand binding assayBinding affinity to human beta2-adrenoceptor by radioligand binding assay
ChEMBL 406 6 4 4 3.5 CCc1cc2c(cc1CC)CC(NCC(O)c1c(C)cc(O)c3[nH]c(=O)ccc13)C2 10.1016/j.bmcl.2012.07.096
CHEMBL2088195 77244 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity to human beta2-adrenoceptor by radioligand binding assayBinding affinity to human beta2-adrenoceptor by radioligand binding assay
ChEMBL 406 6 4 4 3.5 CCc1cc2c(cc1CC)CC(NCC(O)c1c(C)cc(O)c3[nH]c(=O)ccc13)C2 10.1016/j.bmcl.2012.07.096
24937387 17169 0 None 1 2 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 520 9 4 9 3.8 O=C(O)c1ccc(O)cc1OCC(O)CNC1CCN(c2ncnc3scc(-c4ccccc4)c23)CC1 10.1016/j.bmcl.2010.08.039
CHEMBL1257437 17169 0 None 1 2 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 520 9 4 9 3.8 O=C(O)c1ccc(O)cc1OCC(O)CNC1CCN(c2ncnc3scc(-c4ccccc4)c23)CC1 10.1016/j.bmcl.2010.08.039
21138 97986 34 None -1 7 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 259 6 2 3 2.6 CC(C)NC[C@@H](O)COc1cccc2ccccc12 nan
CHEMBL275742 97986 34 None -1 7 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 259 6 2 3 2.6 CC(C)NC[C@@H](O)COc1cccc2ccccc12 nan
10379016 16300 2 None -3 3 Guinea pig 6.3 pKi = 6.3 Binding
Binding affinity against Beta-2 adrenergic receptor was measured using [125I]CYP as radioligandBinding affinity against Beta-2 adrenergic receptor was measured using [125I]CYP as radioligand
ChEMBL 281 1 1 5 0.9 Brc1cnc(N2CCNCC2)c2nccn12 10.1021/jm00099a012
CHEMBL123566 16300 2 None -3 3 Guinea pig 6.3 pKi = 6.3 Binding
Binding affinity against Beta-2 adrenergic receptor was measured using [125I]CYP as radioligandBinding affinity against Beta-2 adrenergic receptor was measured using [125I]CYP as radioligand
ChEMBL 281 1 1 5 0.9 Brc1cnc(N2CCNCC2)c2nccn12 10.1021/jm00099a012
145974110 163912 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-DHA from Nb80-fused beta2 adrenergic receptor (unknown origin) expressed in Sf9 cell membranes after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-DHA from Nb80-fused beta2 adrenergic receptor (unknown origin) expressed in Sf9 cell membranes after 2 hrs by microbeta scintillation counting method
ChEMBL 356 8 1 3 4.6 COc1ccc2c(c1)c(CCNCCCc1ccc(Cl)cc1)cn2C 10.1021/acs.jmedchem.7b01558
CHEMBL4214185 163912 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-DHA from Nb80-fused beta2 adrenergic receptor (unknown origin) expressed in Sf9 cell membranes after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-DHA from Nb80-fused beta2 adrenergic receptor (unknown origin) expressed in Sf9 cell membranes after 2 hrs by microbeta scintillation counting method
ChEMBL 356 8 1 3 4.6 COc1ccc2c(c1)c(CCNCCCc1ccc(Cl)cc1)cn2C 10.1021/acs.jmedchem.7b01558
155541417 172449 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assay
ChEMBL 333 9 4 6 1.7 COc1ccccc1OCCNC[C@H](O)Cc1ccc(O)c(O)c1 10.1021/acs.jmedchem.9b00349
CHEMBL4518727 172449 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assay
ChEMBL 333 9 4 6 1.7 COc1ccccc1OCCNC[C@H](O)Cc1ccc(O)c(O)c1 10.1021/acs.jmedchem.9b00349
46221396 8455 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]cyanopindolol from human recombinant beta2 adrenergic receptor expressed in CHO cells by filtration assayDisplacement of [125I]cyanopindolol from human recombinant beta2 adrenergic receptor expressed in CHO cells by filtration assay
ChEMBL 364 4 4 4 2.6 Cc1cc2c(cc1C)CC(NC[C@H](O)c1ccc(O)c3[nH]c(=O)ccc13)C2 10.1021/jm100068m
CHEMBL1094483 8455 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]cyanopindolol from human recombinant beta2 adrenergic receptor expressed in CHO cells by filtration assayDisplacement of [125I]cyanopindolol from human recombinant beta2 adrenergic receptor expressed in CHO cells by filtration assay
ChEMBL 364 4 4 4 2.6 Cc1cc2c(cc1C)CC(NC[C@H](O)c1ccc(O)c3[nH]c(=O)ccc13)C2 10.1021/jm100068m
145978746 163133 0 None - 1 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]-DHA from Nb80-fused beta2 adrenergic receptor (unknown origin) expressed in Sf9 cell membranes after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-DHA from Nb80-fused beta2 adrenergic receptor (unknown origin) expressed in Sf9 cell membranes after 2 hrs by microbeta scintillation counting method
ChEMBL 300 5 1 3 4.2 CC(CC(F)(F)F)NCc1ccc(-c2nccs2)cc1 10.1021/acs.jmedchem.7b01558
CHEMBL4204907 163133 0 None - 1 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]-DHA from Nb80-fused beta2 adrenergic receptor (unknown origin) expressed in Sf9 cell membranes after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-DHA from Nb80-fused beta2 adrenergic receptor (unknown origin) expressed in Sf9 cell membranes after 2 hrs by microbeta scintillation counting method
ChEMBL 300 5 1 3 4.2 CC(CC(F)(F)F)NCc1ccc(-c2nccs2)cc1 10.1021/acs.jmedchem.7b01558
16735261 85292 0 None 47 2 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 317 7 4 5 2.4 COc1ccc(C[C@@H](C)NC[C@@H](O)c2cc(O)cc(O)c2)cc1 10.1021/jm070030d
CHEMBL228998 85292 0 None 47 2 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 317 7 4 5 2.4 COc1ccc(C[C@@H](C)NC[C@@H](O)c2cc(O)cc(O)c2)cc1 10.1021/jm070030d
123133222 159488 0 None 6 2 Human 5.3 pKi = 5.3 Binding
Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.
ChEMBL 317 7 4 5 2.4 COc1cccc(C[C@@H](C)NC[C@@H](O)c2cc(O)cc(O)c2)c1 nan
CHEMBL4108239 159488 0 None 6 2 Human 5.3 pKi = 5.3 Binding
Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.
ChEMBL 317 7 4 5 2.4 COc1cccc(C[C@@H](C)NC[C@@H](O)c2cc(O)cc(O)c2)c1 nan
16735261 85292 0 None 47 2 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 317 7 4 5 2.4 COc1ccc(C[C@@H](C)NC[C@@H](O)c2cc(O)cc(O)c2)cc1 10.1021/jm070030d
CHEMBL228998 85292 0 None 47 2 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 317 7 4 5 2.4 COc1ccc(C[C@@H](C)NC[C@@H](O)c2cc(O)cc(O)c2)cc1 10.1021/jm070030d
127046952 139558 0 None -4 6 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cellsDisplacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells
ChEMBL 421 12 3 5 4.5 COc1cc(CCNCCc2ccc(O)c(O)c2)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
CHEMBL3800636 139558 0 None -4 6 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cellsDisplacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells
ChEMBL 421 12 3 5 4.5 COc1cc(CCNCCc2ccc(O)c(O)c2)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
44361630 35028 0 None - 1 Dog 5.3 pKi = 5.3 Binding
Beta-2 adrenergic receptor binding affinity by measuring the displacement of [3H]DHA binding in rat lungBeta-2 adrenergic receptor binding affinity by measuring the displacement of [3H]DHA binding in rat lung
ChEMBL 417 6 2 6 2.4 O=C1CSc2ccc(OCC(O)CN3CCN(c4ccc(F)cc4)CC3)cc2N1 10.1016/s0960-894x(00)00016-0
CHEMBL143608 35028 0 None - 1 Dog 5.3 pKi = 5.3 Binding
Beta-2 adrenergic receptor binding affinity by measuring the displacement of [3H]DHA binding in rat lungBeta-2 adrenergic receptor binding affinity by measuring the displacement of [3H]DHA binding in rat lung
ChEMBL 417 6 2 6 2.4 O=C1CSc2ccc(OCC(O)CN3CCN(c4ccc(F)cc4)CC3)cc2N1 10.1016/s0960-894x(00)00016-0
44310958 202992 0 None - 1 Mouse 4.3 pKi = 4.3 Binding
Ki value was determined by accumulation of c-AMP in S-49 mouse lymphoma cells (Beta2).Ki value was determined by accumulation of c-AMP in S-49 mouse lymphoma cells (Beta2).
ChEMBL 441 13 4 5 3.9 CC(=O)Nc1ccc(OC[C@H](O)CN[C@H](C)CCCCC(=O)Nc2ccc(C)cc2)cc1 10.1021/jm00163a036
CHEMBL74122 202992 0 None - 1 Mouse 4.3 pKi = 4.3 Binding
Ki value was determined by accumulation of c-AMP in S-49 mouse lymphoma cells (Beta2).Ki value was determined by accumulation of c-AMP in S-49 mouse lymphoma cells (Beta2).
ChEMBL 441 13 4 5 3.9 CC(=O)Nc1ccc(OC[C@H](O)CN[C@H](C)CCCCC(=O)Nc2ccc(C)cc2)cc1 10.1021/jm00163a036
155545397 172802 0 None 5 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H](-)CGP 12177 from human recombinant beta2 adrenoceptor after 120 mins by scintillation counting methodDisplacement of [3H](-)CGP 12177 from human recombinant beta2 adrenoceptor after 120 mins by scintillation counting method
ChEMBL 1266 41 6 18 5.4 C=CCc1ccccc1OCC(O)CNCCOCCOCCOCCOCCNC(=O)CCCCCC1(C)C(/C=C/C=C/C=C2/N(CCCS(=O)(=O)O)c3ccc(S(=O)(=O)O)cc3C2(C)C)=[N+](CCCS(=O)(=O)[O-])c2ccc(S(=O)(=O)O)cc21 10.1039/C8MD00412A
CHEMBL4527905 172802 0 None 5 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H](-)CGP 12177 from human recombinant beta2 adrenoceptor after 120 mins by scintillation counting methodDisplacement of [3H](-)CGP 12177 from human recombinant beta2 adrenoceptor after 120 mins by scintillation counting method
ChEMBL 1266 41 6 18 5.4 C=CCc1ccccc1OCC(O)CNCCOCCOCCOCCOCCNC(=O)CCCCCC1(C)C(/C=C/C=C/C=C2/N(CCCS(=O)(=O)O)c3ccc(S(=O)(=O)O)cc3C2(C)C)=[N+](CCCS(=O)(=O)[O-])c2ccc(S(=O)(=O)O)cc21 10.1039/C8MD00412A
24886595 17449 0 None 1 3 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 478 8 2 7 4.5 OC(CNC1CCN(c2ncnc3scc(-c4ccccc4)c23)CC1)COc1ccc(F)cc1 10.1016/j.bmcl.2010.08.039
CHEMBL1258370 17449 0 None 1 3 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 478 8 2 7 4.5 OC(CNC1CCN(c2ncnc3scc(-c4ccccc4)c23)CC1)COc1ccc(F)cc1 10.1016/j.bmcl.2010.08.039
594115 19164 2 None -3 2 Rat 5.3 pKi = 5.3 Binding
Binding affinity against adrenergic beta 2 receptor versus 1 nM [3H]dihydroalprenolol in rat cerebral cerebellar membranesBinding affinity against adrenergic beta 2 receptor versus 1 nM [3H]dihydroalprenolol in rat cerebral cerebellar membranes
ChEMBL 187 2 4 4 0.2 NCC(O)c1cc(O)c(O)c(F)c1 10.1021/jm00076a024
CHEMBL129190 19164 2 None -3 2 Rat 5.3 pKi = 5.3 Binding
Binding affinity against adrenergic beta 2 receptor versus 1 nM [3H]dihydroalprenolol in rat cerebral cerebellar membranesBinding affinity against adrenergic beta 2 receptor versus 1 nM [3H]dihydroalprenolol in rat cerebral cerebellar membranes
ChEMBL 187 2 4 4 0.2 NCC(O)c1cc(O)c(O)c(F)c1 10.1021/jm00076a024
105 3392 84 None -10 6 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O nan
2083 3392 84 None -10 6 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O nan
558 3392 84 None -10 6 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O nan
CHEMBL714 3392 84 None -10 6 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O nan
DB01001 3392 84 None -10 6 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O nan
4806 3933 85 None -8 13 Human 6.3 pKi = 6.3 Binding
Binding affinity to human beta 2 adrenergic receptorBinding affinity to human beta 2 adrenergic receptor
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
7351 3933 85 None -8 13 Human 6.3 pKi = 6.3 Binding
Binding affinity to human beta 2 adrenergic receptorBinding affinity to human beta 2 adrenergic receptor
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
9966051 3933 85 None -8 13 Human 6.3 pKi = 6.3 Binding
Binding affinity to human beta 2 adrenergic receptorBinding affinity to human beta 2 adrenergic receptor
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
CHEMBL2104993 3933 85 None -8 13 Human 6.3 pKi = 6.3 Binding
Binding affinity to human beta 2 adrenergic receptorBinding affinity to human beta 2 adrenergic receptor
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
DB09068 3933 85 None -8 13 Human 6.3 pKi = 6.3 Binding
Binding affinity to human beta 2 adrenergic receptorBinding affinity to human beta 2 adrenergic receptor
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
9990035 11901 0 None -4 2 Bovine 5.3 pKi = 5.3 Binding
Binding affinity against beta-2-adrenergic receptor in bovine lungBinding affinity against beta-2-adrenergic receptor in bovine lung
ChEMBL 188 7 2 4 0.8 CCCO/N=C/C(O)CNC(C)C 10.1021/jm00036a018
CHEMBL1183337 11901 0 None -4 2 Bovine 5.3 pKi = 5.3 Binding
Binding affinity against beta-2-adrenergic receptor in bovine lungBinding affinity against beta-2-adrenergic receptor in bovine lung
ChEMBL 188 7 2 4 0.8 CCCO/N=C/C(O)CNC(C)C 10.1021/jm00036a018
CHEMBL291115 11901 0 None -4 2 Bovine 5.3 pKi = 5.3 Binding
Binding affinity against beta-2-adrenergic receptor in bovine lungBinding affinity against beta-2-adrenergic receptor in bovine lung
ChEMBL 188 7 2 4 0.8 CCCO/N=C/C(O)CNC(C)C 10.1021/jm00036a018
123600 2275 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cellsDisplacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cells
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)[C@H](CNC(C)(C)C)O 10.1016/j.bmc.2011.11.054
1575 2275 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cellsDisplacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cells
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)[C@H](CNC(C)(C)C)O 10.1016/j.bmc.2011.11.054
9816 2275 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cellsDisplacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cells
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)[C@H](CNC(C)(C)C)O 10.1016/j.bmc.2011.11.054
CHEMBL1002 2275 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cellsDisplacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cells
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)[C@H](CNC(C)(C)C)O 10.1016/j.bmc.2011.11.054
DB13139 2275 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cellsDisplacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cells
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)[C@H](CNC(C)(C)C)O 10.1016/j.bmc.2011.11.054
123600 2275 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cellsDisplacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cells
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)[C@H](CNC(C)(C)C)O 10.1016/j.bmc.2011.11.054
1575 2275 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cellsDisplacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cells
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)[C@H](CNC(C)(C)C)O 10.1016/j.bmc.2011.11.054
9816 2275 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cellsDisplacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cells
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)[C@H](CNC(C)(C)C)O 10.1016/j.bmc.2011.11.054
CHEMBL1002 2275 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cellsDisplacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cells
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)[C@H](CNC(C)(C)C)O 10.1016/j.bmc.2011.11.054
DB13139 2275 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cellsDisplacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cells
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)[C@H](CNC(C)(C)C)O 10.1016/j.bmc.2011.11.054
44424581 142791 0 None -1 2 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 253 7 4 4 2.3 CCCC[C@H](C)NC[C@@H](O)c1cc(O)cc(O)c1 10.1021/jm070030d
CHEMBL389734 142791 0 None -1 2 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 253 7 4 4 2.3 CCCC[C@H](C)NC[C@@H](O)c1cc(O)cc(O)c1 10.1021/jm070030d
16735276 145437 0 None -1 2 Human 4.3 pKi = 4.3 Binding
Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.
ChEMBL 267 8 4 4 2.7 CCCCC[C@H](C)NC[C@@H](O)c1cc(O)cc(O)c1 nan
CHEMBL3918348 145437 0 None -1 2 Human 4.3 pKi = 4.3 Binding
Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.
ChEMBL 267 8 4 4 2.7 CCCCC[C@H](C)NC[C@@H](O)c1cc(O)cc(O)c1 nan
44424581 142791 0 None -1 2 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 253 7 4 4 2.3 CCCC[C@H](C)NC[C@@H](O)c1cc(O)cc(O)c1 10.1021/jm070030d
CHEMBL389734 142791 0 None -1 2 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 253 7 4 4 2.3 CCCC[C@H](C)NC[C@@H](O)c1cc(O)cc(O)c1 10.1021/jm070030d
46889809 6554 0 None 1 3 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cells
ChEMBL 519 6 2 5 5.0 O=C1c2cccc3cccc(c23)C(=O)N1C1CCN(CC(O)COc2cccc3[nH]c4ccccc4c23)CC1 10.1016/j.bmcl.2010.04.009
CHEMBL1083363 6554 0 None 1 3 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cells
ChEMBL 519 6 2 5 5.0 O=C1c2cccc3cccc(c23)C(=O)N1C1CCN(CC(O)COc2cccc3[nH]c4ccccc4c23)CC1 10.1016/j.bmcl.2010.04.009
44444191 171857 0 None -8 3 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]iodocyanopindolol from human cloned adrenergic beta-2 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human cloned adrenergic beta-2 receptor expressed in CHO cells
ChEMBL 548 13 4 7 4.3 COc1ccc([C@H](CCc2ccccc2Cl)NC[C@H](O)Cc2ccc(O)c(NS(C)(=O)=O)c2)cc1OC 10.1016/j.bmcl.2007.05.030
CHEMBL447786 171857 0 None -8 3 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]iodocyanopindolol from human cloned adrenergic beta-2 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human cloned adrenergic beta-2 receptor expressed in CHO cells
ChEMBL 548 13 4 7 4.3 COc1ccc([C@H](CCc2ccccc2Cl)NC[C@H](O)Cc2ccc(O)c(NS(C)(=O)=O)c2)cc1OC 10.1016/j.bmcl.2007.05.030
155555687 173866 0 None -2 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranesDisplacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranes
ChEMBL 510 19 3 9 3.2 COCCc1ccc(OC[C@@H](O)CNCCc2ccc(OCCSSCCN)c(OC)c2)cc1 10.1016/j.bmc.2019.05.034
CHEMBL4553747 173866 0 None -2 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranesDisplacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranes
ChEMBL 510 19 3 9 3.2 COCCc1ccc(OC[C@@H](O)CNCCc2ccc(OCCSSCCN)c(OC)c2)cc1 10.1016/j.bmc.2019.05.034
5190 106409 31 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]DHA from human beta2 adrenoceptor by liquid scintillation counterDisplacement of [3H]DHA from human beta2 adrenoceptor by liquid scintillation counter
ChEMBL 466 8 2 5 4.2 N#Cc1cc2c(OCC(O)CN3CCN(C(c4ccccc4)c4ccccc4)CC3)cccc2[nH]1 10.1016/j.bmcl.2008.09.046
CHEMBL314639 106409 31 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]DHA from human beta2 adrenoceptor by liquid scintillation counterDisplacement of [3H]DHA from human beta2 adrenoceptor by liquid scintillation counter
ChEMBL 466 8 2 5 4.2 N#Cc1cc2c(OCC(O)CN3CCN(C(c4ccccc4)c4ccccc4)CC3)cccc2[nH]1 10.1016/j.bmcl.2008.09.046
128658 33738 7 None -3 5 Guinea pig 7.2 pKi = 7.2 Binding
Binding affinity against beta-2 adrenergic receptor in guinea pig lung membranesBinding affinity against beta-2 adrenergic receptor in guinea pig lung membranes
ChEMBL 363 5 3 6 2.7 COc1cc(CC2NCCc3cc(O)c(O)c(F)c32)cc(OC)c1OC 10.1021/jm00081a007
CHEMBL142428 33738 7 None -3 5 Guinea pig 7.2 pKi = 7.2 Binding
Binding affinity against beta-2 adrenergic receptor in guinea pig lung membranesBinding affinity against beta-2 adrenergic receptor in guinea pig lung membranes
ChEMBL 363 5 3 6 2.7 COc1cc(CC2NCCc3cc(O)c(O)c(F)c32)cc(OC)c1OC 10.1021/jm00081a007
12582 935 40 None -11 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]CGP1217 from human recombinant adrenergic beta2 receptor transfected in insect Sf9 cells by scintillation countingDisplacement of [3H]CGP1217 from human recombinant adrenergic beta2 receptor transfected in insect Sf9 cells by scintillation counting
ChEMBL 276 3 3 3 3.0 CC(C)(C)NCC(C1=CC(=C(C(=C1)Cl)N)Cl)O 10.1021/jm801211c
2783 935 40 None -11 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]CGP1217 from human recombinant adrenergic beta2 receptor transfected in insect Sf9 cells by scintillation countingDisplacement of [3H]CGP1217 from human recombinant adrenergic beta2 receptor transfected in insect Sf9 cells by scintillation counting
ChEMBL 276 3 3 3 3.0 CC(C)(C)NCC(C1=CC(=C(C(=C1)Cl)N)Cl)O 10.1021/jm801211c
CHEMBL49080 935 40 None -11 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]CGP1217 from human recombinant adrenergic beta2 receptor transfected in insect Sf9 cells by scintillation countingDisplacement of [3H]CGP1217 from human recombinant adrenergic beta2 receptor transfected in insect Sf9 cells by scintillation counting
ChEMBL 276 3 3 3 3.0 CC(C)(C)NCC(C1=CC(=C(C(=C1)Cl)N)Cl)O 10.1021/jm801211c
DB01407 935 40 None -11 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]CGP1217 from human recombinant adrenergic beta2 receptor transfected in insect Sf9 cells by scintillation countingDisplacement of [3H]CGP1217 from human recombinant adrenergic beta2 receptor transfected in insect Sf9 cells by scintillation counting
ChEMBL 276 3 3 3 3.0 CC(C)(C)NCC(C1=CC(=C(C(=C1)Cl)N)Cl)O 10.1021/jm801211c
155519891 169814 0 None -2 6 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-CGP12177 from human recombinant adrenergic Beta2 receptor expressed in Flp-In HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-CGP12177 from human recombinant adrenergic Beta2 receptor expressed in Flp-In HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 249 2 1 4 1.9 COc1cc(OC)c2c(c1)OC[C@@]1(C)NCC[C@@H]21 10.1021/acsmedchemlett.9b00225
CHEMBL4447975 169814 0 None -2 6 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-CGP12177 from human recombinant adrenergic Beta2 receptor expressed in Flp-In HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-CGP12177 from human recombinant adrenergic Beta2 receptor expressed in Flp-In HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 249 2 1 4 1.9 COc1cc(OC)c2c(c1)OC[C@@]1(C)NCC[C@@H]21 10.1021/acsmedchemlett.9b00225
56663519 63299 0 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]CGP-12177 from human beta2-adrenergic receptor expressed in HEK 293 cellsDisplacement of [3H]CGP-12177 from human beta2-adrenergic receptor expressed in HEK 293 cells
ChEMBL 317 7 5 5 2.4 CC[C@@H](Cc1ccc(O)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2009.11.062
CHEMBL1800960 63299 0 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]CGP-12177 from human beta2-adrenergic receptor expressed in HEK 293 cellsDisplacement of [3H]CGP-12177 from human beta2-adrenergic receptor expressed in HEK 293 cells
ChEMBL 317 7 5 5 2.4 CC[C@@H](Cc1ccc(O)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2009.11.062
9992825 83937 16 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]CGP1217 from human recombinant adrenergic beta2 receptor transfected in insect Sf9 cells by scintillation countingDisplacement of [3H]CGP1217 from human recombinant adrenergic beta2 receptor transfected in insect Sf9 cells by scintillation counting
ChEMBL 261 2 3 4 1.1 CC(C)NC1CCn2c(=O)[nH]c3cccc(c32)C1O 10.1021/jm801211c
CHEMBL2218907 83937 16 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]CGP1217 from human recombinant adrenergic beta2 receptor transfected in insect Sf9 cells by scintillation countingDisplacement of [3H]CGP1217 from human recombinant adrenergic beta2 receptor transfected in insect Sf9 cells by scintillation counting
ChEMBL 261 2 3 4 1.1 CC(C)NC1CCn2c(=O)[nH]c3cccc(c32)C1O 10.1021/jm801211c
1862 161 14 None -57 7 Dog 4.2 pKi = 4.2 Binding
Binding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranes
ChEMBL 187 2 4 4 0.2 NCC(c1cc(O)c(cc1F)O)O 10.1021/jm990599h
510 161 14 None -57 7 Dog 4.2 pKi = 4.2 Binding
Binding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranes
ChEMBL 187 2 4 4 0.2 NCC(c1cc(O)c(cc1F)O)O 10.1021/jm990599h
CHEMBL281232 161 14 None -57 7 Dog 4.2 pKi = 4.2 Binding
Binding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranes
ChEMBL 187 2 4 4 0.2 NCC(c1cc(O)c(cc1F)O)O 10.1021/jm990599h
52948728 17250 0 None 2 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 400 7 3 8 2.4 Oc1ccc(OCC(O)CNC2CCN(c3ncnc4sccc34)CC2)cc1 10.1016/j.bmcl.2010.08.039
CHEMBL1257674 17250 0 None 2 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 400 7 3 8 2.4 Oc1ccc(OCC(O)CNC2CCN(c3ncnc4sccc34)CC2)cc1 10.1016/j.bmcl.2010.08.039
146025727 171109 0 None -218 27 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-CGP12177 from recombinant human beta2 adrenergic receptor expressed in HEK Flp-In cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-CGP12177 from recombinant human beta2 adrenergic receptor expressed in HEK Flp-In cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 411 3 0 5 6.4 FC(F)(F)c1cc(Oc2nccc3ccsc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4466483 171109 0 None -218 27 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-CGP12177 from recombinant human beta2 adrenergic receptor expressed in HEK Flp-In cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-CGP12177 from recombinant human beta2 adrenergic receptor expressed in HEK Flp-In cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 411 3 0 5 6.4 FC(F)(F)c1cc(Oc2nccc3ccsc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
24936881 17320 0 None 1 3 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 476 8 3 8 4.1 Oc1cccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)c1 10.1016/j.bmcl.2010.08.039
CHEMBL1257913 17320 0 None 1 3 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 476 8 3 8 4.1 Oc1cccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)c1 10.1016/j.bmcl.2010.08.039
52943919 17524 0 None 14 3 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 500 10 2 7 5.1 C=CCc1ccccc1OCC(O)CNC1CCN(c2ncnc3scc(-c4ccccc4)c23)CC1 10.1016/j.bmcl.2010.08.039
CHEMBL1258597 17524 0 None 14 3 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 500 10 2 7 5.1 C=CCc1ccccc1OCC(O)CNC1CCN(c2ncnc3scc(-c4ccccc4)c23)CC1 10.1016/j.bmcl.2010.08.039
11647002 15447 0 None 22 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptorDisplacement of [3H]CGP12177 from human beta2 adrenoceptor
ChEMBL 400 7 4 6 3.1 O=c1[nH]c2c(O)ccc([C@@H](O)CN[C@H]3CCC[C@@H]3OCc3ccccc3)c2s1 10.1016/j.bmcl.2010.06.136
CHEMBL1221681 15447 0 None 22 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptorDisplacement of [3H]CGP12177 from human beta2 adrenoceptor
ChEMBL 400 7 4 6 3.1 O=c1[nH]c2c(O)ccc([C@@H](O)CN[C@H]3CCC[C@@H]3OCc3ccccc3)c2s1 10.1016/j.bmcl.2010.06.136
49864440 15457 0 None 29 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptorDisplacement of [3H]CGP12177 from human beta2 adrenoceptor
ChEMBL 434 7 4 7 2.3 O=c1[nH]c2c(O)ccc([C@@H](O)CNC3CCN(CCN4CCCCCC4)CC3)c2s1 10.1016/j.bmcl.2010.06.136
CHEMBL1221802 15457 0 None 29 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptorDisplacement of [3H]CGP12177 from human beta2 adrenoceptor
ChEMBL 434 7 4 7 2.3 O=c1[nH]c2c(O)ccc([C@@H](O)CNC3CCN(CCN4CCCCCC4)CC3)c2s1 10.1016/j.bmcl.2010.06.136
127046949 139366 0 None 2 6 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cellsDisplacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells
ChEMBL 472 12 3 5 4.6 COc1cc(CCNCCc2ccc(O)c3[nH]c(=O)ccc23)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
CHEMBL3799455 139366 0 None 2 6 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cellsDisplacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells
ChEMBL 472 12 3 5 4.6 COc1cc(CCNCCc2ccc(O)c3[nH]c(=O)ccc23)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
9871386 111766 4 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assayDisplacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assay
ChEMBL 521 10 5 6 5.5 COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1-c1ccccc1 10.1016/j.bmcl.2014.04.095
CHEMBL3290999 111766 4 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assayDisplacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assay
ChEMBL 521 10 5 6 5.5 COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1-c1ccccc1 10.1016/j.bmcl.2014.04.095
66796015 111955 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assayDisplacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assay
ChEMBL 474 11 6 7 3.2 NCCOc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 10.1016/j.bmcl.2014.04.095
CHEMBL3298328 111955 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assayDisplacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assay
ChEMBL 474 11 6 7 3.2 NCCOc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 10.1016/j.bmcl.2014.04.095
56943546 111973 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assayDisplacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assay
ChEMBL 518 14 6 8 3.2 NCCOCCOc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 10.1016/j.bmcl.2014.04.095
CHEMBL3298691 111973 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assayDisplacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assay
ChEMBL 518 14 6 8 3.2 NCCOCCOc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 10.1016/j.bmcl.2014.04.095
11169365 112007 0 None 99 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assayDisplacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assay
ChEMBL 502 11 6 7 4.0 CC(C)(N)COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 10.1016/j.bmcl.2014.04.095
CHEMBL3298986 112007 0 None 99 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assayDisplacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assay
ChEMBL 502 11 6 7 4.0 CC(C)(N)COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 10.1016/j.bmcl.2014.04.095
10548754 16191 0 None 154 2 Human 8.2 pKi = 8.2 Binding
Binding affinity for human Beta-2 adrenergic receptor expressed in CHO cells by radioligand competition binding assays using [125I]iodocyanopindolol (ICYP)Binding affinity for human Beta-2 adrenergic receptor expressed in CHO cells by radioligand competition binding assays using [125I]iodocyanopindolol (ICYP)
ChEMBL 396 2 4 4 2.7 Nc1ccc(CC2NCCc3cc(O)c(O)cc32)cc1I 10.1021/jm960208o
CHEMBL122990 16191 0 None 154 2 Human 8.2 pKi = 8.2 Binding
Binding affinity for human Beta-2 adrenergic receptor expressed in CHO cells by radioligand competition binding assays using [125I]iodocyanopindolol (ICYP)Binding affinity for human Beta-2 adrenergic receptor expressed in CHO cells by radioligand competition binding assays using [125I]iodocyanopindolol (ICYP)
ChEMBL 396 2 4 4 2.7 Nc1ccc(CC2NCCc3cc(O)c(O)cc32)cc1I 10.1021/jm960208o
44433250 88634 0 None -1 3 Human 8.2 pKi = 8.2 Binding
Binding affinity at human adrenergic beta2 receptorBinding affinity at human adrenergic beta2 receptor
ChEMBL 340 6 3 3 3.5 O[C@@H](CNC12CC3CC(CC(C3)C1)C2)COc1cccc2[nH]ccc12 10.1016/j.bmcl.2007.07.086
CHEMBL236514 88634 0 None -1 3 Human 8.2 pKi = 8.2 Binding
Binding affinity at human adrenergic beta2 receptorBinding affinity at human adrenergic beta2 receptor
ChEMBL 340 6 3 3 3.5 O[C@@H](CNC12CC3CC(CC(C3)C1)C2)COc1cccc2[nH]ccc12 10.1016/j.bmcl.2007.07.086
118710935 113233 0 None 9 3 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assay
ChEMBL 362 5 4 5 3.3 O=c1[nH]c2c(O)ccc([C@@H](O)CN[C@H]3CCC[C@H]3C3CCCC3)c2s1 10.1016/j.bmcl.2014.06.014
CHEMBL3323653 113233 0 None 9 3 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assay
ChEMBL 362 5 4 5 3.3 O=c1[nH]c2c(O)ccc([C@@H](O)CN[C@H]3CCC[C@H]3C3CCCC3)c2s1 10.1016/j.bmcl.2014.06.014
118710947 113247 0 None -1 3 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assay
ChEMBL 386 8 4 5 3.4 CC(C)Cc1ccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)cc1 10.1016/j.bmcl.2014.06.014
CHEMBL3323667 113247 0 None -1 3 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assay
ChEMBL 386 8 4 5 3.4 CC(C)Cc1ccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)cc1 10.1016/j.bmcl.2014.06.014
53319788 58219 0 None -1 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-dihydroalprenolol from human beta2-adrenoceptor expressed in HEK cells after 4 hrsDisplacement of [3H]-dihydroalprenolol from human beta2-adrenoceptor expressed in HEK cells after 4 hrs
ChEMBL 624 17 5 6 5.4 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(CCCCCCCCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)C1 10.1016/j.bmcl.2011.01.043
CHEMBL1683939 58219 0 None -1 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-dihydroalprenolol from human beta2-adrenoceptor expressed in HEK cells after 4 hrsDisplacement of [3H]-dihydroalprenolol from human beta2-adrenoceptor expressed in HEK cells after 4 hrs
ChEMBL 624 17 5 6 5.4 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(CCCCCCCCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)C1 10.1016/j.bmcl.2011.01.043
10324985 76413 7 None -44 17 Human 7.2 pKi = 7.2 Binding
Binding affinity to adrenergic beta-2 receptorBinding affinity to adrenergic beta-2 receptor
ChEMBL 423 7 0 8 1.7 COc1ccc2cccc(N3CCN(CCCCn4ncc(=O)n(C)c4=O)CC3)c2c1 10.1021/jm050725j
CHEMBL199824 76413 7 None -44 17 Human 7.2 pKi = 7.2 Binding
Binding affinity to adrenergic beta-2 receptorBinding affinity to adrenergic beta-2 receptor
ChEMBL 423 7 0 8 1.7 COc1ccc2cccc(N3CCN(CCCCn4ncc(=O)n(C)c4=O)CC3)c2c1 10.1021/jm050725j
CHEMBL2068762 76413 7 None -44 17 Human 7.2 pKi = 7.2 Binding
Binding affinity to adrenergic beta-2 receptorBinding affinity to adrenergic beta-2 receptor
ChEMBL 423 7 0 8 1.7 COc1ccc2cccc(N3CCN(CCCCn4ncc(=O)n(C)c4=O)CC3)c2c1 10.1021/jm050725j
1960 2805 64 None -36 26 Bovine 5.2 pKi = 5.2 Binding
Compound was evaluated for beta adrenergic binding affinity towards beta-2 receptor of bovine lungCompound was evaluated for beta adrenergic binding affinity towards beta-2 receptor of bovine lung
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00084a006
439260 2805 64 None -36 26 Bovine 5.2 pKi = 5.2 Binding
Compound was evaluated for beta adrenergic binding affinity towards beta-2 receptor of bovine lungCompound was evaluated for beta adrenergic binding affinity towards beta-2 receptor of bovine lung
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00084a006
505 2805 64 None -36 26 Bovine 5.2 pKi = 5.2 Binding
Compound was evaluated for beta adrenergic binding affinity towards beta-2 receptor of bovine lungCompound was evaluated for beta adrenergic binding affinity towards beta-2 receptor of bovine lung
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00084a006
CHEMBL1437 2805 64 None -36 26 Bovine 5.2 pKi = 5.2 Binding
Compound was evaluated for beta adrenergic binding affinity towards beta-2 receptor of bovine lungCompound was evaluated for beta adrenergic binding affinity towards beta-2 receptor of bovine lung
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00084a006
DB00368 2805 64 None -36 26 Bovine 5.2 pKi = 5.2 Binding
Compound was evaluated for beta adrenergic binding affinity towards beta-2 receptor of bovine lungCompound was evaluated for beta adrenergic binding affinity towards beta-2 receptor of bovine lung
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00084a006
1960 2805 64 None -36 26 Bovine 5.2 pKi = 5.2 Binding
Tested for binding affinity against beta-2 adrenergic receptor in bovine lung using [3H]DHA as radioligandTested for binding affinity against beta-2 adrenergic receptor in bovine lung using [3H]DHA as radioligand
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00073a006
439260 2805 64 None -36 26 Bovine 5.2 pKi = 5.2 Binding
Tested for binding affinity against beta-2 adrenergic receptor in bovine lung using [3H]DHA as radioligandTested for binding affinity against beta-2 adrenergic receptor in bovine lung using [3H]DHA as radioligand
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00073a006
505 2805 64 None -36 26 Bovine 5.2 pKi = 5.2 Binding
Tested for binding affinity against beta-2 adrenergic receptor in bovine lung using [3H]DHA as radioligandTested for binding affinity against beta-2 adrenergic receptor in bovine lung using [3H]DHA as radioligand
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00073a006
CHEMBL1437 2805 64 None -36 26 Bovine 5.2 pKi = 5.2 Binding
Tested for binding affinity against beta-2 adrenergic receptor in bovine lung using [3H]DHA as radioligandTested for binding affinity against beta-2 adrenergic receptor in bovine lung using [3H]DHA as radioligand
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00073a006
DB00368 2805 64 None -36 26 Bovine 5.2 pKi = 5.2 Binding
Tested for binding affinity against beta-2 adrenergic receptor in bovine lung using [3H]DHA as radioligandTested for binding affinity against beta-2 adrenergic receptor in bovine lung using [3H]DHA as radioligand
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00073a006
16735263 85351 0 None 5 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 302 6 5 5 1.9 C[C@@H](Cc1ccc(N)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1021/jm070030d
CHEMBL229442 85351 0 None 5 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 302 6 5 5 1.9 C[C@@H](Cc1ccc(N)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1021/jm070030d
123133225 144264 0 None 5 2 Human 5.2 pKi = 5.2 Binding
Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.
ChEMBL 302 6 5 5 1.9 C[C@@H](Cc1cccc(N)c1)NC[C@H](O)c1cc(O)cc(O)c1 nan
CHEMBL3909417 144264 0 None 5 2 Human 5.2 pKi = 5.2 Binding
Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.
ChEMBL 302 6 5 5 1.9 C[C@@H](Cc1cccc(N)c1)NC[C@H](O)c1cc(O)cc(O)c1 nan
16735263 85351 0 None 5 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 302 6 5 5 1.9 C[C@@H](Cc1ccc(N)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1021/jm070030d
CHEMBL229442 85351 0 None 5 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 302 6 5 5 1.9 C[C@@H](Cc1ccc(N)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1021/jm070030d
319 1292 39 None -16 9 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-dihydroalprenolol from human beta2-adrenoceptor expressed in HEK cells after 4 hrsDisplacement of [3H]-dihydroalprenolol from human beta2-adrenoceptor expressed in HEK cells after 4 hrs
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2011.01.043
321 1292 39 None -16 9 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-dihydroalprenolol from human beta2-adrenoceptor expressed in HEK cells after 4 hrsDisplacement of [3H]-dihydroalprenolol from human beta2-adrenoceptor expressed in HEK cells after 4 hrs
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2011.01.043
444031 1292 39 None -16 9 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-dihydroalprenolol from human beta2-adrenoceptor expressed in HEK cells after 4 hrsDisplacement of [3H]-dihydroalprenolol from human beta2-adrenoceptor expressed in HEK cells after 4 hrs
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2011.01.043
784 1292 39 None -16 9 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-dihydroalprenolol from human beta2-adrenoceptor expressed in HEK cells after 4 hrsDisplacement of [3H]-dihydroalprenolol from human beta2-adrenoceptor expressed in HEK cells after 4 hrs
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2011.01.043
CHEMBL1346 1292 39 None -16 9 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-dihydroalprenolol from human beta2-adrenoceptor expressed in HEK cells after 4 hrsDisplacement of [3H]-dihydroalprenolol from human beta2-adrenoceptor expressed in HEK cells after 4 hrs
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2011.01.043
DB00496 1292 39 None -16 9 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-dihydroalprenolol from human beta2-adrenoceptor expressed in HEK cells after 4 hrsDisplacement of [3H]-dihydroalprenolol from human beta2-adrenoceptor expressed in HEK cells after 4 hrs
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2011.01.043
10054373 58217 0 None -436 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-dihydroalprenolol from human beta2-adrenoceptor expressed in HEK cells after 4 hrsDisplacement of [3H]-dihydroalprenolol from human beta2-adrenoceptor expressed in HEK cells after 4 hrs
ChEMBL 603 17 5 7 6.6 O=C(Nc1ccccc1-c1ccccc1)OC1CCN(CCCCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)CC1 10.1016/j.bmcl.2011.01.043
CHEMBL1683936 58217 0 None -436 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-dihydroalprenolol from human beta2-adrenoceptor expressed in HEK cells after 4 hrsDisplacement of [3H]-dihydroalprenolol from human beta2-adrenoceptor expressed in HEK cells after 4 hrs
ChEMBL 603 17 5 7 6.6 O=C(Nc1ccccc1-c1ccccc1)OC1CCN(CCCCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)CC1 10.1016/j.bmcl.2011.01.043
127047996 139103 0 None -138 6 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cellsDisplacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells
ChEMBL 303 8 3 5 2.3 COc1ccccc1OCCNCCc1ccc(O)c(O)c1 10.1016/j.bmc.2016.04.028
CHEMBL3797758 139103 0 None -138 6 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cellsDisplacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells
ChEMBL 303 8 3 5 2.3 COc1ccccc1OCCNCCc1ccc(O)c(O)c1 10.1016/j.bmc.2016.04.028
681 1432 65 None -707 39 Human 4.2 pKi = 4.2 Binding
Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cellsDisplacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2016.04.028
940 1432 65 None -707 39 Human 4.2 pKi = 4.2 Binding
Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cellsDisplacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2016.04.028
947 1432 65 None -707 39 Human 4.2 pKi = 4.2 Binding
Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cellsDisplacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2016.04.028
CHEMBL59 1432 65 None -707 39 Human 4.2 pKi = 4.2 Binding
Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cellsDisplacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2016.04.028
DB00988 1432 65 None -707 39 Human 4.2 pKi = 4.2 Binding
Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cellsDisplacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2016.04.028
10544781 202969 0 None 10 3 Human 6.2 pKi = 6.2 Binding
Binding Affinity against human beta-2 adrenergic receptor expressed in Chinese hamster ovary(CHO) cells was measured by using [125I]ICYP radioligandBinding Affinity against human beta-2 adrenergic receptor expressed in Chinese hamster ovary(CHO) cells was measured by using [125I]ICYP radioligand
ChEMBL 335 5 2 7 2.2 COc1cc(CC2NCCc3nc(N)sc32)cc(OC)c1OC 10.1021/jm990012z
CHEMBL73917 202969 0 None 10 3 Human 6.2 pKi = 6.2 Binding
Binding Affinity against human beta-2 adrenergic receptor expressed in Chinese hamster ovary(CHO) cells was measured by using [125I]ICYP radioligandBinding Affinity against human beta-2 adrenergic receptor expressed in Chinese hamster ovary(CHO) cells was measured by using [125I]ICYP radioligand
ChEMBL 335 5 2 7 2.2 COc1cc(CC2NCCc3nc(N)sc32)cc(OC)c1OC 10.1021/jm990012z
12353629 202216 0 None -1 3 Bovine 7.2 pKi = 7.2 Binding
Compound was evaluated for beta adrenergic binding affinity towards Beta-2 adrenergic receptor of bovine lungCompound was evaluated for beta adrenergic binding affinity towards Beta-2 adrenergic receptor of bovine lung
ChEMBL 237 2 4 4 1.4 CC(C)N[C@@H]1CCc2c(ccc(O)c2O)[C@H]1O 10.1021/jm00084a006
CHEMBL6913 202216 0 None -1 3 Bovine 7.2 pKi = 7.2 Binding
Compound was evaluated for beta adrenergic binding affinity towards Beta-2 adrenergic receptor of bovine lungCompound was evaluated for beta adrenergic binding affinity towards Beta-2 adrenergic receptor of bovine lung
ChEMBL 237 2 4 4 1.4 CC(C)N[C@@H]1CCc2c(ccc(O)c2O)[C@H]1O 10.1021/jm00084a006
14485418 202205 0 None - 1 Mouse 4.2 pKi = 4.2 Binding
Ki value was determined by accumulation of c-AMP in S-49 mouse lymphoma cells (Beta2).Ki value was determined by accumulation of c-AMP in S-49 mouse lymphoma cells (Beta2).
ChEMBL 495 13 4 5 4.6 CC(=O)Nc1ccc(OC[C@H](O)CN[C@@H](C)CCCCC(=O)Nc2ccc(C(F)(F)F)cc2)cc1 10.1021/jm00163a036
CHEMBL69036 202205 0 None - 1 Mouse 4.2 pKi = 4.2 Binding
Ki value was determined by accumulation of c-AMP in S-49 mouse lymphoma cells (Beta2).Ki value was determined by accumulation of c-AMP in S-49 mouse lymphoma cells (Beta2).
ChEMBL 495 13 4 5 4.6 CC(=O)Nc1ccc(OC[C@H](O)CN[C@@H](C)CCCCC(=O)Nc2ccc(C(F)(F)F)cc2)cc1 10.1021/jm00163a036
10311070 111755 0 None 316 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assay
ChEMBL 484 11 5 6 5.2 COc1ccc(Nc2ccc(CCNCC(O)c3ccc(O)c(CO)c3)cc2)cc1-c1ccccc1 10.1016/j.bmcl.2014.04.069
CHEMBL3290989 111755 0 None 316 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assay
ChEMBL 484 11 5 6 5.2 COc1ccc(Nc2ccc(CCNCC(O)c3ccc(O)c(CO)c3)cc2)cc1-c1ccccc1 10.1016/j.bmcl.2014.04.069
567 715 10 None -4 5 Human 6.2 pKi = 6.2 Binding
Ability to bind to human Beta-2 adrenergic receptor using membranes of stably transfected CHO cellsAbility to bind to human Beta-2 adrenergic receptor using membranes of stably transfected CHO cells
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1016/S0960-894X(97)00266-7
9841972 715 10 None -4 5 Human 6.2 pKi = 6.2 Binding
Ability to bind to human Beta-2 adrenergic receptor using membranes of stably transfected CHO cellsAbility to bind to human Beta-2 adrenergic receptor using membranes of stably transfected CHO cells
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1016/S0960-894X(97)00266-7
CHEMBL284782 715 10 None -4 5 Human 6.2 pKi = 6.2 Binding
Ability to bind to human Beta-2 adrenergic receptor using membranes of stably transfected CHO cellsAbility to bind to human Beta-2 adrenergic receptor using membranes of stably transfected CHO cells
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1016/S0960-894X(97)00266-7
567 715 10 None -4 5 Human 6.2 pKi = 6.2 Binding
Compound was tested for its binding affinity against beta2 adrenergic receptor in CHO cell membrane using [125I]iodocyanopindolol as the radioligand.Compound was tested for its binding affinity against beta2 adrenergic receptor in CHO cell membrane using [125I]iodocyanopindolol as the radioligand.
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1016/0960-894X(96)00417-9
9841972 715 10 None -4 5 Human 6.2 pKi = 6.2 Binding
Compound was tested for its binding affinity against beta2 adrenergic receptor in CHO cell membrane using [125I]iodocyanopindolol as the radioligand.Compound was tested for its binding affinity against beta2 adrenergic receptor in CHO cell membrane using [125I]iodocyanopindolol as the radioligand.
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1016/0960-894X(96)00417-9
CHEMBL284782 715 10 None -4 5 Human 6.2 pKi = 6.2 Binding
Compound was tested for its binding affinity against beta2 adrenergic receptor in CHO cell membrane using [125I]iodocyanopindolol as the radioligand.Compound was tested for its binding affinity against beta2 adrenergic receptor in CHO cell membrane using [125I]iodocyanopindolol as the radioligand.
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1016/0960-894X(96)00417-9
59119455 111757 0 None 19 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assay
ChEMBL 408 10 5 6 3.5 COc1cccc(Nc2ccc(CCNCC(O)c3ccc(O)c(CO)c3)cc2)c1 10.1016/j.bmcl.2014.04.069
CHEMBL3290990 111757 0 None 19 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assay
ChEMBL 408 10 5 6 3.5 COc1cccc(Nc2ccc(CCNCC(O)c3ccc(O)c(CO)c3)cc2)c1 10.1016/j.bmcl.2014.04.069
90644154 111751 0 None 5 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assay
ChEMBL 428 9 5 5 4.6 OCc1cc(C(O)CNCCc2ccc(Nc3cccc4ccccc34)cc2)ccc1O 10.1016/j.bmcl.2014.04.069
CHEMBL3290985 111751 0 None 5 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assay
ChEMBL 428 9 5 5 4.6 OCc1cc(C(O)CNCCc2ccc(Nc3cccc4ccccc34)cc2)ccc1O 10.1016/j.bmcl.2014.04.069
9960584 154080 0 None -10 3 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]iodocyanopindolol from human cloned adrenergic beta-2 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human cloned adrenergic beta-2 receptor expressed in CHO cells
ChEMBL 500 12 4 7 3.3 COc1ccc([C@@H](Cc2ccccc2)NC[C@@H](O)Cc2ccc(O)c(NS(C)(=O)=O)c2)cc1OC 10.1016/j.bmcl.2007.05.030
CHEMBL399329 154080 0 None -10 3 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]iodocyanopindolol from human cloned adrenergic beta-2 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human cloned adrenergic beta-2 receptor expressed in CHO cells
ChEMBL 500 12 4 7 3.3 COc1ccc([C@@H](Cc2ccccc2)NC[C@@H](O)Cc2ccc(O)c(NS(C)(=O)=O)c2)cc1OC 10.1016/j.bmcl.2007.05.030
1028 287 69 None -30 30 Dog 6.2 pKi = 6.2 Binding
Binding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranes
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm990599h
139148732 287 69 None -30 30 Dog 6.2 pKi = 6.2 Binding
Binding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranes
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm990599h
479 287 69 None -30 30 Dog 6.2 pKi = 6.2 Binding
Binding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranes
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm990599h
5816 287 69 None -30 30 Dog 6.2 pKi = 6.2 Binding
Binding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranes
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm990599h
CHEMBL679 287 69 None -30 30 Dog 6.2 pKi = 6.2 Binding
Binding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranes
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm990599h
DB00668 287 69 None -30 30 Dog 6.2 pKi = 6.2 Binding
Binding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranes
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm990599h
70684522 76409 0 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cellsDisplacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cells
ChEMBL 343 4 3 4 1.4 CC(C)(C)NC[C@H](O)c1ccc2c(c1)C[OH+][B-](O)(c1ccccc1)O2 10.1016/j.bmc.2011.11.054
CHEMBL2068577 76409 0 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cellsDisplacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cells
ChEMBL 343 4 3 4 1.4 CC(C)(C)NC[C@H](O)c1ccc2c(c1)C[OH+][B-](O)(c1ccccc1)O2 10.1016/j.bmc.2011.11.054
70684522 76409 0 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cellsDisplacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cells
ChEMBL 343 4 3 4 1.4 CC(C)(C)NC[C@H](O)c1ccc2c(c1)C[OH+][B-](O)(c1ccccc1)O2 10.1016/j.bmc.2011.11.054
CHEMBL2068577 76409 0 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cellsDisplacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cells
ChEMBL 343 4 3 4 1.4 CC(C)(C)NC[C@H](O)c1ccc2c(c1)C[OH+][B-](O)(c1ccccc1)O2 10.1016/j.bmc.2011.11.054
10352428 100623 1 None 1 4 Dog 7.2 pKi = 7.2 Binding
Binding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranes
ChEMBL 187 2 4 4 0.2 NC[C@H](O)c1ccc(O)c(O)c1F 10.1021/jm990599h
CHEMBL295072 100623 1 None 1 4 Dog 7.2 pKi = 7.2 Binding
Binding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranes
ChEMBL 187 2 4 4 0.2 NC[C@H](O)c1ccc(O)c(O)c1F 10.1021/jm990599h
1499 2052 43 None -33 17 Human 6.2 pKi = 6.2 Binding
Binding Affinity against human beta-2 adrenergic receptor expressed in Chinese hamster ovary(CHO) cells was measured by using [125I]ICYP radioligandBinding Affinity against human beta-2 adrenergic receptor expressed in Chinese hamster ovary(CHO) cells was measured by using [125I]ICYP radioligand
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm990012z
3779 2052 43 None -33 17 Human 6.2 pKi = 6.2 Binding
Binding Affinity against human beta-2 adrenergic receptor expressed in Chinese hamster ovary(CHO) cells was measured by using [125I]ICYP radioligandBinding Affinity against human beta-2 adrenergic receptor expressed in Chinese hamster ovary(CHO) cells was measured by using [125I]ICYP radioligand
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm990012z
536 2052 43 None -33 17 Human 6.2 pKi = 6.2 Binding
Binding Affinity against human beta-2 adrenergic receptor expressed in Chinese hamster ovary(CHO) cells was measured by using [125I]ICYP radioligandBinding Affinity against human beta-2 adrenergic receptor expressed in Chinese hamster ovary(CHO) cells was measured by using [125I]ICYP radioligand
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm990012z
CHEMBL434 2052 43 None -33 17 Human 6.2 pKi = 6.2 Binding
Binding Affinity against human beta-2 adrenergic receptor expressed in Chinese hamster ovary(CHO) cells was measured by using [125I]ICYP radioligandBinding Affinity against human beta-2 adrenergic receptor expressed in Chinese hamster ovary(CHO) cells was measured by using [125I]ICYP radioligand
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm990012z
DB01064 2052 43 None -33 17 Human 6.2 pKi = 6.2 Binding
Binding Affinity against human beta-2 adrenergic receptor expressed in Chinese hamster ovary(CHO) cells was measured by using [125I]ICYP radioligandBinding Affinity against human beta-2 adrenergic receptor expressed in Chinese hamster ovary(CHO) cells was measured by using [125I]ICYP radioligand
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm990012z
52943383 17384 0 None -1 3 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 544 9 2 8 5.3 OC(CNC1CCN(c2ncnc3scc(-c4ccccc4)c23)CC1)COc1cccc(OC(F)(F)F)c1 10.1016/j.bmcl.2010.08.039
CHEMBL1258142 17384 0 None -1 3 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 544 9 2 8 5.3 OC(CNC1CCN(c2ncnc3scc(-c4ccccc4)c23)CC1)COc1cccc(OC(F)(F)F)c1 10.1016/j.bmcl.2010.08.039
6603724 154780 3 None -1 3 Human 4.2 pKi = 4.2 Binding
Displacement of [3H]prazosin from human adrenergic beta2 receptor N293Q mutant expressed in CHO cell membraneDisplacement of [3H]prazosin from human adrenergic beta2 receptor N293Q mutant expressed in CHO cell membrane
ChEMBL 187 2 4 4 0.2 NC[C@H](O)c1cc(O)c(O)cc1F 10.1016/j.bmc.2009.10.015
CHEMBL40317 154780 3 None -1 3 Human 4.2 pKi = 4.2 Binding
Displacement of [3H]prazosin from human adrenergic beta2 receptor N293Q mutant expressed in CHO cell membraneDisplacement of [3H]prazosin from human adrenergic beta2 receptor N293Q mutant expressed in CHO cell membrane
ChEMBL 187 2 4 4 0.2 NC[C@H](O)c1cc(O)c(O)cc1F 10.1016/j.bmc.2009.10.015
155558987 174203 0 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assay
ChEMBL 225 6 3 4 1.9 CC(C)NCCCOc1ccc(O)c(O)c1 10.1021/acs.jmedchem.9b00349
CHEMBL4561683 174203 0 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assay
ChEMBL 225 6 3 4 1.9 CC(C)NCCCOc1ccc(O)c(O)c1 10.1021/acs.jmedchem.9b00349
46221604 8457 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]cyanopindolol from human recombinant beta2 adrenergic receptor expressed in CHO cells by filtration assayDisplacement of [125I]cyanopindolol from human recombinant beta2 adrenergic receptor expressed in CHO cells by filtration assay
ChEMBL 392 6 4 4 3.1 CCc1ccc(CC)c2c1CC(NC[C@H](O)c1ccc(O)c3[nH]c(=O)ccc13)C2 10.1021/jm100068m
CHEMBL1094487 8457 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]cyanopindolol from human recombinant beta2 adrenergic receptor expressed in CHO cells by filtration assayDisplacement of [125I]cyanopindolol from human recombinant beta2 adrenergic receptor expressed in CHO cells by filtration assay
ChEMBL 392 6 4 4 3.1 CCc1ccc(CC)c2c1CC(NC[C@H](O)c1ccc(O)c3[nH]c(=O)ccc13)C2 10.1021/jm100068m
24937013 17252 0 None 4 3 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 504 9 3 8 4.6 CCc1cc(O)ccc1OCC(O)CNC1CCN(c2ncnc3scc(-c4ccccc4)c23)CC1 10.1016/j.bmcl.2010.08.039
CHEMBL1257676 17252 0 None 4 3 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 504 9 3 8 4.6 CCc1cc(O)ccc1OCC(O)CNC1CCN(c2ncnc3scc(-c4ccccc4)c23)CC1 10.1016/j.bmcl.2010.08.039
2769774 6625 16 None 16 3 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cells
ChEMBL 277 7 1 4 1.5 C=CCc1ccccc1OCC(O)CN1CCOCC1 10.1016/j.bmcl.2010.04.009
CHEMBL1083667 6625 16 None 16 3 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cells
ChEMBL 277 7 1 4 1.5 C=CCc1ccccc1OCC(O)CN1CCOCC1 10.1016/j.bmcl.2010.04.009
118710942 113240 0 None 8 3 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assay
ChEMBL 384 5 4 5 3.6 Cc1ccccc1[C@H]1CCC[C@H]1NC[C@H](O)c1ccc(O)c2[nH]c(=O)sc12 10.1016/j.bmcl.2014.06.014
CHEMBL3323660 113240 0 None 8 3 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assay
ChEMBL 384 5 4 5 3.6 Cc1ccccc1[C@H]1CCC[C@H]1NC[C@H](O)c1ccc(O)c2[nH]c(=O)sc12 10.1016/j.bmcl.2014.06.014
146025803 175593 0 None -1 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assay
ChEMBL 467 14 4 7 3.7 COc1cc(CCNC[C@H](O)COc2ccc(O)c(O)c2)ccc1OCCCc1ccccc1 10.1021/acs.jmedchem.9b00349
CHEMBL4593181 175593 0 None -1 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assay
ChEMBL 467 14 4 7 3.7 COc1cc(CCNC[C@H](O)COc2ccc(O)c(O)c2)ccc1OCCCc1ccccc1 10.1021/acs.jmedchem.9b00349
49864412 15451 0 None 5 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptorDisplacement of [3H]CGP12177 from human beta2 adrenoceptor
ChEMBL 414 7 4 6 3.4 O=c1[nH]c2c(O)ccc([C@@H](O)CN[C@@H]3CCCC[C@H]3OCc3ccccc3)c2s1 10.1016/j.bmcl.2010.06.136
CHEMBL1221732 15451 0 None 5 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptorDisplacement of [3H]CGP12177 from human beta2 adrenoceptor
ChEMBL 414 7 4 6 3.4 O=c1[nH]c2c(O)ccc([C@@H](O)CN[C@@H]3CCCC[C@H]3OCc3ccccc3)c2s1 10.1016/j.bmcl.2010.06.136
12147227 61648 0 None -1 2 Human 8.1 pKi = 8.1 Binding
Inhibition of 125 I-Iodocyanopindolol binding to Beta-2 adrenergic receptorInhibition of 125 I-Iodocyanopindolol binding to Beta-2 adrenergic receptor
ChEMBL 578 8 6 9 2.3 CN(C)C(=N)NC1=NC(=O)/C(=C/c2ccc(N3CCC(NC[C@H](O)COc4cccc5[nH]c(O)nc45)CC3)cc2)S1 10.1016/s0960-894x(01)00147-0
142109147 61648 0 None -1 2 Human 8.1 pKi = 8.1 Binding
Inhibition of 125 I-Iodocyanopindolol binding to Beta-2 adrenergic receptorInhibition of 125 I-Iodocyanopindolol binding to Beta-2 adrenergic receptor
ChEMBL 578 8 6 9 2.3 CN(C)C(=N)NC1=NC(=O)/C(=C/c2ccc(N3CCC(NC[C@H](O)COc4cccc5[nH]c(O)nc45)CC3)cc2)S1 10.1016/s0960-894x(01)00147-0
44386630 61648 0 None -1 2 Human 8.1 pKi = 8.1 Binding
Inhibition of 125 I-Iodocyanopindolol binding to Beta-2 adrenergic receptorInhibition of 125 I-Iodocyanopindolol binding to Beta-2 adrenergic receptor
ChEMBL 578 8 6 9 2.3 CN(C)C(=N)NC1=NC(=O)/C(=C/c2ccc(N3CCC(NC[C@H](O)COc4cccc5[nH]c(O)nc45)CC3)cc2)S1 10.1016/s0960-894x(01)00147-0
69921317 61648 0 None -1 2 Human 8.1 pKi = 8.1 Binding
Inhibition of 125 I-Iodocyanopindolol binding to Beta-2 adrenergic receptorInhibition of 125 I-Iodocyanopindolol binding to Beta-2 adrenergic receptor
ChEMBL 578 8 6 9 2.3 CN(C)C(=N)NC1=NC(=O)/C(=C/c2ccc(N3CCC(NC[C@H](O)COc4cccc5[nH]c(O)nc45)CC3)cc2)S1 10.1016/s0960-894x(01)00147-0
CHEMBL177442 61648 0 None -1 2 Human 8.1 pKi = 8.1 Binding
Inhibition of 125 I-Iodocyanopindolol binding to Beta-2 adrenergic receptorInhibition of 125 I-Iodocyanopindolol binding to Beta-2 adrenergic receptor
ChEMBL 578 8 6 9 2.3 CN(C)C(=N)NC1=NC(=O)/C(=C/c2ccc(N3CCC(NC[C@H](O)COc4cccc5[nH]c(O)nc45)CC3)cc2)S1 10.1016/s0960-894x(01)00147-0
10789142 113682 0 None 190 2 Human 8.1 pKi = 8.1 Binding
Binding affinity for human Beta-2 adrenergic receptor expressed in CHO cells by radioligand competition binding assays using [125I]iodocyanopindolol (ICYP)Binding affinity for human Beta-2 adrenergic receptor expressed in CHO cells by radioligand competition binding assays using [125I]iodocyanopindolol (ICYP)
ChEMBL 438 3 4 4 3.1 CC(=O)Nc1ccc(CC2NCCc3cc(O)c(O)cc32)cc1I 10.1021/jm960208o
CHEMBL332964 113682 0 None 190 2 Human 8.1 pKi = 8.1 Binding
Binding affinity for human Beta-2 adrenergic receptor expressed in CHO cells by radioligand competition binding assays using [125I]iodocyanopindolol (ICYP)Binding affinity for human Beta-2 adrenergic receptor expressed in CHO cells by radioligand competition binding assays using [125I]iodocyanopindolol (ICYP)
ChEMBL 438 3 4 4 3.1 CC(=O)Nc1ccc(CC2NCCc3cc(O)c(O)cc32)cc1I 10.1021/jm960208o
44393894 123542 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity for human beta-2 adrenergic receptorBinding affinity for human beta-2 adrenergic receptor
ChEMBL 420 12 4 5 3.4 O=CNc1cc([C@@H](O)CNCCc2ccc(OCCc3ccccc3)cc2)ccc1O 10.1016/j.bmcl.2004.06.086
CHEMBL363260 123542 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity for human beta-2 adrenergic receptorBinding affinity for human beta-2 adrenergic receptor
ChEMBL 420 12 4 5 3.4 O=CNc1cc([C@@H](O)CNCCc2ccc(OCCc3ccccc3)cc2)ccc1O 10.1016/j.bmcl.2004.06.086
44396729 66513 0 None -26 3 Human 7.2 pKi = 7.2 Binding
Binding inhibition constant was determined by inhibition of [125I]iodocyanopindolol binding to Beta-2 adrenergic receptorBinding inhibition constant was determined by inhibition of [125I]iodocyanopindolol binding to Beta-2 adrenergic receptor
ChEMBL 528 10 5 7 2.8 CS(=O)(=O)c1cccc2c(CCNC[C@H](O)c3cccc(NS(=O)(=O)c4cccc(N)c4)c3)c[nH]c12 10.1016/j.bmcl.2004.09.054
CHEMBL186247 66513 0 None -26 3 Human 7.2 pKi = 7.2 Binding
Binding inhibition constant was determined by inhibition of [125I]iodocyanopindolol binding to Beta-2 adrenergic receptorBinding inhibition constant was determined by inhibition of [125I]iodocyanopindolol binding to Beta-2 adrenergic receptor
ChEMBL 528 10 5 7 2.8 CS(=O)(=O)c1cccc2c(CCNC[C@H](O)c3cccc(NS(=O)(=O)c4cccc(N)c4)c3)c[nH]c12 10.1016/j.bmcl.2004.09.054
5187268 6484 11 None 10 3 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cells
ChEMBL 501 9 1 6 3.6 CC(C)c1ccccc1OCC(O)CN1CCN(CCN2C(=O)c3cccc4cccc(c34)C2=O)CC1 10.1016/j.bmcl.2010.04.009
CHEMBL1083053 6484 11 None 10 3 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cells
ChEMBL 501 9 1 6 3.6 CC(C)c1ccccc1OCC(O)CN1CCN(CCN2C(=O)c3cccc4cccc(c34)C2=O)CC1 10.1016/j.bmcl.2010.04.009
2796082 6742 4 None -1 2 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 490 9 2 8 4.4 COc1ccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)cc1 10.1016/j.bmcl.2010.08.039
CHEMBL1083995 6742 4 None -1 2 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 490 9 2 8 4.4 COc1ccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)cc1 10.1016/j.bmcl.2010.08.039
2796082 6742 4 None -1 2 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cells
ChEMBL 490 9 2 8 4.4 COc1ccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)cc1 10.1016/j.bmcl.2010.04.009
CHEMBL1083995 6742 4 None -1 2 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cells
ChEMBL 490 9 2 8 4.4 COc1ccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)cc1 10.1016/j.bmcl.2010.04.009
155512924 169121 0 None 1 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assay
ChEMBL 451 14 3 6 4.7 COc1cc(CCNCCCOc2ccc(O)c(O)c2)ccc1OCCCc1ccccc1 10.1021/acs.jmedchem.9b00349
CHEMBL4437939 169121 0 None 1 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assay
ChEMBL 451 14 3 6 4.7 COc1cc(CCNCCCOc2ccc(O)c(O)c2)ccc1OCCCc1ccccc1 10.1021/acs.jmedchem.9b00349
10352428 100623 1 None -1047 4 Human 4.2 pKi = 4.2 Binding
Displacement of [3H]prazosin from human adrenergic beta2 receptor N293F mutant expressed in CHO cell membraneDisplacement of [3H]prazosin from human adrenergic beta2 receptor N293F mutant expressed in CHO cell membrane
ChEMBL 187 2 4 4 0.2 NC[C@H](O)c1ccc(O)c(O)c1F 10.1016/j.bmc.2009.10.015
CHEMBL295072 100623 1 None -1047 4 Human 4.2 pKi = 4.2 Binding
Displacement of [3H]prazosin from human adrenergic beta2 receptor N293F mutant expressed in CHO cell membraneDisplacement of [3H]prazosin from human adrenergic beta2 receptor N293F mutant expressed in CHO cell membrane
ChEMBL 187 2 4 4 0.2 NC[C@H](O)c1ccc(O)c(O)c1F 10.1016/j.bmc.2009.10.015
44444189 94047 0 None -1 3 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]iodocyanopindolol from human cloned adrenergic beta-2 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human cloned adrenergic beta-2 receptor expressed in CHO cells
ChEMBL 586 15 4 7 4.8 CS(=O)(=O)Nc1cc(C[C@@H](O)CN[C@@H](CCc2ccccc2)c2ccc(OC(F)F)c(OC(F)F)c2)ccc1O 10.1016/j.bmcl.2007.05.030
CHEMBL251555 94047 0 None -1 3 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]iodocyanopindolol from human cloned adrenergic beta-2 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human cloned adrenergic beta-2 receptor expressed in CHO cells
ChEMBL 586 15 4 7 4.8 CS(=O)(=O)Nc1cc(C[C@@H](O)CN[C@@H](CCc2ccccc2)c2ccc(OC(F)F)c(OC(F)F)c2)ccc1O 10.1016/j.bmcl.2007.05.030
541614 17815 1 None 3 2 Rat 6.2 pKi = 6.2 Binding
Binding affinity against adrenergic beta 2 receptor versus 1 nM [3H]dihydroalprenolol in rat cerebral cerebellar membranesBinding affinity against adrenergic beta 2 receptor versus 1 nM [3H]dihydroalprenolol in rat cerebral cerebellar membranes
ChEMBL 219 3 4 4 0.6 CNCC(O)c1cc(F)c(O)c(O)c1F 10.1021/jm00076a024
CHEMBL126347 17815 1 None 3 2 Rat 6.2 pKi = 6.2 Binding
Binding affinity against adrenergic beta 2 receptor versus 1 nM [3H]dihydroalprenolol in rat cerebral cerebellar membranesBinding affinity against adrenergic beta 2 receptor versus 1 nM [3H]dihydroalprenolol in rat cerebral cerebellar membranes
ChEMBL 219 3 4 4 0.6 CNCC(O)c1cc(F)c(O)c(O)c1F 10.1021/jm00076a024
15162894 202672 1 None - 1 Bovine 4.2 pKi = 4.2 Binding
Compound was evaluated for beta adrenergic binding affinity towards Beta-2 adrenergic receptor of bovine lungCompound was evaluated for beta adrenergic binding affinity towards Beta-2 adrenergic receptor of bovine lung
ChEMBL 195 0 4 4 0.4 N[C@@H]1CCc2cc(O)c(O)cc2[C@H]1O 10.1021/jm00084a006
CHEMBL7185 202672 1 None - 1 Bovine 4.2 pKi = 4.2 Binding
Compound was evaluated for beta adrenergic binding affinity towards Beta-2 adrenergic receptor of bovine lungCompound was evaluated for beta adrenergic binding affinity towards Beta-2 adrenergic receptor of bovine lung
ChEMBL 195 0 4 4 0.4 N[C@@H]1CCc2cc(O)c(O)cc2[C@H]1O 10.1021/jm00084a006
1028 287 69 None -12 30 Rat 6.1 pKi = 6.1 Binding
Binding affinity against adrenergic beta 2 receptor versus 1 nM [3H]dihydroalprenolol in rat cerebral cerebellar membranesBinding affinity against adrenergic beta 2 receptor versus 1 nM [3H]dihydroalprenolol in rat cerebral cerebellar membranes
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00076a024
139148732 287 69 None -12 30 Rat 6.1 pKi = 6.1 Binding
Binding affinity against adrenergic beta 2 receptor versus 1 nM [3H]dihydroalprenolol in rat cerebral cerebellar membranesBinding affinity against adrenergic beta 2 receptor versus 1 nM [3H]dihydroalprenolol in rat cerebral cerebellar membranes
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00076a024
479 287 69 None -12 30 Rat 6.1 pKi = 6.1 Binding
Binding affinity against adrenergic beta 2 receptor versus 1 nM [3H]dihydroalprenolol in rat cerebral cerebellar membranesBinding affinity against adrenergic beta 2 receptor versus 1 nM [3H]dihydroalprenolol in rat cerebral cerebellar membranes
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00076a024
5816 287 69 None -12 30 Rat 6.1 pKi = 6.1 Binding
Binding affinity against adrenergic beta 2 receptor versus 1 nM [3H]dihydroalprenolol in rat cerebral cerebellar membranesBinding affinity against adrenergic beta 2 receptor versus 1 nM [3H]dihydroalprenolol in rat cerebral cerebellar membranes
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00076a024
CHEMBL679 287 69 None -12 30 Rat 6.1 pKi = 6.1 Binding
Binding affinity against adrenergic beta 2 receptor versus 1 nM [3H]dihydroalprenolol in rat cerebral cerebellar membranesBinding affinity against adrenergic beta 2 receptor versus 1 nM [3H]dihydroalprenolol in rat cerebral cerebellar membranes
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00076a024
DB00668 287 69 None -12 30 Rat 6.1 pKi = 6.1 Binding
Binding affinity against adrenergic beta 2 receptor versus 1 nM [3H]dihydroalprenolol in rat cerebral cerebellar membranesBinding affinity against adrenergic beta 2 receptor versus 1 nM [3H]dihydroalprenolol in rat cerebral cerebellar membranes
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00076a024
11819522 11896 0 None -4 2 Bovine 5.1 pKi = 5.1 Binding
Binding affinity against beta-2-adrenergic receptor in bovine lungBinding affinity against beta-2-adrenergic receptor in bovine lung
ChEMBL 174 6 2 4 0.4 C/C=N/OCC(O)CNC(C)C 10.1021/jm00036a018
CHEMBL1183318 11896 0 None -4 2 Bovine 5.1 pKi = 5.1 Binding
Binding affinity against beta-2-adrenergic receptor in bovine lungBinding affinity against beta-2-adrenergic receptor in bovine lung
ChEMBL 174 6 2 4 0.4 C/C=N/OCC(O)CNC(C)C 10.1021/jm00036a018
CHEMBL290153 11896 0 None -4 2 Bovine 5.1 pKi = 5.1 Binding
Binding affinity against beta-2-adrenergic receptor in bovine lungBinding affinity against beta-2-adrenergic receptor in bovine lung
ChEMBL 174 6 2 4 0.4 C/C=N/OCC(O)CNC(C)C 10.1021/jm00036a018
44286980 147348 0 None -3 2 Human 4.1 pKi = 4.1 Binding
Ability to bind to human Beta-2 adrenergic receptor using membranes of stably transfected CHO cellsAbility to bind to human Beta-2 adrenergic receptor using membranes of stably transfected CHO cells
ChEMBL 397 9 3 4 3.8 C[C@H](Cc1ccc(OCP(C)(=O)O)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1016/S0960-894X(97)00266-7
CHEMBL39334 147348 0 None -3 2 Human 4.1 pKi = 4.1 Binding
Ability to bind to human Beta-2 adrenergic receptor using membranes of stably transfected CHO cellsAbility to bind to human Beta-2 adrenergic receptor using membranes of stably transfected CHO cells
ChEMBL 397 9 3 4 3.8 C[C@H](Cc1ccc(OCP(C)(=O)O)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1016/S0960-894X(97)00266-7
1621 2386 16 None -218 45 Human 6.1 pKi = 6.1 Binding
Binding affinity towards Beta-2 adrenergic receptorBinding affinity towards Beta-2 adrenergic receptor
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm020153s
17 2386 16 None -218 45 Human 6.1 pKi = 6.1 Binding
Binding affinity towards Beta-2 adrenergic receptorBinding affinity towards Beta-2 adrenergic receptor
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm020153s
5761 2386 16 None -218 45 Human 6.1 pKi = 6.1 Binding
Binding affinity towards Beta-2 adrenergic receptorBinding affinity towards Beta-2 adrenergic receptor
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm020153s
CHEMBL263881 2386 16 None -218 45 Human 6.1 pKi = 6.1 Binding
Binding affinity towards Beta-2 adrenergic receptorBinding affinity towards Beta-2 adrenergic receptor
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm020153s
DB04829 2386 16 None -218 45 Human 6.1 pKi = 6.1 Binding
Binding affinity towards Beta-2 adrenergic receptorBinding affinity towards Beta-2 adrenergic receptor
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm020153s
155526662 170610 0 None 3 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assay
ChEMBL 333 9 4 6 1.7 COc1ccccc1OCCNC[C@@H](O)Cc1ccc(O)c(O)c1 10.1021/acs.jmedchem.9b00349
CHEMBL4459109 170610 0 None 3 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assay
ChEMBL 333 9 4 6 1.7 COc1ccccc1OCCNC[C@@H](O)Cc1ccc(O)c(O)c1 10.1021/acs.jmedchem.9b00349
43634116 164252 1 None - 1 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]-DHA from Nb69-fused beta2 adrenergic receptor (unknown origin) expressed in Sf9 cell membranes after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-DHA from Nb69-fused beta2 adrenergic receptor (unknown origin) expressed in Sf9 cell membranes after 2 hrs by microbeta scintillation counting method
ChEMBL 303 4 1 1 5.1 CC(NC1CC(c2ccc(F)cc2)C1)c1ccc(Cl)cc1 10.1021/acs.jmedchem.7b01558
CHEMBL4218602 164252 1 None - 1 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]-DHA from Nb69-fused beta2 adrenergic receptor (unknown origin) expressed in Sf9 cell membranes after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-DHA from Nb69-fused beta2 adrenergic receptor (unknown origin) expressed in Sf9 cell membranes after 2 hrs by microbeta scintillation counting method
ChEMBL 303 4 1 1 5.1 CC(NC1CC(c2ccc(F)cc2)C1)c1ccc(Cl)cc1 10.1021/acs.jmedchem.7b01558
9827999 130369 0 None -7 2 Human 4.1 pKi = 4.1 Binding
Inhibition of 125 I-Iodocyanopindolol binding to Beta-2 adrenergic receptorInhibition of 125 I-Iodocyanopindolol binding to Beta-2 adrenergic receptor
ChEMBL 519 9 5 10 0.5 CS(=O)(=O)Nc1cc([C@@H](O)CNC2CCN(c3ccc(Cn4oc(=O)[nH]c4=O)cc3)CC2)ccc1O 10.1016/s0960-894x(01)00147-0
CHEMBL368584 130369 0 None -7 2 Human 4.1 pKi = 4.1 Binding
Inhibition of 125 I-Iodocyanopindolol binding to Beta-2 adrenergic receptorInhibition of 125 I-Iodocyanopindolol binding to Beta-2 adrenergic receptor
ChEMBL 519 9 5 10 0.5 CS(=O)(=O)Nc1cc([C@@H](O)CNC2CCN(c3ccc(Cn4oc(=O)[nH]c4=O)cc3)CC2)ccc1O 10.1016/s0960-894x(01)00147-0
155552760 173527 0 None -2 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H](-)CGP 12177 from human recombinant beta2 adrenoceptor after 120 mins by scintillation counting methodDisplacement of [3H](-)CGP 12177 from human recombinant beta2 adrenoceptor after 120 mins by scintillation counting method
ChEMBL 548 24 4 10 -0.2 C=CCc1ccccc1OCC(O)CNCCOCCOCCOCCOCCNC(=O)CS(=O)(=O)O 10.1039/C8MD00412A
CHEMBL4545079 173527 0 None -2 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H](-)CGP 12177 from human recombinant beta2 adrenoceptor after 120 mins by scintillation counting methodDisplacement of [3H](-)CGP 12177 from human recombinant beta2 adrenoceptor after 120 mins by scintillation counting method
ChEMBL 548 24 4 10 -0.2 C=CCc1ccccc1OCC(O)CNCCOCCOCCOCCOCCNC(=O)CS(=O)(=O)O 10.1039/C8MD00412A
4183 1986 62 None 2 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]cyanopindolol from human recombinant beta2 adrenergic receptor expressed in CHO cells by filtration assayDisplacement of [125I]cyanopindolol from human recombinant beta2 adrenergic receptor expressed in CHO cells by filtration assay
ChEMBL 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O 10.1021/jm100068m
6918554 1986 62 None 2 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]cyanopindolol from human recombinant beta2 adrenergic receptor expressed in CHO cells by filtration assayDisplacement of [125I]cyanopindolol from human recombinant beta2 adrenergic receptor expressed in CHO cells by filtration assay
ChEMBL 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O 10.1021/jm100068m
7455 1986 62 None 2 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]cyanopindolol from human recombinant beta2 adrenergic receptor expressed in CHO cells by filtration assayDisplacement of [125I]cyanopindolol from human recombinant beta2 adrenergic receptor expressed in CHO cells by filtration assay
ChEMBL 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O 10.1021/jm100068m
CHEMBL1095777 1986 62 None 2 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]cyanopindolol from human recombinant beta2 adrenergic receptor expressed in CHO cells by filtration assayDisplacement of [125I]cyanopindolol from human recombinant beta2 adrenergic receptor expressed in CHO cells by filtration assay
ChEMBL 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O 10.1021/jm100068m
DB05039 1986 62 None 2 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]cyanopindolol from human recombinant beta2 adrenergic receptor expressed in CHO cells by filtration assayDisplacement of [125I]cyanopindolol from human recombinant beta2 adrenergic receptor expressed in CHO cells by filtration assay
ChEMBL 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O 10.1021/jm100068m
11188590 77252 0 None 1 2 Human 7.1 pKi = 7.1 Binding
Binding affinity to human beta2-adrenoceptor by radioligand binding assayBinding affinity to human beta2-adrenoceptor by radioligand binding assay
ChEMBL 394 6 4 4 4.2 CCC1=C(CC)CC2=C(C1)CC(NC[C@H](O)c1ccc(O)c3[nH]c(=O)ccc13)C2 10.1016/j.bmcl.2012.07.096
CHEMBL2088202 77252 0 None 1 2 Human 7.1 pKi = 7.1 Binding
Binding affinity to human beta2-adrenoceptor by radioligand binding assayBinding affinity to human beta2-adrenoceptor by radioligand binding assay
ChEMBL 394 6 4 4 4.2 CCC1=C(CC)CC2=C(C1)CC(NC[C@H](O)c1ccc(O)c3[nH]c(=O)ccc13)C2 10.1016/j.bmcl.2012.07.096
73056756 103790 0 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-CGP-12177 from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-CGP-12177 from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 345 9 4 5 3.1 CCC[C@H](Cc1ccc(OC)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2013.11.030
CHEMBL3099663 103790 0 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-CGP-12177 from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-CGP-12177 from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 345 9 4 5 3.1 CCC[C@H](Cc1ccc(OC)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2013.11.030
44622849 195106 0 None 1 2 Human 5.1 pKi = 5.1 Binding
Inhibition of beta2 adrenergic receptorInhibition of beta2 adrenergic receptor
ChEMBL 293 2 1 5 1.7 Cc1nc2c3c(nc(Cc4ccccc4)n2n1)CCNCC3 10.1016/j.bmcl.2009.07.063
CHEMBL565547 195106 0 None 1 2 Human 5.1 pKi = 5.1 Binding
Inhibition of beta2 adrenergic receptorInhibition of beta2 adrenergic receptor
ChEMBL 293 2 1 5 1.7 Cc1nc2c3c(nc(Cc4ccccc4)n2n1)CCNCC3 10.1016/j.bmcl.2009.07.063
15580747 64816 0 None -3 3 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]-Iodopindolol from beta2-adrenergic receptor after 1.5 hrs by liquid scintillation countingDisplacement of [125I]-Iodopindolol from beta2-adrenergic receptor after 1.5 hrs by liquid scintillation counting
ChEMBL 397 8 2 7 2.3 COc1ccc2nc(-c3ccc(OCC(O)CNC(C)C)cc3)n(C)c(=O)c2c1 10.1016/j.bmcl.2011.06.106
CHEMBL1824264 64816 0 None -3 3 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]-Iodopindolol from beta2-adrenergic receptor after 1.5 hrs by liquid scintillation countingDisplacement of [125I]-Iodopindolol from beta2-adrenergic receptor after 1.5 hrs by liquid scintillation counting
ChEMBL 397 8 2 7 2.3 COc1ccc2nc(-c3ccc(OCC(O)CNC(C)C)cc3)n(C)c(=O)c2c1 10.1016/j.bmcl.2011.06.106
46889727 6556 0 None 3 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cells
ChEMBL 514 10 1 6 4.3 C=CCc1ccccc1OCC(O)CN1CCC(CN2C(=O)c3cccc4cc(OC)cc(c34)C2=O)CC1 10.1016/j.bmcl.2010.04.009
CHEMBL1083366 6556 0 None 3 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cells
ChEMBL 514 10 1 6 4.3 C=CCc1ccccc1OCC(O)CN1CCC(CN2C(=O)c3cccc4cc(OC)cc(c34)C2=O)CC1 10.1016/j.bmcl.2010.04.009
155524193 170317 0 None 22 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H](-)CGP 12177 from human recombinant beta2 adrenoceptor after 120 mins by scintillation counting methodDisplacement of [3H](-)CGP 12177 from human recombinant beta2 adrenoceptor after 120 mins by scintillation counting method
ChEMBL 685 25 7 11 0.1 CC(C)NCC(O)COc1ccccc1CCCSCC(=O)NCCOCCOCCNC(=O)C1C(C(=O)O)C(C(=O)O)C1C(=O)O 10.1039/C8MD00412A
CHEMBL4454523 170317 0 None 22 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H](-)CGP 12177 from human recombinant beta2 adrenoceptor after 120 mins by scintillation counting methodDisplacement of [3H](-)CGP 12177 from human recombinant beta2 adrenoceptor after 120 mins by scintillation counting method
ChEMBL 685 25 7 11 0.1 CC(C)NCC(O)COc1ccccc1CCCSCC(=O)NCCOCCOCCNC(=O)C1C(C(=O)O)C(C(=O)O)C1C(=O)O 10.1039/C8MD00412A
14485428 202489 0 None - 1 Mouse 4.1 pKi = 4.1 Binding
Ki value was determined by accumulation of c-AMP in S-49 mouse lymphoma cells (Beta2).Ki value was determined by accumulation of c-AMP in S-49 mouse lymphoma cells (Beta2).
ChEMBL 488 12 3 4 5.8 CC(CCCCC(=O)Nc1ccc(C(F)(F)F)cc1)NCC(O)COc1cccc2ccccc12 10.1021/jm00163a036
CHEMBL70840 202489 0 None - 1 Mouse 4.1 pKi = 4.1 Binding
Ki value was determined by accumulation of c-AMP in S-49 mouse lymphoma cells (Beta2).Ki value was determined by accumulation of c-AMP in S-49 mouse lymphoma cells (Beta2).
ChEMBL 488 12 3 4 5.8 CC(CCCCC(=O)Nc1ccc(C(F)(F)F)cc1)NCC(O)COc1cccc2ccccc12 10.1021/jm00163a036
24229559 163608 53 None - 1 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]-DHA from Nb80-fused beta2 adrenergic receptor (unknown origin) expressed in Sf9 cell membranes after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-DHA from Nb80-fused beta2 adrenergic receptor (unknown origin) expressed in Sf9 cell membranes after 2 hrs by microbeta scintillation counting method
ChEMBL 185 2 1 3 1.6 NCc1ccc(-c2ncccn2)cc1 10.1021/acs.jmedchem.7b01558
CHEMBL4210507 163608 53 None - 1 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]-DHA from Nb80-fused beta2 adrenergic receptor (unknown origin) expressed in Sf9 cell membranes after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-DHA from Nb80-fused beta2 adrenergic receptor (unknown origin) expressed in Sf9 cell membranes after 2 hrs by microbeta scintillation counting method
ChEMBL 185 2 1 3 1.6 NCc1ccc(-c2ncccn2)cc1 10.1021/acs.jmedchem.7b01558
43634116 164252 1 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-DHA from Nb80-fused beta2 adrenergic receptor (unknown origin) expressed in Sf9 cell membranes after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-DHA from Nb80-fused beta2 adrenergic receptor (unknown origin) expressed in Sf9 cell membranes after 2 hrs by microbeta scintillation counting method
ChEMBL 303 4 1 1 5.1 CC(NC1CC(c2ccc(F)cc2)C1)c1ccc(Cl)cc1 10.1021/acs.jmedchem.7b01558
CHEMBL4218602 164252 1 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-DHA from Nb80-fused beta2 adrenergic receptor (unknown origin) expressed in Sf9 cell membranes after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-DHA from Nb80-fused beta2 adrenergic receptor (unknown origin) expressed in Sf9 cell membranes after 2 hrs by microbeta scintillation counting method
ChEMBL 303 4 1 1 5.1 CC(NC1CC(c2ccc(F)cc2)C1)c1ccc(Cl)cc1 10.1021/acs.jmedchem.7b01558
90644139 111759 0 None 100 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assay
ChEMBL 424 10 5 6 4.2 CSc1ccc(Nc2ccc(CCNCC(O)c3ccc(O)c(CO)c3)cc2)cc1 10.1016/j.bmcl.2014.04.069
CHEMBL3290992 111759 0 None 100 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assay
ChEMBL 424 10 5 6 4.2 CSc1ccc(Nc2ccc(CCNCC(O)c3ccc(O)c(CO)c3)cc2)cc1 10.1016/j.bmcl.2014.04.069
155540000 172302 0 None -1 2 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assay
ChEMBL 349 10 4 7 1.5 COc1ccccc1OCCNC[C@@H](O)COc1ccc(O)c(O)c1 10.1021/acs.jmedchem.9b00349
CHEMBL4515498 172302 0 None -1 2 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assay
ChEMBL 349 10 4 7 1.5 COc1ccccc1OCCNC[C@@H](O)COc1ccc(O)c(O)c1 10.1021/acs.jmedchem.9b00349
146015362 932 6 None -63 3 Human 4.1 pKi = 4.1 Binding
Inhibition of I-iodocyanopindolol binding to human beta 2 adrenergic receptorsInhibition of I-iodocyanopindolol binding to human beta 2 adrenergic receptors
ChEMBL 421 8 4 6 2.2 C[C@H](Cc1ccc2c(c1)OC(O2)(C(=O)O)C(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1021/jm000544b
3462 932 6 None -63 3 Human 4.1 pKi = 4.1 Binding
Inhibition of I-iodocyanopindolol binding to human beta 2 adrenergic receptorsInhibition of I-iodocyanopindolol binding to human beta 2 adrenergic receptors
ChEMBL 421 8 4 6 2.2 C[C@H](Cc1ccc2c(c1)OC(O2)(C(=O)O)C(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1021/jm000544b
5486546 932 6 None -63 3 Human 4.1 pKi = 4.1 Binding
Inhibition of I-iodocyanopindolol binding to human beta 2 adrenergic receptorsInhibition of I-iodocyanopindolol binding to human beta 2 adrenergic receptors
ChEMBL 421 8 4 6 2.2 C[C@H](Cc1ccc2c(c1)OC(O2)(C(=O)O)C(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1021/jm000544b
CHEMBL1204876 932 6 None -63 3 Human 4.1 pKi = 4.1 Binding
Inhibition of I-iodocyanopindolol binding to human beta 2 adrenergic receptorsInhibition of I-iodocyanopindolol binding to human beta 2 adrenergic receptors
ChEMBL 421 8 4 6 2.2 C[C@H](Cc1ccc2c(c1)OC(O2)(C(=O)O)C(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1021/jm000544b
16737412 85341 0 None 3 2 Human 5.1 pKi = 5.1 Binding
Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.
ChEMBL 287 6 4 4 2.4 C[C@@H](Cc1ccccc1)NC[C@H](O)c1cc(O)cc(O)c1 nan
CHEMBL229388 85341 0 None 3 2 Human 5.1 pKi = 5.1 Binding
Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.
ChEMBL 287 6 4 4 2.4 C[C@@H](Cc1ccccc1)NC[C@H](O)c1cc(O)cc(O)c1 nan
59119472 111752 0 None 31 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assay
ChEMBL 418 9 5 5 4.0 OCc1cc(C(O)CNCCc2ccc(Nc3ccc4c(c3)CCC4)cc2)ccc1O 10.1016/j.bmcl.2014.04.069
CHEMBL3290986 111752 0 None 31 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assay
ChEMBL 418 9 5 5 4.0 OCc1cc(C(O)CNCCc2ccc(Nc3ccc4c(c3)CCC4)cc2)ccc1O 10.1016/j.bmcl.2014.04.069
3323563 76587 14 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]dihydroalprenolol from human ADRB2 expressed in HEK293T cells after 1 hr by liquid scintillation counterDisplacement of [3H]dihydroalprenolol from human ADRB2 expressed in HEK293T cells after 1 hr by liquid scintillation counter
ChEMBL 291 6 1 3 3.3 Cc1ccc(C(C)C)c(OCC(O)CN2CCCCC2)c1 10.1021/jm300280e
CHEMBL2070834 76587 14 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]dihydroalprenolol from human ADRB2 expressed in HEK293T cells after 1 hr by liquid scintillation counterDisplacement of [3H]dihydroalprenolol from human ADRB2 expressed in HEK293T cells after 1 hr by liquid scintillation counter
ChEMBL 291 6 1 3 3.3 Cc1ccc(C(C)C)c(OCC(O)CN2CCCCC2)c1 10.1021/jm300280e
16737412 85341 0 None 3 2 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 287 6 4 4 2.4 C[C@@H](Cc1ccccc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1021/jm070030d
CHEMBL229388 85341 0 None 3 2 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 287 6 4 4 2.4 C[C@@H](Cc1ccccc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1021/jm070030d
16737412 85341 0 None 3 2 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 287 6 4 4 2.4 C[C@@H](Cc1ccccc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1021/jm070030d
CHEMBL229388 85341 0 None 3 2 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 287 6 4 4 2.4 C[C@@H](Cc1ccccc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1021/jm070030d
46889772 6902 0 None -79 3 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cells
ChEMBL 563 8 2 6 5.2 COc1cc2c3c(cccc3c1)C(=O)N(CC1CCN(CC(O)COc3cccc4[nH]c5ccccc5c34)CC1)C2=O 10.1016/j.bmcl.2010.04.009
CHEMBL1084707 6902 0 None -79 3 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cells
ChEMBL 563 8 2 6 5.2 COc1cc2c3c(cccc3c1)C(=O)N(CC1CCN(CC(O)COc3cccc4[nH]c5ccccc5c34)CC1)C2=O 10.1016/j.bmcl.2010.04.009
44393937 168600 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity for human beta-2 adrenergic receptorBinding affinity for human beta-2 adrenergic receptor
ChEMBL 448 14 4 5 4.2 O=CNc1cc([C@@H](O)CNCCc2cccc(OCCCCc3ccccc3)c2)ccc1O 10.1016/j.bmcl.2004.06.086
CHEMBL440561 168600 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity for human beta-2 adrenergic receptorBinding affinity for human beta-2 adrenergic receptor
ChEMBL 448 14 4 5 4.2 O=CNc1cc([C@@H](O)CNCCc2cccc(OCCCCc3ccccc3)c2)ccc1O 10.1016/j.bmcl.2004.06.086
10349225 16192 0 None 40 2 Human 8.1 pKi = 8.1 Binding
Binding affinity for human Beta-2 adrenergic receptor expressed in CHO cells by radioligand competition binding assays using [125I]iodocyanopindolol (ICYP)Binding affinity for human Beta-2 adrenergic receptor expressed in CHO cells by radioligand competition binding assays using [125I]iodocyanopindolol (ICYP)
ChEMBL 564 3 4 4 3.7 CC(=O)Nc1c(I)cc(CC2NCCc3cc(O)c(O)cc32)cc1I 10.1021/jm960208o
CHEMBL122992 16192 0 None 40 2 Human 8.1 pKi = 8.1 Binding
Binding affinity for human Beta-2 adrenergic receptor expressed in CHO cells by radioligand competition binding assays using [125I]iodocyanopindolol (ICYP)Binding affinity for human Beta-2 adrenergic receptor expressed in CHO cells by radioligand competition binding assays using [125I]iodocyanopindolol (ICYP)
ChEMBL 564 3 4 4 3.7 CC(=O)Nc1c(I)cc(CC2NCCc3cc(O)c(O)cc32)cc1I 10.1021/jm960208o
52949934 17451 0 None 1 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 398 7 2 7 3.0 Cc1csc2ncnc(N3CCC(NCC(O)COc4ccccc4)CC3)c12 10.1016/j.bmcl.2010.08.039
CHEMBL1258372 17451 0 None 1 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 398 7 2 7 3.0 Cc1csc2ncnc(N3CCC(NCC(O)COc4ccccc4)CC3)c12 10.1016/j.bmcl.2010.08.039
3687256 6741 6 None 5 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cells
ChEMBL 500 8 1 5 5.0 Cc1ccc(C(C)C)c(OCC(O)CN2CCC(CN3C(=O)c4cccc5cccc(c45)C3=O)CC2)c1 10.1016/j.bmcl.2010.04.009
CHEMBL1083994 6741 6 None 5 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cells
ChEMBL 500 8 1 5 5.0 Cc1ccc(C(C)C)c(OCC(O)CN2CCC(CN3C(=O)c4cccc5cccc(c45)C3=O)CC2)c1 10.1016/j.bmcl.2010.04.009
46889767 6979 0 None 5 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cells
ChEMBL 400 9 1 5 2.4 C=CCc1ccccc1OCC(O)CN1CCC(CN2C(=O)CCCC2=O)CC1 10.1016/j.bmcl.2010.04.009
CHEMBL1085009 6979 0 None 5 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cells
ChEMBL 400 9 1 5 2.4 C=CCc1ccccc1OCC(O)CN1CCC(CN2C(=O)CCCC2=O)CC1 10.1016/j.bmcl.2010.04.009
4421983 7183 5 None -1 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cells
ChEMBL 484 9 1 5 4.3 C=CCc1ccccc1OCC(O)CN1CCC(CN2C(=O)c3cccc4cccc(c34)C2=O)CC1 10.1016/j.bmcl.2010.04.009
CHEMBL1086005 7183 5 None -1 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cells
ChEMBL 484 9 1 5 4.3 C=CCc1ccccc1OCC(O)CN1CCC(CN2C(=O)c3cccc4cccc(c34)C2=O)CC1 10.1016/j.bmcl.2010.04.009
145966568 163476 0 None - 1 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]-DHA from Nb80-fused beta2 adrenergic receptor (unknown origin) expressed in Sf9 cell membranes after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-DHA from Nb80-fused beta2 adrenergic receptor (unknown origin) expressed in Sf9 cell membranes after 2 hrs by microbeta scintillation counting method
ChEMBL 396 7 1 4 4.6 COc1ccc2c(c1)c(CCNCc1cc(OC(F)(F)F)ccc1F)cn2C 10.1021/acs.jmedchem.7b01558
CHEMBL4208846 163476 0 None - 1 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]-DHA from Nb80-fused beta2 adrenergic receptor (unknown origin) expressed in Sf9 cell membranes after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-DHA from Nb80-fused beta2 adrenergic receptor (unknown origin) expressed in Sf9 cell membranes after 2 hrs by microbeta scintillation counting method
ChEMBL 396 7 1 4 4.6 COc1ccc2c(c1)c(CCNCc1cc(OC(F)(F)F)ccc1F)cn2C 10.1021/acs.jmedchem.7b01558
122442272 137807 0 None -28 15 Human 6.1 pKi = 6.1 Binding
Binding affinity to human beta-2 adrenergic receptor by radioligand binding assayBinding affinity to human beta-2 adrenergic receptor by radioligand binding assay
ChEMBL 239 5 1 2 2.6 C=CCOc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769968 137807 0 None -28 15 Human 6.1 pKi = 6.1 Binding
Binding affinity to human beta-2 adrenergic receptor by radioligand binding assayBinding affinity to human beta-2 adrenergic receptor by radioligand binding assay
ChEMBL 239 5 1 2 2.6 C=CCOc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771384 137807 0 None -28 15 Human 6.1 pKi = 6.1 Binding
Binding affinity to human beta-2 adrenergic receptor by radioligand binding assayBinding affinity to human beta-2 adrenergic receptor by radioligand binding assay
ChEMBL 239 5 1 2 2.6 C=CCOc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
24936489 17321 0 None 1 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 476 8 3 8 4.1 Oc1ccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)cc1 10.1016/j.bmcl.2010.08.039
CHEMBL1257914 17321 0 None 1 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 476 8 3 8 4.1 Oc1ccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)cc1 10.1016/j.bmcl.2010.08.039
44423644 84970 0 None 13 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]CYP from human adrenergic beta 2 receptor transfected in CHO cells in presence of 100 uM GTPDisplacement of [125I]CYP from human adrenergic beta 2 receptor transfected in CHO cells in presence of 100 uM GTP
ChEMBL 426 10 2 7 2.6 CCOC(=O)COc1ccc(C[C@@H](C)NC[C@@H](O)c2cc(Br)no2)cc1 10.1016/j.bmc.2007.01.056
CHEMBL226348 84970 0 None 13 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]CYP from human adrenergic beta 2 receptor transfected in CHO cells in presence of 100 uM GTPDisplacement of [125I]CYP from human adrenergic beta 2 receptor transfected in CHO cells in presence of 100 uM GTP
ChEMBL 426 10 2 7 2.6 CCOC(=O)COc1ccc(C[C@@H](C)NC[C@@H](O)c2cc(Br)no2)cc1 10.1016/j.bmc.2007.01.056
14485407 102264 0 None - 1 Mouse 6.1 pKi = 6.1 Binding
Ki value was determined by accumulation of c-AMP in S-49 mouse lymphoma cells (Beta2).Ki value was determined by accumulation of c-AMP in S-49 mouse lymphoma cells (Beta2).
ChEMBL 441 13 4 5 3.9 CC(=O)Nc1ccc(OC[C@@H](O)CN[C@H](C)CCCCC(=O)Nc2ccc(C)cc2)cc1 10.1021/jm00163a036
CHEMBL305051 102264 0 None - 1 Mouse 6.1 pKi = 6.1 Binding
Ki value was determined by accumulation of c-AMP in S-49 mouse lymphoma cells (Beta2).Ki value was determined by accumulation of c-AMP in S-49 mouse lymphoma cells (Beta2).
ChEMBL 441 13 4 5 3.9 CC(=O)Nc1ccc(OC[C@@H](O)CN[C@H](C)CCCCC(=O)Nc2ccc(C)cc2)cc1 10.1021/jm00163a036
122442272 137807 0 None -28 15 Human 6.1 pKi = 6.1 Binding
Binding affinity to human beta-2 adrenergic receptor by radioligand binding assayBinding affinity to human beta-2 adrenergic receptor by radioligand binding assay
ChEMBL 239 5 1 2 2.6 C=CCOc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769968 137807 0 None -28 15 Human 6.1 pKi = 6.1 Binding
Binding affinity to human beta-2 adrenergic receptor by radioligand binding assayBinding affinity to human beta-2 adrenergic receptor by radioligand binding assay
ChEMBL 239 5 1 2 2.6 C=CCOc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771384 137807 0 None -28 15 Human 6.1 pKi = 6.1 Binding
Binding affinity to human beta-2 adrenergic receptor by radioligand binding assayBinding affinity to human beta-2 adrenergic receptor by radioligand binding assay
ChEMBL 239 5 1 2 2.6 C=CCOc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
10376053 13009 0 None -5 3 Guinea pig 6.1 pKi = 6.1 Binding
Binding affinity against Beta-2 adrenergic receptor was measured using [125I]CYP as radioligandBinding affinity against Beta-2 adrenergic receptor was measured using [125I]CYP as radioligand
ChEMBL 217 1 1 5 0.4 Cc1cnc(N2CCNCC2)c2nccn12 10.1021/jm00099a012
CHEMBL1190547 13009 0 None -5 3 Guinea pig 6.1 pKi = 6.1 Binding
Binding affinity against Beta-2 adrenergic receptor was measured using [125I]CYP as radioligandBinding affinity against Beta-2 adrenergic receptor was measured using [125I]CYP as radioligand
ChEMBL 217 1 1 5 0.4 Cc1cnc(N2CCNCC2)c2nccn12 10.1021/jm00099a012
CHEMBL541088 13009 0 None -5 3 Guinea pig 6.1 pKi = 6.1 Binding
Binding affinity against Beta-2 adrenergic receptor was measured using [125I]CYP as radioligandBinding affinity against Beta-2 adrenergic receptor was measured using [125I]CYP as radioligand
ChEMBL 217 1 1 5 0.4 Cc1cnc(N2CCNCC2)c2nccn12 10.1021/jm00099a012
10207209 168649 0 None -5 3 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]iodocyanopindolol from human cloned adrenergic beta-2 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human cloned adrenergic beta-2 receptor expressed in CHO cells
ChEMBL 500 12 4 7 3.3 COc1ccc([C@H](Cc2ccccc2)NC[C@H](O)Cc2ccc(O)c(NS(C)(=O)=O)c2)cc1OC 10.1016/j.bmcl.2007.05.030
CHEMBL440961 168649 0 None -5 3 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]iodocyanopindolol from human cloned adrenergic beta-2 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human cloned adrenergic beta-2 receptor expressed in CHO cells
ChEMBL 500 12 4 7 3.3 COc1ccc([C@H](Cc2ccccc2)NC[C@H](O)Cc2ccc(O)c(NS(C)(=O)=O)c2)cc1OC 10.1016/j.bmcl.2007.05.030
145966568 163476 0 None - 1 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]-DHA from Nb69-fused beta2 adrenergic receptor (unknown origin) expressed in Sf9 cell membranes after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-DHA from Nb69-fused beta2 adrenergic receptor (unknown origin) expressed in Sf9 cell membranes after 2 hrs by microbeta scintillation counting method
ChEMBL 396 7 1 4 4.6 COc1ccc2c(c1)c(CCNCc1cc(OC(F)(F)F)ccc1F)cn2C 10.1021/acs.jmedchem.7b01558
CHEMBL4208846 163476 0 None - 1 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]-DHA from Nb69-fused beta2 adrenergic receptor (unknown origin) expressed in Sf9 cell membranes after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-DHA from Nb69-fused beta2 adrenergic receptor (unknown origin) expressed in Sf9 cell membranes after 2 hrs by microbeta scintillation counting method
ChEMBL 396 7 1 4 4.6 COc1ccc2c(c1)c(CCNCc1cc(OC(F)(F)F)ccc1F)cn2C 10.1021/acs.jmedchem.7b01558
10442852 11095 0 None 1 2 Bovine 6.1 pKi = 6.1 Binding
Binding affinity against beta-2-adrenergic receptor in bovine lungBinding affinity against beta-2-adrenergic receptor in bovine lung
ChEMBL 202 6 2 4 1.1 CCCO/N=C/C(O)CNC(C)(C)C 10.1021/jm00036a018
CHEMBL1178755 11095 0 None 1 2 Bovine 6.1 pKi = 6.1 Binding
Binding affinity against beta-2-adrenergic receptor in bovine lungBinding affinity against beta-2-adrenergic receptor in bovine lung
ChEMBL 202 6 2 4 1.1 CCCO/N=C/C(O)CNC(C)(C)C 10.1021/jm00036a018
CHEMBL39706 11095 0 None 1 2 Bovine 6.1 pKi = 6.1 Binding
Binding affinity against beta-2-adrenergic receptor in bovine lungBinding affinity against beta-2-adrenergic receptor in bovine lung
ChEMBL 202 6 2 4 1.1 CCCO/N=C/C(O)CNC(C)(C)C 10.1021/jm00036a018
127047221 139387 0 None -3 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cellsDisplacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells
ChEMBL 319 8 4 6 1.8 COc1ccccc1OCCNC[C@@H](O)c1ccc(O)c(O)c1 10.1016/j.bmc.2016.04.028
CHEMBL3799593 139387 0 None -3 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cellsDisplacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells
ChEMBL 319 8 4 6 1.8 COc1ccccc1OCCNC[C@@H](O)c1ccc(O)c(O)c1 10.1016/j.bmc.2016.04.028
130442572 171332 0 None -181 24 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-CGP12177 from recombinant human beta2 adrenergic receptor expressed in HEK Flp-In cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-CGP12177 from recombinant human beta2 adrenergic receptor expressed in HEK Flp-In cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 395 3 0 5 6.0 FC(F)(F)c1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4469848 171332 0 None -181 24 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-CGP12177 from recombinant human beta2 adrenergic receptor expressed in HEK Flp-In cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-CGP12177 from recombinant human beta2 adrenergic receptor expressed in HEK Flp-In cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 395 3 0 5 6.0 FC(F)(F)c1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
6603867 101511 16 None -43651 7 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cellsDisplacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells
ChEMBL 247 5 1 2 3.4 CCCN(CCC)[C@@H]1CCc2ccc(O)cc2C1 10.1016/j.bmc.2016.04.028
CHEMBL301559 101511 16 None -43651 7 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cellsDisplacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells
ChEMBL 247 5 1 2 3.4 CCCN(CCC)[C@@H]1CCc2ccc(O)cc2C1 10.1016/j.bmc.2016.04.028
25023950 176368 0 None - 1 Golden hamster 6.1 pKi = 6.1 Binding
Displacement of [125I](-)-iodopindolol from adrenergic beta2 receptor in Syrian hamster DDT1 MF2 cellsDisplacement of [125I](-)-iodopindolol from adrenergic beta2 receptor in Syrian hamster DDT1 MF2 cells
ChEMBL 517 13 8 13 -0.8 O=CNc1cc(C(O)CNCCCCNc2ncnc3c2ncn3[C@@H]2O[C@H](CO)[C@@H](O)[C@H]2O)ccc1O 10.1021/jm800613s
CHEMBL462273 176368 0 None - 1 Golden hamster 6.1 pKi = 6.1 Binding
Displacement of [125I](-)-iodopindolol from adrenergic beta2 receptor in Syrian hamster DDT1 MF2 cellsDisplacement of [125I](-)-iodopindolol from adrenergic beta2 receptor in Syrian hamster DDT1 MF2 cells
ChEMBL 517 13 8 13 -0.8 O=CNc1cc(C(O)CNCCCCNc2ncnc3c2ncn3[C@@H]2O[C@H](CO)[C@@H](O)[C@H]2O)ccc1O 10.1021/jm800613s
52943770 17170 0 None 1 3 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 492 8 4 9 3.8 Oc1ccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)cc1O 10.1016/j.bmcl.2010.08.039
CHEMBL1257438 17170 0 None 1 3 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 492 8 4 9 3.8 Oc1ccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)cc1O 10.1016/j.bmcl.2010.08.039
44361777 118062 0 None 3 2 Dog 7.1 pKi = 7.1 Binding
Beta-2 adrenergic receptor binding affinity by measuring the displacement of [3H]DHA binding in rat lungBeta-2 adrenergic receptor binding affinity by measuring the displacement of [3H]DHA binding in rat lung
ChEMBL 429 7 2 7 2.3 COc1ccccc1N1CCN(CC(O)COc2cccc3c2SCC(=O)N3)CC1 10.1016/s0960-894x(00)00016-0
CHEMBL341614 118062 0 None 3 2 Dog 7.1 pKi = 7.1 Binding
Beta-2 adrenergic receptor binding affinity by measuring the displacement of [3H]DHA binding in rat lungBeta-2 adrenergic receptor binding affinity by measuring the displacement of [3H]DHA binding in rat lung
ChEMBL 429 7 2 7 2.3 COc1ccccc1N1CCN(CC(O)COc2cccc3c2SCC(=O)N3)CC1 10.1016/s0960-894x(00)00016-0
52948792 17523 0 None 1 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 488 9 2 7 4.9 CCc1ccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)cc1 10.1016/j.bmcl.2010.08.039
CHEMBL1258596 17523 0 None 1 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 488 9 2 7 4.9 CCc1ccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)cc1 10.1016/j.bmcl.2010.08.039
24885648 16940 0 None 1 3 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 460 8 2 7 4.4 OC(CNC1CCN(c2ncnc3scc(-c4ccccc4)c23)CC1)COc1ccccc1 10.1016/j.bmcl.2010.08.039
CHEMBL1255596 16940 0 None 1 3 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 460 8 2 7 4.4 OC(CNC1CCN(c2ncnc3scc(-c4ccccc4)c23)CC1)COc1ccccc1 10.1016/j.bmcl.2010.08.039
46889768 6981 0 None 27 3 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cells
ChEMBL 402 8 1 5 2.8 CC(C)c1ccccc1OCC(O)CN1CCC(CN2C(=O)CCCC2=O)CC1 10.1016/j.bmcl.2010.04.009
CHEMBL1085010 6981 0 None 27 3 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta2 receptor expressed in CHOK1 cells
ChEMBL 402 8 1 5 2.8 CC(C)c1ccccc1OCC(O)CN1CCC(CN2C(=O)CCCC2=O)CC1 10.1016/j.bmcl.2010.04.009
2299314 55791 4 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]DHA from beta2-AR (unknown origin) expressed in baculovirus infected sf9 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]DHA from beta2-AR (unknown origin) expressed in baculovirus infected sf9 cell membranes after 1 hr by scintillation counting method
ChEMBL 271 8 1 3 3.0 COCCNCCOc1ccccc1-c1ccccc1 10.1021/acsmedchemlett.6b00363
CHEMBL1625333 55791 4 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]DHA from beta2-AR (unknown origin) expressed in baculovirus infected sf9 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]DHA from beta2-AR (unknown origin) expressed in baculovirus infected sf9 cell membranes after 1 hr by scintillation counting method
ChEMBL 271 8 1 3 3.0 COCCNCCOc1ccccc1-c1ccccc1 10.1021/acsmedchemlett.6b00363
2977358 55877 3 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]DHA from beta2-AR (unknown origin) expressed in baculovirus infected sf9 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]DHA from beta2-AR (unknown origin) expressed in baculovirus infected sf9 cell membranes after 1 hr by scintillation counting method
ChEMBL 271 7 2 3 2.7 CC(O)CNCCOc1ccccc1-c1ccccc1 10.1021/acsmedchemlett.6b00363
CHEMBL1626224 55877 3 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]DHA from beta2-AR (unknown origin) expressed in baculovirus infected sf9 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]DHA from beta2-AR (unknown origin) expressed in baculovirus infected sf9 cell membranes after 1 hr by scintillation counting method
ChEMBL 271 7 2 3 2.7 CC(O)CNCCOc1ccccc1-c1ccccc1 10.1021/acsmedchemlett.6b00363
3146476 69453 5 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]DHA from beta2-AR (unknown origin) expressed in baculovirus infected sf9 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]DHA from beta2-AR (unknown origin) expressed in baculovirus infected sf9 cell membranes after 1 hr by scintillation counting method
ChEMBL 333 2 0 2 4.9 CCN1C(=Cc2sc3ccccc3[n+]2C)C=Cc2cccc(C)c21 10.1021/acsmedchemlett.6b00363
5767654 69453 5 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]DHA from beta2-AR (unknown origin) expressed in baculovirus infected sf9 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]DHA from beta2-AR (unknown origin) expressed in baculovirus infected sf9 cell membranes after 1 hr by scintillation counting method
ChEMBL 333 2 0 2 4.9 CCN1C(=Cc2sc3ccccc3[n+]2C)C=Cc2cccc(C)c21 10.1021/acsmedchemlett.6b00363
6248042 69453 5 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]DHA from beta2-AR (unknown origin) expressed in baculovirus infected sf9 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]DHA from beta2-AR (unknown origin) expressed in baculovirus infected sf9 cell membranes after 1 hr by scintillation counting method
ChEMBL 333 2 0 2 4.9 CCN1C(=Cc2sc3ccccc3[n+]2C)C=Cc2cccc(C)c21 10.1021/acsmedchemlett.6b00363
CHEMBL193627 69453 5 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]DHA from beta2-AR (unknown origin) expressed in baculovirus infected sf9 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]DHA from beta2-AR (unknown origin) expressed in baculovirus infected sf9 cell membranes after 1 hr by scintillation counting method
ChEMBL 333 2 0 2 4.9 CCN1C(=Cc2sc3ccccc3[n+]2C)C=Cc2cccc(C)c21 10.1021/acsmedchemlett.6b00363
CHEMBL584458 69453 5 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]DHA from beta2-AR (unknown origin) expressed in baculovirus infected sf9 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]DHA from beta2-AR (unknown origin) expressed in baculovirus infected sf9 cell membranes after 1 hr by scintillation counting method
ChEMBL 333 2 0 2 4.9 CCN1C(=Cc2sc3ccccc3[n+]2C)C=Cc2cccc(C)c21 10.1021/acsmedchemlett.6b00363
6460058 155458 5 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]DHA from beta2-AR (unknown origin) expressed in baculovirus infected sf9 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]DHA from beta2-AR (unknown origin) expressed in baculovirus infected sf9 cell membranes after 1 hr by scintillation counting method
ChEMBL 241 6 1 2 3.3 CCNCCOc1ccccc1-c1ccccc1 10.1021/acsmedchemlett.6b00363
CHEMBL4062049 155458 5 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]DHA from beta2-AR (unknown origin) expressed in baculovirus infected sf9 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]DHA from beta2-AR (unknown origin) expressed in baculovirus infected sf9 cell membranes after 1 hr by scintillation counting method
ChEMBL 241 6 1 2 3.3 CCNCCOc1ccccc1-c1ccccc1 10.1021/acsmedchemlett.6b00363
93382180 156727 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]DHA from beta2-AR (unknown origin) expressed in baculovirus infected sf9 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]DHA from beta2-AR (unknown origin) expressed in baculovirus infected sf9 cell membranes after 1 hr by scintillation counting method
ChEMBL 325 3 1 5 3.5 Cc1cc(O)c(CN2CCCC2)c2c1C(=O)/C(=C\c1ccco1)O2 10.1021/acsmedchemlett.6b00363
CHEMBL4076830 156727 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]DHA from beta2-AR (unknown origin) expressed in baculovirus infected sf9 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]DHA from beta2-AR (unknown origin) expressed in baculovirus infected sf9 cell membranes after 1 hr by scintillation counting method
ChEMBL 325 3 1 5 3.5 Cc1cc(O)c(CN2CCCC2)c2c1C(=O)/C(=C\c1ccco1)O2 10.1021/acsmedchemlett.6b00363
137660459 158713 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]DHA from beta2-AR (unknown origin) expressed in baculovirus infected sf9 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]DHA from beta2-AR (unknown origin) expressed in baculovirus infected sf9 cell membranes after 1 hr by scintillation counting method
ChEMBL 337 8 2 6 1.9 CCOC(=O)C1Oc2cccc(OCC(O)CNC(C)C)c2C1C 10.1021/acsmedchemlett.6b00363
CHEMBL4099306 158713 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]DHA from beta2-AR (unknown origin) expressed in baculovirus infected sf9 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]DHA from beta2-AR (unknown origin) expressed in baculovirus infected sf9 cell membranes after 1 hr by scintillation counting method
ChEMBL 337 8 2 6 1.9 CCOC(=O)C1Oc2cccc(OCC(O)CNC(C)C)c2C1C 10.1021/acsmedchemlett.6b00363
913103 16269 2 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of radioligand from human adrenergic beta2 receptorDisplacement of radioligand from human adrenergic beta2 receptor
ChEMBL 335 8 2 6 2.7 CCOC(=O)c1oc2cccc(OC[C@@H](O)CNC(C)C)c2c1C 10.1021/jm200371q
CHEMBL1233771 16269 2 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of radioligand from human adrenergic beta2 receptorDisplacement of radioligand from human adrenergic beta2 receptor
ChEMBL 335 8 2 6 2.7 CCOC(=O)c1oc2cccc(OC[C@@H](O)CNC(C)C)c2c1C 10.1021/jm200371q
10411388 65990 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity for human beta-2 adrenergic receptorBinding affinity for human beta-2 adrenergic receptor
ChEMBL 448 14 4 5 4.2 O=CNc1cc([C@@H](O)CNCCc2ccc(OCCCCc3ccccc3)cc2)ccc1O 10.1016/j.bmcl.2004.06.086
CHEMBL185052 65990 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity for human beta-2 adrenergic receptorBinding affinity for human beta-2 adrenergic receptor
ChEMBL 448 14 4 5 4.2 O=CNc1cc([C@@H](O)CNCCc2ccc(OCCCCc3ccccc3)cc2)ccc1O 10.1016/j.bmcl.2004.06.086
49864377 15439 0 None 12 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptorDisplacement of [3H]CGP12177 from human beta2 adrenoceptor
ChEMBL 356 4 4 5 3.0 O=c1[nH]c2c(O)ccc([C@@H](O)CN[C@@H]3CCCc4ccccc43)c2s1 10.1016/j.bmcl.2010.06.136
CHEMBL1221634 15439 0 None 12 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]CGP12177 from human beta2 adrenoceptorDisplacement of [3H]CGP12177 from human beta2 adrenoceptor
ChEMBL 356 4 4 5 3.0 O=c1[nH]c2c(O)ccc([C@@H](O)CN[C@@H]3CCCc4ccccc43)c2s1 10.1016/j.bmcl.2010.06.136
16735261 85292 0 None 47 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 317 7 4 5 2.4 COc1ccc(C[C@@H](C)NC[C@@H](O)c2cc(O)cc(O)c2)cc1 10.1016/j.bmc.2013.11.030
CHEMBL228998 85292 0 None 47 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 317 7 4 5 2.4 COc1ccc(C[C@@H](C)NC[C@@H](O)c2cc(O)cc(O)c2)cc1 10.1016/j.bmc.2013.11.030
68770 44384 49 None -1 2 Human 6.1 pKi = 6.1 Binding
Binding affinity to beta2 adrenergic receptor (unknown origin) by radioligand binding assayBinding affinity to beta2 adrenergic receptor (unknown origin) by radioligand binding assay
ChEMBL 363 7 4 4 3.3 CC(C)(C)NCC(O)COc1ccc(NC(=O)NC2CCCCC2)cc1 10.1021/acsmedchemlett.9b00075
CHEMBL152067 44384 49 None -1 2 Human 6.1 pKi = 6.1 Binding
Binding affinity to beta2 adrenergic receptor (unknown origin) by radioligand binding assayBinding affinity to beta2 adrenergic receptor (unknown origin) by radioligand binding assay
ChEMBL 363 7 4 4 3.3 CC(C)(C)NCC(O)COc1ccc(NC(=O)NC2CCCCC2)cc1 10.1021/acsmedchemlett.9b00075
14485421 202457 0 None - 1 Mouse 5.0 pKi = 5.0 Binding
Ki value was determined by accumulation of c-AMP in S-49 mouse lymphoma cells (Beta2).Ki value was determined by accumulation of c-AMP in S-49 mouse lymphoma cells (Beta2).
ChEMBL 434 12 3 4 5.1 Cc1ccc(NC(=O)CCCC[C@@H](C)NC[C@H](O)COc2cccc3ccccc23)cc1 10.1021/jm00163a036
CHEMBL70679 202457 0 None - 1 Mouse 5.0 pKi = 5.0 Binding
Ki value was determined by accumulation of c-AMP in S-49 mouse lymphoma cells (Beta2).Ki value was determined by accumulation of c-AMP in S-49 mouse lymphoma cells (Beta2).
ChEMBL 434 12 3 4 5.1 Cc1ccc(NC(=O)CCCC[C@@H](C)NC[C@H](O)COc2cccc3ccccc23)cc1 10.1021/jm00163a036
16735261 85292 0 None 47 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 317 7 4 5 2.4 COc1ccc(C[C@@H](C)NC[C@@H](O)c2cc(O)cc(O)c2)cc1 10.1016/j.bmc.2013.11.030
CHEMBL228998 85292 0 None 47 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysisDisplacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
ChEMBL 317 7 4 5 2.4 COc1ccc(C[C@@H](C)NC[C@@H](O)c2cc(O)cc(O)c2)cc1 10.1016/j.bmc.2013.11.030
155543195 172707 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assay
ChEMBL 317 9 3 5 2.7 COc1ccccc1OCCNCCCc1ccc(O)c(O)c1 10.1021/acs.jmedchem.9b00349
CHEMBL4525632 172707 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assay
ChEMBL 317 9 3 5 2.7 COc1ccccc1OCCNCCCc1ccc(O)c(O)c1 10.1021/acs.jmedchem.9b00349
3042920 203289 10 None 1 2 Bovine 5.0 pKi = 5.0 Binding
Compound was evaluated for beta adrenergic binding affinity towards beta-2 receptor of bovine lungCompound was evaluated for beta adrenergic binding affinity towards beta-2 receptor of bovine lung
ChEMBL 195 1 3 4 0.8 Oc1ccc(C2CNCCO2)cc1O 10.1021/jm00084a006
CHEMBL7681 203289 10 None 1 2 Bovine 5.0 pKi = 5.0 Binding
Compound was evaluated for beta adrenergic binding affinity towards beta-2 receptor of bovine lungCompound was evaluated for beta adrenergic binding affinity towards beta-2 receptor of bovine lung
ChEMBL 195 1 3 4 0.8 Oc1ccc(C2CNCCO2)cc1O 10.1021/jm00084a006
13599050 96504 2 None -1 2 Bovine 4.0 pKi = 4.0 Binding
Compound was evaluated for beta adrenergic binding affinity towards Beta-2 adrenergic receptor of bovine lungCompound was evaluated for beta adrenergic binding affinity towards Beta-2 adrenergic receptor of bovine lung
ChEMBL 251 2 3 4 1.8 CC(C)N1CCCC(O)(c2ccc(O)c(O)c2)C1 10.1021/jm00084a006
CHEMBL266290 96504 2 None -1 2 Bovine 4.0 pKi = 4.0 Binding
Compound was evaluated for beta adrenergic binding affinity towards Beta-2 adrenergic receptor of bovine lungCompound was evaluated for beta adrenergic binding affinity towards Beta-2 adrenergic receptor of bovine lung
ChEMBL 251 2 3 4 1.8 CC(C)N1CCCC(O)(c2ccc(O)c(O)c2)C1 10.1021/jm00084a006
14485409 202265 0 None - 1 Mouse 5.0 pKi = 5.0 Binding
Ki value was determined by accumulation of c-AMP in S-49 mouse lymphoma cells (Beta2).Ki value was determined by accumulation of c-AMP in S-49 mouse lymphoma cells (Beta2).
ChEMBL 441 13 4 5 3.9 CC(=O)Nc1ccc(OC[C@H](O)CN[C@@H](C)CCCCC(=O)Nc2ccc(C)cc2)cc1 10.1021/jm00163a036
CHEMBL69449 202265 0 None - 1 Mouse 5.0 pKi = 5.0 Binding
Ki value was determined by accumulation of c-AMP in S-49 mouse lymphoma cells (Beta2).Ki value was determined by accumulation of c-AMP in S-49 mouse lymphoma cells (Beta2).
ChEMBL 441 13 4 5 3.9 CC(=O)Nc1ccc(OC[C@H](O)CN[C@@H](C)CCCCC(=O)Nc2ccc(C)cc2)cc1 10.1021/jm00163a036
16735274 159476 0 None 1 2 Human 5.0 pKi = 5.0 Binding
Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.
ChEMBL 267 8 4 4 2.7 CCCCC[C@@H](C)NC[C@H](O)c1cc(O)cc(O)c1 nan
CHEMBL4108123 159476 0 None 1 2 Human 5.0 pKi = 5.0 Binding
Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.Beta1-AR Binding Assay: Beta1-AR binding was done on rat cortical membrane following a previously described procedure (Beer et al., Biochem. Pharmacol. 37: 1145-1151, 1988). In brief, male Sprague-Dawley rats weighing 250-350 g were decapitated and their brains quickly removed. The cerebral cortices were dissected on ice, weighed and promptly transferred to a 50 ml test tube containing approximately 30 ml of 50 mM Tris-HCl, pH 7.8 (at room temperature). The tissues were homogenized with a polytron and centrifuged at 20,000xg for 12 min at 4° C. The pellet was washed again in the same manner and resuspended at a concentration of 20 mg (original wet wt) per 1 ml in the assay buffer (20 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, 0.1 mM ascorbic acid at pH 7.8). To block the beta2 sites present in the cortical membrane preparation, 30 nM ICI 118-551 was also added to the assay buffer. To wells containing 100 ul of the test drug and 100 ul of [3H]CGP-12177 (1.4 nM final concentration), 0.8 ml of tissue homogenate was added. After 2 hours at 25° C., the incubation was terminated by rapid filtration. Nonspecific binding was determined by 10 uM propranolol.
ChEMBL 267 8 4 4 2.7 CCCCC[C@@H](C)NC[C@H](O)c1cc(O)cc(O)c1 nan
44424578 165482 0 None 1 2 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 253 7 4 4 2.3 CCCC[C@@H](C)NC[C@H](O)c1cc(O)cc(O)c1 10.1021/jm070030d
CHEMBL425658 165482 0 None 1 2 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 253 7 4 4 2.3 CCCC[C@@H](C)NC[C@H](O)c1cc(O)cc(O)c1 10.1021/jm070030d
24937140 17487 0 None 3 2 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 490 9 3 8 3.8 OCc1ccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)cc1 10.1016/j.bmcl.2010.08.039
CHEMBL1258483 17487 0 None 3 2 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 490 9 3 8 3.8 OCc1ccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)cc1 10.1016/j.bmcl.2010.08.039
75201901 165861 14 None -691 24 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-CGP12177 from recombinant human beta2 adrenergic receptor expressed in HEK Flp-In cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-CGP12177 from recombinant human beta2 adrenergic receptor expressed in HEK Flp-In cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4277264 165861 14 None -691 24 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-CGP12177 from recombinant human beta2 adrenergic receptor expressed in HEK Flp-In cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-CGP12177 from recombinant human beta2 adrenergic receptor expressed in HEK Flp-In cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
44424578 165482 0 None 1 2 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 253 7 4 4 2.3 CCCC[C@@H](C)NC[C@H](O)c1cc(O)cc(O)c1 10.1021/jm070030d
CHEMBL425658 165482 0 None 1 2 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells
ChEMBL 253 7 4 4 2.3 CCCC[C@@H](C)NC[C@H](O)c1cc(O)cc(O)c1 10.1021/jm070030d
24936763 17419 0 None 3 3 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 520 9 4 9 3.9 Cc1c(-c2ccccc2)sc2ncnc(N3CCC(NCC(O)COc4ccc(O)c(CO)c4)CC3)c12 10.1016/j.bmcl.2010.08.039
CHEMBL1258260 17419 0 None 3 3 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 520 9 4 9 3.9 Cc1c(-c2ccccc2)sc2ncnc(N3CCC(NCC(O)COc4ccc(O)c(CO)c4)CC3)c12 10.1016/j.bmcl.2010.08.039
145977755 162988 0 None - 1 Human 4.0 pKi = 4.0 Binding
Displacement of [3H]-DHA from Nb80-fused beta2 adrenergic receptor (unknown origin) expressed in Sf9 cell membranes after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-DHA from Nb80-fused beta2 adrenergic receptor (unknown origin) expressed in Sf9 cell membranes after 2 hrs by microbeta scintillation counting method
ChEMBL 300 6 2 5 3.2 OCC(NCc1ccc(-c2nccs2)cc1)c1ccco1 10.1021/acs.jmedchem.7b01558
CHEMBL4202968 162988 0 None - 1 Human 4.0 pKi = 4.0 Binding
Displacement of [3H]-DHA from Nb80-fused beta2 adrenergic receptor (unknown origin) expressed in Sf9 cell membranes after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-DHA from Nb80-fused beta2 adrenergic receptor (unknown origin) expressed in Sf9 cell membranes after 2 hrs by microbeta scintillation counting method
ChEMBL 300 6 2 5 3.2 OCC(NCc1ccc(-c2nccs2)cc1)c1ccco1 10.1021/acs.jmedchem.7b01558
2249 509 106 None -33 12 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-CGP12177 from human beta2 ADR expressed in HEK293T cell membrane after 90 mins by scintillation countingDisplacement of [3H]-CGP12177 from human beta2 ADR expressed in HEK293T cell membrane after 90 mins by scintillation counting
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1021/acs.jmedchem.8b00625
255 509 106 None -33 12 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-CGP12177 from human beta2 ADR expressed in HEK293T cell membrane after 90 mins by scintillation countingDisplacement of [3H]-CGP12177 from human beta2 ADR expressed in HEK293T cell membrane after 90 mins by scintillation counting
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1021/acs.jmedchem.8b00625
548 509 106 None -33 12 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-CGP12177 from human beta2 ADR expressed in HEK293T cell membrane after 90 mins by scintillation countingDisplacement of [3H]-CGP12177 from human beta2 ADR expressed in HEK293T cell membrane after 90 mins by scintillation counting
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1021/acs.jmedchem.8b00625
CHEMBL24 509 106 None -33 12 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-CGP12177 from human beta2 ADR expressed in HEK293T cell membrane after 90 mins by scintillation countingDisplacement of [3H]-CGP12177 from human beta2 ADR expressed in HEK293T cell membrane after 90 mins by scintillation counting
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1021/acs.jmedchem.8b00625
DB00335 509 106 None -33 12 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-CGP12177 from human beta2 ADR expressed in HEK293T cell membrane after 90 mins by scintillation countingDisplacement of [3H]-CGP12177 from human beta2 ADR expressed in HEK293T cell membrane after 90 mins by scintillation counting
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1021/acs.jmedchem.8b00625
137640201 156407 2 None -7585 13 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]CGP12177 from human recombinant beta2 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by beta counting methodDisplacement of [3H]CGP12177 from human recombinant beta2 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by beta counting method
ChEMBL 362 6 0 2 4.3 O=C1CCc2ccccc2N1CCCN1CCC(Cc2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4072818 156407 2 None -7585 13 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]CGP12177 from human recombinant beta2 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by beta counting methodDisplacement of [3H]CGP12177 from human recombinant beta2 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by beta counting method
ChEMBL 362 6 0 2 4.3 O=C1CCc2ccccc2N1CCCN1CCC(Cc2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
24937016 17560 0 None 1 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 400 7 3 8 2.4 Oc1ccc(OCC(O)CNC2CCN(c3ncnc4ccsc34)CC2)cc1 10.1016/j.bmcl.2010.08.039
CHEMBL1258706 17560 0 None 1 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells
ChEMBL 400 7 3 8 2.4 Oc1ccc(OCC(O)CNC2CCN(c3ncnc4ccsc34)CC2)cc1 10.1016/j.bmcl.2010.08.039
1960 2805 64 None -549 26 Human 4.0 pKi = 4.0 Binding
Displacement of [3H]prazosin from human adrenergic beta2 receptor expressed in CHO cell membraneDisplacement of [3H]prazosin from human adrenergic beta2 receptor expressed in CHO cell membrane
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1016/j.bmc.2009.10.015
439260 2805 64 None -549 26 Human 4.0 pKi = 4.0 Binding
Displacement of [3H]prazosin from human adrenergic beta2 receptor expressed in CHO cell membraneDisplacement of [3H]prazosin from human adrenergic beta2 receptor expressed in CHO cell membrane
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1016/j.bmc.2009.10.015
505 2805 64 None -549 26 Human 4.0 pKi = 4.0 Binding
Displacement of [3H]prazosin from human adrenergic beta2 receptor expressed in CHO cell membraneDisplacement of [3H]prazosin from human adrenergic beta2 receptor expressed in CHO cell membrane
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1016/j.bmc.2009.10.015
CHEMBL1437 2805 64 None -549 26 Human 4.0 pKi = 4.0 Binding
Displacement of [3H]prazosin from human adrenergic beta2 receptor expressed in CHO cell membraneDisplacement of [3H]prazosin from human adrenergic beta2 receptor expressed in CHO cell membrane
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1016/j.bmc.2009.10.015
DB00368 2805 64 None -549 26 Human 4.0 pKi = 4.0 Binding
Displacement of [3H]prazosin from human adrenergic beta2 receptor expressed in CHO cell membraneDisplacement of [3H]prazosin from human adrenergic beta2 receptor expressed in CHO cell membrane
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1016/j.bmc.2009.10.015
155286359 185541 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity to beta2 adrenoceptor (unknown origin)Binding affinity to beta2 adrenoceptor (unknown origin)
ChEMBL 255 4 4 4 1.4 Oc1ccc2c(c1O)CC[C@@H](NCCCF)[C@@H]2O 10.1021/acs.jmedchem.0c01195
CHEMBL4871979 185541 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity to beta2 adrenoceptor (unknown origin)Binding affinity to beta2 adrenoceptor (unknown origin)
ChEMBL 255 4 4 4 1.4 Oc1ccc2c(c1O)CC[C@@H](NCCCF)[C@@H]2O 10.1021/acs.jmedchem.0c01195
118710938 113236 0 None -1 3 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assay
ChEMBL 376 5 4 5 3.7 O=c1[nH]c2c(O)ccc([C@@H](O)CN[C@H]3CCC[C@H]3C3CCCCC3)c2s1 10.1016/j.bmcl.2014.06.014
CHEMBL3323656 113236 0 None -1 3 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assay
ChEMBL 376 5 4 5 3.7 O=c1[nH]c2c(O)ccc([C@@H](O)CN[C@H]3CCC[C@H]3C3CCCCC3)c2s1 10.1016/j.bmcl.2014.06.014
127045855 139121 0 None 1 6 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assay
ChEMBL 319 8 4 6 1.8 COc1ccccc1OCCNC[C@H](O)c1ccc(O)c(O)c1 10.1021/acs.jmedchem.9b00349
CHEMBL3797876 139121 0 None 1 6 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assay
ChEMBL 319 8 4 6 1.8 COc1ccccc1OCCNC[C@H](O)c1ccc(O)c(O)c1 10.1021/acs.jmedchem.9b00349
127045855 139121 0 None 1 6 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cellsDisplacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells
ChEMBL 319 8 4 6 1.8 COc1ccccc1OCCNC[C@H](O)c1ccc(O)c(O)c1 10.1016/j.bmc.2016.04.028
CHEMBL3797876 139121 0 None 1 6 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cellsDisplacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells
ChEMBL 319 8 4 6 1.8 COc1ccccc1OCCNC[C@H](O)c1ccc(O)c(O)c1 10.1016/j.bmc.2016.04.028
2464 3570 52 None - 6 Dog 8.3 pIC50 = 8.3 Binding
In vitro Beta-2 adrenergic receptor affinity in partially purified membrane fractions from canine lung tissue using [SH]dihydroalprenolol (4.5 nM)In vitro Beta-2 adrenergic receptor affinity in partially purified membrane fractions from canine lung tissue using [SH]dihydroalprenolol (4.5 nM)
Drug Central 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C None
5253 3570 52 None - 6 Dog 8.3 pIC50 = 8.3 Binding
In vitro Beta-2 adrenergic receptor affinity in partially purified membrane fractions from canine lung tissue using [SH]dihydroalprenolol (4.5 nM)In vitro Beta-2 adrenergic receptor affinity in partially purified membrane fractions from canine lung tissue using [SH]dihydroalprenolol (4.5 nM)
Drug Central 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C None
7297 3570 52 None - 6 Dog 8.3 pIC50 = 8.3 Binding
In vitro Beta-2 adrenergic receptor affinity in partially purified membrane fractions from canine lung tissue using [SH]dihydroalprenolol (4.5 nM)In vitro Beta-2 adrenergic receptor affinity in partially purified membrane fractions from canine lung tissue using [SH]dihydroalprenolol (4.5 nM)
Drug Central 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C None
CHEMBL471 3570 52 None - 6 Dog 8.3 pIC50 = 8.3 Binding
In vitro Beta-2 adrenergic receptor affinity in partially purified membrane fractions from canine lung tissue using [SH]dihydroalprenolol (4.5 nM)In vitro Beta-2 adrenergic receptor affinity in partially purified membrane fractions from canine lung tissue using [SH]dihydroalprenolol (4.5 nM)
Drug Central 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C None
DB00489 3570 52 None - 6 Dog 8.3 pIC50 = 8.3 Binding
In vitro Beta-2 adrenergic receptor affinity in partially purified membrane fractions from canine lung tissue using [SH]dihydroalprenolol (4.5 nM)In vitro Beta-2 adrenergic receptor affinity in partially purified membrane fractions from canine lung tissue using [SH]dihydroalprenolol (4.5 nM)
Drug Central 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C None
2369 615 75 None - 8 Bovine 8.2 pIC50 = 8.2 Binding
Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-2 adrenergic receptor in calf lung membranes.Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-2 adrenergic receptor in calf lung membranes.
Drug Central 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C None
356 615 75 None - 8 Bovine 8.2 pIC50 = 8.2 Binding
Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-2 adrenergic receptor in calf lung membranes.Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-2 adrenergic receptor in calf lung membranes.
Drug Central 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C None
549 615 75 None - 8 Bovine 8.2 pIC50 = 8.2 Binding
Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-2 adrenergic receptor in calf lung membranes.Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-2 adrenergic receptor in calf lung membranes.
Drug Central 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C None
CHEMBL423 615 75 None - 8 Bovine 8.2 pIC50 = 8.2 Binding
Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-2 adrenergic receptor in calf lung membranes.Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-2 adrenergic receptor in calf lung membranes.
Drug Central 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C None
DB00195 615 75 None - 8 Bovine 8.2 pIC50 = 8.2 Binding
Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-2 adrenergic receptor in calf lung membranes.Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-2 adrenergic receptor in calf lung membranes.
Drug Central 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C None
137 367 47 None - 12 Bovine 8.1 pIC50 = 8.1 Binding
Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-2 adrenergic receptor in calf lung membranes.Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-2 adrenergic receptor in calf lung membranes.
Drug Central 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
2119 367 47 None - 12 Bovine 8.1 pIC50 = 8.1 Binding
Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-2 adrenergic receptor in calf lung membranes.Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-2 adrenergic receptor in calf lung membranes.
Drug Central 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
563 367 47 None - 12 Bovine 8.1 pIC50 = 8.1 Binding
Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-2 adrenergic receptor in calf lung membranes.Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-2 adrenergic receptor in calf lung membranes.
Drug Central 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
66368 367 47 None - 12 Bovine 8.1 pIC50 = 8.1 Binding
Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-2 adrenergic receptor in calf lung membranes.Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-2 adrenergic receptor in calf lung membranes.
Drug Central 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
CHEMBL266195 367 47 None - 12 Bovine 8.1 pIC50 = 8.1 Binding
Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-2 adrenergic receptor in calf lung membranes.Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-2 adrenergic receptor in calf lung membranes.
Drug Central 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
DB00866 367 47 None - 12 Bovine 8.1 pIC50 = 8.1 Binding
Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-2 adrenergic receptor in calf lung membranes.Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-2 adrenergic receptor in calf lung membranes.
Drug Central 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
11962616 219 7 None - 0 Human 9.2 pIC50 = 9.2 Binding
Membrane radioligand displacement assay using [<sup>3</sup>H]CGP12177 as tracer.Membrane radioligand displacement assay using [<sup>3</sup>H]CGP12177 as tracer.
Guide to Pharmacology 460 13 4 5 4.2 O=c1ccc2c([nH]1)c(O)ccc2[C@H](CNCCCCCCOCC(c1ccccc1)(F)F)O 22588259
9326 219 7 None - 0 Human 9.2 pIC50 = 9.2 Binding
Membrane radioligand displacement assay using [<sup>3</sup>H]CGP12177 as tracer.Membrane radioligand displacement assay using [<sup>3</sup>H]CGP12177 as tracer.
Guide to Pharmacology 460 13 4 5 4.2 O=c1ccc2c([nH]1)c(O)ccc2[C@H](CNCCCCCCOCC(c1ccccc1)(F)F)O 22588259
CHEMBL3039530 219 7 None - 0 Human 9.2 pIC50 = 9.2 Binding
Membrane radioligand displacement assay using [<sup>3</sup>H]CGP12177 as tracer.Membrane radioligand displacement assay using [<sup>3</sup>H]CGP12177 as tracer.
Guide to Pharmacology 460 13 4 5 4.2 O=c1ccc2c([nH]1)c(O)ccc2[C@H](CNCCCCCCOCC(c1ccccc1)(F)F)O 22588259
DB12100 219 7 None - 0 Human 9.2 pIC50 = 9.2 Binding
Membrane radioligand displacement assay using [<sup>3</sup>H]CGP12177 as tracer.Membrane radioligand displacement assay using [<sup>3</sup>H]CGP12177 as tracer.
Guide to Pharmacology 460 13 4 5 4.2 O=c1ccc2c([nH]1)c(O)ccc2[C@H](CNCCCCCCOCC(c1ccccc1)(F)F)O 22588259
681 1432 65 None -707 39 Human 8.4 pKd = 8.4 Binding
Binding affinity to human adrenergic beta2 receptorBinding affinity to human adrenergic beta2 receptor
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
940 1432 65 None -707 39 Human 8.4 pKd = 8.4 Binding
Binding affinity to human adrenergic beta2 receptorBinding affinity to human adrenergic beta2 receptor
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
947 1432 65 None -707 39 Human 8.4 pKd = 8.4 Binding
Binding affinity to human adrenergic beta2 receptorBinding affinity to human adrenergic beta2 receptor
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
CHEMBL59 1432 65 None -707 39 Human 8.4 pKd = 8.4 Binding
Binding affinity to human adrenergic beta2 receptorBinding affinity to human adrenergic beta2 receptor
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
DB00988 1432 65 None -707 39 Human 8.4 pKd = 8.4 Binding
Binding affinity to human adrenergic beta2 receptorBinding affinity to human adrenergic beta2 receptor
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
3486 3096 51 None -6 11 Bovine 8.3 pKd = 8.3 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
Drug Central 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C None
4883 3096 51 None -6 11 Bovine 8.3 pKd = 8.3 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
Drug Central 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C None
555 3096 51 None -6 11 Bovine 8.3 pKd = 8.3 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
Drug Central 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C None
CHEMBL6995 3096 51 None -6 11 Bovine 8.3 pKd = 8.3 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
Drug Central 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C None
DB01297 3096 51 None -6 11 Bovine 8.3 pKd = 8.3 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
Drug Central 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C None
1720 2901 35 None 2 2 Bovine 8.3 pKd = 8.3 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
Drug Central 211 4 4 4 1.1 OC(c1cc(O)cc(c1)O)CNC(C)C None
4086 2901 35 None 2 2 Bovine 8.3 pKd = 8.3 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
Drug Central 211 4 4 4 1.1 OC(c1cc(O)cc(c1)O)CNC(C)C None
7250 2901 35 None 2 2 Bovine 8.3 pKd = 8.3 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
Drug Central 211 4 4 4 1.1 OC(c1cc(O)cc(c1)O)CNC(C)C None
CHEMBL776 2901 35 None 2 2 Bovine 8.3 pKd = 8.3 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
Drug Central 211 4 4 4 1.1 OC(c1cc(O)cc(c1)O)CNC(C)C None
DB00816 2901 35 None 2 2 Bovine 8.3 pKd = 8.3 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
Drug Central 211 4 4 4 1.1 OC(c1cc(O)cc(c1)O)CNC(C)C None
1054 1549 49 None -6 3 Guinea pig 8.3 pKd = 8.3 Binding
Ability to block Beta-2 adrenergic receptor in guinea pig trachea preparationAbility to block Beta-2 adrenergic receptor in guinea pig trachea preparation
Drug Central 295 9 2 5 1.5 COC(=O)CCc1ccc(cc1)OCC(CNC(C)C)O None
59768 1549 49 None -6 3 Guinea pig 8.3 pKd = 8.3 Binding
Ability to block Beta-2 adrenergic receptor in guinea pig trachea preparationAbility to block Beta-2 adrenergic receptor in guinea pig trachea preparation
Drug Central 295 9 2 5 1.5 COC(=O)CCc1ccc(cc1)OCC(CNC(C)C)O None
7178 1549 49 None -6 3 Guinea pig 8.3 pKd = 8.3 Binding
Ability to block Beta-2 adrenergic receptor in guinea pig trachea preparationAbility to block Beta-2 adrenergic receptor in guinea pig trachea preparation
Drug Central 295 9 2 5 1.5 COC(=O)CCc1ccc(cc1)OCC(CNC(C)C)O None
CHEMBL768 1549 49 None -6 3 Guinea pig 8.3 pKd = 8.3 Binding
Ability to block Beta-2 adrenergic receptor in guinea pig trachea preparationAbility to block Beta-2 adrenergic receptor in guinea pig trachea preparation
Drug Central 295 9 2 5 1.5 COC(=O)CCc1ccc(cc1)OCC(CNC(C)C)O None
DB00187 1549 49 None -6 3 Guinea pig 8.3 pKd = 8.3 Binding
Ability to block Beta-2 adrenergic receptor in guinea pig trachea preparationAbility to block Beta-2 adrenergic receptor in guinea pig trachea preparation
Drug Central 295 9 2 5 1.5 COC(=O)CCc1ccc(cc1)OCC(CNC(C)C)O None
2598 3707 52 None 6 5 Bovine 8.3 pKd = 8.3 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
Drug Central 225 3 4 4 1.5 OC(c1cc(O)cc(c1)O)CNC(C)(C)C None
5403 3707 52 None 6 5 Bovine 8.3 pKd = 8.3 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
Drug Central 225 3 4 4 1.5 OC(c1cc(O)cc(c1)O)CNC(C)(C)C None
560 3707 52 None 6 5 Bovine 8.3 pKd = 8.3 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
Drug Central 225 3 4 4 1.5 OC(c1cc(O)cc(c1)O)CNC(C)(C)C None
CHEMBL1760 3707 52 None 6 5 Bovine 8.3 pKd = 8.3 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
Drug Central 225 3 4 4 1.5 OC(c1cc(O)cc(c1)O)CNC(C)(C)C None
DB00871 3707 52 None 6 5 Bovine 8.3 pKd = 8.3 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
Drug Central 225 3 4 4 1.5 OC(c1cc(O)cc(c1)O)CNC(C)(C)C None
1960 2805 64 None -549 26 Human 8.3 pKd = 8.3 Binding
Binding affinity to human adrenergic beta2 receptorBinding affinity to human adrenergic beta2 receptor
Drug Central 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O None
439260 2805 64 None -549 26 Human 8.3 pKd = 8.3 Binding
Binding affinity to human adrenergic beta2 receptorBinding affinity to human adrenergic beta2 receptor
Drug Central 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O None
505 2805 64 None -549 26 Human 8.3 pKd = 8.3 Binding
Binding affinity to human adrenergic beta2 receptorBinding affinity to human adrenergic beta2 receptor
Drug Central 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O None
CHEMBL1437 2805 64 None -549 26 Human 8.3 pKd = 8.3 Binding
Binding affinity to human adrenergic beta2 receptorBinding affinity to human adrenergic beta2 receptor
Drug Central 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O None
DB00368 2805 64 None -549 26 Human 8.3 pKd = 8.3 Binding
Binding affinity to human adrenergic beta2 receptorBinding affinity to human adrenergic beta2 receptor
Drug Central 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O None
3486 3096 51 None -30 11 Guinea pig 8.2 pKd = 8.2 Binding
Ability to block Beta-2 adrenergic receptor in guinea pig trachea preparationAbility to block Beta-2 adrenergic receptor in guinea pig trachea preparation
Drug Central 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C None
4883 3096 51 None -30 11 Guinea pig 8.2 pKd = 8.2 Binding
Ability to block Beta-2 adrenergic receptor in guinea pig trachea preparationAbility to block Beta-2 adrenergic receptor in guinea pig trachea preparation
Drug Central 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C None
555 3096 51 None -30 11 Guinea pig 8.2 pKd = 8.2 Binding
Ability to block Beta-2 adrenergic receptor in guinea pig trachea preparationAbility to block Beta-2 adrenergic receptor in guinea pig trachea preparation
Drug Central 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C None
CHEMBL6995 3096 51 None -30 11 Guinea pig 8.2 pKd = 8.2 Binding
Ability to block Beta-2 adrenergic receptor in guinea pig trachea preparationAbility to block Beta-2 adrenergic receptor in guinea pig trachea preparation
Drug Central 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C None
DB01297 3096 51 None -30 11 Guinea pig 8.2 pKd = 8.2 Binding
Ability to block Beta-2 adrenergic receptor in guinea pig trachea preparationAbility to block Beta-2 adrenergic receptor in guinea pig trachea preparation
Drug Central 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C None
2249 509 106 None -33 12 Human 8.2 pKd = 8.2 Binding
NoneNone
Drug Central 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C None
255 509 106 None -33 12 Human 8.2 pKd = 8.2 Binding
NoneNone
Drug Central 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C None
548 509 106 None -33 12 Human 8.2 pKd = 8.2 Binding
NoneNone
Drug Central 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C None
CHEMBL24 509 106 None -33 12 Human 8.2 pKd = 8.2 Binding
NoneNone
Drug Central 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C None
DB00335 509 106 None -33 12 Human 8.2 pKd = 8.2 Binding
NoneNone
Drug Central 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C None
6317 18308 36 None - 1 Bovine 8.2 pKd = 8.2 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
Drug Central 224 5 2 4 1.6 CC(C)NCC(O)c1ccc([N+](=O)[O-])cc1 None
CHEMBL127349 18308 36 None - 1 Bovine 8.2 pKd = 8.2 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
Drug Central 224 5 2 4 1.6 CC(C)NCC(O)c1ccc([N+](=O)[O-])cc1 None
2249 509 106 None -6 12 Guinea pig 8.2 pKd = 8.2 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
Drug Central 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C None
255 509 106 None -6 12 Guinea pig 8.2 pKd = 8.2 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
Drug Central 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C None
548 509 106 None -6 12 Guinea pig 8.2 pKd = 8.2 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
Drug Central 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C None
CHEMBL24 509 106 None -6 12 Guinea pig 8.2 pKd = 8.2 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
Drug Central 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C None
DB00335 509 106 None -6 12 Guinea pig 8.2 pKd = 8.2 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
Drug Central 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C None
175540 118737 45 None -1 5 Guinea pig 8.2 pKd = 8.2 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
Drug Central 266 8 3 4 0.5 CC(C)NC[C@H](O)COc1ccc(CC(N)=O)cc1 None
CHEMBL343633 118737 45 None -1 5 Guinea pig 8.2 pKd = 8.2 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
Drug Central 266 8 3 4 0.5 CC(C)NC[C@H](O)COc1ccc(CC(N)=O)cc1 None
105 3392 84 None -5 6 Guinea pig 8.2 pKd = 8.2 Binding
Binding affinity to adrenergic beta2 receptor in Hartley guinea pig tracheal ringBinding affinity to adrenergic beta2 receptor in Hartley guinea pig tracheal ring
Drug Central 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O None
2083 3392 84 None -5 6 Guinea pig 8.2 pKd = 8.2 Binding
Binding affinity to adrenergic beta2 receptor in Hartley guinea pig tracheal ringBinding affinity to adrenergic beta2 receptor in Hartley guinea pig tracheal ring
Drug Central 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O None
558 3392 84 None -5 6 Guinea pig 8.2 pKd = 8.2 Binding
Binding affinity to adrenergic beta2 receptor in Hartley guinea pig tracheal ringBinding affinity to adrenergic beta2 receptor in Hartley guinea pig tracheal ring
Drug Central 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O None
CHEMBL714 3392 84 None -5 6 Guinea pig 8.2 pKd = 8.2 Binding
Binding affinity to adrenergic beta2 receptor in Hartley guinea pig tracheal ringBinding affinity to adrenergic beta2 receptor in Hartley guinea pig tracheal ring
Drug Central 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O None
DB01001 3392 84 None -5 6 Guinea pig 8.2 pKd = 8.2 Binding
Binding affinity to adrenergic beta2 receptor in Hartley guinea pig tracheal ringBinding affinity to adrenergic beta2 receptor in Hartley guinea pig tracheal ring
Drug Central 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O None
2258 3104 36 None -1 2 Bovine 8.2 pKd = 8.2 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
Drug Central 225 6 3 4 1.1 O[C@H](COc1ccc(cc1)O)CNC(C)C None
42396 3104 36 None -1 2 Bovine 8.2 pKd = 8.2 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
Drug Central 225 6 3 4 1.1 O[C@H](COc1ccc(cc1)O)CNC(C)C None
537 3104 36 None -1 2 Bovine 8.2 pKd = 8.2 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
Drug Central 225 6 3 4 1.1 O[C@H](COc1ccc(cc1)O)CNC(C)C None
CHEMBL1160714 3104 36 None -1 2 Bovine 8.2 pKd = 8.2 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
Drug Central 225 6 3 4 1.1 O[C@H](COc1ccc(cc1)O)CNC(C)C None
DB13777 3104 36 None -1 2 Bovine 8.2 pKd = 8.2 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
Drug Central 225 6 3 4 1.1 O[C@H](COc1ccc(cc1)O)CNC(C)C None
3762 14316 24 None - 1 Human 8.2 pKd = 8.2 Binding
Binding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nMBinding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nM
Drug Central 239 5 4 4 1.9 CCC(NC(C)C)C(O)c1ccc(O)c(O)c1 None
CHEMBL1201153 14316 24 None - 1 Human 8.2 pKd = 8.2 Binding
Binding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nMBinding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nM
Drug Central 239 5 4 4 1.9 CCC(NC(C)C)C(O)c1ccc(O)c(O)c1 None
CHEMBL1201213 14316 24 None - 1 Human 8.2 pKd = 8.2 Binding
Binding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nMBinding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nM
Drug Central 239 5 4 4 1.9 CCC(NC(C)C)C(O)c1ccc(O)c(O)c1 None
155774 4021 33 None -5 3 Human 8.2 pKd = 8.2 Binding
Antagonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrsAntagonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrs
Drug Central 339 8 4 6 -0.2 OC(COc1ccc(cc1)O)CNCCNC(=O)N1CCOCC1 None
2848 4021 33 None -5 3 Human 8.2 pKd = 8.2 Binding
Antagonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrsAntagonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrs
Drug Central 339 8 4 6 -0.2 OC(COc1ccc(cc1)O)CNCCNC(=O)N1CCOCC1 None
538 4021 33 None -5 3 Human 8.2 pKd = 8.2 Binding
Antagonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrsAntagonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrs
Drug Central 339 8 4 6 -0.2 OC(COc1ccc(cc1)O)CNCCNC(=O)N1CCOCC1 None
CHEMBL75753 4021 33 None -5 3 Human 8.2 pKd = 8.2 Binding
Antagonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrsAntagonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrs
Drug Central 339 8 4 6 -0.2 OC(COc1ccc(cc1)O)CNCCNC(=O)N1CCOCC1 None
DB13781 4021 33 None -5 3 Human 8.2 pKd = 8.2 Binding
Antagonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrsAntagonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrs
Drug Central 339 8 4 6 -0.2 OC(COc1ccc(cc1)O)CNCCNC(=O)N1CCOCC1 None
1028 287 69 None -89 30 Human 8.2 pKd = 8.2 Binding
Binding affinity to human adrenergic beta2 receptorBinding affinity to human adrenergic beta2 receptor
Drug Central 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
139148732 287 69 None -89 30 Human 8.2 pKd = 8.2 Binding
Binding affinity to human adrenergic beta2 receptorBinding affinity to human adrenergic beta2 receptor
Drug Central 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
479 287 69 None -89 30 Human 8.2 pKd = 8.2 Binding
Binding affinity to human adrenergic beta2 receptorBinding affinity to human adrenergic beta2 receptor
Drug Central 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
5816 287 69 None -89 30 Human 8.2 pKd = 8.2 Binding
Binding affinity to human adrenergic beta2 receptorBinding affinity to human adrenergic beta2 receptor
Drug Central 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
CHEMBL679 287 69 None -89 30 Human 8.2 pKd = 8.2 Binding
Binding affinity to human adrenergic beta2 receptorBinding affinity to human adrenergic beta2 receptor
Drug Central 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
DB00668 287 69 None -89 30 Human 8.2 pKd = 8.2 Binding
Binding affinity to human adrenergic beta2 receptorBinding affinity to human adrenergic beta2 receptor
Drug Central 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
2464 3570 52 None 2 6 Bovine 8.2 pKd = 8.2 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
Drug Central 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C None
5253 3570 52 None 2 6 Bovine 8.2 pKd = 8.2 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
Drug Central 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C None
7297 3570 52 None 2 6 Bovine 8.2 pKd = 8.2 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
Drug Central 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C None
CHEMBL471 3570 52 None 2 6 Bovine 8.2 pKd = 8.2 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
Drug Central 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C None
DB00489 3570 52 None 2 6 Bovine 8.2 pKd = 8.2 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
Drug Central 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C None
105 3392 84 None -1 6 Bovine 8.2 pKd = 8.2 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
Drug Central 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O None
2083 3392 84 None -1 6 Bovine 8.2 pKd = 8.2 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
Drug Central 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O None
558 3392 84 None -1 6 Bovine 8.2 pKd = 8.2 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
Drug Central 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O None
CHEMBL714 3392 84 None -1 6 Bovine 8.2 pKd = 8.2 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
Drug Central 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O None
DB01001 3392 84 None -1 6 Bovine 8.2 pKd = 8.2 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
Drug Central 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O None
1720 2901 35 None -2 2 Human 8.2 pKd = 8.2 Binding
Binding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nMBinding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nM
Drug Central 211 4 4 4 1.1 OC(c1cc(O)cc(c1)O)CNC(C)C None
4086 2901 35 None -2 2 Human 8.2 pKd = 8.2 Binding
Binding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nMBinding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nM
Drug Central 211 4 4 4 1.1 OC(c1cc(O)cc(c1)O)CNC(C)C None
7250 2901 35 None -2 2 Human 8.2 pKd = 8.2 Binding
Binding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nMBinding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nM
Drug Central 211 4 4 4 1.1 OC(c1cc(O)cc(c1)O)CNC(C)C None
CHEMBL776 2901 35 None -2 2 Human 8.2 pKd = 8.2 Binding
Binding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nMBinding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nM
Drug Central 211 4 4 4 1.1 OC(c1cc(O)cc(c1)O)CNC(C)C None
DB00816 2901 35 None -2 2 Human 8.2 pKd = 8.2 Binding
Binding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nMBinding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nM
Drug Central 211 4 4 4 1.1 OC(c1cc(O)cc(c1)O)CNC(C)C None
1499 2052 43 None -8 17 Bovine 8.2 pKd = 8.2 Binding
NoneNone
Drug Central 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
3779 2052 43 None -8 17 Bovine 8.2 pKd = 8.2 Binding
NoneNone
Drug Central 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
536 2052 43 None -8 17 Bovine 8.2 pKd = 8.2 Binding
NoneNone
Drug Central 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
CHEMBL434 2052 43 None -8 17 Bovine 8.2 pKd = 8.2 Binding
NoneNone
Drug Central 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
DB01064 2052 43 None -8 17 Bovine 8.2 pKd = 8.2 Binding
NoneNone
Drug Central 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
1786 2474 79 None -1 11 Guinea pig 8.2 pKd = 8.2 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
Drug Central 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O None
4171 2474 79 None -1 11 Guinea pig 8.2 pKd = 8.2 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
Drug Central 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O None
553 2474 79 None -1 11 Guinea pig 8.2 pKd = 8.2 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
Drug Central 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O None
CHEMBL13 2474 79 None -1 11 Guinea pig 8.2 pKd = 8.2 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
Drug Central 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O None
DB00264 2474 79 None -1 11 Guinea pig 8.2 pKd = 8.2 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
Drug Central 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O None
4930 56856 45 None - 1 Bovine 8.2 pKd = 8.2 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
Drug Central 229 4 2 2 2.9 CC(C)NCC(O)c1ccc2ccccc2c1 None
CHEMBL16476 56856 45 None - 1 Bovine 8.2 pKd = 8.2 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
Drug Central 229 4 2 2 2.9 CC(C)NCC(O)c1ccc2ccccc2c1 None
5606 10083 63 None - 1 Bovine 8.2 pKd = 8.2 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
Drug Central 227 3 2 2 2.8 CC(C)(C)NCC(O)c1ccccc1Cl None
CHEMBL1159717 10083 63 None - 1 Bovine 8.2 pKd = 8.2 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
Drug Central 227 3 2 2 2.8 CC(C)(C)NCC(O)c1ccccc1Cl None
2369 615 75 None -9 8 Guinea pig 8.2 pKd = 8.2 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
Drug Central 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C None
356 615 75 None -9 8 Guinea pig 8.2 pKd = 8.2 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
Drug Central 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C None
549 615 75 None -9 8 Guinea pig 8.2 pKd = 8.2 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
Drug Central 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C None
CHEMBL423 615 75 None -9 8 Guinea pig 8.2 pKd = 8.2 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
Drug Central 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C None
DB00195 615 75 None -9 8 Guinea pig 8.2 pKd = 8.2 Binding
In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alphaIn vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha
Drug Central 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C None
2369 615 75 None -7 8 Human 8.1 pKd = 8.1 Binding
NoneNone
Drug Central 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C None
356 615 75 None -7 8 Human 8.1 pKd = 8.1 Binding
NoneNone
Drug Central 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C None
549 615 75 None -7 8 Human 8.1 pKd = 8.1 Binding
NoneNone
Drug Central 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C None
CHEMBL423 615 75 None -7 8 Human 8.1 pKd = 8.1 Binding
NoneNone
Drug Central 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C None
DB00195 615 75 None -7 8 Human 8.1 pKd = 8.1 Binding
NoneNone
Drug Central 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C None
18047 201915 18 None -4 5 Bovine 8.1 pKd = 8.1 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
Drug Central 223 6 2 3 1.7 Cc1cccc(OCC(O)CNC(C)C)c1 None
CHEMBL67096 201915 18 None -4 5 Bovine 8.1 pKd = 8.1 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
Drug Central 223 6 2 3 1.7 Cc1cccc(OCC(O)CNC(C)C)c1 None
12582 935 40 None -2 5 Bovine 8.1 pKd = 8.1 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
Drug Central 276 3 3 3 3.0 CC(C)(C)NCC(C1=CC(=C(C(=C1)Cl)N)Cl)O None
2783 935 40 None -2 5 Bovine 8.1 pKd = 8.1 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
Drug Central 276 3 3 3 3.0 CC(C)(C)NCC(C1=CC(=C(C(=C1)Cl)N)Cl)O None
CHEMBL49080 935 40 None -2 5 Bovine 8.1 pKd = 8.1 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
Drug Central 276 3 3 3 3.0 CC(C)(C)NCC(C1=CC(=C(C(=C1)Cl)N)Cl)O None
DB01407 935 40 None -2 5 Bovine 8.1 pKd = 8.1 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
Drug Central 276 3 3 3 3.0 CC(C)(C)NCC(C1=CC(=C(C(=C1)Cl)N)Cl)O None
12582 935 40 None -11 5 Human 8.1 pKd = 8.1 Binding
Binding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nMBinding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nM
Drug Central 276 3 3 3 3.0 CC(C)(C)NCC(C1=CC(=C(C(=C1)Cl)N)Cl)O None
2783 935 40 None -11 5 Human 8.1 pKd = 8.1 Binding
Binding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nMBinding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nM
Drug Central 276 3 3 3 3.0 CC(C)(C)NCC(C1=CC(=C(C(=C1)Cl)N)Cl)O None
CHEMBL49080 935 40 None -11 5 Human 8.1 pKd = 8.1 Binding
Binding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nMBinding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nM
Drug Central 276 3 3 3 3.0 CC(C)(C)NCC(C1=CC(=C(C(=C1)Cl)N)Cl)O None
DB01407 935 40 None -11 5 Human 8.1 pKd = 8.1 Binding
Binding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nMBinding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nM
Drug Central 276 3 3 3 3.0 CC(C)(C)NCC(C1=CC(=C(C(=C1)Cl)N)Cl)O None
3083544 462 46 None -5 5 Human 8.1 pKd = 8.1 Binding
displacement of [125I]-iodopindololreceptor in Sf9 cells expressing human recombinant beta2displacement of [125I]-iodopindololreceptor in Sf9 cells expressing human recombinant beta2
Drug Central 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O None
4943 462 46 None -5 5 Human 8.1 pKd = 8.1 Binding
displacement of [125I]-iodopindololreceptor in Sf9 cells expressing human recombinant beta2displacement of [125I]-iodopindololreceptor in Sf9 cells expressing human recombinant beta2
Drug Central 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O None
7479 462 46 None -5 5 Human 8.1 pKd = 8.1 Binding
displacement of [125I]-iodopindololreceptor in Sf9 cells expressing human recombinant beta2displacement of [125I]-iodopindololreceptor in Sf9 cells expressing human recombinant beta2
Drug Central 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O None
CHEMBL1363 462 46 None -5 5 Human 8.1 pKd = 8.1 Binding
displacement of [125I]-iodopindololreceptor in Sf9 cells expressing human recombinant beta2displacement of [125I]-iodopindololreceptor in Sf9 cells expressing human recombinant beta2
Drug Central 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O None
DB01274 462 46 None -5 5 Human 8.1 pKd = 8.1 Binding
displacement of [125I]-iodopindololreceptor in Sf9 cells expressing human recombinant beta2displacement of [125I]-iodopindololreceptor in Sf9 cells expressing human recombinant beta2
Drug Central 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O None
3083544 462 46 None -5 5 Human 8.1 pKd = 8.1 Binding
Binding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nMBinding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nM
Drug Central 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O None
4943 462 46 None -5 5 Human 8.1 pKd = 8.1 Binding
Binding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nMBinding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nM
Drug Central 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O None
7479 462 46 None -5 5 Human 8.1 pKd = 8.1 Binding
Binding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nMBinding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nM
Drug Central 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O None
CHEMBL1363 462 46 None -5 5 Human 8.1 pKd = 8.1 Binding
Binding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nMBinding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nM
Drug Central 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O None
DB01274 462 46 None -5 5 Human 8.1 pKd = 8.1 Binding
Binding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nMBinding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nM
Drug Central 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O None
18047 201915 18 None -2 5 Human 8.1 pKd = 8.1 Binding
Binding affinity to beta2 adrenergic receptorBinding affinity to beta2 adrenergic receptor
Drug Central 223 6 2 3 1.7 Cc1cccc(OCC(O)CNC(C)C)c1 None
CHEMBL67096 201915 18 None -2 5 Human 8.1 pKd = 8.1 Binding
Binding affinity to beta2 adrenergic receptorBinding affinity to beta2 adrenergic receptor
Drug Central 223 6 2 3 1.7 Cc1cccc(OCC(O)CNC(C)C)c1 None
165193 3126 60 None -4 43 Guinea pig 8.1 pKd = 8.1 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
2303 3126 60 None -4 43 Guinea pig 8.1 pKd = 8.1 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
4946 3126 60 None -4 43 Guinea pig 8.1 pKd = 8.1 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
564 3126 60 None -4 43 Guinea pig 8.1 pKd = 8.1 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
62882 3126 60 None -4 43 Guinea pig 8.1 pKd = 8.1 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
63 3126 60 None -4 43 Guinea pig 8.1 pKd = 8.1 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
66366 3126 60 None -4 43 Guinea pig 8.1 pKd = 8.1 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
91536 3126 60 None -4 43 Guinea pig 8.1 pKd = 8.1 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
CHEMBL27 3126 60 None -4 43 Guinea pig 8.1 pKd = 8.1 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
CHEMBL452861 3126 60 None -4 43 Guinea pig 8.1 pKd = 8.1 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
DB00571 3126 60 None -4 43 Guinea pig 8.1 pKd = 8.1 Binding
In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
165193 3126 60 None -2 43 Bovine 8.0 pKd = 8.0 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
2303 3126 60 None -2 43 Bovine 8.0 pKd = 8.0 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
4946 3126 60 None -2 43 Bovine 8.0 pKd = 8.0 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
564 3126 60 None -2 43 Bovine 8.0 pKd = 8.0 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
62882 3126 60 None -2 43 Bovine 8.0 pKd = 8.0 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
63 3126 60 None -2 43 Bovine 8.0 pKd = 8.0 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
66366 3126 60 None -2 43 Bovine 8.0 pKd = 8.0 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
91536 3126 60 None -2 43 Bovine 8.0 pKd = 8.0 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
CHEMBL27 3126 60 None -2 43 Bovine 8.0 pKd = 8.0 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
CHEMBL452861 3126 60 None -2 43 Bovine 8.0 pKd = 8.0 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
DB00571 3126 60 None -2 43 Bovine 8.0 pKd = 8.0 Binding
Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
137 367 47 None -3 12 Human 8.0 pKd = 8.0 Binding
radioligand [3H]CGP12177 0.15nM competition binding; human recombinant beta-adrenoceptors in Sf9 cellsradioligand [3H]CGP12177 0.15nM competition binding; human recombinant beta-adrenoceptors in Sf9 cells
Drug Central 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
2119 367 47 None -3 12 Human 8.0 pKd = 8.0 Binding
radioligand [3H]CGP12177 0.15nM competition binding; human recombinant beta-adrenoceptors in Sf9 cellsradioligand [3H]CGP12177 0.15nM competition binding; human recombinant beta-adrenoceptors in Sf9 cells
Drug Central 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
563 367 47 None -3 12 Human 8.0 pKd = 8.0 Binding
radioligand [3H]CGP12177 0.15nM competition binding; human recombinant beta-adrenoceptors in Sf9 cellsradioligand [3H]CGP12177 0.15nM competition binding; human recombinant beta-adrenoceptors in Sf9 cells
Drug Central 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
66368 367 47 None -3 12 Human 8.0 pKd = 8.0 Binding
radioligand [3H]CGP12177 0.15nM competition binding; human recombinant beta-adrenoceptors in Sf9 cellsradioligand [3H]CGP12177 0.15nM competition binding; human recombinant beta-adrenoceptors in Sf9 cells
Drug Central 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
CHEMBL266195 367 47 None -3 12 Human 8.0 pKd = 8.0 Binding
radioligand [3H]CGP12177 0.15nM competition binding; human recombinant beta-adrenoceptors in Sf9 cellsradioligand [3H]CGP12177 0.15nM competition binding; human recombinant beta-adrenoceptors in Sf9 cells
Drug Central 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
DB00866 367 47 None -3 12 Human 8.0 pKd = 8.0 Binding
radioligand [3H]CGP12177 0.15nM competition binding; human recombinant beta-adrenoceptors in Sf9 cellsradioligand [3H]CGP12177 0.15nM competition binding; human recombinant beta-adrenoceptors in Sf9 cells
Drug Central 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
33624 3749 29 None -1 9 Guinea pig 8.0 pKd = 8.0 Binding
In vitro inhibitory activity against beta-2 adrenoceptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenoceptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
Drug Central 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C None
4061 3749 29 None -1 9 Guinea pig 8.0 pKd = 8.0 Binding
In vitro inhibitory activity against beta-2 adrenoceptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenoceptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
Drug Central 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C None
565 3749 29 None -1 9 Guinea pig 8.0 pKd = 8.0 Binding
In vitro inhibitory activity against beta-2 adrenoceptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenoceptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
Drug Central 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C None
CHEMBL499 3749 29 None -1 9 Guinea pig 8.0 pKd = 8.0 Binding
In vitro inhibitory activity against beta-2 adrenoceptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenoceptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
Drug Central 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C None
DB00373 3749 29 None -1 9 Guinea pig 8.0 pKd = 8.0 Binding
In vitro inhibitory activity against beta-2 adrenoceptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-2 adrenoceptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea
Drug Central 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C None
2687 874 15 None 1 5 Human 9.8 pKd = 9.8 Binding
Binding to human &beta<sub>2</sub>-adrenoceptor expressed in CHO-K1 cells, in a whole cell binding assay.Binding to human &beta<sub>2</sub>-adrenoceptor expressed in CHO-K1 cells, in a whole cell binding assay.
Guide to Pharmacology 279 5 4 4 1.0 OC(COc1cccc2c1[nH]c(=O)[nH]2)CNC(C)(C)C 12237261
532 874 15 None 1 5 Human 9.8 pKd = 9.8 Binding
Binding to human &beta<sub>2</sub>-adrenoceptor expressed in CHO-K1 cells, in a whole cell binding assay.Binding to human &beta<sub>2</sub>-adrenoceptor expressed in CHO-K1 cells, in a whole cell binding assay.
Guide to Pharmacology 279 5 4 4 1.0 OC(COc1cccc2c1[nH]c(=O)[nH]2)CNC(C)(C)C 12237261
5387 874 15 None 1 5 Human 9.8 pKd = 9.8 Binding
Binding to human &beta<sub>2</sub>-adrenoceptor expressed in CHO-K1 cells, in a whole cell binding assay.Binding to human &beta<sub>2</sub>-adrenoceptor expressed in CHO-K1 cells, in a whole cell binding assay.
Guide to Pharmacology 279 5 4 4 1.0 OC(COc1cccc2c1[nH]c(=O)[nH]2)CNC(C)(C)C 12237261
CHEMBL420746 874 15 None 1 5 Human 9.8 pKd = 9.8 Binding
Binding to human &beta<sub>2</sub>-adrenoceptor expressed in CHO-K1 cells, in a whole cell binding assay.Binding to human &beta<sub>2</sub>-adrenoceptor expressed in CHO-K1 cells, in a whole cell binding assay.
Guide to Pharmacology 279 5 4 4 1.0 OC(COc1cccc2c1[nH]c(=O)[nH]2)CNC(C)(C)C 12237261
12165 896 4 None 15 2 Human 11.4 pKd = 11.4 Binding
Binding to human cloned &beta;<sub>2</sub> receptor using 125I-cyanopindolol as tracerBinding to human cloned &beta;<sub>2</sub> receptor using 125I-cyanopindolol as tracer
Guide to Pharmacology 764 16 5 12 4.7 O=C(O[C@@H]1C2CCN(CC2)C1)N[C@@H](c1ccccc1)c1cc(OCc2cc(C(=O)OCCCCNC[C@H](O)c3c4ccc(=O)[nH]c4c(O)cc3)nn2C)ccc1 35901125
90200922 896 4 None 15 2 Human 11.4 pKd = 11.4 Binding
Binding to human cloned &beta;<sub>2</sub> receptor using 125I-cyanopindolol as tracerBinding to human cloned &beta;<sub>2</sub> receptor using 125I-cyanopindolol as tracer
Guide to Pharmacology 764 16 5 12 4.7 O=C(O[C@@H]1C2CCN(CC2)C1)N[C@@H](c1ccccc1)c1cc(OCc2cc(C(=O)OCCCCNC[C@H](O)c3c4ccc(=O)[nH]c4c(O)cc3)nn2C)ccc1 35901125
CHEMBL5172865 896 4 None 15 2 Human 11.4 pKd = 11.4 Binding
Binding to human cloned &beta;<sub>2</sub> receptor using 125I-cyanopindolol as tracerBinding to human cloned &beta;<sub>2</sub> receptor using 125I-cyanopindolol as tracer
Guide to Pharmacology 764 16 5 12 4.7 O=C(O[C@@H]1C2CCN(CC2)C1)N[C@@H](c1ccccc1)c1cc(OCc2cc(C(=O)OCCCCNC[C@H](O)c3c4ccc(=O)[nH]c4c(O)cc3)nn2C)ccc1 35901125
1720 2901 35 None -2 2 Human 5.3 pKd = 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 211 4 4 4 1.1 OC(c1cc(O)cc(c1)O)CNC(C)C 19168263
4086 2901 35 None -2 2 Human 5.3 pKd = 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 211 4 4 4 1.1 OC(c1cc(O)cc(c1)O)CNC(C)C 19168263
7250 2901 35 None -2 2 Human 5.3 pKd = 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 211 4 4 4 1.1 OC(c1cc(O)cc(c1)O)CNC(C)C 19168263
CHEMBL776 2901 35 None -2 2 Human 5.3 pKd = 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 211 4 4 4 1.1 OC(c1cc(O)cc(c1)O)CNC(C)C 19168263
DB00816 2901 35 None -2 2 Human 5.3 pKd = 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 211 4 4 4 1.1 OC(c1cc(O)cc(c1)O)CNC(C)C 19168263
165193 3126 60 125I-ICYP 1 43 Human 11.0 pKi = 11 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
2303 3126 60 125I-ICYP 1 43 Human 11.0 pKi = 11 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
4946 3126 60 125I-ICYP 1 43 Human 11.0 pKi = 11 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
564 3126 60 125I-ICYP 1 43 Human 11.0 pKi = 11 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
62882 3126 60 125I-ICYP 1 43 Human 11.0 pKi = 11 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
63 3126 60 125I-ICYP 1 43 Human 11.0 pKi = 11 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
66366 3126 60 125I-ICYP 1 43 Human 11.0 pKi = 11 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
91536 3126 60 125I-ICYP 1 43 Human 11.0 pKi = 11 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
CHEMBL27 3126 60 125I-ICYP 1 43 Human 11.0 pKi = 11 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
CHEMBL452861 3126 60 125I-ICYP 1 43 Human 11.0 pKi = 11 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
DB00571 3126 60 125I-ICYP 1 43 Human 11.0 pKi = 11 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
None 214476 0 125I-Pindolol 2 30 Human 10.1 pKi = 10.1 Binding
NoneNone
PDSP KiDatabase 316 7 3 3 3.0 CC(CF)NCC(COC1=CC=CC2=C1C3=CC=CC=C3N2)O None
487 779 65 UNDEFINED 4 6 Human 9.9 pKi = 9.9 Binding
NoneNone
PDSP KiDatabase 298 6 3 3 3.1 OC(COc1cccc2c1c1ccccc1[nH]2)CNC(C)C None
569 779 65 UNDEFINED 4 6 Human 9.9 pKi = 9.9 Binding
NoneNone
PDSP KiDatabase 298 6 3 3 3.1 OC(COc1cccc2c1c1ccccc1[nH]2)CNC(C)C None
71739 779 65 UNDEFINED 4 6 Human 9.9 pKi = 9.9 Binding
NoneNone
PDSP KiDatabase 298 6 3 3 3.1 OC(COc1cccc2c1c1ccccc1[nH]2)CNC(C)C None
CHEMBL324665 779 65 UNDEFINED 4 6 Human 9.9 pKi = 9.9 Binding
NoneNone
PDSP KiDatabase 298 6 3 3 3.1 OC(COc1cccc2c1c1ccccc1[nH]2)CNC(C)C None
23968266 188807 0 UNDEFINED - 1 Human 9.8 pKi = 9.8 Binding
NoneNone
PDSP KiDatabase 313 5 2 4 3.7 CC(C)(C)NCC(O)COc1cccc2oc3ccccc3c12 None
CHEMBL513104 188807 0 UNDEFINED - 1 Human 9.8 pKi = 9.8 Binding
NoneNone
PDSP KiDatabase 313 5 2 4 3.7 CC(C)(C)NCC(O)COc1cccc2oc3ccccc3c12 None
None 214476 0 125I-Pindolol 2 30 Human 9.9 pKi = 9.9 Binding
NoneNone
PDSP KiDatabase 316 7 3 3 3.0 CC(CF)NCC(COC1=CC=CC2=C1C3=CC=CC=C3N2)O None
3858663 176284 9 UNDEFINED - 1 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 455 8 2 4 4.6 Cc1c[nH]c2cccc(OCC(O)CN3CCN(C(c4ccccc4)c4ccccc4)CC3)c12 None
CHEMBL461463 176284 9 UNDEFINED - 1 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 455 8 2 4 4.6 Cc1c[nH]c2cccc(OCC(O)CN3CCN(C(c4ccccc4)c4ccccc4)CC3)c12 None
2176 3065 66 125I-ICYP 2 27 Rat 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
4828 3065 66 125I-ICYP 2 27 Rat 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
91 3065 66 125I-ICYP 2 27 Rat 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
CHEMBL500 3065 66 125I-ICYP 2 27 Rat 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
DB00960 3065 66 125I-ICYP 2 27 Rat 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
165193 3126 60 125I-ICYP 1 43 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
2303 3126 60 125I-ICYP 1 43 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
4946 3126 60 125I-ICYP 1 43 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
564 3126 60 125I-ICYP 1 43 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
62882 3126 60 125I-ICYP 1 43 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
63 3126 60 125I-ICYP 1 43 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
66366 3126 60 125I-ICYP 1 43 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
91536 3126 60 125I-ICYP 1 43 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
CHEMBL27 3126 60 125I-ICYP 1 43 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
CHEMBL452861 3126 60 125I-ICYP 1 43 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
DB00571 3126 60 125I-ICYP 1 43 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
2419 3394 80 UNDEFINED 16 6 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O None
5152 3394 80 UNDEFINED 16 6 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O None
559 3394 80 UNDEFINED 16 6 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O None
CHEMBL1263 3394 80 UNDEFINED 16 6 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O None
DB00938 3394 80 UNDEFINED 16 6 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O None
2176 3065 66 UNDEFINED -2 27 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
4828 3065 66 UNDEFINED -2 27 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
91 3065 66 UNDEFINED -2 27 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
CHEMBL500 3065 66 UNDEFINED -2 27 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
DB00960 3065 66 UNDEFINED -2 27 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
165193 3126 60 125I-ICYP -22 43 Rat 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
2303 3126 60 125I-ICYP -22 43 Rat 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
4946 3126 60 125I-ICYP -22 43 Rat 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
564 3126 60 125I-ICYP -22 43 Rat 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
62882 3126 60 125I-ICYP -22 43 Rat 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
63 3126 60 125I-ICYP -22 43 Rat 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
66366 3126 60 125I-ICYP -22 43 Rat 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
91536 3126 60 125I-ICYP -22 43 Rat 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
CHEMBL27 3126 60 125I-ICYP -22 43 Rat 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
CHEMBL452861 3126 60 125I-ICYP -22 43 Rat 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
DB00571 3126 60 125I-ICYP -22 43 Rat 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
137 367 47 3H-DHA 3 12 Rat 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
2119 367 47 3H-DHA 3 12 Rat 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
563 367 47 3H-DHA 3 12 Rat 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
66368 367 47 3H-DHA 3 12 Rat 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
CHEMBL266195 367 47 3H-DHA 3 12 Rat 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
DB00866 367 47 3H-DHA 3 12 Rat 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
None 214414 0 3H-DHA - 1 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 354 8 4 4 3.2 CC(C)(CC1=CC=C(C=C1)O)NCC(COC2=CC=CC3=C2C=CN3)O None
None 214731 0 125I-ICYP -3 3 Rat 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase None None None None None
3682 188837 7 125I-ICYP 1 8 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 277 6 2 3 2.6 Cc1ccc(OCC(O)C(C)NC(C)C)c2c1CCC2 None
CHEMBL1256784 188837 7 125I-ICYP 1 8 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 277 6 2 3 2.6 Cc1ccc(OCC(O)C(C)NC(C)C)c2c1CCC2 None
CHEMBL513389 188837 7 125I-ICYP 1 8 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 277 6 2 3 2.6 Cc1ccc(OCC(O)C(C)NC(C)C)c2c1CCC2 None
137 367 47 125I-ICYP 3 12 Rat 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
2119 367 47 125I-ICYP 3 12 Rat 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
563 367 47 125I-ICYP 3 12 Rat 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
66368 367 47 125I-ICYP 3 12 Rat 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
CHEMBL266195 367 47 125I-ICYP 3 12 Rat 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
DB00866 367 47 125I-ICYP 3 12 Rat 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
165193 3126 60 125I-ICYP 1 43 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
2303 3126 60 125I-ICYP 1 43 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
4946 3126 60 125I-ICYP 1 43 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
564 3126 60 125I-ICYP 1 43 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
62882 3126 60 125I-ICYP 1 43 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
63 3126 60 125I-ICYP 1 43 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
66366 3126 60 125I-ICYP 1 43 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
91536 3126 60 125I-ICYP 1 43 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
CHEMBL27 3126 60 125I-ICYP 1 43 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
CHEMBL452861 3126 60 125I-ICYP 1 43 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
DB00571 3126 60 125I-ICYP 1 43 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
3682 188837 7 125I-ICYP 1 8 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 277 6 2 3 2.6 Cc1ccc(OCC(O)C(C)NC(C)C)c2c1CCC2 None
CHEMBL1256784 188837 7 125I-ICYP 1 8 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 277 6 2 3 2.6 Cc1ccc(OCC(O)C(C)NC(C)C)c2c1CCC2 None
CHEMBL513389 188837 7 125I-ICYP 1 8 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 277 6 2 3 2.6 Cc1ccc(OCC(O)C(C)NC(C)C)c2c1CCC2 None
3682 188837 7 125I-CYP 1 8 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 277 6 2 3 2.6 Cc1ccc(OCC(O)C(C)NC(C)C)c2c1CCC2 None
CHEMBL1256784 188837 7 125I-CYP 1 8 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 277 6 2 3 2.6 Cc1ccc(OCC(O)C(C)NC(C)C)c2c1CCC2 None
CHEMBL513389 188837 7 125I-CYP 1 8 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 277 6 2 3 2.6 Cc1ccc(OCC(O)C(C)NC(C)C)c2c1CCC2 None
165193 3126 60 125I-ICYP -4 43 Guinea pig 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
2303 3126 60 125I-ICYP -4 43 Guinea pig 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
4946 3126 60 125I-ICYP -4 43 Guinea pig 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
564 3126 60 125I-ICYP -4 43 Guinea pig 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
62882 3126 60 125I-ICYP -4 43 Guinea pig 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
63 3126 60 125I-ICYP -4 43 Guinea pig 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
66366 3126 60 125I-ICYP -4 43 Guinea pig 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
91536 3126 60 125I-ICYP -4 43 Guinea pig 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
CHEMBL27 3126 60 125I-ICYP -4 43 Guinea pig 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
CHEMBL452861 3126 60 125I-ICYP -4 43 Guinea pig 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
DB00571 3126 60 125I-ICYP -4 43 Guinea pig 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
165193 3126 60 125I-CYP 1 43 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
2303 3126 60 125I-CYP 1 43 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
4946 3126 60 125I-CYP 1 43 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
564 3126 60 125I-CYP 1 43 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
62882 3126 60 125I-CYP 1 43 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
63 3126 60 125I-CYP 1 43 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
66366 3126 60 125I-CYP 1 43 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
91536 3126 60 125I-CYP 1 43 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
CHEMBL27 3126 60 125I-CYP 1 43 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
CHEMBL452861 3126 60 125I-CYP 1 43 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
DB00571 3126 60 125I-CYP 1 43 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
165193 3126 60 125I-ICYP -4 43 Guinea pig 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
2303 3126 60 125I-ICYP -4 43 Guinea pig 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
4946 3126 60 125I-ICYP -4 43 Guinea pig 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
564 3126 60 125I-ICYP -4 43 Guinea pig 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
62882 3126 60 125I-ICYP -4 43 Guinea pig 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
63 3126 60 125I-ICYP -4 43 Guinea pig 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
66366 3126 60 125I-ICYP -4 43 Guinea pig 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
91536 3126 60 125I-ICYP -4 43 Guinea pig 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
CHEMBL27 3126 60 125I-ICYP -4 43 Guinea pig 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
CHEMBL452861 3126 60 125I-ICYP -4 43 Guinea pig 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
DB00571 3126 60 125I-ICYP -4 43 Guinea pig 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
3682 188837 7 UNDEFINED 1 8 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 277 6 2 3 2.6 Cc1ccc(OCC(O)C(C)NC(C)C)c2c1CCC2 None
CHEMBL1256784 188837 7 UNDEFINED 1 8 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 277 6 2 3 2.6 Cc1ccc(OCC(O)C(C)NC(C)C)c2c1CCC2 None
CHEMBL513389 188837 7 UNDEFINED 1 8 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 277 6 2 3 2.6 Cc1ccc(OCC(O)C(C)NC(C)C)c2c1CCC2 None
None 214400 0 125I-ICYP 8 2 Guinea pig 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 363 5 3 6 2.7 COC1=CC(=CC(=C1OC)OC)CC2C3=CC(=C(C(=C3CCN2)F)O)O None
2585 788 100 125I-CYP 1 22 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
522 788 100 125I-CYP 1 22 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
551 788 100 125I-CYP 1 22 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
CHEMBL723 788 100 125I-CYP 1 22 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
DB01136 788 100 125I-CYP 1 22 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
2176 3065 66 125I-ICYP -5 27 Guinea pig 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
4828 3065 66 125I-ICYP -5 27 Guinea pig 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
91 3065 66 125I-ICYP -5 27 Guinea pig 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
CHEMBL500 3065 66 125I-ICYP -5 27 Guinea pig 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
DB00960 3065 66 125I-ICYP -5 27 Guinea pig 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
137 367 47 125I-CYP -3 12 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
2119 367 47 125I-CYP -3 12 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
563 367 47 125I-CYP -3 12 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
66368 367 47 125I-CYP -3 12 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
CHEMBL266195 367 47 125I-CYP -3 12 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
DB00866 367 47 125I-CYP -3 12 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
3682 188837 7 125I-Pindolol -3 8 Rat 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 277 6 2 3 2.6 Cc1ccc(OCC(O)C(C)NC(C)C)c2c1CCC2 None
CHEMBL1256784 188837 7 125I-Pindolol -3 8 Rat 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 277 6 2 3 2.6 Cc1ccc(OCC(O)C(C)NC(C)C)c2c1CCC2 None
CHEMBL513389 188837 7 125I-Pindolol -3 8 Rat 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 277 6 2 3 2.6 Cc1ccc(OCC(O)C(C)NC(C)C)c2c1CCC2 None
3682 188837 7 125I-ICYP -3 8 Rat 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 277 6 2 3 2.6 Cc1ccc(OCC(O)C(C)NC(C)C)c2c1CCC2 None
CHEMBL1256784 188837 7 125I-ICYP -3 8 Rat 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 277 6 2 3 2.6 Cc1ccc(OCC(O)C(C)NC(C)C)c2c1CCC2 None
CHEMBL513389 188837 7 125I-ICYP -3 8 Rat 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 277 6 2 3 2.6 Cc1ccc(OCC(O)C(C)NC(C)C)c2c1CCC2 None
3682 188837 7 125I-ICYP -3 8 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 277 6 2 3 2.6 Cc1ccc(OCC(O)C(C)NC(C)C)c2c1CCC2 None
CHEMBL1256784 188837 7 125I-ICYP -3 8 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 277 6 2 3 2.6 Cc1ccc(OCC(O)C(C)NC(C)C)c2c1CCC2 None
CHEMBL513389 188837 7 125I-ICYP -3 8 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 277 6 2 3 2.6 Cc1ccc(OCC(O)C(C)NC(C)C)c2c1CCC2 None
5806 102690 16 3H-DHA -1 3 Human 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 247 4 2 2 3.0 CC(C)NCC(O)c1ccc(Cl)c(Cl)c1 None
CHEMBL30816 102690 16 3H-DHA -1 3 Human 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 247 4 2 2 3.0 CC(C)NCC(O)c1ccc(Cl)c(Cl)c1 None
202 1475 0 UNDEFINED -9 33 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
60835 1475 0 UNDEFINED -9 33 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
972 1475 0 UNDEFINED -9 33 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
CHEMBL1175 1475 0 UNDEFINED -9 33 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
DB00476 1475 0 UNDEFINED -9 33 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
121881 3421 21 125I-CYP -48977 15 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 382 6 1 6 3.4 CCCCN1CCC(CC1)COC(=O)c1cc(Cl)c(c2c1OCCO2)N None
256 3421 21 125I-CYP -48977 15 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 382 6 1 6 3.4 CCCCN1CCC(CC1)COC(=O)c1cc(Cl)c(c2c1OCCO2)N None
CHEMBL68131 3421 21 125I-CYP -48977 15 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 382 6 1 6 3.4 CCCCN1CCC(CC1)COC(=O)c1cc(Cl)c(c2c1OCCO2)N None
46222048 8881 0 UNDEFINED -4365 13 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 260 4 1 2 4.0 CC(C)(C)c1ccc(SCCc2c[nH]cn2)cc1 None
CHEMBL1098230 8881 0 UNDEFINED -4365 13 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 260 4 1 2 4.0 CC(C)(C)c1ccc(SCCc2c[nH]cn2)cc1 None
18922713 98033 0 3H-DHA -12882 9 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 298 6 1 2 4.0 CCCN(CCC)C1Cc2c[nH]c3ccc(C(C)=O)c(c23)C1 None
CHEMBL276031 98033 0 3H-DHA -12882 9 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 298 6 1 2 4.0 CCCN(CCC)C1Cc2c[nH]c3ccc(C(C)=O)c(c23)C1 None
5656 201368 82 UNDEFINED -7 43 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 277 5 1 3 3.0 COc1ccc(C(CN(C)C)C2(O)CCCCC2)cc1 None
CHEMBL637 201368 82 UNDEFINED -7 43 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 277 5 1 3 3.0 COc1ccc(C(CN(C)C)C2(O)CCCCC2)cc1 None
54841 201428 51 UNDEFINED -1 30 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 255 6 1 2 3.7 CNCC[C@@H](Oc1ccccc1C)c1ccccc1 None
CHEMBL641 201428 51 UNDEFINED -1 30 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 255 6 1 2 3.7 CNCC[C@@H](Oc1ccccc1C)c1ccccc1 None
104911 214239 0 3H-DHA -13182 38 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 530 7 0 5 5.1 COC1=CC=CC=C1N2CCN(CC2)CCN(C3=CC=CC=N3)C(=O)C4CCCCC4.Cl.Cl.Cl None
3075702 215584 0 3H-CPG-12177 (-) -2 37 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 198 3 1 3 1.5 C1CNC1COC2=CN=C(C=C2)Cl None
5 139 66 3H-DHA -23442 55 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 66 3H-DHA -23442 55 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 66 3H-DHA -23442 55 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 66 3H-DHA -23442 55 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
1862 161 14 UNDEFINED -10 7 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 187 2 4 4 0.2 NCC(c1cc(O)c(cc1F)O)O None
510 161 14 UNDEFINED -10 7 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 187 2 4 4 0.2 NCC(c1cc(O)c(cc1F)O)O None
CHEMBL281232 161 14 UNDEFINED -10 7 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 187 2 4 4 0.2 NCC(c1cc(O)c(cc1F)O)O None
179 396 107 125I-Iodopindolol -4365 51 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
179 396 107 3H-DHA -4365 51 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
2159 396 107 125I-Iodopindolol -4365 51 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
2159 396 107 3H-DHA -4365 51 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
963 396 107 125I-Iodopindolol -4365 51 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
963 396 107 3H-DHA -4365 51 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
CHEMBL243712 396 107 125I-Iodopindolol -4365 51 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
CHEMBL243712 396 107 3H-DHA -4365 51 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
DB06288 396 107 125I-Iodopindolol -4365 51 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
DB06288 396 107 3H-DHA -4365 51 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
180 397 50 3H-DHA -19498 39 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
200 397 50 3H-DHA -19498 39 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2160 397 50 3H-DHA -19498 39 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
CHEMBL629 397 50 3H-DHA -19498 39 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
DB00321 397 50 3H-DHA -19498 39 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
125564 659 88 3H-DHA -17378 7 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 367 3 0 3 4.7 CCN1CCN(CC1)c1nc2CCCCCCc2c(c1)c1ccc(cc1)F None
388 659 88 3H-DHA -17378 7 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 367 3 0 3 4.7 CCN1CCN(CC1)c1nc2CCCCCCc2c(c1)c1ccc(cc1)F None
7670 659 88 3H-DHA -17378 7 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 367 3 0 3 4.7 CCN1CCN(CC1)c1nc2CCCCCCc2c(c1)c1ccc(cc1)F None
CHEMBL178803 659 88 3H-DHA -17378 7 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 367 3 0 3 4.7 CCN1CCN(CC1)c1nc2CCCCCCc2c(c1)c1ccc(cc1)F None
DB09223 659 88 3H-DHA -17378 7 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 367 3 0 3 4.7 CCN1CCN(CC1)c1nc2CCCCCCc2c(c1)c1ccc(cc1)F None
2726 904 64 125I-Pindolol -5888 73 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
2726 904 64 3H-DHA -5888 73 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 904 64 125I-Pindolol -5888 73 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 904 64 3H-DHA -5888 73 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 904 64 125I-Pindolol -5888 73 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 904 64 3H-DHA -5888 73 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 904 64 125I-Pindolol -5888 73 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 904 64 3H-DHA -5888 73 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 904 64 125I-Pindolol -5888 73 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 904 64 3H-DHA -5888 73 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
11976 905 54 3H-DHA -9332 24 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
667467 905 54 3H-DHA -9332 24 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
CHEMBL908 905 54 3H-DHA -9332 24 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
DB01239 905 54 3H-DHA -9332 24 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
135398737 942 89 125I-Pindolol -190 92 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398737 942 89 3H-DHA -4168 92 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 942 89 125I-Pindolol -190 92 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 942 89 3H-DHA -4168 92 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 942 89 125I-Pindolol -190 92 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 942 89 3H-DHA -4168 92 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 942 89 125I-Pindolol -190 92 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 942 89 3H-DHA -4168 92 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 942 89 125I-Pindolol -190 92 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 942 89 3H-DHA -4168 92 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
2147 1369 16 3H-DHA -53 7 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 135 2 1 1 1.6 C[C@@H](Cc1ccccc1)N None
5826 1369 16 3H-DHA -53 7 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 135 2 1 1 1.6 C[C@@H](Cc1ccccc1)N None
841 1369 16 3H-DHA -53 7 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 135 2 1 1 1.6 C[C@@H](Cc1ccccc1)N None
CHEMBL612 1369 16 3H-DHA -53 7 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 135 2 1 1 1.6 C[C@@H](Cc1ccccc1)N None
DB01576 1369 16 3H-DHA -53 7 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 135 2 1 1 1.6 C[C@@H](Cc1ccccc1)N None
681 1432 65 3H-DHA -707 39 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
940 1432 65 3H-DHA -707 39 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
947 1432 65 3H-DHA -707 39 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
CHEMBL59 1432 65 3H-DHA -707 39 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
DB00988 1432 65 3H-DHA -707 39 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
1209 1620 69 3H-DHA -1862 32 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
203 1620 69 3H-DHA -1862 32 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
3386 1620 69 3H-DHA -1862 32 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
CHEMBL41 1620 69 3H-DHA -1862 32 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
DB00472 1620 69 3H-DHA -1862 32 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
1212 1624 45 125I-Pindolol -19952 66 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 1624 45 125I-Pindolol -19952 66 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 1624 45 125I-Pindolol -19952 66 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 1624 45 125I-Pindolol -19952 66 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 1624 45 125I-Pindolol -19952 66 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
119376 1803 41 125I-CYP -54954 27 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C None
247 1803 41 125I-CYP -54954 27 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C None
CHEMBL33884 1803 41 125I-CYP -54954 27 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C None
1353 1872 85 125I-Pindolol -446 86 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
1353 1872 85 3H-DHA -446 86 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
1353 1872 85 3H-DHA -6918 86 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1872 85 125I-Pindolol -446 86 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1872 85 3H-DHA -446 86 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1872 85 3H-DHA -6918 86 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1872 85 125I-Pindolol -446 86 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1872 85 3H-DHA -446 86 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1872 85 3H-DHA -6918 86 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1872 85 125I-Pindolol -446 86 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1872 85 3H-DHA -446 86 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1872 85 3H-DHA -6918 86 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1872 85 125I-Pindolol -446 86 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1872 85 3H-DHA -446 86 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1872 85 3H-DHA -6918 86 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3294 1967 106 3H-CGP-12177 -14454 45 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
71360 1967 106 3H-CGP-12177 -14454 45 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
87 1967 106 3H-CGP-12177 -14454 45 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
CHEMBL14376 1967 106 3H-CGP-12177 -14454 45 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
DB04946 1967 106 3H-CGP-12177 -14454 45 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
1427 1974 50 3H-DHA -977 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
357 1974 50 3H-DHA -977 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
3696 1974 50 3H-DHA -977 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
CHEMBL11 1974 50 3H-DHA -977 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
DB00458 1974 50 3H-DHA -977 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
1613 2306 44 125I-Pindolol -2754 45 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 2306 44 125I-Pindolol -2754 45 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 2306 44 125I-Pindolol -2754 45 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 2306 44 125I-Pindolol -2754 45 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 2306 44 125I-Pindolol -2754 45 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
18971832 2375 0 125I-CYP -1621 13 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 351 3 2 2 4.0 CN(C1CCc2c(C1)c1cc(ccc1[nH]2)NC(=O)c1ccc(cc1)F)C None
21 2375 0 125I-CYP -1621 13 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 351 3 2 2 4.0 CN(C1CCc2c(C1)c1cc(ccc1[nH]2)NC(=O)c1ccc(cc1)F)C None
CHEMBL3186179 2375 0 125I-CYP -1621 13 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 351 3 2 2 4.0 CN(C1CCc2c(C1)c1cc(ccc1[nH]2)NC(=O)c1ccc(cc1)F)C None
134 2468 19 125I-Pindolol -8511 68 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2468 19 125I-Pindolol -8511 68 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2468 19 125I-Pindolol -8511 68 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2468 19 125I-Pindolol -8511 68 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2468 19 125I-Pindolol -8511 68 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1782 2472 81 3H-DHA -676 23 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC None
241 2472 81 3H-DHA -676 23 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC None
4168 2472 81 3H-DHA -676 23 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC None
CHEMBL86 2472 81 3H-DHA -676 23 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC None
DB01233 2472 81 3H-DHA -676 23 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC None
1890 2708 44 3H-DHA -1548 16 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl None
4449 2708 44 3H-DHA -1548 16 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl None
7247 2708 44 3H-DHA -1548 16 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl None
CHEMBL623 2708 44 3H-DHA -1548 16 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl None
DB01149 2708 44 3H-DHA -1548 16 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl None
484 2804 45 125I-CYP -31 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
484 2804 45 125I-ICYP -31 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
484 2804 45 3H-DHA -31 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
484 2804 45 UNDEFINED -31 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
951 2804 45 125I-CYP -31 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
951 2804 45 125I-ICYP -31 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
951 2804 45 3H-DHA -31 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
951 2804 45 UNDEFINED -31 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
CHEMBL432 2804 45 125I-CYP -31 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
CHEMBL432 2804 45 125I-ICYP -31 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
CHEMBL432 2804 45 3H-DHA -31 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
CHEMBL432 2804 45 UNDEFINED -31 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
15897 2807 0 125I-Pindolol -354 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
215 2807 0 125I-Pindolol -354 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
CHEMBL1979333 2807 0 125I-Pindolol -354 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
135398745 2858 108 125I-Pindolol -331 66 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
135398745 2858 108 3H-DHA -331 66 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
135398745 2858 108 UNDEFINED -331 66 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2858 108 125I-Pindolol -331 66 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2858 108 3H-DHA -331 66 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2858 108 UNDEFINED -331 66 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2858 108 125I-Pindolol -331 66 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2858 108 3H-DHA -331 66 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2858 108 UNDEFINED -331 66 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2858 108 125I-Pindolol -331 66 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2858 108 3H-DHA -331 66 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2858 108 UNDEFINED -331 66 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
2105 2993 34 3H-CGP-12177 -16218 33 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
47811 2993 34 3H-CGP-12177 -16218 33 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
48 2993 34 3H-CGP-12177 -16218 33 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
CHEMBL531 2993 34 3H-CGP-12177 -16218 33 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
DB01186 2993 34 3H-CGP-12177 -16218 33 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
2136 3034 29 3H-DHA -2187 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 303 8 0 2 4.2 ClCCN(C(COc1ccccc1)C)Cc1ccccc1 None
4768 3034 29 3H-DHA -2187 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 303 8 0 2 4.2 ClCCN(C(COc1ccccc1)C)Cc1ccccc1 None
7268 3034 29 3H-DHA -2187 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 303 8 0 2 4.2 ClCCN(C(COc1ccccc1)C)Cc1ccccc1 None
CHEMBL753 3034 29 3H-DHA -2187 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 303 8 0 2 4.2 ClCCN(C(COc1ccccc1)C)Cc1ccccc1 None
DB00925 3034 29 3H-DHA -2187 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 303 8 0 2 4.2 ClCCN(C(COc1ccccc1)C)Cc1ccccc1 None
2142 3035 54 3H-DHA -3801 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
4920903 3035 54 3H-DHA -3801 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
502 3035 54 3H-DHA -3801 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
5775 3035 54 3H-DHA -3801 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
CHEMBL597 3035 54 3H-DHA -3801 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
DB00692 3035 54 3H-DHA -3801 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
2146 3039 63 3H-DHA -1445 8 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O None
485 3039 63 3H-DHA -1445 8 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O None
6041 3039 63 3H-DHA -1445 8 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O None
CHEMBL1215 3039 63 3H-DHA -1445 8 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O None
DB00388 3039 63 3H-DHA -1445 8 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O None
2202 3071 91 3H-CGP-12177 -316 21 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
4850 3071 91 3H-CGP-12177 -316 21 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
49 3071 91 3H-CGP-12177 -316 21 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
CHEMBL1371770 3071 91 3H-CGP-12177 -316 21 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
DB12478 3071 91 3H-CGP-12177 -316 21 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
4508 3078 91 3H-DHA -1995 13 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 183 3 4 4 0.4 CNCC(c1ccc(c(c1)O)O)O None
4866774 3078 91 3H-DHA -1995 13 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 183 3 4 4 0.4 CNCC(c1ccc(c(c1)O)O)O None
509 3078 91 3H-DHA -1995 13 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 183 3 4 4 0.4 CNCC(c1ccc(c(c1)O)O)O None
838 3078 91 3H-DHA -1995 13 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 183 3 4 4 0.4 CNCC(c1ccc(c(c1)O)O)O None
CHEMBL1740 3078 91 3H-DHA -1995 13 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 183 3 4 4 0.4 CNCC(c1ccc(c(c1)O)O)O None
3486 3096 51 3H-DHA -60 11 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C None
3486 3096 51 125I-ICYP -436 11 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C None
4883 3096 51 3H-DHA -60 11 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C None
4883 3096 51 125I-ICYP -436 11 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C None
555 3096 51 3H-DHA -60 11 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C None
555 3096 51 125I-ICYP -436 11 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C None
CHEMBL6995 3096 51 3H-DHA -60 11 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C None
CHEMBL6995 3096 51 125I-ICYP -436 11 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C None
DB01297 3096 51 3H-DHA -60 11 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C None
DB01297 3096 51 125I-ICYP -436 11 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C None
119570 3098 90 125I-Pindolol -1202 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
119570 3098 90 3H-CGP-12177 -1202 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
2233 3098 90 125I-Pindolol -1202 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
2233 3098 90 3H-CGP-12177 -1202 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
953 3098 90 125I-Pindolol -1202 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
953 3098 90 3H-CGP-12177 -1202 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
CHEMBL301265 3098 90 125I-Pindolol -1202 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
CHEMBL301265 3098 90 3H-CGP-12177 -1202 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
DB00413 3098 90 125I-Pindolol -1202 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
DB00413 3098 90 3H-CGP-12177 -1202 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
2284 3121 27 3H-DHA -4265 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
4926 3121 27 3H-DHA -4265 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
7281 3121 27 3H-DHA -4265 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
CHEMBL564 3121 27 3H-DHA -4265 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
DB00420 3121 27 3H-DHA -4265 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
165193 3126 60 3H-DHA -22 43 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
2303 3126 60 3H-DHA -22 43 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
4946 3126 60 3H-DHA -22 43 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
564 3126 60 3H-DHA -22 43 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
62882 3126 60 3H-DHA -22 43 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
63 3126 60 3H-DHA -22 43 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
66366 3126 60 3H-DHA -22 43 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
91536 3126 60 3H-DHA -22 43 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
CHEMBL27 3126 60 3H-DHA -22 43 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
CHEMBL452861 3126 60 3H-DHA -22 43 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
DB00571 3126 60 3H-DHA -22 43 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
243 3141 85 125I-ICYP -1096 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
3052762 3141 85 125I-ICYP -1096 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
3502 3141 85 125I-ICYP -1096 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
CHEMBL117287 3141 85 125I-ICYP -1096 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
DB06480 3141 85 125I-ICYP -1096 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
2337 3193 72 125I-Pindolol -72 63 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3193 72 125I-Pindolol -72 63 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3193 72 125I-Pindolol -72 63 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3193 72 125I-Pindolol -72 63 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3193 72 125I-Pindolol -72 63 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
2 3198 19 3H-CGP-12177 -6606 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 None
54562 3198 19 3H-CGP-12177 -6606 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 None
CHEMBL240773 3198 19 3H-CGP-12177 -6606 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 None
3033769 3217 54 3H-DHA -2754 19 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
3299 3217 54 3H-DHA -2754 19 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
94 3217 54 3H-DHA -2754 19 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
CHEMBL8809 3217 54 3H-DHA -2754 19 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
DB12518 3217 54 3H-DHA -2754 19 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
1562 3225 22 3H-DHA - 1 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 135 2 1 1 1.6 C[C@H](Cc1ccccc1)N None
2146 3225 22 3H-DHA - 1 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 135 2 1 1 1.6 C[C@H](Cc1ccccc1)N None
32893 3225 22 3H-DHA - 1 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 135 2 1 1 1.6 C[C@H](Cc1ccccc1)N None
CHEMBL19393 3225 22 3H-DHA - 1 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 135 2 1 1 1.6 C[C@H](Cc1ccccc1)N None
2389 3267 114 125I-Pindolol -2089 68 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3267 114 125I-Pindolol -2089 68 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3267 114 125I-Pindolol -2089 68 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3267 114 125I-Pindolol -2089 68 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3267 114 125I-Pindolol -2089 68 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
2402 3306 58 3H-CGP-12177 -660 25 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
5095 3306 58 3H-CGP-12177 -660 25 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
7295 3306 58 3H-CGP-12177 -660 25 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
CHEMBL589 3306 58 3H-CGP-12177 -660 25 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
DB00268 3306 58 3H-CGP-12177 -660 25 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
183782 3334 15 3H-CGP-12177 -2398 15 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 352 8 1 4 4.4 CCCCN1CCC(CC1)CCC(=O)c1cc(Cl)c(cc1OC)N None
237 3334 15 3H-CGP-12177 -2398 15 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 352 8 1 4 4.4 CCCCN1CCC(CC1)CCC(=O)c1cc(Cl)c(cc1OC)N None
CHEMBL85251 3334 15 3H-CGP-12177 -2398 15 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 352 8 1 4 4.4 CCCCN1CCC(CC1)CCC(=O)c1cc(Cl)c(cc1OC)N None
128563 3395 28 125I-Pindolol -2398 42 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
1666 3395 28 125I-Pindolol -2398 42 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
CHEMBL445332 3395 28 125I-Pindolol -2398 42 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
DB12327 3395 28 125I-Pindolol -2398 42 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
2464 3570 52 3H-DHA -7 6 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C None
5253 3570 52 3H-DHA -7 6 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C None
7297 3570 52 3H-DHA -7 6 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C None
CHEMBL471 3570 52 3H-DHA -7 6 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C None
DB00489 3570 52 3H-DHA -7 6 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C None
6917970 3622 54 125I-Pindolol -2290 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O None
8370 3622 54 125I-Pindolol -2290 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O None
CHEMBL487387 3622 54 125I-Pindolol -2290 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O None
1577 3634 104 3H-DHA -389 26 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
164512405 3634 104 3H-DHA -389 26 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
2537 3634 104 3H-DHA -389 26 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
5355 3634 104 3H-DHA -389 26 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
5501 3634 104 3H-DHA -389 26 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
643497 3634 104 3H-DHA -389 26 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
688272 3634 104 3H-DHA -389 26 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
958 3634 104 3H-DHA -389 26 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
960 3634 104 3H-DHA -389 26 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL196677 3634 104 3H-DHA -389 26 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL26 3634 104 3H-DHA -389 26 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL267044 3634 104 3H-DHA -389 26 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
DB00391 3634 104 3H-DHA -389 26 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
DB16021 3634 104 3H-DHA -389 26 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
2598 3707 52 125I-CYP -6 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 225 3 4 4 1.5 OC(c1cc(O)cc(c1)O)CNC(C)(C)C None
2598 3707 52 3H-DHA -6 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 225 3 4 4 1.5 OC(c1cc(O)cc(c1)O)CNC(C)(C)C None
5403 3707 52 125I-CYP -6 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 225 3 4 4 1.5 OC(c1cc(O)cc(c1)O)CNC(C)(C)C None
5403 3707 52 3H-DHA -6 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 225 3 4 4 1.5 OC(c1cc(O)cc(c1)O)CNC(C)(C)C None
560 3707 52 125I-CYP -6 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 225 3 4 4 1.5 OC(c1cc(O)cc(c1)O)CNC(C)(C)C None
560 3707 52 3H-DHA -6 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 225 3 4 4 1.5 OC(c1cc(O)cc(c1)O)CNC(C)(C)C None
CHEMBL1760 3707 52 125I-CYP -6 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 225 3 4 4 1.5 OC(c1cc(O)cc(c1)O)CNC(C)(C)C None
CHEMBL1760 3707 52 3H-DHA -6 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 225 3 4 4 1.5 OC(c1cc(O)cc(c1)O)CNC(C)(C)C None
DB00871 3707 52 125I-CYP -6 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 225 3 4 4 1.5 OC(c1cc(O)cc(c1)O)CNC(C)(C)C None
DB00871 3707 52 3H-DHA -6 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 225 3 4 4 1.5 OC(c1cc(O)cc(c1)O)CNC(C)(C)C None
1267 3732 43 3H-DHA -4168 28 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 None
3035905 3732 43 3H-DHA -4168 28 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 None
CHEMBL260374 3732 43 3H-DHA -4168 28 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 None
100 3733 52 125I-Pindolol -4897 56 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
100 3733 52 3H-DHA -4897 56 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 3733 52 125I-Pindolol -4897 56 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 3733 52 3H-DHA -4897 56 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 3733 52 125I-Pindolol -4897 56 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 3733 52 3H-DHA -4897 56 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 3733 52 125I-Pindolol -4897 56 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 3733 52 3H-DHA -4897 56 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 3733 52 125I-Pindolol -4897 56 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 3733 52 3H-DHA -4897 56 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
213 3780 50 125I-Pindolol -912 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
2717 3780 50 125I-Pindolol -912 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
5533 3780 50 125I-Pindolol -912 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
CHEMBL621 3780 50 125I-Pindolol -912 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
DB00656 3780 50 125I-Pindolol -912 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
185 3931 54 125I-Pindolol -30902 38 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
185 3931 54 125I-Pindolol -30902 38 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
5311271 3931 54 125I-Pindolol -30902 38 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
5311271 3931 54 125I-Pindolol -30902 38 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
CHEMBL74355 3931 54 125I-Pindolol -30902 38 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
CHEMBL74355 3931 54 125I-Pindolol -30902 38 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
DB16351 3931 54 125I-Pindolol -30902 38 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
DB16351 3931 54 125I-Pindolol -30902 38 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
2865 4064 67 125I-Pindolol -1318 54 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 4064 67 125I-Pindolol -1318 54 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 4064 67 125I-Pindolol -1318 54 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 4064 67 125I-Pindolol -1318 54 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 4064 67 125I-Pindolol -1318 54 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
103 4074 56 125I-Pindolol -416 54 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2875 4074 56 125I-Pindolol -416 54 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5736 4074 56 125I-Pindolol -416 54 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL285802 4074 56 125I-Pindolol -416 54 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
DB09225 4074 56 125I-Pindolol -416 54 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
10297 26890 29 125I-Pindolol -38 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 C[C@H](N)[C@H](O)c1ccccc1 None
CHEMBL136560 26890 29 125I-Pindolol -38 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 C[C@H](N)[C@H](O)c1ccccc1 None
7028 52086 21 3H-DHA - 1 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 165 3 2 2 1.3 CN[C@@H](C)[C@@H](O)c1ccccc1 None
CHEMBL1590 52086 21 3H-DHA - 1 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 165 3 2 2 1.3 CN[C@@H](C)[C@@H](O)c1ccccc1 None
115237 55281 113 125I-Pindolol -2754 55 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
CHEMBL1621 55281 113 125I-Pindolol -2754 55 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
54477 84216 34 3H-DHA -138 23 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC None
CHEMBL22242 84216 34 3H-DHA -138 23 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC None
21830793 91389 5 3H-8-OH-DPAT -66069 46 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 373 7 0 8 0.6 COc1ccccc1N1CCN(CCCCn2ncc(=O)n(C)c2=O)CC1 None
CHEMBL2413154 91389 5 3H-8-OH-DPAT -66069 46 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 373 7 0 8 0.6 COc1ccccc1N1CCN(CCCCn2ncc(=O)n(C)c2=O)CC1 None
6603820 95317 13 3H-Iodopindolol -1071 13 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 None
CHEMBL25856 95317 13 3H-Iodopindolol -1071 13 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 None
104870 98410 39 3H-CGP-12177 -549 21 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 209 2 1 4 1.3 C=CCN1CCc2nc(N)sc2CC1 None
5374 98410 39 3H-CGP-12177 -549 21 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 209 2 1 4 1.3 C=CCN1CCc2nc(N)sc2CC1 None
CHEMBL279085 98410 39 3H-CGP-12177 -549 21 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 209 2 1 4 1.3 C=CCN1CCc2nc(N)sc2CC1 None
172745 99648 7 UNDEFINED -70 6 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 187 2 4 4 0.2 NCC(O)c1ccc(O)c(O)c1F None
CHEMBL287587 99648 7 UNDEFINED -70 6 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 187 2 4 4 0.2 NCC(O)c1ccc(O)c(O)c1F None
7172 116178 90 3H-DHA -19 2 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 167 3 3 3 0.6 CNCC(O)c1ccc(O)cc1 None
CHEMBL33720 116178 90 3H-DHA -19 2 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 167 3 3 3 0.6 CNCC(O)c1ccc(O)cc1 None
3452843 119007 13 3H-DHA -1 10 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 516 6 2 4 5.5 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)c3ccccc3C)C2=O)c1 None
CHEMBL345686 119007 13 3H-DHA -1 10 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 516 6 2 4 5.5 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)c3ccccc3C)C2=O)c1 None
446220 132985 13 125I-Pindolol -1778 46 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 303 3 0 5 1.9 COC(=O)[C@H]1[C@@H](OC(=O)c2ccccc2)C[C@@H]2CC[C@H]1N2C None
CHEMBL370805 132985 13 125I-Pindolol -1778 46 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 303 3 0 5 1.9 COC(=O)[C@H]1[C@@H](OC(=O)c2ccccc2)C[C@@H]2CC[C@H]1N2C None
44208932 140163 6 UNDEFINED -120226 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 475 5 1 3 6.8 Cc1ccc(Cn2nc(C(=O)NC3C4(C)CCC(C4)C3(C)C)cc2-c2ccc(Cl)c(C)c2)cc1 None
CHEMBL381689 140163 6 UNDEFINED -120226 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 475 5 1 3 6.8 Cc1ccc(Cn2nc(C(=O)NC3C4(C)CCC(C4)C3(C)C)cc2-c2ccc(Cl)c(C)c2)cc1 None
1615 167217 22 125I-Pindolol -26 45 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 193 3 1 3 1.6 CNC(C)Cc1ccc2c(c1)OCO2 None
1615 167217 22 125I-Pindolol -26 45 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 193 3 1 3 1.6 CNC(C)Cc1ccc2c(c1)OCO2 None
CHEMBL43048 167217 22 125I-Pindolol -26 45 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 193 3 1 3 1.6 CNC(C)Cc1ccc2c(c1)OCO2 None
CHEMBL43048 167217 22 125I-Pindolol -26 45 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 193 3 1 3 1.6 CNC(C)Cc1ccc2c(c1)OCO2 None
4543 169972 36 3H-DHA -1995 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2ccccc21 None
CHEMBL1201156 169972 36 3H-DHA -1995 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2ccccc21 None
CHEMBL445 169972 36 3H-DHA -1995 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2ccccc21 None
43815 186327 58 3H-DHA -1995 25 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 None
CHEMBL1708 186327 58 3H-DHA -1995 25 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 None
CHEMBL490 186327 58 3H-DHA -1995 25 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 None
5280343 187681 119 125I-Pindolol -147 32 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 None
CHEMBL1520590 187681 119 125I-Pindolol -147 32 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 None
CHEMBL50 187681 119 125I-Pindolol -147 32 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 None
2771 193337 67 3H-DHA -120 27 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 None
CHEMBL1200781 193337 67 3H-DHA -120 27 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 None
CHEMBL549 193337 67 3H-DHA -120 27 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 None
162265 200578 19 125I-Pindolol -239 45 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
4786 200578 19 125I-Pindolol -239 45 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
CHEMBL61006 200578 19 125I-Pindolol -239 45 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
5281600 201327 85 125I-Pindolol -275 33 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 538 3 6 10 5.1 O=c1cc(-c2ccc(O)c(-c3c(O)cc(O)c4c(=O)cc(-c5ccc(O)cc5)oc34)c2)oc2cc(O)cc(O)c12 None
CHEMBL63354 201327 85 125I-Pindolol -275 33 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 538 3 6 10 5.1 O=c1cc(-c2ccc(O)c(-c3c(O)cc(O)c4c(=O)cc(-c5ccc(O)cc5)oc34)c2)oc2cc(O)cc(O)c12 None
1973 201781 12 3H-CGP-12177 -3 37 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 462 3 1 7 3.9 Nc1ncnc2nc(-c3ccc(N4CCOCC4)nc3)cc(-c3cccc(Br)c3)c12 None
CHEMBL1394464 201781 12 3H-CGP-12177 -3 37 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 462 3 1 7 3.9 Nc1ncnc2nc(-c3ccc(N4CCOCC4)nc3)cc(-c3cccc(Br)c3)c12 None
CHEMBL66089 201781 12 3H-CGP-12177 -3 37 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 462 3 1 7 3.9 Nc1ncnc2nc(-c3ccc(N4CCOCC4)nc3)cc(-c3cccc(Br)c3)c12 None
4976 201876 27 3H-DHA -1548 12 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 263 4 1 1 4.3 CNCCCC1c2ccccc2C=Cc2ccccc21 None
CHEMBL668 201876 27 3H-DHA -1548 12 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 263 4 1 1 4.3 CNCCCC1c2ccccc2C=Cc2ccccc21 None
2995 202690 49 3H-DHA -1412 23 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
CHEMBL1696 202690 49 3H-DHA -1412 23 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
CHEMBL72 202690 49 3H-DHA -1412 23 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
202478 202971 15 125I-Pindolol -97 26 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 219 3 1 2 3.0 CCCN1CCC[C@H](c2cccc(O)c2)C1 None
CHEMBL7393 202971 15 125I-Pindolol -97 26 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 219 3 1 2 3.0 CCCN1CCC[C@H](c2cccc(O)c2)C1 None
5311189 203123 4 125I-Pindolol -194 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 219 3 1 2 3.0 CCCN1CCC[C@@H](c2cccc(O)c2)C1 None
CHEMBL7549 203123 4 125I-Pindolol -194 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 219 3 1 2 3.0 CCCN1CCC[C@@H](c2cccc(O)c2)C1 None
4054 203780 64 3H-PL17 -1 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 179 0 1 1 2.7 CC12CC3CC(C)(C1)CC(N)(C3)C2 None
CHEMBL1699 203780 64 3H-PL17 -1 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 179 0 1 1 2.7 CC12CC3CC(C)(C1)CC(N)(C3)C2 None
CHEMBL807 203780 64 3H-PL17 -1 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 179 0 1 1 2.7 CC12CC3CC(C)(C1)CC(N)(C3)C2 None
68617 203806 60 3H-DHA -1445 26 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 None
CHEMBL1709 203806 60 3H-DHA -1445 26 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 None
CHEMBL809 203806 60 3H-DHA -1445 26 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 None
5324346 203860 53 3H-DHA -1 10 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 318 9 1 4 3.2 COCCCC/C(=N\OCCN)c1ccc(C(F)(F)F)cc1 None
CHEMBL1409 203860 53 3H-DHA -1 10 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 318 9 1 4 3.2 COCCCC/C(=N\OCCN)c1ccc(C(F)(F)F)cc1 None
CHEMBL814 203860 53 3H-DHA -1 10 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 318 9 1 4 3.2 COCCCC/C(=N\OCCN)c1ccc(C(F)(F)F)cc1 None
11954224 214164 0 125I-Pindolol -3388 60 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
11954224 214164 0 3H-DHA -3388 60 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
25058166 214171 0 3H-CGP-12177 -5011 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
6852389 214171 0 3H-CGP-12177 -5011 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
3246155 214173 0 3H-DHA -43651 17 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 307 4 0 2 4.4 CN1C2CCC1CC(C2)OC(C3=CC=CC=C3)C4=CC=CC=C4 None
11954259 214191 0 125I-Pindolol -33113 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 443 5 0 5 3.5 CN1CCN(CC1)CCC=C2C3=CC=CC=C3SC4=C2C=C(C=C4)S(=O)(=O)N(C)C None
11954259 214191 0 3H-DHA -33113 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 443 5 0 5 3.5 CN1CCN(CC1)CCC=C2C3=CC=CC=C3SC4=C2C=C(C=C4)S(=O)(=O)N(C)C None
44134711 214205 0 3H-DHA -112201 14 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 340 6 2 4 2.8 CCC1=CC(=C(C(=C1O)C(=O)NCC2CCCN2CC)OC)Cl None
21722 214229 0 3H-DHA -120 6 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 284 4 0 2 4.3 CN(C)CCCN1C2=C(CCCCCC2)C3=CC=CC=C31 None
444 214235 0 3H-DHA -2089 18 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 239 3 1 2 3.3 CC(C(=O)C1=CC(=CC=C1)Cl)NC(C)(C)C None
104911 214239 0 125I-Pindolol -13182 38 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 530 7 0 5 5.1 COC1=CC=CC=C1N2CCN(CC2)CCN(C3=CC=CC=N3)C(=O)C4CCCCC4.Cl.Cl.Cl None
None 214246 0 3H-CGP-12177 -6309 14 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 453 9 2 6 2.6 COC1=CC(=C(C=C1C(=O)CCC2CCN(CC2)CCNS(=O)(=O)C)Cl)N.Cl None
6102 214261 0 3H-DHA -6 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 167 3 3 3 0.6 CNCC(C1=CC(=CC=C1)O)O None
None 214348 0 3H-DHA -1 13 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 164 3 1 3 0.8 C1CNC1COC2=CN=CC=C2 None
119380 214349 0 3H-DHA 1 8 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 166 1 0 3 1.8 CC1=NOC(=C1)C2CCCN2C None
16219195 214352 0 3H-DHA -12 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 325 1 1 5 2.9 CN1CCC2=CC3=C(C4=C2C1CC5=C4C(=C(C=C5)OC)O)OCO3 None
3947 214368 0 3H-DHA -1479 16 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 418 7 0 3 5.8 CN(CCCN1C2=CC=CC=C2CCC3=CC=CC=C31)CC(=O)C4=CC=C(C=C4)Cl None
None 214399 0 125I-ICYP -2 4 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 381 5 3 5 -1.5 COC1=CC(=CC(=C1OC)OC)CC2C3=CC(=C(C=C3CC[NH2+]2)O)O.[Cl-] None
None 214399 0 125I-ICYP -2 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 381 5 3 5 -1.5 COC1=CC(=CC(=C1OC)OC)CC2C3=CC(=C(C=C3CC[NH2+]2)O)O.[Cl-] None
None 214407 0 3H-DHA -1258 2 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 408 7 2 4 3.9 CC(C1=CC=CC=N1)C2=C(CC3=CC=CC=C32)CCN(C)C.C(=CC(=O)O)C(=O)O None
25137849 214415 0 125I-Pindolol -4 41 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 165 3 2 2 1.3 CC(C(C1=CC=CC=C1)O)NC None
25137849 214415 0 3H-DHA -4 41 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 165 3 2 2 1.3 CC(C(C1=CC=CC=C1)O)NC None
71290 214415 0 125I-Pindolol -4 41 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 165 3 2 2 1.3 CC(C(C1=CC=CC=C1)O)NC None
71290 214415 0 3H-DHA -4 41 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 165 3 2 2 1.3 CC(C(C1=CC=CC=C1)O)NC None
None 214416 0 3H-DHA - 1 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 294 5 3 4 1.1 CC(C(C1=CC=C(C=C1)NS(=O)(=O)C)O)NC.Cl None
3337 214431 0 125I-Pindolol -199 41 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
65801 214431 0 125I-Pindolol -199 41 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
66264 214431 0 125I-Pindolol -199 41 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
91452 214431 0 125I-Pindolol -199 41 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
None 214487 0 3H-DHA -501 3 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 468 12 0 9 -0.1 C1COCCN1CCCN2CN(CN(C2)CCCN3CCOCC3)CCCN4CCOCC4 None
None 214488 0 3H-DHA -1258 3 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 434 6 4 8 2.2 CC(C)O.COC1=C(C=CC(=C1)CC2COC(=O)C2(CC3=CC(=C(C=C3)O)OC)O)O None
None 214489 0 3H-DHA -3981 3 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 234 2 1 3 2.0 CC(=O)NC1=C(C(=C(C=C1F)F)F)[N+](=O)[O-] None
None 214490 0 3H-DHA -4677 3 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 314 0 1 2 4.0 CC12CCC(CC1CCC3C2CCC4(C3CCC4=O)C)(C#C)O None
None 214491 0 3H-DHA -6025 3 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 329 5 1 3 4.5 CCCC1=CC2=C(C=C1NC(=O)C3C(C3(C)C)C=C(C)C)OCO2 None
None 214492 0 3H-DHA -8317 21 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 416 9 3 4 2.8 C1=CC(=CC=C1CCNC(N)SCCCC2=CN=CN2)I None
None 214550 0 125I-Pindolol -1 34 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 240 7 4 6 -0.8 C(C(C(=O)O)N)SSCC(C(=O)O)N None
None 214551 0 125I-Pindolol -1 34 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 149 4 2 3 0.2 CSCCC(C(=O)O)N None
None 214552 0 125I-Pindolol -1 34 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 135 3 3 3 -0.3 C(CS)C(C(=O)O)N None
None 214553 0 125I-Pindolol -1 34 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 121 2 3 3 -0.7 C(C(C(=O)O)N)S None
None 214554 0 125I-Pindolol -1 29 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 117 0 1 3 -0.0 C1CSC(=O)C1N None
None 214555 0 125I-Pindolol -1 40 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 3 3 3 -1.4 C(C(C(=O)O)N)S(=O)O None
None 214556 0 125I-Pindolol -1 39 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 169 3 3 4 -1.7 C(C(C(=O)O)N)S(=O)(=O)O None
None 214557 0 125I-Pindolol -1 30 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 183 4 3 4 -1.3 C(CS(=O)(=O)O)C(C(=O)O)N None
None 214564 0 125I-Pindolol -13 41 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 149 2 1 2 1.2 CC(C(=O)C1=CC=CC=C1)N None
1576 214565 0 125I-Pindolol -16 41 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 163 3 1 2 1.5 CC(C(=O)C1=CC=CC=C1)NC None
None 214566 0 125I-Pindolol -16 28 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 536 11 1 4 9.0 CC(C)C(=O)C12C(=O)C(=C(C(C1=O)(CC(C2(C)CCC=C(C)C)CC=C(C)C)CC=C(C)C)O)CC=C(C)C None
4978 214567 0 125I-Pindolol -16 28 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 520 1 7 9 4.3 CC1=CC(=C2C3=C1C4=C5C(=C(C=C4CO)O)C(=O)C6=C(C=C(C7=C6C5=C3C8=C7C(=CC(=C8C2=O)O)O)O)O)O None
None 214568 0 125I-Pindolol -3 28 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 464 4 8 12 -0.6 C1=CC(=C(C=C1C2=C(C(=C3C(=CC(=O)C=C3O2)O)O)OC4C(C(C(C(O4)CO)O)O)O)O)O None
None 214569 0 125I-Pindolol -281 28 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 610 6 10 16 -1.7 CC1C(C(C(C(O1)OCC2C(C(C(C(O2)OC3=C(OC4=CC(=CC(=C4C3=O)O)O)C5=CC(=C(C=C5)O)O)O)O)O)O)O)O None
None 214570 0 125I-Pindolol -1 28 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 448 3 7 11 0.4 CC1C(C(C(C(O1)OC2=C(OC3=CC(=O)C=C(C3=C2O)O)C4=CC(=C(C=C4)O)O)O)O)O None
None 214580 0 3H-CGP-12177 -13182 19 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 451 8 2 4 3.2 CCNC(=O)N(CCCN(C)C)C(=O)C1CC2C(CC3=CNC4=CC=CC2=C34)N(C1)CC=C None
None 214581 0 3H-CGP-12177 -1862 19 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 246 2 1 4 1.6 CCCN1CCCC2C1CC3=CN=C(N=C3C2)N None
None 214628 0 3H-DHA -1 2 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 313 5 1 3 3.5 CN(C)CC(C1=CC=C(C=C1)OC)C2(CCCCC2)O.Cl None
None 214693 0 Functional -660 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 322 5 2 3 4.1 CC(CC1=CNC2=C1C=C(C=C2)OCC3=CC=CS3)N.Cl None
None 214693 0 UNDEFINED -660 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 322 5 2 3 4.1 CC(CC1=CNC2=C1C=C(C=C2)OCC3=CC=CS3)N.Cl None
None 214737 0 125I-Pindolol -4570 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 347 6 0 3 5.0 CC(=O)N(CC1=CC=CC=C1OC)C2=CC=CC=C2OC3=CC=CC=C3 None
None 214742 0 3H-DHA -10471285 17 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 372 2 1 3 4.4 CC(C)(C)C1=CC=C(C=C1)NC(=O)N2CCN(CC2)C3=C(C=CC=N3)Cl None
None 215922 0 UNDEFINED - 1 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 568 9 7 9 0.7 CCC1=C(C=C2CC(CC2=C1)NCC(C3=C4C=CC(=O)NC4=C(C=C3)OC5C(C(C(C(O5)C(=O)O)O)O)O)O)CC None
1499 2052 43 125I-ICYP -9 17 Guinea pig 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
3779 2052 43 125I-ICYP -9 17 Guinea pig 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
536 2052 43 125I-ICYP -9 17 Guinea pig 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
CHEMBL434 2052 43 125I-ICYP -9 17 Guinea pig 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
DB01064 2052 43 125I-ICYP -9 17 Guinea pig 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
1028 287 69 3H-DHA -89 30 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
139148732 287 69 3H-DHA -89 30 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
479 287 69 3H-DHA -89 30 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
5816 287 69 3H-DHA -89 30 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
CHEMBL679 287 69 3H-DHA -89 30 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
DB00668 287 69 3H-DHA -89 30 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
None 215917 0 UNDEFINED - 1 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 448 10 4 4 4.7 CCCCC1=C(C=C2CC(CC2=C1)NCC(C3=C4C=CC(=O)NC4=C(C=C3)O)O)CCCC None
2405 658 71 125I-CYP -58 4 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 325 12 2 5 2.4 OC(COc1ccc(cc1)COCCOC(C)C)CNC(C)C None
380 658 71 125I-CYP -58 4 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 325 12 2 5 2.4 OC(COc1ccc(cc1)COCCOC(C)C)CNC(C)C None
7129 658 71 125I-CYP -58 4 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 325 12 2 5 2.4 OC(COc1ccc(cc1)COCCOC(C)C)CNC(C)C None
CHEMBL645 658 71 125I-CYP -58 4 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 325 12 2 5 2.4 OC(COc1ccc(cc1)COCCOC(C)C)CNC(C)C None
DB00612 658 71 125I-CYP -58 4 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 325 12 2 5 2.4 OC(COc1ccc(cc1)COCCOC(C)C)CNC(C)C None
None 215918 0 UNDEFINED - 1 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 420 8 4 4 3.9 CCCC1=C(C=C2CC(CC2=C1)NCC(C3=C4C=CC(=O)NC4=C(C=C3)O)O)CCC None
128658 33738 7 125I-ICYP -3 5 Guinea pig 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 363 5 3 6 2.7 COc1cc(CC2NCCc3cc(O)c(O)c(F)c32)cc(OC)c1OC None
CHEMBL142428 33738 7 125I-ICYP -3 5 Guinea pig 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 363 5 3 6 2.7 COc1cc(CC2NCCc3cc(O)c(O)c(F)c32)cc(OC)c1OC None
1499 2052 43 3H-CGP-12177 -33 17 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
3779 2052 43 3H-CGP-12177 -33 17 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
536 2052 43 3H-CGP-12177 -33 17 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
CHEMBL434 2052 43 3H-CGP-12177 -33 17 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
DB01064 2052 43 3H-CGP-12177 -33 17 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
71149 214641 0 125I-CYP 1 3 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 262 3 2 4 1.9 CC(C)(C)NCC(C1=CC(=NO1)Br)O None
123707 214732 0 125I-ICYP -3 3 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 416 9 3 6 1.8 CC1=C(C=C(C=C1)C(CNCCOC2=CC=CC=C2OC)O)S(=O)(=O)N.Cl None
123686 1942 44 125I-ICYP -109 9 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 354 9 4 5 1.7 C1=CC=C(C=C1)NC(=O)NCCNCC(COC2=CC=CC=C2C#N)O None
12581 1942 44 125I-ICYP -109 9 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 354 9 4 5 1.7 C1=CC=C(C=C1)NC(=O)NCCNCC(COC2=CC=CC=C2C#N)O None
CHEMBL11268 1942 44 125I-ICYP -109 9 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 354 9 4 5 1.7 C1=CC=C(C=C1)NC(=O)NCCNCC(COC2=CC=CC=C2C#N)O None
1499 2052 43 125I-ICYP -33 17 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
3779 2052 43 125I-ICYP -33 17 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
536 2052 43 125I-ICYP -33 17 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
CHEMBL434 2052 43 125I-ICYP -33 17 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
DB01064 2052 43 125I-ICYP -33 17 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
242 467 117 125I-Pindolol -23 52 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
242 467 117 3H-Pindolol -23 52 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 467 117 125I-Pindolol -23 52 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 467 117 3H-Pindolol -23 52 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 467 117 125I-Pindolol -23 52 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 467 117 3H-Pindolol -23 52 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 467 117 125I-Pindolol -23 52 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 467 117 3H-Pindolol -23 52 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 467 117 125I-Pindolol -23 52 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 467 117 3H-Pindolol -23 52 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
135398737 942 89 125I-ICYP -190 92 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 942 89 125I-ICYP -190 92 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 942 89 125I-ICYP -190 92 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 942 89 125I-ICYP -190 92 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 942 89 125I-ICYP -190 92 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
1786 2474 79 125I-ICYP -89 11 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O None
4171 2474 79 125I-ICYP -89 11 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O None
553 2474 79 125I-ICYP -89 11 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O None
CHEMBL13 2474 79 125I-ICYP -89 11 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O None
DB00264 2474 79 125I-ICYP -89 11 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O None
137 367 47 3H-DHA -3 12 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
2119 367 47 3H-DHA -3 12 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
563 367 47 3H-DHA -3 12 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
66368 367 47 3H-DHA -3 12 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
CHEMBL266195 367 47 3H-DHA -3 12 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
DB00866 367 47 3H-DHA -3 12 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
10455 3218 34 UNDEFINED - 1 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 301 7 4 4 2.7 CC(NCC(c1ccc(cc1)O)O)CCc1ccc(cc1)O None
56052 3218 34 UNDEFINED - 1 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 301 7 4 4 2.7 CC(NCC(c1ccc(cc1)O)O)CCc1ccc(cc1)O None
CHEMBL509336 3218 34 UNDEFINED - 1 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 301 7 4 4 2.7 CC(NCC(c1ccc(cc1)O)O)CCc1ccc(cc1)O None
DB11541 3218 34 UNDEFINED - 1 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 301 7 4 4 2.7 CC(NCC(c1ccc(cc1)O)O)CCc1ccc(cc1)O None
193350 67305 7 3H-DHA - 1 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 303 6 5 5 2.1 CC(Cc1ccc(O)cc1)NCC(O)c1ccc(O)c(O)c1 None
CHEMBL1902287 67305 7 3H-DHA - 1 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 303 6 5 5 2.1 CC(Cc1ccc(O)cc1)NCC(O)c1ccc(O)c(O)c1 None
CHEMBL1906949 67305 7 3H-DHA - 1 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 303 6 5 5 2.1 CC(Cc1ccc(O)cc1)NCC(O)c1ccc(O)c(O)c1 None
105 3392 84 UNDEFINED -10 6 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O None
2083 3392 84 UNDEFINED -10 6 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O None
558 3392 84 UNDEFINED -10 6 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O None
CHEMBL714 3392 84 UNDEFINED -10 6 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O None
DB01001 3392 84 UNDEFINED -10 6 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O None
2601 3709 30 3H-CGP-12177 -14 21 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
443951 3709 30 3H-CGP-12177 -14 21 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
56 3709 30 3H-CGP-12177 -14 21 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL73151 3709 30 3H-CGP-12177 -14 21 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
DB13399 3709 30 3H-CGP-12177 -14 21 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
2464 3570 52 3H-DHA -7 6 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C None
5253 3570 52 3H-DHA -7 6 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C None
7297 3570 52 3H-DHA -7 6 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C None
CHEMBL471 3570 52 3H-DHA -7 6 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C None
DB00489 3570 52 3H-DHA -7 6 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C None
1028 287 69 3H-CGP-12177 -89 30 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
139148732 287 69 3H-CGP-12177 -89 30 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
479 287 69 3H-CGP-12177 -89 30 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
5816 287 69 3H-CGP-12177 -89 30 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
CHEMBL679 287 69 3H-CGP-12177 -89 30 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
DB00668 287 69 3H-CGP-12177 -89 30 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
165193 3126 60 3H-DHA 1 43 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
2303 3126 60 3H-DHA 1 43 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
4946 3126 60 3H-DHA 1 43 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
564 3126 60 3H-DHA 1 43 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
62882 3126 60 3H-DHA 1 43 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
63 3126 60 3H-DHA 1 43 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
66366 3126 60 3H-DHA 1 43 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
91536 3126 60 3H-DHA 1 43 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
CHEMBL27 3126 60 3H-DHA 1 43 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
CHEMBL452861 3126 60 3H-DHA 1 43 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
DB00571 3126 60 3H-DHA 1 43 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
137 367 47 3H-DHA -3 12 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
2119 367 47 3H-DHA -3 12 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
563 367 47 3H-DHA -3 12 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
66368 367 47 3H-DHA -3 12 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
CHEMBL266195 367 47 3H-DHA -3 12 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
DB00866 367 47 3H-DHA -3 12 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
165193 3126 60 125I-ICYP -22 43 Rat 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
2303 3126 60 125I-ICYP -22 43 Rat 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
4946 3126 60 125I-ICYP -22 43 Rat 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
564 3126 60 125I-ICYP -22 43 Rat 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
62882 3126 60 125I-ICYP -22 43 Rat 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
63 3126 60 125I-ICYP -22 43 Rat 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
66366 3126 60 125I-ICYP -22 43 Rat 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
91536 3126 60 125I-ICYP -22 43 Rat 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
CHEMBL27 3126 60 125I-ICYP -22 43 Rat 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
CHEMBL452861 3126 60 125I-ICYP -22 43 Rat 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
DB00571 3126 60 125I-ICYP -22 43 Rat 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
43216 10086 7 3H-DHA -4 2 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 251 8 2 3 2.4 CCCc1ccccc1OCC(O)CNC(C)C None
CHEMBL1159723 10086 7 3H-DHA -4 2 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 251 8 2 3 2.4 CCCc1ccccc1OCC(O)CNC(C)C None
2176 3065 66 125I-ICYP -5 27 Guinea pig 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
4828 3065 66 125I-ICYP -5 27 Guinea pig 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
91 3065 66 125I-ICYP -5 27 Guinea pig 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
CHEMBL500 3065 66 125I-ICYP -5 27 Guinea pig 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
DB00960 3065 66 125I-ICYP -5 27 Guinea pig 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
2369 615 75 125I-ICYP -724 8 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C None
356 615 75 125I-ICYP -724 8 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C None
549 615 75 125I-ICYP -724 8 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C None
CHEMBL423 615 75 125I-ICYP -724 8 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C None
DB00195 615 75 125I-ICYP -724 8 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C None
5581 101175 10 125I-ICYP -1 7 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 345 5 3 6 2.6 COc1cc(CC2NCCc3cc(O)c(O)cc32)cc(OC)c1OC None
CHEMBL299175 101175 10 125I-ICYP -1 7 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 345 5 3 6 2.6 COc1cc(CC2NCCc3cc(O)c(O)cc32)cc(OC)c1OC None
105 3392 84 125I-CYP -10 6 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O None
2083 3392 84 125I-CYP -10 6 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O None
558 3392 84 125I-CYP -10 6 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O None
CHEMBL714 3392 84 125I-CYP -10 6 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O None
DB01001 3392 84 125I-CYP -10 6 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O None
None 215921 0 UNDEFINED - 1 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 336 4 4 4 2.0 C1C(CC2=CC=CC=C21)NCC(C3=C4C=CC(=O)NC4=C(C=C3)O)O None
3083544 462 46 UNDEFINED -5 5 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O None
4943 462 46 UNDEFINED -5 5 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O None
7479 462 46 UNDEFINED -5 5 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O None
CHEMBL1363 462 46 UNDEFINED -5 5 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O None
DB01274 462 46 UNDEFINED -5 5 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O None
4292932 169646 1 UNDEFINED - 1 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 319 7 4 4 1.3 CC(C)(C)NCC(O)COc1cccc2[nH]cc(CC(N)=O)c12 None
CHEMBL444553 169646 1 UNDEFINED - 1 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 319 7 4 4 1.3 CC(C)(C)NCC(O)COc1cccc2[nH]cc(CC(N)=O)c12 None
103 4074 56 125I-ICYP -416 54 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2875 4074 56 125I-ICYP -416 54 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5736 4074 56 125I-ICYP -416 54 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL285802 4074 56 125I-ICYP -416 54 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
DB09225 4074 56 125I-ICYP -416 54 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
105 3392 84 125I-ICYP -5 6 Guinea pig 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O None
2083 3392 84 125I-ICYP -5 6 Guinea pig 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O None
558 3392 84 125I-ICYP -5 6 Guinea pig 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O None
CHEMBL714 3392 84 125I-ICYP -5 6 Guinea pig 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O None
DB01001 3392 84 125I-ICYP -5 6 Guinea pig 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O None
2419 3394 80 125I-CYP 16 6 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O None
5152 3394 80 125I-CYP 16 6 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O None
559 3394 80 125I-CYP 16 6 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O None
CHEMBL1263 3394 80 125I-CYP 16 6 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O None
DB00938 3394 80 125I-CYP 16 6 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O None
2419 3394 80 3H-CGP-12177 16 6 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O None
5152 3394 80 3H-CGP-12177 16 6 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O None
559 3394 80 3H-CGP-12177 16 6 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O None
CHEMBL1263 3394 80 3H-CGP-12177 16 6 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O None
DB00938 3394 80 3H-CGP-12177 16 6 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O None
7153 97557 74 3H-DHA -154 34 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
CHEMBL272942 97557 74 3H-DHA -154 34 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
2598 3707 52 3H-CGP-12177 -6 5 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 225 3 4 4 1.5 OC(c1cc(O)cc(c1)O)CNC(C)(C)C None
5403 3707 52 3H-CGP-12177 -6 5 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 225 3 4 4 1.5 OC(c1cc(O)cc(c1)O)CNC(C)(C)C None
560 3707 52 3H-CGP-12177 -6 5 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 225 3 4 4 1.5 OC(c1cc(O)cc(c1)O)CNC(C)(C)C None
CHEMBL1760 3707 52 3H-CGP-12177 -6 5 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 225 3 4 4 1.5 OC(c1cc(O)cc(c1)O)CNC(C)(C)C None
DB00871 3707 52 3H-CGP-12177 -6 5 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 225 3 4 4 1.5 OC(c1cc(O)cc(c1)O)CNC(C)(C)C None
3083544 462 46 125I-CYP -5 5 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O None
4943 462 46 125I-CYP -5 5 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O None
7479 462 46 125I-CYP -5 5 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O None
CHEMBL1363 462 46 125I-CYP -5 5 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O None
DB01274 462 46 125I-CYP -5 5 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O None
3663 99492 79 125I-Pindolol -75 29 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 504 0 6 8 5.1 Cc1cc(O)c2c(=O)c3c(O)cc(O)c4c5c(O)cc(O)c6c(=O)c7c(O)cc(C)c8c1c2c(c34)c(c78)c65 None
CHEMBL286494 99492 79 125I-Pindolol -75 29 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 504 0 6 8 5.1 Cc1cc(O)c2c(=O)c3c(O)cc(O)c4c5c(O)cc(O)c6c(=O)c7c(O)cc(C)c8c1c2c(c34)c(c78)c65 None
5581 101175 10 125I-ICYP 1 7 Guinea pig 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 345 5 3 6 2.6 COc1cc(CC2NCCc3cc(O)c(O)cc32)cc(OC)c1OC None
CHEMBL299175 101175 10 125I-ICYP 1 7 Guinea pig 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 345 5 3 6 2.6 COc1cc(CC2NCCc3cc(O)c(O)cc32)cc(OC)c1OC None
105 3392 84 3H-DHA -10 6 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O None
2083 3392 84 3H-DHA -10 6 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O None
558 3392 84 3H-DHA -10 6 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O None
CHEMBL714 3392 84 3H-DHA -10 6 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O None
DB01001 3392 84 3H-DHA -10 6 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O None
1499 2052 43 3H-DHA -33 17 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
3779 2052 43 3H-DHA -33 17 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
536 2052 43 3H-DHA -33 17 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
CHEMBL434 2052 43 3H-DHA -33 17 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
DB01064 2052 43 3H-DHA -33 17 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
2249 509 106 125I-ICYP -83 12 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C None
255 509 106 125I-ICYP -83 12 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C None
548 509 106 125I-ICYP -83 12 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C None
CHEMBL24 509 106 125I-ICYP -83 12 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C None
DB00335 509 106 125I-ICYP -83 12 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C None
2249 509 106 125I-ICYP -83 12 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C None
255 509 106 125I-ICYP -83 12 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C None
548 509 106 125I-ICYP -83 12 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C None
CHEMBL24 509 106 125I-ICYP -83 12 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C None
DB00335 509 106 125I-ICYP -83 12 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C None
123686 1942 44 125I-Pindolol -3090 9 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 354 9 4 5 1.7 C1=CC=C(C=C1)NC(=O)NCCNCC(COC2=CC=CC=C2C#N)O None
12581 1942 44 125I-Pindolol -3090 9 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 354 9 4 5 1.7 C1=CC=C(C=C1)NC(=O)NCCNCC(COC2=CC=CC=C2C#N)O None
CHEMBL11268 1942 44 125I-Pindolol -3090 9 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 354 9 4 5 1.7 C1=CC=C(C=C1)NC(=O)NCCNCC(COC2=CC=CC=C2C#N)O None
173 3199 88 3H-DHA -33 23 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
5011 3199 88 3H-DHA -33 23 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
CHEMBL18772 3199 88 3H-DHA -33 23 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
1786 2474 79 125I-CYP -25 11 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O None
4171 2474 79 125I-CYP -25 11 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O None
553 2474 79 125I-CYP -25 11 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O None
CHEMBL13 2474 79 125I-CYP -25 11 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O None
DB00264 2474 79 125I-CYP -25 11 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O None
None 215914 0 UNDEFINED - 1 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 368 7 4 5 2.5 CC(CC1=CC=C(C=C1)OC)NCC(C2=C3C=CC(=O)NC3=C(C=C2)O)O None
124433 150887 10 UNDEFINED -1 3 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 288 6 3 3 2.8 OC(CNC1CCCCC1)COc1cccc2[nH]ccc12 None
CHEMBL396185 150887 10 UNDEFINED -1 3 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 288 6 3 3 2.8 OC(CNC1CCCCC1)COc1cccc2[nH]ccc12 None
484 2804 45 3H-CGP-12177 -31 36 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
951 2804 45 3H-CGP-12177 -31 36 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
CHEMBL432 2804 45 3H-CGP-12177 -31 36 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
9992825 83937 16 UNDEFINED - 1 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 261 2 3 4 1.1 CC(C)NC1CCn2c(=O)[nH]c3cccc(c32)C1O None
CHEMBL2218907 83937 16 UNDEFINED - 1 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 261 2 3 4 1.1 CC(C)NC1CCn2c(=O)[nH]c3cccc(c32)C1O None
1499 2052 43 125I-ICYP -9 17 Guinea pig 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
3779 2052 43 125I-ICYP -9 17 Guinea pig 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
536 2052 43 125I-ICYP -9 17 Guinea pig 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
CHEMBL434 2052 43 125I-ICYP -9 17 Guinea pig 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
DB01064 2052 43 125I-ICYP -9 17 Guinea pig 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
2464 3570 52 125I-ICYP -5 6 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C None
5253 3570 52 125I-ICYP -5 6 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C None
7297 3570 52 125I-ICYP -5 6 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C None
CHEMBL471 3570 52 125I-ICYP -5 6 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C None
DB00489 3570 52 125I-ICYP -5 6 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C None
12016890 190172 4 3H-DHA -575 12 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 318 4 1 3 2.6 NC(=O)c1ccc(F)c2c1CC(N(C1CCC1)C1CCC1)CO2 None
CHEMBL5183389 190172 4 3H-DHA -575 12 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 318 4 1 3 2.6 NC(=O)c1ccc(F)c2c1CC(N(C1CCC1)C1CCC1)CO2 None
None 215916 0 UNDEFINED - 1 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 396 6 4 6 2.0 COC1=C(C=C2CC(CC2=C1)NCC(C3=C4C=CC(=O)NC4=C(C=C3)O)O)OC None
1028 287 69 125I-ICYP -89 30 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
139148732 287 69 125I-ICYP -89 30 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
479 287 69 125I-ICYP -89 30 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
5816 287 69 125I-ICYP -89 30 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
CHEMBL679 287 69 125I-ICYP -89 30 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
DB00668 287 69 125I-ICYP -89 30 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
7153 97557 74 125I-Pindolol -154 34 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
CHEMBL272942 97557 74 125I-Pindolol -154 34 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
5581 101175 10 125I-ICYP -1 7 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 345 5 3 6 2.6 COc1cc(CC2NCCc3cc(O)c(O)cc32)cc(OC)c1OC None
CHEMBL299175 101175 10 125I-ICYP -1 7 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 345 5 3 6 2.6 COc1cc(CC2NCCc3cc(O)c(O)cc32)cc(OC)c1OC None
119570 3098 90 None -1202 40 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cellsDisplacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells
Drug Central 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
2233 3098 90 None -1202 40 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cellsDisplacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells
Drug Central 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
953 3098 90 None -1202 40 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cellsDisplacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells
Drug Central 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
CHEMBL301265 3098 90 None -1202 40 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cellsDisplacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells
Drug Central 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
DB00413 3098 90 None -1202 40 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cellsDisplacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells
Drug Central 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
681 1432 65 None -93 39 Dog 8.4 pKi = 8.4 Binding
Binding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranes
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
940 1432 65 None -93 39 Dog 8.4 pKi = 8.4 Binding
Binding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranes
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
947 1432 65 None -93 39 Dog 8.4 pKi = 8.4 Binding
Binding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranes
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
CHEMBL59 1432 65 None -93 39 Dog 8.4 pKi = 8.4 Binding
Binding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranes
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
DB00988 1432 65 None -93 39 Dog 8.4 pKi = 8.4 Binding
Binding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranes
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
2687 874 15 125I-CYP 1 5 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 279 5 4 4 1.0 OC(COc1cccc2c1[nH]c(=O)[nH]2)CNC(C)(C)C None
532 874 15 125I-CYP 1 5 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 279 5 4 4 1.0 OC(COc1cccc2c1[nH]c(=O)[nH]2)CNC(C)(C)C None
5387 874 15 125I-CYP 1 5 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 279 5 4 4 1.0 OC(COc1cccc2c1[nH]c(=O)[nH]2)CNC(C)(C)C None
CHEMBL420746 874 15 125I-CYP 1 5 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 279 5 4 4 1.0 OC(COc1cccc2c1[nH]c(=O)[nH]2)CNC(C)(C)C None
2176 3065 66 125I-CYP -2 27 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
4828 3065 66 125I-CYP -2 27 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
91 3065 66 125I-CYP -2 27 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
CHEMBL500 3065 66 125I-CYP -2 27 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
DB00960 3065 66 125I-CYP -2 27 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
104903 56035 14 None -5 6 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
Drug Central 624 6 0 8 5.5 C[C@@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)C3=CC[C@]2(C)[C@H]1C(=O)CN1CCN(c2cc(N3CCCC3)nc(N3CCCC3)n2)CC1 None
CHEMBL1630578 56035 14 None -5 6 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
Drug Central 624 6 0 8 5.5 C[C@@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)C3=CC[C@]2(C)[C@H]1C(=O)CN1CCN(c2cc(N3CCCC3)nc(N3CCCC3)n2)CC1 None
3486 3096 51 None -5 11 Mouse 8.3 pKi = 8.3 Binding
Ki value was determined by accumulation of c-AMP in S-49 mouse lymphoma cells (Beta2).Ki value was determined by accumulation of c-AMP in S-49 mouse lymphoma cells (Beta2).
Drug Central 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C None
4883 3096 51 None -5 11 Mouse 8.3 pKi = 8.3 Binding
Ki value was determined by accumulation of c-AMP in S-49 mouse lymphoma cells (Beta2).Ki value was determined by accumulation of c-AMP in S-49 mouse lymphoma cells (Beta2).
Drug Central 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C None
555 3096 51 None -5 11 Mouse 8.3 pKi = 8.3 Binding
Ki value was determined by accumulation of c-AMP in S-49 mouse lymphoma cells (Beta2).Ki value was determined by accumulation of c-AMP in S-49 mouse lymphoma cells (Beta2).
Drug Central 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C None
CHEMBL6995 3096 51 None -5 11 Mouse 8.3 pKi = 8.3 Binding
Ki value was determined by accumulation of c-AMP in S-49 mouse lymphoma cells (Beta2).Ki value was determined by accumulation of c-AMP in S-49 mouse lymphoma cells (Beta2).
Drug Central 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C None
DB01297 3096 51 None -5 11 Mouse 8.3 pKi = 8.3 Binding
Ki value was determined by accumulation of c-AMP in S-49 mouse lymphoma cells (Beta2).Ki value was determined by accumulation of c-AMP in S-49 mouse lymphoma cells (Beta2).
Drug Central 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C None
165193 3126 60 3H-DHA 1 43 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
2303 3126 60 3H-DHA 1 43 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
4946 3126 60 3H-DHA 1 43 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
564 3126 60 3H-DHA 1 43 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
62882 3126 60 3H-DHA 1 43 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
63 3126 60 3H-DHA 1 43 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
66366 3126 60 3H-DHA 1 43 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
91536 3126 60 3H-DHA 1 43 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
CHEMBL27 3126 60 3H-DHA 1 43 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
CHEMBL452861 3126 60 3H-DHA 1 43 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
DB00571 3126 60 3H-DHA 1 43 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
2685 875 15 125I-CYP -1096 7 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 494 11 4 8 2.3 OC(COc1ccc(cc1)c1nc(cn1C)C(F)(F)F)CNCCOc1ccc(c(c1)C(=O)N)O None
541 875 15 125I-CYP -1096 7 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 494 11 4 8 2.3 OC(COc1ccc(cc1)c1nc(cn1C)C(F)(F)F)CNCCOc1ccc(c(c1)C(=O)N)O None
CHEMBL280822 875 15 125I-CYP -1096 7 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 494 11 4 8 2.3 OC(COc1ccc(cc1)c1nc(cn1C)C(F)(F)F)CNCCOc1ccc(c(c1)C(=O)N)O None
21138 97986 34 125I-ICYP 1 7 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NC[C@@H](O)COc1cccc2ccccc12 None
CHEMBL275742 97986 34 125I-ICYP 1 7 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NC[C@@H](O)COc1cccc2ccccc12 None
1499 2052 43 125I-CYP -33 17 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
3779 2052 43 125I-CYP -33 17 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
536 2052 43 125I-CYP -33 17 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
CHEMBL434 2052 43 125I-CYP -33 17 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
DB01064 2052 43 125I-CYP -33 17 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
1499 2052 43 3H-DHA -33 17 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
3779 2052 43 3H-DHA -33 17 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
536 2052 43 3H-DHA -33 17 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
CHEMBL434 2052 43 3H-DHA -33 17 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
DB01064 2052 43 3H-DHA -33 17 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
3466 4063 38 3H-DHA - 1 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 378 8 4 5 2.4 OC(c1ccc(c(c1)NS(=O)(=O)C)O)CNC(Cc1ccccc1)(C)C None
37990 4063 38 3H-DHA - 1 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 378 8 4 5 2.4 OC(c1ccc(c(c1)NS(=O)(=O)C)O)CNC(Cc1ccccc1)(C)C None
CHEMBL1243407 4063 38 3H-DHA - 1 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 378 8 4 5 2.4 OC(c1ccc(c(c1)NS(=O)(=O)C)O)CNC(Cc1ccccc1)(C)C None
688390 214733 0 125I-ICYP 7 3 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 267 5 2 4 2.5 C[C@H]([C@H](C1=C(C=CC(=C1)OC)OC)O)NC(C)(C)C None
688390 214733 0 125I-ICYP 7 3 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 267 5 2 4 2.5 C[C@H]([C@H](C1=C(C=CC(=C1)OC)OC)O)NC(C)(C)C None
135409468 1996 63 125I-Pindolol -1659 40 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
333 1996 63 125I-Pindolol -1659 40 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
CHEMBL845 1996 63 125I-Pindolol -1659 40 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
1155 1592 45 125I-ICYP -2 5 Guinea pig 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O None
3343 1592 45 125I-ICYP -2 5 Guinea pig 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O None
557 1592 45 125I-ICYP -2 5 Guinea pig 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O None
CHEMBL32800 1592 45 125I-ICYP -2 5 Guinea pig 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O None
DB01288 1592 45 125I-ICYP -2 5 Guinea pig 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O None
175540 118737 45 None 1 5 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
Drug Central 266 8 3 4 0.5 CC(C)NC[C@H](O)COc1ccc(CC(N)=O)cc1 None
CHEMBL343633 118737 45 None 1 5 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
Drug Central 266 8 3 4 0.5 CC(C)NC[C@H](O)COc1ccc(CC(N)=O)cc1 None
1960 2805 64 None -36 26 Bovine 8.3 pKi = 8.3 Binding
Tested for binding affinity against beta-2 adrenergic receptor in bovine lung using [3H]DHA as radioligandTested for binding affinity against beta-2 adrenergic receptor in bovine lung using [3H]DHA as radioligand
Drug Central 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O None
439260 2805 64 None -36 26 Bovine 8.3 pKi = 8.3 Binding
Tested for binding affinity against beta-2 adrenergic receptor in bovine lung using [3H]DHA as radioligandTested for binding affinity against beta-2 adrenergic receptor in bovine lung using [3H]DHA as radioligand
Drug Central 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O None
505 2805 64 None -36 26 Bovine 8.3 pKi = 8.3 Binding
Tested for binding affinity against beta-2 adrenergic receptor in bovine lung using [3H]DHA as radioligandTested for binding affinity against beta-2 adrenergic receptor in bovine lung using [3H]DHA as radioligand
Drug Central 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O None
CHEMBL1437 2805 64 None -36 26 Bovine 8.3 pKi = 8.3 Binding
Tested for binding affinity against beta-2 adrenergic receptor in bovine lung using [3H]DHA as radioligandTested for binding affinity against beta-2 adrenergic receptor in bovine lung using [3H]DHA as radioligand
Drug Central 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O None
DB00368 2805 64 None -36 26 Bovine 8.3 pKi = 8.3 Binding
Tested for binding affinity against beta-2 adrenergic receptor in bovine lung using [3H]DHA as radioligandTested for binding affinity against beta-2 adrenergic receptor in bovine lung using [3H]DHA as radioligand
Drug Central 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O None
1960 2805 64 None -338 26 Dog 8.3 pKi = 8.3 Binding
Binding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranes
Drug Central 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O None
439260 2805 64 None -338 26 Dog 8.3 pKi = 8.3 Binding
Binding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranes
Drug Central 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O None
505 2805 64 None -338 26 Dog 8.3 pKi = 8.3 Binding
Binding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranes
Drug Central 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O None
CHEMBL1437 2805 64 None -338 26 Dog 8.3 pKi = 8.3 Binding
Binding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranes
Drug Central 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O None
DB00368 2805 64 None -338 26 Dog 8.3 pKi = 8.3 Binding
Binding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranes
Drug Central 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O None
1960 2805 64 None -30 26 Rat 8.3 pKi = 8.3 Binding
Binding affinity against adrenergic beta 2 receptor versus 1 nM [3H]dihydroalprenolol in rat cerebral cerebellar membranesBinding affinity against adrenergic beta 2 receptor versus 1 nM [3H]dihydroalprenolol in rat cerebral cerebellar membranes
Drug Central 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O None
439260 2805 64 None -30 26 Rat 8.3 pKi = 8.3 Binding
Binding affinity against adrenergic beta 2 receptor versus 1 nM [3H]dihydroalprenolol in rat cerebral cerebellar membranesBinding affinity against adrenergic beta 2 receptor versus 1 nM [3H]dihydroalprenolol in rat cerebral cerebellar membranes
Drug Central 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O None
505 2805 64 None -30 26 Rat 8.3 pKi = 8.3 Binding
Binding affinity against adrenergic beta 2 receptor versus 1 nM [3H]dihydroalprenolol in rat cerebral cerebellar membranesBinding affinity against adrenergic beta 2 receptor versus 1 nM [3H]dihydroalprenolol in rat cerebral cerebellar membranes
Drug Central 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O None
CHEMBL1437 2805 64 None -30 26 Rat 8.3 pKi = 8.3 Binding
Binding affinity against adrenergic beta 2 receptor versus 1 nM [3H]dihydroalprenolol in rat cerebral cerebellar membranesBinding affinity against adrenergic beta 2 receptor versus 1 nM [3H]dihydroalprenolol in rat cerebral cerebellar membranes
Drug Central 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O None
DB00368 2805 64 None -30 26 Rat 8.3 pKi = 8.3 Binding
Binding affinity against adrenergic beta 2 receptor versus 1 nM [3H]dihydroalprenolol in rat cerebral cerebellar membranesBinding affinity against adrenergic beta 2 receptor versus 1 nM [3H]dihydroalprenolol in rat cerebral cerebellar membranes
Drug Central 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O None
123600 2275 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cells in presence of 100 uM boric acidDisplacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cells in presence of 100 uM boric acid
Drug Central 239 4 4 4 1.3 OCc1cc(ccc1O)[C@H](CNC(C)(C)C)O None
1575 2275 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cells in presence of 100 uM boric acidDisplacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cells in presence of 100 uM boric acid
Drug Central 239 4 4 4 1.3 OCc1cc(ccc1O)[C@H](CNC(C)(C)C)O None
9816 2275 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cells in presence of 100 uM boric acidDisplacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cells in presence of 100 uM boric acid
Drug Central 239 4 4 4 1.3 OCc1cc(ccc1O)[C@H](CNC(C)(C)C)O None
CHEMBL1002 2275 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cells in presence of 100 uM boric acidDisplacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cells in presence of 100 uM boric acid
Drug Central 239 4 4 4 1.3 OCc1cc(ccc1O)[C@H](CNC(C)(C)C)O None
DB13139 2275 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cells in presence of 100 uM boric acidDisplacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cells in presence of 100 uM boric acid
Drug Central 239 4 4 4 1.3 OCc1cc(ccc1O)[C@H](CNC(C)(C)C)O None
1024 1535 27 None - 1 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 165 3 2 2 1.3 CN[C@H]([C@@H](c1ccccc1)O)C None
556 1535 27 None - 1 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 165 3 2 2 1.3 CN[C@H]([C@@H](c1ccccc1)O)C None
9294 1535 27 None - 1 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 165 3 2 2 1.3 CN[C@H]([C@@H](c1ccccc1)O)C None
CHEMBL211456 1535 27 None - 1 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 165 3 2 2 1.3 CN[C@H]([C@@H](c1ccccc1)O)C None
DB01364 1535 27 None - 1 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 165 3 2 2 1.3 CN[C@H]([C@@H](c1ccccc1)O)C None
2598 3707 52 None -6 5 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 225 3 4 4 1.5 OC(c1cc(O)cc(c1)O)CNC(C)(C)C None
5403 3707 52 None -6 5 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 225 3 4 4 1.5 OC(c1cc(O)cc(c1)O)CNC(C)(C)C None
560 3707 52 None -6 5 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 225 3 4 4 1.5 OC(c1cc(O)cc(c1)O)CNC(C)(C)C None
CHEMBL1760 3707 52 None -6 5 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 225 3 4 4 1.5 OC(c1cc(O)cc(c1)O)CNC(C)(C)C None
DB00871 3707 52 None -6 5 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 225 3 4 4 1.5 OC(c1cc(O)cc(c1)O)CNC(C)(C)C None
1836 2544 56 None -53 15 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
Drug Central 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 None
3340 2544 56 None -53 15 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
Drug Central 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 None
5281040 2544 56 None -53 15 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
Drug Central 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 None
CHEMBL787 2544 56 None -53 15 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
Drug Central 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 None
DB00471 2544 56 None -53 15 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
Drug Central 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 None
103 4074 56 None -416 54 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2875 4074 56 None -416 54 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5736 4074 56 None -416 54 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL285802 4074 56 None -416 54 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
DB09225 4074 56 None -416 54 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
1599 2299 47 None -131 16 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
Drug Central 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 None
3955 2299 47 None -131 16 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
Drug Central 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 None
7215 2299 47 None -131 16 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
Drug Central 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 None
CHEMBL841 2299 47 None -131 16 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
Drug Central 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 None
DB00836 2299 47 None -131 16 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
Drug Central 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 None
3157 1437 69 None -97 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
Drug Central 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 None
7170 1437 69 None -97 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
Drug Central 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 None
954 1437 69 None -97 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
Drug Central 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 None
CHEMBL707 1437 69 None -97 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
Drug Central 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 None
DB00590 1437 69 None -97 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
Drug Central 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 None
11954224 214164 0 None -3388 60 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
Drug Central 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
2810 67245 50 None 1 2 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
Drug Central 213 4 2 2 2.4 CC(C)NCC(O)c1ccccc1Cl None
CHEMBL1902627 67245 50 None 1 2 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
Drug Central 213 4 2 2 2.4 CC(C)NCC(O)c1ccccc1Cl None
2405 658 71 None -58 4 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 325 12 2 5 2.4 OC(COc1ccc(cc1)COCCOC(C)C)CNC(C)C None
380 658 71 None -58 4 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 325 12 2 5 2.4 OC(COc1ccc(cc1)COCCOC(C)C)CNC(C)C None
7129 658 71 None -58 4 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 325 12 2 5 2.4 OC(COc1ccc(cc1)COCCOC(C)C)CNC(C)C None
CHEMBL645 658 71 None -58 4 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 325 12 2 5 2.4 OC(COc1ccc(cc1)COCCOC(C)C)CNC(C)C None
DB00612 658 71 None -58 4 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 325 12 2 5 2.4 OC(COc1ccc(cc1)COCCOC(C)C)CNC(C)C None
105 3392 84 None -10 6 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O None
2083 3392 84 None -10 6 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O None
558 3392 84 None -10 6 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O None
CHEMBL714 3392 84 None -10 6 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O None
DB01001 3392 84 None -10 6 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O None
1353 1872 85 125I-ICYP -446 86 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1872 85 125I-ICYP -446 86 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1872 85 125I-ICYP -446 86 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1872 85 125I-ICYP -446 86 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1872 85 125I-ICYP -446 86 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
135398745 2858 108 125I-ICYP -331 66 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2858 108 125I-ICYP -331 66 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2858 108 125I-ICYP -331 66 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2858 108 125I-ICYP -331 66 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
2181 3067 0 125I-ICYP -134 35 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
4830 3067 0 125I-ICYP -134 35 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
92 3067 0 125I-ICYP -134 35 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
CHEMBL440294 3067 0 125I-ICYP -134 35 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
DB09286 3067 0 125I-ICYP -134 35 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
2337 3193 72 125I-ICYP -72 63 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3193 72 125I-ICYP -72 63 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3193 72 125I-ICYP -72 63 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3193 72 125I-ICYP -72 63 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3193 72 125I-ICYP -72 63 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
2389 3267 114 125I-ICYP -2089 68 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3267 114 125I-ICYP -2089 68 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3267 114 125I-ICYP -2089 68 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3267 114 125I-ICYP -2089 68 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3267 114 125I-ICYP -2089 68 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
2435 3520 78 125I-ICYP -316 49 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
60149 3520 78 125I-ICYP -316 49 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
98 3520 78 125I-ICYP -316 49 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
CHEMBL12713 3520 78 125I-ICYP -316 49 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
DB06144 3520 78 125I-ICYP -316 49 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
2865 4064 67 125I-ICYP -1318 54 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 4064 67 125I-ICYP -1318 54 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 4064 67 125I-ICYP -1318 54 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 4064 67 125I-ICYP -1318 54 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 4064 67 125I-ICYP -1318 54 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
115237 55281 113 125I-ICYP -2754 55 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
CHEMBL1621 55281 113 125I-ICYP -2754 55 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
46780481 107032 18 125I-ICYP -954 54 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
9903970 107032 18 125I-ICYP -954 54 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3187365 107032 18 125I-ICYP -954 54 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3544974 107032 18 125I-ICYP -954 54 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
105 3392 84 3H-CGP-12177 -10 6 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O None
2083 3392 84 3H-CGP-12177 -10 6 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O None
558 3392 84 3H-CGP-12177 -10 6 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O None
CHEMBL714 3392 84 3H-CGP-12177 -10 6 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O None
DB01001 3392 84 3H-CGP-12177 -10 6 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O None
1222 1626 44 125I-ICYP -95 33 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3396 1626 44 125I-ICYP -95 33 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
85 1626 44 125I-ICYP -95 33 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL46516 1626 44 125I-ICYP -95 33 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
DB04842 1626 44 125I-ICYP -95 33 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
105 3392 84 UNDEFINED -10 6 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O None
2083 3392 84 UNDEFINED -10 6 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O None
558 3392 84 UNDEFINED -10 6 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O None
CHEMBL714 3392 84 UNDEFINED -10 6 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O None
DB01001 3392 84 UNDEFINED -10 6 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O None
1155 1592 45 125I-ICYP -2 5 Guinea pig 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O None
3343 1592 45 125I-ICYP -2 5 Guinea pig 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O None
557 1592 45 125I-ICYP -2 5 Guinea pig 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O None
CHEMBL32800 1592 45 125I-ICYP -2 5 Guinea pig 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O None
DB01288 1592 45 125I-ICYP -2 5 Guinea pig 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O None
None 215920 0 UNDEFINED - 1 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 364 4 4 4 2.6 CC1=C(C=C2CC(CC2=C1)NCC(C3=C4C=CC(=O)NC4=C(C=C3)O)O)C None
5190 106409 31 UNDEFINED - 1 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 466 8 2 5 4.2 N#Cc1cc2c(OCC(O)CN3CCN(C(c4ccccc4)c4ccccc4)CC3)cccc2[nH]1 None
CHEMBL314639 106409 31 UNDEFINED - 1 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 466 8 2 5 4.2 N#Cc1cc2c(OCC(O)CN3CCN(C(c4ccccc4)c4ccccc4)CC3)cccc2[nH]1 None
128658 33738 7 125I-ICYP -3 5 Guinea pig 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 363 5 3 6 2.7 COc1cc(CC2NCCc3cc(O)c(O)c(F)c32)cc(OC)c1OC None
CHEMBL142428 33738 7 125I-ICYP -3 5 Guinea pig 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 363 5 3 6 2.7 COc1cc(CC2NCCc3cc(O)c(O)c(F)c32)cc(OC)c1OC None
12582 935 40 UNDEFINED -11 5 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 276 3 3 3 3.0 CC(C)(C)NCC(C1=CC(=C(C(=C1)Cl)N)Cl)O None
2783 935 40 UNDEFINED -11 5 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 276 3 3 3 3.0 CC(C)(C)NCC(C1=CC(=C(C(=C1)Cl)N)Cl)O None
CHEMBL49080 935 40 UNDEFINED -11 5 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 276 3 3 3 3.0 CC(C)(C)NCC(C1=CC(=C(C(=C1)Cl)N)Cl)O None
DB01407 935 40 UNDEFINED -11 5 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 276 3 3 3 3.0 CC(C)(C)NCC(C1=CC(=C(C(=C1)Cl)N)Cl)O None
9992825 83937 16 UNDEFINED - 1 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 261 2 3 4 1.1 CC(C)NC1CCn2c(=O)[nH]c3cccc(c32)C1O None
CHEMBL2218907 83937 16 UNDEFINED - 1 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 261 2 3 4 1.1 CC(C)NC1CCn2c(=O)[nH]c3cccc(c32)C1O None
4418 33985 80 None -23 7 Dog 8.2 pKi = 8.2 Binding
Beta-2 adrenergic receptor binding affinity by measuring the displacement of [3H]DHA binding in rat lungBeta-2 adrenergic receptor binding affinity by measuring the displacement of [3H]DHA binding in rat lung
Drug Central 392 7 1 5 3.4 COc1ccccc1N1CCN(CC(O)COc2cccc3ccccc23)CC1 None
CHEMBL142635 33985 80 None -23 7 Dog 8.2 pKi = 8.2 Binding
Beta-2 adrenergic receptor binding affinity by measuring the displacement of [3H]DHA binding in rat lungBeta-2 adrenergic receptor binding affinity by measuring the displacement of [3H]DHA binding in rat lung
Drug Central 392 7 1 5 3.4 COc1ccccc1N1CCN(CC(O)COc2cccc3ccccc23)CC1 None
68770 44384 49 None -1 2 Human 8.2 pKi = 8.2 Binding
Binding affinity to beta2 adrenergic receptor (unknown origin) by radioligand binding assayBinding affinity to beta2 adrenergic receptor (unknown origin) by radioligand binding assay
Drug Central 363 7 4 4 3.3 CC(C)(C)NCC(O)COc1ccc(NC(=O)NC2CCCCC2)cc1 None
CHEMBL152067 44384 49 None -1 2 Human 8.2 pKi = 8.2 Binding
Binding affinity to beta2 adrenergic receptor (unknown origin) by radioligand binding assayBinding affinity to beta2 adrenergic receptor (unknown origin) by radioligand binding assay
Drug Central 363 7 4 4 3.3 CC(C)(C)NCC(O)COc1ccc(NC(=O)NC2CCCCC2)cc1 None
105 3392 84 125I-ICYP -10 6 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O None
2083 3392 84 125I-ICYP -10 6 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O None
558 3392 84 125I-ICYP -10 6 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O None
CHEMBL714 3392 84 125I-ICYP -10 6 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O None
DB01001 3392 84 125I-ICYP -10 6 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O None
1621 2386 16 None -218 45 Human 8.2 pKi = 8.2 Binding
Binding affinity towards Beta-2 adrenergic receptorBinding affinity towards Beta-2 adrenergic receptor
Drug Central 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
17 2386 16 None -218 45 Human 8.2 pKi = 8.2 Binding
Binding affinity towards Beta-2 adrenergic receptorBinding affinity towards Beta-2 adrenergic receptor
Drug Central 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
5761 2386 16 None -218 45 Human 8.2 pKi = 8.2 Binding
Binding affinity towards Beta-2 adrenergic receptorBinding affinity towards Beta-2 adrenergic receptor
Drug Central 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL263881 2386 16 None -218 45 Human 8.2 pKi = 8.2 Binding
Binding affinity towards Beta-2 adrenergic receptorBinding affinity towards Beta-2 adrenergic receptor
Drug Central 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB04829 2386 16 None -218 45 Human 8.2 pKi = 8.2 Binding
Binding affinity towards Beta-2 adrenergic receptorBinding affinity towards Beta-2 adrenergic receptor
Drug Central 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
1028 287 69 None -12 30 Rat 8.2 pKi = 8.2 Binding
Binding affinity against adrenergic beta 2 receptor versus 1 nM [3H]dihydroalprenolol in rat cerebral cerebellar membranesBinding affinity against adrenergic beta 2 receptor versus 1 nM [3H]dihydroalprenolol in rat cerebral cerebellar membranes
Drug Central 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
139148732 287 69 None -12 30 Rat 8.2 pKi = 8.2 Binding
Binding affinity against adrenergic beta 2 receptor versus 1 nM [3H]dihydroalprenolol in rat cerebral cerebellar membranesBinding affinity against adrenergic beta 2 receptor versus 1 nM [3H]dihydroalprenolol in rat cerebral cerebellar membranes
Drug Central 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
479 287 69 None -12 30 Rat 8.2 pKi = 8.2 Binding
Binding affinity against adrenergic beta 2 receptor versus 1 nM [3H]dihydroalprenolol in rat cerebral cerebellar membranesBinding affinity against adrenergic beta 2 receptor versus 1 nM [3H]dihydroalprenolol in rat cerebral cerebellar membranes
Drug Central 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
5816 287 69 None -12 30 Rat 8.2 pKi = 8.2 Binding
Binding affinity against adrenergic beta 2 receptor versus 1 nM [3H]dihydroalprenolol in rat cerebral cerebellar membranesBinding affinity against adrenergic beta 2 receptor versus 1 nM [3H]dihydroalprenolol in rat cerebral cerebellar membranes
Drug Central 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
CHEMBL679 287 69 None -12 30 Rat 8.2 pKi = 8.2 Binding
Binding affinity against adrenergic beta 2 receptor versus 1 nM [3H]dihydroalprenolol in rat cerebral cerebellar membranesBinding affinity against adrenergic beta 2 receptor versus 1 nM [3H]dihydroalprenolol in rat cerebral cerebellar membranes
Drug Central 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
DB00668 287 69 None -12 30 Rat 8.2 pKi = 8.2 Binding
Binding affinity against adrenergic beta 2 receptor versus 1 nM [3H]dihydroalprenolol in rat cerebral cerebellar membranesBinding affinity against adrenergic beta 2 receptor versus 1 nM [3H]dihydroalprenolol in rat cerebral cerebellar membranes
Drug Central 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
1028 287 69 None -30 30 Dog 8.2 pKi = 8.2 Binding
Binding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranes
Drug Central 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
139148732 287 69 None -30 30 Dog 8.2 pKi = 8.2 Binding
Binding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranes
Drug Central 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
479 287 69 None -30 30 Dog 8.2 pKi = 8.2 Binding
Binding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranes
Drug Central 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
5816 287 69 None -30 30 Dog 8.2 pKi = 8.2 Binding
Binding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranes
Drug Central 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
CHEMBL679 287 69 None -30 30 Dog 8.2 pKi = 8.2 Binding
Binding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranes
Drug Central 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
DB00668 287 69 None -30 30 Dog 8.2 pKi = 8.2 Binding
Binding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranes
Drug Central 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
146294 913 0 None -6 2 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 323 12 2 5 2.2 OC(COc1ccc(cc1)OCCOCC1CC1)CNC(C)C None
552 913 0 None -6 2 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 323 12 2 5 2.2 OC(COc1ccc(cc1)OCCOCC1CC1)CNC(C)C None
637 913 0 None -6 2 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 323 12 2 5 2.2 OC(COc1ccc(cc1)OCCOCC1CC1)CNC(C)C None
CHEMBL2110772 913 0 None -6 2 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 323 12 2 5 2.2 OC(COc1ccc(cc1)OCCOCC1CC1)CNC(C)C None
4806 3933 85 None -8 13 Human 8.2 pKi = 8.2 Binding
Binding affinity to human beta 2 adrenergic receptorBinding affinity to human beta 2 adrenergic receptor
Drug Central 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 None
7351 3933 85 None -8 13 Human 8.2 pKi = 8.2 Binding
Binding affinity to human beta 2 adrenergic receptorBinding affinity to human beta 2 adrenergic receptor
Drug Central 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 None
9966051 3933 85 None -8 13 Human 8.2 pKi = 8.2 Binding
Binding affinity to human beta 2 adrenergic receptorBinding affinity to human beta 2 adrenergic receptor
Drug Central 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 None
CHEMBL2104993 3933 85 None -8 13 Human 8.2 pKi = 8.2 Binding
Binding affinity to human beta 2 adrenergic receptorBinding affinity to human beta 2 adrenergic receptor
Drug Central 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 None
DB09068 3933 85 None -8 13 Human 8.2 pKi = 8.2 Binding
Binding affinity to human beta 2 adrenergic receptorBinding affinity to human beta 2 adrenergic receptor
Drug Central 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 None
1222 1626 44 None -95 33 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3396 1626 44 None -95 33 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
85 1626 44 None -95 33 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL46516 1626 44 None -95 33 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
DB04842 1626 44 None -95 33 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3793 201510 70 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cellsDisplacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cells
Drug Central 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O None
45039617 201510 70 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cellsDisplacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cells
Drug Central 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O None
CHEMBL64391 201510 70 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cellsDisplacement of [3H]-DHA from recombinant human beta2 adrenoceptor expressed in HEK293T cells
Drug Central 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O None
1786 2474 79 None -25 11 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O None
4171 2474 79 None -25 11 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O None
553 2474 79 None -25 11 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O None
CHEMBL13 2474 79 None -25 11 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O None
DB00264 2474 79 None -25 11 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O None
1978 248 54 None 16 6 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 336 10 3 5 3.0 CCCC(=Nc1ccc(c(c1)C(=O)C)OCC(CNC(C)C)O)O None
40 248 54 None 16 6 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 336 10 3 5 3.0 CCCC(=Nc1ccc(c(c1)C(=O)C)OCC(CNC(C)C)O)O None
7107 248 54 None 16 6 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 336 10 3 5 3.0 CCCC(=Nc1ccc(c(c1)C(=O)C)OCC(CNC(C)C)O)O None
CHEMBL642 248 54 None 16 6 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 336 10 3 5 3.0 CCCC(=Nc1ccc(c(c1)C(=O)C)OCC(CNC(C)C)O)O None
DB01193 248 54 None 16 6 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 336 10 3 5 3.0 CCCC(=Nc1ccc(c(c1)C(=O)C)OCC(CNC(C)C)O)O None
21268191 89203 0 UNDEFINED 1 3 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 340 6 3 3 3.5 OC(CNC12CC3CC(CC(C3)C1)C2)COc1cccc2[nH]ccc12 None
CHEMBL237572 89203 0 UNDEFINED 1 3 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 340 6 3 3 3.5 OC(CNC12CC3CC(CC(C3)C1)C2)COc1cccc2[nH]ccc12 None
2663 98294 30 None 1 3 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 379 9 3 5 2.9 CCN(CC)C(=O)Nc1ccc(OCC(O)CNC(C)(C)C)c(C(C)=O)c1 None
CHEMBL27810 98294 30 None 1 3 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 379 9 3 5 2.9 CCN(CC)C(=O)Nc1ccc(OCC(O)CNC(C)(C)C)c(C(C)=O)c1 None
1499 2052 43 None 5 17 Golden hamster 8.2 pKi = 8.2 Binding
Displacement of [125I](-)-iodopindolol from adrenergic beta2 receptor in Syrian hamster DDT1 MF2 cellsDisplacement of [125I](-)-iodopindolol from adrenergic beta2 receptor in Syrian hamster DDT1 MF2 cells
Drug Central 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
3779 2052 43 None 5 17 Golden hamster 8.2 pKi = 8.2 Binding
Displacement of [125I](-)-iodopindolol from adrenergic beta2 receptor in Syrian hamster DDT1 MF2 cellsDisplacement of [125I](-)-iodopindolol from adrenergic beta2 receptor in Syrian hamster DDT1 MF2 cells
Drug Central 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
536 2052 43 None 5 17 Golden hamster 8.2 pKi = 8.2 Binding
Displacement of [125I](-)-iodopindolol from adrenergic beta2 receptor in Syrian hamster DDT1 MF2 cellsDisplacement of [125I](-)-iodopindolol from adrenergic beta2 receptor in Syrian hamster DDT1 MF2 cells
Drug Central 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
CHEMBL434 2052 43 None 5 17 Golden hamster 8.2 pKi = 8.2 Binding
Displacement of [125I](-)-iodopindolol from adrenergic beta2 receptor in Syrian hamster DDT1 MF2 cellsDisplacement of [125I](-)-iodopindolol from adrenergic beta2 receptor in Syrian hamster DDT1 MF2 cells
Drug Central 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
DB01064 2052 43 None 5 17 Golden hamster 8.2 pKi = 8.2 Binding
Displacement of [125I](-)-iodopindolol from adrenergic beta2 receptor in Syrian hamster DDT1 MF2 cellsDisplacement of [125I](-)-iodopindolol from adrenergic beta2 receptor in Syrian hamster DDT1 MF2 cells
Drug Central 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
443372 10123 23 None 1 3 Golden hamster 8.2 pKi = 8.2 Binding
Displacement of [125I](-)-iodopindolol from adrenergic beta2 receptor in Syrian hamster DDT1 MF2 cellsDisplacement of [125I](-)-iodopindolol from adrenergic beta2 receptor in Syrian hamster DDT1 MF2 cells
Drug Central 211 4 4 4 1.1 CC(C)NC[C@H](O)c1ccc(O)c(O)c1 None
CHEMBL1160723 10123 23 None 1 3 Golden hamster 8.2 pKi = 8.2 Binding
Displacement of [125I](-)-iodopindolol from adrenergic beta2 receptor in Syrian hamster DDT1 MF2 cellsDisplacement of [125I](-)-iodopindolol from adrenergic beta2 receptor in Syrian hamster DDT1 MF2 cells
Drug Central 211 4 4 4 1.1 CC(C)NC[C@H](O)c1ccc(O)c(O)c1 None
CHEMBL2062275 10123 23 None 1 3 Golden hamster 8.2 pKi = 8.2 Binding
Displacement of [125I](-)-iodopindolol from adrenergic beta2 receptor in Syrian hamster DDT1 MF2 cellsDisplacement of [125I](-)-iodopindolol from adrenergic beta2 receptor in Syrian hamster DDT1 MF2 cells
Drug Central 211 4 4 4 1.1 CC(C)NC[C@H](O)c1ccc(O)c(O)c1 None
2464 3570 52 None -7 6 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C None
5253 3570 52 None -7 6 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C None
7297 3570 52 None -7 6 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C None
CHEMBL471 3570 52 None -7 6 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C None
DB00489 3570 52 None -7 6 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C None
1531 2226 64 125I-ICYP -10 15 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O None
3869 2226 64 125I-ICYP -10 15 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O None
7207 2226 64 125I-ICYP -10 15 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O None
CHEMBL429 2226 64 125I-ICYP -10 15 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O None
DB00598 2226 64 125I-ICYP -10 15 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O None
None 215915 0 UNDEFINED - 1 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 392 6 4 4 3.1 CCC1=C2CC(CC2=C(C=C1)CC)NCC(C3=C4C=CC(=O)NC4=C(C=C3)O)O None
11978813 712 72 None -8 24 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 None
5014 712 72 None -8 24 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 None
7672 712 72 None -8 24 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 None
CHEMBL2105760 712 72 None -8 24 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 None
DB09128 712 72 None -8 24 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 None
319 1292 39 None -16 9 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 None
321 1292 39 None -16 9 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 None
444031 1292 39 None -16 9 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 None
784 1292 39 None -16 9 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 None
CHEMBL1346 1292 39 None -16 9 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 None
DB00496 1292 39 None -16 9 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 None
2291 3123 52 None -3 12 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
Drug Central 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O None
2561 3123 52 None -3 12 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
Drug Central 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O None
4932 3123 52 None -3 12 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
Drug Central 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O None
CHEMBL631 3123 52 None -3 12 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
Drug Central 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O None
DB01182 3123 52 None -3 12 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
Drug Central 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O None
4752 2269 29 None -3 3 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 307 11 2 4 2.4 O[C@H](COc1ccc(cc1)CCOCC1CC1)CNC(C)C None
60657 2269 29 None -3 3 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 307 11 2 4 2.4 O[C@H](COc1ccc(cc1)CCOCC1CC1)CNC(C)C None
8035 2269 29 None -3 3 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 307 11 2 4 2.4 O[C@H](COc1ccc(cc1)CCOCC1CC1)CNC(C)C None
CHEMBL1201274 2269 29 None -3 3 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 307 11 2 4 2.4 O[C@H](COc1ccc(cc1)CCOCC1CC1)CNC(C)C None
DB09351 2269 29 None -3 3 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 307 11 2 4 2.4 O[C@H](COc1ccc(cc1)CCOCC1CC1)CNC(C)C None
118422671 2706 0 None -3 4 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O None
1887 2706 0 None -3 4 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O None
71301 2706 0 None -3 4 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O None
7246 2706 0 None -3 4 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O None
CHEMBL434394 2706 0 None -3 4 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O None
DB04861 2706 0 None -3 4 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O None
1588 2284 24 None -50 44 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
28864 2284 24 None -50 44 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
43 2284 24 None -50 44 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL157138 2284 24 None -50 44 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB00589 2284 24 None -50 44 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
4183 1986 62 None 2 3 Human 8.1 pKi = 8.1 Binding
Binding affinity to human beta2-adrenoceptor by radioligand binding assayBinding affinity to human beta2-adrenoceptor by radioligand binding assay
Drug Central 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O None
6918554 1986 62 None 2 3 Human 8.1 pKi = 8.1 Binding
Binding affinity to human beta2-adrenoceptor by radioligand binding assayBinding affinity to human beta2-adrenoceptor by radioligand binding assay
Drug Central 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O None
7455 1986 62 None 2 3 Human 8.1 pKi = 8.1 Binding
Binding affinity to human beta2-adrenoceptor by radioligand binding assayBinding affinity to human beta2-adrenoceptor by radioligand binding assay
Drug Central 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O None
CHEMBL1095777 1986 62 None 2 3 Human 8.1 pKi = 8.1 Binding
Binding affinity to human beta2-adrenoceptor by radioligand binding assayBinding affinity to human beta2-adrenoceptor by radioligand binding assay
Drug Central 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O None
DB05039 1986 62 None 2 3 Human 8.1 pKi = 8.1 Binding
Binding affinity to human beta2-adrenoceptor by radioligand binding assayBinding affinity to human beta2-adrenoceptor by radioligand binding assay
Drug Central 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O None
3083544 462 46 125I-ICYP -5 5 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O None
4943 462 46 125I-ICYP -5 5 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O None
7479 462 46 125I-ICYP -5 5 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O None
CHEMBL1363 462 46 125I-ICYP -5 5 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O None
DB01274 462 46 125I-ICYP -5 5 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O None
1588 2284 24 3H-CGP-12177 -50 44 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
28864 2284 24 3H-CGP-12177 -50 44 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
43 2284 24 3H-CGP-12177 -50 44 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL157138 2284 24 3H-CGP-12177 -50 44 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB00589 2284 24 3H-CGP-12177 -50 44 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
1531 2226 64 None -1 15 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
Drug Central 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O None
3869 2226 64 None -1 15 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
Drug Central 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O None
7207 2226 64 None -1 15 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
Drug Central 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O None
CHEMBL429 2226 64 None -1 15 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
Drug Central 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O None
DB00598 2226 64 None -1 15 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
Drug Central 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O None
1978 248 54 125I-ICYP -1096 6 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 336 10 3 5 3.0 CCCC(=Nc1ccc(c(c1)C(=O)C)OCC(CNC(C)C)O)O None
40 248 54 125I-ICYP -1096 6 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 336 10 3 5 3.0 CCCC(=Nc1ccc(c(c1)C(=O)C)OCC(CNC(C)C)O)O None
7107 248 54 125I-ICYP -1096 6 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 336 10 3 5 3.0 CCCC(=Nc1ccc(c(c1)C(=O)C)OCC(CNC(C)C)O)O None
CHEMBL642 248 54 125I-ICYP -1096 6 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 336 10 3 5 3.0 CCCC(=Nc1ccc(c(c1)C(=O)C)OCC(CNC(C)C)O)O None
DB01193 248 54 125I-ICYP -1096 6 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 336 10 3 5 3.0 CCCC(=Nc1ccc(c(c1)C(=O)C)OCC(CNC(C)C)O)O None
1155 1592 45 125I-CYP 2 5 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O None
3343 1592 45 125I-CYP 2 5 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O None
557 1592 45 125I-CYP 2 5 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O None
CHEMBL32800 1592 45 125I-CYP 2 5 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O None
DB01288 1592 45 125I-CYP 2 5 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O None
1028 287 69 125I-CYP -89 30 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
139148732 287 69 125I-CYP -89 30 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
479 287 69 125I-CYP -89 30 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
5816 287 69 125I-CYP -89 30 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
CHEMBL679 287 69 125I-CYP -89 30 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
DB00668 287 69 125I-CYP -89 30 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
1621 2386 16 125I-Pindolol -2398 45 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
17 2386 16 125I-Pindolol -2398 45 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
5761 2386 16 125I-Pindolol -2398 45 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL263881 2386 16 125I-Pindolol -2398 45 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB04829 2386 16 125I-Pindolol -2398 45 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
31101 719 39 3H-CGP-12177 -97 36 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
35 719 39 3H-CGP-12177 -97 36 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
403 719 39 3H-CGP-12177 -97 36 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
CHEMBL493 719 39 3H-CGP-12177 -97 36 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
DB01200 719 39 3H-CGP-12177 -97 36 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
None 215919 0 UNDEFINED - 1 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 392 6 4 4 3.1 CCC1=C(C=C2CC(CC2=C1)NCC(C3=C4C=CC(=O)NC4=C(C=C3)O)O)CC None
3337 214431 0 125I-Pindolol -199 41 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
65801 214431 0 125I-Pindolol -199 41 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
66264 214431 0 125I-Pindolol -199 41 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
91452 214431 0 125I-Pindolol -199 41 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
3337 214431 0 125I-Pindolol -199 41 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
65801 214431 0 125I-Pindolol -199 41 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
66264 214431 0 125I-Pindolol -199 41 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
91452 214431 0 125I-Pindolol -199 41 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
4631 193292 25 None -1 7 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 265 9 2 4 2.0 C=CCOc1ccccc1OCC(O)CNC(C)C None
CHEMBL546 193292 25 None -1 7 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 265 9 2 4 2.0 C=CCOc1ccccc1OCC(O)CNC(C)C None
165193 3126 60 None 1 43 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
2303 3126 60 None 1 43 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
4946 3126 60 None 1 43 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
564 3126 60 None 1 43 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
62882 3126 60 None 1 43 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
63 3126 60 None 1 43 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
66366 3126 60 None 1 43 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
91536 3126 60 None 1 43 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
CHEMBL27 3126 60 None 1 43 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
CHEMBL452861 3126 60 None 1 43 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
DB00571 3126 60 None 1 43 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
None 214400 0 125I-ICYP 8 2 Guinea pig 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 363 5 3 6 2.7 COC1=CC(=CC(=C1OC)OC)CC2C3=CC(=C(C(=C3CCN2)F)O)O None
11823027 192006 33 None -1 3 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 309 5 4 5 0.6 CC(C)(C)NCC(O)COc1cccc2c1CC(O)C(O)C2 None
4411 192006 33 None -1 3 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 309 5 4 5 0.6 CC(C)(C)NCC(O)COc1cccc2c1CC(O)C(O)C2 None
CHEMBL521606 192006 33 None -1 3 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 309 5 4 5 0.6 CC(C)(C)NCC(O)COc1cccc2c1CC(O)C(O)C2 None
128658 33738 7 125I-ICYP 3 5 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 363 5 3 6 2.7 COc1cc(CC2NCCc3cc(O)c(O)c(F)c32)cc(OC)c1OC None
CHEMBL142428 33738 7 125I-ICYP 3 5 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 363 5 3 6 2.7 COc1cc(CC2NCCc3cc(O)c(O)c(F)c32)cc(OC)c1OC None
71733 215953 0 None -1 2 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 261 4 2 3 3.4 CCC1=CC=CC2=C1OC(=C2)C(O)CNC(C)(C)C None
484 2804 45 3H-DHA -31 36 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
951 2804 45 3H-DHA -31 36 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
CHEMBL432 2804 45 3H-DHA -31 36 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
27402 203963 15 3H-DHA -151 7 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 223 5 1 3 2.2 CCc1cc(OC)c(CC(C)N)cc1OC None
CHEMBL8224 203963 15 3H-DHA -151 7 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 223 5 1 3 2.2 CCc1cc(OC)c(CC(C)N)cc1OC None
2249 509 106 125I-CYP -33 12 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C None
255 509 106 125I-CYP -33 12 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C None
548 509 106 125I-CYP -33 12 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C None
CHEMBL24 509 106 125I-CYP -33 12 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C None
DB00335 509 106 125I-CYP -33 12 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C None
3486 3096 51 3H-DHA -60 11 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C None
4883 3096 51 3H-DHA -60 11 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C None
555 3096 51 3H-DHA -60 11 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C None
CHEMBL6995 3096 51 3H-DHA -60 11 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C None
DB01297 3096 51 3H-DHA -60 11 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C None
2176 3065 66 None -2 27 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
4828 3065 66 None -2 27 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
91 3065 66 None -2 27 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
CHEMBL500 3065 66 None -2 27 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
DB00960 3065 66 None -2 27 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
37464 19010 23 None -1 4 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 291 6 2 3 3.5 CC(C)(C)NC[C@H](O)COc1ccccc1C1CCCC1 None
CHEMBL1290 19010 23 None -1 4 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 291 6 2 3 3.5 CC(C)(C)NC[C@H](O)COc1ccccc1C1CCCC1 None
2475 728 0 None 1 3 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 271 5 2 3 2.8 OC(COc1cc(C)ccc1Cl)CNC(C)(C)C None
433 728 0 None 1 3 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 271 5 2 3 2.8 OC(COc1cc(C)ccc1Cl)CNC(C)(C)C None
550 728 0 None 1 3 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 271 5 2 3 2.8 OC(COc1cc(C)ccc1Cl)CNC(C)(C)C None
CHEMBL305380 728 0 None 1 3 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 271 5 2 3 2.8 OC(COc1cc(C)ccc1Cl)CNC(C)(C)C None
DB08808 728 0 None 1 3 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 271 5 2 3 2.8 OC(COc1cc(C)ccc1Cl)CNC(C)(C)C None
11504295 2867 40 None -1 3 Human 8.0 pKi = 8.0 Binding
competitive binding experiments against [3H]CGP 12177 in the presence of 5'-guanylyl-imidodiphosphatecompetitive binding experiments against [3H]CGP 12177 in the presence of 5'-guanylyl-imidodiphosphate
Drug Central 386 7 4 6 2.4 COc1ccc(cc1)CC(NC[C@@H](c1cc(O)cc2c1OCC(=O)N2)O)(C)C None
4814 2867 40 None -1 3 Human 8.0 pKi = 8.0 Binding
competitive binding experiments against [3H]CGP 12177 in the presence of 5'-guanylyl-imidodiphosphatecompetitive binding experiments against [3H]CGP 12177 in the presence of 5'-guanylyl-imidodiphosphate
Drug Central 386 7 4 6 2.4 COc1ccc(cc1)CC(NC[C@@H](c1cc(O)cc2c1OCC(=O)N2)O)(C)C None
7543 2867 40 None -1 3 Human 8.0 pKi = 8.0 Binding
competitive binding experiments against [3H]CGP 12177 in the presence of 5'-guanylyl-imidodiphosphatecompetitive binding experiments against [3H]CGP 12177 in the presence of 5'-guanylyl-imidodiphosphate
Drug Central 386 7 4 6 2.4 COc1ccc(cc1)CC(NC[C@@H](c1cc(O)cc2c1OCC(=O)N2)O)(C)C None
CHEMBL605846 2867 40 None -1 3 Human 8.0 pKi = 8.0 Binding
competitive binding experiments against [3H]CGP 12177 in the presence of 5'-guanylyl-imidodiphosphatecompetitive binding experiments against [3H]CGP 12177 in the presence of 5'-guanylyl-imidodiphosphate
Drug Central 386 7 4 6 2.4 COc1ccc(cc1)CC(NC[C@@H](c1cc(O)cc2c1OCC(=O)N2)O)(C)C None
DB09080 2867 40 None -1 3 Human 8.0 pKi = 8.0 Binding
competitive binding experiments against [3H]CGP 12177 in the presence of 5'-guanylyl-imidodiphosphatecompetitive binding experiments against [3H]CGP 12177 in the presence of 5'-guanylyl-imidodiphosphate
Drug Central 386 7 4 6 2.4 COc1ccc(cc1)CC(NC[C@@H](c1cc(O)cc2c1OCC(=O)N2)O)(C)C None
2419 3394 80 125I-ICYP 16 6 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O None
5152 3394 80 125I-ICYP 16 6 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O None
559 3394 80 125I-ICYP 16 6 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O None
CHEMBL1263 3394 80 125I-ICYP 16 6 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O None
DB00938 3394 80 125I-ICYP 16 6 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O None
2583 204168 46 None -2 2 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 292 5 3 4 1.7 CC(C)(C)NCC(O)COc1cccc2c1CCC(=O)N2 None
CHEMBL839 204168 46 None -2 2 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 292 5 3 4 1.7 CC(C)(C)NCC(O)COc1cccc2c1CCC(=O)N2 None
39468 2270 33 None 3 7 Human 8.0 pKi = 8.0 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
Drug Central 291 5 2 4 2.3 O[C@H](COc1cccc2c1CCCC2=O)CNC(C)(C)C None
431 2270 33 None 3 7 Human 8.0 pKi = 8.0 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
Drug Central 291 5 2 4 2.3 O[C@H](COc1cccc2c1CCCC2=O)CNC(C)(C)C None
570 2270 33 None 3 7 Human 8.0 pKi = 8.0 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
Drug Central 291 5 2 4 2.3 O[C@H](COc1cccc2c1CCCC2=O)CNC(C)(C)C None
CHEMBL1201237 2270 33 None 3 7 Human 8.0 pKi = 8.0 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
Drug Central 291 5 2 4 2.3 O[C@H](COc1cccc2c1CCCC2=O)CNC(C)(C)C None
DB01210 2270 33 None 3 7 Human 8.0 pKi = 8.0 Binding
DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
Drug Central 291 5 2 4 2.3 O[C@H](COc1cccc2c1CCCC2=O)CNC(C)(C)C None
2419 3394 80 None 16 6 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]cyanopindolol from human recombinant beta2 adrenergic receptor expressed in CHO cells by filtration assayDisplacement of [125I]cyanopindolol from human recombinant beta2 adrenergic receptor expressed in CHO cells by filtration assay
Drug Central 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O None
5152 3394 80 None 16 6 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]cyanopindolol from human recombinant beta2 adrenergic receptor expressed in CHO cells by filtration assayDisplacement of [125I]cyanopindolol from human recombinant beta2 adrenergic receptor expressed in CHO cells by filtration assay
Drug Central 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O None
559 3394 80 None 16 6 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]cyanopindolol from human recombinant beta2 adrenergic receptor expressed in CHO cells by filtration assayDisplacement of [125I]cyanopindolol from human recombinant beta2 adrenergic receptor expressed in CHO cells by filtration assay
Drug Central 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O None
CHEMBL1263 3394 80 None 16 6 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]cyanopindolol from human recombinant beta2 adrenergic receptor expressed in CHO cells by filtration assayDisplacement of [125I]cyanopindolol from human recombinant beta2 adrenergic receptor expressed in CHO cells by filtration assay
Drug Central 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O None
DB00938 3394 80 None 16 6 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]cyanopindolol from human recombinant beta2 adrenergic receptor expressed in CHO cells by filtration assayDisplacement of [125I]cyanopindolol from human recombinant beta2 adrenergic receptor expressed in CHO cells by filtration assay
Drug Central 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O None
44112 120764 41 None -1 7 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 380 7 2 4 4.5 Cc1cc2c(OCC(CNC(C)(C)C)OC(=O)c3ccccc3)cccc2[nH]1 None
CHEMBL357995 120764 41 None -1 7 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 380 7 2 4 4.5 Cc1cc2c(OCC(CNC(C)(C)C)OC(=O)c3ccccc3)cccc2[nH]1 None
33624 3749 29 None 1 9 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C None
4061 3749 29 None 1 9 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C None
565 3749 29 None 1 9 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C None
CHEMBL499 3749 29 None 1 9 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C None
DB00373 3749 29 None 1 9 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C None
5581 101175 10 125I-ICYP 1 7 Guinea pig 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 345 5 3 6 2.6 COc1cc(CC2NCCc3cc(O)c(O)cc32)cc(OC)c1OC None
CHEMBL299175 101175 10 125I-ICYP 1 7 Guinea pig 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 345 5 3 6 2.6 COc1cc(CC2NCCc3cc(O)c(O)cc32)cc(OC)c1OC None
4631 193292 25 125I-ICYP -1 7 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 265 9 2 4 2.0 C=CCOc1ccccc1OCC(O)CNC(C)C None
CHEMBL546 193292 25 125I-ICYP -1 7 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 265 9 2 4 2.0 C=CCOc1ccccc1OCC(O)CNC(C)C None
2585 788 100 None 1 22 Human 8.0 pKi = 8 Binding
NoneNone
Drug Central 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
522 788 100 None 1 22 Human 8.0 pKi = 8 Binding
NoneNone
Drug Central 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
551 788 100 None 1 22 Human 8.0 pKi = 8 Binding
NoneNone
Drug Central 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
CHEMBL723 788 100 None 1 22 Human 8.0 pKi = 8 Binding
NoneNone
Drug Central 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
DB01136 788 100 None 1 22 Human 8.0 pKi = 8 Binding
NoneNone
Drug Central 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
487 779 65 None 4 6 Human 8.0 pKi = 8 Binding
Displacement of [3H]DHA from human beta2 adrenoceptor by liquid scintillation counterDisplacement of [3H]DHA from human beta2 adrenoceptor by liquid scintillation counter
Drug Central 298 6 3 3 3.1 OC(COc1cccc2c1c1ccccc1[nH]2)CNC(C)C None
569 779 65 None 4 6 Human 8.0 pKi = 8 Binding
Displacement of [3H]DHA from human beta2 adrenoceptor by liquid scintillation counterDisplacement of [3H]DHA from human beta2 adrenoceptor by liquid scintillation counter
Drug Central 298 6 3 3 3.1 OC(COc1cccc2c1c1ccccc1[nH]2)CNC(C)C None
71739 779 65 None 4 6 Human 8.0 pKi = 8 Binding
Displacement of [3H]DHA from human beta2 adrenoceptor by liquid scintillation counterDisplacement of [3H]DHA from human beta2 adrenoceptor by liquid scintillation counter
Drug Central 298 6 3 3 3.1 OC(COc1cccc2c1c1ccccc1[nH]2)CNC(C)C None
CHEMBL324665 779 65 None 4 6 Human 8.0 pKi = 8 Binding
Displacement of [3H]DHA from human beta2 adrenoceptor by liquid scintillation counterDisplacement of [3H]DHA from human beta2 adrenoceptor by liquid scintillation counter
Drug Central 298 6 3 3 3.1 OC(COc1cccc2c1c1ccccc1[nH]2)CNC(C)C None
None 214640 0 125I-CYP -21 3 Human 5.0 pKi = 5.0 Binding
NoneNone
PDSP KiDatabase 363 9 3 4 3.1 CC(CC1=CC=C(C=C1)OCC(=O)O)NCC(C2=CC(=CC=C2)Cl)O None
219050 3309 21 3H-CGP-12177 -5754 21 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 346 6 2 2 5.0 Oc1ccc2c(c1)c(CCCCN1CCC(=CC1)c1ccccc1)c[nH]2 None
52 3309 21 3H-CGP-12177 -5754 21 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 346 6 2 2 5.0 Oc1ccc2c(c1)c(CCCCN1CCC(=CC1)c1ccccc1)c[nH]2 None
CHEMBL431367 3309 21 3H-CGP-12177 -5754 21 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 346 6 2 2 5.0 Oc1ccc2c(c1)c(CCCCN1CCC(=CC1)c1ccccc1)c[nH]2 None
None 214399 0 125I-ICYP -2 4 Guinea pig 5.0 pKi = 5.0 Binding
NoneNone
PDSP KiDatabase 381 5 3 5 -1.5 COC1=CC(=CC(=C1OC)OC)CC2C3=CC(=C(C=C3CC[NH2+]2)O)O.[Cl-] None
10455 3218 34 None - 1 Human 6.7 pKi = 6.7 Binding
Inhibitory constant determined from a standard radioligand displacement assay using human &beta;2-adrenoceptors expressed in Sf-9 cells and [<sup>3</sup>H]CGP1217 as tracer.Inhibitory constant determined from a standard radioligand displacement assay using human &beta;2-adrenoceptors expressed in Sf-9 cells and [<sup>3</sup>H]CGP1217 as tracer.
Guide to Pharmacology 301 7 4 4 2.7 CC(NCC(c1ccc(cc1)O)O)CCc1ccc(cc1)O 19245211
10455 3218 34 None - 1 Human 6.7 pKi = 6.7 Binding
Inhibitory constant determined from a standard radioligand displacement assay using human &beta;2-adrenoceptors expressed in Sf-9 cells and [<sup>3</sup>H]CGP1217 as tracer.Inhibitory constant determined from a standard radioligand displacement assay using human &beta;2-adrenoceptors expressed in Sf-9 cells and [<sup>3</sup>H]CGP1217 as tracer.
Guide to Pharmacology 301 7 4 4 2.7 CC(NCC(c1ccc(cc1)O)O)CCc1ccc(cc1)O 35732075
56052 3218 34 None - 1 Human 6.7 pKi = 6.7 Binding
Inhibitory constant determined from a standard radioligand displacement assay using human &beta;2-adrenoceptors expressed in Sf-9 cells and [<sup>3</sup>H]CGP1217 as tracer.Inhibitory constant determined from a standard radioligand displacement assay using human &beta;2-adrenoceptors expressed in Sf-9 cells and [<sup>3</sup>H]CGP1217 as tracer.
Guide to Pharmacology 301 7 4 4 2.7 CC(NCC(c1ccc(cc1)O)O)CCc1ccc(cc1)O 19245211
56052 3218 34 None - 1 Human 6.7 pKi = 6.7 Binding
Inhibitory constant determined from a standard radioligand displacement assay using human &beta;2-adrenoceptors expressed in Sf-9 cells and [<sup>3</sup>H]CGP1217 as tracer.Inhibitory constant determined from a standard radioligand displacement assay using human &beta;2-adrenoceptors expressed in Sf-9 cells and [<sup>3</sup>H]CGP1217 as tracer.
Guide to Pharmacology 301 7 4 4 2.7 CC(NCC(c1ccc(cc1)O)O)CCc1ccc(cc1)O 35732075
CHEMBL509336 3218 34 None - 1 Human 6.7 pKi = 6.7 Binding
Inhibitory constant determined from a standard radioligand displacement assay using human &beta;2-adrenoceptors expressed in Sf-9 cells and [<sup>3</sup>H]CGP1217 as tracer.Inhibitory constant determined from a standard radioligand displacement assay using human &beta;2-adrenoceptors expressed in Sf-9 cells and [<sup>3</sup>H]CGP1217 as tracer.
Guide to Pharmacology 301 7 4 4 2.7 CC(NCC(c1ccc(cc1)O)O)CCc1ccc(cc1)O 19245211
CHEMBL509336 3218 34 None - 1 Human 6.7 pKi = 6.7 Binding
Inhibitory constant determined from a standard radioligand displacement assay using human &beta;2-adrenoceptors expressed in Sf-9 cells and [<sup>3</sup>H]CGP1217 as tracer.Inhibitory constant determined from a standard radioligand displacement assay using human &beta;2-adrenoceptors expressed in Sf-9 cells and [<sup>3</sup>H]CGP1217 as tracer.
Guide to Pharmacology 301 7 4 4 2.7 CC(NCC(c1ccc(cc1)O)O)CCc1ccc(cc1)O 35732075
DB11541 3218 34 None - 1 Human 6.7 pKi = 6.7 Binding
Inhibitory constant determined from a standard radioligand displacement assay using human &beta;2-adrenoceptors expressed in Sf-9 cells and [<sup>3</sup>H]CGP1217 as tracer.Inhibitory constant determined from a standard radioligand displacement assay using human &beta;2-adrenoceptors expressed in Sf-9 cells and [<sup>3</sup>H]CGP1217 as tracer.
Guide to Pharmacology 301 7 4 4 2.7 CC(NCC(c1ccc(cc1)O)O)CCc1ccc(cc1)O 19245211
DB11541 3218 34 None - 1 Human 6.7 pKi = 6.7 Binding
Inhibitory constant determined from a standard radioligand displacement assay using human &beta;2-adrenoceptors expressed in Sf-9 cells and [<sup>3</sup>H]CGP1217 as tracer.Inhibitory constant determined from a standard radioligand displacement assay using human &beta;2-adrenoceptors expressed in Sf-9 cells and [<sup>3</sup>H]CGP1217 as tracer.
Guide to Pharmacology 301 7 4 4 2.7 CC(NCC(c1ccc(cc1)O)O)CCc1ccc(cc1)O 35732075
123600 2275 0 None - 1 Human 5.3 pKi = 5.3 Binding
Measuring displacement of [<sup>3</sup>H]-DHA from recombinant human &beta;<sub>2</sub> adrenoceptors expressed in HEK293T cells.Measuring displacement of [<sup>3</sup>H]-DHA from recombinant human &beta;<sub>2</sub> adrenoceptors expressed in HEK293T cells.
Guide to Pharmacology 239 4 4 4 1.3 OCc1cc(ccc1O)[C@H](CNC(C)(C)C)O 22182578
1575 2275 0 None - 1 Human 5.3 pKi = 5.3 Binding
Measuring displacement of [<sup>3</sup>H]-DHA from recombinant human &beta;<sub>2</sub> adrenoceptors expressed in HEK293T cells.Measuring displacement of [<sup>3</sup>H]-DHA from recombinant human &beta;<sub>2</sub> adrenoceptors expressed in HEK293T cells.
Guide to Pharmacology 239 4 4 4 1.3 OCc1cc(ccc1O)[C@H](CNC(C)(C)C)O 22182578
9816 2275 0 None - 1 Human 5.3 pKi = 5.3 Binding
Measuring displacement of [<sup>3</sup>H]-DHA from recombinant human &beta;<sub>2</sub> adrenoceptors expressed in HEK293T cells.Measuring displacement of [<sup>3</sup>H]-DHA from recombinant human &beta;<sub>2</sub> adrenoceptors expressed in HEK293T cells.
Guide to Pharmacology 239 4 4 4 1.3 OCc1cc(ccc1O)[C@H](CNC(C)(C)C)O 22182578
CHEMBL1002 2275 0 None - 1 Human 5.3 pKi = 5.3 Binding
Measuring displacement of [<sup>3</sup>H]-DHA from recombinant human &beta;<sub>2</sub> adrenoceptors expressed in HEK293T cells.Measuring displacement of [<sup>3</sup>H]-DHA from recombinant human &beta;<sub>2</sub> adrenoceptors expressed in HEK293T cells.
Guide to Pharmacology 239 4 4 4 1.3 OCc1cc(ccc1O)[C@H](CNC(C)(C)C)O 22182578
DB13139 2275 0 None - 1 Human 5.3 pKi = 5.3 Binding
Measuring displacement of [<sup>3</sup>H]-DHA from recombinant human &beta;<sub>2</sub> adrenoceptors expressed in HEK293T cells.Measuring displacement of [<sup>3</sup>H]-DHA from recombinant human &beta;<sub>2</sub> adrenoceptors expressed in HEK293T cells.
Guide to Pharmacology 239 4 4 4 1.3 OCc1cc(ccc1O)[C@H](CNC(C)(C)C)O 22182578
118422671 2706 0 None -3 4 Human 8.0 pKi = 8.0 Binding
Radioligand bindingRadioligand binding
Guide to Pharmacology 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 21172342
1887 2706 0 None -3 4 Human 8.0 pKi = 8.0 Binding
Radioligand bindingRadioligand binding
Guide to Pharmacology 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 21172342
71301 2706 0 None -3 4 Human 8.0 pKi = 8.0 Binding
Radioligand bindingRadioligand binding
Guide to Pharmacology 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 21172342
7246 2706 0 None -3 4 Human 8.0 pKi = 8.0 Binding
Radioligand bindingRadioligand binding
Guide to Pharmacology 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 21172342
CHEMBL434394 2706 0 None -3 4 Human 8.0 pKi = 8.0 Binding
Radioligand bindingRadioligand binding
Guide to Pharmacology 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 21172342
DB04861 2706 0 None -3 4 Human 8.0 pKi = 8.0 Binding
Radioligand bindingRadioligand binding
Guide to Pharmacology 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 21172342
1960 2805 64 None -549 26 Human 4.7 pKi = 4.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 14730417
1960 2805 64 None -549 26 Human 4.7 pKi = 4.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 2849109
439260 2805 64 None -549 26 Human 4.7 pKi = 4.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 14730417
439260 2805 64 None -549 26 Human 4.7 pKi = 4.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 2849109
505 2805 64 None -549 26 Human 4.7 pKi = 4.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 14730417
505 2805 64 None -549 26 Human 4.7 pKi = 4.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 2849109
CHEMBL1437 2805 64 None -549 26 Human 4.7 pKi = 4.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 14730417
CHEMBL1437 2805 64 None -549 26 Human 4.7 pKi = 4.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 2849109
DB00368 2805 64 None -549 26 Human 4.7 pKi = 4.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 14730417
DB00368 2805 64 None -549 26 Human 4.7 pKi = 4.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 2849109
1024 1535 27 None - 1 Human 5.6 pKi = 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 165 3 2 2 1.3 CN[C@H]([C@@H](c1ccccc1)O)C 9295336
556 1535 27 None - 1 Human 5.6 pKi = 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 165 3 2 2 1.3 CN[C@H]([C@@H](c1ccccc1)O)C 9295336
9294 1535 27 None - 1 Human 5.6 pKi = 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 165 3 2 2 1.3 CN[C@H]([C@@H](c1ccccc1)O)C 9295336
CHEMBL211456 1535 27 None - 1 Human 5.6 pKi = 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 165 3 2 2 1.3 CN[C@H]([C@@H](c1ccccc1)O)C 9295336
DB01364 1535 27 None - 1 Human 5.6 pKi = 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 165 3 2 2 1.3 CN[C@H]([C@@H](c1ccccc1)O)C 9295336
2598 3707 52 None -6 5 Human 5.6 pKi = 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 225 3 4 4 1.5 OC(c1cc(O)cc(c1)O)CNC(C)(C)C 15655528
5403 3707 52 None -6 5 Human 5.6 pKi = 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 225 3 4 4 1.5 OC(c1cc(O)cc(c1)O)CNC(C)(C)C 15655528
560 3707 52 None -6 5 Human 5.6 pKi = 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 225 3 4 4 1.5 OC(c1cc(O)cc(c1)O)CNC(C)(C)C 15655528
CHEMBL1760 3707 52 None -6 5 Human 5.6 pKi = 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 225 3 4 4 1.5 OC(c1cc(O)cc(c1)O)CNC(C)(C)C 15655528
DB00871 3707 52 None -6 5 Human 5.6 pKi = 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 225 3 4 4 1.5 OC(c1cc(O)cc(c1)O)CNC(C)(C)C 15655528
105 3392 84 None -10 6 Human 6.0 pKi = 6.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10531390
105 3392 84 None -10 6 Human 6.0 pKi = 6.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 15655528
2083 3392 84 None -10 6 Human 6.0 pKi = 6.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10531390
2083 3392 84 None -10 6 Human 6.0 pKi = 6.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 15655528
558 3392 84 None -10 6 Human 6.0 pKi = 6.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10531390
558 3392 84 None -10 6 Human 6.0 pKi = 6.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 15655528
CHEMBL714 3392 84 None -10 6 Human 6.0 pKi = 6.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10531390
CHEMBL714 3392 84 None -10 6 Human 6.0 pKi = 6.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 15655528
DB01001 3392 84 None -10 6 Human 6.0 pKi = 6.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10531390
DB01001 3392 84 None -10 6 Human 6.0 pKi = 6.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 15655528
1028 287 69 None -89 30 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 14730417
1028 287 69 None -89 30 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 2849109
1028 287 69 None -89 30 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 9295336
139148732 287 69 None -89 30 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 14730417
139148732 287 69 None -89 30 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 2849109
139148732 287 69 None -89 30 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 9295336
479 287 69 None -89 30 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 14730417
479 287 69 None -89 30 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 2849109
479 287 69 None -89 30 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 9295336
5816 287 69 None -89 30 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 14730417
5816 287 69 None -89 30 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 2849109
5816 287 69 None -89 30 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 9295336
CHEMBL679 287 69 None -89 30 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 14730417
CHEMBL679 287 69 None -89 30 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 2849109
CHEMBL679 287 69 None -89 30 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 9295336
DB00668 287 69 None -89 30 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 14730417
DB00668 287 69 None -89 30 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 2849109
DB00668 287 69 None -89 30 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 9295336
2464 3570 52 None -7 6 Human 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C 15655528
5253 3570 52 None -7 6 Human 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C 15655528
7297 3570 52 None -7 6 Human 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C 15655528
CHEMBL471 3570 52 None -7 6 Human 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C 15655528
DB00489 3570 52 None -7 6 Human 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C 15655528
1499 2052 43 None -33 17 Human 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 8982677
3779 2052 43 None -33 17 Human 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 8982677
536 2052 43 None -33 17 Human 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 8982677
CHEMBL434 2052 43 None -33 17 Human 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 8982677
DB01064 2052 43 None -33 17 Human 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 8982677
134495 736 18 None -2 3 Rat 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 5 2 4 2.5 COc1ccc(cc1C(C(NC(C)(C)C)C)O)OC 1968985
134495 736 18 None -2 3 Rat 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 5 2 4 2.5 COc1ccc(cc1C(C(NC(C)(C)C)C)O)OC 6140042
18026 736 18 None -2 3 Rat 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 5 2 4 2.5 COc1ccc(cc1C(C(NC(C)(C)C)C)O)OC 1968985
18026 736 18 None -2 3 Rat 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 5 2 4 2.5 COc1ccc(cc1C(C(NC(C)(C)C)C)O)OC 6140042
9809 736 18 None -2 3 Rat 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 5 2 4 2.5 COc1ccc(cc1C(C(NC(C)(C)C)C)O)OC 1968985
9809 736 18 None -2 3 Rat 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 5 2 4 2.5 COc1ccc(cc1C(C(NC(C)(C)C)C)O)OC 6140042
CHEMBL289093 736 18 None -2 3 Rat 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 5 2 4 2.5 COc1ccc(cc1C(C(NC(C)(C)C)C)O)OC 1968985
CHEMBL289093 736 18 None -2 3 Rat 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 5 2 4 2.5 COc1ccc(cc1C(C(NC(C)(C)C)C)O)OC 6140042
1155 1592 45 None 2 5 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 24454993
1155 1592 45 None 2 5 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 25324048
1155 1592 45 None 2 5 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 35732075
3343 1592 45 None 2 5 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 24454993
3343 1592 45 None 2 5 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 25324048
3343 1592 45 None 2 5 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 35732075
557 1592 45 None 2 5 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 24454993
557 1592 45 None 2 5 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 25324048
557 1592 45 None 2 5 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 35732075
CHEMBL32800 1592 45 None 2 5 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 24454993
CHEMBL32800 1592 45 None 2 5 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 25324048
CHEMBL32800 1592 45 None 2 5 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 35732075
DB01288 1592 45 None 2 5 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 24454993
DB01288 1592 45 None 2 5 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 25324048
DB01288 1592 45 None 2 5 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 35732075
2291 3123 52 None -3 12 Human 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O None
2561 3123 52 None -3 12 Human 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O None
4932 3123 52 None -3 12 Human 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O None
CHEMBL631 3123 52 None -3 12 Human 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O None
DB01182 3123 52 None -3 12 Human 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O None
4752 2269 29 None -3 3 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 307 11 2 4 2.4 O[C@H](COc1ccc(cc1)CCOCC1CC1)CNC(C)C 11572462
60657 2269 29 None -3 3 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 307 11 2 4 2.4 O[C@H](COc1ccc(cc1)CCOCC1CC1)CNC(C)C 11572462
8035 2269 29 None -3 3 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 307 11 2 4 2.4 O[C@H](COc1ccc(cc1)CCOCC1CC1)CNC(C)C 11572462
CHEMBL1201274 2269 29 None -3 3 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 307 11 2 4 2.4 O[C@H](COc1ccc(cc1)CCOCC1CC1)CNC(C)C 11572462
DB09351 2269 29 None -3 3 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 307 11 2 4 2.4 O[C@H](COc1ccc(cc1)CCOCC1CC1)CNC(C)C 11572462
39147 2662 0 None 7 3 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 5 4 5 0.6 OC(COc1cccc2c1C[C@H](O)[C@@H](C2)O)CNC(C)(C)C 10411574
39147 2662 0 None 7 3 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 5 4 5 0.6 OC(COc1cccc2c1C[C@H](O)[C@@H](C2)O)CNC(C)(C)C 15655528
554 2662 0 None 7 3 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 5 4 5 0.6 OC(COc1cccc2c1C[C@H](O)[C@@H](C2)O)CNC(C)(C)C 10411574
554 2662 0 None 7 3 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 5 4 5 0.6 OC(COc1cccc2c1C[C@H](O)[C@@H](C2)O)CNC(C)(C)C 15655528
CHEMBL649 2662 0 None 7 3 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 5 4 5 0.6 OC(COc1cccc2c1C[C@H](O)[C@@H](C2)O)CNC(C)(C)C 10411574
CHEMBL649 2662 0 None 7 3 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 5 4 5 0.6 OC(COc1cccc2c1C[C@H](O)[C@@H](C2)O)CNC(C)(C)C 15655528
DB01203 2662 0 None 7 3 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 5 4 5 0.6 OC(COc1cccc2c1C[C@H](O)[C@@H](C2)O)CNC(C)(C)C 10411574
DB01203 2662 0 None 7 3 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 5 4 5 0.6 OC(COc1cccc2c1C[C@H](O)[C@@H](C2)O)CNC(C)(C)C 15655528
4183 1986 62 None 2 3 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O 16434564
4183 1986 62 None 2 3 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O 22932315
6918554 1986 62 None 2 3 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O 16434564
6918554 1986 62 None 2 3 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O 22932315
7455 1986 62 None 2 3 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O 16434564
7455 1986 62 None 2 3 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O 22932315
CHEMBL1095777 1986 62 None 2 3 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O 16434564
CHEMBL1095777 1986 62 None 2 3 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O 22932315
DB05039 1986 62 None 2 3 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O 16434564
DB05039 1986 62 None 2 3 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O 22932315
1531 2226 64 None -1 15 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O None
3869 2226 64 None -1 15 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O None
7207 2226 64 None -1 15 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O None
CHEMBL429 2226 64 None -1 15 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O None
DB00598 2226 64 None -1 15 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O None
3083544 462 46 None -5 5 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O 15324892
4943 462 46 None -5 5 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O 15324892
7479 462 46 None -5 5 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O 15324892
CHEMBL1363 462 46 None -5 5 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O 15324892
DB01274 462 46 None -5 5 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O 15324892
2475 728 0 None 1 3 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 271 5 2 3 2.8 OC(COc1cc(C)ccc1Cl)CNC(C)(C)C 10079020
2475 728 0 None 1 3 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 271 5 2 3 2.8 OC(COc1cc(C)ccc1Cl)CNC(C)(C)C 10411574
2475 728 0 None 1 3 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 271 5 2 3 2.8 OC(COc1cc(C)ccc1Cl)CNC(C)(C)C 15655528
433 728 0 None 1 3 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 271 5 2 3 2.8 OC(COc1cc(C)ccc1Cl)CNC(C)(C)C 10079020
433 728 0 None 1 3 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 271 5 2 3 2.8 OC(COc1cc(C)ccc1Cl)CNC(C)(C)C 10411574
433 728 0 None 1 3 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 271 5 2 3 2.8 OC(COc1cc(C)ccc1Cl)CNC(C)(C)C 15655528
550 728 0 None 1 3 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 271 5 2 3 2.8 OC(COc1cc(C)ccc1Cl)CNC(C)(C)C 10079020
550 728 0 None 1 3 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 271 5 2 3 2.8 OC(COc1cc(C)ccc1Cl)CNC(C)(C)C 10411574
550 728 0 None 1 3 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 271 5 2 3 2.8 OC(COc1cc(C)ccc1Cl)CNC(C)(C)C 15655528
CHEMBL305380 728 0 None 1 3 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 271 5 2 3 2.8 OC(COc1cc(C)ccc1Cl)CNC(C)(C)C 10079020
CHEMBL305380 728 0 None 1 3 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 271 5 2 3 2.8 OC(COc1cc(C)ccc1Cl)CNC(C)(C)C 10411574
CHEMBL305380 728 0 None 1 3 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 271 5 2 3 2.8 OC(COc1cc(C)ccc1Cl)CNC(C)(C)C 15655528
DB08808 728 0 None 1 3 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 271 5 2 3 2.8 OC(COc1cc(C)ccc1Cl)CNC(C)(C)C 10079020
DB08808 728 0 None 1 3 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 271 5 2 3 2.8 OC(COc1cc(C)ccc1Cl)CNC(C)(C)C 10411574
DB08808 728 0 None 1 3 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 271 5 2 3 2.8 OC(COc1cc(C)ccc1Cl)CNC(C)(C)C 15655528
5311452 3601 8 None 7 3 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 325 7 2 3 3.7 CCc1ccccc1OC[C@H](CN[C@H]1CCCc2c1cccc2)O 10411574
5311452 3601 8 None 7 3 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 325 7 2 3 3.7 CCc1ccccc1OC[C@H](CN[C@H]1CCCc2c1cccc2)O 15655528
547 3601 8 None 7 3 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 325 7 2 3 3.7 CCc1ccccc1OC[C@H](CN[C@H]1CCCc2c1cccc2)O 10411574
547 3601 8 None 7 3 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 325 7 2 3 3.7 CCc1ccccc1OC[C@H](CN[C@H]1CCCc2c1cccc2)O 15655528
CHEMBL1326499 3601 8 None 7 3 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 325 7 2 3 3.7 CCc1ccccc1OC[C@H](CN[C@H]1CCCc2c1cccc2)O 10411574
CHEMBL1326499 3601 8 None 7 3 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 325 7 2 3 3.7 CCc1ccccc1OC[C@H](CN[C@H]1CCCc2c1cccc2)O 15655528
137 367 47 None -3 12 Human 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 15655528
2119 367 47 None -3 12 Human 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 15655528
563 367 47 None -3 12 Human 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 15655528
66368 367 47 None -3 12 Human 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 15655528
CHEMBL266195 367 47 None -3 12 Human 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 15655528
DB00866 367 47 None -3 12 Human 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 15655528
39468 2270 33 None 3 7 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 5 2 4 2.3 O[C@H](COc1cccc2c1CCCC2=O)CNC(C)(C)C None
431 2270 33 None 3 7 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 5 2 4 2.3 O[C@H](COc1cccc2c1CCCC2=O)CNC(C)(C)C None
570 2270 33 None 3 7 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 5 2 4 2.3 O[C@H](COc1cccc2c1CCCC2=O)CNC(C)(C)C None
CHEMBL1201237 2270 33 None 3 7 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 5 2 4 2.3 O[C@H](COc1cccc2c1CCCC2=O)CNC(C)(C)C None
DB01210 2270 33 None 3 7 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 5 2 4 2.3 O[C@H](COc1cccc2c1CCCC2=O)CNC(C)(C)C None
165193 3126 60 None 1 43 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10079020
165193 3126 60 None 1 43 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10531390
165193 3126 60 None 1 43 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 12920204
165193 3126 60 None 1 43 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 15655528
2303 3126 60 None 1 43 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10079020
2303 3126 60 None 1 43 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10531390
2303 3126 60 None 1 43 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 12920204
2303 3126 60 None 1 43 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 15655528
4946 3126 60 None 1 43 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10079020
4946 3126 60 None 1 43 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10531390
4946 3126 60 None 1 43 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 12920204
4946 3126 60 None 1 43 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 15655528
564 3126 60 None 1 43 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10079020
564 3126 60 None 1 43 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10531390
564 3126 60 None 1 43 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 12920204
564 3126 60 None 1 43 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 15655528
62882 3126 60 None 1 43 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10079020
62882 3126 60 None 1 43 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10531390
62882 3126 60 None 1 43 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 12920204
62882 3126 60 None 1 43 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 15655528
63 3126 60 None 1 43 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10079020
63 3126 60 None 1 43 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10531390
63 3126 60 None 1 43 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 12920204
63 3126 60 None 1 43 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 15655528
66366 3126 60 None 1 43 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10079020
66366 3126 60 None 1 43 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10531390
66366 3126 60 None 1 43 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 12920204
66366 3126 60 None 1 43 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 15655528
91536 3126 60 None 1 43 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10079020
91536 3126 60 None 1 43 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10531390
91536 3126 60 None 1 43 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 12920204
91536 3126 60 None 1 43 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 15655528
CHEMBL27 3126 60 None 1 43 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10079020
CHEMBL27 3126 60 None 1 43 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10531390
CHEMBL27 3126 60 None 1 43 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 12920204
CHEMBL27 3126 60 None 1 43 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 15655528
CHEMBL452861 3126 60 None 1 43 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10079020
CHEMBL452861 3126 60 None 1 43 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10531390
CHEMBL452861 3126 60 None 1 43 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 12920204
CHEMBL452861 3126 60 None 1 43 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 15655528
DB00571 3126 60 None 1 43 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10079020
DB00571 3126 60 None 1 43 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10531390
DB00571 3126 60 None 1 43 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 12920204
DB00571 3126 60 None 1 43 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 15655528
5311179 1935 18 None 85 3 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 6 2 3 2.6 Cc1c2CCCc2c(cc1)OC[C@H]([C@H](C)NC(C)C)O 10079020
5311179 1935 18 None 85 3 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 6 2 3 2.6 Cc1c2CCCc2c(cc1)OC[C@H]([C@H](C)NC(C)C)O 12920204
5311179 1935 18 None 85 3 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 6 2 3 2.6 Cc1c2CCCc2c(cc1)OC[C@H]([C@H](C)NC(C)C)O 15655528
543 1935 18 None 85 3 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 6 2 3 2.6 Cc1c2CCCc2c(cc1)OC[C@H]([C@H](C)NC(C)C)O 10079020
543 1935 18 None 85 3 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 6 2 3 2.6 Cc1c2CCCc2c(cc1)OC[C@H]([C@H](C)NC(C)C)O 12920204
543 1935 18 None 85 3 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 6 2 3 2.6 Cc1c2CCCc2c(cc1)OC[C@H]([C@H](C)NC(C)C)O 15655528
5484725 1935 18 None 85 3 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 6 2 3 2.6 Cc1c2CCCc2c(cc1)OC[C@H]([C@H](C)NC(C)C)O 10079020
5484725 1935 18 None 85 3 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 6 2 3 2.6 Cc1c2CCCc2c(cc1)OC[C@H]([C@H](C)NC(C)C)O 12920204
5484725 1935 18 None 85 3 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 6 2 3 2.6 Cc1c2CCCc2c(cc1)OC[C@H]([C@H](C)NC(C)C)O 15655528
CHEMBL1233766 1935 18 None 85 3 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 6 2 3 2.6 Cc1c2CCCc2c(cc1)OC[C@H]([C@H](C)NC(C)C)O 10079020
CHEMBL1233766 1935 18 None 85 3 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 6 2 3 2.6 Cc1c2CCCc2c(cc1)OC[C@H]([C@H](C)NC(C)C)O 12920204
CHEMBL1233766 1935 18 None 85 3 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 6 2 3 2.6 Cc1c2CCCc2c(cc1)OC[C@H]([C@H](C)NC(C)C)O 15655528
CHEMBL198059 1935 18 None 85 3 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 6 2 3 2.6 Cc1c2CCCc2c(cc1)OC[C@H]([C@H](C)NC(C)C)O 10079020
CHEMBL198059 1935 18 None 85 3 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 6 2 3 2.6 Cc1c2CCCc2c(cc1)OC[C@H]([C@H](C)NC(C)C)O 12920204
CHEMBL198059 1935 18 None 85 3 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 277 6 2 3 2.6 Cc1c2CCCc2c(cc1)OC[C@H]([C@H](C)NC(C)C)O 15655528
2176 3065 66 None -2 27 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C 17804228
4828 3065 66 None -2 27 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C 17804228
91 3065 66 None -2 27 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C 17804228
CHEMBL500 3065 66 None -2 27 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C 17804228
DB00960 3065 66 None -2 27 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C 17804228
2585 788 100 None 1 22 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10411574
2585 788 100 None 1 22 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 15655528
522 788 100 None 1 22 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10411574
522 788 100 None 1 22 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 15655528
551 788 100 None 1 22 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10411574
551 788 100 None 1 22 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 15655528
CHEMBL723 788 100 None 1 22 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10411574
CHEMBL723 788 100 None 1 22 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 15655528
DB01136 788 100 None 1 22 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10411574
DB01136 788 100 None 1 22 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 15655528
33624 3749 29 None 1 9 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C 15655528
4061 3749 29 None 1 9 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C 15655528
565 3749 29 None 1 9 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C 15655528
CHEMBL499 3749 29 None 1 9 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C 15655528
DB00373 3749 29 None 1 9 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C 15655528
487 779 65 None 4 6 Human 9.9 pKi = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 6 3 3 3.1 OC(COc1cccc2c1c1ccccc1[nH]2)CNC(C)C 18829308
569 779 65 None 4 6 Human 9.9 pKi = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 6 3 3 3.1 OC(COc1cccc2c1c1ccccc1[nH]2)CNC(C)C 18829308
71739 779 65 None 4 6 Human 9.9 pKi = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 6 3 3 3.1 OC(COc1cccc2c1c1ccccc1[nH]2)CNC(C)C 18829308
CHEMBL324665 779 65 None 4 6 Human 9.9 pKi = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 6 3 3 3.1 OC(COc1cccc2c1c1ccccc1[nH]2)CNC(C)C 18829308
3337 214431 0 None -199 41 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
65801 214431 0 None -199 41 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
66264 214431 0 None -199 41 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
91452 214431 0 None -199 41 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
1353 1872 85 None -446 86 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1872 85 None -446 86 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1872 85 None -446 86 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1872 85 None -446 86 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1872 85 None -446 86 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
135398745 2858 108 None -331 66 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2858 108 None -331 66 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2858 108 None -331 66 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2858 108 None -331 66 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
2181 3067 0 None -134 35 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
4830 3067 0 None -134 35 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
92 3067 0 None -134 35 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
CHEMBL440294 3067 0 None -134 35 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
DB09286 3067 0 None -134 35 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
2337 3193 72 None -72 63 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3193 72 None -72 63 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3193 72 None -72 63 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3193 72 None -72 63 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3193 72 None -72 63 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
2389 3267 114 None -2089 68 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3267 114 None -2089 68 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3267 114 None -2089 68 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3267 114 None -2089 68 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3267 114 None -2089 68 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
2435 3520 78 None -316 49 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
60149 3520 78 None -316 49 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
98 3520 78 None -316 49 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
CHEMBL12713 3520 78 None -316 49 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
DB06144 3520 78 None -316 49 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
2865 4064 67 None -1318 54 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 4064 67 None -1318 54 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 4064 67 None -1318 54 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 4064 67 None -1318 54 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 4064 67 None -1318 54 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
115237 55281 113 None -2754 55 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
CHEMBL1621 55281 113 None -2754 55 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
46780481 107032 18 None -954 54 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
9903970 107032 18 None -954 54 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3187365 107032 18 None -954 54 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3544974 107032 18 None -954 54 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
135398737 942 89 None -190 92 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 942 89 None -190 92 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 942 89 None -190 92 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 942 89 None -190 92 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 942 89 None -190 92 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
31101 719 39 None -97 36 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
35 719 39 None -97 36 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
403 719 39 None -97 36 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
CHEMBL493 719 39 None -97 36 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
DB01200 719 39 None -97 36 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
242 467 117 None -23 52 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 467 117 None -23 52 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 467 117 None -23 52 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 467 117 None -23 52 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 467 117 None -23 52 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
65772 215997 0 None 1 2 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 345 5 3 6 2.6 COC1=CC(C[C@@H]2NCCC3=CC(O)=C(O)C=C23)=CC(OC)=C1OC None
2601 3709 30 None -14 21 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
443951 3709 30 None -14 21 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
56 3709 30 None -14 21 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL73151 3709 30 None -14 21 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
DB13399 3709 30 None -14 21 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
32051 4072 0 None - 1 Human 3.3 pKi None 3.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 64 0 0 0 -0.0 [Zn+2] 11752207
32051 4072 0 None - 1 Human 3.3 pKi None 3.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 64 0 0 0 -0.0 [Zn+2] 12409304
566 4072 0 None - 1 Human 3.3 pKi None 3.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 64 0 0 0 -0.0 [Zn+2] 11752207
566 4072 0 None - 1 Human 3.3 pKi None 3.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 64 0 0 0 -0.0 [Zn+2] 12409304
5311116 2293 6 None -1258 3 Human 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 484 15 5 8 2.2 N#Cc1cc(OCCOCC2CC2)ccc1OCC(CNCCNC(=O)Nc1ccc(cc1)O)O 10079020
544 2293 6 None -1258 3 Human 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 484 15 5 8 2.2 N#Cc1cc(OCCOCC2CC2)ccc1OCC(CNCCNC(=O)Nc1ccc(cc1)O)O 10079020
CHEMBL207802 2293 6 None -1258 3 Human 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 484 15 5 8 2.2 N#Cc1cc(OCCOCC2CC2)ccc1OCC(CNCCNC(=O)Nc1ccc(cc1)O)O 10079020
32051 4072 0 None - 1 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 64 0 0 0 -0.0 [Zn+2] 11752207
32051 4072 0 None - 1 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 64 0 0 0 -0.0 [Zn+2] 12409304
566 4072 0 None - 1 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 64 0 0 0 -0.0 [Zn+2] 11752207
566 4072 0 None - 1 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 64 0 0 0 -0.0 [Zn+2] 12409304
484 2804 45 None -31 36 Human 5.4 pKi None 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O 15102946
951 2804 45 None -31 36 Human 5.4 pKi None 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O 15102946
CHEMBL432 2804 45 None -31 36 Human 5.4 pKi None 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O 15102946
2249 509 106 None -33 12 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10079020
2249 509 106 None -33 12 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 15655528
255 509 106 None -33 12 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10079020
255 509 106 None -33 12 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 15655528
548 509 106 None -33 12 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10079020
548 509 106 None -33 12 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 15655528
CHEMBL24 509 106 None -33 12 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10079020
CHEMBL24 509 106 None -33 12 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 15655528
DB00335 509 106 None -33 12 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10079020
DB00335 509 106 None -33 12 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 15655528
10587912 2772 0 None -12 2 Human 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 9 3 4 1.3 OCCCc1ccc(cc1)OCC(CNC(C)C)O 10079020
545 2772 0 None -12 2 Human 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 9 3 4 1.3 OCCCc1ccc(cc1)OCC(CNC(C)C)O 10079020
146294 913 0 None -6 2 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 323 12 2 5 2.2 OC(COc1ccc(cc1)OCCOCC1CC1)CNC(C)C 10079020
552 913 0 None -6 2 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 323 12 2 5 2.2 OC(COc1ccc(cc1)OCCOCC1CC1)CNC(C)C 10079020
637 913 0 None -6 2 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 323 12 2 5 2.2 OC(COc1ccc(cc1)OCCOCC1CC1)CNC(C)C 10079020
CHEMBL2110772 913 0 None -6 2 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 323 12 2 5 2.2 OC(COc1ccc(cc1)OCCOCC1CC1)CNC(C)C 10079020
1786 2474 79 None -25 11 Human 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10079020
4171 2474 79 None -25 11 Human 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10079020
553 2474 79 None -25 11 Human 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10079020
CHEMBL13 2474 79 None -25 11 Human 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10079020
DB00264 2474 79 None -25 11 Human 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10079020
2369 615 75 None -7 8 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C 10079020
356 615 75 None -7 8 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C 10079020
549 615 75 None -7 8 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C 10079020
CHEMBL423 615 75 None -7 8 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C 10079020
DB00195 615 75 None -7 8 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C 10079020
3123920 2774 79 None -18 6 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 209 6 2 3 1.4 OC(COc1ccccc1)CNC(C)C 10079020
546 2774 79 None -18 6 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 209 6 2 3 1.4 OC(COc1ccccc1)CNC(C)C 10079020
CHEMBL7154 2774 79 None -18 6 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 209 6 2 3 1.4 OC(COc1ccccc1)CNC(C)C 10079020
2687 874 15 None 1 5 Human 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 279 5 4 4 1.0 OC(COc1cccc2c1[nH]c(=O)[nH]2)CNC(C)(C)C 10079020
2687 874 15 None 1 5 Human 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 279 5 4 4 1.0 OC(COc1cccc2c1[nH]c(=O)[nH]2)CNC(C)(C)C 15655528
532 874 15 None 1 5 Human 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 279 5 4 4 1.0 OC(COc1cccc2c1[nH]c(=O)[nH]2)CNC(C)(C)C 10079020
532 874 15 None 1 5 Human 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 279 5 4 4 1.0 OC(COc1cccc2c1[nH]c(=O)[nH]2)CNC(C)(C)C 15655528
5387 874 15 None 1 5 Human 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 279 5 4 4 1.0 OC(COc1cccc2c1[nH]c(=O)[nH]2)CNC(C)(C)C 10079020
5387 874 15 None 1 5 Human 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 279 5 4 4 1.0 OC(COc1cccc2c1[nH]c(=O)[nH]2)CNC(C)(C)C 15655528
CHEMBL420746 874 15 None 1 5 Human 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 279 5 4 4 1.0 OC(COc1cccc2c1[nH]c(=O)[nH]2)CNC(C)(C)C 10079020
CHEMBL420746 874 15 None 1 5 Human 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 279 5 4 4 1.0 OC(COc1cccc2c1[nH]c(=O)[nH]2)CNC(C)(C)C 15655528