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
9849126 12318 0 None 3 4 Guinea pig 10.4 pEC50 = 10.4 Functional
Agonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contractionAgonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contraction
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 Guinea pig 10.4 pEC50 = 10.4 Functional
Agonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contractionAgonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contraction
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 Guinea pig 10.4 pEC50 = 10.4 Functional
Agonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contractionAgonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contraction
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
1499 2052 43 None -64 36 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm701324c
3779 2052 43 None -64 36 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm701324c
536 2052 43 None -64 36 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm701324c
CHEMBL434 2052 43 None -64 36 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm701324c
DB01064 2052 43 None -64 36 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm701324c
1499 2052 43 None -64 36 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta-1 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.bmcl.2008.08.009
3779 2052 43 None -64 36 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta-1 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.bmcl.2008.08.009
536 2052 43 None -64 36 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta-1 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.bmcl.2008.08.009
CHEMBL434 2052 43 None -64 36 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta-1 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.bmcl.2008.08.009
DB01064 2052 43 None -64 36 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta-1 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.bmcl.2008.08.009
1499 2052 43 None -64 36 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta-1 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 -64 36 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta-1 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 -64 36 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta-1 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 -64 36 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta-1 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 -64 36 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta-1 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
1499 2052 43 None -64 36 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 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 -64 36 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 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 -64 36 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 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 -64 36 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 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 -64 36 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 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 -64 36 Human 10.1 pEC50 = 10.1 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 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 -64 36 Human 10.1 pEC50 = 10.1 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 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 -64 36 Human 10.1 pEC50 = 10.1 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 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 -64 36 Human 10.1 pEC50 = 10.1 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 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 -64 36 Human 10.1 pEC50 = 10.1 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 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
11268355 95936 0 None 1 3 Human 9.9 pEC50 = 9.9 Functional
Agonistic activity against human Beta-1 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonistic activity against human Beta-1 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 1 3 Human 9.9 pEC50 = 9.9 Functional
Agonistic activity against human Beta-1 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonistic activity against human Beta-1 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
1239 1639 46 None 1 5 Guinea pig 9.5 pEC50 = 9.5 Functional
Agonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contractionAgonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contraction
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 Guinea pig 9.5 pEC50 = 9.5 Functional
Agonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contractionAgonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contraction
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 Guinea pig 9.5 pEC50 = 9.5 Functional
Agonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contractionAgonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contraction
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 Guinea pig 9.5 pEC50 = 9.5 Functional
Agonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contractionAgonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contraction
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 Guinea pig 9.5 pEC50 = 9.5 Functional
Agonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contractionAgonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contraction
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1021/jm801016j
24936881 17320 0 None 1 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as 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 1 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as 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
12065 621 21 None -6 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human adrenergic beta 1 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 1 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 9.2 pEC50 = 9.2 Functional
Agonist activity at human adrenergic beta 1 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 1 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 9.2 pEC50 = 9.2 Functional
Agonist activity at human adrenergic beta 1 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 1 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
164622827 187969 0 None -26 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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 9.2 pEC50 = 9.2 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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 9.2 pEC50 = 9.2 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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
9891927 183605 6 None -5 4 Guinea pig 9.1 pEC50 = 9.1 Functional
Agonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contractionAgonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contraction
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 Guinea pig 9.1 pEC50 = 9.1 Functional
Agonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contractionAgonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contraction
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 Guinea pig 9.1 pEC50 = 9.1 Functional
Agonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contractionAgonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contraction
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 Guinea pig 9.1 pEC50 = 9.1 Functional
Agonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contractionAgonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contraction
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
45483810 195458 0 None -3 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human adrenergic beta 1 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 1 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 9.1 pEC50 = 9.1 Functional
Agonist activity at human adrenergic beta 1 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 1 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
123686 1942 44 None 74 3 Human 9.1 pEC50 = 9.1 Functional
Partial agonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsPartial agonist activity at human beta1 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 9.1 pEC50 = 9.1 Functional
Partial agonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsPartial agonist activity at human beta1 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 9.1 pEC50 = 9.1 Functional
Partial agonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsPartial agonist activity at human beta1 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
1499 2052 43 None -64 36 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 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 -64 36 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 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 -64 36 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 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 -64 36 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 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 -64 36 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 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
164623105 187973 0 None -47 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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 9.1 pEC50 = 9.1 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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 9.1 pEC50 = 9.1 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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
13345218 195535 0 None -8 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human adrenergic beta 1 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 1 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 9.1 pEC50 = 9.1 Functional
Agonist activity at human adrenergic beta 1 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 1 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
44392175 131259 0 None 1 2 Human 9.1 pEC50 = 9.1 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptor
ChEMBL 480 12 5 7 3.2 O=C(Nc1ccc(C[C@@H](CO)NC[C@H](O)COc2ccccc2)cc1)Nc1cccc([N+](=O)[O-])c1 10.1016/j.bmcl.2004.11.001
CHEMBL369346 131259 0 None 1 2 Human 9.1 pEC50 = 9.1 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptor
ChEMBL 480 12 5 7 3.2 O=C(Nc1ccc(C[C@@H](CO)NC[C@H](O)COc2ccccc2)cc1)Nc1cccc([N+](=O)[O-])c1 10.1016/j.bmcl.2004.11.001
1499 2052 43 None -64 36 Human 9.0 pEC50 = 9 Functional
Activity against human beta 1 adrenergic receptor (AR), expressed in CHO cells.Activity against human beta 1 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 -64 36 Human 9.0 pEC50 = 9 Functional
Activity against human beta 1 adrenergic receptor (AR), expressed in CHO cells.Activity against human beta 1 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 -64 36 Human 9.0 pEC50 = 9 Functional
Activity against human beta 1 adrenergic receptor (AR), expressed in CHO cells.Activity against human beta 1 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 -64 36 Human 9.0 pEC50 = 9 Functional
Activity against human beta 1 adrenergic receptor (AR), expressed in CHO cells.Activity against human beta 1 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 -64 36 Human 9.0 pEC50 = 9 Functional
Activity against human beta 1 adrenergic receptor (AR), expressed in CHO cells.Activity against human beta 1 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 -64 36 Human 9.0 pEC50 = 9 Functional
Activity at human beta-1 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-1 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 -64 36 Human 9.0 pEC50 = 9 Functional
Activity at human beta-1 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-1 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 -64 36 Human 9.0 pEC50 = 9 Functional
Activity at human beta-1 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-1 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 -64 36 Human 9.0 pEC50 = 9 Functional
Activity at human beta-1 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-1 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 -64 36 Human 9.0 pEC50 = 9 Functional
Activity at human beta-1 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-1 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
1499 2052 43 None -64 36 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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 -64 36 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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 -64 36 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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 -64 36 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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 -64 36 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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
44392230 65251 0 None 1 2 Human 8.9 pEC50 = 8.9 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptor
ChEMBL 479 12 6 6 3.0 O=C(Nc1ccc(C[C@@H](CO)NC[C@H](O)COc2ccccc2)cc1)Nc1cccc(C(=O)O)c1 10.1016/j.bmcl.2004.11.001
CHEMBL183283 65251 0 None 1 2 Human 8.9 pEC50 = 8.9 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptor
ChEMBL 479 12 6 6 3.0 O=C(Nc1ccc(C[C@@H](CO)NC[C@H](O)COc2ccccc2)cc1)Nc1cccc(C(=O)O)c1 10.1016/j.bmcl.2004.11.001
24822304 97402 0 None 6 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 412 9 3 5 4.1 O=C(O)c1ccc(Oc2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)nc1 10.1021/jm701324c
CHEMBL272234 97402 0 None 6 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 412 9 3 5 4.1 O=C(O)c1ccc(Oc2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)nc1 10.1021/jm701324c
105 3392 84 None -3 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at beta1 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta1 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 -3 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at beta1 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta1 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 -3 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at beta1 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta1 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 -3 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at beta1 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta1 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 -3 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at beta1 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta1 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
164615126 187910 0 None -104 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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 8.8 pEC50 = 8.8 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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 8.8 pEC50 = 8.8 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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
90645347 112008 0 None -7 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta1 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 8.8 pEC50 = 8.8 Functional
Agonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta1 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
164618895 187940 0 None -95 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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 8.8 pEC50 = 8.8 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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 8.8 pEC50 = 8.8 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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
45101519 196836 0 None -1 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human beta-1 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta-1 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 8.7 pEC50 = 8.7 Functional
Agonist activity at human beta-1 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta-1 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
24936492 17352 0 None -1 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as 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 -1 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as 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
164612078 187884 0 None -64 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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 8.7 pEC50 = 8.7 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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 8.7 pEC50 = 8.7 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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
9927453 96226 0 None -1 3 Human 8.7 pEC50 = 8.7 Functional
Agonistic activity against human Beta-1 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonistic activity against human Beta-1 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 -1 3 Human 8.7 pEC50 = 8.7 Functional
Agonistic activity against human Beta-1 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonistic activity against human Beta-1 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
42625513 12437 0 None -3 4 Guinea pig 8.7 pEC50 = 8.7 Functional
Agonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contractionAgonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contraction
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 Guinea pig 8.7 pEC50 = 8.7 Functional
Agonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contractionAgonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contraction
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 Guinea pig 8.7 pEC50 = 8.7 Functional
Agonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contractionAgonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contraction
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1ccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc1 10.1021/jm801016j
90645346 111990 0 None -2 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta1 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 8.7 pEC50 = 8.7 Functional
Agonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta1 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
42625517 12597 0 None -19 4 Guinea pig 8.0 pEC50 = 8 Functional
Agonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contractionAgonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contraction
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 Guinea pig 8.0 pEC50 = 8 Functional
Agonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contractionAgonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contraction
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 Guinea pig 8.0 pEC50 = 8 Functional
Agonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contractionAgonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contraction
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
11180293 112003 0 None -22 3 Human 8.0 pEC50 = 8 Functional
Agonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta1 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 8.0 pEC50 = 8 Functional
Agonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta1 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
56668796 66254 0 None -31 3 Human 8.0 pEC50 = 8 Functional
Agonist activity at human beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta1 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 8.0 pEC50 = 8 Functional
Agonist activity at human beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta1 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 8.0 pEC50 = 8 Functional
Agonist activity at human beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta1 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
45273268 193946 0 None 194 2 Human 8.0 pEC50 = 8 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 362 10 3 4 4.0 O[C@@H](CNCCc1ccc(Nc2ccccc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL1204004 193946 0 None 194 2 Human 8.0 pEC50 = 8 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 362 10 3 4 4.0 O[C@@H](CNCCc1ccc(Nc2ccccc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL556274 193946 0 None 194 2 Human 8.0 pEC50 = 8 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 362 10 3 4 4.0 O[C@@H](CNCCc1ccc(Nc2ccccc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
10217757 111765 0 None -31 4 Human 8.0 pEC50 = 8 Functional
Agonist activity at human recombinant beta1 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta1 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 -31 4 Human 8.0 pEC50 = 8 Functional
Agonist activity at human recombinant beta1 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta1 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
164614147 187898 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 400 7 4 4 3.9 CC(C)(CCc1cccc(Cl)c1)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
CHEMBL4856990 187898 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 400 7 4 4 3.9 CC(C)(CCc1cccc(Cl)c1)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
CHEMBL5028233 187898 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 400 7 4 4 3.9 CC(C)(CCc1cccc(Cl)c1)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
164618813 187939 0 None -275 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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 8.0 pEC50 = 8.0 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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 8.0 pEC50 = 8.0 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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
164619360 187943 0 None -371 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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 8.0 pEC50 = 8.0 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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 8.0 pEC50 = 8.0 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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
155774 4021 33 None 64 3 Human 8.0 pEC50 = 8.0 Functional
Partial agonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsPartial agonist activity at human beta1 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 8.0 pEC50 = 8.0 Functional
Partial agonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsPartial agonist activity at human beta1 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 8.0 pEC50 = 8.0 Functional
Partial agonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsPartial agonist activity at human beta1 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 8.0 pEC50 = 8.0 Functional
Partial agonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsPartial agonist activity at human beta1 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 8.0 pEC50 = 8.0 Functional
Partial agonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsPartial agonist activity at human beta1 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
10863093 50041 0 None -19 3 Human 7.0 pEC50 = 7 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-1 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-1 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 -19 3 Human 7.0 pEC50 = 7 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-1 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-1 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
16049450 63747 0 None -125 2 Human 7.0 pEC50 = 7 Functional
Agonist activity at adrenergic beta1 receptorAgonist activity at adrenergic beta1 receptor
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 7.0 pEC50 = 7 Functional
Agonist activity at adrenergic beta1 receptorAgonist activity at adrenergic beta1 receptor
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
16049234 63748 0 None -177 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at adrenergic beta1 receptorAgonist activity at adrenergic beta1 receptor
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 7.0 pEC50 = 7 Functional
Agonist activity at adrenergic beta1 receptorAgonist activity at adrenergic beta1 receptor
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
16049448 63749 0 None -56 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at adrenergic beta1 receptorAgonist activity at adrenergic beta1 receptor
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 7.0 pEC50 = 7 Functional
Agonist activity at adrenergic beta1 receptorAgonist activity at adrenergic beta1 receptor
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
16049374 63753 0 None -89 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at adrenergic beta1 receptorAgonist activity at adrenergic beta1 receptor
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 7.0 pEC50 = 7 Functional
Agonist activity at adrenergic beta1 receptorAgonist activity at adrenergic beta1 receptor
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
1499 2052 43 None -64 36 Human 7.0 pEC50 = 7 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 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 -64 36 Human 7.0 pEC50 = 7 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 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 -64 36 Human 7.0 pEC50 = 7 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 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 -64 36 Human 7.0 pEC50 = 7 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 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 -64 36 Human 7.0 pEC50 = 7 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 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
9888047 92936 0 None -398 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 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 -398 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 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
44441231 147510 0 None -50 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 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-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 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
44441235 150448 0 None -251 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 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 -251 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 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
45271523 193448 0 None -10 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 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 7.0 pEC50 = 7 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 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 7.0 pEC50 = 7 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 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
45272417 193760 0 None -1 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 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 7.0 pEC50 = 7 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 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 7.0 pEC50 = 7 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 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
42625823 12555 0 None -501 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta-1 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 -501 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta-1 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 -501 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta-1 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
46832804 6893 0 None -50 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta-1 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 7.0 pEC50 = 7 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta-1 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
10553603 99224 0 None 1 3 Human 7.0 pEC50 = 7 Functional
Increased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 1 Adrenergic receptorIncreased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 1 Adrenergic receptor
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 1 3 Human 7.0 pEC50 = 7 Functional
Increased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 1 Adrenergic receptorIncreased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 1 Adrenergic receptor
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
1499 2052 43 None -64 36 Human 6.0 pEC50 = 6 Functional
Agonist activity at beta1 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta1 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 -64 36 Human 6.0 pEC50 = 6 Functional
Agonist activity at beta1 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta1 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 -64 36 Human 6.0 pEC50 = 6 Functional
Agonist activity at beta1 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta1 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 -64 36 Human 6.0 pEC50 = 6 Functional
Agonist activity at beta1 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta1 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 -64 36 Human 6.0 pEC50 = 6 Functional
Agonist activity at beta1 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta1 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
1499 2052 43 None -64 36 Human 6.0 pEC50 = 6 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 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 -64 36 Human 6.0 pEC50 = 6 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 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 -64 36 Human 6.0 pEC50 = 6 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 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 -64 36 Human 6.0 pEC50 = 6 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 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 -64 36 Human 6.0 pEC50 = 6 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 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
42625517 12597 0 None -1995 4 Human 6.0 pEC50 = 6 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta-1 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 -1995 4 Human 6.0 pEC50 = 6 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta-1 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 -1995 4 Human 6.0 pEC50 = 6 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta-1 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
42625588 179835 0 None -630 3 Human 6.0 pEC50 = 6 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta-1 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 6.0 pEC50 = 6 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta-1 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
10121328 4357 0 None -100 3 Human 6.0 pEC50 = 6 Functional
Beta-1 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-1-adrenoceptorBeta-1 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-1-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 -100 3 Human 6.0 pEC50 = 6 Functional
Beta-1 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-1-adrenoceptorBeta-1 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-1-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
11575154 76847 0 None -100000 2 Human 5.0 pEC50 = 5 Functional
Activity at human beta-1 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-1 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 411 9 4 5 3.8 O=C(O)c1ccncc1-c1cccc(NCCNC[C@H](O)c2cccc(Cl)c2)c1 10.1021/jm0509445
CHEMBL207943 76847 0 None -100000 2 Human 5.0 pEC50 = 5 Functional
Activity at human beta-1 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-1 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 411 9 4 5 3.8 O=C(O)c1ccncc1-c1cccc(NCCNC[C@H](O)c2cccc(Cl)c2)c1 10.1021/jm0509445
44237766 57916 0 None -10000 2 Rat 5.0 pEC50 = 5 Functional
Agonist activity at beta1 adrenoceptor in rat left atria assessed as induction of ionotropic effectAgonist activity at beta1 adrenoceptor in rat left atria assessed as induction of ionotropic effect
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 Rat 5.0 pEC50 = 5 Functional
Agonist activity at beta1 adrenoceptor in rat left atria assessed as induction of ionotropic effectAgonist activity at beta1 adrenoceptor in rat left atria assessed as induction of ionotropic effect
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
155517986 169629 0 None -478630 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 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 5.0 pEC50 = 5 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 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
164622775 187968 0 None -120226 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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 5.0 pEC50 = 5 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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 5.0 pEC50 = 5 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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
44313150 103288 0 None -6 3 Human 5.0 pEC50 = 5 Functional
Compound was evaluated for its inhibitory activity against human beta-1 adrenergic receptor (AR)Compound was evaluated for its inhibitory activity against human beta-1 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 -6 3 Human 5.0 pEC50 = 5 Functional
Compound was evaluated for its inhibitory activity against human beta-1 adrenergic receptor (AR)Compound was evaluated for its inhibitory activity against human beta-1 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
1960 2805 64 None -79 13 Guinea pig 5.0 pEC50 = 5 Functional
Effective dose required to stimulate contractions in isolated guinea pig atrium.Effective dose required to stimulate contractions in isolated guinea pig atrium.
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00019a001
439260 2805 64 None -79 13 Guinea pig 5.0 pEC50 = 5 Functional
Effective dose required to stimulate contractions in isolated guinea pig atrium.Effective dose required to stimulate contractions in isolated guinea pig atrium.
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00019a001
505 2805 64 None -79 13 Guinea pig 5.0 pEC50 = 5 Functional
Effective dose required to stimulate contractions in isolated guinea pig atrium.Effective dose required to stimulate contractions in isolated guinea pig atrium.
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00019a001
CHEMBL1437 2805 64 None -79 13 Guinea pig 5.0 pEC50 = 5 Functional
Effective dose required to stimulate contractions in isolated guinea pig atrium.Effective dose required to stimulate contractions in isolated guinea pig atrium.
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00019a001
DB00368 2805 64 None -79 13 Guinea pig 5.0 pEC50 = 5 Functional
Effective dose required to stimulate contractions in isolated guinea pig atrium.Effective dose required to stimulate contractions in isolated guinea pig atrium.
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00019a001
10301101 102474 0 None -1659 2 Human 4.0 pEC50 = 4 Functional
Agonistic activity against cloned human beta1-AR (beta-1-adrenergic receptor) in CHO cellsAgonistic activity against cloned human beta1-AR (beta-1-adrenergic receptor) in CHO cells
ChEMBL 509 9 3 6 3.5 COc1ccc(S(=O)(=O)N2CCC(NC[C@H](O)COc3cccc4[nH]c5ccccc5c34)CC2)cc1 10.1016/s0960-894x(03)00387-1
CHEMBL306423 102474 0 None -1659 2 Human 4.0 pEC50 = 4 Functional
Agonistic activity against cloned human beta1-AR (beta-1-adrenergic receptor) in CHO cellsAgonistic activity against cloned human beta1-AR (beta-1-adrenergic receptor) in CHO cells
ChEMBL 509 9 3 6 3.5 COc1ccc(S(=O)(=O)N2CCC(NC[C@H](O)COc3cccc4[nH]c5ccccc5c34)CC2)cc1 10.1016/s0960-894x(03)00387-1
145984792 165165 0 None -12882 3 Human 4.0 pEC50 = 4 Functional
Antagonist activity at human beta1 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 beta1 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 -12882 3 Human 4.0 pEC50 = 4 Functional
Antagonist activity at human beta1 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 beta1 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
45483848 195454 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human adrenergic beta 1 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 1 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 394 7 3 3 5.3 CC(C)c1ccc(CC(C)(C)NCC(O)c2cc(Cl)c(N)c(Cl)c2)cc1 10.1016/j.bmcl.2009.10.013
CHEMBL567843 195454 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human adrenergic beta 1 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 1 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 394 7 3 3 5.3 CC(C)c1ccc(CC(C)(C)NCC(O)c2cc(Cl)c(N)c(Cl)c2)cc1 10.1016/j.bmcl.2009.10.013
11567751 199065 0 None -29 2 Human 7.0 pEC50 = 7 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta-1 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 7.0 pEC50 = 7 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta-1 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
10145482 4091 0 None -34 2 Human 6.0 pEC50 = 6 Functional
In vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-1 adrenergic receptorIn vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-1 adrenergic receptor
ChEMBL 604 12 5 7 3.4 O=C(NCc1cc(F)ccc1F)Nc1ccc(S(=O)(=O)N2CCC(CNC[C@H](O)COc3ccc(O)cc3)CC2)cc1 10.1016/s0960-894x(02)00607-8
CHEMBL100057 4091 0 None -34 2 Human 6.0 pEC50 = 6 Functional
In vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-1 adrenergic receptorIn vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-1 adrenergic receptor
ChEMBL 604 12 5 7 3.4 O=C(NCc1cc(F)ccc1F)Nc1ccc(S(=O)(=O)N2CCC(CNC[C@H](O)COc3ccc(O)cc3)CC2)cc1 10.1016/s0960-894x(02)00607-8
10281165 4332 0 None -16 2 Human 6.0 pEC50 = 6.0 Functional
In vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-1 adrenergic receptorIn vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-1 adrenergic receptor
ChEMBL 560 11 5 7 3.3 O=C(Nc1ccc(S(=O)(=O)N2CCC(CNC[C@H](O)COc3ccc(O)cc3)CC2)cc1)NC1CCCCC1 10.1016/s0960-894x(02)00607-8
CHEMBL101485 4332 0 None -16 2 Human 6.0 pEC50 = 6.0 Functional
In vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-1 adrenergic receptorIn vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-1 adrenergic receptor
ChEMBL 560 11 5 7 3.3 O=C(Nc1ccc(S(=O)(=O)N2CCC(CNC[C@H](O)COc3ccc(O)cc3)CC2)cc1)NC1CCCCC1 10.1016/s0960-894x(02)00607-8
11539348 199093 0 None -9 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta-1 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 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta-1 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
44309649 202579 0 None -186 2 Human 5.0 pEC50 = 5.0 Functional
Agonistic activity against cloned human beta1-AR (beta-1-adrenergic receptor) in CHO cellsAgonistic activity against cloned human beta1-AR (beta-1-adrenergic receptor) in CHO cells
ChEMBL 436 9 3 7 1.6 COc1ccc(S(=O)(=O)N2CCC(NC[C@H](O)COc3ccc(O)cc3)CC2)cc1 10.1016/s0960-894x(03)00387-1
CHEMBL71348 202579 0 None -186 2 Human 5.0 pEC50 = 5.0 Functional
Agonistic activity against cloned human beta1-AR (beta-1-adrenergic receptor) in CHO cellsAgonistic activity against cloned human beta1-AR (beta-1-adrenergic receptor) in CHO cells
ChEMBL 436 9 3 7 1.6 COc1ccc(S(=O)(=O)N2CCC(NC[C@H](O)COc3ccc(O)cc3)CC2)cc1 10.1016/s0960-894x(03)00387-1
3083544 462 46 None -89 4 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human beta1 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technologyAgonist activity at human beta1 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 -89 4 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human beta1 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technologyAgonist activity at human beta1 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 -89 4 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human beta1 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technologyAgonist activity at human beta1 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 -89 4 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human beta1 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technologyAgonist activity at human beta1 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 -89 4 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human beta1 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technologyAgonist activity at human beta1 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
10280301 109236 0 None -2 2 Human 7.0 pEC50 = 7.0 Functional
In vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta1-AR receptorIn vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta1-AR receptor
ChEMBL 536 12 5 6 3.9 O=C(NCc1ccc(F)cc1)N1CCC(Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)CC1 10.1016/s0960-894x(01)00645-x
CHEMBL322973 109236 0 None -2 2 Human 7.0 pEC50 = 7.0 Functional
In vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta1-AR receptorIn vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta1-AR receptor
ChEMBL 536 12 5 6 3.9 O=C(NCc1ccc(F)cc1)N1CCC(Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)CC1 10.1016/s0960-894x(01)00645-x
10231394 167242 0 None -190 2 Human 5.0 pEC50 = 5.0 Functional
In vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-1 adrenergic receptorIn vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-1 adrenergic receptor
ChEMBL 562 15 5 7 3.5 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)N2CCC(CNC[C@H](O)COc3ccc(O)cc3)CC2)cc1 10.1016/s0960-894x(02)00607-8
CHEMBL430662 167242 0 None -190 2 Human 5.0 pEC50 = 5.0 Functional
In vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-1 adrenergic receptorIn vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-1 adrenergic receptor
ChEMBL 562 15 5 7 3.5 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)N2CCC(CNC[C@H](O)COc3ccc(O)cc3)CC2)cc1 10.1016/s0960-894x(02)00607-8
24823782 97582 0 None 3 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 396 8 3 4 4.0 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)nc1 10.1021/jm701324c
CHEMBL273097 97582 0 None 3 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 396 8 3 4 4.0 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)nc1 10.1021/jm701324c
45484646 195608 0 None -1 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human beta-1 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta-1 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 8.0 pEC50 = 8.0 Functional
Agonist activity at human beta-1 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta-1 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
24894323 175874 0 None -52 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 468 12 4 5 5.2 CCCOc1cc(-c2ccc(NCCNC[C@H](O)c3cccc(Cl)c3)cc2)ccc1C(=O)O 10.1021/jm8000345
CHEMBL459645 175874 0 None -52 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 468 12 4 5 5.2 CCCOc1cc(-c2ccc(NCCNC[C@H](O)c3cccc(Cl)c3)cc2)ccc1C(=O)O 10.1021/jm8000345
155536813 171630 0 None -263 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 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 8.0 pEC50 = 8.0 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 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
45270680 193358 0 None 5 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 421 10 4 4 4.1 O[C@@H](CNCCc1ccc(NC(=S)Nc2ccccc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL1203993 193358 0 None 5 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 421 10 4 4 4.1 O[C@@H](CNCCc1ccc(NC(=S)Nc2ccccc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL549421 193358 0 None 5 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 421 10 4 4 4.1 O[C@@H](CNCCc1ccc(NC(=S)Nc2ccccc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
45269853 194883 0 None -4 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 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)(Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1)c1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL563872 194883 0 None -4 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 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)(Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1)c1ccccc1 10.1016/j.bmc.2009.06.031
52943968 17597 0 None 1 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as 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 1 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as 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
16222840 194048 0 None -316 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassayAgonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassay
ChEMBL 566 11 4 7 4.7 C[C@H](NCCc1ccc(-c2ccc(C(=O)NS(C)(=O)=O)c(OC3CCCCC3)c2)cc1)[C@H](O)c1ccc(O)cc1 10.1016/j.bmcl.2009.06.083
CHEMBL557253 194048 0 None -316 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassayAgonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassay
ChEMBL 566 11 4 7 4.7 C[C@H](NCCc1ccc(-c2ccc(C(=O)NS(C)(=O)=O)c(OC3CCCCC3)c2)cc1)[C@H](O)c1ccc(O)cc1 10.1016/j.bmcl.2009.06.083
24895559 172521 0 None -338 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 483 12 3 5 5.4 CC(C)COc1cc(-c2ccc(OCCNC[C@H](O)c3cccc(Cl)c3)cc2)ccc1C(=O)O 10.1021/jm8000345
CHEMBL452034 172521 0 None -338 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 483 12 3 5 5.4 CC(C)COc1cc(-c2ccc(OCCNC[C@H](O)c3cccc(Cl)c3)cc2)ccc1C(=O)O 10.1021/jm8000345
105 3392 84 None -3 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human beta1 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technologyAgonist activity at human beta1 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 -3 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human beta1 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technologyAgonist activity at human beta1 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 -3 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human beta1 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technologyAgonist activity at human beta1 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 -3 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human beta1 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technologyAgonist activity at human beta1 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 -3 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human beta1 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technologyAgonist activity at human beta1 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
44377726 56509 0 None -389 2 Human 5.9 pEC50 = 5.9 Functional
Agonistic activity as cAMP accumulation in CHO cells expressing human beta-1-adrenergic receptorAgonistic activity as cAMP accumulation in CHO cells expressing human beta-1-adrenergic receptor
ChEMBL 550 10 5 10 1.6 CS(=O)(=O)Nc1cc(O[C@@H](O)CNC2CCN(c3ccc(CC4SC(=O)NC4=O)cc3)CC2)ccc1O 10.1016/s0960-894x(01)00063-4
CHEMBL164378 56509 0 None -389 2 Human 5.9 pEC50 = 5.9 Functional
Agonistic activity as cAMP accumulation in CHO cells expressing human beta-1-adrenergic receptorAgonistic activity as cAMP accumulation in CHO cells expressing human beta-1-adrenergic receptor
ChEMBL 550 10 5 10 1.6 CS(=O)(=O)Nc1cc(O[C@@H](O)CNC2CCN(c3ccc(CC4SC(=O)NC4=O)cc3)CC2)ccc1O 10.1016/s0960-894x(01)00063-4
1499 2052 43 None -64 36 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 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 -64 36 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 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 -64 36 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 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 -64 36 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 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 -64 36 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 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 -64 36 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 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 -64 36 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 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 -64 36 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 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 -64 36 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 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 -64 36 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 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
16223251 175875 0 None -204 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 449 11 4 6 3.9 CC(C)Cc1cc(-c2ccc(OCCNC[C@H](O)c3ccc(N)nc3)cc2)ccc1C(=O)O 10.1021/jm8000345
CHEMBL459646 175875 0 None -204 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 449 11 4 6 3.9 CC(C)Cc1cc(-c2ccc(OCCNC[C@H](O)c3ccc(N)nc3)cc2)ccc1C(=O)O 10.1021/jm8000345
24895787 186102 0 None -1 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 409 8 3 3 5.0 C[C@@H](Cc1ccc(-c2ccc(C(=O)O)cc2)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm8000345
CHEMBL488431 186102 0 None -1 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 409 8 3 3 5.0 C[C@@H](Cc1ccc(-c2ccc(C(=O)O)cc2)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm8000345
44309272 202171 0 None -2 3 Human 7.9 pEC50 = 7.9 Functional
Agonistic activity against cloned human beta1-AR (beta-1-adrenergic receptor) in CHO cellsAgonistic activity against cloned human beta1-AR (beta-1-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 -2 3 Human 7.9 pEC50 = 7.9 Functional
Agonistic activity against cloned human beta1-AR (beta-1-adrenergic receptor) in CHO cellsAgonistic activity against cloned human beta1-AR (beta-1-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
44392181 65725 0 None -10 2 Human 7.9 pEC50 = 7.9 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptor
ChEMBL 465 12 5 6 3.3 COc1ccccc1NC(=O)Nc1ccc(C[C@@H](CO)NC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmcl.2004.11.001
CHEMBL183744 65725 0 None -10 2 Human 7.9 pEC50 = 7.9 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptor
ChEMBL 465 12 5 6 3.3 COc1ccccc1NC(=O)Nc1ccc(C[C@@H](CO)NC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmcl.2004.11.001
44441230 93341 0 None -7 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 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 -7 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 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
2687 874 15 None 162 2 Human 7.9 pEC50 = 7.9 Functional
Partial agonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsPartial agonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 279 5 4 4 1.0 OC(COc1cccc2c1[nH]c(=O)[nH]2)CNC(C)(C)C 10.1021/jm400348g
532 874 15 None 162 2 Human 7.9 pEC50 = 7.9 Functional
Partial agonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsPartial agonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 279 5 4 4 1.0 OC(COc1cccc2c1[nH]c(=O)[nH]2)CNC(C)(C)C 10.1021/jm400348g
5387 874 15 None 162 2 Human 7.9 pEC50 = 7.9 Functional
Partial agonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsPartial agonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 279 5 4 4 1.0 OC(COc1cccc2c1[nH]c(=O)[nH]2)CNC(C)(C)C 10.1021/jm400348g
CHEMBL420746 874 15 None 162 2 Human 7.9 pEC50 = 7.9 Functional
Partial agonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsPartial agonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 279 5 4 4 1.0 OC(COc1cccc2c1[nH]c(=O)[nH]2)CNC(C)(C)C 10.1021/jm400348g
44441226 93222 0 None 1 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 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 1 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 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
1239 1639 46 None -109 5 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta1 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 -109 5 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta1 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 -109 5 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta1 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 -109 5 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta1 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 -109 5 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta1 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
90645345 111974 0 None -11 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta1 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 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta1 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
56943485 111998 0 None -12 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta1 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 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta1 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
46832798 14073 0 None -31 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta-1 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 -31 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta-1 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 -31 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta-1 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
46832509 14082 0 None -50 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta-1 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 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta-1 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 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta-1 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
46832232 14085 0 None -100 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta-1 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 -100 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta-1 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 -100 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta-1 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
1239 1639 46 None -109 5 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant beta1 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta1 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 -109 5 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant beta1 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta1 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 -109 5 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant beta1 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta1 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 -109 5 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant beta1 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta1 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 -109 5 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant beta1 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta1 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
24895557 172520 0 None -575 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 469 12 3 5 5.2 CCCOc1cc(-c2ccc(OCCNC[C@H](O)c3cccc(Cl)c3)cc2)ccc1C(=O)O 10.1021/jm8000345
CHEMBL452033 172520 0 None -575 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 469 12 3 5 5.2 CCCOc1cc(-c2ccc(OCCNC[C@H](O)c3cccc(Cl)c3)cc2)ccc1C(=O)O 10.1021/jm8000345
44392490 64897 0 None -1 3 Human 6.9 pEC50 = 6.9 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-1 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-1 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 6.9 pEC50 = 6.9 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-1 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-1 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
44268327 97834 0 None -1 3 Human 5.9 pEC50 = 5.9 Functional
Compound was tested for agonist activity against cloned human beta-1 adrenergic receptorCompound was tested for agonist activity against cloned human beta-1 adrenergic receptor
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 -1 3 Human 5.9 pEC50 = 5.9 Functional
Compound was tested for agonist activity against cloned human beta-1 adrenergic receptorCompound was tested for agonist activity against cloned human beta-1 adrenergic receptor
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
10575455 99503 0 None -60 3 Human 5.9 pEC50 = 5.9 Functional
Increased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 1 Adrenergic receptorIncreased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 1 Adrenergic receptor
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 -60 3 Human 5.9 pEC50 = 5.9 Functional
Increased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 1 Adrenergic receptorIncreased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 1 Adrenergic receptor
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
11504295 2867 40 None -1047 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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 6.9 pEC50 = 6.9 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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 6.9 pEC50 = 6.9 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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 6.9 pEC50 = 6.9 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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 6.9 pEC50 = 6.9 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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
145982668 165350 0 None -15 3 Human 6.9 pEC50 = 6.9 Functional
Antagonist activity at human beta1 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 beta1 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 -15 3 Human 6.9 pEC50 = 6.9 Functional
Antagonist activity at human beta1 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 beta1 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
2419 3394 80 None -1621 6 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 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 -1621 6 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 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 -1621 6 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 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 -1621 6 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 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 -1621 6 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 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
53357711 64152 0 None -125 4 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta1 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 -125 4 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta1 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 -125 4 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta1 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
56675511 66061 0 None -100 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta1 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 -100 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta1 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 -100 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta1 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
42625587 12576 0 None -125 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta-1 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 6.9 pEC50 = 6.9 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta-1 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 6.9 pEC50 = 6.9 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta-1 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
9845280 76959 0 None -7 3 Human 5.9 pEC50 = 5.9 Functional
Activity at human beta-1 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-1 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 -7 3 Human 5.9 pEC50 = 5.9 Functional
Activity at human beta-1 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-1 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
23661589 92975 0 None -19952 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 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 -19952 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 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
42625741 12476 0 None -158 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta-1 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 5.9 pEC50 = 5.9 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta-1 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 5.9 pEC50 = 5.9 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta-1 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
42625898 184663 0 None -501 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta-1 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 -501 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta-1 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
145983711 164820 0 None -2691 3 Human 4.9 pEC50 = 4.9 Functional
Antagonist activity at human beta1 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 beta1 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 -2691 3 Human 4.9 pEC50 = 4.9 Functional
Antagonist activity at human beta1 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 beta1 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
24895265 186101 0 None -70 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 409 8 3 3 5.0 C[C@H](Cc1ccc(-c2ccc(C(=O)O)cc2)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm8000345
CHEMBL488430 186101 0 None -70 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 409 8 3 3 5.0 C[C@H](Cc1ccc(-c2ccc(C(=O)O)cc2)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm8000345
44392552 64180 0 None -23 3 Human 7.9 pEC50 = 7.9 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-1 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-1 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 -23 3 Human 7.9 pEC50 = 7.9 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-1 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-1 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
155564340 174841 0 None -263 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 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 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 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
44574826 178015 0 None 2 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 484 13 3 6 3.7 O=C(Cc1cn(Cc2ccccc2)cn1)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.03.044
CHEMBL467301 178015 0 None 2 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 484 13 3 6 3.7 O=C(Cc1cn(Cc2ccccc2)cn1)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.03.044
45270697 193490 0 None -20 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 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 6.9 pEC50 = 6.9 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 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 6.9 pEC50 = 6.9 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 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
44580039 186357 0 None -15 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 530 11 4 5 5.9 O=C(Nc1ccc(Oc2cccc(CCNC[C@H](O)c3cccc(Cl)c3)c2)cc1C(=O)O)c1ccccc1 10.1016/j.bmcl.2008.08.009
CHEMBL490222 186357 0 None -15 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 530 11 4 5 5.9 O=C(Nc1ccc(Oc2cccc(CCNC[C@H](O)c3cccc(Cl)c3)c2)cc1C(=O)O)c1ccccc1 10.1016/j.bmcl.2008.08.009
45271036 193548 0 None -2951 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassayAgonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassay
ChEMBL 526 11 4 7 3.8 CC(C)Oc1cc(-c2ccc(CCN[C@@H](C)[C@H](O)c3cccc(O)c3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1016/j.bmcl.2009.06.083
CHEMBL550871 193548 0 None -2951 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassayAgonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassay
ChEMBL 526 11 4 7 3.8 CC(C)Oc1cc(-c2ccc(CCN[C@@H](C)[C@H](O)c3cccc(O)c3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1016/j.bmcl.2009.06.083
24895363 173009 0 None -3162 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 447 11 3 4 5.3 CC(C)COc1cc(-c2ccc(C[C@@H](C)NC[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm8000345
CHEMBL453322 173009 0 None -3162 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 447 11 3 4 5.3 CC(C)COc1cc(-c2ccc(C[C@@H](C)NC[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm8000345
24895261 186072 0 None -676 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 435 10 4 6 3.7 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3ccc(N)nc3)cc2)ccc1C(=O)O 10.1021/jm8000345
CHEMBL488223 186072 0 None -676 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 435 10 4 6 3.7 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3ccc(N)nc3)cc2)ccc1C(=O)O 10.1021/jm8000345
42639967 12391 0 None -128 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 497 11 3 7 3.1 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3cccnc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
CHEMBL1186557 12391 0 None -128 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 497 11 3 7 3.1 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3cccnc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
CHEMBL469610 12391 0 None -128 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 497 11 3 7 3.1 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3cccnc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
44591506 178742 0 None -676 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 435 10 4 6 3.7 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3cnccc3N)cc2)ccc1C(=O)O 10.1021/jm9000709
CHEMBL473495 178742 0 None -676 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 435 10 4 6 3.7 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3cnccc3N)cc2)ccc1C(=O)O 10.1021/jm9000709
11152564 99540 0 None -4 2 Human 6.9 pEC50 = 6.9 Functional
Agonistic activity against human Beta-1 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonistic activity against human Beta-1 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
CHEMBL286818 99540 0 None -4 2 Human 6.9 pEC50 = 6.9 Functional
Agonistic activity against human Beta-1 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonistic activity against human Beta-1 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
44574651 177932 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 444 11 4 5 3.3 O=C(Cc1ccccn1)Nc1ccc(CCNC[C@H](O)COc2cccc3[nH]ccc23)cc1 10.1016/j.bmc.2009.03.044
CHEMBL466704 177932 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 444 11 4 5 3.3 O=C(Cc1ccccn1)Nc1ccc(CCNC[C@H](O)COc2cccc3[nH]ccc23)cc1 10.1016/j.bmc.2009.03.044
213051 92133 2 None -4 2 Human 7.9 pEC50 = 7.9 Functional
Agonistic activity against human Beta-1 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonistic activity against human Beta-1 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
CHEMBL24350 92133 2 None -4 2 Human 7.9 pEC50 = 7.9 Functional
Agonistic activity against human Beta-1 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonistic activity against human Beta-1 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
5581 101175 10 None -5 6 Human 7.9 pEC50 = 7.9 Functional
Compound was evaluated for its inhibitory activity against human Beta-1 adrenergic receptorCompound was evaluated for its inhibitory activity against human Beta-1 adrenergic receptor
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 -5 6 Human 7.9 pEC50 = 7.9 Functional
Compound was evaluated for its inhibitory activity against human Beta-1 adrenergic receptorCompound was evaluated for its inhibitory activity against human Beta-1 adrenergic receptor
ChEMBL 345 5 3 6 2.6 COc1cc(CC2NCCc3cc(O)c(O)cc32)cc(OC)c1OC 10.1016/s0960-894x(00)00459-5
164623433 187977 0 None -380 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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 7.8 pEC50 = 7.8 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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 7.8 pEC50 = 7.8 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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
9804536 165133 0 None -7 3 Human 7.8 pEC50 = 7.8 Functional
Antagonist activity at human beta1 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 beta1 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 -7 3 Human 7.8 pEC50 = 7.8 Functional
Antagonist activity at human beta1 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 beta1 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
44574825 178013 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 534 13 3 6 4.8 O=C(Cc1nc2ccccc2n1Cc1ccccc1)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.03.044
CHEMBL467298 178013 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 534 13 3 6 4.8 O=C(Cc1nc2ccccc2n1Cc1ccccc1)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.03.044
45273276 194001 0 None -2 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 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 6.9 pEC50 = 6.9 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 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 6.9 pEC50 = 6.9 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 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
44579966 192008 0 None -15 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 429 9 3 4 4.8 O=C(O)c1cc(Oc2cccc(CCNC[C@H](O)c3cccc(Cl)c3)c2)ccc1F 10.1016/j.bmcl.2008.08.009
CHEMBL521611 192008 0 None -15 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 429 9 3 4 4.8 O=C(O)c1cc(Oc2cccc(CCNC[C@H](O)c3cccc(Cl)c3)c2)ccc1F 10.1016/j.bmcl.2008.08.009
24949572 176442 0 None -34 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 438 7 3 5 4.4 O=C(O)c1cccc(Oc2ccc3c(c2)C[C@@H](NC[C@H](O)c2ccc(Cl)nc2)CC3)c1 10.1021/jm800222k
CHEMBL463182 176442 0 None -34 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 438 7 3 5 4.4 O=C(O)c1cccc(Oc2ccc3c(c2)C[C@@H](NC[C@H](O)c2ccc(Cl)nc2)CC3)c1 10.1021/jm800222k
44565931 12324 0 None -4677 4 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 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 -4677 4 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 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 -4677 4 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 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
11381882 98832 0 None 2 2 Human 6.9 pEC50 = 6.9 Functional
Agonistic activity against human Beta-1 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonistic activity against human Beta-1 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
CHEMBL282039 98832 0 None 2 2 Human 6.9 pEC50 = 6.9 Functional
Agonistic activity against human Beta-1 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonistic activity against human Beta-1 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
155515718 169385 0 None -2884 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 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 5.8 pEC50 = 5.8 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 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
24894317 173118 0 None -22 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 467 11 3 4 5.6 CC(C)Cc1cc(-c2ccc(OCCNC[C@H](O)c3cccc(Cl)c3)cc2)ccc1C(=O)O 10.1021/jm8000345
CHEMBL453575 173118 0 None -22 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 467 11 3 4 5.6 CC(C)Cc1cc(-c2ccc(OCCNC[C@H](O)c3cccc(Cl)c3)cc2)ccc1C(=O)O 10.1021/jm8000345
44392228 64516 0 None -7 2 Human 7.8 pEC50 = 7.8 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptor
ChEMBL 441 11 5 5 3.1 O=C(Nc1ccc(C[C@@H](CO)NC[C@H](O)COc2ccccc2)cc1)NC1CCCCC1 10.1016/j.bmcl.2004.11.001
CHEMBL182127 64516 0 None -7 2 Human 7.8 pEC50 = 7.8 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptor
ChEMBL 441 11 5 5 3.1 O=C(Nc1ccc(C[C@@H](CO)NC[C@H](O)COc2ccccc2)cc1)NC1CCCCC1 10.1016/j.bmcl.2004.11.001
1028 287 69 None -3 16 Guinea pig 7.8 pEC50 = 7.8 Functional
Effective dose required to stimulate contractions in isolated guinea pig atrium.Effective dose required to stimulate contractions in isolated guinea pig atrium.
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00019a001
139148732 287 69 None -3 16 Guinea pig 7.8 pEC50 = 7.8 Functional
Effective dose required to stimulate contractions in isolated guinea pig atrium.Effective dose required to stimulate contractions in isolated guinea pig atrium.
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00019a001
479 287 69 None -3 16 Guinea pig 7.8 pEC50 = 7.8 Functional
Effective dose required to stimulate contractions in isolated guinea pig atrium.Effective dose required to stimulate contractions in isolated guinea pig atrium.
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00019a001
5816 287 69 None -3 16 Guinea pig 7.8 pEC50 = 7.8 Functional
Effective dose required to stimulate contractions in isolated guinea pig atrium.Effective dose required to stimulate contractions in isolated guinea pig atrium.
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00019a001
CHEMBL679 287 69 None -3 16 Guinea pig 7.8 pEC50 = 7.8 Functional
Effective dose required to stimulate contractions in isolated guinea pig atrium.Effective dose required to stimulate contractions in isolated guinea pig atrium.
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00019a001
DB00668 287 69 None -3 16 Guinea pig 7.8 pEC50 = 7.8 Functional
Effective dose required to stimulate contractions in isolated guinea pig atrium.Effective dose required to stimulate contractions in isolated guinea pig atrium.
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00019a001
155524038 170314 0 None -120 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 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 7.8 pEC50 = 7.8 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 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
155550544 173727 0 None -1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 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 7.8 pEC50 = 7.8 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 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
44126933 194481 0 None 1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 470 11 4 5 4.3 O=C(Cc1ccc2ccccc2c1)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/j.ejmech.2009.01.022
CHEMBL561291 194481 0 None 1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 470 11 4 5 4.3 O=C(Cc1ccc2ccccc2c1)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/j.ejmech.2009.01.022
45268516 194559 0 None -588 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassayAgonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassay
ChEMBL 605 13 5 9 2.8 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1016/j.bmcl.2009.06.083
CHEMBL561743 194559 0 None -588 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassayAgonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassay
ChEMBL 605 13 5 9 2.8 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1016/j.bmcl.2009.06.083
16222940 185882 0 None -2290 4 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 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 -2290 4 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 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
24895259 188697 0 None -588 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 528 12 5 7 3.8 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)cc2)ccc1C(=O)O 10.1021/jm8000345
CHEMBL512147 188697 0 None -588 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 528 12 5 7 3.8 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)cc2)ccc1C(=O)O 10.1021/jm8000345
44591507 178769 0 None -2290 4 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 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 -2290 4 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 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
9842600 187523 0 None -38 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 375 7 3 4 3.0 O=C(O)COc1ccc2c(c1)C[C@@H](NC[C@H](O)c1cccc(Cl)c1)CC2 10.1021/jm800222k
CHEMBL498305 187523 0 None -38 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 375 7 3 4 3.0 O=C(O)COc1ccc2c(c1)C[C@@H](NC[C@H](O)c1cccc(Cl)c1)CC2 10.1021/jm800222k
44377535 55115 0 None -117 2 Human 5.8 pEC50 = 5.8 Functional
Agonistic activity as cAMP accumulation in CHO cells expressing human beta-1-adrenergic receptorAgonistic activity as cAMP accumulation in CHO cells expressing human beta-1-adrenergic receptor
ChEMBL 508 8 4 9 2.8 O=C1NC(=O)C(Cc2ccc(N3CCC(NC[C@H](O)Oc4cccc5nc(O)ccc45)CC3)cc2)S1 10.1016/s0960-894x(01)00063-4
CHEMBL161949 55115 0 None -117 2 Human 5.8 pEC50 = 5.8 Functional
Agonistic activity as cAMP accumulation in CHO cells expressing human beta-1-adrenergic receptorAgonistic activity as cAMP accumulation in CHO cells expressing human beta-1-adrenergic receptor
ChEMBL 508 8 4 9 2.8 O=C1NC(=O)C(Cc2ccc(N3CCC(NC[C@H](O)Oc4cccc5nc(O)ccc45)CC3)cc2)S1 10.1016/s0960-894x(01)00063-4
56673609 63757 0 None -112 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at adrenergic beta1 receptorAgonist activity at adrenergic beta1 receptor
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 6.8 pEC50 = 6.8 Functional
Agonist activity at adrenergic beta1 receptorAgonist activity at adrenergic beta1 receptor
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
56672116 66018 0 None -630 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta1 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 -630 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta1 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 -630 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta1 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
44441227 147505 0 None -10 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 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 -10 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 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
145981079 166118 0 None -39 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 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 5.8 pEC50 = 5.8 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 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
164626310 188000 0 None -346 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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 7.8 pEC50 = 7.8 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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 7.8 pEC50 = 7.8 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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
164614249 187900 0 None -295 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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 7.8 pEC50 = 7.8 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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 7.8 pEC50 = 7.8 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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
24949889 187562 0 None -35 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 451 7 3 4 5.4 O=C(O)c1cccc(Oc2ccc3c(c2)C[C@@H](NC[C@H](O)c2cccc(Cl)c2)CCC3)c1 10.1021/jm800222k
CHEMBL498531 187562 0 None -35 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 451 7 3 4 5.4 O=C(O)c1cccc(Oc2ccc3c(c2)C[C@@H](NC[C@H](O)c2cccc(Cl)c2)CCC3)c1 10.1021/jm800222k
42639311 12403 0 None -56 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 524 14 3 6 4.5 CCCCCOc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
CHEMBL1186600 12403 0 None -56 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 524 14 3 6 4.5 CCCCCOc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
CHEMBL472089 12403 0 None -56 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 524 14 3 6 4.5 CCCCCOc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
44392558 64909 0 None -2 3 Human 6.8 pEC50 = 6.8 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-1 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-1 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 6.8 pEC50 = 6.8 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-1 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-1 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
44237669 57912 0 None -7943 2 Rat 5.8 pEC50 = 5.8 Functional
Agonist activity at beta1 adrenoceptor in rat left atria assessed as induction of ionotropic effectAgonist activity at beta1 adrenoceptor in rat left atria assessed as induction of ionotropic effect
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 Rat 5.8 pEC50 = 5.8 Functional
Agonist activity at beta1 adrenoceptor in rat left atria assessed as induction of ionotropic effectAgonist activity at beta1 adrenoceptor in rat left atria assessed as induction of ionotropic effect
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
9933039 162483 0 None -6 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
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 -6 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
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
9933039 162483 0 None -6 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 442 11 4 6 2.8 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1)c1ccccc1 10.1016/j.ejmech.2009.01.022
CHEMBL417613 162483 0 None -6 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 442 11 4 6 2.8 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1)c1ccccc1 10.1016/j.ejmech.2009.01.022
44309523 101706 0 None -52 3 Human 5.8 pEC50 = 5.8 Functional
Agonistic activity against cloned human beta1-AR (beta-1-adrenergic receptor) in CHO cellsAgonistic activity against cloned human beta1-AR (beta-1-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 -52 3 Human 5.8 pEC50 = 5.8 Functional
Agonistic activity against cloned human beta1-AR (beta-1-adrenergic receptor) in CHO cellsAgonistic activity against cloned human beta1-AR (beta-1-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
10601234 111502 0 None -23 3 Human 5.8 pEC50 = 5.8 Functional
Increased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 1 Adrenergic receptorIncreased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 1 Adrenergic receptor
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 -23 3 Human 5.8 pEC50 = 5.8 Functional
Increased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 1 Adrenergic receptorIncreased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 1 Adrenergic receptor
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
10140889 5974 0 None -4 2 Human 6.8 pEC50 = 6.8 Functional
In vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta1-AR receptorIn vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta1-AR receptor
ChEMBL 484 12 4 6 3.3 CCN(CC)C(=O)N1CCC(Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)CC1 10.1016/s0960-894x(01)00645-x
CHEMBL108061 5974 0 None -4 2 Human 6.8 pEC50 = 6.8 Functional
In vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta1-AR receptorIn vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta1-AR receptor
ChEMBL 484 12 4 6 3.3 CCN(CC)C(=O)N1CCC(Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)CC1 10.1016/s0960-894x(01)00645-x
44574978 188691 0 None -1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 524 12 2 6 4.0 O=C(Cc1nccn1Cc1ccccc1)N1CCCc2cc(CCNC[C@H](O)COc3ccccc3)ccc21 10.1016/j.bmc.2009.03.044
CHEMBL512099 188691 0 None -1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 524 12 2 6 4.0 O=C(Cc1nccn1Cc1ccccc1)N1CCCc2cc(CCNC[C@H](O)COc3ccccc3)ccc21 10.1016/j.bmc.2009.03.044
24823464 97156 0 None -588 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 418 10 4 4 4.7 CC(C)Nc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm701324c
CHEMBL270964 97156 0 None -588 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 418 10 4 4 4.7 CC(C)Nc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm701324c
24823464 97156 0 None -588 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 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 -588 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 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
44392457 165393 0 None -34 3 Human 6.8 pEC50 = 6.8 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-1 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-1 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 6.8 pEC50 = 6.8 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-1 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-1 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
44127677 193724 0 None -2 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 471 11 4 6 3.7 O=C(Cc1ccc2ccccc2n1)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/j.ejmech.2009.01.022
CHEMBL552089 193724 0 None -2 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 471 11 4 6 3.7 O=C(Cc1ccc2ccccc2n1)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/j.ejmech.2009.01.022
567 715 10 None -676 7 Human 5.8 pEC50 = 5.8 Functional
Agonistic activity against human Beta-1 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonistic activity against human Beta-1 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 -676 7 Human 5.8 pEC50 = 5.8 Functional
Agonistic activity against human Beta-1 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonistic activity against human Beta-1 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 -676 7 Human 5.8 pEC50 = 5.8 Functional
Agonistic activity against human Beta-1 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonistic activity against human Beta-1 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
11703823 199460 0 None -131 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta-1 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 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta-1 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
24950234 175414 0 None -223 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 494 10 4 5 5.8 CCCNc1cc(Oc2ccc3c(c2)C[C@@H](NC[C@H](O)c2cccc(Cl)c2)CC3)cc(C(=O)O)c1 10.1021/jm800222k
CHEMBL458923 175414 0 None -223 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 494 10 4 5 5.8 CCCNc1cc(Oc2ccc3c(c2)C[C@@H](NC[C@H](O)c2cccc(Cl)c2)CC3)cc(C(=O)O)c1 10.1021/jm800222k
131487 4897 12 None - 1 Guinea pig 6.8 pEC50 = 6.8 Functional
Agonistic activity (beta-1 adrenergic receptor) for the percent maximal increase in contraction rate of isolated guinea pig atriaAgonistic activity (beta-1 adrenergic receptor) for the percent maximal increase in contraction rate of isolated guinea pig atria
ChEMBL 273 5 4 5 1.4 CC(C)(C)NCC(O)COc1cc(O)c(O)cc1F 10.1021/jm00107a027
CHEMBL10494 4897 12 None - 1 Guinea pig 6.8 pEC50 = 6.8 Functional
Agonistic activity (beta-1 adrenergic receptor) for the percent maximal increase in contraction rate of isolated guinea pig atriaAgonistic activity (beta-1 adrenergic receptor) for the percent maximal increase in contraction rate of isolated guinea pig atria
ChEMBL 273 5 4 5 1.4 CC(C)(C)NCC(O)COc1cc(O)c(O)cc1F 10.1021/jm00107a027
24822648 97145 0 None -28 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 425 9 3 4 4.6 COc1cc(C(=O)O)ccc1-c1ccc(CCNC[C@H](O)c2cccc(Cl)c2)cc1 10.1021/jm701324c
CHEMBL270889 97145 0 None -28 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 425 9 3 4 4.6 COc1cc(C(=O)O)ccc1-c1ccc(CCNC[C@H](O)c2cccc(Cl)c2)cc1 10.1021/jm701324c
45484558 195149 0 None -4 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human beta-1 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta-1 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 7.8 pEC50 = 7.8 Functional
Agonist activity at human beta-1 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta-1 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
44574687 177936 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 406 11 3 6 2.2 O=C(Cc1ccccn1)Nc1ccc(CCNC[C@H](O)COc2cccnc2)cc1 10.1016/j.bmc.2009.03.044
CHEMBL466713 177936 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 406 11 3 6 2.2 O=C(Cc1ccccn1)Nc1ccc(CCNC[C@H](O)COc2cccnc2)cc1 10.1016/j.bmc.2009.03.044
44219629 177984 0 None -1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 484 13 3 6 3.7 O=C(Cc1nccn1Cc1ccccc1)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.03.044
CHEMBL467083 177984 0 None -1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 484 13 3 6 3.7 O=C(Cc1nccn1Cc1ccccc1)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.03.044
44126931 193674 0 None -1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 496 12 4 5 4.7 O=C(Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1)C(c1ccccc1)c1ccccc1 10.1016/j.ejmech.2009.01.022
CHEMBL551831 193674 0 None -1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 496 12 4 5 4.7 O=C(Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1)C(c1ccccc1)c1ccccc1 10.1016/j.ejmech.2009.01.022
24895664 176112 0 None -251 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 467 12 3 4 5.8 CCCOc1cc(-c2ccc(CCCNC[C@H](O)c3cccc(Cl)c3)cc2)ccc1C(=O)O 10.1021/jm8000345
CHEMBL459863 176112 0 None -251 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 467 12 3 4 5.8 CCCOc1cc(-c2ccc(CCCNC[C@H](O)c3cccc(Cl)c3)cc2)ccc1C(=O)O 10.1021/jm8000345
44396568 66934 0 None -34 3 Human 6.8 pEC50 = 6.8 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-1 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-1 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 6.8 pEC50 = 6.8 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-1 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-1 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
9853471 203136 0 None -389 3 Human 5.8 pEC50 = 5.8 Functional
Compound was evaluated for its inhibitory activity against human beta-1 adrenergic receptor (AR)Compound was evaluated for its inhibitory activity against human beta-1 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 -389 3 Human 5.8 pEC50 = 5.8 Functional
Compound was evaluated for its inhibitory activity against human beta-1 adrenergic receptor (AR)Compound was evaluated for its inhibitory activity against human beta-1 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
44331425 4364 0 None -186 3 Human 5.7 pEC50 = 5.7 Functional
Beta-1 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-1-adrenoceptorBeta-1 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-1-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 -186 3 Human 5.7 pEC50 = 5.7 Functional
Beta-1 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-1-adrenoceptorBeta-1 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-1-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
45483838 195247 0 None -14 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human adrenergic beta 1 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 1 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 5.7 pEC50 = 5.7 Functional
Agonist activity at human adrenergic beta 1 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 1 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
10302342 109285 0 None -3 2 Human 6.7 pEC50 = 6.7 Functional
In vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta1-AR receptorIn vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta1-AR receptor
ChEMBL 538 14 5 6 4.5 O=C(NCCCC1CCCC1)N1CCC(Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)CC1 10.1016/s0960-894x(01)00645-x
CHEMBL323258 109285 0 None -3 2 Human 6.7 pEC50 = 6.7 Functional
In vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta1-AR receptorIn vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta1-AR receptor
ChEMBL 538 14 5 6 4.5 O=C(NCCCC1CCCC1)N1CCC(Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)CC1 10.1016/s0960-894x(01)00645-x
44396488 66383 0 None -14 3 Human 7.7 pEC50 = 7.7 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-1 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-1 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 -14 3 Human 7.7 pEC50 = 7.7 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-1 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-1 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
9831168 202986 0 None -2 3 Human 7.7 pEC50 = 7.7 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 -2 3 Human 7.7 pEC50 = 7.7 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
11005613 119281 0 None -1 3 Human 7.7 pEC50 = 7.7 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-1 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-1 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 7.7 pEC50 = 7.7 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-1 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-1 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
44441234 93343 0 None -63 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 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 -63 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 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
44441228 167198 0 None -3 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 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 -3 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 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
46832507 14084 0 None -12 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta-1 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 7.7 pEC50 = 7.7 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta-1 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 7.7 pEC50 = 7.7 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta-1 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
10203169 14109 0 None -25 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta-1 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 7.7 pEC50 = 7.7 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta-1 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 7.7 pEC50 = 7.7 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta-1 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
44574867 177988 0 None -2 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 562 13 3 6 4.4 O=C(Cc1nccn1Cc1ccc(Br)cc1)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.03.044
CHEMBL467102 177988 0 None -2 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 562 13 3 6 4.4 O=C(Cc1nccn1Cc1ccc(Br)cc1)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.03.044
44579650 186562 0 None -15 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 435 10 4 6 3.4 CC(=O)Nc1ccc(Oc2cccc(CCNC[C@H](O)c3cccnc3)c2)cc1C(=O)O 10.1016/j.bmcl.2008.08.009
CHEMBL492005 186562 0 None -15 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 435 10 4 6 3.4 CC(=O)Nc1ccc(Oc2cccc(CCNC[C@H](O)c3cccnc3)c2)cc1C(=O)O 10.1016/j.bmcl.2008.08.009
44580041 192695 0 None -9 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 530 11 4 5 5.9 O=C(O)c1cc(NC(=O)c2ccccc2)cc(Oc2cccc(CCNC[C@H](O)c3cccc(Cl)c3)c2)c1 10.1016/j.bmcl.2008.08.009
CHEMBL524145 192695 0 None -9 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 530 11 4 5 5.9 O=C(O)c1cc(NC(=O)c2ccccc2)cc(Oc2cccc(CCNC[C@H](O)c3cccc(Cl)c3)c2)c1 10.1016/j.bmcl.2008.08.009
44127480 194872 0 None 6 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 454 11 4 5 3.8 O=C(Cc1ccc(Cl)cc1)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/j.ejmech.2009.01.022
CHEMBL563810 194872 0 None 6 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 454 11 4 5 3.8 O=C(Cc1ccc(Cl)cc1)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/j.ejmech.2009.01.022
44560793 188300 0 None -2951 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 434 11 3 5 4.5 CCCOc1cc(-c2ccc(C[C@@H](C)NC[C@H](O)c3cccnc3)cc2)ccc1C(=O)O 10.1021/jm8000345
CHEMBL507506 188300 0 None -2951 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 434 11 3 5 4.5 CCCOc1cc(-c2ccc(C[C@@H](C)NC[C@H](O)c3cccnc3)cc2)ccc1C(=O)O 10.1021/jm8000345
9873257 84507 12 None -74 3 Human 5.7 pEC50 = 5.7 Functional
Agonistic activity against the cloned human Beta-1 adrenergic receptor was measured by its by its ability to stimulate adenylyl cyclaseAgonistic activity against the cloned human Beta-1 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 -74 3 Human 5.7 pEC50 = 5.7 Functional
Agonistic activity against the cloned human Beta-1 adrenergic receptor was measured by its by its ability to stimulate adenylyl cyclaseAgonistic activity against the cloned human Beta-1 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
155527926 170677 0 None -8709 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 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 5.7 pEC50 = 5.7 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 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
164612026 184777 0 None -776 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human beta1 adrenoceptor expressed in HEK293 cells assessed as increase in cAMP accumulation measured after 60 mins by HTRF assayAgonist activity at human beta1 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 6.7 pEC50 = 6.7 Functional
Agonist activity at human beta1 adrenoceptor expressed in HEK293 cells assessed as increase in cAMP accumulation measured after 60 mins by HTRF assayAgonist activity at human beta1 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
56670092 63758 0 None -112 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at adrenergic beta1 receptorAgonist activity at adrenergic beta1 receptor
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 6.7 pEC50 = 6.7 Functional
Agonist activity at adrenergic beta1 receptorAgonist activity at adrenergic beta1 receptor
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
56675509 64150 0 None -79 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta1 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 6.7 pEC50 = 6.7 Functional
Agonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta1 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
53357712 66059 0 None -251 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta1 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 -251 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta1 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 -251 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta1 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
56658244 66060 0 None -79 4 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta1 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 -79 4 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta1 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 -79 4 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta1 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
9958539 102618 0 None -5 3 Human 8.7 pEC50 = 8.7 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 8.7 pEC50 = 8.7 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
164615222 187912 0 None -91 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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 8.7 pEC50 = 8.7 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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 8.7 pEC50 = 8.7 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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
164615492 187915 0 None -120 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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 8.7 pEC50 = 8.7 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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 8.7 pEC50 = 8.7 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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
443372 10123 23 None 1 8 Guinea pig 8.7 pEC50 = 8.7 Functional
Activity for Beta-1 adrenergic receptor was assessed from ability to stimulate contractions in isolated guinea pig atrium.Activity for Beta-1 adrenergic receptor was assessed from ability to stimulate contractions in isolated guinea pig atrium.
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 8.7 pEC50 = 8.7 Functional
Activity for Beta-1 adrenergic receptor was assessed from ability to stimulate contractions in isolated guinea pig atrium.Activity for Beta-1 adrenergic receptor was assessed from ability to stimulate contractions in isolated guinea pig atrium.
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 8.7 pEC50 = 8.7 Functional
Activity for Beta-1 adrenergic receptor was assessed from ability to stimulate contractions in isolated guinea pig atrium.Activity for Beta-1 adrenergic receptor was assessed from ability to stimulate contractions in isolated guinea pig atrium.
ChEMBL 211 4 4 4 1.1 CC(C)NC[C@H](O)c1ccc(O)c(O)c1 10.1021/jm00019a001
44392215 65256 0 None 1 2 Human 8.7 pEC50 = 8.7 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptor
ChEMBL 465 12 5 6 3.3 COc1ccc(NC(=O)Nc2ccc(C[C@@H](CO)NC[C@H](O)COc3ccccc3)cc2)cc1 10.1016/j.bmcl.2004.11.001
CHEMBL183307 65256 0 None 1 2 Human 8.7 pEC50 = 8.7 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptor
ChEMBL 465 12 5 6 3.3 COc1ccc(NC(=O)Nc2ccc(C[C@@H](CO)NC[C@H](O)COc3ccccc3)cc2)cc1 10.1016/j.bmcl.2004.11.001
5311116 2293 6 None 4365 3 Human 8.6 pEC50 = 8.6 Functional
Partial agonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsPartial agonist activity at human beta1 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 8.6 pEC50 = 8.6 Functional
Partial agonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsPartial agonist activity at human beta1 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 8.6 pEC50 = 8.6 Functional
Partial agonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsPartial agonist activity at human beta1 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
56598832 87826 0 None 4365 3 Human 8.6 pEC50 = 8.6 Functional
Partial agonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsPartial agonist activity at human beta1 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 8.6 pEC50 = 8.6 Functional
Partial agonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsPartial agonist activity at human beta1 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
164617772 187929 0 None -173 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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 8.6 pEC50 = 8.6 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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 8.6 pEC50 = 8.6 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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
164611794 187881 0 None -131 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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 8.6 pEC50 = 8.6 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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 8.6 pEC50 = 8.6 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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
10289065 12423 0 None - 1 Guinea pig 8.6 pEC50 = 8.6 Functional
Agonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contractionAgonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contraction
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1cccc(CCCOCCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
CHEMBL1186683 12423 0 None - 1 Guinea pig 8.6 pEC50 = 8.6 Functional
Agonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contractionAgonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contraction
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1cccc(CCCOCCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
CHEMBL474616 12423 0 None - 1 Guinea pig 8.6 pEC50 = 8.6 Functional
Agonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contractionAgonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contraction
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1cccc(CCCOCCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
42625511 12613 0 None -3 4 Guinea pig 8.6 pEC50 = 8.6 Functional
Agonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contractionAgonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contraction
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 Guinea pig 8.6 pEC50 = 8.6 Functional
Agonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contractionAgonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contraction
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 Guinea pig 8.6 pEC50 = 8.6 Functional
Agonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contractionAgonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contraction
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1ccccc1CCCCOCCCCCCNC[C@H](O)c1ccc(O)c(CO)c1 10.1021/jm801016j
90645344 111951 0 None -7 3 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta1 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 8.6 pEC50 = 8.6 Functional
Agonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta1 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
10239722 111953 0 None -11 3 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta1 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 8.6 pEC50 = 8.6 Functional
Agonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta1 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
164621302 187956 0 None -120 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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 8.6 pEC50 = 8.6 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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 8.6 pEC50 = 8.6 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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
164610792 187874 0 None -134 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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 8.6 pEC50 = 8.6 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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 8.6 pEC50 = 8.6 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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
145984584 165323 0 None -5 3 Human 8.5 pEC50 = 8.5 Functional
Antagonist activity at human beta1 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 beta1 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 -5 3 Human 8.5 pEC50 = 8.5 Functional
Antagonist activity at human beta1 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 beta1 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
24822643 157100 0 None -4 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 413 8 3 3 4.7 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)c(F)c1 10.1021/jm701324c
CHEMBL408145 157100 0 None -4 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 413 8 3 3 4.7 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)c(F)c1 10.1021/jm701324c
44392212 167794 0 None 12 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 405 10 4 4 3.9 O=C(Nc1ccccc1)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.06.031
CHEMBL1204383 167794 0 None 12 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 405 10 4 4 3.9 O=C(Nc1ccccc1)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.06.031
CHEMBL434524 167794 0 None 12 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 405 10 4 4 3.9 O=C(Nc1ccccc1)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.06.031
45271492 193554 0 None 16 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 390 10 3 4 3.5 O=C(Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1)c1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL1203997 193554 0 None 16 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 390 10 3 4 3.5 O=C(Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1)c1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL550906 193554 0 None 16 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 390 10 3 4 3.5 O=C(Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1)c1ccccc1 10.1016/j.bmc.2009.06.031
10113837 65223 0 None -39 2 Human 7.7 pEC50 = 7.7 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptor
ChEMBL 435 11 5 5 3.3 O=C(Nc1ccccc1)Nc1ccc(C[C@@H](CO)NC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmcl.2004.11.001
CHEMBL183129 65223 0 None -39 2 Human 7.7 pEC50 = 7.7 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptor
ChEMBL 435 11 5 5 3.3 O=C(Nc1ccccc1)Nc1ccc(C[C@@H](CO)NC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmcl.2004.11.001
44396531 66486 0 None -38 3 Human 7.7 pEC50 = 7.7 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-1 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-1 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 7.7 pEC50 = 7.7 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-1 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-1 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
24822469 97315 0 None -26 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 401 8 3 4 4.6 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)s1 10.1021/jm701324c
CHEMBL271765 97315 0 None -26 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 401 8 3 4 4.6 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)s1 10.1021/jm701324c
24950568 189163 0 None -234 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 422 6 3 4 4.3 O=C(O)c1ccc(-c2ccc3c(c2)C[C@@H](NC[C@H](O)c2ccc(Cl)nc2)CC3)cc1 10.1021/jm800222k
CHEMBL516002 189163 0 None -234 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 422 6 3 4 4.3 O=C(O)c1ccc(-c2ccc3c(c2)C[C@@H](NC[C@H](O)c2ccc(Cl)nc2)CC3)cc1 10.1021/jm800222k
11625493 199018 0 None -12 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta-1 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 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta-1 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
44565908 186531 0 None -1513 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 512 11 4 8 2.7 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3cnccc3N)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
CHEMBL491726 186531 0 None -1513 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 512 11 4 8 2.7 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3cnccc3N)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
10139127 57172 0 None -50 2 Human 5.7 pEC50 = 5.7 Functional
Agonistic activity as cAMP accumulation in CHO cells expressing human beta-1-adrenergic receptorAgonistic activity as cAMP accumulation in CHO cells expressing human beta-1-adrenergic receptor
ChEMBL 455 9 3 7 2.6 O=C1NC(=O)C(Cc2ccc(N3CCC(NC[C@H](O)COc4ccccc4)CC3)cc2)S1 10.1016/s0960-894x(01)00063-4
CHEMBL165893 57172 0 None -50 2 Human 5.7 pEC50 = 5.7 Functional
Agonistic activity as cAMP accumulation in CHO cells expressing human beta-1-adrenergic receptorAgonistic activity as cAMP accumulation in CHO cells expressing human beta-1-adrenergic receptor
ChEMBL 455 9 3 7 2.6 O=C1NC(=O)C(Cc2ccc(N3CCC(NC[C@H](O)COc4ccccc4)CC3)cc2)S1 10.1016/s0960-894x(01)00063-4
44589133 175261 0 None -2 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at adrenergic beta-1 receptorAgonist activity at adrenergic beta-1 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 -2 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at adrenergic beta-1 receptorAgonist activity at adrenergic beta-1 receptor
ChEMBL 354 8 2 4 3.4 CC(C)NCC(O)COc1ccc2c(c1)CCCN2Cc1ccccc1 10.1016/j.bmc.2008.11.030
10145446 4104 0 None -102 2 Human 5.7 pEC50 = 5.7 Functional
In vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-1 adrenergic receptorIn vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-1 adrenergic receptor
ChEMBL 602 14 5 8 3.6 O=C(NCCCc1cccs1)Nc1ccc(S(=O)(=O)N2CCC(CNC[C@H](O)COc3ccc(O)cc3)CC2)cc1 10.1016/s0960-894x(02)00607-8
CHEMBL100124 4104 0 None -102 2 Human 5.7 pEC50 = 5.7 Functional
In vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-1 adrenergic receptorIn vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-1 adrenergic receptor
ChEMBL 602 14 5 8 3.6 O=C(NCCCc1cccs1)Nc1ccc(S(=O)(=O)N2CCC(CNC[C@H](O)COc3ccc(O)cc3)CC2)cc1 10.1016/s0960-894x(02)00607-8
46232816 199259 0 None -3 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta-1 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 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta-1 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
11632691 199847 0 None -3 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta-1 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 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta-1 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
44377523 55923 0 None 1 2 Human 7.7 pEC50 = 7.7 Functional
Agonistic activity as cAMP accumulation in CHO cells expressing human beta-1-adrenergic receptorAgonistic activity as cAMP accumulation in CHO cells expressing human beta-1-adrenergic receptor
ChEMBL 509 9 3 8 1.0 O=C1N=c2cccc(OC[C@@H](O)CNC3CCN(c4ccc(CC5SC(=O)NC5=O)cc4)CC3)c2=N1 10.1016/s0960-894x(01)00063-4
CHEMBL162711 55923 0 None 1 2 Human 7.7 pEC50 = 7.7 Functional
Agonistic activity as cAMP accumulation in CHO cells expressing human beta-1-adrenergic receptorAgonistic activity as cAMP accumulation in CHO cells expressing human beta-1-adrenergic receptor
ChEMBL 509 9 3 8 1.0 O=C1N=c2cccc(OC[C@@H](O)CNC3CCN(c4ccc(CC5SC(=O)NC5=O)cc4)CC3)c2=N1 10.1016/s0960-894x(01)00063-4
9933039 162483 0 None -6 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 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 -6 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 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
24895563 176154 0 None -173 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 435 12 3 5 4.5 CCCOc1cc(-c2ccc(OCCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm8000345
CHEMBL460256 176154 0 None -173 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 435 12 3 5 4.5 CCCOc1cc(-c2ccc(OCCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm8000345
11668125 199316 0 None -4 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta-1 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 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta-1 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
155536314 171599 0 None -6025 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 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 6.7 pEC50 = 6.7 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 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
24895789 188270 0 None -72 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 375 8 3 3 4.3 C[C@H](Cc1ccc(-c2ccc(C(=O)O)cc2)cc1)NC[C@H](O)c1ccccc1 10.1021/jm8000345
CHEMBL507003 188270 0 None -72 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 375 8 3 3 4.3 C[C@H](Cc1ccc(-c2ccc(C(=O)O)cc2)cc1)NC[C@H](O)c1ccccc1 10.1021/jm8000345
44396715 67097 0 None -20 3 Human 7.7 pEC50 = 7.7 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-1 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-1 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 7.7 pEC50 = 7.7 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-1 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-1 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
155551006 173363 0 None -44 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 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 7.7 pEC50 = 7.7 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 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
164620585 187950 0 None -616 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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 7.7 pEC50 = 7.7 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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 7.7 pEC50 = 7.7 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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
56598833 87825 0 None 436 3 Human 7.6 pEC50 = 7.6 Functional
Partial agonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsPartial agonist activity at human beta1 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 7.6 pEC50 = 7.6 Functional
Partial agonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsPartial agonist activity at human beta1 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
42639314 12448 0 None -575 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 550 11 3 6 5.0 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)cc1OC1CCCCCC1 10.1021/jm9000709
CHEMBL1186804 12448 0 None -575 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 550 11 3 6 5.0 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)cc1OC1CCCCCC1 10.1021/jm9000709
CHEMBL479341 12448 0 None -575 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 550 11 3 6 5.0 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)cc1OC1CCCCCC1 10.1021/jm9000709
5808 176196 20 None -5 5 Guinea pig 5.7 pEC50 = 5.7 Functional
Activity for Beta-1 adrenergic receptor was assessed from ability to stimulate contractions in isolated guinea pig atrium.Activity for Beta-1 adrenergic receptor was assessed from ability to stimulate contractions in isolated guinea pig atrium.
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 -5 5 Guinea pig 5.7 pEC50 = 5.7 Functional
Activity for Beta-1 adrenergic receptor was assessed from ability to stimulate contractions in isolated guinea pig atrium.Activity for Beta-1 adrenergic receptor was assessed from ability to stimulate contractions in isolated guinea pig atrium.
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 -5 5 Guinea pig 5.7 pEC50 = 5.7 Functional
Activity for Beta-1 adrenergic receptor was assessed from ability to stimulate contractions in isolated guinea pig atrium.Activity for Beta-1 adrenergic receptor was assessed from ability to stimulate contractions in isolated guinea pig atrium.
ChEMBL 211 4 4 4 1.1 CC(C)NC[C@@H](O)c1ccc(O)c(O)c1 10.1021/jm00019a001
145983266 164965 0 None -66 3 Human 6.7 pEC50 = 6.7 Functional
Antagonist activity at human beta1 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 beta1 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 -66 3 Human 6.7 pEC50 = 6.7 Functional
Antagonist activity at human beta1 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 beta1 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
319 1292 39 None -2290 6 Rat 5.6 pEC50 = 5.6 Functional
Agonist activity at beta1 adrenoceptor in rat left atria assessed as induction of ionotropic effectAgonist activity at beta1 adrenoceptor in rat left atria assessed as induction of ionotropic effect
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 -2290 6 Rat 5.6 pEC50 = 5.6 Functional
Agonist activity at beta1 adrenoceptor in rat left atria assessed as induction of ionotropic effectAgonist activity at beta1 adrenoceptor in rat left atria assessed as induction of ionotropic effect
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 -2290 6 Rat 5.6 pEC50 = 5.6 Functional
Agonist activity at beta1 adrenoceptor in rat left atria assessed as induction of ionotropic effectAgonist activity at beta1 adrenoceptor in rat left atria assessed as induction of ionotropic effect
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 -2290 6 Rat 5.6 pEC50 = 5.6 Functional
Agonist activity at beta1 adrenoceptor in rat left atria assessed as induction of ionotropic effectAgonist activity at beta1 adrenoceptor in rat left atria assessed as induction of ionotropic effect
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 -2290 6 Rat 5.6 pEC50 = 5.6 Functional
Agonist activity at beta1 adrenoceptor in rat left atria assessed as induction of ionotropic effectAgonist activity at beta1 adrenoceptor in rat left atria assessed as induction of ionotropic effect
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 -2290 6 Rat 5.6 pEC50 = 5.6 Functional
Agonist activity at beta1 adrenoceptor in rat left atria assessed as induction of ionotropic effectAgonist activity at beta1 adrenoceptor in rat left atria assessed as induction of ionotropic effect
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
155543518 174416 0 None -794 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 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 6.6 pEC50 = 6.6 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 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
45101521 195142 0 None -4 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human beta-1 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta-1 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 7.6 pEC50 = 7.6 Functional
Agonist activity at human beta-1 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta-1 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
44560794 172919 0 None -346 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 474 10 3 5 5.4 C[C@H](Cc1ccc(-c2ccc(C(=O)O)c(OC3CCCCC3)c2)cc1)NC[C@H](O)c1cccnc1 10.1021/jm8000345
CHEMBL453056 172919 0 None -346 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 474 10 3 5 5.4 C[C@H](Cc1ccc(-c2ccc(C(=O)O)c(OC3CCCCC3)c2)cc1)NC[C@H](O)c1cccnc1 10.1021/jm8000345
164623230 187976 0 None -1479 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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 7.6 pEC50 = 7.6 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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 7.6 pEC50 = 7.6 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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
44579940 191285 0 None -37 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 468 10 4 5 4.7 CC(=O)Nc1cc(Oc2cccc(CCNC[C@H](O)c3cccc(Cl)c3)c2)cc(C(=O)O)c1 10.1016/j.bmcl.2008.08.009
CHEMBL519985 191285 0 None -37 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 468 10 4 5 4.7 CC(=O)Nc1cc(Oc2cccc(CCNC[C@H](O)c3cccc(Cl)c3)c2)cc(C(=O)O)c1 10.1016/j.bmcl.2008.08.009
46232857 199064 0 None -19 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta-1 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 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta-1 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
42639654 12516 0 None -1258 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 513 11 3 7 3.8 CC(C)Sc1cc(-c2ccc(CCNC[C@H](O)c3cccnc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
CHEMBL1187156 12516 0 None -1258 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 513 11 3 7 3.8 CC(C)Sc1cc(-c2ccc(CCNC[C@H](O)c3cccnc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
CHEMBL491891 12516 0 None -1258 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 513 11 3 7 3.8 CC(C)Sc1cc(-c2ccc(CCNC[C@H](O)c3cccnc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
164615990 184710 0 None -831 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human beta1 adrenoceptor expressed in CHO cells assessed as increase in cAMP level incubated for 30 mins by immunoassayAgonist activity at human beta1 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 5.6 pEC50 = 5.6 Functional
Agonist activity at human beta1 adrenoceptor expressed in CHO cells assessed as increase in cAMP level incubated for 30 mins by immunoassayAgonist activity at human beta1 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
9832011 104989 0 None -138 3 Human 5.6 pEC50 = 5.6 Functional
Compound was evaluated for its inhibitory activity against human beta-1 adrenergic receptor (AR)Compound was evaluated for its inhibitory activity against human beta-1 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 -138 3 Human 5.6 pEC50 = 5.6 Functional
Compound was evaluated for its inhibitory activity against human beta-1 adrenergic receptor (AR)Compound was evaluated for its inhibitory activity against human beta-1 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
11091850 46952 0 None -25 3 Human 7.6 pEC50 = 7.6 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-1 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-1 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 7.6 pEC50 = 7.6 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-1 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-1 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
44441232 93342 0 None -19 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 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 -19 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 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
9892481 69875 11 None -501 4 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta1 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 -501 4 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta1 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
9849126 12318 0 None -630 4 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta-1 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 -630 4 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta-1 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 -630 4 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta-1 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
9892481 69875 11 None -501 4 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at recombinant human beta1-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta1-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 -501 4 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at recombinant human beta1-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta1-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
44574720 177965 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 494 11 4 5 4.5 O=C(Cc1ccccn1)Nc1ccc(CCNC[C@H](O)COc2cccc3[nH]c4ccccc4c23)cc1 10.1016/j.bmc.2009.03.044
CHEMBL466923 177965 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 494 11 4 5 4.5 O=C(Cc1ccccn1)Nc1ccc(CCNC[C@H](O)COc2cccc3[nH]c4ccccc4c23)cc1 10.1016/j.bmc.2009.03.044
49861320 54666 0 None -6 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
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 6.6 pEC50 = 6.6 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
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 6.6 pEC50 = 6.6 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
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
10048077 97432 12 None -52 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 425 9 3 4 4.6 COc1cc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)ccc1C(=O)O 10.1021/jm9000709
CHEMBL272383 97432 12 None -52 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 425 9 3 4 4.6 COc1cc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)ccc1C(=O)O 10.1021/jm9000709
44574757 177900 0 None -12 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 511 14 3 6 4.4 O=C(Cc1cccc(OCc2ccccc2)n1)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.03.044
CHEMBL466467 177900 0 None -12 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 511 14 3 6 4.4 O=C(Cc1cccc(OCc2ccccc2)n1)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.03.044
10048077 97432 12 None -52 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 425 9 3 4 4.6 COc1cc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)ccc1C(=O)O 10.1021/jm701324c
CHEMBL272383 97432 12 None -52 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 425 9 3 4 4.6 COc1cc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)ccc1C(=O)O 10.1021/jm701324c
11003341 46021 0 None -10 3 Human 6.6 pEC50 = 6.6 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-1 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-1 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 -10 3 Human 6.6 pEC50 = 6.6 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-1 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-1 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
56658246 64151 0 None -1258 4 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta1 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 -1258 4 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta1 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 -1258 4 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta1 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
11003341 46021 0 None -10 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 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 -10 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 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
2419 3394 80 None -1621 6 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta1 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 -1621 6 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta1 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 -1621 6 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta1 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 -1621 6 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta1 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 -1621 6 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta1 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
42625511 12613 0 None -316 4 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta-1 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 -316 4 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta-1 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 -316 4 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta-1 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
2419 3394 80 None -1621 6 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant beta1 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta1 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 -1621 6 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant beta1 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta1 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 -1621 6 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant beta1 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta1 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 -1621 6 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant beta1 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta1 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 -1621 6 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant beta1 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta1 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 -1621 6 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human beta1-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta1-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 -1621 6 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human beta1-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta1-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 -1621 6 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human beta1-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta1-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 -1621 6 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human beta1-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta1-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 -1621 6 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human beta1-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta1-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
10180590 69873 0 None -707 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human beta1-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta1-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 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human beta1-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta1-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
10202462 69874 0 None -223 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human beta1-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta1-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 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human beta1-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta1-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
11669967 76152 0 None -12589 2 Human 5.6 pEC50 = 5.6 Functional
Activity at human beta-1 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-1 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 468 10 5 5 4.5 C[C@H](CNc1cccc(-c2ccc(C(=O)O)cc2C(=O)O)c1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0509445
CHEMBL206002 76152 0 None -12589 2 Human 5.6 pEC50 = 5.6 Functional
Activity at human beta-1 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-1 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 468 10 5 5 4.5 C[C@H](CNc1cccc(-c2ccc(C(=O)O)cc2C(=O)O)c1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0509445
45375919 195326 0 None -87 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human adrenergic beta 1 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 1 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 6.6 pEC50 = 6.6 Functional
Agonist activity at human adrenergic beta 1 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 1 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
10232096 107166 0 None -1 2 Human 6.6 pEC50 = 6.6 Functional
In vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta1-AR receptorIn vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta1-AR receptor
ChEMBL 586 12 5 6 5.1 O=C(NCc1ccc(Cl)cc1Cl)N1CCC(Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)CC1 10.1016/s0960-894x(01)00645-x
CHEMBL319041 107166 0 None -1 2 Human 6.6 pEC50 = 6.6 Functional
In vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta1-AR receptorIn vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta1-AR receptor
ChEMBL 586 12 5 6 5.1 O=C(NCc1ccc(Cl)cc1Cl)N1CCC(Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)CC1 10.1016/s0960-894x(01)00645-x
44396530 66738 0 None -23 3 Human 7.6 pEC50 = 7.6 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-1 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-1 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 7.6 pEC50 = 7.6 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-1 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-1 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
44396798 168815 0 None -56 3 Human 7.6 pEC50 = 7.6 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-1 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-1 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 -56 3 Human 7.6 pEC50 = 7.6 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-1 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-1 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
45483846 195126 0 None -1 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human adrenergic beta 1 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 1 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 7.6 pEC50 = 7.6 Functional
Agonist activity at human adrenergic beta 1 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 1 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
44574868 177989 0 None -3 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 534 13 3 6 4.8 O=C(Cc1nccn1Cc1ccc2ccccc2c1)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.03.044
CHEMBL467103 177989 0 None -3 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 534 13 3 6 4.8 O=C(Cc1nccn1Cc1ccc2ccccc2c1)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.03.044
24823131 96939 0 None -15 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 429 8 3 3 5.2 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)cc1Cl 10.1021/jm701324c
CHEMBL269823 96939 0 None -15 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 429 8 3 3 5.2 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)cc1Cl 10.1021/jm701324c
24823294 158510 0 None -870 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 459 10 3 4 5.6 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)cc1OC1CCCCC1 10.1021/jm701324c
CHEMBL409718 158510 0 None -870 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 459 10 3 4 5.6 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)cc1OC1CCCCC1 10.1021/jm701324c
44127374 194550 0 None 1 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 421 11 4 6 2.5 O=C(Cc1ccncc1)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/j.ejmech.2009.01.022
CHEMBL561693 194550 0 None 1 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 421 11 4 6 2.5 O=C(Cc1ccncc1)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/j.ejmech.2009.01.022
24823294 158510 0 None -870 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 459 10 3 4 5.6 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)cc1OC1CCCCC1 10.1021/jm8000345
CHEMBL409718 158510 0 None -870 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 459 10 3 4 5.6 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)cc1OC1CCCCC1 10.1021/jm8000345
11420551 12398 0 None -436 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 495 11 4 6 3.7 CC(C)Nc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
CHEMBL1186589 12398 0 None -436 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 495 11 4 6 3.7 CC(C)Nc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
CHEMBL471060 12398 0 None -436 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 495 11 4 6 3.7 CC(C)Nc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
24823294 158510 0 None -870 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 459 10 3 4 5.6 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)cc1OC1CCCCC1 10.1021/jm9000709
CHEMBL409718 158510 0 None -870 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 459 10 3 4 5.6 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)cc1OC1CCCCC1 10.1021/jm9000709
1028 287 69 None -3 16 Guinea pig 6.6 pEC50 = 6.6 Functional
Agonistic potency at beta-1 adrenergic receptor for the percent maximal increase in contraction rate of isolated guinea pig atriaAgonistic potency at beta-1 adrenergic receptor for the percent maximal increase in contraction rate of isolated guinea pig atria
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00118a019
139148732 287 69 None -3 16 Guinea pig 6.6 pEC50 = 6.6 Functional
Agonistic potency at beta-1 adrenergic receptor for the percent maximal increase in contraction rate of isolated guinea pig atriaAgonistic potency at beta-1 adrenergic receptor for the percent maximal increase in contraction rate of isolated guinea pig atria
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00118a019
479 287 69 None -3 16 Guinea pig 6.6 pEC50 = 6.6 Functional
Agonistic potency at beta-1 adrenergic receptor for the percent maximal increase in contraction rate of isolated guinea pig atriaAgonistic potency at beta-1 adrenergic receptor for the percent maximal increase in contraction rate of isolated guinea pig atria
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00118a019
5816 287 69 None -3 16 Guinea pig 6.6 pEC50 = 6.6 Functional
Agonistic potency at beta-1 adrenergic receptor for the percent maximal increase in contraction rate of isolated guinea pig atriaAgonistic potency at beta-1 adrenergic receptor for the percent maximal increase in contraction rate of isolated guinea pig atria
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00118a019
CHEMBL679 287 69 None -3 16 Guinea pig 6.6 pEC50 = 6.6 Functional
Agonistic potency at beta-1 adrenergic receptor for the percent maximal increase in contraction rate of isolated guinea pig atriaAgonistic potency at beta-1 adrenergic receptor for the percent maximal increase in contraction rate of isolated guinea pig atria
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00118a019
DB00668 287 69 None -3 16 Guinea pig 6.6 pEC50 = 6.6 Functional
Agonistic potency at beta-1 adrenergic receptor for the percent maximal increase in contraction rate of isolated guinea pig atriaAgonistic potency at beta-1 adrenergic receptor for the percent maximal increase in contraction rate of isolated guinea pig atria
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00118a019
10119515 107890 0 None -7 2 Human 6.6 pEC50 = 6.6 Functional
In vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta1-AR receptorIn vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta1-AR receptor
ChEMBL 536 12 5 6 3.9 O=C(NCc1ccccc1F)N1CCC(Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)CC1 10.1016/s0960-894x(01)00645-x
CHEMBL319840 107890 0 None -7 2 Human 6.6 pEC50 = 6.6 Functional
In vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta1-AR receptorIn vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta1-AR receptor
ChEMBL 536 12 5 6 3.9 O=C(NCc1ccccc1F)N1CCC(Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)CC1 10.1016/s0960-894x(01)00645-x
11758172 100454 0 None -181 3 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-1 receptor.In vitro functional efficacy in stimulating increase in cAMP in chinese hamster ovary (CHO) cells expressing the cloned human beta-1 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 -181 3 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-1 receptor.In vitro functional efficacy in stimulating increase in cAMP in chinese hamster ovary (CHO) cells expressing the cloned human beta-1 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
44336319 6271 0 None -524 2 Human 5.6 pEC50 = 5.6 Functional
In vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta1-AR receptorIn vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta1-AR receptor
ChEMBL 617 12 6 7 3.7 CS(=O)(=O)Nc1cc([C@@H](O)CNCCc2ccc(NC3CCN(C(=O)NCc4cc(F)ccc4F)CC3)cc2)ccc1O 10.1016/s0960-894x(01)00645-x
CHEMBL108214 6271 0 None -524 2 Human 5.6 pEC50 = 5.6 Functional
In vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta1-AR receptorIn vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta1-AR receptor
ChEMBL 617 12 6 7 3.7 CS(=O)(=O)Nc1cc([C@@H](O)CNCCc2ccc(NC3CCN(C(=O)NCc4cc(F)ccc4F)CC3)cc2)ccc1O 10.1016/s0960-894x(01)00645-x
46232973 199094 0 None -19 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta-1 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 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta-1 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
44392255 165397 0 None -5 2 Human 7.6 pEC50 = 7.6 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptor
ChEMBL 401 11 5 5 2.1 CC(C)NC(=O)Nc1ccc(C[C@@H](CO)NC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmcl.2004.11.001
CHEMBL425173 165397 0 None -5 2 Human 7.6 pEC50 = 7.6 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptor
ChEMBL 401 11 5 5 2.1 CC(C)NC(=O)Nc1ccc(C[C@@H](CO)NC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmcl.2004.11.001
44574827 178046 0 None -3 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 518 13 3 6 4.3 O=C(Cc1nccn1Cc1ccc(Cl)cc1)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.03.044
CHEMBL467502 178046 0 None -3 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 518 13 3 6 4.3 O=C(Cc1nccn1Cc1ccc(Cl)cc1)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.03.044
24950401 176441 0 None -147 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 481 8 3 6 4.5 CN(C)c1cc(Oc2ccc3c(c2)C[C@@H](NC[C@H](O)c2ccc(Cl)nc2)CC3)cc(C(=O)O)c1 10.1021/jm800222k
CHEMBL463181 176441 0 None -147 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 481 8 3 6 4.5 CN(C)c1cc(Oc2ccc3c(c2)C[C@@H](NC[C@H](O)c2ccc(Cl)nc2)CC3)cc(C(=O)O)c1 10.1021/jm800222k
44127171 177933 0 None 1 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 421 11 4 6 2.5 O=C(Cc1ccccn1)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/j.ejmech.2009.01.022
CHEMBL466705 177933 0 None 1 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 421 11 4 6 2.5 O=C(Cc1ccccn1)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/j.ejmech.2009.01.022
10722793 112835 0 None -407 3 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-1 receptor.In vitro functional efficacy in stimulating increase in cAMP in chinese hamster ovary (CHO) cells expressing the cloned human beta-1 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 -407 3 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-1 receptor.In vitro functional efficacy in stimulating increase in cAMP in chinese hamster ovary (CHO) cells expressing the cloned human beta-1 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
9871800 56179 0 None -269 3 Human 5.6 pEC50 = 5.6 Functional
Agonistic activity as cAMP accumulation in CHO cells expressing human beta-1-adrenergic receptorAgonistic activity as cAMP accumulation in CHO cells expressing human beta-1-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 -269 3 Human 5.6 pEC50 = 5.6 Functional
Agonistic activity as cAMP accumulation in CHO cells expressing human beta-1-adrenergic receptorAgonistic activity as cAMP accumulation in CHO cells expressing human beta-1-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
46232974 199115 5 None -27 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta-1 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 5.6 pEC50 = 5.6 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta-1 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
46233013 199609 0 None -19 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta-1 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 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta-1 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
45484538 13968 0 None -2 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human beta-1 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta-1 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 7.6 pEC50 = 7.6 Functional
Agonist activity at human beta-1 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta-1 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 7.6 pEC50 = 7.6 Functional
Agonist activity at human beta-1 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta-1 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
44579651 186563 0 None -14 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 425 9 3 4 5.1 C[C@H](Cc1cccc(Oc2cccc(C(=O)O)c2)c1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2008.08.009
CHEMBL492006 186563 0 None -14 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 425 9 3 4 5.1 C[C@H](Cc1cccc(Oc2cccc(C(=O)O)c2)c1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2008.08.009
24894202 188428 0 None -676 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 473 10 3 4 6.0 C[C@H](Cc1ccc(-c2ccc(C(=O)O)c(OC3CCCCC3)c2)cc1)NC[C@H](O)c1ccccc1 10.1021/jm8000345
CHEMBL509156 188428 0 None -676 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 473 10 3 4 6.0 C[C@H](Cc1ccc(-c2ccc(C(=O)O)c(OC3CCCCC3)c2)cc1)NC[C@H](O)c1ccccc1 10.1021/jm8000345
44574688 177903 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 461 11 5 6 2.0 O=C(Cc1ccccn1)Nc1ccc(CCNC[C@H](O)COc2cccc3[nH]c(=O)[nH]c23)cc1 10.1016/j.bmc.2009.03.044
CHEMBL466519 177903 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 461 11 5 6 2.0 O=C(Cc1ccccn1)Nc1ccc(CCNC[C@H](O)COc2cccc3[nH]c(=O)[nH]c23)cc1 10.1016/j.bmc.2009.03.044
44574722 177967 0 None 1 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 433 11 3 5 3.5 Cc1cc(C)nc(CC(=O)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)c1 10.1016/j.bmc.2009.03.044
CHEMBL466925 177967 0 None 1 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 433 11 3 5 3.5 Cc1cc(C)nc(CC(=O)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)c1 10.1016/j.bmc.2009.03.044
44219630 177990 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 498 13 2 6 3.7 CN(C(=O)Cc1nccn1Cc1ccccc1)c1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.03.044
CHEMBL467116 177990 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 498 13 2 6 3.7 CN(C(=O)Cc1nccn1Cc1ccccc1)c1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.03.044
24822310 97279 0 None -41 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 395 8 3 3 4.6 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)cc1 10.1021/jm701324c
CHEMBL271576 97279 0 None -41 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 395 8 3 3 4.6 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)cc1 10.1021/jm701324c
24822310 97279 0 None -41 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 395 8 3 3 4.6 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)cc1 10.1016/j.bmcl.2008.08.009
CHEMBL271576 97279 0 None -41 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 395 8 3 3 4.6 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)cc1 10.1016/j.bmcl.2008.08.009
44127054 193606 0 None 6 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 450 12 4 6 3.2 COc1ccc(CC(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/j.ejmech.2009.01.022
CHEMBL551350 193606 0 None 6 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 450 12 4 6 3.2 COc1ccc(CC(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/j.ejmech.2009.01.022
24822310 97279 0 None -41 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 395 8 3 3 4.6 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)cc1 10.1021/jm800222k
CHEMBL271576 97279 0 None -41 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 395 8 3 3 4.6 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)cc1 10.1021/jm800222k
24895365 173010 0 None -309 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 447 10 3 4 5.5 CC(C)Oc1cc(-c2ccc(CC(C)(C)NC[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm8000345
CHEMBL453323 173010 0 None -309 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 447 10 3 4 5.5 CC(C)Oc1cc(-c2ccc(CC(C)(C)NC[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm8000345
10298968 57188 0 None -239 2 Human 5.5 pEC50 = 5.5 Functional
Agonistic activity as cAMP accumulation in CHO cells expressing human beta-1-adrenergic receptorAgonistic activity as cAMP accumulation in CHO cells expressing human beta-1-adrenergic receptor
ChEMBL 471 9 4 8 2.3 O=C1NC(=O)C(Cc2ccc(N3CCC(NC[C@H](O)COc4ccc(O)cc4)CC3)cc2)S1 10.1016/s0960-894x(01)00063-4
CHEMBL166085 57188 0 None -239 2 Human 5.5 pEC50 = 5.5 Functional
Agonistic activity as cAMP accumulation in CHO cells expressing human beta-1-adrenergic receptorAgonistic activity as cAMP accumulation in CHO cells expressing human beta-1-adrenergic receptor
ChEMBL 471 9 4 8 2.3 O=C1NC(=O)C(Cc2ccc(N3CCC(NC[C@H](O)COc4ccc(O)cc4)CC3)cc2)S1 10.1016/s0960-894x(01)00063-4
44396596 122771 0 None -25 3 Human 7.5 pEC50 = 7.5 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-1 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-1 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 7.5 pEC50 = 7.5 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-1 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-1 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
44396521 123150 0 None -6 2 Human 7.5 pEC50 = 7.5 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-1 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-1 adrenergic receptor
ChEMBL 514 12 5 7 3.6 C[C@H](Cc1c[nH]c2c(OCCN)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2004.10.035
CHEMBL362136 123150 0 None -6 2 Human 7.5 pEC50 = 7.5 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-1 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-1 adrenergic receptor
ChEMBL 514 12 5 7 3.6 C[C@H](Cc1c[nH]c2c(OCCN)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2004.10.035
44127171 177933 0 None 1 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 421 11 4 6 2.5 O=C(Cc1ccccn1)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/j.bmc.2009.03.044
CHEMBL466705 177933 0 None 1 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 421 11 4 6 2.5 O=C(Cc1ccccn1)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/j.bmc.2009.03.044
1028 287 69 None -7 16 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human beta1 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 beta1 adrenergic receptor expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium influx by measuring fluorescence intensity by FLIPR assay
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/acs.jnatprod.9b00418
139148732 287 69 None -7 16 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human beta1 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 beta1 adrenergic receptor expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium influx by measuring fluorescence intensity by FLIPR assay
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/acs.jnatprod.9b00418
479 287 69 None -7 16 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human beta1 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 beta1 adrenergic receptor expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium influx by measuring fluorescence intensity by FLIPR assay
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/acs.jnatprod.9b00418
5816 287 69 None -7 16 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human beta1 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 beta1 adrenergic receptor expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium influx by measuring fluorescence intensity by FLIPR assay
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/acs.jnatprod.9b00418
CHEMBL679 287 69 None -7 16 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human beta1 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 beta1 adrenergic receptor expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium influx by measuring fluorescence intensity by FLIPR assay
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/acs.jnatprod.9b00418
DB00668 287 69 None -7 16 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human beta1 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 beta1 adrenergic receptor expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium influx by measuring fluorescence intensity by FLIPR assay
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/acs.jnatprod.9b00418
45101537 193594 0 None -1819 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassayAgonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassay
ChEMBL 526 11 4 7 3.8 CC(C)Oc1cc(-c2ccc(CCN[C@@H](C)[C@H](O)c3ccc(O)cc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1016/j.bmcl.2009.06.083
CHEMBL551272 193594 0 None -1819 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassayAgonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassay
ChEMBL 526 11 4 7 3.8 CC(C)Oc1cc(-c2ccc(CCN[C@@H](C)[C@H](O)c3ccc(O)cc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1016/j.bmcl.2009.06.083
45483830 195310 0 None -14 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human adrenergic beta 1 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 1 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 6.5 pEC50 = 6.5 Functional
Agonist activity at human adrenergic beta 1 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 1 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
44237720 57915 0 None -91 2 Rat 6.5 pEC50 = 6.5 Functional
Agonist activity at beta1 adrenoceptor in rat left atria assessed as induction of ionotropic effectAgonist activity at beta1 adrenoceptor in rat left atria assessed as induction of ionotropic effect
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 Rat 6.5 pEC50 = 6.5 Functional
Agonist activity at beta1 adrenoceptor in rat left atria assessed as induction of ionotropic effectAgonist activity at beta1 adrenoceptor in rat left atria assessed as induction of ionotropic effect
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
145983355 165237 0 None -26 3 Human 6.5 pEC50 = 6.5 Functional
Antagonist activity at human beta1 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 beta1 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 -26 3 Human 6.5 pEC50 = 6.5 Functional
Antagonist activity at human beta1 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 beta1 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
44268273 96620 0 None 1 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity against cloned human beta-1 adrenergic receptor as percent activation of adenyl cyclase activity at a concentration of 1000 nMAgonist activity against cloned human beta-1 adrenergic receptor as percent activation of adenyl cyclase activity at a concentration of 1000 nM
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 1 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity against cloned human beta-1 adrenergic receptor as percent activation of adenyl cyclase activity at a concentration of 1000 nMAgonist activity against cloned human beta-1 adrenergic receptor as percent activation of adenyl cyclase activity at a concentration of 1000 nM
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
44392190 65237 0 None 4 2 Human 8.5 pEC50 = 8.5 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptor
ChEMBL 421 10 5 5 3.2 O=C(Nc1ccccc1)Nc1ccc(C[C@H](O)NC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmcl.2004.11.001
CHEMBL183211 65237 0 None 4 2 Human 8.5 pEC50 = 8.5 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptor
ChEMBL 421 10 5 5 3.2 O=C(Nc1ccccc1)Nc1ccc(C[C@H](O)NC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmcl.2004.11.001
9896742 203226 0 None -13 3 Human 8.5 pEC50 = 8.5 Functional
Compound was evaluated for its inhibitory activity against human beta-1 adrenergic receptor (AR) at a concentration of 10000 nmCompound was evaluated for its inhibitory activity against human beta-1 adrenergic receptor (AR) at a concentration of 10000 nm
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 -13 3 Human 8.5 pEC50 = 8.5 Functional
Compound was evaluated for its inhibitory activity against human beta-1 adrenergic receptor (AR) at a concentration of 10000 nmCompound was evaluated for its inhibitory activity against human beta-1 adrenergic receptor (AR) at a concentration of 10000 nm
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
66653268 87809 0 None 3311 3 Human 8.5 pEC50 = 8.5 Functional
Partial agonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsPartial agonist activity at human beta1 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 8.5 pEC50 = 8.5 Functional
Partial agonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsPartial agonist activity at human beta1 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
164622954 187971 0 None -245 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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 8.5 pEC50 = 8.5 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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 8.5 pEC50 = 8.5 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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
164624634 187990 0 None -131 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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 8.5 pEC50 = 8.5 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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 8.5 pEC50 = 8.5 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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
24822971 94991 0 None 3 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 429 8 3 3 5.2 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2Cl)cc1 10.1021/jm701324c
CHEMBL257106 94991 0 None 3 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 429 8 3 3 5.2 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2Cl)cc1 10.1021/jm701324c
11134054 46704 0 None -2 3 Human 8.5 pEC50 = 8.5 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-1 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-1 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 -2 3 Human 8.5 pEC50 = 8.5 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-1 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-1 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
1499 2052 43 None -64 36 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 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 -64 36 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 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 -64 36 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 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 -64 36 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 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 -64 36 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 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 -64 36 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 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 -64 36 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 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 -64 36 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 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 -64 36 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 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 -64 36 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 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
45484583 196805 0 None -3 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human beta-1 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta-1 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 8.5 pEC50 = 8.5 Functional
Agonist activity at human beta-1 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta-1 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
45484585 13969 0 None -3 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human beta-1 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta-1 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 8.5 pEC50 = 8.5 Functional
Agonist activity at human beta-1 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta-1 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 8.5 pEC50 = 8.5 Functional
Agonist activity at human beta-1 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta-1 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
24936626 17212 0 None -173 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as 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 -173 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as 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
45483814 195586 0 None -5 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human adrenergic beta 1 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 1 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 8.4 pEC50 = 8.4 Functional
Agonist activity at human adrenergic beta 1 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 1 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
44392212 167794 0 None 12 2 Human 8.4 pEC50 = 8.4 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptor
ChEMBL 405 10 4 4 3.9 O=C(Nc1ccccc1)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmcl.2004.11.001
CHEMBL1204383 167794 0 None 12 2 Human 8.4 pEC50 = 8.4 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptor
ChEMBL 405 10 4 4 3.9 O=C(Nc1ccccc1)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmcl.2004.11.001
CHEMBL434524 167794 0 None 12 2 Human 8.4 pEC50 = 8.4 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptor
ChEMBL 405 10 4 4 3.9 O=C(Nc1ccccc1)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmcl.2004.11.001
56597179 87827 0 None 2754 3 Human 8.4 pEC50 = 8.4 Functional
Partial agonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsPartial agonist activity at human beta1 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 8.4 pEC50 = 8.4 Functional
Partial agonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsPartial agonist activity at human beta1 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
45483868 195536 0 None -6 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human adrenergic beta 1 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 1 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 8.4 pEC50 = 8.4 Functional
Agonist activity at human adrenergic beta 1 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 1 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
45483864 197221 0 None -9 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human adrenergic beta 1 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 1 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 8.4 pEC50 = 8.4 Functional
Agonist activity at human adrenergic beta 1 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 1 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
24823624 158603 0 None 1 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 410 9 4 4 4.6 O=C(O)c1ccc(Nc2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)cc1 10.1021/jm701324c
CHEMBL409827 158603 0 None 1 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 410 9 4 4 4.6 O=C(O)c1ccc(Nc2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)cc1 10.1021/jm701324c
16049028 63739 0 None -50 3 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at adrenergic beta1 receptorAgonist activity at adrenergic beta1 receptor
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 8.4 pEC50 = 8.4 Functional
Agonist activity at adrenergic beta1 receptorAgonist activity at adrenergic beta1 receptor
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 8.4 pEC50 = 8.4 Functional
Agonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta1 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 8.4 pEC50 = 8.4 Functional
Agonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta1 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
24822645 95036 0 None -15 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 429 8 3 3 5.2 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)c(Cl)c1 10.1021/jm701324c
CHEMBL257297 95036 0 None -15 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 429 8 3 3 5.2 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)c(Cl)c1 10.1021/jm701324c
45269866 193614 0 None 1 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 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 beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 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 beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 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
45269025 194463 0 None -3 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 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 7.5 pEC50 = 7.5 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 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 7.5 pEC50 = 7.5 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 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 7.5 pEC50 = 7.5 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 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 7.5 pEC50 = 7.5 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 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 7.5 pEC50 = 7.5 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 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
10283146 106776 0 None -2 3 Human 7.5 pEC50 = 7.5 Functional
Beta-1 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-1-adrenoceptorBeta-1 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-1-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-1 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-1-adrenoceptorBeta-1 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-1-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
1960 2805 64 None -79 13 Guinea pig 7.5 pEC50 = 7.5 Functional
Effective concentration for Beta-1 adrenergic receptor mediated inhibition of neurotransmission in field-stimulated reserpine pretreated guinea pig ileum.Effective concentration for Beta-1 adrenergic receptor mediated inhibition of neurotransmission in field-stimulated reserpine pretreated guinea pig ileum.
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00019a001
439260 2805 64 None -79 13 Guinea pig 7.5 pEC50 = 7.5 Functional
Effective concentration for Beta-1 adrenergic receptor mediated inhibition of neurotransmission in field-stimulated reserpine pretreated guinea pig ileum.Effective concentration for Beta-1 adrenergic receptor mediated inhibition of neurotransmission in field-stimulated reserpine pretreated guinea pig ileum.
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00019a001
505 2805 64 None -79 13 Guinea pig 7.5 pEC50 = 7.5 Functional
Effective concentration for Beta-1 adrenergic receptor mediated inhibition of neurotransmission in field-stimulated reserpine pretreated guinea pig ileum.Effective concentration for Beta-1 adrenergic receptor mediated inhibition of neurotransmission in field-stimulated reserpine pretreated guinea pig ileum.
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00019a001
CHEMBL1437 2805 64 None -79 13 Guinea pig 7.5 pEC50 = 7.5 Functional
Effective concentration for Beta-1 adrenergic receptor mediated inhibition of neurotransmission in field-stimulated reserpine pretreated guinea pig ileum.Effective concentration for Beta-1 adrenergic receptor mediated inhibition of neurotransmission in field-stimulated reserpine pretreated guinea pig ileum.
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00019a001
DB00368 2805 64 None -79 13 Guinea pig 7.5 pEC50 = 7.5 Functional
Effective concentration for Beta-1 adrenergic receptor mediated inhibition of neurotransmission in field-stimulated reserpine pretreated guinea pig ileum.Effective concentration for Beta-1 adrenergic receptor mediated inhibition of neurotransmission in field-stimulated reserpine pretreated guinea pig ileum.
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00019a001
164623583 187981 0 None -316 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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 7.5 pEC50 = 7.5 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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 7.5 pEC50 = 7.5 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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
24822970 157563 0 None -9 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 409 9 3 3 4.5 O=C(O)Cc1ccc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)cc1 10.1021/jm701324c
CHEMBL408694 157563 0 None -9 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 409 9 3 3 4.5 O=C(O)Cc1ccc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)cc1 10.1021/jm701324c
11224220 172388 0 None -2137 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 431 10 3 3 5.5 CC(C)Cc1cc(-c2ccc(CCN[C@@H](C)[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm8000345
CHEMBL451760 172388 0 None -2137 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 431 10 3 3 5.5 CC(C)Cc1cc(-c2ccc(CCN[C@@H](C)[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm8000345
172745 99648 7 None 234 2 Guinea pig 6.5 pEC50 = 6.5 Functional
Beta-1 adrenergic receptor agonist activity by stimulation of contraction rate of isolated guinea pig atrial preparationsBeta-1 adrenergic receptor agonist activity by stimulation of contraction rate of isolated guinea pig atrial preparations
ChEMBL 187 2 4 4 0.2 NCC(O)c1ccc(O)c(O)c1F 10.1021/jm00118a019
CHEMBL287587 99648 7 None 234 2 Guinea pig 6.5 pEC50 = 6.5 Functional
Beta-1 adrenergic receptor agonist activity by stimulation of contraction rate of isolated guinea pig atrial preparationsBeta-1 adrenergic receptor agonist activity by stimulation of contraction rate of isolated guinea pig atrial preparations
ChEMBL 187 2 4 4 0.2 NCC(O)c1ccc(O)c(O)c1F 10.1021/jm00118a019
44268268 18449 0 None -301 3 Human 6.5 pEC50 = 6.5 Functional
Compound was tested for agonist activity against cloned human beta-1 adrenergic receptorCompound was tested for agonist activity against cloned human beta-1 adrenergic receptor
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 -301 3 Human 6.5 pEC50 = 6.5 Functional
Compound was tested for agonist activity against cloned human beta-1 adrenergic receptorCompound was tested for agonist activity against cloned human beta-1 adrenergic receptor
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
16049377 63752 0 None -112 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at adrenergic beta1 receptorAgonist activity at adrenergic beta1 receptor
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 7.5 pEC50 = 7.5 Functional
Agonist activity at adrenergic beta1 receptorAgonist activity at adrenergic beta1 receptor
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
56665368 66111 0 None -31 4 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta1 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 -31 4 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta1 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 -31 4 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta1 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
56672271 66193 0 None -125 4 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta1 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 -125 4 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta1 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 -125 4 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta1 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
56672269 66239 0 None -50 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta1 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 7.5 pEC50 = 7.5 Functional
Agonist activity at human beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta1 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 7.5 pEC50 = 7.5 Functional
Agonist activity at human beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta1 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
56658405 66240 0 None -63 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta1 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 -63 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta1 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 -63 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta1 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
46832505 14105 0 None -12 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta-1 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 7.5 pEC50 = 7.5 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta-1 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 7.5 pEC50 = 7.5 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta-1 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
46889854 7212 0 None -9 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human adrenergic beta-1 receptor expressed in CHOK1 cells assessed as cAMP accumulation by HTRF assayAgonist activity at human adrenergic beta-1 receptor expressed in CHOK1 cells assessed as 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 6.5 pEC50 = 6.5 Functional
Agonist activity at human adrenergic beta-1 receptor expressed in CHOK1 cells assessed as cAMP accumulation by HTRF assayAgonist activity at human adrenergic beta-1 receptor expressed in CHOK1 cells assessed as 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
24949728 174658 0 None -436 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 479 8 3 4 5.7 CC(C)Oc1cc(-c2ccc3c(c2)C[C@@H](NC[C@H](O)c2ccc(Cl)cc2)CC3)ccc1C(=O)O 10.1021/jm800222k
CHEMBL457199 174658 0 None -436 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 479 8 3 4 5.7 CC(C)Oc1cc(-c2ccc3c(c2)C[C@@H](NC[C@H](O)c2ccc(Cl)cc2)CC3)ccc1C(=O)O 10.1021/jm800222k
44127679 193781 0 None -37 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 422 11 4 7 1.9 O=C(Cc1cnccn1)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/j.ejmech.2009.01.022
CHEMBL552497 193781 0 None -37 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 422 11 4 7 1.9 O=C(Cc1cnccn1)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/j.ejmech.2009.01.022
9891927 183605 6 None -1995 4 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta-1 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 -1995 4 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta-1 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 -1995 4 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta-1 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 -1995 4 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta-1 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 -1995 4 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta-1 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 -1995 4 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta-1 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 -1995 4 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta-1 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 -1995 4 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta-1 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
44331302 206577 0 None -630 3 Human 5.5 pEC50 = 5.5 Functional
Beta-1 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-1-adrenoceptorBeta-1 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-1-adrenoceptor
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 -630 3 Human 5.5 pEC50 = 5.5 Functional
Beta-1 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-1-adrenoceptorBeta-1 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-1-adrenoceptor
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
11661536 75608 0 None -50 3 Human 5.5 pEC50 = 5.5 Functional
Activity at human beta-1 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-1 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 -50 3 Human 5.5 pEC50 = 5.5 Functional
Activity at human beta-1 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-1 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
145987415 166684 0 None -1258 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 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 5.5 pEC50 = 5.5 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 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
24895192 189262 0 None -151 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 437 10 3 4 4.8 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3cccc(F)c3)cc2)ccc1C(=O)O 10.1021/jm8000345
CHEMBL516804 189262 0 None -151 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 437 10 3 4 4.8 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3cccc(F)c3)cc2)ccc1C(=O)O 10.1021/jm8000345
42639969 12450 0 None -1584 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 496 11 4 7 3.1 CC(C)Nc1cc(-c2ccc(CCNC[C@H](O)c3cccnc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
CHEMBL1186809 12450 0 None -1584 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 496 11 4 7 3.1 CC(C)Nc1cc(-c2ccc(CCNC[C@H](O)c3cccnc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
CHEMBL479530 12450 0 None -1584 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 496 11 4 7 3.1 CC(C)Nc1cc(-c2ccc(CCNC[C@H](O)c3cccnc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
16118894 2203 3 None -147 3 Human 6.5 pEC50 = 6.5 Functional
Compound was tested for agonist activity against cloned human beta-1 adrenergic receptorCompound was tested for agonist activity against cloned human beta-1 adrenergic receptor
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 -147 3 Human 6.5 pEC50 = 6.5 Functional
Compound was tested for agonist activity against cloned human beta-1 adrenergic receptorCompound was tested for agonist activity against cloned human beta-1 adrenergic receptor
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 -147 3 Human 6.5 pEC50 = 6.5 Functional
Compound was tested for agonist activity against cloned human beta-1 adrenergic receptorCompound was tested for agonist activity against cloned human beta-1 adrenergic receptor
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
45483815 196755 0 None -11 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human adrenergic beta 1 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 1 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 7.5 pEC50 = 7.5 Functional
Agonist activity at human adrenergic beta 1 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 1 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
44574721 177966 0 None 1 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 419 11 3 5 3.1 Cc1cccnc1CC(=O)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.03.044
CHEMBL466924 177966 0 None 1 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 419 11 3 5 3.1 Cc1cccnc1CC(=O)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.03.044
24950238 174372 0 None -69 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 437 7 3 4 5.0 O=C(O)c1cccc(Oc2ccc3c(c2)C[C@@H](NC[C@H](O)c2ccc(Cl)cc2)CC3)c1 10.1021/jm800222k
CHEMBL456578 174372 0 None -69 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 437 7 3 4 5.0 O=C(O)c1cccc(Oc2ccc3c(c2)C[C@@H](NC[C@H](O)c2ccc(Cl)cc2)CC3)c1 10.1021/jm800222k
45270697 193490 0 None -20 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
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 6.5 pEC50 = 6.5 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
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 6.5 pEC50 = 6.5 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 451 11 4 5 4.1 COc1ccccc1NC(=S)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.06.031
24949568 189081 0 None -338 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 536 9 4 6 5.6 O=C(O)c1cc(NC2CCOCC2)cc(Oc2ccc3c(c2)C[C@@H](NC[C@H](O)c2cccc(Cl)c2)CC3)c1 10.1021/jm800222k
CHEMBL515349 189081 0 None -338 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 536 9 4 6 5.6 O=C(O)c1cc(NC2CCOCC2)cc(Oc2ccc3c(c2)C[C@@H](NC[C@H](O)c2cccc(Cl)c2)CC3)c1 10.1021/jm800222k
10075383 96645 0 None -537 3 Human 6.5 pEC50 = 6.5 Functional
Compound was tested for agonist activity against cloned human beta-1 adrenergic receptorCompound was tested for agonist activity against cloned human beta-1 adrenergic receptor
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 -537 3 Human 6.5 pEC50 = 6.5 Functional
Compound was tested for agonist activity against cloned human beta-1 adrenergic receptorCompound was tested for agonist activity against cloned human beta-1 adrenergic receptor
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
46232768 197943 0 None -14 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta-1 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 7.5 pEC50 = 7.5 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta-1 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
164624092 187986 0 None -794 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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 7.5 pEC50 = 7.5 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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 7.5 pEC50 = 7.5 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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
145986105 164807 0 None -25 3 Human 7.4 pEC50 = 7.4 Functional
Antagonist activity at human beta1 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 beta1 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 -25 3 Human 7.4 pEC50 = 7.4 Functional
Antagonist activity at human beta1 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 beta1 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
44219641 177854 0 None -5 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 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 -5 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 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
24822815 97480 0 None -588 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 467 11 3 4 5.6 CC(C)COc1cc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)ccc1C(=O)O 10.1021/jm701324c
CHEMBL272583 97480 0 None -588 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 467 11 3 4 5.6 CC(C)COc1cc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)ccc1C(=O)O 10.1021/jm701324c
44127678 194618 0 None -2 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 471 11 4 6 3.7 O=C(Cc1cc2ccccc2cn1)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/j.ejmech.2009.01.022
CHEMBL562153 194618 0 None -2 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 471 11 4 6 3.7 O=C(Cc1cc2ccccc2cn1)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/j.ejmech.2009.01.022
1960 2805 64 None -79 13 Guinea pig 6.5 pEC50 = 6.5 Functional
Agonistic potency at beta-1 adrenergic receptor for the percent maximal increase in contraction rate of isolated guinea pig atriaAgonistic potency at beta-1 adrenergic receptor for the percent maximal increase in contraction rate of isolated guinea pig atria
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00118a019
439260 2805 64 None -79 13 Guinea pig 6.5 pEC50 = 6.5 Functional
Agonistic potency at beta-1 adrenergic receptor for the percent maximal increase in contraction rate of isolated guinea pig atriaAgonistic potency at beta-1 adrenergic receptor for the percent maximal increase in contraction rate of isolated guinea pig atria
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00118a019
505 2805 64 None -79 13 Guinea pig 6.5 pEC50 = 6.5 Functional
Agonistic potency at beta-1 adrenergic receptor for the percent maximal increase in contraction rate of isolated guinea pig atriaAgonistic potency at beta-1 adrenergic receptor for the percent maximal increase in contraction rate of isolated guinea pig atria
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00118a019
CHEMBL1437 2805 64 None -79 13 Guinea pig 6.5 pEC50 = 6.5 Functional
Agonistic potency at beta-1 adrenergic receptor for the percent maximal increase in contraction rate of isolated guinea pig atriaAgonistic potency at beta-1 adrenergic receptor for the percent maximal increase in contraction rate of isolated guinea pig atria
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00118a019
DB00368 2805 64 None -79 13 Guinea pig 6.5 pEC50 = 6.5 Functional
Agonistic potency at beta-1 adrenergic receptor for the percent maximal increase in contraction rate of isolated guinea pig atriaAgonistic potency at beta-1 adrenergic receptor for the percent maximal increase in contraction rate of isolated guinea pig atria
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00118a019
10275157 5290 0 None -7 2 Human 6.5 pEC50 = 6.5 Functional
In vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta1-AR receptorIn vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta1-AR receptor
ChEMBL 442 10 5 6 2.2 CNC(=O)N1CCC(Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)CC1 10.1016/s0960-894x(01)00645-x
CHEMBL107012 5290 0 None -7 2 Human 6.5 pEC50 = 6.5 Functional
In vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta1-AR receptorIn vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta1-AR receptor
ChEMBL 442 10 5 6 2.2 CNC(=O)N1CCC(Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)CC1 10.1016/s0960-894x(01)00645-x
10283539 167291 0 None -1479 3 Human 6.5 pEC50 = 6.5 Functional
In vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-1 adrenergic receptorIn vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-1 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 -1479 3 Human 6.5 pEC50 = 6.5 Functional
In vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-1 adrenergic receptorIn vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-1 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
9800339 199458 6 None -251 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta-1 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 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta-1 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
24823626 97583 0 None -6 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 410 9 4 4 4.6 O=C(O)c1cccc(Nc2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)c1 10.1021/jm701324c
CHEMBL273098 97583 0 None -6 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 410 9 4 4 4.6 O=C(O)c1cccc(Nc2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)c1 10.1021/jm701324c
155557083 173959 0 None -724 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 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 7.4 pEC50 = 7.4 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 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
145982607 165156 0 None -4 3 Human 7.4 pEC50 = 7.4 Functional
Antagonist activity at human beta1 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 beta1 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 -4 3 Human 7.4 pEC50 = 7.4 Functional
Antagonist activity at human beta1 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 beta1 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
24949566 174290 0 None -281 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 494 8 4 5 5.0 CC(=O)Nc1cc(Oc2ccc3c(c2)C[C@@H](NC[C@H](O)c2cccc(Cl)c2)CC3)cc(C(=O)O)c1 10.1021/jm800222k
CHEMBL456353 174290 0 None -281 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 494 8 4 5 5.0 CC(=O)Nc1cc(Oc2ccc3c(c2)C[C@@H](NC[C@H](O)c2cccc(Cl)c2)CC3)cc(C(=O)O)c1 10.1021/jm800222k
1862 161 14 None -9 2 Guinea pig 4.4 pEC50 = 4.4 Functional
Beta-1 adrenergic receptor agonist activity by stimulation of contraction rate of isolated guinea pig atrial preparationsBeta-1 adrenergic receptor agonist activity by stimulation of contraction rate of isolated guinea pig atrial preparations
ChEMBL 187 2 4 4 0.2 NCC(c1cc(O)c(cc1F)O)O 10.1021/jm00118a019
510 161 14 None -9 2 Guinea pig 4.4 pEC50 = 4.4 Functional
Beta-1 adrenergic receptor agonist activity by stimulation of contraction rate of isolated guinea pig atrial preparationsBeta-1 adrenergic receptor agonist activity by stimulation of contraction rate of isolated guinea pig atrial preparations
ChEMBL 187 2 4 4 0.2 NCC(c1cc(O)c(cc1F)O)O 10.1021/jm00118a019
CHEMBL281232 161 14 None -9 2 Guinea pig 4.4 pEC50 = 4.4 Functional
Beta-1 adrenergic receptor agonist activity by stimulation of contraction rate of isolated guinea pig atrial preparationsBeta-1 adrenergic receptor agonist activity by stimulation of contraction rate of isolated guinea pig atrial preparations
ChEMBL 187 2 4 4 0.2 NCC(c1cc(O)c(cc1F)O)O 10.1021/jm00118a019
24824079 12769 0 None 1 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 441 11 3 5 4.5 O=C(O)COc1ccc(Oc2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)cc1 10.1021/jm701324c
CHEMBL1188934 12769 0 None 1 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 441 11 3 5 4.5 O=C(O)COc1ccc(Oc2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)cc1 10.1021/jm701324c
CHEMBL537693 12769 0 None 1 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 441 11 3 5 4.5 O=C(O)COc1ccc(Oc2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)cc1 10.1021/jm701324c
24895357 185703 0 None -194 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 467 10 3 4 5.7 CC(C)Oc1cc(-c2ccc(C[C@@H](C)NC[C@H](O)c3cccc(Cl)c3)cc2)ccc1C(=O)O 10.1021/jm8000345
CHEMBL487443 185703 0 None -194 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 467 10 3 4 5.7 CC(C)Oc1cc(-c2ccc(C[C@@H](C)NC[C@H](O)c3cccc(Cl)c3)cc2)ccc1C(=O)O 10.1021/jm8000345
42639965 12594 0 None -691 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 534 11 3 5 5.0 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)cc1CC1CCCCC1 10.1021/jm9000709
CHEMBL1187643 12594 0 None -691 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 534 11 3 5 5.0 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)cc1CC1CCCCC1 10.1021/jm9000709
CHEMBL513419 12594 0 None -691 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 534 11 3 5 5.0 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)cc1CC1CCCCC1 10.1021/jm9000709
44457929 84339 0 None -114 3 Human 6.4 pEC50 = 6.4 Functional
Agonistic activity against the cloned human Beta-1 adrenergic receptor was measured by its by its ability to stimulate adenylyl cyclaseAgonistic activity against the cloned human Beta-1 adrenergic receptor was measured by its by its ability to stimulate adenylyl cyclase
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 -114 3 Human 6.4 pEC50 = 6.4 Functional
Agonistic activity against the cloned human Beta-1 adrenergic receptor was measured by its by its ability to stimulate adenylyl cyclaseAgonistic activity against the cloned human Beta-1 adrenergic receptor was measured by its by its ability to stimulate adenylyl cyclase
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
2419 3394 80 None -1621 6 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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 -1621 6 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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 -1621 6 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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 -1621 6 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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 -1621 6 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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
24823130 97242 0 None -38 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 413 8 3 3 4.7 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)cc1F 10.1021/jm701324c
CHEMBL271367 97242 0 None -38 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 413 8 3 3 4.7 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)cc1F 10.1021/jm701324c
44580011 186208 0 None -52 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 468 10 4 5 4.7 CC(=O)Nc1ccc(Oc2cccc(CCNC[C@H](O)c3cccc(Cl)c3)c2)cc1C(=O)O 10.1016/j.bmcl.2008.08.009
CHEMBL489200 186208 0 None -52 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 468 10 4 5 4.7 CC(=O)Nc1ccc(Oc2cccc(CCNC[C@H](O)c3cccc(Cl)c3)c2)cc1C(=O)O 10.1016/j.bmcl.2008.08.009
9997789 185709 0 None -107 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at beta1 adrenoceptor (unknown origin)Agonist activity at beta1 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 5.4 pEC50 = 5.4 Functional
Agonist activity at beta1 adrenoceptor (unknown origin)Agonist activity at beta1 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 5.4 pEC50 = 5.4 Functional
Agonist activity at beta1 adrenoceptor (unknown origin)Agonist activity at beta1 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
24895263 192943 0 None -1122 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 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 -1122 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 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 -1122 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 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 -1122 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 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
319 1292 39 None -43 6 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at adrenergic beta1 receptorAgonist activity at adrenergic beta1 receptor
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 -43 6 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at adrenergic beta1 receptorAgonist activity at adrenergic beta1 receptor
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 -43 6 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at adrenergic beta1 receptorAgonist activity at adrenergic beta1 receptor
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 -43 6 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at adrenergic beta1 receptorAgonist activity at adrenergic beta1 receptor
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 -43 6 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at adrenergic beta1 receptorAgonist activity at adrenergic beta1 receptor
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 -43 6 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at adrenergic beta1 receptorAgonist activity at adrenergic beta1 receptor
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
56670158 63750 0 None -15 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at adrenergic beta1 receptorAgonist activity at adrenergic beta1 receptor
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 7.4 pEC50 = 7.4 Functional
Agonist activity at adrenergic beta1 receptorAgonist activity at adrenergic beta1 receptor
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
16049309 63754 0 None -100 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at adrenergic beta1 receptorAgonist activity at adrenergic beta1 receptor
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 7.4 pEC50 = 7.4 Functional
Agonist activity at adrenergic beta1 receptorAgonist activity at adrenergic beta1 receptor
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
56663238 63756 0 None -251 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at adrenergic beta1 receptorAgonist activity at adrenergic beta1 receptor
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 7.4 pEC50 = 7.4 Functional
Agonist activity at adrenergic beta1 receptorAgonist activity at adrenergic beta1 receptor
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
1239 1639 46 None -109 5 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta1 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 -109 5 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta1 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 -109 5 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta1 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 -109 5 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta1 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 -109 5 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta1 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
3083544 462 46 None -89 4 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta1 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 -89 4 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta1 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 -89 4 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta1 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 -89 4 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta1 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 -89 4 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta1 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
10288976 66232 0 None -251 4 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta1 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 -251 4 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta1 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 -251 4 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta1 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
1239 1639 46 None -109 5 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta-1 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 -109 5 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta-1 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 -109 5 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta-1 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 -109 5 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta-1 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 -109 5 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta-1 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
3083544 462 46 None -89 4 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta-1 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 -89 4 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta-1 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 -89 4 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta-1 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 -89 4 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta-1 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 -89 4 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta-1 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
49861320 54666 0 None -6 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 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 6.4 pEC50 = 6.4 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 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 6.4 pEC50 = 6.4 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 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
44565932 186418 0 None -4897 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 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 -4897 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 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
10305108 110942 0 None -77 3 Human 6.4 pEC50 = 6.4 Functional
In vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-1 adrenergic receptorIn vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-1 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 -77 3 Human 6.4 pEC50 = 6.4 Functional
In vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-1 adrenergic receptorIn vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-1 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
44441233 147512 0 None -100 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 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 -100 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 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
10184665 3916 48 None -44 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta1 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 6.4 pEC50 = 6.4 Functional
Agonist activity at human beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta1 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 6.4 pEC50 = 6.4 Functional
Agonist activity at human beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta1 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 6.4 pEC50 = 6.4 Functional
Agonist activity at human beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta1 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 6.4 pEC50 = 6.4 Functional
Agonist activity at human beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta1 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
10184665 3916 48 None -44 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta-1 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 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta-1 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 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta-1 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 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta-1 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 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta-1 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
11038599 47589 0 None -25 3 Human 6.4 pEC50 = 6.4 Functional
Concentration that causes 50% inhibition of human beta 1 adrenergic receptor (AR), expressed in CHO cells.Concentration that causes 50% inhibition of human beta 1 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 -25 3 Human 6.4 pEC50 = 6.4 Functional
Concentration that causes 50% inhibition of human beta 1 adrenergic receptor (AR), expressed in CHO cells.Concentration that causes 50% inhibition of human beta 1 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
9512 3566 35 None -1000 3 Human 5.4 pEC50 = 5.4 Functional
Activity at human beta-1 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-1 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 -1000 3 Human 5.4 pEC50 = 5.4 Functional
Activity at human beta-1 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-1 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 -1000 3 Human 5.4 pEC50 = 5.4 Functional
Activity at human beta-1 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-1 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 -1000 3 Human 5.4 pEC50 = 5.4 Functional
Activity at human beta-1 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-1 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
44441236 92977 0 None -3162 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 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 -3162 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 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
10298567 65607 0 None -5 2 Human 8.4 pEC50 = 8.4 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptor
ChEMBL 465 12 5 6 3.3 COc1cccc(NC(=O)Nc2ccc(C[C@@H](CO)NC[C@H](O)COc3ccccc3)cc2)c1 10.1016/j.bmcl.2004.11.001
CHEMBL183611 65607 0 None -5 2 Human 8.4 pEC50 = 8.4 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptor
ChEMBL 465 12 5 6 3.3 COc1cccc(NC(=O)Nc2ccc(C[C@@H](CO)NC[C@H](O)COc3ccccc3)cc2)c1 10.1016/j.bmcl.2004.11.001
164625303 187994 0 None -316 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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 8.4 pEC50 = 8.4 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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 8.4 pEC50 = 8.4 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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
164623918 187983 0 None -199 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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 8.4 pEC50 = 8.4 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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 8.4 pEC50 = 8.4 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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
164608750 187864 0 None -181 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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 8.4 pEC50 = 8.4 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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 8.4 pEC50 = 8.4 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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
164615474 187914 0 None -61 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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 8.4 pEC50 = 8.4 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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 8.4 pEC50 = 8.4 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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
164617688 187927 0 None -416 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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 8.4 pEC50 = 8.4 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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 8.4 pEC50 = 8.4 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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
56598967 87819 0 None 2238 3 Human 8.4 pEC50 = 8.4 Functional
Partial agonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsPartial agonist activity at human beta1 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 8.4 pEC50 = 8.4 Functional
Partial agonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsPartial agonist activity at human beta1 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
45101520 197096 0 None -3 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human beta-1 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta-1 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 8.4 pEC50 = 8.4 Functional
Agonist activity at human beta-1 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta-1 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
46232769 199146 0 None -6 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta-1 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 8.4 pEC50 = 8.4 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta-1 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
164614743 187905 0 None -134 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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 8.3 pEC50 = 8.3 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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 8.3 pEC50 = 8.3 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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
45484536 195528 0 None -5 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human beta-1 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta-1 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 8.3 pEC50 = 8.3 Functional
Agonist activity at human beta-1 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta-1 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
559926 96546 5 None 27 2 Guinea pig 8.3 pEC50 = 8.3 Functional
Agonistic activity (beta-1 adrenergic receptor) for the percent maximal increase in contraction rate of isolated guinea pig atriaAgonistic activity (beta-1 adrenergic receptor) for the percent maximal increase in contraction rate of isolated guinea pig atria
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 8.3 pEC50 = 8.3 Functional
Agonistic activity (beta-1 adrenergic receptor) for the percent maximal increase in contraction rate of isolated guinea pig atriaAgonistic activity (beta-1 adrenergic receptor) for the percent maximal increase in contraction rate of isolated guinea pig atria
ChEMBL 255 5 4 5 1.2 CC(C)(C)NCC(O)COc1ccc(O)c(O)c1 10.1021/jm00107a027
45270673 193743 0 None 58 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 406 10 3 5 3.9 O=C(Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1)Oc1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL1203992 193743 0 None 58 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 406 10 3 5 3.9 O=C(Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1)Oc1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL552253 193743 0 None 58 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 406 10 3 5 3.9 O=C(Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1)Oc1ccccc1 10.1016/j.bmc.2009.06.031
45273280 194036 0 None -1 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 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 7.4 pEC50 = 7.4 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 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 7.4 pEC50 = 7.4 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 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
44396513 66375 0 None -30 3 Human 7.4 pEC50 = 7.4 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-1 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-1 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 7.4 pEC50 = 7.4 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-1 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-1 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
10420352 168164 10 None 83 2 Guinea pig 7.4 pEC50 = 7.4 Functional
Agonistic potency at beta-1 adrenergic receptor for the percent maximal increase in contraction rate of isolated guinea pig atriaAgonistic potency at beta-1 adrenergic receptor for the percent maximal increase in contraction rate of isolated guinea pig atria
ChEMBL 201 3 4 4 0.5 CNCC(O)c1ccc(O)c(O)c1F 10.1021/jm00118a019
CHEMBL43711 168164 10 None 83 2 Guinea pig 7.4 pEC50 = 7.4 Functional
Agonistic potency at beta-1 adrenergic receptor for the percent maximal increase in contraction rate of isolated guinea pig atriaAgonistic potency at beta-1 adrenergic receptor for the percent maximal increase in contraction rate of isolated guinea pig atria
ChEMBL 201 3 4 4 0.5 CNCC(O)c1ccc(O)c(O)c1F 10.1021/jm00118a019
10076548 162701 0 None -4 3 Human 7.4 pEC50 = 7.4 Functional
Increased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 1 Adrenergic receptorIncreased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 1 Adrenergic receptor
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 -4 3 Human 7.4 pEC50 = 7.4 Functional
Increased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 1 Adrenergic receptorIncreased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 1 Adrenergic receptor
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
24893966 176155 0 None -724 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 449 12 3 5 4.8 CC(C)COc1cc(-c2ccc(OCCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm8000345
CHEMBL460257 176155 0 None -724 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 449 12 3 5 4.8 CC(C)COc1cc(-c2ccc(OCCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm8000345
44331766 4575 0 None -2 2 Human 6.4 pEC50 = 6.4 Functional
In vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-1 adrenergic receptorIn vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-1 adrenergic receptor
ChEMBL 449 9 3 4 4.3 O[C@@H](CNCC1CCN(CCC(F)(F)F)CC1)COc1cccc2[nH]c3ccccc3c12 10.1016/s0960-894x(02)00607-8
CHEMBL103137 4575 0 None -2 2 Human 6.4 pEC50 = 6.4 Functional
In vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-1 adrenergic receptorIn vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-1 adrenergic receptor
ChEMBL 449 9 3 4 4.3 O[C@@H](CNCC1CCN(CCC(F)(F)F)CC1)COc1cccc2[nH]c3ccccc3c12 10.1016/s0960-894x(02)00607-8
22063464 199315 0 None -10 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta-1 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 7.4 pEC50 = 7.4 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta-1 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
10189730 5190 0 None -426 2 Human 6.4 pEC50 = 6.4 Functional
In vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta1-AR receptorIn vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta1-AR receptor
ChEMBL 647 14 6 8 3.4 CS(=O)(=O)Nc1cc(OC[C@@H](O)CNCCc2ccc(NC3CCN(C(=O)NCc4cc(F)ccc4F)CC3)cc2)ccc1O 10.1016/s0960-894x(01)00645-x
CHEMBL106511 5190 0 None -426 2 Human 6.4 pEC50 = 6.4 Functional
In vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta1-AR receptorIn vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta1-AR receptor
ChEMBL 647 14 6 8 3.4 CS(=O)(=O)Nc1cc(OC[C@@H](O)CNCCc2ccc(NC3CCN(C(=O)NCc4cc(F)ccc4F)CC3)cc2)ccc1O 10.1016/s0960-894x(01)00645-x
145984324 165275 0 None -7 3 Human 6.4 pEC50 = 6.4 Functional
Antagonist activity at human beta1 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 beta1 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 -7 3 Human 6.4 pEC50 = 6.4 Functional
Antagonist activity at human beta1 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 beta1 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
44574723 177938 0 None 1 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 439 11 3 5 3.5 O=C(Cc1cccc(Cl)n1)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.03.044
CHEMBL466726 177938 0 None 1 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 439 11 3 5 3.5 O=C(Cc1cccc(Cl)n1)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.03.044
155567283 175387 0 None -588 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 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 7.4 pEC50 = 7.4 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 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
44377771 164984 0 None -70 3 Human 6.4 pEC50 = 6.4 Functional
Agonistic activity as cAMP accumulation in CHO cells expressing human beta-1-adrenergic receptorAgonistic activity as cAMP accumulation in CHO cells expressing human beta-1-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 -70 3 Human 6.4 pEC50 = 6.4 Functional
Agonistic activity as cAMP accumulation in CHO cells expressing human beta-1-adrenergic receptorAgonistic activity as cAMP accumulation in CHO cells expressing human beta-1-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
1028 287 69 None -3 16 Guinea pig 6.4 pEC50 = 6.4 Functional
Effective dose required to stimulate contractions in isolated guinea pig atrium.Effective dose required to stimulate contractions in isolated guinea pig atrium.
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00019a001
139148732 287 69 None -3 16 Guinea pig 6.4 pEC50 = 6.4 Functional
Effective dose required to stimulate contractions in isolated guinea pig atrium.Effective dose required to stimulate contractions in isolated guinea pig atrium.
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00019a001
479 287 69 None -3 16 Guinea pig 6.4 pEC50 = 6.4 Functional
Effective dose required to stimulate contractions in isolated guinea pig atrium.Effective dose required to stimulate contractions in isolated guinea pig atrium.
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00019a001
5816 287 69 None -3 16 Guinea pig 6.4 pEC50 = 6.4 Functional
Effective dose required to stimulate contractions in isolated guinea pig atrium.Effective dose required to stimulate contractions in isolated guinea pig atrium.
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00019a001
CHEMBL679 287 69 None -3 16 Guinea pig 6.4 pEC50 = 6.4 Functional
Effective dose required to stimulate contractions in isolated guinea pig atrium.Effective dose required to stimulate contractions in isolated guinea pig atrium.
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00019a001
DB00668 287 69 None -3 16 Guinea pig 6.4 pEC50 = 6.4 Functional
Effective dose required to stimulate contractions in isolated guinea pig atrium.Effective dose required to stimulate contractions in isolated guinea pig atrium.
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00019a001
46232856 199648 0 None -128 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta-1 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 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta-1 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
10651147 110181 0 None -10964 3 Human 4.4 pEC50 = 4.4 Functional
Increased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 1 Adrenergic receptorIncreased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 1 Adrenergic receptor
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 -10964 3 Human 4.4 pEC50 = 4.4 Functional
Increased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 1 Adrenergic receptorIncreased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 1 Adrenergic receptor
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
44392542 65516 0 None -6 3 Human 7.4 pEC50 = 7.4 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-1 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-1 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 7.4 pEC50 = 7.4 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-1 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-1 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
11432806 65851 0 None -134 3 Human 7.4 pEC50 = 7.4 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-1 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-1 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 7.4 pEC50 = 7.4 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-1 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-1 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 7.4 pEC50 = 7.4 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-1 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-1 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 7.4 pEC50 = 7.4 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-1 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-1 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
164612025 187883 0 None -2454 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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 7.4 pEC50 = 7.4 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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 7.4 pEC50 = 7.4 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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
24895669 190063 0 None -7079 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 435 10 4 5 4.4 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3cccc(O)c3)cc2)ccc1C(=O)O 10.1021/jm8000345
CHEMBL518168 190063 0 None -7079 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 435 10 4 5 4.4 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3cccc(O)c3)cc2)ccc1C(=O)O 10.1021/jm8000345
44392575 64026 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-1 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-1 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 7.4 pEC50 = 7.4 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-1 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-1 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
52949489 17350 0 None -21 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as 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 -21 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as 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
44268324 16590 0 None -141 3 Human 6.4 pEC50 = 6.4 Functional
Compound was tested for agonist activity against cloned human beta-1 adrenergic receptorCompound was tested for agonist activity against cloned human beta-1 adrenergic receptor
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 -141 3 Human 6.4 pEC50 = 6.4 Functional
Compound was tested for agonist activity against cloned human beta-1 adrenergic receptorCompound was tested for agonist activity against cloned human beta-1 adrenergic receptor
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
10626150 99551 0 None -295 3 Human 5.4 pEC50 = 5.4 Functional
Increased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 1 Adrenergic receptorIncreased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 1 Adrenergic receptor
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 -295 3 Human 5.4 pEC50 = 5.4 Functional
Increased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 1 Adrenergic receptorIncreased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 1 Adrenergic receptor
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
44336180 6376 0 None -15 2 Human 6.3 pEC50 = 6.3 Functional
In vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta1-AR receptorIn vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta1-AR receptor
ChEMBL 554 12 5 6 4.0 O=C(NCc1ccc(F)cc1F)N1CCC(Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)CC1 10.1016/s0960-894x(01)00645-x
CHEMBL108263 6376 0 None -15 2 Human 6.3 pEC50 = 6.3 Functional
In vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta1-AR receptorIn vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta1-AR receptor
ChEMBL 554 12 5 6 4.0 O=C(NCc1ccc(F)cc1F)N1CCC(Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)CC1 10.1016/s0960-894x(01)00645-x
11270071 98520 0 None 1 3 Human 7.3 pEC50 = 7.3 Functional
Agonistic activity against human Beta-1 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonistic activity against human Beta-1 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 1 3 Human 7.3 pEC50 = 7.3 Functional
Agonistic activity against human Beta-1 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonistic activity against human Beta-1 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
24949564 188920 0 None -147 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 452 7 4 5 4.6 Nc1cc(Oc2ccc3c(c2)C[C@@H](NC[C@H](O)c2cccc(Cl)c2)CC3)cc(C(=O)O)c1 10.1021/jm800222k
CHEMBL514094 188920 0 None -147 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 452 7 4 5 4.6 Nc1cc(Oc2ccc3c(c2)C[C@@H](NC[C@H](O)c2cccc(Cl)c2)CC3)cc(C(=O)O)c1 10.1021/jm800222k
24893964 186073 0 None -1862 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 460 10 3 5 5.0 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1OC1CCCCC1 10.1021/jm8000345
CHEMBL488224 186073 0 None -1862 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 460 10 3 5 5.0 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1OC1CCCCC1 10.1021/jm8000345
24893964 186073 0 None -1862 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 460 10 3 5 5.0 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1OC1CCCCC1 10.1021/jm9000709
CHEMBL488224 186073 0 None -1862 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 460 10 3 5 5.0 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1OC1CCCCC1 10.1021/jm9000709
3038500 9235 8 None -831 6 Human 5.3 pEC50 = 5.3 Functional
In vitro functional efficacy in stimulating increase in cAMP in chinese hamster ovary (CHO) cells expressing the cloned human beta-1 receptor.In vitro functional efficacy in stimulating increase in cAMP in chinese hamster ovary (CHO) cells expressing the cloned human beta-1 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 -831 6 Human 5.3 pEC50 = 5.3 Functional
In vitro functional efficacy in stimulating increase in cAMP in chinese hamster ovary (CHO) cells expressing the cloned human beta-1 receptor.In vitro functional efficacy in stimulating increase in cAMP in chinese hamster ovary (CHO) cells expressing the cloned human beta-1 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
10187653 4255 0 None -3 2 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-1 adrenergic receptorIn vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-1 adrenergic receptor
ChEMBL 554 11 5 7 3.5 O=C(Nc1ccccc1)Nc1ccc(S(=O)(=O)N2CCC(CNC[C@H](O)COc3ccc(O)cc3)CC2)cc1 10.1016/s0960-894x(02)00607-8
CHEMBL100970 4255 0 None -3 2 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-1 adrenergic receptorIn vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-1 adrenergic receptor
ChEMBL 554 11 5 7 3.5 O=C(Nc1ccccc1)Nc1ccc(S(=O)(=O)N2CCC(CNC[C@H](O)COc3ccc(O)cc3)CC2)cc1 10.1016/s0960-894x(02)00607-8
44396736 66519 0 None -11 3 Human 7.3 pEC50 = 7.3 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-1 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-1 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 7.3 pEC50 = 7.3 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-1 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-1 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
44127056 193685 0 None 1 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 426 11 4 6 3.2 O=C(Cc1ccsc1)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/j.ejmech.2009.01.022
CHEMBL551892 193685 0 None 1 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 426 11 4 6 3.2 O=C(Cc1ccsc1)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/j.ejmech.2009.01.022
24949420 187522 0 None -51 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 422 6 3 4 4.3 O=C(O)c1ccc(-c2ccc3c(c2)C[C@@H](NC[C@H](O)c2cccc(Cl)c2)CC3)nc1 10.1021/jm800222k
CHEMBL498304 187522 0 None -51 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 422 6 3 4 4.3 O=C(O)c1ccc(-c2ccc3c(c2)C[C@@H](NC[C@H](O)c2cccc(Cl)c2)CC3)nc1 10.1021/jm800222k
42639652 12607 0 None -1513 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 495 11 3 6 3.5 CC(C)Cc1cc(-c2ccc(CCNC[C@H](O)c3cccnc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
CHEMBL1187716 12607 0 None -1513 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 495 11 3 6 3.5 CC(C)Cc1cc(-c2ccc(CCNC[C@H](O)c3cccnc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
CHEMBL516209 12607 0 None -1513 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 495 11 3 6 3.5 CC(C)Cc1cc(-c2ccc(CCNC[C@H](O)c3cccnc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
45483847 195127 0 None -2 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human adrenergic beta 1 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 1 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 8.3 pEC50 = 8.3 Functional
Agonist activity at human adrenergic beta 1 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 1 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
45483816 195450 0 None -12 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human adrenergic beta 1 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 1 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 8.3 pEC50 = 8.3 Functional
Agonist activity at human adrenergic beta 1 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 1 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
52947562 17490 0 None 3 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as 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 3 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as 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
11026016 46422 0 None 1 3 Human 8.3 pEC50 = 8.3 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-1 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-1 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-1 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-1 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
10902809 47798 0 None 1 3 Human 8.3 pEC50 = 8.3 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-1 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-1 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 8.3 pEC50 = 8.3 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-1 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-1 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
2419 3394 80 None -17 6 Guinea pig 8.3 pEC50 = 8.3 Functional
Agonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contractionAgonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contraction
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/jm801016j
5152 3394 80 None -17 6 Guinea pig 8.3 pEC50 = 8.3 Functional
Agonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contractionAgonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contraction
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/jm801016j
559 3394 80 None -17 6 Guinea pig 8.3 pEC50 = 8.3 Functional
Agonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contractionAgonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contraction
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/jm801016j
CHEMBL1263 3394 80 None -17 6 Guinea pig 8.3 pEC50 = 8.3 Functional
Agonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contractionAgonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contraction
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/jm801016j
DB00938 3394 80 None -17 6 Guinea pig 8.3 pEC50 = 8.3 Functional
Agonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contractionAgonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contraction
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/jm801016j
155543358 174191 0 None -102 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 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 8.3 pEC50 = 8.3 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 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
45484568 196663 0 None -10 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human beta-1 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta-1 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 8.3 pEC50 = 8.3 Functional
Agonist activity at human beta-1 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta-1 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
45483843 195350 0 None -9 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human adrenergic beta 1 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 1 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 8.3 pEC50 = 8.3 Functional
Agonist activity at human adrenergic beta 1 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 1 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
45484569 195947 0 None -4 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human beta-1 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta-1 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 8.2 pEC50 = 8.2 Functional
Agonist activity at human beta-1 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta-1 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
45268128 194638 0 None -1 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 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 7.3 pEC50 = 7.3 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 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 7.3 pEC50 = 7.3 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 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
10233153 4150 0 None -5 3 Human 7.3 pEC50 = 7.3 Functional
Beta-1 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-1-adrenoceptorBeta-1 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-1-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 -5 3 Human 7.3 pEC50 = 7.3 Functional
Beta-1 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-1-adrenoceptorBeta-1 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-1-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
10553602 126618 0 None -1 3 Human 7.3 pEC50 = 7.3 Functional
Increased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 1 Adrenergic receptorIncreased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 1 Adrenergic receptor
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 7.3 pEC50 = 7.3 Functional
Increased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 1 Adrenergic receptorIncreased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 1 Adrenergic receptor
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
9893058 66035 0 None -39 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta1 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 7.3 pEC50 = 7.3 Functional
Agonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta1 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 7.3 pEC50 = 7.3 Functional
Agonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta1 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
56678849 66278 0 None -63 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta1 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 -63 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta1 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 -63 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta1 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
56675663 66241 0 None -50 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta1 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 -50 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta1 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 -50 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta1 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
46833102 14076 0 None -31 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta-1 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 7.3 pEC50 = 7.3 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta-1 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 7.3 pEC50 = 7.3 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta-1 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
44574913 177991 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 526 15 2 6 4.5 CCCN(C(=O)Cc1nccn1Cc1ccccc1)c1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.03.044
CHEMBL467117 177991 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 526 15 2 6 4.5 CCCN(C(=O)Cc1nccn1Cc1ccccc1)c1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.03.044
24895667 176267 0 None -208 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 453 10 3 4 5.4 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3ccc(Cl)cc3)cc2)ccc1C(=O)O 10.1021/jm8000345
CHEMBL461282 176267 0 None -208 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 453 10 3 4 5.4 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3ccc(Cl)cc3)cc2)ccc1C(=O)O 10.1021/jm8000345
10003858 188496 0 None -3548 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 449 10 4 5 4.8 CC(C)Oc1cc(-c2ccc(CCN[C@@H](C)[C@H](O)c3ccc(O)cc3)cc2)ccc1C(=O)O 10.1021/jm8000345
CHEMBL510100 188496 0 None -3548 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 449 10 4 5 4.8 CC(C)Oc1cc(-c2ccc(CCN[C@@H](C)[C@H](O)c3ccc(O)cc3)cc2)ccc1C(=O)O 10.1021/jm8000345
42625513 12437 0 None -1000 4 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta-1 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 -1000 4 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta-1 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 -1000 4 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta-1 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
42625515 12606 0 None -794 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta-1 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 6.3 pEC50 = 6.3 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta-1 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 6.3 pEC50 = 6.3 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta-1 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
11718543 165268 0 None -125 3 Human 5.3 pEC50 = 5.3 Functional
Activity at human beta-1 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-1 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 -125 3 Human 5.3 pEC50 = 5.3 Functional
Activity at human beta-1 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-1 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
9801145 92976 0 None -630 3 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 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 -630 3 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 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
11605652 12433 0 None -501 3 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta-1 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 5.3 pEC50 = 5.3 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta-1 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 5.3 pEC50 = 5.3 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta-1 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
44392240 63973 0 None -6 2 Human 7.3 pEC50 = 7.3 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptor
ChEMBL 401 12 5 5 2.2 CCCNC(=O)Nc1ccc(C[C@@H](CO)NC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmcl.2004.11.001
CHEMBL181115 63973 0 None -6 2 Human 7.3 pEC50 = 7.3 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptor
ChEMBL 401 12 5 5 2.2 CCCNC(=O)Nc1ccc(C[C@@H](CO)NC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmcl.2004.11.001
44580010 186207 0 None -46 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 441 10 3 5 4.7 COc1ccc(Oc2cccc(CCNC[C@H](O)c3cccc(Cl)c3)c2)cc1C(=O)O 10.1016/j.bmcl.2008.08.009
CHEMBL489199 186207 0 None -46 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 441 10 3 5 4.7 COc1ccc(Oc2cccc(CCNC[C@H](O)c3cccc(Cl)c3)c2)cc1C(=O)O 10.1016/j.bmcl.2008.08.009
24894319 189257 0 None -213 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 435 11 3 5 4.5 CC(C)Oc1cc(-c2ccc(OCCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm8000345
CHEMBL516785 189257 0 None -213 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 435 11 3 5 4.5 CC(C)Oc1cc(-c2ccc(OCCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm8000345
10202842 163596 0 None -16 2 Human 6.3 pEC50 = 6.3 Functional
In vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta1-AR receptorIn vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta1-AR receptor
ChEMBL 428 10 5 6 1.9 NC(=O)N1CCC(Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)CC1 10.1016/s0960-894x(01)00645-x
CHEMBL421030 163596 0 None -16 2 Human 6.3 pEC50 = 6.3 Functional
In vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta1-AR receptorIn vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta1-AR receptor
ChEMBL 428 10 5 6 1.9 NC(=O)N1CCC(Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)CC1 10.1016/s0960-894x(01)00645-x
24895561 176269 0 None -194 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 509 11 3 5 6.1 O=C(O)c1ccc(-c2ccc(OCCNC[C@H](O)c3cccc(Cl)c3)cc2)cc1OC1CCCCC1 10.1021/jm8000345
CHEMBL461301 176269 0 None -194 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 509 11 3 5 6.1 O=C(O)c1ccc(-c2ccc(OCCNC[C@H](O)c3cccc(Cl)c3)cc2)cc1OC1CCCCC1 10.1021/jm8000345
44331443 4368 0 None -26 3 Human 6.3 pEC50 = 6.3 Functional
Beta-1 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-1-adrenoceptorBeta-1 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-1-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 -26 3 Human 6.3 pEC50 = 6.3 Functional
Beta-1 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-1-adrenoceptorBeta-1 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-1-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
44331351 206390 0 None -16 3 Human 6.3 pEC50 = 6.3 Functional
Beta-1 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-1-adrenoceptorBeta-1 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-1-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 -16 3 Human 6.3 pEC50 = 6.3 Functional
Beta-1 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-1-adrenoceptorBeta-1 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-1-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
10209574 5351 0 None -22 2 Human 6.3 pEC50 = 6.3 Functional
In vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta1-AR receptorIn vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta1-AR receptor
ChEMBL 554 12 5 6 4.0 O=C(NCc1cc(F)ccc1F)N1CCC(Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)CC1 10.1016/s0960-894x(01)00645-x
CHEMBL107382 5351 0 None -22 2 Human 6.3 pEC50 = 6.3 Functional
In vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta1-AR receptorIn vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta1-AR receptor
ChEMBL 554 12 5 6 4.0 O=C(NCc1cc(F)ccc1F)N1CCC(Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)CC1 10.1016/s0960-894x(01)00645-x
10304565 106880 0 None -11 2 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-1 adrenergic receptorIn vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-1 adrenergic receptor
ChEMBL 622 12 5 7 3.6 O=C(NCc1cc(F)ccc1F)Nc1ccc(S(=O)(=O)N2CCC(CNC[C@H](O)COc3ccc(O)c(F)c3)CC2)cc1 10.1016/s0960-894x(02)00607-8
CHEMBL317809 106880 0 None -11 2 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-1 adrenergic receptorIn vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-1 adrenergic receptor
ChEMBL 622 12 5 7 3.6 O=C(NCc1cc(F)ccc1F)Nc1ccc(S(=O)(=O)N2CCC(CNC[C@H](O)COc3ccc(O)c(F)c3)CC2)cc1 10.1016/s0960-894x(02)00607-8
44396577 66603 0 None -25 3 Human 7.3 pEC50 = 7.3 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-1 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-1 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 7.3 pEC50 = 7.3 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-1 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-1 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
24822817 94838 0 None -120 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 493 10 3 4 6.3 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)cc1OC1CCCCC1 10.1021/jm701324c
CHEMBL256418 94838 0 None -120 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 493 10 3 4 6.3 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)cc1OC1CCCCC1 10.1021/jm701324c
24822817 94838 0 None -120 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 493 10 3 4 6.3 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)cc1OC1CCCCC1 10.1021/jm8000345
CHEMBL256418 94838 0 None -120 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 493 10 3 4 6.3 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)cc1OC1CCCCC1 10.1021/jm8000345
24822817 94838 0 None -120 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 493 10 3 4 6.3 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)cc1OC1CCCCC1 10.1021/jm9000709
CHEMBL256418 94838 0 None -120 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 493 10 3 4 6.3 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)cc1OC1CCCCC1 10.1021/jm9000709
44237613 57910 0 None -2754 2 Rat 6.3 pEC50 = 6.3 Functional
Agonist activity at beta1 adrenoceptor in rat left atria assessed as induction of ionotropic effectAgonist activity at beta1 adrenoceptor in rat left atria assessed as induction of ionotropic effect
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 Rat 6.3 pEC50 = 6.3 Functional
Agonist activity at beta1 adrenoceptor in rat left atria assessed as induction of ionotropic effectAgonist activity at beta1 adrenoceptor in rat left atria assessed as induction of ionotropic effect
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
44580009 186209 0 None -42 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 425 9 3 4 5.0 Cc1ccc(Oc2cccc(CCNC[C@H](O)c3cccc(Cl)c3)c2)cc1C(=O)O 10.1016/j.bmcl.2008.08.009
CHEMBL489201 186209 0 None -42 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 425 9 3 4 5.0 Cc1ccc(Oc2cccc(CCNC[C@H](O)c3cccc(Cl)c3)c2)cc1C(=O)O 10.1016/j.bmcl.2008.08.009
44127575 193146 0 None -1 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 426 11 4 6 3.2 O=C(Cc1cccs1)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/j.ejmech.2009.01.022
CHEMBL539226 193146 0 None -1 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 426 11 4 6 3.2 O=C(Cc1cccs1)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/j.ejmech.2009.01.022
45270391 193773 0 None -1 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 459 11 4 6 3.8 O=C(CC1C=Nc2ccccc21)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/j.ejmech.2009.01.022
CHEMBL552434 193773 0 None -1 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 459 11 4 6 3.8 O=C(CC1C=Nc2ccccc21)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/j.ejmech.2009.01.022
45273276 194001 0 None -2 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
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 7.3 pEC50 = 7.3 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
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 7.3 pEC50 = 7.3 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
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
24822472 96951 0 None -38 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 409 8 3 3 4.9 Cc1cc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)ccc1C(=O)O 10.1021/jm701324c
CHEMBL269920 96951 0 None -38 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 409 8 3 3 4.9 Cc1cc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)ccc1C(=O)O 10.1021/jm701324c
44237670 57914 0 None -8128 2 Rat 5.2 pEC50 = 5.2 Functional
Agonist activity at beta1 adrenoceptor in rat left atria assessed as induction of ionotropic effectAgonist activity at beta1 adrenoceptor in rat left atria assessed as induction of ionotropic effect
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 Rat 5.2 pEC50 = 5.2 Functional
Agonist activity at beta1 adrenoceptor in rat left atria assessed as induction of ionotropic effectAgonist activity at beta1 adrenoceptor in rat left atria assessed as induction of ionotropic effect
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
44396737 66509 0 None -47 3 Human 7.2 pEC50 = 7.2 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-1 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-1 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 -47 3 Human 7.2 pEC50 = 7.2 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-1 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-1 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
44444173 93534 0 None -8 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP levelAgonist activity at human beta-1 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 -8 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP levelAgonist activity at human beta-1 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
44331426 4342 0 None -114 3 Human 6.2 pEC50 = 6.2 Functional
Beta-1 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-1-adrenoceptorBeta-1 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-1-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 -114 3 Human 6.2 pEC50 = 6.2 Functional
Beta-1 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-1-adrenoceptorBeta-1 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-1-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
44127048 193675 0 None 1 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 436 11 5 6 2.6 O=C(Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1)C(O)c1ccccc1 10.1016/j.ejmech.2009.01.022
CHEMBL551832 193675 0 None 1 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 436 11 5 6 2.6 O=C(Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1)C(O)c1ccccc1 10.1016/j.ejmech.2009.01.022
1499 2052 43 None -60 36 Guinea pig 8.2 pEC50 = 8.2 Functional
Agonistic activity (beta-1 adrenergic receptor) for the percent maximal increase in contraction rate of isolated guinea pig atriaAgonistic activity (beta-1 adrenergic receptor) for the percent maximal increase in contraction rate of isolated guinea pig atria
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm00107a027
3779 2052 43 None -60 36 Guinea pig 8.2 pEC50 = 8.2 Functional
Agonistic activity (beta-1 adrenergic receptor) for the percent maximal increase in contraction rate of isolated guinea pig atriaAgonistic activity (beta-1 adrenergic receptor) for the percent maximal increase in contraction rate of isolated guinea pig atria
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm00107a027
536 2052 43 None -60 36 Guinea pig 8.2 pEC50 = 8.2 Functional
Agonistic activity (beta-1 adrenergic receptor) for the percent maximal increase in contraction rate of isolated guinea pig atriaAgonistic activity (beta-1 adrenergic receptor) for the percent maximal increase in contraction rate of isolated guinea pig atria
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm00107a027
CHEMBL434 2052 43 None -60 36 Guinea pig 8.2 pEC50 = 8.2 Functional
Agonistic activity (beta-1 adrenergic receptor) for the percent maximal increase in contraction rate of isolated guinea pig atriaAgonistic activity (beta-1 adrenergic receptor) for the percent maximal increase in contraction rate of isolated guinea pig atria
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm00107a027
DB01064 2052 43 None -60 36 Guinea pig 8.2 pEC50 = 8.2 Functional
Agonistic activity (beta-1 adrenergic receptor) for the percent maximal increase in contraction rate of isolated guinea pig atriaAgonistic activity (beta-1 adrenergic receptor) for the percent maximal increase in contraction rate of isolated guinea pig atria
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm00107a027
24936491 17323 0 None -2 3 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as 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 -2 3 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as 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
9845282 75584 0 None -63 3 Human 8.2 pEC50 = 8.2 Functional
Activity at human beta-1 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-1 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 -63 3 Human 8.2 pEC50 = 8.2 Functional
Activity at human beta-1 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-1 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
155564079 174828 0 None -97 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 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 8.2 pEC50 = 8.2 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 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
56943515 111939 0 None -7 3 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta1 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 8.2 pEC50 = 8.2 Functional
Agonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta1 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
11169365 112007 0 None -22 3 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta1 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 8.2 pEC50 = 8.2 Functional
Agonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta1 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
164612262 187885 0 None -190 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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 8.2 pEC50 = 8.2 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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 8.2 pEC50 = 8.2 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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
5493324 98432 18 None -208 3 Human 8.2 pEC50 = 8.2 Functional
Agonistic activity against human Beta-1 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonistic activity against human Beta-1 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 -208 3 Human 8.2 pEC50 = 8.2 Functional
Agonistic activity against human Beta-1 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonistic activity against human Beta-1 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
24822972 97069 0 None 1 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 425 9 3 4 4.6 COc1cc(CCNC[C@H](O)c2cccc(Cl)c2)ccc1-c1ccc(C(=O)O)cc1 10.1021/jm701324c
CHEMBL270460 97069 0 None 1 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 425 9 3 4 4.6 COc1cc(CCNC[C@H](O)c2cccc(Cl)c2)ccc1-c1ccc(C(=O)O)cc1 10.1021/jm701324c
52948056 17322 0 None 1 3 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as 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 1 3 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as 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
45483844 196709 0 None -4 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human adrenergic beta 1 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 1 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 8.2 pEC50 = 8.2 Functional
Agonist activity at human adrenergic beta 1 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 1 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
155513474 169162 0 None -83 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 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 8.2 pEC50 = 8.2 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 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
164618278 187932 0 None -389 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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 8.2 pEC50 = 8.2 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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 8.2 pEC50 = 8.2 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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
45271518 193404 0 None -6 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 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 7.2 pEC50 = 7.2 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 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 7.2 pEC50 = 7.2 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 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
45270690 193441 0 None -3 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 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 7.2 pEC50 = 7.2 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 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 7.2 pEC50 = 7.2 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 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
45273281 194055 0 None -1 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 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 7.2 pEC50 = 7.2 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 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 7.2 pEC50 = 7.2 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 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
10008017 99397 5 None -7 3 Human 7.2 pEC50 = 7.2 Functional
Increased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 1 Adrenergic receptorIncreased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 1 Adrenergic receptor
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 -7 3 Human 7.2 pEC50 = 7.2 Functional
Increased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 1 Adrenergic receptorIncreased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 1 Adrenergic receptor
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
44127782 194990 0 None -1 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 470 11 4 5 4.3 O=C(Cc1cccc2ccccc12)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/j.ejmech.2009.01.022
CHEMBL564556 194990 0 None -1 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 470 11 4 5 4.3 O=C(Cc1cccc2ccccc12)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/j.ejmech.2009.01.022
52944986 17416 0 None -72 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as 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 -72 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as 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
10187201 5095 0 None -77 2 Human 6.2 pEC50 = 6.2 Functional
In vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta1-AR receptorIn vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta1-AR receptor
ChEMBL 540 17 5 6 4.9 CCCCCCCCNC(=O)N1CCC(Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)CC1 10.1016/s0960-894x(01)00645-x
CHEMBL106022 5095 0 None -77 2 Human 6.2 pEC50 = 6.2 Functional
In vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta1-AR receptorIn vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta1-AR receptor
ChEMBL 540 17 5 6 4.9 CCCCCCCCNC(=O)N1CCC(Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)CC1 10.1016/s0960-894x(01)00645-x
44312924 164263 0 None -123 3 Human 5.2 pEC50 = 5.2 Functional
Compound was evaluated for its inhibitory activity against human beta-1 adrenergic receptor (AR)Compound was evaluated for its inhibitory activity against human beta-1 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 -123 3 Human 5.2 pEC50 = 5.2 Functional
Compound was evaluated for its inhibitory activity against human beta-1 adrenergic receptor (AR)Compound was evaluated for its inhibitory activity against human beta-1 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
44219641 177854 0 None -5 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 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 -5 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 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
24895791 186048 0 None -199 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 419 10 3 4 4.7 CCOc1cc(-c2ccc(C[C@@H](C)NC[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm8000345
CHEMBL488051 186048 0 None -199 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 419 10 3 4 4.7 CCOc1cc(-c2ccc(C[C@@H](C)NC[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm8000345
44580040 186527 0 None -389 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 510 10 4 5 5.7 CC(C)(C)C(=O)Nc1ccc(Oc2cccc(CCNC[C@H](O)c3cccc(Cl)c3)c2)cc1C(=O)O 10.1016/j.bmcl.2008.08.009
CHEMBL491645 186527 0 None -389 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 510 10 4 5 5.7 CC(C)(C)C(=O)Nc1ccc(Oc2cccc(CCNC[C@H](O)c3cccc(Cl)c3)c2)cc1C(=O)O 10.1016/j.bmcl.2008.08.009
24950560 172165 0 None -16 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 421 6 3 3 4.9 O=C(O)c1ccc(-c2ccc3c(c2)C[C@@H](NC[C@H](O)c2ccccc2Cl)CC3)cc1 10.1021/jm800222k
CHEMBL450842 172165 0 None -16 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 421 6 3 3 4.9 O=C(O)c1ccc(-c2ccc3c(c2)C[C@@H](NC[C@H](O)c2ccccc2Cl)CC3)cc1 10.1021/jm800222k
145984042 165112 0 None -1348 3 Human 5.2 pEC50 = 5.2 Functional
Antagonist activity at human beta1 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 beta1 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 -1348 3 Human 5.2 pEC50 = 5.2 Functional
Antagonist activity at human beta1 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 beta1 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
24824225 12699 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 454 11 3 5 4.4 CN(c1ccc(CCNC[C@H](O)c2cccc(Cl)c2)cc1)c1ccc(OCC(=O)O)cc1 10.1021/jm701324c
CHEMBL1188359 12699 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 454 11 3 5 4.4 CN(c1ccc(CCNC[C@H](O)c2cccc(Cl)c2)cc1)c1ccc(OCC(=O)O)cc1 10.1021/jm701324c
CHEMBL536108 12699 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 454 11 3 5 4.4 CN(c1ccc(CCNC[C@H](O)c2cccc(Cl)c2)cc1)c1ccc(OCC(=O)O)cc1 10.1021/jm701324c
10092953 97572 0 None -34 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 409 8 3 3 4.9 Cc1cc(C(=O)O)ccc1-c1ccc(CCNC[C@H](O)c2cccc(Cl)c2)cc1 10.1021/jm701324c
CHEMBL273028 97572 0 None -34 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 409 8 3 3 4.9 Cc1cc(C(=O)O)ccc1-c1ccc(CCNC[C@H](O)c2cccc(Cl)c2)cc1 10.1021/jm701324c
16049376 63755 0 None -44 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at adrenergic beta1 receptorAgonist activity at adrenergic beta1 receptor
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 7.2 pEC50 = 7.2 Functional
Agonist activity at adrenergic beta1 receptorAgonist activity at adrenergic beta1 receptor
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
10238776 66128 0 None -79 4 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta1 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 -79 4 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta1 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 -79 4 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta1 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
24900689 70005 0 None -112 5 Human 7.2 pEC50 = 7.2 Functional
Binding affinity to beta1 adrenoceptor expressed in CHO cells by cAMP accumulation assayBinding affinity to beta1 adrenoceptor expressed in CHO cells by cAMP accumulation assay
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 -112 5 Human 7.2 pEC50 = 7.2 Functional
Binding affinity to beta1 adrenoceptor expressed in CHO cells by cAMP accumulation assayBinding affinity to beta1 adrenoceptor expressed in CHO cells by cAMP accumulation assay
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
11002571 47820 0 None 1 3 Human 6.2 pEC50 = 6.2 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-1 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-1 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 1 3 Human 6.2 pEC50 = 6.2 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-1 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-1 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
10346448 119312 0 None -891 3 Human 6.2 pEC50 = 6.2 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-1 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-1 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 -891 3 Human 6.2 pEC50 = 6.2 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-1 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-1 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
11647543 137695 0 None -2511 3 Human 6.2 pEC50 = 6.2 Functional
Activity at human beta-1 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-1 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 -2511 3 Human 6.2 pEC50 = 6.2 Functional
Activity at human beta-1 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-1 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
145987168 166651 0 None -316 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 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 6.2 pEC50 = 6.2 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 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
42625897 12355 0 None -501 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta-1 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 6.2 pEC50 = 6.2 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta-1 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 6.2 pEC50 = 6.2 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta-1 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
42625821 12422 0 None -630 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta-1 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 6.2 pEC50 = 6.2 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta-1 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 6.2 pEC50 = 6.2 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta-1 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
44237614 57911 0 None -31622 2 Rat 5.2 pEC50 = 5.2 Functional
Agonist activity at beta1 adrenoceptor in rat left atria assessed as induction of ionotropic effectAgonist activity at beta1 adrenoceptor in rat left atria assessed as induction of ionotropic effect
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 Rat 5.2 pEC50 = 5.2 Functional
Agonist activity at beta1 adrenoceptor in rat left atria assessed as induction of ionotropic effectAgonist activity at beta1 adrenoceptor in rat left atria assessed as induction of ionotropic effect
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
44331444 4190 0 None -524 3 Human 5.2 pEC50 = 5.2 Functional
Beta-1 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-1-adrenoceptorBeta-1 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-1-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 -524 3 Human 5.2 pEC50 = 5.2 Functional
Beta-1 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-1-adrenoceptorBeta-1 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-1-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
24824226 96980 0 None -1 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 439 11 3 4 4.3 O=C(O)COc1ccc(Cc2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)cc1 10.1021/jm701324c
CHEMBL270027 96980 0 None -1 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 439 11 3 4 4.3 O=C(O)COc1ccc(Cc2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)cc1 10.1021/jm701324c
44579925 183733 0 None -6 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 445 9 3 4 5.4 O=C(O)c1cc(Oc2cccc(CCNC[C@H](O)c3cccc(Cl)c3)c2)ccc1Cl 10.1016/j.bmcl.2008.08.009
CHEMBL484265 183733 0 None -6 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 445 9 3 4 5.4 O=C(O)c1cc(Oc2cccc(CCNC[C@H](O)c3cccc(Cl)c3)c2)ccc1Cl 10.1016/j.bmcl.2008.08.009
45483849 195491 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human adrenergic beta 1 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 1 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 388 6 3 3 4.5 CC(C)(Cc1cc(F)cc(F)c1)NCC(O)c1cc(Cl)c(N)c(Cl)c1 10.1016/j.bmcl.2009.10.013
CHEMBL568060 195491 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human adrenergic beta 1 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 1 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 388 6 3 3 4.5 CC(C)(Cc1cc(F)cc(F)c1)NCC(O)c1cc(Cl)c(N)c(Cl)c1 10.1016/j.bmcl.2009.10.013
24936488 17452 0 None -3 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as 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 -3 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as 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
44574759 177983 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 470 12 3 6 3.6 O=C(Cc1nccn1-c1ccccc1)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.03.044
CHEMBL467082 177983 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 470 12 3 6 3.6 O=C(Cc1nccn1-c1ccccc1)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.03.044
24950570 174847 0 None -794 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 439 6 3 3 5.0 O=C(O)c1ccc(-c2ccc3c(c2)C[C@@H](NC[C@H](O)c2ccc(Cl)cc2)CC3)cc1F 10.1021/jm800222k
CHEMBL457629 174847 0 None -794 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 439 6 3 3 5.0 O=C(O)c1ccc(-c2ccc3c(c2)C[C@@H](NC[C@H](O)c2ccc(Cl)cc2)CC3)cc1F 10.1021/jm800222k
44396532 66408 0 None -42 3 Human 7.2 pEC50 = 7.2 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-1 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-1 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 7.2 pEC50 = 7.2 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-1 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-1 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
44127478 193534 0 None 1 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 435 11 5 6 2.6 NC(C(=O)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1)c1ccccc1 10.1016/j.ejmech.2009.01.022
CHEMBL550743 193534 0 None 1 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 435 11 5 6 2.6 NC(C(=O)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1)c1ccccc1 10.1016/j.ejmech.2009.01.022
2419 3394 80 None -1621 6 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human beta1 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technologyAgonist activity at human beta1 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 -1621 6 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human beta1 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technologyAgonist activity at human beta1 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 -1621 6 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human beta1 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technologyAgonist activity at human beta1 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 -1621 6 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human beta1 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technologyAgonist activity at human beta1 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 -1621 6 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human beta1 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technologyAgonist activity at human beta1 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
24950053 187394 0 None -117 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 443 7 3 5 5.1 O=C(O)c1ccc(Oc2ccc3c(c2)C[C@@H](NC[C@H](O)c2cccc(Cl)c2)CC3)s1 10.1021/jm800222k
CHEMBL497280 187394 0 None -117 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 443 7 3 5 5.1 O=C(O)c1ccc(Oc2ccc3c(c2)C[C@@H](NC[C@H](O)c2cccc(Cl)c2)CC3)s1 10.1021/jm800222k
24950236 188474 0 None -89 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 534 9 4 5 6.8 O=C(O)c1cc(NC2CCCCC2)cc(Oc2ccc3c(c2)C[C@@H](NC[C@H](O)c2cccc(Cl)c2)CC3)c1 10.1021/jm800222k
CHEMBL509729 188474 0 None -89 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 534 9 4 5 6.8 O=C(O)c1cc(NC2CCCCC2)cc(Oc2ccc3c(c2)C[C@@H](NC[C@H](O)c2cccc(Cl)c2)CC3)c1 10.1021/jm800222k
44579649 186374 0 None -12 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 408 10 3 6 3.4 COc1ccc(Oc2cccc(CCNC[C@H](O)c3cccnc3)c2)cc1C(=O)O 10.1016/j.bmcl.2008.08.009
CHEMBL490415 186374 0 None -12 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 408 10 3 6 3.4 COc1ccc(Oc2cccc(CCNC[C@H](O)c3cccnc3)c2)cc1C(=O)O 10.1016/j.bmcl.2008.08.009
11224275 172912 0 None -1621 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 433 11 3 4 5.1 CCCOc1cc(-c2ccc(CCN[C@@H](C)[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm8000345
CHEMBL453048 172912 0 None -1621 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 433 11 3 4 5.1 CCCOc1cc(-c2ccc(CCN[C@@H](C)[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm8000345
45483839 195248 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human adrenergic beta 1 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 1 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 380 7 3 3 4.8 CCc1ccc(CC(C)(C)NCC(O)c2cc(Cl)c(N)c(Cl)c2)cc1 10.1016/j.bmcl.2009.10.013
CHEMBL566353 195248 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human adrenergic beta 1 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 1 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 380 7 3 3 4.8 CCc1ccc(CC(C)(C)NCC(O)c2cc(Cl)c(N)c(Cl)c2)cc1 10.1016/j.bmcl.2009.10.013
45483852 195072 0 None -14 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human adrenergic beta 1 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 1 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 8.1 pEC50 = 8.1 Functional
Agonist activity at human adrenergic beta 1 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 1 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
155564766 174906 0 None -181 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 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 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 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
12578 921 55 None 1348 3 Human 8.1 pEC50 = 8.1 Functional
Partial agonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsPartial agonist activity at human beta1 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 8.1 pEC50 = 8.1 Functional
Partial agonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsPartial agonist activity at human beta1 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 8.1 pEC50 = 8.1 Functional
Partial agonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsPartial agonist activity at human beta1 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
164620479 187949 0 None -288 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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
145985242 164982 0 None -6 3 Human 8.1 pEC50 = 8.1 Functional
Antagonist activity at human beta1 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 beta1 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 -6 3 Human 8.1 pEC50 = 8.1 Functional
Antagonist activity at human beta1 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 beta1 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
164617235 187924 0 None -251 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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
11810896 118964 0 None -2 3 Human 8.1 pEC50 = 8.1 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-1 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-1 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 8.1 pEC50 = 8.1 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-1 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-1 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
1499 2052 43 None -64 36 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta1 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 -64 36 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta1 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 -64 36 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta1 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 -64 36 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta1 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 -64 36 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta1 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
9871386 111766 4 None -35 4 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta1 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 -35 4 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta1 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
66796015 111955 0 None -35 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta1 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 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta1 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
56943518 111956 0 None -25 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta1 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 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta1 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
56943545 111957 0 None -28 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta1 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 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta1 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
56943546 111973 0 None -25 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta1 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 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta1 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
56943517 111999 0 None -3 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta1 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 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta1 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
1499 2052 43 None -64 36 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta1 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 -64 36 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta1 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 -64 36 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta1 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 -64 36 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta1 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 -64 36 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta1 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
56678973 66231 0 None -7 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta1 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 -7 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta1 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 -7 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta1 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
56658407 66290 0 None -15 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta1 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 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta1 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 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta1 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
1499 2052 43 None -64 36 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta-1 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 -64 36 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta-1 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 -64 36 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta-1 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 -64 36 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta-1 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 -64 36 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta-1 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 -64 36 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta-1 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 -64 36 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta-1 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 -64 36 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta-1 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 -64 36 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta-1 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 -64 36 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta-1 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
10225563 14079 0 None -19 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta-1 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 -19 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta-1 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 -19 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta-1 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
9871386 111766 4 None -35 4 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human recombinant beta1 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta1 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 -35 4 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human recombinant beta1 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta1 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
45271517 193371 0 None -3 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 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 7.2 pEC50 = 7.2 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 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 7.2 pEC50 = 7.2 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 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
45272431 193429 0 None -6 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 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 7.2 pEC50 = 7.2 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 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 7.2 pEC50 = 7.2 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 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
44517694 193491 0 None -3 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 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 7.2 pEC50 = 7.2 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 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 7.2 pEC50 = 7.2 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 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 7.2 pEC50 = 7.2 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 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 7.2 pEC50 = 7.2 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 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 7.2 pEC50 = 7.2 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 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
24949891 187575 0 None -46 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 438 7 3 5 4.4 O=C(O)c1ccc(Oc2ccc3c(c2)C[C@@H](NC[C@H](O)c2cccc(Cl)c2)CC3)nc1 10.1021/jm800222k
CHEMBL498703 187575 0 None -46 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 438 7 3 5 4.4 O=C(O)c1ccc(Oc2ccc3c(c2)C[C@@H](NC[C@H](O)c2cccc(Cl)c2)CC3)nc1 10.1021/jm800222k
24937269 17450 0 None -2 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as 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 -2 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as 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
44127481 194468 0 None -1 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 450 12 4 6 3.2 COc1cccc(CC(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)c1 10.1016/j.ejmech.2009.01.022
CHEMBL561211 194468 0 None -1 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 450 12 4 6 3.2 COc1cccc(CC(=O)Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)c1 10.1016/j.ejmech.2009.01.022
11189433 199189 0 None -57 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta-1 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 6.2 pEC50 = 6.2 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta-1 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
44396779 66711 0 None -17 3 Human 7.1 pEC50 = 7.1 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-1 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-1 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 7.1 pEC50 = 7.1 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-1 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-1 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
155551133 173414 0 None -446 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 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 7.1 pEC50 = 7.1 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 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
24823127 97481 0 None -724 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 453 10 3 4 5.4 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)ccc1C(=O)O 10.1021/jm701324c
CHEMBL272584 97481 0 None -724 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 453 10 3 4 5.4 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)ccc1C(=O)O 10.1021/jm701324c
24823127 97481 0 None -724 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 453 10 3 4 5.4 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)ccc1C(=O)O 10.1016/j.bmcl.2008.08.009
CHEMBL272584 97481 0 None -724 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 453 10 3 4 5.4 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)ccc1C(=O)O 10.1016/j.bmcl.2008.08.009
44127050 194988 0 None 1 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 454 11 4 5 3.8 O=C(Cc1ccccc1Cl)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/j.ejmech.2009.01.022
CHEMBL564544 194988 0 None 1 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 454 11 4 5 3.8 O=C(Cc1ccccc1Cl)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/j.ejmech.2009.01.022
24823127 97481 0 None -724 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 453 10 3 4 5.4 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)ccc1C(=O)O 10.1021/jm8000345
CHEMBL272584 97481 0 None -724 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 453 10 3 4 5.4 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)ccc1C(=O)O 10.1021/jm8000345
24823127 97481 0 None -724 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 453 10 3 4 5.4 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)ccc1C(=O)O 10.1021/jm9000709
CHEMBL272584 97481 0 None -724 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 453 10 3 4 5.4 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)ccc1C(=O)O 10.1021/jm9000709
44589400 192973 0 None -3 3 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at adrenergic beta-1 receptorAgonist activity at adrenergic beta-1 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 -3 3 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at adrenergic beta-1 receptorAgonist activity at adrenergic beta-1 receptor
ChEMBL 446 11 2 5 4.2 COc1ccc(CCNCC(O)COc2ccc3c(c2)CCCN3Cc2ccccc2)cc1 10.1016/j.bmc.2008.11.030
45271886 193635 0 None -724 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassayAgonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassay
ChEMBL 508 11 3 5 4.5 CC(C)Cc1cc(-c2ccc(C[C@@H](C)NC[C@H](O)c3ccccc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1016/j.bmcl.2009.06.083
CHEMBL551532 193635 0 None -724 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassayAgonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassay
ChEMBL 508 11 3 5 4.5 CC(C)Cc1cc(-c2ccc(C[C@@H](C)NC[C@H](O)c3ccccc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1016/j.bmcl.2009.06.083
42639806 12397 0 None -40 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 468 10 3 6 2.9 COc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
CHEMBL1186584 12397 0 None -40 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 468 10 3 6 2.9 COc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
CHEMBL470858 12397 0 None -40 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 468 10 3 6 2.9 COc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
44331346 206638 0 None -120 3 Human 6.1 pEC50 = 6.1 Functional
Beta-1 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-1-adrenoceptorBeta-1 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-1-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 -120 3 Human 6.1 pEC50 = 6.1 Functional
Beta-1 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-1-adrenoceptorBeta-1 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-1-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
44560791 188497 0 None -154 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 376 8 3 4 3.7 C[C@H](Cc1ccc(-c2ccc(C(=O)O)cc2)cc1)NC[C@H](O)c1cccnc1 10.1021/jm8000345
CHEMBL510102 188497 0 None -154 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 376 8 3 4 3.7 C[C@H](Cc1ccc(-c2ccc(C(=O)O)cc2)cc1)NC[C@H](O)c1cccnc1 10.1021/jm8000345
42639808 12404 0 None -1230 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 522 11 3 6 4.2 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)cc1OC1CCCC1 10.1021/jm9000709
CHEMBL1186601 12404 0 None -1230 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 522 11 3 6 4.2 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)cc1OC1CCCC1 10.1021/jm9000709
CHEMBL472090 12404 0 None -1230 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 522 11 3 6 4.2 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)cc1OC1CCCC1 10.1021/jm9000709
10302915 5261 0 None -23 2 Human 6.1 pEC50 = 6.1 Functional
In vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta1-AR receptorIn vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta1-AR receptor
ChEMBL 554 12 5 6 4.0 O=C(NCc1c(F)cccc1F)N1CCC(Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)CC1 10.1016/s0960-894x(01)00645-x
CHEMBL106884 5261 0 None -23 2 Human 6.1 pEC50 = 6.1 Functional
In vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta1-AR receptorIn vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta1-AR receptor
ChEMBL 554 12 5 6 4.0 O=C(NCc1c(F)cccc1F)N1CCC(Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)CC1 10.1016/s0960-894x(01)00645-x
44127681 193536 0 None 2 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 420 11 4 5 3.1 O=C(Cc1ccccc1)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/j.ejmech.2009.01.022
CHEMBL550746 193536 0 None 2 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 420 11 4 5 3.1 O=C(Cc1ccccc1)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/j.ejmech.2009.01.022
164623544 187979 0 None -2754 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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 7.1 pEC50 = 7.1 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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 7.1 pEC50 = 7.1 Functional
Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta1 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
24949722 174948 0 None -223 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 455 6 3 3 5.3 O=C(O)c1ccc(-c2ccc3c(c2)C[C@@H](NC[C@H](O)c2ccc(C(F)(F)F)cc2)CC3)cc1 10.1021/jm800222k
CHEMBL457839 174948 0 None -223 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 455 6 3 3 5.3 O=C(O)c1ccc(-c2ccc3c(c2)C[C@@H](NC[C@H](O)c2ccc(C(F)(F)F)cc2)CC3)cc1 10.1021/jm800222k
11476004 172911 0 None -954 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 433 10 3 4 5.1 CC(C)Oc1cc(-c2ccc(CCN[C@@H](C)[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm8000345
CHEMBL453047 172911 0 None -954 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 433 10 3 4 5.1 CC(C)Oc1cc(-c2ccc(CCN[C@@H](C)[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm8000345
45269853 194883 0 None -4 2 Human 4.1 pEC50 = 4.1 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 426 11 3 5 3.1 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1)c1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL563872 194883 0 None -4 2 Human 4.1 pEC50 = 4.1 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 426 11 3 5 3.1 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1)c1ccccc1 10.1016/j.bmc.2009.06.031
9799092 47027 0 None -17 3 Human 7.1 pEC50 = 7.1 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-1 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-1 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 -17 3 Human 7.1 pEC50 = 7.1 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-1 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-1 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
9799092 47027 0 None -17 3 Human 7.1 pEC50 = 7.1 Functional
Activity at human beta-1 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-1 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 -17 3 Human 7.1 pEC50 = 7.1 Functional
Activity at human beta-1 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-1 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
56678847 66030 0 None -125 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta1 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 -125 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta1 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 -125 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta1 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
56678845 66058 0 None -39 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta1 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 -39 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta1 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 -39 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta1 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
9871096 66302 0 None -125 4 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta1 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 -125 4 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta1 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 -125 4 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta1 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
9799092 47027 0 None -17 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 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 -17 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 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
44441229 93303 0 None -100 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 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 -100 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 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
46833103 7317 0 None -10 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta-1 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 -10 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta-1 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
11060184 119212 0 None -1000 3 Human 6.1 pEC50 = 6.1 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-1 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-1 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 -1000 3 Human 6.1 pEC50 = 6.1 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-1 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-1 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
9823696 75408 0 None -501 3 Human 6.1 pEC50 = 6.1 Functional
Activity at human beta-1 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-1 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 -501 3 Human 6.1 pEC50 = 6.1 Functional
Activity at human beta-1 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-1 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
11495581 76954 0 None -25 3 Human 6.1 pEC50 = 6.1 Functional
Activity at human beta-1 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-1 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 -25 3 Human 6.1 pEC50 = 6.1 Functional
Activity at human beta-1 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-1 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 -25 3 Human 6.1 pEC50 = 6.1 Functional
Activity at human beta-1 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-1 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 -25 3 Human 6.1 pEC50 = 6.1 Functional
Activity at human beta-1 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-1 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
2419 3394 80 None -1621 6 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at adrenergic beta1 receptorAgonist activity at adrenergic beta1 receptor
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.05.097
5152 3394 80 None -1621 6 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at adrenergic beta1 receptorAgonist activity at adrenergic beta1 receptor
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.05.097
559 3394 80 None -1621 6 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at adrenergic beta1 receptorAgonist activity at adrenergic beta1 receptor
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.05.097
CHEMBL1263 3394 80 None -1621 6 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at adrenergic beta1 receptorAgonist activity at adrenergic beta1 receptor
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.05.097
DB00938 3394 80 None -1621 6 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at adrenergic beta1 receptorAgonist activity at adrenergic beta1 receptor
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.05.097
2419 3394 80 None -1621 6 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta1 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 -1621 6 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta1 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 -1621 6 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta1 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 -1621 6 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta1 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 -1621 6 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta1 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
2419 3394 80 None -1621 6 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta1 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 -1621 6 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta1 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 -1621 6 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta1 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 -1621 6 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta1 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 -1621 6 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta1 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
2419 3394 80 None -1621 6 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta-1 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 -1621 6 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta-1 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 -1621 6 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta-1 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 -1621 6 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta-1 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 -1621 6 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta-1 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 -1621 6 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta-1 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 -1621 6 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta-1 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 -1621 6 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta-1 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 -1621 6 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta-1 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 -1621 6 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta-1 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
10940242 164635 0 None -79 3 Human 6.1 pEC50 = 6.1 Functional
Concentration that causes 50% inhibition of human beta 1 adrenergic receptor (AR), expressed in CHO cells.Concentration that causes 50% inhibition of human beta 1 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 -79 3 Human 6.1 pEC50 = 6.1 Functional
Concentration that causes 50% inhibition of human beta 1 adrenergic receptor (AR), expressed in CHO cells.Concentration that causes 50% inhibition of human beta 1 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
42625743 12478 0 None -39 3 Human 4.1 pEC50 = 4.1 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta-1 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 -39 3 Human 4.1 pEC50 = 4.1 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta-1 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 -39 3 Human 4.1 pEC50 = 4.1 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta-1 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
559929 4816 10 None 4 2 Guinea pig 8.1 pEC50 = 8.1 Functional
Agonistic activity (beta-1 adrenergic receptor) for the percent maximal increase in contraction rate of isolated guinea pig atriaAgonistic activity (beta-1 adrenergic receptor) for the percent maximal increase in contraction rate of isolated guinea pig atria
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 8.1 pEC50 = 8.1 Functional
Agonistic activity (beta-1 adrenergic receptor) for the percent maximal increase in contraction rate of isolated guinea pig atriaAgonistic activity (beta-1 adrenergic receptor) for the percent maximal increase in contraction rate of isolated guinea pig atria
ChEMBL 273 5 4 5 1.4 CC(C)(C)NCC(O)COc1ccc(O)c(O)c1F 10.1021/jm00107a027
44419332 141216 0 None -1 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP levelsAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP levels
ChEMBL 505 11 4 8 2.5 Cn1c(=O)[nH]c2cccc(OC[C@@H](O)CNC(C)(C)Cc3ccc(Oc4ccc(C(N)=O)cn4)cc3)c21 10.1016/j.bmcl.2006.08.010
CHEMBL386016 141216 0 None -1 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP levelsAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP levels
ChEMBL 505 11 4 8 2.5 Cn1c(=O)[nH]c2cccc(OC[C@@H](O)CNC(C)(C)Cc3ccc(Oc4ccc(C(N)=O)cn4)cc3)c21 10.1016/j.bmcl.2006.08.010
46889771 6901 0 None 1 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human adrenergic beta-1 receptor expressed in CHOK1 cells assessed as cAMP accumulation by HTRF assayAgonist activity at human adrenergic beta-1 receptor expressed in CHOK1 cells assessed as 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 7.1 pEC50 = 7.1 Functional
Agonist activity at human adrenergic beta-1 receptor expressed in CHOK1 cells assessed as cAMP accumulation by HTRF assayAgonist activity at human adrenergic beta-1 receptor expressed in CHOK1 cells assessed as 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
45268136 194701 0 None -2 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 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 7.1 pEC50 = 7.1 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 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 7.1 pEC50 = 7.1 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 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
44560792 172806 0 None -794 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 434 10 3 5 4.5 CC(C)Oc1cc(-c2ccc(C[C@@H](C)NC[C@H](O)c3cccnc3)cc2)ccc1C(=O)O 10.1021/jm8000345
CHEMBL452798 172806 0 None -794 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 434 10 3 5 4.5 CC(C)Oc1cc(-c2ccc(C[C@@H](C)NC[C@H](O)c3cccnc3)cc2)ccc1C(=O)O 10.1021/jm8000345
24950718 175415 0 None -398 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 435 6 3 3 5.2 Cc1cc(C(=O)O)ccc1-c1ccc2c(c1)C[C@@H](NC[C@H](O)c1ccc(Cl)cc1)CC2 10.1021/jm800222k
CHEMBL458927 175415 0 None -398 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 435 6 3 3 5.2 Cc1cc(C(=O)O)ccc1-c1ccc2c(c1)C[C@@H](NC[C@H](O)c1ccc(Cl)cc1)CC2 10.1021/jm800222k
11272641 12322 0 None -6165 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 537 11 3 7 4.0 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1OC1CCCCC1 10.1021/jm9000709
CHEMBL1186009 12322 0 None -6165 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 537 11 3 7 4.0 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1OC1CCCCC1 10.1021/jm9000709
CHEMBL445481 12322 0 None -6165 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 537 11 3 7 4.0 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1OC1CCCCC1 10.1021/jm9000709
25071020 192572 0 None -251 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 469 11 3 5 5.5 CC(C)Oc1ccc(Oc2cccc(CCNC[C@H](O)c3cccc(Cl)c3)c2)cc1C(=O)O 10.1016/j.bmcl.2008.08.009
CHEMBL523265 192572 0 None -251 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 469 11 3 5 5.5 CC(C)Oc1ccc(Oc2cccc(CCNC[C@H](O)c3cccc(Cl)c3)c2)cc1C(=O)O 10.1016/j.bmcl.2008.08.009
24949726 188939 0 None -457 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 435 6 3 3 5.2 Cc1cc(-c2ccc3c(c2)C[C@@H](NC[C@H](O)c2ccc(Cl)cc2)CC3)ccc1C(=O)O 10.1021/jm800222k
CHEMBL514265 188939 0 None -457 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 435 6 3 3 5.2 Cc1cc(-c2ccc3c(c2)C[C@@H](NC[C@H](O)c2ccc(Cl)cc2)CC3)ccc1C(=O)O 10.1021/jm800222k
44127479 194495 0 None 10 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 454 11 4 5 3.8 O=C(Cc1cccc(Cl)c1)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/j.ejmech.2009.01.022
CHEMBL561348 194495 0 None 10 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 454 11 4 5 3.8 O=C(Cc1cccc(Cl)c1)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/j.ejmech.2009.01.022
24895359 191886 0 None -104 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 405 9 3 4 4.3 COc1cc(-c2ccc(C[C@@H](C)NC[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm8000345
CHEMBL520903 191886 0 None -104 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 405 9 3 4 4.3 COc1cc(-c2ccc(C[C@@H](C)NC[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm8000345
145989075 166528 0 None -524 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 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 6.1 pEC50 = 6.1 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 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
145994130 166816 0 None -83 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 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 6.1 pEC50 = 6.1 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 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
24894315 172394 0 None -165 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 469 11 3 5 5.2 CC(C)Oc1cc(-c2ccc(OCCNC[C@H](O)c3cccc(Cl)c3)cc2)ccc1C(=O)O 10.1021/jm8000345
CHEMBL451772 172394 0 None -165 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 469 11 3 5 5.2 CC(C)Oc1cc(-c2ccc(OCCNC[C@H](O)c3cccc(Cl)c3)cc2)ccc1C(=O)O 10.1021/jm8000345
44580042 192487 0 None -26 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 396 9 3 5 3.6 O=C(O)c1cc(Oc2cccc(CCNC[C@H](O)c3cccnc3)c2)ccc1F 10.1016/j.bmcl.2008.08.009
CHEMBL522641 192487 0 None -26 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 396 9 3 5 3.6 O=C(O)c1cc(Oc2cccc(CCNC[C@H](O)c3cccnc3)c2)ccc1F 10.1016/j.bmcl.2008.08.009
42639491 12449 0 None -1659 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 552 11 3 6 5.3 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)cc1SC1CCCCC1 10.1021/jm9000709
CHEMBL1186805 12449 0 None -1659 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 552 11 3 6 5.3 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)cc1SC1CCCCC1 10.1021/jm9000709
CHEMBL479342 12449 0 None -1659 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 552 11 3 6 5.3 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)cc1SC1CCCCC1 10.1021/jm9000709
44396738 123353 0 None -77 3 Human 7.1 pEC50 = 7.1 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-1 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-1 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 -77 3 Human 7.1 pEC50 = 7.1 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-1 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-1 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
10142284 4805 0 None -1 2 Human 7.1 pEC50 = 7.1 Functional
In vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta1-AR receptorIn vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta1-AR receptor
ChEMBL 510 11 5 6 3.9 O=C(NC1CCCCC1)N1CCC(Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)CC1 10.1016/s0960-894x(01)00645-x
CHEMBL104481 4805 0 None -1 2 Human 7.1 pEC50 = 7.1 Functional
In vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta1-AR receptorIn vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta1-AR receptor
ChEMBL 510 11 5 6 3.9 O=C(NC1CCCCC1)N1CCC(Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)CC1 10.1016/s0960-894x(01)00645-x
1239 1639 46 None -109 5 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human adrenergic beta 1 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 1 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 -109 5 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human adrenergic beta 1 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 1 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 -109 5 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human adrenergic beta 1 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 1 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 -109 5 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human adrenergic beta 1 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 1 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 -109 5 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human adrenergic beta 1 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 1 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
1239 1639 46 None -109 5 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human beta-1 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta-1 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 -109 5 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human beta-1 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta-1 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 -109 5 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human beta-1 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta-1 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 -109 5 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human beta-1 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta-1 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 -109 5 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human beta-1 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta-1 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 -109 5 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta-1 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 -109 5 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta-1 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 -109 5 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta-1 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 -109 5 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta-1 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 -109 5 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta-1 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
24895361 184782 0 None -933 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 433 10 3 4 5.1 CC(C)Oc1cc(-c2ccc(C[C@@H](C)NC[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm8000345
CHEMBL486051 184782 0 None -933 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 433 10 3 4 5.1 CC(C)Oc1cc(-c2ccc(C[C@@H](C)NC[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm8000345
155550964 173368 0 None -575 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 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 7.1 pEC50 = 7.1 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 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
10232593 5310 0 None -1 2 Human 7.1 pEC50 = 7.1 Functional
In vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta1-AR receptorIn vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta1-AR receptor
ChEMBL 609 17 6 7 4.8 CCCCCCCCNC(=O)N1CCC(Nc2ccc(CCNC[C@H](O)COc3ccc(O)c4c3CCC(=O)N4)cc2)CC1 10.1016/s0960-894x(01)00645-x
CHEMBL107129 5310 0 None -1 2 Human 7.1 pEC50 = 7.1 Functional
In vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta1-AR receptorIn vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta1-AR receptor
ChEMBL 609 17 6 7 4.8 CCCCCCCCNC(=O)N1CCC(Nc2ccc(CCNC[C@H](O)COc3ccc(O)c4c3CCC(=O)N4)cc2)CC1 10.1016/s0960-894x(01)00645-x
9873245 4434 0 None -38 3 Human 6.1 pEC50 = 6.1 Functional
In vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-1 adrenergic receptorIn vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-1 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 -38 3 Human 6.1 pEC50 = 6.1 Functional
In vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-1 adrenergic receptorIn vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-1 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
10028830 2206 33 None -74 3 Human 6.1 pEC50 = 6.1 Functional
Antagonist activity at human beta1 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 beta1 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 -74 3 Human 6.1 pEC50 = 6.1 Functional
Antagonist activity at human beta1 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 beta1 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 -74 3 Human 6.1 pEC50 = 6.1 Functional
Antagonist activity at human beta1 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 beta1 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
44237666 57913 0 None -44668 2 Rat 5.1 pEC50 = 5.1 Functional
Agonist activity at beta1 adrenoceptor in rat left atria assessed as induction of ionotropic effectAgonist activity at beta1 adrenoceptor in rat left atria assessed as induction of ionotropic effect
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 Rat 5.1 pEC50 = 5.1 Functional
Agonist activity at beta1 adrenoceptor in rat left atria assessed as induction of ionotropic effectAgonist activity at beta1 adrenoceptor in rat left atria assessed as induction of ionotropic effect
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
24950059 174288 0 None -169 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 467 8 3 5 5.0 COc1cc(Oc2ccc3c(c2)C[C@@H](NC[C@H](O)c2cccc(Cl)c2)CC3)cc(C(=O)O)c1 10.1021/jm800222k
CHEMBL456352 174288 0 None -169 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 467 8 3 5 5.0 COc1cc(Oc2ccc3c(c2)C[C@@H](NC[C@H](O)c2cccc(Cl)c2)CC3)cc(C(=O)O)c1 10.1021/jm800222k
24823466 12707 0 None 1 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 440 11 4 5 4.4 O=C(O)COc1ccc(Nc2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)cc1 10.1021/jm701324c
CHEMBL1188436 12707 0 None 1 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 440 11 4 5 4.4 O=C(O)COc1ccc(Nc2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)cc1 10.1021/jm701324c
CHEMBL536330 12707 0 None 1 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 440 11 4 5 4.4 O=C(O)COc1ccc(Nc2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)cc1 10.1021/jm701324c
11270069 95244 0 None 6 2 Human 8.0 pEC50 = 8.0 Functional
Agonistic activity against human Beta-1 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonistic activity against human Beta-1 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
CHEMBL25823 95244 0 None 6 2 Human 8.0 pEC50 = 8.0 Functional
Agonistic activity against human Beta-1 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonistic activity against human Beta-1 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
52949488 17349 0 None -3 3 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as 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 -3 3 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as 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
155548071 173167 0 None -131 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 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 8.0 pEC50 = 8.0 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 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
56598831 88699 0 None 1023 3 Human 8.0 pEC50 = 8.0 Functional
Partial agonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsPartial agonist activity at human beta1 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 8.0 pEC50 = 8.0 Functional
Partial agonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsPartial agonist activity at human beta1 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 8.0 pEC50 = 8.0 Functional
Partial agonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsPartial agonist activity at human beta1 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
45101522 197329 0 None -5 2 Human 8.0 pEC50 = 8 Functional
Agonist activity at human beta-1 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta-1 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 8.0 pEC50 = 8 Functional
Agonist activity at human beta-1 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta-1 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
45272430 193763 0 None -8 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 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 7.1 pEC50 = 7.1 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 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 7.1 pEC50 = 7.1 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 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
44517692 194984 0 None -4 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 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 7.1 pEC50 = 7.1 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 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 7.1 pEC50 = 7.1 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 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
44237612 57906 0 None -4466 2 Rat 6.1 pEC50 = 6.1 Functional
Agonist activity at beta1 adrenoceptor in rat left atria assessed as induction of ionotropic effectAgonist activity at beta1 adrenoceptor in rat left atria assessed as induction of ionotropic effect
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 Rat 6.1 pEC50 = 6.1 Functional
Agonist activity at beta1 adrenoceptor in rat left atria assessed as induction of ionotropic effectAgonist activity at beta1 adrenoceptor in rat left atria assessed as induction of ionotropic effect
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
11398536 12354 0 None -6309 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 535 11 4 6 4.7 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)cc1NC1CCCCC1 10.1021/jm9000709
CHEMBL1186241 12354 0 None -6309 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 535 11 4 6 4.7 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)cc1NC1CCCCC1 10.1021/jm9000709
CHEMBL455773 12354 0 None -6309 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 535 11 4 6 4.7 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)cc1NC1CCCCC1 10.1021/jm9000709
24895565 176111 0 None -575 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 475 11 3 5 5.5 O=C(O)c1ccc(-c2ccc(OCCNC[C@H](O)c3ccccc3)cc2)cc1OC1CCCCC1 10.1021/jm8000345
CHEMBL459862 176111 0 None -575 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 475 11 3 5 5.5 O=C(O)c1ccc(-c2ccc(OCCNC[C@H](O)c3ccccc3)cc2)cc1OC1CCCCC1 10.1021/jm8000345
44127167 194572 0 None 1 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 421 11 4 6 2.5 O=C(Cc1cccnc1)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/j.ejmech.2009.01.022
CHEMBL561818 194572 0 None 1 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 421 11 4 6 2.5 O=C(Cc1cccnc1)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/j.ejmech.2009.01.022
24949720 188921 0 None -2398 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 421 6 3 3 4.9 O=C(O)c1ccc(-c2ccc3c(c2)C[C@@H](NC[C@H](O)c2ccc(Cl)cc2)CC3)cc1 10.1021/jm800222k
CHEMBL514102 188921 0 None -2398 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 421 6 3 3 4.9 O=C(O)c1ccc(-c2ccc3c(c2)C[C@@H](NC[C@H](O)c2ccc(Cl)cc2)CC3)cc1 10.1021/jm800222k
44565907 192557 0 None -138 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 498 11 4 8 2.3 CCOc1cc(-c2ccc(CCNC[C@H](O)c3cnccc3N)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
CHEMBL523149 192557 0 None -138 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 498 11 4 8 2.3 CCOc1cc(-c2ccc(CCNC[C@H](O)c3cnccc3N)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
10205463 5413 0 None -10 2 Human 6.0 pEC50 = 6.0 Functional
In vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta1-AR receptorIn vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta1-AR receptor
ChEMBL 470 11 5 6 3.0 CC(C)NC(=O)N1CCC(Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)CC1 10.1016/s0960-894x(01)00645-x
CHEMBL107633 5413 0 None -10 2 Human 6.0 pEC50 = 6.0 Functional
In vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta1-AR receptorIn vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta1-AR receptor
ChEMBL 470 11 5 6 3.0 CC(C)NC(=O)N1CCC(Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)CC1 10.1016/s0960-894x(01)00645-x
44127052 194053 0 None -2 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 450 12 4 6 3.2 COc1ccccc1CC(=O)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/j.ejmech.2009.01.022
CHEMBL557269 194053 0 None -2 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 450 12 4 6 3.2 COc1ccccc1CC(=O)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/j.ejmech.2009.01.022
44574758 177958 0 None -18 2 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 394 11 4 5 2.2 O=C(Cc1ncc[nH]1)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.03.044
CHEMBL466879 177958 0 None -18 2 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 394 11 4 5 2.2 O=C(Cc1ncc[nH]1)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.03.044
9896817 102399 0 None -22 3 Human 6.0 pEC50 = 6.0 Functional
Compound was evaluated for its inhibitory activity against human beta-1 adrenergic receptor (AR)Compound was evaluated for its inhibitory activity against human beta-1 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 -22 3 Human 6.0 pEC50 = 6.0 Functional
Compound was evaluated for its inhibitory activity against human beta-1 adrenergic receptor (AR)Compound was evaluated for its inhibitory activity against human beta-1 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
24823296 97569 0 None -2884 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 453 10 3 4 5.7 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)cc1Oc1ccccc1 10.1021/jm701324c
CHEMBL273006 97569 0 None -2884 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 453 10 3 4 5.7 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)cc1Oc1ccccc1 10.1021/jm701324c
24949883 175511 0 None -691 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 439 6 3 3 5.0 O=C(O)c1ccc(-c2ccc3c(c2)C[C@@H](NC[C@H](O)c2ccc(Cl)cc2)CC3)c(F)c1 10.1021/jm800222k
CHEMBL459133 175511 0 None -691 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 439 6 3 3 5.0 O=C(O)c1ccc(-c2ccc3c(c2)C[C@@H](NC[C@H](O)c2ccc(Cl)cc2)CC3)c(F)c1 10.1021/jm800222k
24823296 97569 0 None -2884 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 453 10 3 4 5.7 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)cc1Oc1ccccc1 10.1021/jm9000709
CHEMBL273006 97569 0 None -2884 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 453 10 3 4 5.7 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)cc1Oc1ccccc1 10.1021/jm9000709
10648298 99245 0 None -251 3 Human 5.0 pEC50 = 5.0 Functional
Increased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 1 Adrenergic receptorIncreased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 1 Adrenergic receptor
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 -251 3 Human 5.0 pEC50 = 5.0 Functional
Increased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 1 Adrenergic receptorIncreased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 1 Adrenergic receptor
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
46232815 199986 0 None 5 2 Human 6.0 pEC50 = 6 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta-1 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 6.0 pEC50 = 6 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta-1 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
9896817 102399 0 None -22 3 Human 5.0 pIC50 = 5 Functional
Compound was evaluated for its inhibitory activity against CHO cells expressing the cloned human beta-1 adrenergic receptor (AR) in the presence of [125I]iodocyanopindololCompound was evaluated for its inhibitory activity against CHO cells expressing the cloned human beta-1 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 -22 3 Human 5.0 pIC50 = 5 Functional
Compound was evaluated for its inhibitory activity against CHO cells expressing the cloned human beta-1 adrenergic receptor (AR) in the presence of [125I]iodocyanopindololCompound was evaluated for its inhibitory activity against CHO cells expressing the cloned human beta-1 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
9962058 203064 0 None -165 3 Human 4.0 pIC50 = 4 Functional
Compound was evaluated for its inhibitory activity against CHO cells expressing the cloned human beta-1 adrenergic receptor (AR) in the presence of [125I]iodocyanopindololCompound was evaluated for its inhibitory activity against CHO cells expressing the cloned human beta-1 adrenergic receptor (AR) in the presence of [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 -165 3 Human 4.0 pIC50 = 4 Functional
Compound was evaluated for its inhibitory activity against CHO cells expressing the cloned human beta-1 adrenergic receptor (AR) in the presence of [125I]iodocyanopindololCompound was evaluated for its inhibitory activity against CHO cells expressing the cloned human beta-1 adrenergic receptor (AR) in the presence of [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
53318280 58332 0 None -95 3 Human 6.0 pIC50 = 6.0 Functional
Agonist activity at human beta1 adrenergic receptorAgonist activity at human beta1 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 -95 3 Human 6.0 pIC50 = 6.0 Functional
Agonist activity at human beta1 adrenergic receptorAgonist activity at human beta1 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
11722516 90446 0 None - 1 Guinea pig 5.9 pIC50 = 5.9 Functional
Tested for beta-1-adrenergic blocking effect by measuring the ability to inhibit the positive inotropic effect of isoproterenol on the isolated right atrium of guinea pigsTested for beta-1-adrenergic blocking effect by measuring the ability to inhibit the positive inotropic effect of isoproterenol on the isolated right atrium of guinea pigs
ChEMBL 303 9 2 4 2.2 COCCc1ccc(OC(F)(F)[C@@H](O)CNC(C)C)cc1 10.1016/S0960-894X(97)00207-2
CHEMBL23929 90446 0 None - 1 Guinea pig 5.9 pIC50 = 5.9 Functional
Tested for beta-1-adrenergic blocking effect by measuring the ability to inhibit the positive inotropic effect of isoproterenol on the isolated right atrium of guinea pigsTested for beta-1-adrenergic blocking effect by measuring the ability to inhibit the positive inotropic effect of isoproterenol on the isolated right atrium of guinea pigs
ChEMBL 303 9 2 4 2.2 COCCc1ccc(OC(F)(F)[C@@H](O)CNC(C)C)cc1 10.1016/S0960-894X(97)00207-2
44268214 18367 0 None 4 3 Human 7.8 pIC50 = 7.8 Functional
Compound was tested for agonist activity against cloned human beta-1 adrenergic receptorCompound was tested for agonist activity against cloned human beta-1 adrenergic receptor
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 4 3 Human 7.8 pIC50 = 7.8 Functional
Compound was tested for agonist activity against cloned human beta-1 adrenergic receptorCompound was tested for agonist activity against cloned human beta-1 adrenergic receptor
ChEMBL 331 10 3 5 2.4 COc1ccc(CCCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/s0960-894x(98)00169-3
53319639 58335 0 None -1 3 Human 5.8 pIC50 = 5.8 Functional
Agonist activity at human beta1 adrenergic receptorAgonist activity at human beta1 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 -1 3 Human 5.8 pIC50 = 5.8 Functional
Agonist activity at human beta1 adrenergic receptorAgonist activity at human beta1 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
145990586 166279 0 None -1 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human beta1-adrenergic receptor expressed in CHO-K1 cells assessed as decrease in isoproterenol-induced cAMP accumulation after 15 mins by HTRF assayAntagonist activity at human beta1-adrenergic receptor expressed in CHO-K1 cells assessed as decrease in isoproterenol-induced cAMP accumulation after 15 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 7.8 pIC50 = 7.8 Functional
Antagonist activity at human beta1-adrenergic receptor expressed in CHO-K1 cells assessed as decrease in isoproterenol-induced cAMP accumulation after 15 mins by HTRF assayAntagonist activity at human beta1-adrenergic receptor expressed in CHO-K1 cells assessed as decrease in isoproterenol-induced cAMP accumulation after 15 mins by HTRF assay
ChEMBL 297 2 2 4 2.6 COc1cc2c3c(c1OC)-c1ccccc1[C@@H](O)[C@@H]3NCC2 10.1039/C7MD00656J
53326196 58333 0 None 1 3 Human 5.8 pIC50 = 5.8 Functional
Agonist activity at human beta1 adrenergic receptorAgonist activity at human beta1 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 5.8 pIC50 = 5.8 Functional
Agonist activity at human beta1 adrenergic receptorAgonist activity at human beta1 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
567 715 10 None -186 7 Rat 6.7 pIC50 = 6.7 Functional
In vitro beta-adrenergic activity against beta-1 adrenergic receptor by the inhibition of insulin stimulated [14C]- glucose incorporation into glycogen in isolated rat soleus muscleIn vitro beta-adrenergic activity against beta-1 adrenergic receptor by the inhibition of insulin stimulated [14C]- glucose incorporation into glycogen in isolated rat soleus muscle
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 -186 7 Rat 6.7 pIC50 = 6.7 Functional
In vitro beta-adrenergic activity against beta-1 adrenergic receptor by the inhibition of insulin stimulated [14C]- glucose incorporation into glycogen in isolated rat soleus muscleIn vitro beta-adrenergic activity against beta-1 adrenergic receptor by the inhibition of insulin stimulated [14C]- glucose incorporation into glycogen in isolated rat soleus muscle
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 -186 7 Rat 6.7 pIC50 = 6.7 Functional
In vitro beta-adrenergic activity against beta-1 adrenergic receptor by the inhibition of insulin stimulated [14C]- glucose incorporation into glycogen in isolated rat soleus muscleIn vitro beta-adrenergic activity against beta-1 adrenergic receptor by the inhibition of insulin stimulated [14C]- glucose incorporation into glycogen in isolated rat soleus muscle
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
1786 2474 79 None -4 6 Guinea pig 6.7 pIC50 = 6.7 Functional
Tested for beta-1-adrenergic blocking effect by measuring the ability to inhibit the positive inotropic effect of isoproterenol on the isolated right atrium of guinea pigsTested for beta-1-adrenergic blocking effect by measuring the ability to inhibit the positive inotropic effect of isoproterenol on the isolated right atrium of guinea pigs
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1016/S0960-894X(97)00207-2
4171 2474 79 None -4 6 Guinea pig 6.7 pIC50 = 6.7 Functional
Tested for beta-1-adrenergic blocking effect by measuring the ability to inhibit the positive inotropic effect of isoproterenol on the isolated right atrium of guinea pigsTested for beta-1-adrenergic blocking effect by measuring the ability to inhibit the positive inotropic effect of isoproterenol on the isolated right atrium of guinea pigs
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1016/S0960-894X(97)00207-2
553 2474 79 None -4 6 Guinea pig 6.7 pIC50 = 6.7 Functional
Tested for beta-1-adrenergic blocking effect by measuring the ability to inhibit the positive inotropic effect of isoproterenol on the isolated right atrium of guinea pigsTested for beta-1-adrenergic blocking effect by measuring the ability to inhibit the positive inotropic effect of isoproterenol on the isolated right atrium of guinea pigs
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1016/S0960-894X(97)00207-2
CHEMBL13 2474 79 None -4 6 Guinea pig 6.7 pIC50 = 6.7 Functional
Tested for beta-1-adrenergic blocking effect by measuring the ability to inhibit the positive inotropic effect of isoproterenol on the isolated right atrium of guinea pigsTested for beta-1-adrenergic blocking effect by measuring the ability to inhibit the positive inotropic effect of isoproterenol on the isolated right atrium of guinea pigs
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1016/S0960-894X(97)00207-2
DB00264 2474 79 None -4 6 Guinea pig 6.7 pIC50 = 6.7 Functional
Tested for beta-1-adrenergic blocking effect by measuring the ability to inhibit the positive inotropic effect of isoproterenol on the isolated right atrium of guinea pigsTested for beta-1-adrenergic blocking effect by measuring the ability to inhibit the positive inotropic effect of isoproterenol on the isolated right atrium of guinea pigs
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1016/S0960-894X(97)00207-2
127034967 135952 0 None -1 3 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human beta1 receptor expressed in CHO-K1 cells assessed as isoproterenol-induced cAMP level by HTRF assayAntagonist activity at human beta1 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 6.7 pIC50 = 6.7 Functional
Antagonist activity at human beta1 receptor expressed in CHO-K1 cells assessed as isoproterenol-induced cAMP level by HTRF assayAntagonist activity at human beta1 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
53326839 58334 0 None -26 3 Human 5.7 pIC50 = 5.7 Functional
Agonist activity at human beta1 adrenergic receptorAgonist activity at human beta1 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 -26 3 Human 5.7 pIC50 = 5.7 Functional
Agonist activity at human beta1 adrenergic receptorAgonist activity at human beta1 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
11722516 90446 0 None - 1 Guinea pig 5.7 pIC50 = 5.7 Functional
Tested for beta-2-adrenergic blocking effect by measuring the ability to inhibit the relaxing effect of epinephrine on the isolated tracheal muscle of guinea pigsTested for beta-2-adrenergic blocking effect by measuring the ability to inhibit the relaxing effect of epinephrine on the isolated tracheal muscle of guinea pigs
ChEMBL 303 9 2 4 2.2 COCCc1ccc(OC(F)(F)[C@@H](O)CNC(C)C)cc1 10.1016/S0960-894X(97)00207-2
CHEMBL23929 90446 0 None - 1 Guinea pig 5.7 pIC50 = 5.7 Functional
Tested for beta-2-adrenergic blocking effect by measuring the ability to inhibit the relaxing effect of epinephrine on the isolated tracheal muscle of guinea pigsTested for beta-2-adrenergic blocking effect by measuring the ability to inhibit the relaxing effect of epinephrine on the isolated tracheal muscle of guinea pigs
ChEMBL 303 9 2 4 2.2 COCCc1ccc(OC(F)(F)[C@@H](O)CNC(C)C)cc1 10.1016/S0960-894X(97)00207-2
51346867 58336 0 None -537 3 Human 5.7 pIC50 = 5.7 Functional
Agonist activity at human beta1 adrenergic receptorAgonist activity at human beta1 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 -537 3 Human 5.7 pIC50 = 5.7 Functional
Agonist activity at human beta1 adrenergic receptorAgonist activity at human beta1 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
53326197 58337 0 None -28 3 Human 6.6 pIC50 = 6.6 Functional
Agonist activity at human beta1 adrenergic receptorAgonist activity at human beta1 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 -28 3 Human 6.6 pIC50 = 6.6 Functional
Agonist activity at human beta1 adrenergic receptorAgonist activity at human beta1 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
165193 3126 60 None -6 13 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human beta1 receptor expressed in CHO-K1 cells assessed as isoproterenol-induced cAMP level by HTRF assayAntagonist activity at human beta1 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 6.6 pIC50 = 6.6 Functional
Antagonist activity at human beta1 receptor expressed in CHO-K1 cells assessed as isoproterenol-induced cAMP level by HTRF assayAntagonist activity at human beta1 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 6.6 pIC50 = 6.6 Functional
Antagonist activity at human beta1 receptor expressed in CHO-K1 cells assessed as isoproterenol-induced cAMP level by HTRF assayAntagonist activity at human beta1 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 6.6 pIC50 = 6.6 Functional
Antagonist activity at human beta1 receptor expressed in CHO-K1 cells assessed as isoproterenol-induced cAMP level by HTRF assayAntagonist activity at human beta1 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 6.6 pIC50 = 6.6 Functional
Antagonist activity at human beta1 receptor expressed in CHO-K1 cells assessed as isoproterenol-induced cAMP level by HTRF assayAntagonist activity at human beta1 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 6.6 pIC50 = 6.6 Functional
Antagonist activity at human beta1 receptor expressed in CHO-K1 cells assessed as isoproterenol-induced cAMP level by HTRF assayAntagonist activity at human beta1 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 6.6 pIC50 = 6.6 Functional
Antagonist activity at human beta1 receptor expressed in CHO-K1 cells assessed as isoproterenol-induced cAMP level by HTRF assayAntagonist activity at human beta1 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 6.6 pIC50 = 6.6 Functional
Antagonist activity at human beta1 receptor expressed in CHO-K1 cells assessed as isoproterenol-induced cAMP level by HTRF assayAntagonist activity at human beta1 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 6.6 pIC50 = 6.6 Functional
Antagonist activity at human beta1 receptor expressed in CHO-K1 cells assessed as isoproterenol-induced cAMP level by HTRF assayAntagonist activity at human beta1 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 6.6 pIC50 = 6.6 Functional
Antagonist activity at human beta1 receptor expressed in CHO-K1 cells assessed as isoproterenol-induced cAMP level by HTRF assayAntagonist activity at human beta1 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 6.6 pIC50 = 6.6 Functional
Antagonist activity at human beta1 receptor expressed in CHO-K1 cells assessed as isoproterenol-induced cAMP level by HTRF assayAntagonist activity at human beta1 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
9873245 4434 0 None -38 3 Human 7.6 pIC50 = 7.6 Functional
Compound was tested for the antagonistic activity against Beta-1 adrenergic receptorCompound was tested for the antagonistic activity against Beta-1 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 -38 3 Human 7.6 pIC50 = 7.6 Functional
Compound was tested for the antagonistic activity against Beta-1 adrenergic receptorCompound was tested for the antagonistic activity against Beta-1 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
14739907 163570 0 None 1 2 Human 6.6 pIC50 = 6.6 Functional
Tested for beta1-receptor selectivity in canine cardiac tissue in anesthetized dogsTested for beta1-receptor selectivity in canine cardiac 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 Human 6.6 pIC50 = 6.6 Functional
Tested for beta1-receptor selectivity in canine cardiac tissue in anesthetized dogsTested for beta1-receptor selectivity in canine cardiac tissue in anesthetized dogs
ChEMBL 367 10 2 6 2.6 Cc1cccc(OCC(O)CNCCOc2ccc(-n3ccnc3)cc2)c1 10.1021/jm00172a033
14739906 205943 0 None 16 2 Human 6.6 pIC50 = 6.6 Functional
Tested for beta1-receptor selectivity in canine cardiac tissue in anesthetized dogsTested for beta1-receptor selectivity in canine cardiac 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 Human 6.6 pIC50 = 6.6 Functional
Tested for beta1-receptor selectivity in canine cardiac tissue in anesthetized dogsTested for beta1-receptor selectivity in canine cardiac tissue in anesthetized dogs
ChEMBL 411 13 2 7 2.5 COCCc1ccc(OCC(O)CNCCOc2ccc(-n3ccnc3)cc2)cc1 10.1021/jm00172a033
53326195 58331 0 None -194 3 Human 5.5 pIC50 = 5.5 Functional
Agonist activity at human beta1 adrenergic receptorAgonist activity at human beta1 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 -194 3 Human 5.5 pIC50 = 5.5 Functional
Agonist activity at human beta1 adrenergic receptorAgonist activity at human beta1 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
9853471 203136 0 None -389 3 Human 5.5 pIC50 = 5.5 Functional
Compound was evaluated for its inhibitory activity against CHO cells expressing the cloned human beta-1 adrenergic receptor (AR) in the presence of [125I]iodocyanopindololCompound was evaluated for its inhibitory activity against CHO cells expressing the cloned human beta-1 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 -389 3 Human 5.5 pIC50 = 5.5 Functional
Compound was evaluated for its inhibitory activity against CHO cells expressing the cloned human beta-1 adrenergic receptor (AR) in the presence of [125I]iodocyanopindololCompound was evaluated for its inhibitory activity against CHO cells expressing the cloned human beta-1 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
146015362 932 6 None -53703 5 Rat 4.5 pIC50 = 4.5 Functional
In vitro beta-adrenergic activity against beta-1 adrenergic receptor by the inhibition of insulin stimulated [14C]- glucose incorporation into glycogen in isolated rat soleus muscleIn vitro beta-adrenergic activity against beta-1 adrenergic receptor by the inhibition of insulin stimulated [14C]- glucose incorporation into glycogen in isolated rat soleus muscle
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/jm00094a025
3462 932 6 None -53703 5 Rat 4.5 pIC50 = 4.5 Functional
In vitro beta-adrenergic activity against beta-1 adrenergic receptor by the inhibition of insulin stimulated [14C]- glucose incorporation into glycogen in isolated rat soleus muscleIn vitro beta-adrenergic activity against beta-1 adrenergic receptor by the inhibition of insulin stimulated [14C]- glucose incorporation into glycogen in isolated rat soleus muscle
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/jm00094a025
5486546 932 6 None -53703 5 Rat 4.5 pIC50 = 4.5 Functional
In vitro beta-adrenergic activity against beta-1 adrenergic receptor by the inhibition of insulin stimulated [14C]- glucose incorporation into glycogen in isolated rat soleus muscleIn vitro beta-adrenergic activity against beta-1 adrenergic receptor by the inhibition of insulin stimulated [14C]- glucose incorporation into glycogen in isolated rat soleus muscle
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/jm00094a025
CHEMBL1204876 932 6 None -53703 5 Rat 4.5 pIC50 = 4.5 Functional
In vitro beta-adrenergic activity against beta-1 adrenergic receptor by the inhibition of insulin stimulated [14C]- glucose incorporation into glycogen in isolated rat soleus muscleIn vitro beta-adrenergic activity against beta-1 adrenergic receptor by the inhibition of insulin stimulated [14C]- glucose incorporation into glycogen in isolated rat soleus muscle
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/jm00094a025
1786 2474 79 None -4 6 Guinea pig 6.5 pIC50 = 6.5 Functional
Tested for beta-2-adrenergic blocking effect by measuring the ability to inhibit the relaxing effect of epinephrine on the isolated tracheal muscle of guinea pigsTested for beta-2-adrenergic blocking effect by measuring the ability to inhibit the relaxing effect of epinephrine on the isolated tracheal muscle of guinea pigs
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1016/S0960-894X(97)00207-2
4171 2474 79 None -4 6 Guinea pig 6.5 pIC50 = 6.5 Functional
Tested for beta-2-adrenergic blocking effect by measuring the ability to inhibit the relaxing effect of epinephrine on the isolated tracheal muscle of guinea pigsTested for beta-2-adrenergic blocking effect by measuring the ability to inhibit the relaxing effect of epinephrine on the isolated tracheal muscle of guinea pigs
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1016/S0960-894X(97)00207-2
553 2474 79 None -4 6 Guinea pig 6.5 pIC50 = 6.5 Functional
Tested for beta-2-adrenergic blocking effect by measuring the ability to inhibit the relaxing effect of epinephrine on the isolated tracheal muscle of guinea pigsTested for beta-2-adrenergic blocking effect by measuring the ability to inhibit the relaxing effect of epinephrine on the isolated tracheal muscle of guinea pigs
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1016/S0960-894X(97)00207-2
CHEMBL13 2474 79 None -4 6 Guinea pig 6.5 pIC50 = 6.5 Functional
Tested for beta-2-adrenergic blocking effect by measuring the ability to inhibit the relaxing effect of epinephrine on the isolated tracheal muscle of guinea pigsTested for beta-2-adrenergic blocking effect by measuring the ability to inhibit the relaxing effect of epinephrine on the isolated tracheal muscle of guinea pigs
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1016/S0960-894X(97)00207-2
DB00264 2474 79 None -4 6 Guinea pig 6.5 pIC50 = 6.5 Functional
Tested for beta-2-adrenergic blocking effect by measuring the ability to inhibit the relaxing effect of epinephrine on the isolated tracheal muscle of guinea pigsTested for beta-2-adrenergic blocking effect by measuring the ability to inhibit the relaxing effect of epinephrine on the isolated tracheal muscle of guinea pigs
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1016/S0960-894X(97)00207-2
3687256 6741 6 None 3 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human adrenergic beta-1 receptor expressed in CHOK1 cells assessed as inhibition of cAMP accumulation by HTRF assayAntagonist activity at human adrenergic beta-1 receptor expressed in CHOK1 cells assessed as inhibition of cAMP accumulation by HTRF assay
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 3 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human adrenergic beta-1 receptor expressed in CHOK1 cells assessed as inhibition of cAMP accumulation by HTRF assayAntagonist activity at human adrenergic beta-1 receptor expressed in CHOK1 cells assessed as inhibition of cAMP accumulation by HTRF assay
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
14739905 206534 0 None 7 2 Human 7.4 pIC50 = 7.4 Functional
Tested for beta1-receptor selectivity in canine cardiac tissue in anesthetized dogsTested for beta1-receptor selectivity in canine cardiac 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 Human 7.4 pIC50 = 7.4 Functional
Tested for beta1-receptor selectivity in canine cardiac tissue in anesthetized dogsTested for beta1-receptor selectivity in canine cardiac tissue in anesthetized dogs
ChEMBL 353 10 2 6 2.3 OC(CNCCOc1ccc(-n2ccnc2)cc1)COc1ccccc1 10.1021/jm00172a033
1499 2052 43 None -269 36 Rat 8.3 pIC50 = 8.3 Functional
In vitro beta-adrenergic activity against beta-1 adrenergic receptor by the inhibition of insulin stimulated [14C]- glucose incorporation into glycogen in isolated rat soleus muscleIn vitro beta-adrenergic activity against beta-1 adrenergic receptor by the inhibition of insulin stimulated [14C]- glucose incorporation into glycogen in isolated rat soleus muscle
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm00094a025
3779 2052 43 None -269 36 Rat 8.3 pIC50 = 8.3 Functional
In vitro beta-adrenergic activity against beta-1 adrenergic receptor by the inhibition of insulin stimulated [14C]- glucose incorporation into glycogen in isolated rat soleus muscleIn vitro beta-adrenergic activity against beta-1 adrenergic receptor by the inhibition of insulin stimulated [14C]- glucose incorporation into glycogen in isolated rat soleus muscle
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm00094a025
536 2052 43 None -269 36 Rat 8.3 pIC50 = 8.3 Functional
In vitro beta-adrenergic activity against beta-1 adrenergic receptor by the inhibition of insulin stimulated [14C]- glucose incorporation into glycogen in isolated rat soleus muscleIn vitro beta-adrenergic activity against beta-1 adrenergic receptor by the inhibition of insulin stimulated [14C]- glucose incorporation into glycogen in isolated rat soleus muscle
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm00094a025
CHEMBL434 2052 43 None -269 36 Rat 8.3 pIC50 = 8.3 Functional
In vitro beta-adrenergic activity against beta-1 adrenergic receptor by the inhibition of insulin stimulated [14C]- glucose incorporation into glycogen in isolated rat soleus muscleIn vitro beta-adrenergic activity against beta-1 adrenergic receptor by the inhibition of insulin stimulated [14C]- glucose incorporation into glycogen in isolated rat soleus muscle
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm00094a025
DB01064 2052 43 None -269 36 Rat 8.3 pIC50 = 8.3 Functional
In vitro beta-adrenergic activity against beta-1 adrenergic receptor by the inhibition of insulin stimulated [14C]- glucose incorporation into glycogen in isolated rat soleus muscleIn vitro beta-adrenergic activity against beta-1 adrenergic receptor by the inhibition of insulin stimulated [14C]- glucose incorporation into glycogen in isolated rat soleus muscle
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm00094a025
14823035 141019 2 None -10 4 Rat 6.3 pIC50 = 6.3 Functional
In vitro beta-adrenergic activity against beta-1 adrenergic receptor by the inhibition of insulin stimulated [14C]- glucose incorporation into glycogen in isolated rat soleus muscleIn vitro beta-adrenergic activity against beta-1 adrenergic receptor by the inhibition of insulin stimulated [14C]- glucose incorporation into glycogen in isolated rat soleus muscle
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 -10 4 Rat 6.3 pIC50 = 6.3 Functional
In vitro beta-adrenergic activity against beta-1 adrenergic receptor by the inhibition of insulin stimulated [14C]- glucose incorporation into glycogen in isolated rat soleus muscleIn vitro beta-adrenergic activity against beta-1 adrenergic receptor by the inhibition of insulin stimulated [14C]- glucose incorporation into glycogen in isolated rat soleus muscle
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
14739908 106749 0 None 1 2 Human 5.3 pIC50 = 5.3 Functional
Tested for beta1-receptor selectivity in canine cardiac tissue in anesthetized dogsTested for beta1-receptor selectivity in canine cardiac 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 Human 5.3 pIC50 = 5.3 Functional
Tested for beta1-receptor selectivity in canine cardiac tissue in anesthetized dogsTested for beta1-receptor selectivity in canine cardiac tissue in anesthetized dogs
ChEMBL 416 10 3 7 1.9 CS(=O)(=O)Nc1ccc(C(O)CNCCOc2ccc(-n3ccnc3)cc2)cc1 10.1021/jm00172a033
44313150 103288 0 None -6 3 Human 6.3 pIC50 = 6.3 Functional
Compound was evaluated for its inhibitory activity against CHO cells expressing the cloned human beta-1 adrenergic receptor (AR) in the presence of [125I]iodocyanopindololCompound was evaluated for its inhibitory activity against CHO cells expressing the cloned human beta-1 adrenergic receptor (AR) in the presence of [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 -6 3 Human 6.3 pIC50 = 6.3 Functional
Compound was evaluated for its inhibitory activity against CHO cells expressing the cloned human beta-1 adrenergic receptor (AR) in the presence of [125I]iodocyanopindololCompound was evaluated for its inhibitory activity against CHO cells expressing the cloned human beta-1 adrenergic receptor (AR) in the presence of [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
5581 101175 10 None -5 6 Human 8.2 pIC50 = 8.2 Functional
Compound was evaluated for its inhibitory activity against CHO cells expressing the cloned human beta-1 adrenergic receptor (AR) in the presence of [125I]iodocyanopindololCompound was evaluated for its inhibitory activity against CHO cells expressing the cloned human beta-1 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 -5 6 Human 8.2 pIC50 = 8.2 Functional
Compound was evaluated for its inhibitory activity against CHO cells expressing the cloned human beta-1 adrenergic receptor (AR) in the presence of [125I]iodocyanopindololCompound was evaluated for its inhibitory activity against CHO cells expressing the cloned human beta-1 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
10283539 167291 0 None -1479 3 Human 5.2 pIC50 = 5.2 Functional
Compound was tested for the antagonistic activity against Beta-1 adrenergic receptorCompound was tested for the antagonistic activity against Beta-1 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 -1479 3 Human 5.2 pIC50 = 5.2 Functional
Compound was tested for the antagonistic activity against Beta-1 adrenergic receptorCompound was tested for the antagonistic activity against Beta-1 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
127034966 135991 0 None -1 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human beta1 receptor expressed in CHO-K1 cells assessed as isoproterenol-induced cAMP level by HTRF assayAntagonist activity at human beta1 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 6.2 pIC50 = 6.2 Functional
Antagonist activity at human beta1 receptor expressed in CHO-K1 cells assessed as isoproterenol-induced cAMP level by HTRF assayAntagonist activity at human beta1 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
187238 77751 9 None - 0 Rat 10.2 pKd = 10.2 Functional
Antagonist activity at rat beta-1 adrenergic receptor S190A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor S190A mutant expressed in CHO cells
ChEMBL 413 5 3 4 2.8 CC(C)(C)NCC(O)COc1cccc2[nH]c(C#N)c(I)c12 10.1021/jm050624l
CHEMBL210309 77751 9 None - 0 Rat 10.2 pKd = 10.2 Functional
Antagonist activity at rat beta-1 adrenergic receptor S190A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor S190A mutant expressed in CHO cells
ChEMBL 413 5 3 4 2.8 CC(C)(C)NCC(O)COc1cccc2[nH]c(C#N)c(I)c12 10.1021/jm050624l
187238 77751 9 None - 0 Rat 10.2 pKd = 10.2 Functional
Antagonist activity at rat beta-1 adrenergic receptor W134A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor W134A mutant expressed in CHO cells
ChEMBL 413 5 3 4 2.8 CC(C)(C)NCC(O)COc1cccc2[nH]c(C#N)c(I)c12 10.1021/jm050624l
CHEMBL210309 77751 9 None - 0 Rat 10.2 pKd = 10.2 Functional
Antagonist activity at rat beta-1 adrenergic receptor W134A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor W134A mutant expressed in CHO cells
ChEMBL 413 5 3 4 2.8 CC(C)(C)NCC(O)COc1cccc2[nH]c(C#N)c(I)c12 10.1021/jm050624l
187238 77751 9 None - 0 Rat 10.2 pKd = 10.2 Functional
Antagonist activity at rat wild type beta-1 adrenergic receptor expressed in CHO cellsAntagonist activity at rat wild type beta-1 adrenergic receptor expressed in CHO cells
ChEMBL 413 5 3 4 2.8 CC(C)(C)NCC(O)COc1cccc2[nH]c(C#N)c(I)c12 10.1021/jm050624l
CHEMBL210309 77751 9 None - 0 Rat 10.2 pKd = 10.2 Functional
Antagonist activity at rat wild type beta-1 adrenergic receptor expressed in CHO cellsAntagonist activity at rat wild type beta-1 adrenergic receptor expressed in CHO cells
ChEMBL 413 5 3 4 2.8 CC(C)(C)NCC(O)COc1cccc2[nH]c(C#N)c(I)c12 10.1021/jm050624l
187238 77751 9 None - 0 Rat 10.1 pKd = 10.1 Functional
Antagonist activity at rat beta-1 adrenergic receptor Y356F mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor Y356F mutant expressed in CHO cells
ChEMBL 413 5 3 4 2.8 CC(C)(C)NCC(O)COc1cccc2[nH]c(C#N)c(I)c12 10.1021/jm050624l
CHEMBL210309 77751 9 None - 0 Rat 10.1 pKd = 10.1 Functional
Antagonist activity at rat beta-1 adrenergic receptor Y356F mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor Y356F mutant expressed in CHO cells
ChEMBL 413 5 3 4 2.8 CC(C)(C)NCC(O)COc1cccc2[nH]c(C#N)c(I)c12 10.1021/jm050624l
13040915 102446 0 None - 0 Guinea pig 10.0 pKd = 10 Functional
Ability to block Beta-1 adrenergic receptor in guinea pig right atria preparation at a duration of 3hAbility to block Beta-1 adrenergic receptor in guinea pig right atria preparation at a duration of 3h
ChEMBL 325 10 2 7 0.8 CCOC(=O)CCNCC(O)COc1ccccc1C(=O)OC 10.1021/jm00354a003
CHEMBL30622 102446 0 None - 0 Guinea pig 10.0 pKd = 10 Functional
Ability to block Beta-1 adrenergic receptor in guinea pig right atria preparation at a duration of 3hAbility to block Beta-1 adrenergic receptor in guinea pig right atria preparation at a duration of 3h
ChEMBL 325 10 2 7 0.8 CCOC(=O)CCNCC(O)COc1ccccc1C(=O)OC 10.1021/jm00354a003
3047497 13273 10 None - 0 Rat 9.6 pKd = 9.6 Functional
Cardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated rat atriaCardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated rat atria
ChEMBL 321 11 2 4 2.8 CC(C)NCC(O)COc1ccc(CCOCC2CCC2)cc1 10.1021/jm00389a008
CHEMBL1192675 13273 10 None - 0 Rat 9.6 pKd = 9.6 Functional
Cardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated rat atriaCardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated rat atria
ChEMBL 321 11 2 4 2.8 CC(C)NCC(O)COc1ccc(CCOCC2CCC2)cc1 10.1021/jm00389a008
CHEMBL543955 13273 10 None - 0 Rat 9.6 pKd = 9.6 Functional
Cardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated rat atriaCardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated rat atria
ChEMBL 321 11 2 4 2.8 CC(C)NCC(O)COc1ccc(CCOCC2CCC2)cc1 10.1021/jm00389a008
3047497 13273 10 None - 0 Rat 9.6 pKd = 9.6 Functional
Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atriaAntagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria
ChEMBL 321 11 2 4 2.8 CC(C)NCC(O)COc1ccc(CCOCC2CCC2)cc1 10.1021/jm00389a008
CHEMBL1192675 13273 10 None - 0 Rat 9.6 pKd = 9.6 Functional
Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atriaAntagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria
ChEMBL 321 11 2 4 2.8 CC(C)NCC(O)COc1ccc(CCOCC2CCC2)cc1 10.1021/jm00389a008
CHEMBL543955 13273 10 None - 0 Rat 9.6 pKd = 9.6 Functional
Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atriaAntagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria
ChEMBL 321 11 2 4 2.8 CC(C)NCC(O)COc1ccc(CCOCC2CCC2)cc1 10.1021/jm00389a008
187238 77751 9 None - 0 Rat 9.5 pKd = 9.5 Functional
Antagonist activity at rat beta-1 adrenergic receptor Y356A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor Y356A mutant expressed in CHO cells
ChEMBL 413 5 3 4 2.8 CC(C)(C)NCC(O)COc1cccc2[nH]c(C#N)c(I)c12 10.1021/jm050624l
CHEMBL210309 77751 9 None - 0 Rat 9.5 pKd = 9.5 Functional
Antagonist activity at rat beta-1 adrenergic receptor Y356A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor Y356A mutant expressed in CHO cells
ChEMBL 413 5 3 4 2.8 CC(C)(C)NCC(O)COc1cccc2[nH]c(C#N)c(I)c12 10.1021/jm050624l
2685 875 15 None - 1 Human 9.5 pKd = 9.5 Functional
Antagonist activity at human beta1 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 beta1 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 9.5 pKd = 9.5 Functional
Antagonist activity at human beta1 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 beta1 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 9.5 pKd = 9.5 Functional
Antagonist activity at human beta1 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 beta1 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
123686 1942 44 None 74 3 Human 9.5 pKd = 9.5 Functional
Antagonist activity at human beta1 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 beta1 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 9.5 pKd = 9.5 Functional
Antagonist activity at human beta1 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 beta1 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 9.5 pKd = 9.5 Functional
Antagonist activity at human beta1 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 beta1 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
33624 3749 29 None - 5 Guinea pig 9.4 pKd = 9.4 Functional
Compound was tested for its Beta-1 adrenergic receptor antagonistic activity on guinea pig atriaCompound was tested for its Beta-1 adrenergic receptor antagonistic activity on guinea pig atria
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 9.4 pKd = 9.4 Functional
Compound was tested for its Beta-1 adrenergic receptor antagonistic activity on guinea pig atriaCompound was tested for its Beta-1 adrenergic receptor antagonistic activity on guinea pig atria
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 9.4 pKd = 9.4 Functional
Compound was tested for its Beta-1 adrenergic receptor antagonistic activity on guinea pig atriaCompound was tested for its Beta-1 adrenergic receptor antagonistic activity on guinea pig atria
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 9.4 pKd = 9.4 Functional
Compound was tested for its Beta-1 adrenergic receptor antagonistic activity on guinea pig atriaCompound was tested for its Beta-1 adrenergic receptor antagonistic activity on guinea pig atria
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 9.4 pKd = 9.4 Functional
Compound was tested for its Beta-1 adrenergic receptor antagonistic activity on guinea pig atriaCompound was tested for its Beta-1 adrenergic receptor antagonistic activity on guinea pig atria
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C 10.1021/jm00350a009
13187527 96631 0 None - 0 Rat 9.3 pKd = 9.3 Functional
Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atriaAntagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria
ChEMBL 321 10 2 4 2.9 CC(C)NCC(O)COc1ccc(CCOC2CCCC2)cc1 10.1021/jm00389a008
CHEMBL267375 96631 0 None - 0 Rat 9.3 pKd = 9.3 Functional
Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atriaAntagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria
ChEMBL 321 10 2 4 2.9 CC(C)NCC(O)COc1ccc(CCOC2CCCC2)cc1 10.1021/jm00389a008
CHEMBL542536 96631 0 None - 0 Rat 9.3 pKd = 9.3 Functional
Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atriaAntagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria
ChEMBL 321 10 2 4 2.9 CC(C)NCC(O)COc1ccc(CCOC2CCCC2)cc1 10.1021/jm00389a008
56598832 87826 0 None 4365 3 Human 9.0 pKd = 9 Functional
Antagonist activity at human beta1 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 beta1 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 9.0 pKd = 9 Functional
Antagonist activity at human beta1 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 beta1 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
66653268 87809 0 None 3311 3 Human 8.8 pKd = 8.8 Functional
Antagonist activity at human beta1 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 beta1 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 8.8 pKd = 8.8 Functional
Antagonist activity at human beta1 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 beta1 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
5311116 2293 6 None 4365 3 Human 8.8 pKd = 8.8 Functional
Antagonist activity at human beta1 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 beta1 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 8.8 pKd = 8.8 Functional
Antagonist activity at human beta1 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 beta1 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 8.8 pKd = 8.8 Functional
Antagonist activity at human beta1 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 beta1 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
165193 3126 60 None -6 13 Human 8.7 pKd = 8.7 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-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 8.7 pKd = 8.7 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-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 8.7 pKd = 8.7 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-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 8.7 pKd = 8.7 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-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 8.7 pKd = 8.7 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-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 8.7 pKd = 8.7 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-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 8.7 pKd = 8.7 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-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 8.7 pKd = 8.7 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-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 8.7 pKd = 8.7 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-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 8.7 pKd = 8.7 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-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 8.7 pKd = 8.7 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-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
12733305 60053 0 None - 0 Guinea pig 8.7 pKd = 8.7 Functional
Antagonist activity of compound against Beta-1 adrenergic receptor in isolated guinea pig left atriaAntagonist activity of compound against Beta-1 adrenergic receptor in isolated guinea pig left atria
ChEMBL 357 8 2 6 2.5 COc1ccc(CCNCC(O)C2=COc3ccccc3O2)cc1OC 10.1021/jm00140a015
CHEMBL174853 60053 0 None - 0 Guinea pig 8.7 pKd = 8.7 Functional
Antagonist activity of compound against Beta-1 adrenergic receptor in isolated guinea pig left atriaAntagonist activity of compound against Beta-1 adrenergic receptor in isolated guinea pig left atria
ChEMBL 357 8 2 6 2.5 COc1ccc(CCNCC(O)C2=COc3ccccc3O2)cc1OC 10.1021/jm00140a015
13187527 96631 0 None - 0 Rat 8.7 pKd = 8.7 Functional
Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atriaAntagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria
ChEMBL 321 10 2 4 2.9 CC(C)NCC(O)COc1ccc(CCOC2CCCC2)cc1 10.1021/jm00389a008
CHEMBL267375 96631 0 None - 0 Rat 8.7 pKd = 8.7 Functional
Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atriaAntagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria
ChEMBL 321 10 2 4 2.9 CC(C)NCC(O)COc1ccc(CCOC2CCCC2)cc1 10.1021/jm00389a008
CHEMBL542536 96631 0 None - 0 Rat 8.7 pKd = 8.7 Functional
Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atriaAntagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria
ChEMBL 321 10 2 4 2.9 CC(C)NCC(O)COc1ccc(CCOC2CCCC2)cc1 10.1021/jm00389a008
44288749 163707 0 None - 0 Rat 8.0 pKd = 8.0 Functional
Beta-1 adrenergic receptor-Antagonism in isolated rat heart ventricle. ( for S-enantiomer)Beta-1 adrenergic receptor-Antagonism in isolated rat heart ventricle. ( for S-enantiomer)
ChEMBL 330 8 2 4 4.0 CC(C)(C)c1ccc(NCC(O)CON=C(C2CC2)C2CC2)cc1 10.1021/jm970338c
CHEMBL42117 163707 0 None - 0 Rat 8.0 pKd = 8.0 Functional
Beta-1 adrenergic receptor-Antagonism in isolated rat heart ventricle. ( for S-enantiomer)Beta-1 adrenergic receptor-Antagonism in isolated rat heart ventricle. ( for S-enantiomer)
ChEMBL 330 8 2 4 4.0 CC(C)(C)c1ccc(NCC(O)CON=C(C2CC2)C2CC2)cc1 10.1021/jm970338c
44288749 163707 0 None - 0 Rat 8.0 pKd = 8.0 Functional
Beta-1 adrenergic receptor-Antagonism in isolated rat heart ventricle. ( for R-enantiomer)Beta-1 adrenergic receptor-Antagonism in isolated rat heart ventricle. ( for R-enantiomer)
ChEMBL 330 8 2 4 4.0 CC(C)(C)c1ccc(NCC(O)CON=C(C2CC2)C2CC2)cc1 10.1021/jm970338c
CHEMBL42117 163707 0 None - 0 Rat 8.0 pKd = 8.0 Functional
Beta-1 adrenergic receptor-Antagonism in isolated rat heart ventricle. ( for R-enantiomer)Beta-1 adrenergic receptor-Antagonism in isolated rat heart ventricle. ( for R-enantiomer)
ChEMBL 330 8 2 4 4.0 CC(C)(C)c1ccc(NCC(O)CON=C(C2CC2)C2CC2)cc1 10.1021/jm970338c
11722868 103887 0 None - 0 Guinea pig 7.0 pKd = 7 Functional
Ability to block Beta-1 adrenergic receptor in guinea pig right atria preparation at a duration of 40 minAbility to block Beta-1 adrenergic receptor in guinea pig right atria preparation at a duration of 40 min
ChEMBL 309 8 2 5 1.9 COC(=O)CCc1ccc(OCC(O)CNC(C)(C)C)cc1 10.1021/jm00354a003
CHEMBL31025 103887 0 None - 0 Guinea pig 7.0 pKd = 7 Functional
Ability to block Beta-1 adrenergic receptor in guinea pig right atria preparation at a duration of 40 minAbility to block Beta-1 adrenergic receptor in guinea pig right atria preparation at a duration of 40 min
ChEMBL 309 8 2 5 1.9 COC(=O)CCc1ccc(OCC(O)CNC(C)(C)C)cc1 10.1021/jm00354a003
13040919 105574 0 None - 0 Guinea pig 5.0 pKd = 5 Functional
Ability to block Beta-1 adrenergic receptor in guinea pig right atria preparation at a duration of 3hAbility to block Beta-1 adrenergic receptor in guinea pig right atria preparation at a duration of 3h
ChEMBL 339 9 2 7 1.1 CCOC(=O)C(C)(C)NCC(O)COc1ccccc1C(=O)OC 10.1021/jm00354a003
CHEMBL31335 105574 0 None - 0 Guinea pig 5.0 pKd = 5 Functional
Ability to block Beta-1 adrenergic receptor in guinea pig right atria preparation at a duration of 3hAbility to block Beta-1 adrenergic receptor in guinea pig right atria preparation at a duration of 3h
ChEMBL 339 9 2 7 1.1 CCOC(=O)C(C)(C)NCC(O)COc1ccccc1C(=O)OC 10.1021/jm00354a003
44371562 49435 0 None - 0 Guinea pig 5.0 pKd = 5.0 Functional
Antagonist activity against beta-1 adrenergic receptor in isolated guinea pig atriaAntagonist activity against beta-1 adrenergic receptor in isolated guinea pig atria
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 = 5.0 Functional
Antagonist activity against beta-1 adrenergic receptor in isolated guinea pig atriaAntagonist activity against beta-1 adrenergic receptor in isolated guinea pig atria
ChEMBL 257 7 2 5 1.2 CC(C)NCC(O)COC(=O)Cc1cccs1 10.1021/jm00387a006
20554487 13173 0 None - 0 Rat 7.9 pKd = 7.9 Functional
Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atriaAntagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria
ChEMBL 369 11 2 5 2.2 CC(C)NCC(O)COc1ccc(CCS(=O)(=O)CC2CCC2)cc1 10.1021/jm00389a008
CHEMBL1191855 13173 0 None - 0 Rat 7.9 pKd = 7.9 Functional
Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atriaAntagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria
ChEMBL 369 11 2 5 2.2 CC(C)NCC(O)COc1ccc(CCS(=O)(=O)CC2CCC2)cc1 10.1021/jm00389a008
CHEMBL543011 13173 0 None - 0 Rat 7.9 pKd = 7.9 Functional
Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atriaAntagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria
ChEMBL 369 11 2 5 2.2 CC(C)NCC(O)COc1ccc(CCS(=O)(=O)CC2CCC2)cc1 10.1021/jm00389a008
54757126 65147 0 None - 0 Human 7.0 pKd = 7.0 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in CGP 12177-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in CGP 12177-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 7.0 pKd = 7.0 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in CGP 12177-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in CGP 12177-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
14856222 172070 0 None - 0 Guinea pig 4.9 pKd = 4.9 Functional
Antagonist activity against beta-1 adrenergic receptor in isolated guinea pig atriaAntagonist activity against beta-1 adrenergic receptor in isolated guinea pig atria
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 4.9 pKd = 4.9 Functional
Antagonist activity against beta-1 adrenergic receptor in isolated guinea pig atriaAntagonist activity against beta-1 adrenergic receptor in isolated guinea pig atria
ChEMBL 217 5 2 4 0.9 CC(C)C(=O)OCC(O)CNC(C)(C)C 10.1021/jm00387a006
12733304 127702 0 None - 0 Guinea pig 5.9 pKd = 5.9 Functional
Antagonist activity of compound against Beta-1 adrenergic receptor in isolated guinea pig left atriaAntagonist activity of compound against Beta-1 adrenergic receptor in isolated guinea pig left atria
ChEMBL 275 3 1 4 2.5 OC(CN1CCCCCC1)C1=COc2ccccc2O1 10.1021/jm00140a015
CHEMBL366558 127702 0 None - 0 Guinea pig 5.9 pKd = 5.9 Functional
Antagonist activity of compound against Beta-1 adrenergic receptor in isolated guinea pig left atriaAntagonist activity of compound against Beta-1 adrenergic receptor in isolated guinea pig left atria
ChEMBL 275 3 1 4 2.5 OC(CN1CCCCCC1)C1=COc2ccccc2O1 10.1021/jm00140a015
44288217 154602 0 None - 0 Rat 7.9 pKd = 7.9 Functional
Beta-1 adrenergic receptor-Antagonism in isolated rat heart ventricle. ( for R-enantiomer)Beta-1 adrenergic receptor-Antagonism in isolated rat heart ventricle. ( for R-enantiomer)
ChEMBL 288 8 2 4 3.0 Cc1ccc(NCC(O)CON=C(C2CC2)C2CC2)cc1 10.1021/jm970338c
CHEMBL40217 154602 0 None - 0 Rat 7.9 pKd = 7.9 Functional
Beta-1 adrenergic receptor-Antagonism in isolated rat heart ventricle. ( for R-enantiomer)Beta-1 adrenergic receptor-Antagonism in isolated rat heart ventricle. ( for R-enantiomer)
ChEMBL 288 8 2 4 3.0 Cc1ccc(NCC(O)CON=C(C2CC2)C2CC2)cc1 10.1021/jm970338c
165193 3126 60 None -27 13 Guinea pig 7.9 pKd = 7.9 Functional
Cardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated guinea pig tracheaCardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated guinea pig trachea
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00389a008
2303 3126 60 None -27 13 Guinea pig 7.9 pKd = 7.9 Functional
Cardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated guinea pig tracheaCardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated guinea pig trachea
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00389a008
4946 3126 60 None -27 13 Guinea pig 7.9 pKd = 7.9 Functional
Cardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated guinea pig tracheaCardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated guinea pig trachea
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00389a008
564 3126 60 None -27 13 Guinea pig 7.9 pKd = 7.9 Functional
Cardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated guinea pig tracheaCardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated guinea pig trachea
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00389a008
62882 3126 60 None -27 13 Guinea pig 7.9 pKd = 7.9 Functional
Cardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated guinea pig tracheaCardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated guinea pig trachea
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00389a008
63 3126 60 None -27 13 Guinea pig 7.9 pKd = 7.9 Functional
Cardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated guinea pig tracheaCardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated guinea pig trachea
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00389a008
66366 3126 60 None -27 13 Guinea pig 7.9 pKd = 7.9 Functional
Cardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated guinea pig tracheaCardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated guinea pig trachea
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00389a008
91536 3126 60 None -27 13 Guinea pig 7.9 pKd = 7.9 Functional
Cardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated guinea pig tracheaCardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated guinea pig trachea
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00389a008
CHEMBL27 3126 60 None -27 13 Guinea pig 7.9 pKd = 7.9 Functional
Cardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated guinea pig tracheaCardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated guinea pig trachea
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00389a008
CHEMBL452861 3126 60 None -27 13 Guinea pig 7.9 pKd = 7.9 Functional
Cardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated guinea pig tracheaCardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated guinea pig trachea
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00389a008
DB00571 3126 60 None -27 13 Guinea pig 7.9 pKd = 7.9 Functional
Cardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated guinea pig tracheaCardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated guinea pig trachea
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00389a008
44371486 14116 0 None - 0 Guinea pig 6.9 pKd = 6.9 Functional
Antagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pigAntagonism of the isoprenaline-induced positive chronotropic effect on the atria 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 6.9 pKd = 6.9 Functional
Antagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pigAntagonism of the isoprenaline-induced positive chronotropic effect on the atria 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 6.9 pKd = 6.9 Functional
Antagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pigAntagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pig
ChEMBL 230 7 2 4 1.9 CCC/C(C)=N\OCC(O)CNC(C)(C)C 10.1021/jm00180a007
54757229 65169 0 None - 0 Human 6.9 pKd = 6.9 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in CGP 12177-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in CGP 12177-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 6.9 pKd = 6.9 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in CGP 12177-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in CGP 12177-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
44371537 50382 0 None - 0 Guinea pig 4.9 pKd = 4.9 Functional
Antagonist activity against beta-1 adrenergic receptor in isolated guinea pig atriaAntagonist activity against beta-1 adrenergic receptor in isolated guinea pig atria
ChEMBL 243 6 2 4 1.5 CC(C)NCC(O)COC(=O)C1CCCCC1 10.1021/jm00387a006
CHEMBL157557 50382 0 None - 0 Guinea pig 4.9 pKd = 4.9 Functional
Antagonist activity against beta-1 adrenergic receptor in isolated guinea pig atriaAntagonist activity against beta-1 adrenergic receptor in isolated guinea pig atria
ChEMBL 243 6 2 4 1.5 CC(C)NCC(O)COC(=O)C1CCCCC1 10.1021/jm00387a006
12348305 96535 0 None - 0 Guinea pig 6.9 pKd = 6.9 Functional
Antagonist activity against beta-1 adrenergic receptor in isolated guinea pig atriaAntagonist activity against beta-1 adrenergic receptor in isolated guinea pig atria
ChEMBL 281 6 2 6 0.9 CC(C)NCC(O)COC(=O)c1ccc2c(c1)OCO2 10.1021/jm00387a006
CHEMBL266548 96535 0 None - 0 Guinea pig 6.9 pKd = 6.9 Functional
Antagonist activity against beta-1 adrenergic receptor in isolated guinea pig atriaAntagonist activity against beta-1 adrenergic receptor in isolated guinea pig atria
ChEMBL 281 6 2 6 0.9 CC(C)NCC(O)COC(=O)c1ccc2c(c1)OCO2 10.1021/jm00387a006
2369 615 75 None - 2 Rat 6.9 pKd = 6.9 Functional
Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atriaAntagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria
ChEMBL 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C 10.1021/jm00389a008
356 615 75 None - 2 Rat 6.9 pKd = 6.9 Functional
Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atriaAntagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria
ChEMBL 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C 10.1021/jm00389a008
549 615 75 None - 2 Rat 6.9 pKd = 6.9 Functional
Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atriaAntagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria
ChEMBL 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C 10.1021/jm00389a008
CHEMBL423 615 75 None - 2 Rat 6.9 pKd = 6.9 Functional
Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atriaAntagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria
ChEMBL 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C 10.1021/jm00389a008
DB00195 615 75 None - 2 Rat 6.9 pKd = 6.9 Functional
Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atriaAntagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria
ChEMBL 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C 10.1021/jm00389a008
12606708 12954 0 None - 0 Guinea pig 5.9 pKd = 5.9 Functional
Antagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pigAntagonism of the isoprenaline-induced positive chronotropic effect on the atria 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 5.9 pKd = 5.9 Functional
Antagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pigAntagonism of the isoprenaline-induced positive chronotropic effect on the atria 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 5.9 pKd = 5.9 Functional
Antagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pigAntagonism of the isoprenaline-induced positive chronotropic effect on the atria 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
44287476 11892 0 None - 0 Guinea pig 5.9 pKd = 5.9 Functional
Antagonistic activity against beta-1 adrenergic receptor of isolated guinea pig atriaAntagonistic activity against beta-1 adrenergic receptor of isolated guinea pig atria
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 5.9 pKd = 5.9 Functional
Antagonistic activity against beta-1 adrenergic receptor of isolated guinea pig atriaAntagonistic activity against beta-1 adrenergic receptor of isolated guinea pig atria
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 5.9 pKd = 5.9 Functional
Antagonistic activity against beta-1 adrenergic receptor of isolated guinea pig atriaAntagonistic activity against beta-1 adrenergic receptor of isolated guinea pig atria
ChEMBL 230 7 2 4 1.9 CCC(CC)=NOCC(O)CNC(C)(C)C 10.1021/jm00380a001
3047527 201918 1 None - 0 Rat 6.9 pKd = 6.9 Functional
Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atriaAntagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria
ChEMBL 335 11 2 4 3.2 CC(C)NCC(O)COc1ccc(CCOCC2CCCC2)cc1 10.1021/jm00389a008
CHEMBL6712 201918 1 None - 0 Rat 6.9 pKd = 6.9 Functional
Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atriaAntagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria
ChEMBL 335 11 2 4 3.2 CC(C)NCC(O)COc1ccc(CCOCC2CCCC2)cc1 10.1021/jm00389a008
2447486 62716 1 None - 2 Guinea pig 7.9 pKd = 7.9 Functional
Compound was tested for its Beta-1 adrenergic receptor antagonistic activity on guinea pig atriaCompound was tested for its Beta-1 adrenergic receptor antagonistic activity on guinea pig atria
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 7.9 pKd = 7.9 Functional
Compound was tested for its Beta-1 adrenergic receptor antagonistic activity on guinea pig atriaCompound was tested for its Beta-1 adrenergic receptor antagonistic activity on guinea pig atria
ChEMBL 324 5 2 4 3.2 CC(C)(C)NC[C@@H](O)CON=C1c2ccccc2-c2ccccc21 10.1021/jm00350a009
54756927 65141 0 None - 0 Human 7.9 pKd = 7.9 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-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 7.9 pKd = 7.9 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-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
44288217 154602 0 None - 0 Rat 7.9 pKd = 7.9 Functional
Beta-1 adrenergic receptor-Antagonism in isolated rat heart ventricle. ( for S-enantiomer)Beta-1 adrenergic receptor-Antagonism in isolated rat heart ventricle. ( for S-enantiomer)
ChEMBL 288 8 2 4 3.0 Cc1ccc(NCC(O)CON=C(C2CC2)C2CC2)cc1 10.1021/jm970338c
CHEMBL40217 154602 0 None - 0 Rat 7.9 pKd = 7.9 Functional
Beta-1 adrenergic receptor-Antagonism in isolated rat heart ventricle. ( for S-enantiomer)Beta-1 adrenergic receptor-Antagonism in isolated rat heart ventricle. ( for S-enantiomer)
ChEMBL 288 8 2 4 3.0 Cc1ccc(NCC(O)CON=C(C2CC2)C2CC2)cc1 10.1021/jm970338c
12606686 92413 3 None - 0 Guinea pig 4.9 pKd = 4.9 Functional
Antagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pigAntagonism of the isoprenaline-induced positive chronotropic effect on the atria 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 4.9 pKd = 4.9 Functional
Antagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pigAntagonism of the isoprenaline-induced positive chronotropic effect on the atria 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 4.9 pKd = 4.9 Functional
Antagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pigAntagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pig
ChEMBL 189 5 2 3 1.2 CC(C)OCC(O)CNC(C)(C)C 10.1021/jm00180a007
1786 2474 79 None -4 6 Guinea pig 7.8 pKd = 7.8 Functional
Compound was tested for its Beta-1 adrenergic receptor antagonistic activity on guinea pig arteriaCompound was tested for its Beta-1 adrenergic receptor antagonistic activity on guinea pig arteria
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm00350a009
4171 2474 79 None -4 6 Guinea pig 7.8 pKd = 7.8 Functional
Compound was tested for its Beta-1 adrenergic receptor antagonistic activity on guinea pig arteriaCompound was tested for its Beta-1 adrenergic receptor antagonistic activity on guinea pig arteria
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm00350a009
553 2474 79 None -4 6 Guinea pig 7.8 pKd = 7.8 Functional
Compound was tested for its Beta-1 adrenergic receptor antagonistic activity on guinea pig arteriaCompound was tested for its Beta-1 adrenergic receptor antagonistic activity on guinea pig arteria
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm00350a009
CHEMBL13 2474 79 None -4 6 Guinea pig 7.8 pKd = 7.8 Functional
Compound was tested for its Beta-1 adrenergic receptor antagonistic activity on guinea pig arteriaCompound was tested for its Beta-1 adrenergic receptor antagonistic activity on guinea pig arteria
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm00350a009
DB00264 2474 79 None -4 6 Guinea pig 7.8 pKd = 7.8 Functional
Compound was tested for its Beta-1 adrenergic receptor antagonistic activity on guinea pig arteriaCompound was tested for its Beta-1 adrenergic receptor antagonistic activity on guinea pig arteria
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm00350a009
12733308 122023 0 None - 0 Guinea pig 6.8 pKd = 6.8 Functional
Antagonist activity of compound against Beta-1 adrenergic receptor in isolated guinea pig left atriaAntagonist activity of compound against Beta-1 adrenergic receptor in isolated guinea pig left atria
ChEMBL 393 4 2 7 3.1 Oc1nc2ccccc2n1C1CCN(CC(O)C2=COc3ccccc3O2)CC1 10.1021/jm00140a015
CHEMBL360139 122023 0 None - 0 Guinea pig 6.8 pKd = 6.8 Functional
Antagonist activity of compound against Beta-1 adrenergic receptor in isolated guinea pig left atriaAntagonist activity of compound against Beta-1 adrenergic receptor in isolated guinea pig left atria
ChEMBL 393 4 2 7 3.1 Oc1nc2ccccc2n1C1CCN(CC(O)C2=COc3ccccc3O2)CC1 10.1021/jm00140a015
3047500 13151 1 None - 0 Rat 6.8 pKd = 6.8 Functional
Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atriaAntagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria
ChEMBL 349 11 2 4 3.6 CC(C)NCC(O)COc1ccc(CCOCC2CCCCC2)cc1 10.1021/jm00389a008
CHEMBL1191645 13151 1 None - 0 Rat 6.8 pKd = 6.8 Functional
Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atriaAntagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria
ChEMBL 349 11 2 4 3.6 CC(C)NCC(O)COc1ccc(CCOCC2CCCCC2)cc1 10.1021/jm00389a008
CHEMBL542776 13151 1 None - 0 Rat 6.8 pKd = 6.8 Functional
Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atriaAntagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria
ChEMBL 349 11 2 4 3.6 CC(C)NCC(O)COc1ccc(CCOCC2CCCCC2)cc1 10.1021/jm00389a008
3047500 13151 1 None - 0 Rat 6.8 pKd = 6.8 Functional
Cardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated rat atriaCardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated rat atria
ChEMBL 349 11 2 4 3.6 CC(C)NCC(O)COc1ccc(CCOCC2CCCCC2)cc1 10.1021/jm00389a008
CHEMBL1191645 13151 1 None - 0 Rat 6.8 pKd = 6.8 Functional
Cardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated rat atriaCardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated rat atria
ChEMBL 349 11 2 4 3.6 CC(C)NCC(O)COc1ccc(CCOCC2CCCCC2)cc1 10.1021/jm00389a008
CHEMBL542776 13151 1 None - 0 Rat 6.8 pKd = 6.8 Functional
Cardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated rat atriaCardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated rat atria
ChEMBL 349 11 2 4 3.6 CC(C)NCC(O)COc1ccc(CCOCC2CCCCC2)cc1 10.1021/jm00389a008
44287622 11881 0 None - 0 Guinea pig 4.8 pKd = 4.8 Functional
Antagonistic activity against beta-1 adrenergic receptor of isolated guinea pig atriaAntagonistic activity against beta-1 adrenergic receptor of isolated guinea pig atria
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 4.8 pKd = 4.8 Functional
Antagonistic activity against beta-1 adrenergic receptor of isolated guinea pig atriaAntagonistic activity against beta-1 adrenergic receptor of isolated guinea pig atria
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 4.8 pKd = 4.8 Functional
Antagonistic activity against beta-1 adrenergic receptor of isolated guinea pig atriaAntagonistic activity against beta-1 adrenergic receptor of isolated guinea pig atria
ChEMBL 258 7 2 4 2.4 CC(C)C(=NOCC(O)CNC(C)(C)C)C(C)C 10.1021/jm00380a001
10403687 2465 2 None - 2 Guinea pig 4.8 pKd = 4.8 Functional
Compound was evaluated for its antagonist affinity towards Beta-1 adrenergic receptor of guinea pigCompound was evaluated for its antagonist affinity towards Beta-1 adrenergic receptor of guinea pig
ChEMBL 319 8 2 2 3.9 CNCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm991056a
1205 2465 2 None - 2 Guinea pig 4.8 pKd = 4.8 Functional
Compound was evaluated for its antagonist affinity towards Beta-1 adrenergic receptor of guinea pigCompound was evaluated for its antagonist affinity towards Beta-1 adrenergic receptor of guinea pig
ChEMBL 319 8 2 2 3.9 CNCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm991056a
CHEMBL275035 2465 2 None - 2 Guinea pig 4.8 pKd = 4.8 Functional
Compound was evaluated for its antagonist affinity towards Beta-1 adrenergic receptor of guinea pigCompound was evaluated for its antagonist affinity towards Beta-1 adrenergic receptor of guinea pig
ChEMBL 319 8 2 2 3.9 CNCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm991056a
12733301 60074 1 None - 0 Guinea pig 7.8 pKd = 7.8 Functional
Antagonist activity of compound against Beta-1 adrenergic receptor in isolated guinea pig left atriaAntagonist activity of compound against Beta-1 adrenergic receptor in isolated guinea pig left atria
ChEMBL 235 4 2 4 1.7 CC(C)NCC(O)C1=COc2ccccc2O1 10.1021/jm00140a015
CHEMBL175010 60074 1 None - 0 Guinea pig 7.8 pKd = 7.8 Functional
Antagonist activity of compound against Beta-1 adrenergic receptor in isolated guinea pig left atriaAntagonist activity of compound against Beta-1 adrenergic receptor in isolated guinea pig left atria
ChEMBL 235 4 2 4 1.7 CC(C)NCC(O)C1=COc2ccccc2O1 10.1021/jm00140a015
44371406 11544 0 None - 0 Guinea pig 6.8 pKd = 6.8 Functional
Antagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pigAntagonism of the isoprenaline-induced positive chronotropic effect on the atria 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 6.8 pKd = 6.8 Functional
Antagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pigAntagonism of the isoprenaline-induced positive chronotropic effect on the atria 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 6.8 pKd = 6.8 Functional
Antagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pigAntagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pig
ChEMBL 278 9 2 4 2.4 C/C(CCc1ccccc1)=N/OCC(O)CNC(C)C 10.1021/jm00180a007
44264144 13152 0 None - 0 Rat 6.8 pKd = 6.8 Functional
Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atriaAntagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria
ChEMBL 385 11 2 6 1.6 CC(C)NCC(O)COc1ccc(CCS(=O)(=O)CC2CCCO2)cc1 10.1021/jm00389a008
CHEMBL1191646 13152 0 None - 0 Rat 6.8 pKd = 6.8 Functional
Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atriaAntagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria
ChEMBL 385 11 2 6 1.6 CC(C)NCC(O)COc1ccc(CCS(=O)(=O)CC2CCCO2)cc1 10.1021/jm00389a008
CHEMBL542777 13152 0 None - 0 Rat 6.8 pKd = 6.8 Functional
Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atriaAntagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria
ChEMBL 385 11 2 6 1.6 CC(C)NCC(O)COc1ccc(CCS(=O)(=O)CC2CCCO2)cc1 10.1021/jm00389a008
361497 48800 2 None - 0 Guinea pig 5.8 pKd = 5.8 Functional
Antagonist activity against beta-1 adrenergic receptor in isolated guinea pig atriaAntagonist activity against beta-1 adrenergic receptor in isolated guinea pig atria
ChEMBL 243 6 2 5 1.3 CC(C)NCC(O)COC(=O)c1cccs1 10.1021/jm00387a006
CHEMBL156147 48800 2 None - 0 Guinea pig 5.8 pKd = 5.8 Functional
Antagonist activity against beta-1 adrenergic receptor in isolated guinea pig atriaAntagonist activity against beta-1 adrenergic receptor in isolated guinea pig atria
ChEMBL 243 6 2 5 1.3 CC(C)NCC(O)COC(=O)c1cccs1 10.1021/jm00387a006
12778441 77948 0 None - 0 Guinea pig 7.8 pKd = 7.8 Functional
Compound was tested for its Beta-1 adrenergic receptor antagonistic activity on guinea pig atriaCompound was tested for its Beta-1 adrenergic receptor antagonistic activity on guinea pig atria
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 7.8 pKd = 7.8 Functional
Compound was tested for its Beta-1 adrenergic receptor antagonistic activity on guinea pig atriaCompound was tested for its Beta-1 adrenergic receptor antagonistic activity on guinea pig atria
ChEMBL 338 7 2 4 3.6 CCC(C)(C)NC[C@H](O)CON=C1c2ccccc2-c2ccccc21 10.1021/jm00350a009
3486 3096 51 None - 0 Guinea pig 5.8 pKd = 5.8 Functional
Antagonist activity against beta-1 adrenergic receptor in isolated guinea pig atriaAntagonist activity against beta-1 adrenergic receptor in isolated guinea pig atria
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 5.8 pKd = 5.8 Functional
Antagonist activity against beta-1 adrenergic receptor in isolated guinea pig atriaAntagonist activity against beta-1 adrenergic receptor in isolated guinea pig atria
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 5.8 pKd = 5.8 Functional
Antagonist activity against beta-1 adrenergic receptor in isolated guinea pig atriaAntagonist activity against beta-1 adrenergic receptor in isolated guinea pig atria
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 5.8 pKd = 5.8 Functional
Antagonist activity against beta-1 adrenergic receptor in isolated guinea pig atriaAntagonist activity against beta-1 adrenergic receptor in isolated guinea pig atria
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 5.8 pKd = 5.8 Functional
Antagonist activity against beta-1 adrenergic receptor in isolated guinea pig atriaAntagonist activity against beta-1 adrenergic receptor in isolated guinea pig atria
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 5.8 pKd = 5.8 Functional
Antagonistic activity against beta-1 adrenergic receptor of isolated guinea pig atriaAntagonistic activity against beta-1 adrenergic receptor of isolated guinea pig atria
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 5.8 pKd = 5.8 Functional
Antagonistic activity against beta-1 adrenergic receptor of isolated guinea pig atriaAntagonistic activity against beta-1 adrenergic receptor of isolated guinea pig atria
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 5.8 pKd = 5.8 Functional
Antagonistic activity against beta-1 adrenergic receptor of isolated guinea pig atriaAntagonistic activity against beta-1 adrenergic receptor of isolated guinea pig atria
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 5.8 pKd = 5.8 Functional
Antagonistic activity against beta-1 adrenergic receptor of isolated guinea pig atriaAntagonistic activity against beta-1 adrenergic receptor of isolated guinea pig atria
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 5.8 pKd = 5.8 Functional
Antagonistic activity against beta-1 adrenergic receptor of isolated guinea pig atriaAntagonistic activity against beta-1 adrenergic receptor of isolated guinea pig atria
ChEMBL 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C 10.1021/jm00380a001
12606710 13270 0 None - 0 Guinea pig 4.8 pKd = 4.8 Functional
Antagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pigAntagonism of the isoprenaline-induced positive chronotropic effect on the atria 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 4.8 pKd = 4.8 Functional
Antagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pigAntagonism of the isoprenaline-induced positive chronotropic effect on the atria 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 4.8 pKd = 4.8 Functional
Antagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pigAntagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pig
ChEMBL 204 6 3 4 0.7 CC(C)NOCC(O)CNC(C)(C)C 10.1021/jm00180a007
44287431 11109 0 None - 0 Guinea pig 4.8 pKd = 4.8 Functional
Antagonistic activity against beta-1 adrenergic receptor of isolated guinea pig atriaAntagonistic activity against beta-1 adrenergic receptor of isolated guinea pig atria
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 4.8 pKd = 4.8 Functional
Antagonistic activity against beta-1 adrenergic receptor of isolated guinea pig atriaAntagonistic activity against beta-1 adrenergic receptor of isolated guinea pig atria
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 4.8 pKd = 4.8 Functional
Antagonistic activity against beta-1 adrenergic receptor of isolated guinea pig atriaAntagonistic activity against beta-1 adrenergic receptor of isolated guinea pig atria
ChEMBL 244 8 2 4 2.0 CC(C)NCC(O)CON=C(C(C)C)C(C)C 10.1021/jm00380a001
54757331 65171 0 None - 0 Human 7.8 pKd = 7.8 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-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 7.8 pKd = 7.8 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-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
155774 4021 33 None 64 3 Human 7.8 pKd = 7.8 Functional
Antagonist activity at human beta1 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 beta1 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 7.8 pKd = 7.8 Functional
Antagonist activity at human beta1 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 beta1 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 7.8 pKd = 7.8 Functional
Antagonist activity at human beta1 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 beta1 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 7.8 pKd = 7.8 Functional
Antagonist activity at human beta1 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 beta1 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 7.8 pKd = 7.8 Functional
Antagonist activity at human beta1 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 beta1 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
56598831 88699 0 None 1023 3 Human 7.8 pKd = 7.8 Functional
Antagonist activity at human beta1 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 beta1 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 7.8 pKd = 7.8 Functional
Antagonist activity at human beta1 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 beta1 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 7.8 pKd = 7.8 Functional
Antagonist activity at human beta1 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 beta1 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
44264411 13274 0 None - 0 Rat 7.8 pKd = 7.8 Functional
Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atriaAntagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria
ChEMBL 443 15 2 6 3.6 COc1ccc(CCNCC(O)COc2ccc(CCOCC3CCC3)cc2)cc1OC 10.1021/jm00389a008
CHEMBL1192677 13274 0 None - 0 Rat 7.8 pKd = 7.8 Functional
Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atriaAntagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria
ChEMBL 443 15 2 6 3.6 COc1ccc(CCNCC(O)COc2ccc(CCOCC3CCC3)cc2)cc1OC 10.1021/jm00389a008
CHEMBL543957 13274 0 None - 0 Rat 7.8 pKd = 7.8 Functional
Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atriaAntagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria
ChEMBL 443 15 2 6 3.6 COc1ccc(CCNCC(O)COc2ccc(CCOCC3CCC3)cc2)cc1OC 10.1021/jm00389a008
3486 3096 51 None - 0 Guinea pig 6.8 pKd = 6.8 Functional
Antagonist activity of compound against Beta-1 adrenergic receptor in isolated guinea pig left atriaAntagonist activity of compound against Beta-1 adrenergic receptor in isolated guinea pig left atria
ChEMBL 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C 10.1021/jm00140a015
4883 3096 51 None - 0 Guinea pig 6.8 pKd = 6.8 Functional
Antagonist activity of compound against Beta-1 adrenergic receptor in isolated guinea pig left atriaAntagonist activity of compound against Beta-1 adrenergic receptor in isolated guinea pig left atria
ChEMBL 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C 10.1021/jm00140a015
555 3096 51 None - 0 Guinea pig 6.8 pKd = 6.8 Functional
Antagonist activity of compound against Beta-1 adrenergic receptor in isolated guinea pig left atriaAntagonist activity of compound against Beta-1 adrenergic receptor in isolated guinea pig left atria
ChEMBL 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C 10.1021/jm00140a015
CHEMBL6995 3096 51 None - 0 Guinea pig 6.8 pKd = 6.8 Functional
Antagonist activity of compound against Beta-1 adrenergic receptor in isolated guinea pig left atriaAntagonist activity of compound against Beta-1 adrenergic receptor in isolated guinea pig left atria
ChEMBL 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C 10.1021/jm00140a015
DB01297 3096 51 None - 0 Guinea pig 6.8 pKd = 6.8 Functional
Antagonist activity of compound against Beta-1 adrenergic receptor in isolated guinea pig left atriaAntagonist activity of compound against Beta-1 adrenergic receptor in isolated guinea pig left atria
ChEMBL 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C 10.1021/jm00140a015
137 367 47 None -2 4 Human 6.8 pKd = 6.8 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in CGP 12177-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in CGP 12177-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 -2 4 Human 6.8 pKd = 6.8 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in CGP 12177-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in CGP 12177-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 -2 4 Human 6.8 pKd = 6.8 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in CGP 12177-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in CGP 12177-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 -2 4 Human 6.8 pKd = 6.8 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in CGP 12177-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in CGP 12177-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 -2 4 Human 6.8 pKd = 6.8 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in CGP 12177-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in CGP 12177-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 -2 4 Human 6.8 pKd = 6.8 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in CGP 12177-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in CGP 12177-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
54756927 65141 0 None - 0 Human 6.7 pKd = 6.7 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in CGP 12177-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in CGP 12177-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 6.7 pKd = 6.7 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in CGP 12177-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in CGP 12177-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
12606701 11108 0 None - 0 Guinea pig 5.7 pKd = 5.7 Functional
Antagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pigAntagonism of the isoprenaline-induced positive chronotropic effect on the atria 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 5.7 pKd = 5.7 Functional
Antagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pigAntagonism of the isoprenaline-induced positive chronotropic effect on the atria 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 5.7 pKd = 5.7 Functional
Antagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pigAntagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pig
ChEMBL 228 6 2 4 1.7 CC(C)NCC(O)CON=C1CCCCC1 10.1021/jm00180a007
44371426 14177 0 None - 0 Guinea pig 6.7 pKd = 6.7 Functional
Antagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pigAntagonism of the isoprenaline-induced positive chronotropic effect on the atria 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 6.7 pKd = 6.7 Functional
Antagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pigAntagonism of the isoprenaline-induced positive chronotropic effect on the atria 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 6.7 pKd = 6.7 Functional
Antagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pigAntagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pig
ChEMBL 216 6 2 4 1.5 CC/C(C)=N\OCC(O)CNC(C)(C)C 10.1021/jm00180a007
165193 3126 60 None -6 13 Human 6.7 pKd = 6.7 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in CGP 12177-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in CGP 12177-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 6.7 pKd = 6.7 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in CGP 12177-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in CGP 12177-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 6.7 pKd = 6.7 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in CGP 12177-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in CGP 12177-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 6.7 pKd = 6.7 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in CGP 12177-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in CGP 12177-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 6.7 pKd = 6.7 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in CGP 12177-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in CGP 12177-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 6.7 pKd = 6.7 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in CGP 12177-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in CGP 12177-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 6.7 pKd = 6.7 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in CGP 12177-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in CGP 12177-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 6.7 pKd = 6.7 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in CGP 12177-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in CGP 12177-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 6.7 pKd = 6.7 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in CGP 12177-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in CGP 12177-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 6.7 pKd = 6.7 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in CGP 12177-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in CGP 12177-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 6.7 pKd = 6.7 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in CGP 12177-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in CGP 12177-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
11768868 13035 4 None - 0 Guinea pig 4.7 pKd = 4.7 Functional
Antagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pigAntagonism of the isoprenaline-induced positive chronotropic effect on the atria 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 4.7 pKd = 4.7 Functional
Antagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pigAntagonism of the isoprenaline-induced positive chronotropic effect on the atria 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 4.7 pKd = 4.7 Functional
Antagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pigAntagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pig
ChEMBL 161 4 2 3 0.4 COCC(O)CNC(C)(C)C 10.1021/jm00180a007
12606701 11108 0 None - 0 Guinea pig 4.7 pKd = 4.7 Functional
Antagonistic activity against beta-1 adrenergic receptor of isolated guinea pig atriaAntagonistic activity against beta-1 adrenergic receptor of isolated guinea pig atria
ChEMBL 228 6 2 4 1.7 CC(C)NCC(O)CON=C1CCCCC1 10.1021/jm00380a001
CHEMBL1178787 11108 0 None - 0 Guinea pig 4.7 pKd = 4.7 Functional
Antagonistic activity against beta-1 adrenergic receptor of isolated guinea pig atriaAntagonistic activity against beta-1 adrenergic receptor of isolated guinea pig atria
ChEMBL 228 6 2 4 1.7 CC(C)NCC(O)CON=C1CCCCC1 10.1021/jm00380a001
CHEMBL41378 11108 0 None - 0 Guinea pig 4.7 pKd = 4.7 Functional
Antagonistic activity against beta-1 adrenergic receptor of isolated guinea pig atriaAntagonistic activity against beta-1 adrenergic receptor of isolated guinea pig atria
ChEMBL 228 6 2 4 1.7 CC(C)NCC(O)CON=C1CCCCC1 10.1021/jm00380a001
165193 3126 60 None -27 13 Guinea pig 8.6 pKd = 8.6 Functional
Antagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pigAntagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pig
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00180a007
2303 3126 60 None -27 13 Guinea pig 8.6 pKd = 8.6 Functional
Antagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pigAntagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pig
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00180a007
4946 3126 60 None -27 13 Guinea pig 8.6 pKd = 8.6 Functional
Antagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pigAntagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pig
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00180a007
564 3126 60 None -27 13 Guinea pig 8.6 pKd = 8.6 Functional
Antagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pigAntagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pig
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00180a007
62882 3126 60 None -27 13 Guinea pig 8.6 pKd = 8.6 Functional
Antagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pigAntagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pig
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00180a007
63 3126 60 None -27 13 Guinea pig 8.6 pKd = 8.6 Functional
Antagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pigAntagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pig
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00180a007
66366 3126 60 None -27 13 Guinea pig 8.6 pKd = 8.6 Functional
Antagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pigAntagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pig
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00180a007
91536 3126 60 None -27 13 Guinea pig 8.6 pKd = 8.6 Functional
Antagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pigAntagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pig
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00180a007
CHEMBL27 3126 60 None -27 13 Guinea pig 8.6 pKd = 8.6 Functional
Antagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pigAntagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pig
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00180a007
CHEMBL452861 3126 60 None -27 13 Guinea pig 8.6 pKd = 8.6 Functional
Antagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pigAntagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pig
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00180a007
DB00571 3126 60 None -27 13 Guinea pig 8.6 pKd = 8.6 Functional
Antagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pigAntagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pig
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00180a007
2176 3065 66 None -1 6 Human 8.6 pKd = 8.6 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-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 8.6 pKd = 8.6 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-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 8.6 pKd = 8.6 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-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 8.6 pKd = 8.6 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-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 8.6 pKd = 8.6 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-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
165193 3126 60 None - 13 Rat 8.6 pKd = 8.6 Functional
Beta-1 adrenergic receptor-Antagonism in isolated rat heart ventricle. ( for R-enantiomer)Beta-1 adrenergic receptor-Antagonism in isolated rat heart ventricle. ( for R-enantiomer)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm970338c
2303 3126 60 None - 13 Rat 8.6 pKd = 8.6 Functional
Beta-1 adrenergic receptor-Antagonism in isolated rat heart ventricle. ( for R-enantiomer)Beta-1 adrenergic receptor-Antagonism in isolated rat heart ventricle. ( for R-enantiomer)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm970338c
4946 3126 60 None - 13 Rat 8.6 pKd = 8.6 Functional
Beta-1 adrenergic receptor-Antagonism in isolated rat heart ventricle. ( for R-enantiomer)Beta-1 adrenergic receptor-Antagonism in isolated rat heart ventricle. ( for R-enantiomer)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm970338c
564 3126 60 None - 13 Rat 8.6 pKd = 8.6 Functional
Beta-1 adrenergic receptor-Antagonism in isolated rat heart ventricle. ( for R-enantiomer)Beta-1 adrenergic receptor-Antagonism in isolated rat heart ventricle. ( for R-enantiomer)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm970338c
62882 3126 60 None - 13 Rat 8.6 pKd = 8.6 Functional
Beta-1 adrenergic receptor-Antagonism in isolated rat heart ventricle. ( for R-enantiomer)Beta-1 adrenergic receptor-Antagonism in isolated rat heart ventricle. ( for R-enantiomer)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm970338c
63 3126 60 None - 13 Rat 8.6 pKd = 8.6 Functional
Beta-1 adrenergic receptor-Antagonism in isolated rat heart ventricle. ( for R-enantiomer)Beta-1 adrenergic receptor-Antagonism in isolated rat heart ventricle. ( for R-enantiomer)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm970338c
66366 3126 60 None - 13 Rat 8.6 pKd = 8.6 Functional
Beta-1 adrenergic receptor-Antagonism in isolated rat heart ventricle. ( for R-enantiomer)Beta-1 adrenergic receptor-Antagonism in isolated rat heart ventricle. ( for R-enantiomer)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm970338c
91536 3126 60 None - 13 Rat 8.6 pKd = 8.6 Functional
Beta-1 adrenergic receptor-Antagonism in isolated rat heart ventricle. ( for R-enantiomer)Beta-1 adrenergic receptor-Antagonism in isolated rat heart ventricle. ( for R-enantiomer)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm970338c
CHEMBL27 3126 60 None - 13 Rat 8.6 pKd = 8.6 Functional
Beta-1 adrenergic receptor-Antagonism in isolated rat heart ventricle. ( for R-enantiomer)Beta-1 adrenergic receptor-Antagonism in isolated rat heart ventricle. ( for R-enantiomer)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm970338c
CHEMBL452861 3126 60 None - 13 Rat 8.6 pKd = 8.6 Functional
Beta-1 adrenergic receptor-Antagonism in isolated rat heart ventricle. ( for R-enantiomer)Beta-1 adrenergic receptor-Antagonism in isolated rat heart ventricle. ( for R-enantiomer)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm970338c
DB00571 3126 60 None - 13 Rat 8.6 pKd = 8.6 Functional
Beta-1 adrenergic receptor-Antagonism in isolated rat heart ventricle. ( for R-enantiomer)Beta-1 adrenergic receptor-Antagonism in isolated rat heart ventricle. ( for R-enantiomer)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm970338c
56597179 87827 0 None 2754 3 Human 8.6 pKd = 8.6 Functional
Antagonist activity at human beta1 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 beta1 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 8.6 pKd = 8.6 Functional
Antagonist activity at human beta1 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 beta1 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
2369 615 75 None - 2 Rat 8.5 pKd = 8.5 Functional
Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atriaAntagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria
ChEMBL 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C 10.1021/jm00389a008
356 615 75 None - 2 Rat 8.5 pKd = 8.5 Functional
Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atriaAntagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria
ChEMBL 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C 10.1021/jm00389a008
549 615 75 None - 2 Rat 8.5 pKd = 8.5 Functional
Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atriaAntagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria
ChEMBL 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C 10.1021/jm00389a008
CHEMBL423 615 75 None - 2 Rat 8.5 pKd = 8.5 Functional
Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atriaAntagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria
ChEMBL 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C 10.1021/jm00389a008
DB00195 615 75 None - 2 Rat 8.5 pKd = 8.5 Functional
Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atriaAntagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria
ChEMBL 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C 10.1021/jm00389a008
44264404 13298 0 None - 0 Rat 8.5 pKd = 8.5 Functional
Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atriaAntagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria
ChEMBL 319 11 2 4 2.5 OC(CNC1CC1)COc1ccc(CCOCC2CCC2)cc1 10.1021/jm00389a008
CHEMBL1192875 13298 0 None - 0 Rat 8.5 pKd = 8.5 Functional
Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atriaAntagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria
ChEMBL 319 11 2 4 2.5 OC(CNC1CC1)COc1ccc(CCOCC2CCC2)cc1 10.1021/jm00389a008
CHEMBL544190 13298 0 None - 0 Rat 8.5 pKd = 8.5 Functional
Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atriaAntagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria
ChEMBL 319 11 2 4 2.5 OC(CNC1CC1)COc1ccc(CCOCC2CCC2)cc1 10.1021/jm00389a008
2369 615 75 None - 2 Rat 8.5 pKd = 8.5 Functional
Cardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated rat atriaCardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated rat atria
ChEMBL 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C 10.1021/jm00389a008
356 615 75 None - 2 Rat 8.5 pKd = 8.5 Functional
Cardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated rat atriaCardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated rat atria
ChEMBL 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C 10.1021/jm00389a008
549 615 75 None - 2 Rat 8.5 pKd = 8.5 Functional
Cardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated rat atriaCardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated rat atria
ChEMBL 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C 10.1021/jm00389a008
CHEMBL423 615 75 None - 2 Rat 8.5 pKd = 8.5 Functional
Cardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated rat atriaCardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated rat atria
ChEMBL 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C 10.1021/jm00389a008
DB00195 615 75 None - 2 Rat 8.5 pKd = 8.5 Functional
Cardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated rat atriaCardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated rat atria
ChEMBL 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C 10.1021/jm00389a008
44287522 11105 0 None - 0 Guinea pig 4.7 pKd = 4.7 Functional
Antagonistic activity against beta-1 adrenergic receptor of isolated guinea pig atriaAntagonistic activity against beta-1 adrenergic receptor of isolated guinea pig atria
ChEMBL 244 10 2 4 2.3 CCCC(CCC)=NOCC(O)CNC(C)C 10.1021/jm00380a001
CHEMBL1178778 11105 0 None - 0 Guinea pig 4.7 pKd = 4.7 Functional
Antagonistic activity against beta-1 adrenergic receptor of isolated guinea pig atriaAntagonistic activity against beta-1 adrenergic receptor of isolated guinea pig atria
ChEMBL 244 10 2 4 2.3 CCCC(CCC)=NOCC(O)CNC(C)C 10.1021/jm00380a001
CHEMBL40783 11105 0 None - 0 Guinea pig 4.7 pKd = 4.7 Functional
Antagonistic activity against beta-1 adrenergic receptor of isolated guinea pig atriaAntagonistic activity against beta-1 adrenergic receptor of isolated guinea pig atria
ChEMBL 244 10 2 4 2.3 CCCC(CCC)=NOCC(O)CNC(C)C 10.1021/jm00380a001
54757027 65145 0 None - 0 Human 6.7 pKd = 6.7 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-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 6.7 pKd = 6.7 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-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
1786 2474 79 None - 6 Rat 7.6 pKd = 7.6 Functional
Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atriaAntagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm00389a008
4171 2474 79 None - 6 Rat 7.6 pKd = 7.6 Functional
Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atriaAntagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm00389a008
553 2474 79 None - 6 Rat 7.6 pKd = 7.6 Functional
Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atriaAntagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm00389a008
CHEMBL13 2474 79 None - 6 Rat 7.6 pKd = 7.6 Functional
Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atriaAntagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm00389a008
DB00264 2474 79 None - 6 Rat 7.6 pKd = 7.6 Functional
Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atriaAntagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm00389a008
1786 2474 79 None - 6 Rat 7.6 pKd = 7.6 Functional
Cardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated rat atriaCardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated rat atria
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm00389a008
4171 2474 79 None - 6 Rat 7.6 pKd = 7.6 Functional
Cardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated rat atriaCardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated rat atria
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm00389a008
553 2474 79 None - 6 Rat 7.6 pKd = 7.6 Functional
Cardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated rat atriaCardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated rat atria
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm00389a008
CHEMBL13 2474 79 None - 6 Rat 7.6 pKd = 7.6 Functional
Cardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated rat atriaCardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated rat atria
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm00389a008
DB00264 2474 79 None - 6 Rat 7.6 pKd = 7.6 Functional
Cardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated rat atriaCardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated rat atria
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm00389a008
54757026 65144 0 None - 0 Human 6.6 pKd = 6.6 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in CGP 12177-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in CGP 12177-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 6.6 pKd = 6.6 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in CGP 12177-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in CGP 12177-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
44287498 12282 0 None - 0 Guinea pig 4.6 pKd = 4.6 Functional
Antagonistic activity against beta-1 adrenergic receptor of isolated guinea pig atriaAntagonistic activity against beta-1 adrenergic receptor of isolated guinea pig atria
ChEMBL 214 6 2 4 1.3 CC(C)NCC(O)CON=C1CCCC1 10.1021/jm00380a001
CHEMBL1185760 12282 0 None - 0 Guinea pig 4.6 pKd = 4.6 Functional
Antagonistic activity against beta-1 adrenergic receptor of isolated guinea pig atriaAntagonistic activity against beta-1 adrenergic receptor of isolated guinea pig atria
ChEMBL 214 6 2 4 1.3 CC(C)NCC(O)CON=C1CCCC1 10.1021/jm00380a001
CHEMBL431713 12282 0 None - 0 Guinea pig 4.6 pKd = 4.6 Functional
Antagonistic activity against beta-1 adrenergic receptor of isolated guinea pig atriaAntagonistic activity against beta-1 adrenergic receptor of isolated guinea pig atria
ChEMBL 214 6 2 4 1.3 CC(C)NCC(O)CON=C1CCCC1 10.1021/jm00380a001
127940 203166 4 None - 0 Human 6.6 pKd = 6.6 Functional
The compound was evaluated for the antagonistic activity against alpha-1 adrenergic receptor.The compound was evaluated for the antagonistic activity against alpha-1 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 Human 6.6 pKd = 6.6 Functional
The compound was evaluated for the antagonistic activity against alpha-1 adrenergic receptor.The compound was evaluated for the antagonistic activity against alpha-1 adrenergic receptor.
ChEMBL 351 8 4 3 2.9 CC(CCc1ccccc1)NCC(O)c1cc(C(N)=O)c2[nH]ccc2c1 10.1021/jm00156a019
56598833 87825 0 None 436 3 Human 7.6 pKd = 7.6 Functional
Antagonist activity at human beta1 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 beta1 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 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 7.6 pKd = 7.6 Functional
Antagonist activity at human beta1 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 beta1 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 433 14 5 7 2.0 CCOCCOc1ccc(OCC(O)CNCCNC(=O)Nc2ccc(O)cc2)cc1 10.1021/jm400348g
168613 59987 21 None - 0 Guinea pig 7.6 pKd = 7.6 Functional
Compound was tested for its Beta-1 adrenergic receptor antagonistic activity on guinea pig atriaCompound was tested for its Beta-1 adrenergic receptor antagonistic activity on guinea pig atria
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 7.6 pKd = 7.6 Functional
Compound was tested for its Beta-1 adrenergic receptor antagonistic activity on guinea pig atriaCompound was tested for its Beta-1 adrenergic receptor antagonistic activity on guinea pig atria
ChEMBL 316 6 2 8 0.5 CC(C)(C)NC[C@@H](O)COc1nsnc1N1CCOCC1 10.1021/jm00350a009
12733306 59750 0 None - 0 Guinea pig 6.6 pKd = 6.6 Functional
Antagonist activity of compound against Beta-1 adrenergic receptor in isolated guinea pig left atriaAntagonist activity of compound against Beta-1 adrenergic receptor in isolated guinea pig left atria
ChEMBL 368 5 1 6 2.5 COc1ccccc1N1CCN(CC(O)C2=COc3ccccc3O2)CC1 10.1021/jm00140a015
CHEMBL173882 59750 0 None - 0 Guinea pig 6.6 pKd = 6.6 Functional
Antagonist activity of compound against Beta-1 adrenergic receptor in isolated guinea pig left atriaAntagonist activity of compound against Beta-1 adrenergic receptor in isolated guinea pig left atria
ChEMBL 368 5 1 6 2.5 COc1ccccc1N1CCN(CC(O)C2=COc3ccccc3O2)CC1 10.1021/jm00140a015
165193 3126 60 None - 13 Rat 5.6 pKd = 5.6 Functional
Beta-1 adrenergic receptor-Antagonism in isolated rat heart ventricle. ( for S-enantiomer)Beta-1 adrenergic receptor-Antagonism in isolated rat heart ventricle. ( for S-enantiomer)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm970338c
2303 3126 60 None - 13 Rat 5.6 pKd = 5.6 Functional
Beta-1 adrenergic receptor-Antagonism in isolated rat heart ventricle. ( for S-enantiomer)Beta-1 adrenergic receptor-Antagonism in isolated rat heart ventricle. ( for S-enantiomer)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm970338c
4946 3126 60 None - 13 Rat 5.6 pKd = 5.6 Functional
Beta-1 adrenergic receptor-Antagonism in isolated rat heart ventricle. ( for S-enantiomer)Beta-1 adrenergic receptor-Antagonism in isolated rat heart ventricle. ( for S-enantiomer)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm970338c
564 3126 60 None - 13 Rat 5.6 pKd = 5.6 Functional
Beta-1 adrenergic receptor-Antagonism in isolated rat heart ventricle. ( for S-enantiomer)Beta-1 adrenergic receptor-Antagonism in isolated rat heart ventricle. ( for S-enantiomer)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm970338c
62882 3126 60 None - 13 Rat 5.6 pKd = 5.6 Functional
Beta-1 adrenergic receptor-Antagonism in isolated rat heart ventricle. ( for S-enantiomer)Beta-1 adrenergic receptor-Antagonism in isolated rat heart ventricle. ( for S-enantiomer)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm970338c
63 3126 60 None - 13 Rat 5.6 pKd = 5.6 Functional
Beta-1 adrenergic receptor-Antagonism in isolated rat heart ventricle. ( for S-enantiomer)Beta-1 adrenergic receptor-Antagonism in isolated rat heart ventricle. ( for S-enantiomer)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm970338c
66366 3126 60 None - 13 Rat 5.6 pKd = 5.6 Functional
Beta-1 adrenergic receptor-Antagonism in isolated rat heart ventricle. ( for S-enantiomer)Beta-1 adrenergic receptor-Antagonism in isolated rat heart ventricle. ( for S-enantiomer)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm970338c
91536 3126 60 None - 13 Rat 5.6 pKd = 5.6 Functional
Beta-1 adrenergic receptor-Antagonism in isolated rat heart ventricle. ( for S-enantiomer)Beta-1 adrenergic receptor-Antagonism in isolated rat heart ventricle. ( for S-enantiomer)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm970338c
CHEMBL27 3126 60 None - 13 Rat 5.6 pKd = 5.6 Functional
Beta-1 adrenergic receptor-Antagonism in isolated rat heart ventricle. ( for S-enantiomer)Beta-1 adrenergic receptor-Antagonism in isolated rat heart ventricle. ( for S-enantiomer)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm970338c
CHEMBL452861 3126 60 None - 13 Rat 5.6 pKd = 5.6 Functional
Beta-1 adrenergic receptor-Antagonism in isolated rat heart ventricle. ( for S-enantiomer)Beta-1 adrenergic receptor-Antagonism in isolated rat heart ventricle. ( for S-enantiomer)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm970338c
DB00571 3126 60 None - 13 Rat 5.6 pKd = 5.6 Functional
Beta-1 adrenergic receptor-Antagonism in isolated rat heart ventricle. ( for S-enantiomer)Beta-1 adrenergic receptor-Antagonism in isolated rat heart ventricle. ( for S-enantiomer)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm970338c
10042467 1393 1 None - 2 Guinea pig 4.6 pKd = 4.6 Functional
Compound was evaluated for its antagonist affinity towards Beta-1 adrenergic receptor of guinea pigCompound was evaluated for its antagonist affinity towards Beta-1 adrenergic receptor of guinea pig
ChEMBL 333 8 1 2 4.3 CN(CCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1)C 10.1021/jm991056a
1203 1393 1 None - 2 Guinea pig 4.6 pKd = 4.6 Functional
Compound was evaluated for its antagonist affinity towards Beta-1 adrenergic receptor of guinea pigCompound was evaluated for its antagonist affinity towards Beta-1 adrenergic receptor of guinea pig
ChEMBL 333 8 1 2 4.3 CN(CCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1)C 10.1021/jm991056a
CHEMBL11553 1393 1 None - 2 Guinea pig 4.6 pKd = 4.6 Functional
Compound was evaluated for its antagonist affinity towards Beta-1 adrenergic receptor of guinea pigCompound was evaluated for its antagonist affinity towards Beta-1 adrenergic receptor of guinea pig
ChEMBL 333 8 1 2 4.3 CN(CCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1)C 10.1021/jm991056a
44371642 48938 0 None - 0 Guinea pig 4.6 pKd = 4.6 Functional
Antagonist activity against beta-1 adrenergic receptor in isolated guinea pig atriaAntagonist activity against beta-1 adrenergic receptor in isolated guinea pig atria
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 4.6 pKd = 4.6 Functional
Antagonist activity against beta-1 adrenergic receptor in isolated guinea pig atriaAntagonist activity against beta-1 adrenergic receptor in isolated guinea pig atria
ChEMBL 203 6 2 4 0.5 CC(C)NCC(O)COC(=O)C(C)C 10.1021/jm00387a006
12606702 11893 0 None - 0 Guinea pig 6.6 pKd = 6.6 Functional
Antagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pigAntagonism of the isoprenaline-induced positive chronotropic effect on the atria 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 6.6 pKd = 6.6 Functional
Antagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pigAntagonism of the isoprenaline-induced positive chronotropic effect on the atria 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 6.6 pKd = 6.6 Functional
Antagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pigAntagonism of the isoprenaline-induced positive chronotropic effect on the atria 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 6.6 pKd = 6.6 Functional
Antagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pigAntagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pig
ChEMBL 242 5 2 4 2.1 CC(C)(C)NCC(O)CON=C1CCCCC1 10.1021/jm00180a007
12606704 14186 0 None - 0 Guinea pig 6.6 pKd = 6.6 Functional
Antagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pigAntagonism of the isoprenaline-induced positive chronotropic effect on the atria 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 6.6 pKd = 6.6 Functional
Antagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pigAntagonism of the isoprenaline-induced positive chronotropic effect on the atria 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 6.6 pKd = 6.6 Functional
Antagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pigAntagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pig
ChEMBL 290 7 2 4 2.8 CC(/C=C/c1ccccc1)=N\OCC(O)CNC(C)(C)C 10.1021/jm00180a007
44371312 48978 2 None - 0 Guinea pig 4.6 pKd = 4.6 Functional
Antagonist activity against beta-1 adrenergic receptor in isolated guinea pig atriaAntagonist activity against beta-1 adrenergic receptor in isolated guinea pig atria
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-1 adrenergic receptor in isolated guinea pig atriaAntagonist activity against beta-1 adrenergic receptor in isolated guinea pig atria
ChEMBL 203 5 2 4 0.7 CCC(=O)OCC(O)CNC(C)(C)C 10.1021/jm00387a006
44264509 201984 0 None - 0 Rat 5.5 pKd = 5.5 Functional
Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atriaAntagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria
ChEMBL 429 14 2 4 4.5 CC(CCc1ccc(F)cc1)NCC(O)COc1ccc(CCOCC2CCC2)cc1 10.1021/jm00389a008
CHEMBL6749 201984 0 None - 0 Rat 5.5 pKd = 5.5 Functional
Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atriaAntagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria
ChEMBL 429 14 2 4 4.5 CC(CCc1ccc(F)cc1)NCC(O)COc1ccc(CCOCC2CCC2)cc1 10.1021/jm00389a008
3047492 202259 8 None - 0 Guinea pig 5.5 pKd = 5.5 Functional
Cardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated guinea pig tracheaCardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated guinea pig trachea
ChEMBL 293 10 2 4 2.4 CC(C)NCC(O)COc1ccc(COCC2CC2)cc1 10.1021/jm00389a008
CHEMBL6939 202259 8 None - 0 Guinea pig 5.5 pKd = 5.5 Functional
Cardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated guinea pig tracheaCardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated guinea pig trachea
ChEMBL 293 10 2 4 2.4 CC(C)NCC(O)COc1ccc(COCC2CC2)cc1 10.1021/jm00389a008
165193 3126 60 None -27 13 Guinea pig 8.5 pKd = 8.5 Functional
Compound was evaluated for competitive antagonism of beta-1 adrenergic receptor in guinea pig atria measured as pA2 (-log KB)Compound was evaluated for competitive antagonism of beta-1 adrenergic receptor in guinea pig atria measured as pA2 (-log KB)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00373a008
2303 3126 60 None -27 13 Guinea pig 8.5 pKd = 8.5 Functional
Compound was evaluated for competitive antagonism of beta-1 adrenergic receptor in guinea pig atria measured as pA2 (-log KB)Compound was evaluated for competitive antagonism of beta-1 adrenergic receptor in guinea pig atria measured as pA2 (-log KB)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00373a008
4946 3126 60 None -27 13 Guinea pig 8.5 pKd = 8.5 Functional
Compound was evaluated for competitive antagonism of beta-1 adrenergic receptor in guinea pig atria measured as pA2 (-log KB)Compound was evaluated for competitive antagonism of beta-1 adrenergic receptor in guinea pig atria measured as pA2 (-log KB)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00373a008
564 3126 60 None -27 13 Guinea pig 8.5 pKd = 8.5 Functional
Compound was evaluated for competitive antagonism of beta-1 adrenergic receptor in guinea pig atria measured as pA2 (-log KB)Compound was evaluated for competitive antagonism of beta-1 adrenergic receptor in guinea pig atria measured as pA2 (-log KB)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00373a008
62882 3126 60 None -27 13 Guinea pig 8.5 pKd = 8.5 Functional
Compound was evaluated for competitive antagonism of beta-1 adrenergic receptor in guinea pig atria measured as pA2 (-log KB)Compound was evaluated for competitive antagonism of beta-1 adrenergic receptor in guinea pig atria measured as pA2 (-log KB)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00373a008
63 3126 60 None -27 13 Guinea pig 8.5 pKd = 8.5 Functional
Compound was evaluated for competitive antagonism of beta-1 adrenergic receptor in guinea pig atria measured as pA2 (-log KB)Compound was evaluated for competitive antagonism of beta-1 adrenergic receptor in guinea pig atria measured as pA2 (-log KB)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00373a008
66366 3126 60 None -27 13 Guinea pig 8.5 pKd = 8.5 Functional
Compound was evaluated for competitive antagonism of beta-1 adrenergic receptor in guinea pig atria measured as pA2 (-log KB)Compound was evaluated for competitive antagonism of beta-1 adrenergic receptor in guinea pig atria measured as pA2 (-log KB)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00373a008
91536 3126 60 None -27 13 Guinea pig 8.5 pKd = 8.5 Functional
Compound was evaluated for competitive antagonism of beta-1 adrenergic receptor in guinea pig atria measured as pA2 (-log KB)Compound was evaluated for competitive antagonism of beta-1 adrenergic receptor in guinea pig atria measured as pA2 (-log KB)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00373a008
CHEMBL27 3126 60 None -27 13 Guinea pig 8.5 pKd = 8.5 Functional
Compound was evaluated for competitive antagonism of beta-1 adrenergic receptor in guinea pig atria measured as pA2 (-log KB)Compound was evaluated for competitive antagonism of beta-1 adrenergic receptor in guinea pig atria measured as pA2 (-log KB)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00373a008
CHEMBL452861 3126 60 None -27 13 Guinea pig 8.5 pKd = 8.5 Functional
Compound was evaluated for competitive antagonism of beta-1 adrenergic receptor in guinea pig atria measured as pA2 (-log KB)Compound was evaluated for competitive antagonism of beta-1 adrenergic receptor in guinea pig atria measured as pA2 (-log KB)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00373a008
DB00571 3126 60 None -27 13 Guinea pig 8.5 pKd = 8.5 Functional
Compound was evaluated for competitive antagonism of beta-1 adrenergic receptor in guinea pig atria measured as pA2 (-log KB)Compound was evaluated for competitive antagonism of beta-1 adrenergic receptor in guinea pig atria measured as pA2 (-log KB)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00373a008
54669764 65146 0 None - 0 Human 8.5 pKd = 8.5 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-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 8.5 pKd = 8.5 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-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
56598967 87819 0 None 2238 3 Human 8.5 pKd = 8.5 Functional
Antagonist activity at human beta1 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 beta1 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 8.5 pKd = 8.5 Functional
Antagonist activity at human beta1 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 beta1 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
54757026 65144 0 None - 0 Human 7.5 pKd = 7.5 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-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 7.5 pKd = 7.5 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-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
54758320 65172 0 None - 0 Human 6.5 pKd = 6.5 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-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 6.5 pKd = 6.5 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-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
12606706 92788 0 None - 0 Guinea pig 6.5 pKd = 6.5 Functional
Antagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pigAntagonism of the isoprenaline-induced positive chronotropic effect on the atria 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 6.5 pKd = 6.5 Functional
Antagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pigAntagonism of the isoprenaline-induced positive chronotropic effect on the atria 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 6.5 pKd = 6.5 Functional
Antagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pigAntagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pig
ChEMBL 202 5 2 4 1.1 CC(C)=NOCC(O)CNC(C)(C)C 10.1021/jm00180a007
1531 2226 64 None - 7 Guinea pig 7.5 pKd = 7.5 Functional
The compound was evaluated for the antagonistic activity against beta-1 adrenergic receptor.The compound was evaluated for the antagonistic activity against beta-1 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 7.5 pKd = 7.5 Functional
The compound was evaluated for the antagonistic activity against beta-1 adrenergic receptor.The compound was evaluated for the antagonistic activity against beta-1 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 7.5 pKd = 7.5 Functional
The compound was evaluated for the antagonistic activity against beta-1 adrenergic receptor.The compound was evaluated for the antagonistic activity against beta-1 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 7.5 pKd = 7.5 Functional
The compound was evaluated for the antagonistic activity against beta-1 adrenergic receptor.The compound was evaluated for the antagonistic activity against beta-1 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 7.5 pKd = 7.5 Functional
The compound was evaluated for the antagonistic activity against beta-1 adrenergic receptor.The compound was evaluated for the antagonistic activity against beta-1 adrenergic receptor.
ChEMBL 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O 10.1021/jm00156a019
121848 130175 4 None - 2 Guinea pig 7.5 pKd = 7.5 Functional
Compound was tested for its Beta-1 adrenergic receptor antagonistic activity on guinea pig atriaCompound was tested for its Beta-1 adrenergic receptor antagonistic activity on guinea pig atria
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 7.5 pKd = 7.5 Functional
Compound was tested for its Beta-1 adrenergic receptor antagonistic activity on guinea pig atriaCompound was tested for its Beta-1 adrenergic receptor antagonistic activity on guinea pig atria
ChEMBL 324 5 2 4 3.2 CC(C)(C)NCC(O)CON=C1c2ccccc2-c2ccccc21 10.1021/jm00350a009
44264298 13248 0 None - 0 Rat 6.5 pKd = 6.5 Functional
Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atriaAntagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria
ChEMBL 346 12 2 5 2.7 CC(CC#N)NCC(O)COc1ccc(CCOCC2CCC2)cc1 10.1021/jm00389a008
CHEMBL1192477 13248 0 None - 0 Rat 6.5 pKd = 6.5 Functional
Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atriaAntagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria
ChEMBL 346 12 2 5 2.7 CC(CC#N)NCC(O)COc1ccc(CCOCC2CCC2)cc1 10.1021/jm00389a008
CHEMBL543717 13248 0 None - 0 Rat 6.5 pKd = 6.5 Functional
Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atriaAntagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria
ChEMBL 346 12 2 5 2.7 CC(CC#N)NCC(O)COc1ccc(CCOCC2CCC2)cc1 10.1021/jm00389a008
12778440 59841 0 None - 0 Guinea pig 7.5 pKd = 7.5 Functional
Compound was tested for its Beta-1 adrenergic receptor antagonistic activity on guinea pig atriaCompound was tested for its Beta-1 adrenergic receptor antagonistic activity on guinea pig atria
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 7.5 pKd = 7.5 Functional
Compound was tested for its Beta-1 adrenergic receptor antagonistic activity on guinea pig atriaCompound was tested for its Beta-1 adrenergic receptor antagonistic activity on guinea pig atria
ChEMBL 338 7 2 4 3.6 CCC(C)(C)NCC(O)CON=C1c2ccccc2-c2ccccc21 10.1021/jm00350a009
54756929 65143 0 None - 0 Human 6.5 pKd = 6.5 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in CGP 12177-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in CGP 12177-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 6.5 pKd = 6.5 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in CGP 12177-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in CGP 12177-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
44263933 13531 0 None - 0 Rat 7.4 pKd = 7.4 Functional
Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atriaAntagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria
ChEMBL 307 10 2 4 2.7 CC(C)NCC(O)COc1ccc(COCC2CCC2)cc1 10.1021/jm00389a008
CHEMBL1194583 13531 0 None - 0 Rat 7.4 pKd = 7.4 Functional
Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atriaAntagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria
ChEMBL 307 10 2 4 2.7 CC(C)NCC(O)COc1ccc(COCC2CCC2)cc1 10.1021/jm00389a008
CHEMBL552898 13531 0 None - 0 Rat 7.4 pKd = 7.4 Functional
Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atriaAntagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria
ChEMBL 307 10 2 4 2.7 CC(C)NCC(O)COc1ccc(COCC2CCC2)cc1 10.1021/jm00389a008
2447484 102282 2 None - 2 Guinea pig 7.4 pKd = 7.4 Functional
Compound was tested for its Beta-1 adrenergic receptor antagonistic activity on guinea pig atriaCompound was tested for its Beta-1 adrenergic receptor antagonistic activity on guinea pig atria
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 7.4 pKd = 7.4 Functional
Compound was tested for its Beta-1 adrenergic receptor antagonistic activity on guinea pig atriaCompound was tested for its Beta-1 adrenergic receptor antagonistic activity on guinea pig atria
ChEMBL 324 5 2 4 3.2 CC(C)(C)NC[C@H](O)CON=C1c2ccccc2-c2ccccc21 10.1021/jm00350a009
54758415 65173 0 None - 0 Human 7.4 pKd = 7.4 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-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 7.4 pKd = 7.4 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-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
12606709 14213 0 None - 0 Guinea pig 5.4 pKd = 5.4 Functional
Antagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pigAntagonism of the isoprenaline-induced positive chronotropic effect on the atria 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 5.4 pKd = 5.4 Functional
Antagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pigAntagonism of the isoprenaline-induced positive chronotropic effect on the atria 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 5.4 pKd = 5.4 Functional
Antagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pigAntagonism of the isoprenaline-induced positive chronotropic effect on the atria 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
3047500 13151 1 None - 0 Guinea pig 5.4 pKd = 5.4 Functional
Cardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated guinea pig tracheaCardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated guinea pig trachea
ChEMBL 349 11 2 4 3.6 CC(C)NCC(O)COc1ccc(CCOCC2CCCCC2)cc1 10.1021/jm00389a008
CHEMBL1191645 13151 1 None - 0 Guinea pig 5.4 pKd = 5.4 Functional
Cardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated guinea pig tracheaCardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated guinea pig trachea
ChEMBL 349 11 2 4 3.6 CC(C)NCC(O)COc1ccc(CCOCC2CCCCC2)cc1 10.1021/jm00389a008
CHEMBL542776 13151 1 None - 0 Guinea pig 5.4 pKd = 5.4 Functional
Cardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated guinea pig tracheaCardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated guinea pig trachea
ChEMBL 349 11 2 4 3.6 CC(C)NCC(O)COc1ccc(CCOCC2CCCCC2)cc1 10.1021/jm00389a008
44371514 11581 0 None - 0 Guinea pig 6.4 pKd = 6.4 Functional
Antagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pigAntagonism of the isoprenaline-induced positive chronotropic effect on the atria 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 6.4 pKd = 6.4 Functional
Antagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pigAntagonism of the isoprenaline-induced positive chronotropic effect on the atria 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 6.4 pKd = 6.4 Functional
Antagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pigAntagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pig
ChEMBL 216 8 2 4 1.5 CCC/C(C)=N\OCC(O)CNC(C)C 10.1021/jm00180a007
127940 203166 4 None - 0 Guinea pig 7.4 pKd = 7.4 Functional
The compound was evaluated for the antagonistic activity against beta-1 adrenergic receptorThe compound was evaluated for the antagonistic activity against beta-1 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 7.4 pKd = 7.4 Functional
The compound was evaluated for the antagonistic activity against beta-1 adrenergic receptorThe compound was evaluated for the antagonistic activity against beta-1 adrenergic receptor
ChEMBL 351 8 4 3 2.9 CC(CCc1ccccc1)NCC(O)c1cc(C(N)=O)c2[nH]ccc2c1 10.1021/jm00156a019
2369 615 75 None - 2 Guinea pig 5.4 pKd = 5.4 Functional
Cardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated guinea pig tracheaCardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated guinea pig trachea
ChEMBL 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C 10.1021/jm00389a008
356 615 75 None - 2 Guinea pig 5.4 pKd = 5.4 Functional
Cardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated guinea pig tracheaCardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated guinea pig trachea
ChEMBL 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C 10.1021/jm00389a008
549 615 75 None - 2 Guinea pig 5.4 pKd = 5.4 Functional
Cardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated guinea pig tracheaCardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated guinea pig trachea
ChEMBL 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C 10.1021/jm00389a008
CHEMBL423 615 75 None - 2 Guinea pig 5.4 pKd = 5.4 Functional
Cardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated guinea pig tracheaCardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated guinea pig trachea
ChEMBL 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C 10.1021/jm00389a008
DB00195 615 75 None - 2 Guinea pig 5.4 pKd = 5.4 Functional
Cardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated guinea pig tracheaCardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated guinea pig trachea
ChEMBL 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C 10.1021/jm00389a008
137 367 47 None -2 4 Human 8.4 pKd = 8.4 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-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 -2 4 Human 8.4 pKd = 8.4 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-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 -2 4 Human 8.4 pKd = 8.4 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-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 -2 4 Human 8.4 pKd = 8.4 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-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 -2 4 Human 8.4 pKd = 8.4 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-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 -2 4 Human 8.4 pKd = 8.4 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-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
165193 3126 60 None - 13 Rat 8.4 pKd = 8.4 Functional
Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atriaAntagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00389a008
2303 3126 60 None - 13 Rat 8.4 pKd = 8.4 Functional
Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atriaAntagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00389a008
4946 3126 60 None - 13 Rat 8.4 pKd = 8.4 Functional
Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atriaAntagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00389a008
564 3126 60 None - 13 Rat 8.4 pKd = 8.4 Functional
Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atriaAntagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00389a008
62882 3126 60 None - 13 Rat 8.4 pKd = 8.4 Functional
Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atriaAntagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00389a008
63 3126 60 None - 13 Rat 8.4 pKd = 8.4 Functional
Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atriaAntagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00389a008
66366 3126 60 None - 13 Rat 8.4 pKd = 8.4 Functional
Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atriaAntagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00389a008
91536 3126 60 None - 13 Rat 8.4 pKd = 8.4 Functional
Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atriaAntagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00389a008
CHEMBL27 3126 60 None - 13 Rat 8.4 pKd = 8.4 Functional
Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atriaAntagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00389a008
CHEMBL452861 3126 60 None - 13 Rat 8.4 pKd = 8.4 Functional
Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atriaAntagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00389a008
DB00571 3126 60 None - 13 Rat 8.4 pKd = 8.4 Functional
Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atriaAntagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00389a008
165193 3126 60 None - 13 Rat 8.4 pKd = 8.4 Functional
Cardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated rat atriaCardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated rat atria
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00389a008
2303 3126 60 None - 13 Rat 8.4 pKd = 8.4 Functional
Cardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated rat atriaCardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated rat atria
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00389a008
4946 3126 60 None - 13 Rat 8.4 pKd = 8.4 Functional
Cardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated rat atriaCardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated rat atria
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00389a008
564 3126 60 None - 13 Rat 8.4 pKd = 8.4 Functional
Cardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated rat atriaCardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated rat atria
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00389a008
62882 3126 60 None - 13 Rat 8.4 pKd = 8.4 Functional
Cardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated rat atriaCardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated rat atria
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00389a008
63 3126 60 None - 13 Rat 8.4 pKd = 8.4 Functional
Cardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated rat atriaCardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated rat atria
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00389a008
66366 3126 60 None - 13 Rat 8.4 pKd = 8.4 Functional
Cardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated rat atriaCardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated rat atria
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00389a008
91536 3126 60 None - 13 Rat 8.4 pKd = 8.4 Functional
Cardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated rat atriaCardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated rat atria
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00389a008
CHEMBL27 3126 60 None - 13 Rat 8.4 pKd = 8.4 Functional
Cardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated rat atriaCardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated rat atria
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00389a008
CHEMBL452861 3126 60 None - 13 Rat 8.4 pKd = 8.4 Functional
Cardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated rat atriaCardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated rat atria
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00389a008
DB00571 3126 60 None - 13 Rat 8.4 pKd = 8.4 Functional
Cardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated rat atriaCardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated rat atria
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00389a008
54757232 65170 0 None - 0 Human 7.4 pKd = 7.4 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in CGP 12177-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in CGP 12177-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 7.4 pKd = 7.4 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in CGP 12177-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in CGP 12177-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 7.4 pKd = 7.4 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-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 7.4 pKd = 7.4 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-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
44264188 202203 0 None - 0 Rat 7.4 pKd = 7.4 Functional
Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atriaAntagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria
ChEMBL 325 10 2 4 2.1 CC(C)NCC(O)COc1ccc(C[S+]([O-])CC2CC2)cc1 10.1021/jm00389a008
CHEMBL6902 202203 0 None - 0 Rat 7.4 pKd = 7.4 Functional
Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atriaAntagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria
ChEMBL 325 10 2 4 2.1 CC(C)NCC(O)COc1ccc(C[S+]([O-])CC2CC2)cc1 10.1021/jm00389a008
54757229 65169 0 None - 0 Human 7.4 pKd = 7.4 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-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 7.4 pKd = 7.4 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-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
12606687 12100 0 None - 0 Guinea pig 5.4 pKd = 5.4 Functional
Antagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pigAntagonism of the isoprenaline-induced positive chronotropic effect on the atria 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 5.4 pKd = 5.4 Functional
Antagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pigAntagonism of the isoprenaline-induced positive chronotropic effect on the atria 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 5.4 pKd = 5.4 Functional
Antagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pigAntagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pig
ChEMBL 175 6 2 3 0.8 CC(C)NCC(O)COC(C)C 10.1021/jm00180a007
134495 736 18 None - 1 Guinea pig 4.4 pKd = 4.4 Functional
Antagonist activity against beta-1 adrenergic receptor in isolated guinea pig atriaAntagonist activity against beta-1 adrenergic receptor in isolated guinea pig atria
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 4.4 pKd = 4.4 Functional
Antagonist activity against beta-1 adrenergic receptor in isolated guinea pig atriaAntagonist activity against beta-1 adrenergic receptor in isolated guinea pig atria
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 4.4 pKd = 4.4 Functional
Antagonist activity against beta-1 adrenergic receptor in isolated guinea pig atriaAntagonist activity against beta-1 adrenergic receptor in isolated guinea pig atria
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 4.4 pKd = 4.4 Functional
Antagonist activity against beta-1 adrenergic receptor in isolated guinea pig atriaAntagonist activity against beta-1 adrenergic receptor in isolated guinea pig atria
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 4.4 pKd = 4.4 Functional
Antagonistic activity against beta-1 adrenergic receptor of isolated guinea pig atriaAntagonistic activity against beta-1 adrenergic receptor of isolated guinea pig atria
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 4.4 pKd = 4.4 Functional
Antagonistic activity against beta-1 adrenergic receptor of isolated guinea pig atriaAntagonistic activity against beta-1 adrenergic receptor of isolated guinea pig atria
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 4.4 pKd = 4.4 Functional
Antagonistic activity against beta-1 adrenergic receptor of isolated guinea pig atriaAntagonistic activity against beta-1 adrenergic receptor of isolated guinea pig atria
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 4.4 pKd = 4.4 Functional
Antagonistic activity against beta-1 adrenergic receptor of isolated guinea pig atriaAntagonistic activity against beta-1 adrenergic receptor of isolated guinea pig atria
ChEMBL 267 5 2 4 2.5 COc1ccc(cc1C(C(NC(C)(C)C)C)O)OC 10.1021/jm00380a001
44371383 49332 0 None - 0 Guinea pig 6.3 pKd = 6.3 Functional
Antagonist activity against beta-1 adrenergic receptor in isolated guinea pig atriaAntagonist activity against beta-1 adrenergic receptor in isolated guinea pig atria
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 6.3 pKd = 6.3 Functional
Antagonist activity against beta-1 adrenergic receptor in isolated guinea pig atriaAntagonist activity against beta-1 adrenergic receptor in isolated guinea pig atria
ChEMBL 257 5 2 5 1.7 CC(C)(C)NCC(O)COC(=O)c1cccs1 10.1021/jm00387a006
10447834 1894 4 None - 3 Guinea pig 4.3 pKd = 4.3 Functional
Compound was evaluated for its antagonist affinity towards Beta-1 adrenergic receptor of guinea pigCompound was evaluated for its antagonist affinity towards Beta-1 adrenergic receptor of guinea pig
ChEMBL 305 7 2 2 3.7 NCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm991056a
4026 1894 4 None - 3 Guinea pig 4.3 pKd = 4.3 Functional
Compound was evaluated for its antagonist affinity towards Beta-1 adrenergic receptor of guinea pigCompound was evaluated for its antagonist affinity towards Beta-1 adrenergic receptor of guinea pig
ChEMBL 305 7 2 2 3.7 NCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm991056a
CHEMBL275507 1894 4 None - 3 Guinea pig 4.3 pKd = 4.3 Functional
Compound was evaluated for its antagonist affinity towards Beta-1 adrenergic receptor of guinea pigCompound was evaluated for its antagonist affinity towards Beta-1 adrenergic receptor of guinea pig
ChEMBL 305 7 2 2 3.7 NCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm991056a
54757129 65148 0 None - 0 Human 7.3 pKd = 7.3 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-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 7.3 pKd = 7.3 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-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
44287469 11877 0 None - 0 Guinea pig 5.3 pKd = 5.3 Functional
Antagonistic activity against beta-1 adrenergic receptor of isolated guinea pig atriaAntagonistic activity against beta-1 adrenergic receptor of isolated guinea pig atria
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 5.3 pKd = 5.3 Functional
Antagonistic activity against beta-1 adrenergic receptor of isolated guinea pig atriaAntagonistic activity against beta-1 adrenergic receptor of isolated guinea pig atria
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 5.3 pKd = 5.3 Functional
Antagonistic activity against beta-1 adrenergic receptor of isolated guinea pig atriaAntagonistic activity against beta-1 adrenergic receptor of isolated guinea pig atria
ChEMBL 258 9 2 4 2.7 CCCC(CCC)=NOCC(O)CNC(C)(C)C 10.1021/jm00380a001
44288489 168326 0 None - 0 Rat 7.3 pKd = 7.3 Functional
Beta-1 adrenergic receptor-Antagonism in isolated rat heart ventricle. ( for S-enantiomer)Beta-1 adrenergic receptor-Antagonism in isolated rat heart ventricle. ( for S-enantiomer)
ChEMBL 314 8 3 5 2.5 OC(CNc1nc2ccccc2[nH]1)CON=C(C1CC1)C1CC1 10.1021/jm970338c
CHEMBL43850 168326 0 None - 0 Rat 7.3 pKd = 7.3 Functional
Beta-1 adrenergic receptor-Antagonism in isolated rat heart ventricle. ( for S-enantiomer)Beta-1 adrenergic receptor-Antagonism in isolated rat heart ventricle. ( for S-enantiomer)
ChEMBL 314 8 3 5 2.5 OC(CNc1nc2ccccc2[nH]1)CON=C(C1CC1)C1CC1 10.1021/jm970338c
12606684 95615 3 None - 0 Guinea pig 6.3 pKd = 6.3 Functional
Antagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pigAntagonism of the isoprenaline-induced positive chronotropic effect on the atria 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 6.3 pKd = 6.3 Functional
Antagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pigAntagonism of the isoprenaline-induced positive chronotropic effect on the atria 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 6.3 pKd = 6.3 Functional
Antagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pigAntagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pig
ChEMBL 203 6 2 3 1.4 CC(C)COCC(O)CNC(C)(C)C 10.1021/jm00180a007
4752 2269 29 None - 0 Rat 8.3 pKd = 8.3 Functional
Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atriaAntagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria
ChEMBL 307 11 2 4 2.4 O[C@H](COc1ccc(cc1)CCOCC1CC1)CNC(C)C 10.1021/jm00389a008
60657 2269 29 None - 0 Rat 8.3 pKd = 8.3 Functional
Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atriaAntagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria
ChEMBL 307 11 2 4 2.4 O[C@H](COc1ccc(cc1)CCOCC1CC1)CNC(C)C 10.1021/jm00389a008
8035 2269 29 None - 0 Rat 8.3 pKd = 8.3 Functional
Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atriaAntagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria
ChEMBL 307 11 2 4 2.4 O[C@H](COc1ccc(cc1)CCOCC1CC1)CNC(C)C 10.1021/jm00389a008
CHEMBL1201274 2269 29 None - 0 Rat 8.3 pKd = 8.3 Functional
Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atriaAntagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria
ChEMBL 307 11 2 4 2.4 O[C@H](COc1ccc(cc1)CCOCC1CC1)CNC(C)C 10.1021/jm00389a008
DB09351 2269 29 None - 0 Rat 8.3 pKd = 8.3 Functional
Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atriaAntagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria
ChEMBL 307 11 2 4 2.4 O[C@H](COc1ccc(cc1)CCOCC1CC1)CNC(C)C 10.1021/jm00389a008
44371512 11551 0 None - 0 Guinea pig 8.3 pKd = 8.3 Functional
Antagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pigAntagonism of the isoprenaline-induced positive chronotropic effect on the atria 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 8.3 pKd = 8.3 Functional
Antagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pigAntagonism of the isoprenaline-induced positive chronotropic effect on the atria 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 8.3 pKd = 8.3 Functional
Antagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pigAntagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pig
ChEMBL 292 8 2 4 2.8 C/C(CCc1ccccc1)=N/OCC(O)CNC(C)(C)C 10.1021/jm00180a007
91565 9692 18 None - 0 Guinea pig 8.2 pKd = 8.2 Functional
Compound was evaluated for competitive antagonism of beta-1 adrenergic receptor in guinea pig atria measured as pA2 (-log KB)Compound was evaluated for competitive antagonism of beta-1 adrenergic receptor in guinea pig atria 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 Guinea pig 8.2 pKd = 8.2 Functional
Compound was evaluated for competitive antagonism of beta-1 adrenergic receptor in guinea pig atria measured as pA2 (-log KB)Compound was evaluated for competitive antagonism of beta-1 adrenergic receptor in guinea pig atria measured as pA2 (-log KB)
ChEMBL 275 6 3 4 2.3 CC(C)NCC(O)COc1ccc(O)c2ccccc12 10.1021/jm00373a008
13187531 202776 0 None - 0 Rat 8.2 pKd = 8.2 Functional
Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atriaAntagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria
ChEMBL 335 10 2 4 3.3 CC(C)NCC(O)COc1ccc(CCOC2CCCCC2)cc1 10.1021/jm00389a008
CHEMBL7250 202776 0 None - 0 Rat 8.2 pKd = 8.2 Functional
Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atriaAntagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria
ChEMBL 335 10 2 4 3.3 CC(C)NCC(O)COc1ccc(CCOC2CCCCC2)cc1 10.1021/jm00389a008
44381395 59161 0 None - 0 Guinea pig 7.3 pKd = 7.3 Functional
Compound was evaluated for competitive antagonism of beta-1 adrenergic receptor in guinea pig atria measured as pA2 (-log KB)Compound was evaluated for competitive antagonism of beta-1 adrenergic receptor in guinea pig atria 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 Guinea pig 7.3 pKd = 7.3 Functional
Compound was evaluated for competitive antagonism of beta-1 adrenergic receptor in guinea pig atria measured as pA2 (-log KB)Compound was evaluated for competitive antagonism of beta-1 adrenergic receptor in guinea pig atria 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
54756928 65142 0 None - 0 Human 7.3 pKd = 7.3 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-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 7.3 pKd = 7.3 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-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
44287620 11106 0 None - 0 Guinea pig 4.3 pKd = 4.3 Functional
Antagonistic activity against beta-1 adrenergic receptor of isolated guinea pig atriaAntagonistic activity against beta-1 adrenergic receptor of isolated guinea pig atria
ChEMBL 228 5 2 4 1.7 CC(C)(C)NCC(O)CON=C1CCCC1 10.1021/jm00380a001
CHEMBL1178780 11106 0 None - 0 Guinea pig 4.3 pKd = 4.3 Functional
Antagonistic activity against beta-1 adrenergic receptor of isolated guinea pig atriaAntagonistic activity against beta-1 adrenergic receptor of isolated guinea pig atria
ChEMBL 228 5 2 4 1.7 CC(C)(C)NCC(O)CON=C1CCCC1 10.1021/jm00380a001
CHEMBL40971 11106 0 None - 0 Guinea pig 4.3 pKd = 4.3 Functional
Antagonistic activity against beta-1 adrenergic receptor of isolated guinea pig atriaAntagonistic activity against beta-1 adrenergic receptor of isolated guinea pig atria
ChEMBL 228 5 2 4 1.7 CC(C)(C)NCC(O)CON=C1CCCC1 10.1021/jm00380a001
12606705 11810 0 None - 0 Guinea pig 6.2 pKd = 6.2 Functional
Antagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pigAntagonism of the isoprenaline-induced positive chronotropic effect on the atria 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 6.2 pKd = 6.2 Functional
Antagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pigAntagonism of the isoprenaline-induced positive chronotropic effect on the atria 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 6.2 pKd = 6.2 Functional
Antagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pigAntagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pig
ChEMBL 188 6 2 4 0.8 CC(C)=NOCC(O)CNC(C)C 10.1021/jm00180a007
2685 875 15 None - 1 Human 7.2 pKd = 7.2 Functional
Antagonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as inhibition of CGP12177-induced [3H]cAMP accumulationAntagonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as inhibition of CGP12177-induced [3H]cAMP accumulation
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 7.2 pKd = 7.2 Functional
Antagonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as inhibition of CGP12177-induced [3H]cAMP accumulationAntagonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as inhibition of CGP12177-induced [3H]cAMP accumulation
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 7.2 pKd = 7.2 Functional
Antagonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as inhibition of CGP12177-induced [3H]cAMP accumulationAntagonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as inhibition of CGP12177-induced [3H]cAMP accumulation
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
20554490 13224 0 None - 0 Rat 7.2 pKd = 7.2 Functional
Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atriaAntagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria
ChEMBL 364 13 3 5 1.5 CC(=O)NCCNCC(O)COc1ccc(CCOCC2CCC2)cc1 10.1021/jm00389a008
CHEMBL1192270 13224 0 None - 0 Rat 7.2 pKd = 7.2 Functional
Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atriaAntagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria
ChEMBL 364 13 3 5 1.5 CC(=O)NCCNCC(O)COc1ccc(CCOCC2CCC2)cc1 10.1021/jm00389a008
CHEMBL543484 13224 0 None - 0 Rat 7.2 pKd = 7.2 Functional
Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atriaAntagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria
ChEMBL 364 13 3 5 1.5 CC(=O)NCCNCC(O)COc1ccc(CCOCC2CCC2)cc1 10.1021/jm00389a008
12733303 60059 0 None - 0 Guinea pig 6.2 pKd = 6.2 Functional
Antagonist activity of compound against Beta-1 adrenergic receptor in isolated guinea pig left atriaAntagonist activity of compound against Beta-1 adrenergic receptor in isolated guinea pig left atria
ChEMBL 261 3 1 4 2.1 OC(CN1CCCCC1)C1=COc2ccccc2O1 10.1021/jm00140a015
CHEMBL174882 60059 0 None - 0 Guinea pig 6.2 pKd = 6.2 Functional
Antagonist activity of compound against Beta-1 adrenergic receptor in isolated guinea pig left atriaAntagonist activity of compound against Beta-1 adrenergic receptor in isolated guinea pig left atria
ChEMBL 261 3 1 4 2.1 OC(CN1CCCCC1)C1=COc2ccccc2O1 10.1021/jm00140a015
54669764 65146 0 None - 0 Human 7.2 pKd = 7.2 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in CGP 12177-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in CGP 12177-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 7.2 pKd = 7.2 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in CGP 12177-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in CGP 12177-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
44264149 13356 0 None - 0 Rat 8.1 pKd = 8.1 Functional
Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atriaAntagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria
ChEMBL 397 11 2 5 3.0 CC(C)NCC(O)COc1ccc(CCS(=O)(=O)CC2CCCCC2)cc1 10.1021/jm00389a008
CHEMBL1193283 13356 0 None - 0 Rat 8.1 pKd = 8.1 Functional
Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atriaAntagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria
ChEMBL 397 11 2 5 3.0 CC(C)NCC(O)COc1ccc(CCS(=O)(=O)CC2CCCCC2)cc1 10.1021/jm00389a008
CHEMBL544661 13356 0 None - 0 Rat 8.1 pKd = 8.1 Functional
Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atriaAntagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria
ChEMBL 397 11 2 5 3.0 CC(C)NCC(O)COc1ccc(CCS(=O)(=O)CC2CCCCC2)cc1 10.1021/jm00389a008
54757232 65170 0 None - 0 Human 8.1 pKd = 8.1 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-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 8.1 pKd = 8.1 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-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
157716 40260 40 None - 0 Guinea pig 8.1 pKd = 8.1 Functional
Compound was tested for its Beta-1 adrenergic receptor antagonistic activity on guinea pig arteriaCompound was tested for its Beta-1 adrenergic receptor antagonistic activity on guinea pig arteria
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 8.1 pKd = 8.1 Functional
Compound was tested for its Beta-1 adrenergic receptor antagonistic activity on guinea pig arteriaCompound was tested for its Beta-1 adrenergic receptor antagonistic activity on guinea pig arteria
ChEMBL 267 9 2 4 1.6 COCCc1ccc(OC[C@@H](O)CNC(C)C)cc1 10.1021/jm00350a009
44371389 12094 0 None - 0 Guinea pig 6.1 pKd = 6.1 Functional
Antagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pigAntagonism of the isoprenaline-induced positive chronotropic effect on the atria 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
Antagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pigAntagonism of the isoprenaline-induced positive chronotropic effect on the atria 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
Antagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pigAntagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pig
ChEMBL 202 7 2 4 1.1 CC/C(C)=N\OCC(O)CNC(C)C 10.1021/jm00180a007
1786 2474 79 None -4 6 Guinea pig 6.1 pKd = 6.1 Functional
Cardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated guinea pig tracheaCardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated guinea pig trachea
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm00389a008
4171 2474 79 None -4 6 Guinea pig 6.1 pKd = 6.1 Functional
Cardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated guinea pig tracheaCardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated guinea pig trachea
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm00389a008
553 2474 79 None -4 6 Guinea pig 6.1 pKd = 6.1 Functional
Cardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated guinea pig tracheaCardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated guinea pig trachea
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm00389a008
CHEMBL13 2474 79 None -4 6 Guinea pig 6.1 pKd = 6.1 Functional
Cardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated guinea pig tracheaCardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated guinea pig trachea
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm00389a008
DB00264 2474 79 None -4 6 Guinea pig 6.1 pKd = 6.1 Functional
Cardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated guinea pig tracheaCardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated guinea pig trachea
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm00389a008
54757129 65148 0 None - 0 Human 7.1 pKd = 7.1 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in CGP 12177-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in CGP 12177-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 7.1 pKd = 7.1 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in CGP 12177-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in CGP 12177-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
157717 59911 33 None - 1 Guinea pig 6.1 pKd = 6.1 Functional
Compound was tested for its Beta-1 adrenergic receptor antagonistic activity on guinea pig arteriaCompound was tested for its Beta-1 adrenergic receptor antagonistic activity on guinea pig arteria
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 6.1 pKd = 6.1 Functional
Compound was tested for its Beta-1 adrenergic receptor antagonistic activity on guinea pig arteriaCompound was tested for its Beta-1 adrenergic receptor antagonistic activity on guinea pig arteria
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 6.1 pKd = 6.1 Functional
Compound was tested for its Beta-1 adrenergic receptor antagonistic activity on guinea pig arteriaCompound was tested for its Beta-1 adrenergic receptor antagonistic activity on guinea pig arteria
ChEMBL 267 9 2 4 1.6 COCCc1ccc(OC[C@H](O)CNC(C)C)cc1 10.1021/jm00350a009
54756929 65143 0 None - 0 Human 7.1 pKd = 7.1 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-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 7.1 pKd = 7.1 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-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
54757331 65171 0 None - 0 Human 7.1 pKd = 7.1 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in CGP 12177-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in CGP 12177-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 7.1 pKd = 7.1 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in CGP 12177-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in CGP 12177-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
20554484 202426 0 None - 0 Rat 7.1 pKd = 7.1 Functional
Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atriaAntagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria
ChEMBL 337 11 2 4 3.5 CC(C)NCC(O)COc1ccc(CCSCC2CCC2)cc1 10.1021/jm00389a008
CHEMBL7043 202426 0 None - 0 Rat 7.1 pKd = 7.1 Functional
Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atriaAntagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria
ChEMBL 337 11 2 4 3.5 CC(C)NCC(O)COc1ccc(CCSCC2CCC2)cc1 10.1021/jm00389a008
44264171 96609 0 None - 0 Rat 5.1 pKd = 5.1 Functional
Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atriaAntagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria
ChEMBL 411 14 2 4 4.4 CC(CCc1ccccc1)NCC(O)COc1ccc(CCOCC2CCC2)cc1 10.1021/jm00389a008
CHEMBL267220 96609 0 None - 0 Rat 5.1 pKd = 5.1 Functional
Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atriaAntagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria
ChEMBL 411 14 2 4 4.4 CC(CCc1ccccc1)NCC(O)COc1ccc(CCOCC2CCC2)cc1 10.1021/jm00389a008
54756928 65142 0 None - 0 Human 6.1 pKd = 6.1 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in CGP 12177-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in CGP 12177-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 6.1 pKd = 6.1 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in CGP 12177-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in CGP 12177-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
44371561 49434 0 None - 0 Guinea pig 5.1 pKd = 5.1 Functional
Antagonist activity against beta-1 adrenergic receptor in isolated guinea pig atriaAntagonist activity against beta-1 adrenergic receptor in isolated guinea pig atria
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 5.1 pKd = 5.1 Functional
Antagonist activity against beta-1 adrenergic receptor in isolated guinea pig atriaAntagonist activity against beta-1 adrenergic receptor in isolated guinea pig atria
ChEMBL 257 5 2 4 1.9 CC(C)(C)NCC(O)COC(=O)C1CCCCC1 10.1021/jm00387a006
54758417 65140 0 None - 0 Human 8.1 pKd = 8.1 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-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 8.1 pKd = 8.1 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-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
12733302 165779 1 None - 0 Guinea pig 8.1 pKd = 8.1 Functional
Antagonist activity of compound against Beta-1 adrenergic receptor in isolated guinea pig left atriaAntagonist activity of compound against Beta-1 adrenergic receptor in isolated guinea pig left atria
ChEMBL 249 3 2 4 2.0 CC(C)(C)NCC(O)C1=COc2ccccc2O1 10.1021/jm00140a015
CHEMBL427310 165779 1 None - 0 Guinea pig 8.1 pKd = 8.1 Functional
Antagonist activity of compound against Beta-1 adrenergic receptor in isolated guinea pig left atriaAntagonist activity of compound against Beta-1 adrenergic receptor in isolated guinea pig left atria
ChEMBL 249 3 2 4 2.0 CC(C)(C)NCC(O)C1=COc2ccccc2O1 10.1021/jm00140a015
165193 3126 60 None -27 13 Guinea pig 8.1 pKd = 8.1 Functional
Antagonist activity of compound against Beta-1 adrenergic receptor in isolated guinea pig left atriaAntagonist activity of compound against Beta-1 adrenergic receptor in isolated guinea pig left atria
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00140a015
2303 3126 60 None -27 13 Guinea pig 8.1 pKd = 8.1 Functional
Antagonist activity of compound against Beta-1 adrenergic receptor in isolated guinea pig left atriaAntagonist activity of compound against Beta-1 adrenergic receptor in isolated guinea pig left atria
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00140a015
4946 3126 60 None -27 13 Guinea pig 8.1 pKd = 8.1 Functional
Antagonist activity of compound against Beta-1 adrenergic receptor in isolated guinea pig left atriaAntagonist activity of compound against Beta-1 adrenergic receptor in isolated guinea pig left atria
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00140a015
564 3126 60 None -27 13 Guinea pig 8.1 pKd = 8.1 Functional
Antagonist activity of compound against Beta-1 adrenergic receptor in isolated guinea pig left atriaAntagonist activity of compound against Beta-1 adrenergic receptor in isolated guinea pig left atria
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00140a015
62882 3126 60 None -27 13 Guinea pig 8.1 pKd = 8.1 Functional
Antagonist activity of compound against Beta-1 adrenergic receptor in isolated guinea pig left atriaAntagonist activity of compound against Beta-1 adrenergic receptor in isolated guinea pig left atria
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00140a015
63 3126 60 None -27 13 Guinea pig 8.1 pKd = 8.1 Functional
Antagonist activity of compound against Beta-1 adrenergic receptor in isolated guinea pig left atriaAntagonist activity of compound against Beta-1 adrenergic receptor in isolated guinea pig left atria
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00140a015
66366 3126 60 None -27 13 Guinea pig 8.1 pKd = 8.1 Functional
Antagonist activity of compound against Beta-1 adrenergic receptor in isolated guinea pig left atriaAntagonist activity of compound against Beta-1 adrenergic receptor in isolated guinea pig left atria
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00140a015
91536 3126 60 None -27 13 Guinea pig 8.1 pKd = 8.1 Functional
Antagonist activity of compound against Beta-1 adrenergic receptor in isolated guinea pig left atriaAntagonist activity of compound against Beta-1 adrenergic receptor in isolated guinea pig left atria
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00140a015
CHEMBL27 3126 60 None -27 13 Guinea pig 8.1 pKd = 8.1 Functional
Antagonist activity of compound against Beta-1 adrenergic receptor in isolated guinea pig left atriaAntagonist activity of compound against Beta-1 adrenergic receptor in isolated guinea pig left atria
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00140a015
CHEMBL452861 3126 60 None -27 13 Guinea pig 8.1 pKd = 8.1 Functional
Antagonist activity of compound against Beta-1 adrenergic receptor in isolated guinea pig left atriaAntagonist activity of compound against Beta-1 adrenergic receptor in isolated guinea pig left atria
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00140a015
DB00571 3126 60 None -27 13 Guinea pig 8.1 pKd = 8.1 Functional
Antagonist activity of compound against Beta-1 adrenergic receptor in isolated guinea pig left atriaAntagonist activity of compound against Beta-1 adrenergic receptor in isolated guinea pig left atria
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00140a015
12606702 11893 0 None - 0 Guinea pig 5.1 pKd = 5.1 Functional
Antagonistic activity against beta-1 adrenergic receptor of isolated guinea pig atriaAntagonistic activity against beta-1 adrenergic receptor of isolated guinea pig atria
ChEMBL 242 5 2 4 2.1 CC(C)(C)NCC(O)CON=C1CCCCC1 10.1021/jm00380a001
CHEMBL1161383 11893 0 None - 0 Guinea pig 5.1 pKd = 5.1 Functional
Antagonistic activity against beta-1 adrenergic receptor of isolated guinea pig atriaAntagonistic activity against beta-1 adrenergic receptor of isolated guinea pig atria
ChEMBL 242 5 2 4 2.1 CC(C)(C)NCC(O)CON=C1CCCCC1 10.1021/jm00380a001
CHEMBL1183312 11893 0 None - 0 Guinea pig 5.1 pKd = 5.1 Functional
Antagonistic activity against beta-1 adrenergic receptor of isolated guinea pig atriaAntagonistic activity against beta-1 adrenergic receptor of isolated guinea pig atria
ChEMBL 242 5 2 4 2.1 CC(C)(C)NCC(O)CON=C1CCCCC1 10.1021/jm00380a001
CHEMBL289868 11893 0 None - 0 Guinea pig 5.1 pKd = 5.1 Functional
Antagonistic activity against beta-1 adrenergic receptor of isolated guinea pig atriaAntagonistic activity against beta-1 adrenergic receptor of isolated guinea pig atria
ChEMBL 242 5 2 4 2.1 CC(C)(C)NCC(O)CON=C1CCCCC1 10.1021/jm00380a001
3486 3096 51 None - 0 Guinea pig 5.1 pKd = 5.1 Functional
Cardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated guinea pig tracheaCardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated guinea pig trachea
ChEMBL 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C 10.1021/jm00389a008
4883 3096 51 None - 0 Guinea pig 5.1 pKd = 5.1 Functional
Cardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated guinea pig tracheaCardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated guinea pig trachea
ChEMBL 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C 10.1021/jm00389a008
555 3096 51 None - 0 Guinea pig 5.1 pKd = 5.1 Functional
Cardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated guinea pig tracheaCardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated guinea pig trachea
ChEMBL 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C 10.1021/jm00389a008
CHEMBL6995 3096 51 None - 0 Guinea pig 5.1 pKd = 5.1 Functional
Cardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated guinea pig tracheaCardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated guinea pig trachea
ChEMBL 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C 10.1021/jm00389a008
DB01297 3096 51 None - 0 Guinea pig 5.1 pKd = 5.1 Functional
Cardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated guinea pig tracheaCardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated guinea pig trachea
ChEMBL 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C 10.1021/jm00389a008
12606703 13459 0 None - 0 Guinea pig 6.1 pKd = 6.1 Functional
Antagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pigAntagonism of the isoprenaline-induced positive chronotropic effect on the atria 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
Antagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pigAntagonism of the isoprenaline-induced positive chronotropic effect on the atria 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
Antagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pigAntagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pig
ChEMBL 276 8 2 4 2.5 CC(/C=C/c1ccccc1)=N\OCC(O)CNC(C)C 10.1021/jm00180a007
3047492 202259 8 None - 0 Rat 8.0 pKd = 8.0 Functional
Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atriaAntagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria
ChEMBL 293 10 2 4 2.4 CC(C)NCC(O)COc1ccc(COCC2CC2)cc1 10.1021/jm00389a008
CHEMBL6939 202259 8 None - 0 Rat 8.0 pKd = 8.0 Functional
Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atriaAntagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria
ChEMBL 293 10 2 4 2.4 CC(C)NCC(O)COc1ccc(COCC2CC2)cc1 10.1021/jm00389a008
3047492 202259 8 None - 0 Rat 8.0 pKd = 8.0 Functional
Cardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated rat atriaCardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated rat atria
ChEMBL 293 10 2 4 2.4 CC(C)NCC(O)COc1ccc(COCC2CC2)cc1 10.1021/jm00389a008
CHEMBL6939 202259 8 None - 0 Rat 8.0 pKd = 8.0 Functional
Cardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated rat atriaCardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated rat atria
ChEMBL 293 10 2 4 2.4 CC(C)NCC(O)COc1ccc(COCC2CC2)cc1 10.1021/jm00389a008
54758417 65140 0 None - 0 Human 7.0 pKd = 7.0 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in CGP 12177-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in CGP 12177-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 7.0 pKd = 7.0 Functional
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in CGP 12177-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysisAntagonist activity at human beta-1 adrenergic receptor site 1 expressed in CGP 12177-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
110857 12096 55 None - 0 Guinea pig 4.0 pKd = 4.0 Functional
Antagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pigAntagonism of the isoprenaline-induced positive chronotropic effect on the atria 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 4.0 pKd = 4.0 Functional
Antagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pigAntagonism of the isoprenaline-induced positive chronotropic effect on the atria 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 4.0 pKd = 4.0 Functional
Antagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pigAntagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pig
ChEMBL 133 4 3 3 -0.7 CC(C)NCC(O)CO 10.1021/jm00180a007
44264446 10958 0 None - 0 Rat 7.0 pKd = 7.0 Functional
Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atriaAntagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria
ChEMBL 335 12 2 4 3.2 CC(C)NCC(O)COc1ccc(CCCOCC2CCC2)cc1 10.1021/jm00389a008
CHEMBL1177932 10958 0 None - 0 Rat 7.0 pKd = 7.0 Functional
Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atriaAntagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria
ChEMBL 335 12 2 4 3.2 CC(C)NCC(O)COc1ccc(CCCOCC2CCC2)cc1 10.1021/jm00389a008
CHEMBL7209 10958 0 None - 0 Rat 7.0 pKd = 7.0 Functional
Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atriaAntagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria
ChEMBL 335 12 2 4 3.2 CC(C)NCC(O)COc1ccc(CCCOCC2CCC2)cc1 10.1021/jm00389a008
44287467 11104 0 None - 0 Guinea pig 6.0 pKd = 6.0 Functional
Antagonistic activity against beta-1 adrenergic receptor of isolated guinea pig atriaAntagonistic activity against beta-1 adrenergic receptor of isolated guinea pig atria
ChEMBL 216 8 2 4 1.5 CCC(CC)=NOCC(O)CNC(C)C 10.1021/jm00380a001
CHEMBL1178777 11104 0 None - 0 Guinea pig 6.0 pKd = 6.0 Functional
Antagonistic activity against beta-1 adrenergic receptor of isolated guinea pig atriaAntagonistic activity against beta-1 adrenergic receptor of isolated guinea pig atria
ChEMBL 216 8 2 4 1.5 CCC(CC)=NOCC(O)CNC(C)C 10.1021/jm00380a001
CHEMBL40626 11104 0 None - 0 Guinea pig 6.0 pKd = 6.0 Functional
Antagonistic activity against beta-1 adrenergic receptor of isolated guinea pig atriaAntagonistic activity against beta-1 adrenergic receptor of isolated guinea pig atria
ChEMBL 216 8 2 4 1.5 CCC(CC)=NOCC(O)CNC(C)C 10.1021/jm00380a001
3047497 13273 10 None - 0 Guinea pig 6.0 pKd = 6.0 Functional
Cardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated guinea pig tracheaCardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated guinea pig trachea
ChEMBL 321 11 2 4 2.8 CC(C)NCC(O)COc1ccc(CCOCC2CCC2)cc1 10.1021/jm00389a008
CHEMBL1192675 13273 10 None - 0 Guinea pig 6.0 pKd = 6.0 Functional
Cardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated guinea pig tracheaCardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated guinea pig trachea
ChEMBL 321 11 2 4 2.8 CC(C)NCC(O)COc1ccc(CCOCC2CCC2)cc1 10.1021/jm00389a008
CHEMBL543955 13273 10 None - 0 Guinea pig 6.0 pKd = 6.0 Functional
Cardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated guinea pig tracheaCardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated guinea pig trachea
ChEMBL 321 11 2 4 2.8 CC(C)NCC(O)COc1ccc(CCOCC2CCC2)cc1 10.1021/jm00389a008
44276727 96852 0 None - 2 Guinea pig 7.0 pKd = 7.0 Functional
Compound was tested for its Beta-1 adrenergic receptor antagonistic activity on guinea pig atriaCompound was tested for its Beta-1 adrenergic receptor antagonistic activity on guinea pig atria
ChEMBL 263 6 2 3 2.2 Cc1ccc(OCC(O)CNC(C)C)c2c1CCC2 10.1021/jm00350a009
CHEMBL26917 96852 0 None - 2 Guinea pig 7.0 pKd = 7.0 Functional
Compound was tested for its Beta-1 adrenergic receptor antagonistic activity on guinea pig atriaCompound was tested for its Beta-1 adrenergic receptor antagonistic activity on guinea pig atria
ChEMBL 263 6 2 3 2.2 Cc1ccc(OCC(O)CNC(C)C)c2c1CCC2 10.1021/jm00350a009
12606685 11547 0 None - 0 Guinea pig 6.0 pKd = 6.0 Functional
Antagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pigAntagonism of the isoprenaline-induced positive chronotropic effect on the atria 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 6.0 pKd = 6.0 Functional
Antagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pigAntagonism of the isoprenaline-induced positive chronotropic effect on the atria 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 6.0 pKd = 6.0 Functional
Antagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pigAntagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pig
ChEMBL 189 7 2 3 1.0 CC(C)COCC(O)CNC(C)C 10.1021/jm00180a007
132 1244 9 None - 0 Rat 10.4 pKi = 10.4 Functional
Antagonist activity at rat beta-1 adrenergic receptor Y356F mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor Y356F mutant expressed in CHO cells
ChEMBL 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 10.1021/jm050624l
155346 1244 9 None - 0 Rat 10.4 pKi = 10.4 Functional
Antagonist activity at rat beta-1 adrenergic receptor Y356F mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor Y356F mutant expressed in CHO cells
ChEMBL 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 10.1021/jm050624l
CHEMBL378501 1244 9 None - 0 Rat 10.4 pKi = 10.4 Functional
Antagonist activity at rat beta-1 adrenergic receptor Y356F mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor Y356F mutant expressed in CHO cells
ChEMBL 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 10.1021/jm050624l
132 1244 9 None - 0 Rat 10.3 pKi = 10.3 Functional
Antagonist activity at rat wild type beta-1 adrenergic receptor expressed in CHO cellsAntagonist activity at rat wild type beta-1 adrenergic receptor expressed in CHO cells
ChEMBL 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 10.1021/jm050624l
155346 1244 9 None - 0 Rat 10.3 pKi = 10.3 Functional
Antagonist activity at rat wild type beta-1 adrenergic receptor expressed in CHO cellsAntagonist activity at rat wild type beta-1 adrenergic receptor expressed in CHO cells
ChEMBL 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 10.1021/jm050624l
CHEMBL378501 1244 9 None - 0 Rat 10.3 pKi = 10.3 Functional
Antagonist activity at rat wild type beta-1 adrenergic receptor expressed in CHO cellsAntagonist activity at rat wild type beta-1 adrenergic receptor expressed in CHO cells
ChEMBL 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 10.1021/jm050624l
132 1244 9 None - 0 Rat 9.9 pKi = 9.9 Functional
Antagonist activity at rat beta-1 adrenergic receptor W134A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor W134A mutant expressed in CHO cells
ChEMBL 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 10.1021/jm050624l
155346 1244 9 None - 0 Rat 9.9 pKi = 9.9 Functional
Antagonist activity at rat beta-1 adrenergic receptor W134A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor W134A mutant expressed in CHO cells
ChEMBL 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 10.1021/jm050624l
CHEMBL378501 1244 9 None - 0 Rat 9.9 pKi = 9.9 Functional
Antagonist activity at rat beta-1 adrenergic receptor W134A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor W134A mutant expressed in CHO cells
ChEMBL 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 10.1021/jm050624l
132 1244 9 None - 0 Rat 9.5 pKi = 9.5 Functional
Antagonist activity at rat beta-1 adrenergic receptor S190A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor S190A mutant expressed in CHO cells
ChEMBL 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 10.1021/jm050624l
155346 1244 9 None - 0 Rat 9.5 pKi = 9.5 Functional
Antagonist activity at rat beta-1 adrenergic receptor S190A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor S190A mutant expressed in CHO cells
ChEMBL 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 10.1021/jm050624l
CHEMBL378501 1244 9 None - 0 Rat 9.5 pKi = 9.5 Functional
Antagonist activity at rat beta-1 adrenergic receptor S190A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor S190A mutant expressed in CHO cells
ChEMBL 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 10.1021/jm050624l
2685 875 15 None - 1 Rat 8.9 pKi = 8.9 Functional
Antagonist activity at rat wild type beta-1 adrenergic receptor expressed in CHO cellsAntagonist activity at rat wild type beta-1 adrenergic receptor expressed in CHO cells
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/jm050624l
541 875 15 None - 1 Rat 8.9 pKi = 8.9 Functional
Antagonist activity at rat wild type beta-1 adrenergic receptor expressed in CHO cellsAntagonist activity at rat wild type beta-1 adrenergic receptor expressed in CHO cells
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/jm050624l
CHEMBL280822 875 15 None - 1 Rat 8.9 pKi = 8.9 Functional
Antagonist activity at rat wild type beta-1 adrenergic receptor expressed in CHO cellsAntagonist activity at rat wild type beta-1 adrenergic receptor expressed in CHO cells
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/jm050624l
2685 875 15 None - 1 Rat 8.7 pKi = 8.7 Functional
Antagonist activity at rat beta-1 adrenergic receptor Y356F mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor Y356F mutant expressed in CHO cells
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/jm050624l
541 875 15 None - 1 Rat 8.7 pKi = 8.7 Functional
Antagonist activity at rat beta-1 adrenergic receptor Y356F mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor Y356F mutant expressed in CHO cells
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/jm050624l
CHEMBL280822 875 15 None - 1 Rat 8.7 pKi = 8.7 Functional
Antagonist activity at rat beta-1 adrenergic receptor Y356F mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor Y356F mutant expressed in CHO cells
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/jm050624l
165193 3126 60 None - 13 Rat 8.0 pKi = 8 Functional
Antagonist activity at rat beta-1 adrenergic receptor W134A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor W134A mutant expressed in CHO cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm050624l
2303 3126 60 None - 13 Rat 8.0 pKi = 8 Functional
Antagonist activity at rat beta-1 adrenergic receptor W134A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor W134A mutant expressed in CHO cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm050624l
4946 3126 60 None - 13 Rat 8.0 pKi = 8 Functional
Antagonist activity at rat beta-1 adrenergic receptor W134A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor W134A mutant expressed in CHO cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm050624l
564 3126 60 None - 13 Rat 8.0 pKi = 8 Functional
Antagonist activity at rat beta-1 adrenergic receptor W134A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor W134A mutant expressed in CHO cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm050624l
62882 3126 60 None - 13 Rat 8.0 pKi = 8 Functional
Antagonist activity at rat beta-1 adrenergic receptor W134A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor W134A mutant expressed in CHO cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm050624l
63 3126 60 None - 13 Rat 8.0 pKi = 8 Functional
Antagonist activity at rat beta-1 adrenergic receptor W134A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor W134A mutant expressed in CHO cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm050624l
66366 3126 60 None - 13 Rat 8.0 pKi = 8 Functional
Antagonist activity at rat beta-1 adrenergic receptor W134A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor W134A mutant expressed in CHO cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm050624l
91536 3126 60 None - 13 Rat 8.0 pKi = 8 Functional
Antagonist activity at rat beta-1 adrenergic receptor W134A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor W134A mutant expressed in CHO cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm050624l
CHEMBL27 3126 60 None - 13 Rat 8.0 pKi = 8 Functional
Antagonist activity at rat beta-1 adrenergic receptor W134A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor W134A mutant expressed in CHO cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm050624l
CHEMBL452861 3126 60 None - 13 Rat 8.0 pKi = 8 Functional
Antagonist activity at rat beta-1 adrenergic receptor W134A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor W134A mutant expressed in CHO cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm050624l
DB00571 3126 60 None - 13 Rat 8.0 pKi = 8 Functional
Antagonist activity at rat beta-1 adrenergic receptor W134A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor W134A mutant expressed in CHO cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm050624l
5311116 2293 6 None - 3 Rat 7.0 pKi = 7 Functional
Antagonist activity at rat beta-1 adrenergic receptor S190A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor S190A mutant expressed in CHO cells
ChEMBL 484 15 5 8 2.2 N#Cc1cc(OCCOCC2CC2)ccc1OCC(CNCCNC(=O)Nc1ccc(cc1)O)O 10.1021/jm050624l
544 2293 6 None - 3 Rat 7.0 pKi = 7 Functional
Antagonist activity at rat beta-1 adrenergic receptor S190A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor S190A mutant expressed in CHO cells
ChEMBL 484 15 5 8 2.2 N#Cc1cc(OCCOCC2CC2)ccc1OCC(CNCCNC(=O)Nc1ccc(cc1)O)O 10.1021/jm050624l
CHEMBL207802 2293 6 None - 3 Rat 7.0 pKi = 7 Functional
Antagonist activity at rat beta-1 adrenergic receptor S190A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor S190A mutant expressed in CHO cells
ChEMBL 484 15 5 8 2.2 N#Cc1cc(OCCOCC2CC2)ccc1OCC(CNCCNC(=O)Nc1ccc(cc1)O)O 10.1021/jm050624l
9909993 76925 0 None - 0 Rat 7.0 pKi = 7 Functional
Antagonist activity at rat beta-1 adrenergic receptor Y356F mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor Y356F mutant expressed in CHO cells
ChEMBL 419 15 2 7 2.7 CCOCCOc1ccc(OC[C@@H](O)CNCCc2ccc(OC)c(OC)c2)cc1 10.1021/jm050624l
CHEMBL208185 76925 0 None - 0 Rat 7.0 pKi = 7 Functional
Antagonist activity at rat beta-1 adrenergic receptor Y356F mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor Y356F mutant expressed in CHO cells
ChEMBL 419 15 2 7 2.7 CCOCCOc1ccc(OC[C@@H](O)CNCCc2ccc(OC)c(OC)c2)cc1 10.1021/jm050624l
2685 875 15 None - 1 Rat 5.0 pKi = 5 Functional
Antagonist activity at rat beta-1 adrenergic receptor Y356A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor Y356A mutant expressed in CHO cells
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/jm050624l
541 875 15 None - 1 Rat 5.0 pKi = 5 Functional
Antagonist activity at rat beta-1 adrenergic receptor Y356A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor Y356A mutant expressed in CHO cells
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/jm050624l
CHEMBL280822 875 15 None - 1 Rat 5.0 pKi = 5 Functional
Antagonist activity at rat beta-1 adrenergic receptor Y356A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor Y356A mutant expressed in CHO cells
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/jm050624l
9909993 76925 0 None - 0 Rat 4.9 pKi = 4.9 Functional
Antagonist activity at rat beta-1 adrenergic receptor S190A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor S190A mutant expressed in CHO cells
ChEMBL 419 15 2 7 2.7 CCOCCOc1ccc(OC[C@@H](O)CNCCc2ccc(OC)c(OC)c2)cc1 10.1021/jm050624l
CHEMBL208185 76925 0 None - 0 Rat 4.9 pKi = 4.9 Functional
Antagonist activity at rat beta-1 adrenergic receptor S190A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor S190A mutant expressed in CHO cells
ChEMBL 419 15 2 7 2.7 CCOCCOc1ccc(OC[C@@H](O)CNCCc2ccc(OC)c(OC)c2)cc1 10.1021/jm050624l
33624 3749 29 None - 5 Rat 7.8 pKi = 7.8 Functional
Antagonist activity at rat beta-1 adrenergic receptor Y356F mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor Y356F mutant expressed in CHO cells
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C 10.1021/jm050624l
4061 3749 29 None - 5 Rat 7.8 pKi = 7.8 Functional
Antagonist activity at rat beta-1 adrenergic receptor Y356F mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor Y356F mutant expressed in CHO cells
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C 10.1021/jm050624l
565 3749 29 None - 5 Rat 7.8 pKi = 7.8 Functional
Antagonist activity at rat beta-1 adrenergic receptor Y356F mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor Y356F mutant expressed in CHO cells
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C 10.1021/jm050624l
CHEMBL499 3749 29 None - 5 Rat 7.8 pKi = 7.8 Functional
Antagonist activity at rat beta-1 adrenergic receptor Y356F mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor Y356F mutant expressed in CHO cells
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C 10.1021/jm050624l
DB00373 3749 29 None - 5 Rat 7.8 pKi = 7.8 Functional
Antagonist activity at rat beta-1 adrenergic receptor Y356F mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor Y356F mutant expressed in CHO cells
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C 10.1021/jm050624l
165193 3126 60 None - 13 Rat 6.7 pKi = 6.7 Functional
Antagonist activity at rat beta-1 adrenergic receptor Y356A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor Y356A mutant expressed in CHO cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm050624l
2303 3126 60 None - 13 Rat 6.7 pKi = 6.7 Functional
Antagonist activity at rat beta-1 adrenergic receptor Y356A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor Y356A mutant expressed in CHO cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm050624l
4946 3126 60 None - 13 Rat 6.7 pKi = 6.7 Functional
Antagonist activity at rat beta-1 adrenergic receptor Y356A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor Y356A mutant expressed in CHO cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm050624l
564 3126 60 None - 13 Rat 6.7 pKi = 6.7 Functional
Antagonist activity at rat beta-1 adrenergic receptor Y356A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor Y356A mutant expressed in CHO cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm050624l
62882 3126 60 None - 13 Rat 6.7 pKi = 6.7 Functional
Antagonist activity at rat beta-1 adrenergic receptor Y356A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor Y356A mutant expressed in CHO cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm050624l
63 3126 60 None - 13 Rat 6.7 pKi = 6.7 Functional
Antagonist activity at rat beta-1 adrenergic receptor Y356A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor Y356A mutant expressed in CHO cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm050624l
66366 3126 60 None - 13 Rat 6.7 pKi = 6.7 Functional
Antagonist activity at rat beta-1 adrenergic receptor Y356A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor Y356A mutant expressed in CHO cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm050624l
91536 3126 60 None - 13 Rat 6.7 pKi = 6.7 Functional
Antagonist activity at rat beta-1 adrenergic receptor Y356A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor Y356A mutant expressed in CHO cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm050624l
CHEMBL27 3126 60 None - 13 Rat 6.7 pKi = 6.7 Functional
Antagonist activity at rat beta-1 adrenergic receptor Y356A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor Y356A mutant expressed in CHO cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm050624l
CHEMBL452861 3126 60 None - 13 Rat 6.7 pKi = 6.7 Functional
Antagonist activity at rat beta-1 adrenergic receptor Y356A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor Y356A mutant expressed in CHO cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm050624l
DB00571 3126 60 None - 13 Rat 6.7 pKi = 6.7 Functional
Antagonist activity at rat beta-1 adrenergic receptor Y356A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor Y356A mutant expressed in CHO cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm050624l
1786 2474 79 None - 6 Rat 5.6 pKi = 5.6 Functional
Antagonist activity at rat beta-1 adrenergic receptor S190A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor S190A mutant expressed in CHO cells
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm050624l
4171 2474 79 None - 6 Rat 5.6 pKi = 5.6 Functional
Antagonist activity at rat beta-1 adrenergic receptor S190A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor S190A mutant expressed in CHO cells
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm050624l
553 2474 79 None - 6 Rat 5.6 pKi = 5.6 Functional
Antagonist activity at rat beta-1 adrenergic receptor S190A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor S190A mutant expressed in CHO cells
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm050624l
CHEMBL13 2474 79 None - 6 Rat 5.6 pKi = 5.6 Functional
Antagonist activity at rat beta-1 adrenergic receptor S190A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor S190A mutant expressed in CHO cells
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm050624l
DB00264 2474 79 None - 6 Rat 5.6 pKi = 5.6 Functional
Antagonist activity at rat beta-1 adrenergic receptor S190A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor S190A mutant expressed in CHO cells
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm050624l
1786 2474 79 None - 6 Rat 5.6 pKi = 5.6 Functional
Antagonist activity at rat beta-1 adrenergic receptor Y356F mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor Y356F mutant expressed in CHO cells
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm050624l
4171 2474 79 None - 6 Rat 5.6 pKi = 5.6 Functional
Antagonist activity at rat beta-1 adrenergic receptor Y356F mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor Y356F mutant expressed in CHO cells
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm050624l
553 2474 79 None - 6 Rat 5.6 pKi = 5.6 Functional
Antagonist activity at rat beta-1 adrenergic receptor Y356F mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor Y356F mutant expressed in CHO cells
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm050624l
CHEMBL13 2474 79 None - 6 Rat 5.6 pKi = 5.6 Functional
Antagonist activity at rat beta-1 adrenergic receptor Y356F mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor Y356F mutant expressed in CHO cells
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm050624l
DB00264 2474 79 None - 6 Rat 5.6 pKi = 5.6 Functional
Antagonist activity at rat beta-1 adrenergic receptor Y356F mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor Y356F mutant expressed in CHO cells
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm050624l
165193 3126 60 None - 13 Rat 8.5 pKi = 8.5 Functional
Antagonist activity at rat wild type beta-1 adrenergic receptor expressed in CHO cellsAntagonist activity at rat wild type beta-1 adrenergic receptor expressed in CHO cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm050624l
2303 3126 60 None - 13 Rat 8.5 pKi = 8.5 Functional
Antagonist activity at rat wild type beta-1 adrenergic receptor expressed in CHO cellsAntagonist activity at rat wild type beta-1 adrenergic receptor expressed in CHO cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm050624l
4946 3126 60 None - 13 Rat 8.5 pKi = 8.5 Functional
Antagonist activity at rat wild type beta-1 adrenergic receptor expressed in CHO cellsAntagonist activity at rat wild type beta-1 adrenergic receptor expressed in CHO cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm050624l
564 3126 60 None - 13 Rat 8.5 pKi = 8.5 Functional
Antagonist activity at rat wild type beta-1 adrenergic receptor expressed in CHO cellsAntagonist activity at rat wild type beta-1 adrenergic receptor expressed in CHO cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm050624l
62882 3126 60 None - 13 Rat 8.5 pKi = 8.5 Functional
Antagonist activity at rat wild type beta-1 adrenergic receptor expressed in CHO cellsAntagonist activity at rat wild type beta-1 adrenergic receptor expressed in CHO cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm050624l
63 3126 60 None - 13 Rat 8.5 pKi = 8.5 Functional
Antagonist activity at rat wild type beta-1 adrenergic receptor expressed in CHO cellsAntagonist activity at rat wild type beta-1 adrenergic receptor expressed in CHO cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm050624l
66366 3126 60 None - 13 Rat 8.5 pKi = 8.5 Functional
Antagonist activity at rat wild type beta-1 adrenergic receptor expressed in CHO cellsAntagonist activity at rat wild type beta-1 adrenergic receptor expressed in CHO cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm050624l
91536 3126 60 None - 13 Rat 8.5 pKi = 8.5 Functional
Antagonist activity at rat wild type beta-1 adrenergic receptor expressed in CHO cellsAntagonist activity at rat wild type beta-1 adrenergic receptor expressed in CHO cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm050624l
CHEMBL27 3126 60 None - 13 Rat 8.5 pKi = 8.5 Functional
Antagonist activity at rat wild type beta-1 adrenergic receptor expressed in CHO cellsAntagonist activity at rat wild type beta-1 adrenergic receptor expressed in CHO cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm050624l
CHEMBL452861 3126 60 None - 13 Rat 8.5 pKi = 8.5 Functional
Antagonist activity at rat wild type beta-1 adrenergic receptor expressed in CHO cellsAntagonist activity at rat wild type beta-1 adrenergic receptor expressed in CHO cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm050624l
DB00571 3126 60 None - 13 Rat 8.5 pKi = 8.5 Functional
Antagonist activity at rat wild type beta-1 adrenergic receptor expressed in CHO cellsAntagonist activity at rat wild type beta-1 adrenergic receptor expressed in CHO cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm050624l
33624 3749 29 None - 5 Rat 8.5 pKi = 8.5 Functional
Antagonist activity at rat wild type beta-1 adrenergic receptor expressed in CHO cellsAntagonist activity at rat wild type beta-1 adrenergic receptor expressed in CHO cells
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C 10.1021/jm050624l
4061 3749 29 None - 5 Rat 8.5 pKi = 8.5 Functional
Antagonist activity at rat wild type beta-1 adrenergic receptor expressed in CHO cellsAntagonist activity at rat wild type beta-1 adrenergic receptor expressed in CHO cells
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C 10.1021/jm050624l
565 3749 29 None - 5 Rat 8.5 pKi = 8.5 Functional
Antagonist activity at rat wild type beta-1 adrenergic receptor expressed in CHO cellsAntagonist activity at rat wild type beta-1 adrenergic receptor expressed in CHO cells
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C 10.1021/jm050624l
CHEMBL499 3749 29 None - 5 Rat 8.5 pKi = 8.5 Functional
Antagonist activity at rat wild type beta-1 adrenergic receptor expressed in CHO cellsAntagonist activity at rat wild type beta-1 adrenergic receptor expressed in CHO cells
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C 10.1021/jm050624l
DB00373 3749 29 None - 5 Rat 8.5 pKi = 8.5 Functional
Antagonist activity at rat wild type beta-1 adrenergic receptor expressed in CHO cellsAntagonist activity at rat wild type beta-1 adrenergic receptor expressed in CHO cells
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C 10.1021/jm050624l
33624 3749 29 None - 5 Rat 7.5 pKi = 7.5 Functional
Antagonist activity at rat beta-1 adrenergic receptor S190A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor S190A mutant expressed in CHO cells
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C 10.1021/jm050624l
4061 3749 29 None - 5 Rat 7.5 pKi = 7.5 Functional
Antagonist activity at rat beta-1 adrenergic receptor S190A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor S190A mutant expressed in CHO cells
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C 10.1021/jm050624l
565 3749 29 None - 5 Rat 7.5 pKi = 7.5 Functional
Antagonist activity at rat beta-1 adrenergic receptor S190A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor S190A mutant expressed in CHO cells
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C 10.1021/jm050624l
CHEMBL499 3749 29 None - 5 Rat 7.5 pKi = 7.5 Functional
Antagonist activity at rat beta-1 adrenergic receptor S190A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor S190A mutant expressed in CHO cells
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C 10.1021/jm050624l
DB00373 3749 29 None - 5 Rat 7.5 pKi = 7.5 Functional
Antagonist activity at rat beta-1 adrenergic receptor S190A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor S190A mutant expressed in CHO cells
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C 10.1021/jm050624l
165193 3126 60 None - 13 Rat 7.5 pKi = 7.5 Functional
Antagonist activity at rat beta-1 adrenergic receptor Y356F mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor Y356F mutant expressed in CHO cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm050624l
2303 3126 60 None - 13 Rat 7.5 pKi = 7.5 Functional
Antagonist activity at rat beta-1 adrenergic receptor Y356F mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor Y356F mutant expressed in CHO cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm050624l
4946 3126 60 None - 13 Rat 7.5 pKi = 7.5 Functional
Antagonist activity at rat beta-1 adrenergic receptor Y356F mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor Y356F mutant expressed in CHO cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm050624l
564 3126 60 None - 13 Rat 7.5 pKi = 7.5 Functional
Antagonist activity at rat beta-1 adrenergic receptor Y356F mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor Y356F mutant expressed in CHO cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm050624l
62882 3126 60 None - 13 Rat 7.5 pKi = 7.5 Functional
Antagonist activity at rat beta-1 adrenergic receptor Y356F mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor Y356F mutant expressed in CHO cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm050624l
63 3126 60 None - 13 Rat 7.5 pKi = 7.5 Functional
Antagonist activity at rat beta-1 adrenergic receptor Y356F mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor Y356F mutant expressed in CHO cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm050624l
66366 3126 60 None - 13 Rat 7.5 pKi = 7.5 Functional
Antagonist activity at rat beta-1 adrenergic receptor Y356F mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor Y356F mutant expressed in CHO cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm050624l
91536 3126 60 None - 13 Rat 7.5 pKi = 7.5 Functional
Antagonist activity at rat beta-1 adrenergic receptor Y356F mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor Y356F mutant expressed in CHO cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm050624l
CHEMBL27 3126 60 None - 13 Rat 7.5 pKi = 7.5 Functional
Antagonist activity at rat beta-1 adrenergic receptor Y356F mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor Y356F mutant expressed in CHO cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm050624l
CHEMBL452861 3126 60 None - 13 Rat 7.5 pKi = 7.5 Functional
Antagonist activity at rat beta-1 adrenergic receptor Y356F mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor Y356F mutant expressed in CHO cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm050624l
DB00571 3126 60 None - 13 Rat 7.5 pKi = 7.5 Functional
Antagonist activity at rat beta-1 adrenergic receptor Y356F mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor Y356F mutant expressed in CHO cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm050624l
132 1244 9 None - 0 Rat 6.5 pKi = 6.5 Functional
Antagonist activity at rat beta-1 adrenergic receptor Y356A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor Y356A mutant expressed in CHO cells
ChEMBL 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 10.1021/jm050624l
155346 1244 9 None - 0 Rat 6.5 pKi = 6.5 Functional
Antagonist activity at rat beta-1 adrenergic receptor Y356A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor Y356A mutant expressed in CHO cells
ChEMBL 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 10.1021/jm050624l
CHEMBL378501 1244 9 None - 0 Rat 6.5 pKi = 6.5 Functional
Antagonist activity at rat beta-1 adrenergic receptor Y356A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor Y356A mutant expressed in CHO cells
ChEMBL 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 10.1021/jm050624l
165193 3126 60 None - 13 Rat 7.4 pKi = 7.4 Functional
Antagonist activity at rat beta-1 adrenergic receptor S190A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor S190A mutant expressed in CHO cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm050624l
2303 3126 60 None - 13 Rat 7.4 pKi = 7.4 Functional
Antagonist activity at rat beta-1 adrenergic receptor S190A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor S190A mutant expressed in CHO cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm050624l
4946 3126 60 None - 13 Rat 7.4 pKi = 7.4 Functional
Antagonist activity at rat beta-1 adrenergic receptor S190A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor S190A mutant expressed in CHO cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm050624l
564 3126 60 None - 13 Rat 7.4 pKi = 7.4 Functional
Antagonist activity at rat beta-1 adrenergic receptor S190A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor S190A mutant expressed in CHO cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm050624l
62882 3126 60 None - 13 Rat 7.4 pKi = 7.4 Functional
Antagonist activity at rat beta-1 adrenergic receptor S190A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor S190A mutant expressed in CHO cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm050624l
63 3126 60 None - 13 Rat 7.4 pKi = 7.4 Functional
Antagonist activity at rat beta-1 adrenergic receptor S190A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor S190A mutant expressed in CHO cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm050624l
66366 3126 60 None - 13 Rat 7.4 pKi = 7.4 Functional
Antagonist activity at rat beta-1 adrenergic receptor S190A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor S190A mutant expressed in CHO cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm050624l
91536 3126 60 None - 13 Rat 7.4 pKi = 7.4 Functional
Antagonist activity at rat beta-1 adrenergic receptor S190A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor S190A mutant expressed in CHO cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm050624l
CHEMBL27 3126 60 None - 13 Rat 7.4 pKi = 7.4 Functional
Antagonist activity at rat beta-1 adrenergic receptor S190A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor S190A mutant expressed in CHO cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm050624l
CHEMBL452861 3126 60 None - 13 Rat 7.4 pKi = 7.4 Functional
Antagonist activity at rat beta-1 adrenergic receptor S190A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor S190A mutant expressed in CHO cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm050624l
DB00571 3126 60 None - 13 Rat 7.4 pKi = 7.4 Functional
Antagonist activity at rat beta-1 adrenergic receptor S190A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor S190A mutant expressed in CHO cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm050624l
1786 2474 79 None - 6 Rat 6.4 pKi = 6.4 Functional
Antagonist activity at rat wild type beta-1 adrenergic receptor expressed in CHO cellsAntagonist activity at rat wild type beta-1 adrenergic receptor expressed in CHO cells
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm050624l
4171 2474 79 None - 6 Rat 6.4 pKi = 6.4 Functional
Antagonist activity at rat wild type beta-1 adrenergic receptor expressed in CHO cellsAntagonist activity at rat wild type beta-1 adrenergic receptor expressed in CHO cells
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm050624l
553 2474 79 None - 6 Rat 6.4 pKi = 6.4 Functional
Antagonist activity at rat wild type beta-1 adrenergic receptor expressed in CHO cellsAntagonist activity at rat wild type beta-1 adrenergic receptor expressed in CHO cells
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm050624l
CHEMBL13 2474 79 None - 6 Rat 6.4 pKi = 6.4 Functional
Antagonist activity at rat wild type beta-1 adrenergic receptor expressed in CHO cellsAntagonist activity at rat wild type beta-1 adrenergic receptor expressed in CHO cells
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm050624l
DB00264 2474 79 None - 6 Rat 6.4 pKi = 6.4 Functional
Antagonist activity at rat wild type beta-1 adrenergic receptor expressed in CHO cellsAntagonist activity at rat wild type beta-1 adrenergic receptor expressed in CHO cells
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm050624l
9909993 76925 0 None - 0 Rat 7.3 pKi = 7.3 Functional
Antagonist activity at rat wild type beta-1 adrenergic receptor expressed in CHO cellsAntagonist activity at rat wild type beta-1 adrenergic receptor expressed in CHO cells
ChEMBL 419 15 2 7 2.7 CCOCCOc1ccc(OC[C@@H](O)CNCCc2ccc(OC)c(OC)c2)cc1 10.1021/jm050624l
CHEMBL208185 76925 0 None - 0 Rat 7.3 pKi = 7.3 Functional
Antagonist activity at rat wild type beta-1 adrenergic receptor expressed in CHO cellsAntagonist activity at rat wild type beta-1 adrenergic receptor expressed in CHO cells
ChEMBL 419 15 2 7 2.7 CCOCCOc1ccc(OC[C@@H](O)CNCCc2ccc(OC)c(OC)c2)cc1 10.1021/jm050624l
1786 2474 79 None - 6 Rat 5.3 pKi = 5.3 Functional
Antagonist activity at rat beta-1 adrenergic receptor Y356A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor Y356A mutant expressed in CHO cells
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm050624l
4171 2474 79 None - 6 Rat 5.3 pKi = 5.3 Functional
Antagonist activity at rat beta-1 adrenergic receptor Y356A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor Y356A mutant expressed in CHO cells
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm050624l
553 2474 79 None - 6 Rat 5.3 pKi = 5.3 Functional
Antagonist activity at rat beta-1 adrenergic receptor Y356A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor Y356A mutant expressed in CHO cells
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm050624l
CHEMBL13 2474 79 None - 6 Rat 5.3 pKi = 5.3 Functional
Antagonist activity at rat beta-1 adrenergic receptor Y356A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor Y356A mutant expressed in CHO cells
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm050624l
DB00264 2474 79 None - 6 Rat 5.3 pKi = 5.3 Functional
Antagonist activity at rat beta-1 adrenergic receptor Y356A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor Y356A mutant expressed in CHO cells
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm050624l
5311116 2293 6 None - 3 Rat 7.2 pKi = 7.2 Functional
Antagonist activity at rat beta-1 adrenergic receptor W134A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor W134A mutant expressed in CHO cells
ChEMBL 484 15 5 8 2.2 N#Cc1cc(OCCOCC2CC2)ccc1OCC(CNCCNC(=O)Nc1ccc(cc1)O)O 10.1021/jm050624l
544 2293 6 None - 3 Rat 7.2 pKi = 7.2 Functional
Antagonist activity at rat beta-1 adrenergic receptor W134A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor W134A mutant expressed in CHO cells
ChEMBL 484 15 5 8 2.2 N#Cc1cc(OCCOCC2CC2)ccc1OCC(CNCCNC(=O)Nc1ccc(cc1)O)O 10.1021/jm050624l
CHEMBL207802 2293 6 None - 3 Rat 7.2 pKi = 7.2 Functional
Antagonist activity at rat beta-1 adrenergic receptor W134A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor W134A mutant expressed in CHO cells
ChEMBL 484 15 5 8 2.2 N#Cc1cc(OCCOCC2CC2)ccc1OCC(CNCCNC(=O)Nc1ccc(cc1)O)O 10.1021/jm050624l
1786 2474 79 None - 6 Rat 6.2 pKi = 6.2 Functional
Antagonist activity at rat beta-1 adrenergic receptor W134A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor W134A mutant expressed in CHO cells
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm050624l
4171 2474 79 None - 6 Rat 6.2 pKi = 6.2 Functional
Antagonist activity at rat beta-1 adrenergic receptor W134A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor W134A mutant expressed in CHO cells
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm050624l
553 2474 79 None - 6 Rat 6.2 pKi = 6.2 Functional
Antagonist activity at rat beta-1 adrenergic receptor W134A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor W134A mutant expressed in CHO cells
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm050624l
CHEMBL13 2474 79 None - 6 Rat 6.2 pKi = 6.2 Functional
Antagonist activity at rat beta-1 adrenergic receptor W134A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor W134A mutant expressed in CHO cells
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm050624l
DB00264 2474 79 None - 6 Rat 6.2 pKi = 6.2 Functional
Antagonist activity at rat beta-1 adrenergic receptor W134A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor W134A mutant expressed in CHO cells
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm050624l
33624 3749 29 None - 5 Rat 6.2 pKi = 6.2 Functional
Antagonist activity at rat beta-1 adrenergic receptor Y356A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor Y356A mutant expressed in CHO cells
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C 10.1021/jm050624l
4061 3749 29 None - 5 Rat 6.2 pKi = 6.2 Functional
Antagonist activity at rat beta-1 adrenergic receptor Y356A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor Y356A mutant expressed in CHO cells
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C 10.1021/jm050624l
565 3749 29 None - 5 Rat 6.2 pKi = 6.2 Functional
Antagonist activity at rat beta-1 adrenergic receptor Y356A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor Y356A mutant expressed in CHO cells
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C 10.1021/jm050624l
CHEMBL499 3749 29 None - 5 Rat 6.2 pKi = 6.2 Functional
Antagonist activity at rat beta-1 adrenergic receptor Y356A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor Y356A mutant expressed in CHO cells
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C 10.1021/jm050624l
DB00373 3749 29 None - 5 Rat 6.2 pKi = 6.2 Functional
Antagonist activity at rat beta-1 adrenergic receptor Y356A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor Y356A mutant expressed in CHO cells
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C 10.1021/jm050624l
44331346 206638 0 None -120 3 Human 5.2 pKi = 5.2 Functional
Binding affinity of compound against Beta-1 adrenergic receptor was determinedBinding affinity of compound against Beta-1 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 -120 3 Human 5.2 pKi = 5.2 Functional
Binding affinity of compound against Beta-1 adrenergic receptor was determinedBinding affinity of compound against Beta-1 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
2685 875 15 None - 1 Rat 8.1 pKi = 8.1 Functional
Antagonist activity at rat beta-1 adrenergic receptor W134A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor W134A mutant expressed in CHO cells
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/jm050624l
541 875 15 None - 1 Rat 8.1 pKi = 8.1 Functional
Antagonist activity at rat beta-1 adrenergic receptor W134A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor W134A mutant expressed in CHO cells
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/jm050624l
CHEMBL280822 875 15 None - 1 Rat 8.1 pKi = 8.1 Functional
Antagonist activity at rat beta-1 adrenergic receptor W134A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor W134A mutant expressed in CHO cells
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/jm050624l
33624 3749 29 None - 5 Rat 8.1 pKi = 8.1 Functional
Antagonist activity at rat beta-1 adrenergic receptor W134A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor W134A mutant expressed in CHO cells
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C 10.1021/jm050624l
4061 3749 29 None - 5 Rat 8.1 pKi = 8.1 Functional
Antagonist activity at rat beta-1 adrenergic receptor W134A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor W134A mutant expressed in CHO cells
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C 10.1021/jm050624l
565 3749 29 None - 5 Rat 8.1 pKi = 8.1 Functional
Antagonist activity at rat beta-1 adrenergic receptor W134A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor W134A mutant expressed in CHO cells
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C 10.1021/jm050624l
CHEMBL499 3749 29 None - 5 Rat 8.1 pKi = 8.1 Functional
Antagonist activity at rat beta-1 adrenergic receptor W134A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor W134A mutant expressed in CHO cells
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C 10.1021/jm050624l
DB00373 3749 29 None - 5 Rat 8.1 pKi = 8.1 Functional
Antagonist activity at rat beta-1 adrenergic receptor W134A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor W134A mutant expressed in CHO cells
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C 10.1021/jm050624l
5311116 2293 6 None - 3 Rat 8.1 pKi = 8.1 Functional
Antagonist activity at rat wild type beta-1 adrenergic receptor expressed in CHO cellsAntagonist activity at rat wild type beta-1 adrenergic receptor expressed in CHO cells
ChEMBL 484 15 5 8 2.2 N#Cc1cc(OCCOCC2CC2)ccc1OCC(CNCCNC(=O)Nc1ccc(cc1)O)O 10.1021/jm050624l
544 2293 6 None - 3 Rat 8.1 pKi = 8.1 Functional
Antagonist activity at rat wild type beta-1 adrenergic receptor expressed in CHO cellsAntagonist activity at rat wild type beta-1 adrenergic receptor expressed in CHO cells
ChEMBL 484 15 5 8 2.2 N#Cc1cc(OCCOCC2CC2)ccc1OCC(CNCCNC(=O)Nc1ccc(cc1)O)O 10.1021/jm050624l
CHEMBL207802 2293 6 None - 3 Rat 8.1 pKi = 8.1 Functional
Antagonist activity at rat wild type beta-1 adrenergic receptor expressed in CHO cellsAntagonist activity at rat wild type beta-1 adrenergic receptor expressed in CHO cells
ChEMBL 484 15 5 8 2.2 N#Cc1cc(OCCOCC2CC2)ccc1OCC(CNCCNC(=O)Nc1ccc(cc1)O)O 10.1021/jm050624l
9909993 76925 0 None - 0 Rat 7.1 pKi = 7.1 Functional
Antagonist activity at rat beta-1 adrenergic receptor W134A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor W134A mutant expressed in CHO cells
ChEMBL 419 15 2 7 2.7 CCOCCOc1ccc(OC[C@@H](O)CNCCc2ccc(OC)c(OC)c2)cc1 10.1021/jm050624l
CHEMBL208185 76925 0 None - 0 Rat 7.1 pKi = 7.1 Functional
Antagonist activity at rat beta-1 adrenergic receptor W134A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor W134A mutant expressed in CHO cells
ChEMBL 419 15 2 7 2.7 CCOCCOc1ccc(OC[C@@H](O)CNCCc2ccc(OC)c(OC)c2)cc1 10.1021/jm050624l
5311116 2293 6 None - 3 Rat 7.1 pKi = 7.1 Functional
Antagonist activity at rat beta-1 adrenergic receptor Y356F mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor Y356F mutant expressed in CHO cells
ChEMBL 484 15 5 8 2.2 N#Cc1cc(OCCOCC2CC2)ccc1OCC(CNCCNC(=O)Nc1ccc(cc1)O)O 10.1021/jm050624l
544 2293 6 None - 3 Rat 7.1 pKi = 7.1 Functional
Antagonist activity at rat beta-1 adrenergic receptor Y356F mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor Y356F mutant expressed in CHO cells
ChEMBL 484 15 5 8 2.2 N#Cc1cc(OCCOCC2CC2)ccc1OCC(CNCCNC(=O)Nc1ccc(cc1)O)O 10.1021/jm050624l
CHEMBL207802 2293 6 None - 3 Rat 7.1 pKi = 7.1 Functional
Antagonist activity at rat beta-1 adrenergic receptor Y356F mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor Y356F mutant expressed in CHO cells
ChEMBL 484 15 5 8 2.2 N#Cc1cc(OCCOCC2CC2)ccc1OCC(CNCCNC(=O)Nc1ccc(cc1)O)O 10.1021/jm050624l
2685 875 15 None - 1 Rat 6.1 pKi = 6.1 Functional
Antagonist activity at rat beta-1 adrenergic receptor S190A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor S190A mutant expressed in CHO cells
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/jm050624l
541 875 15 None - 1 Rat 6.1 pKi = 6.1 Functional
Antagonist activity at rat beta-1 adrenergic receptor S190A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor S190A mutant expressed in CHO cells
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/jm050624l
CHEMBL280822 875 15 None - 1 Rat 6.1 pKi = 6.1 Functional
Antagonist activity at rat beta-1 adrenergic receptor S190A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor S190A mutant expressed in CHO cells
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/jm050624l
9909993 76925 0 None - 0 Rat 6.1 pKi = 6.1 Functional
Antagonist activity at rat beta-1 adrenergic receptor Y356A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor Y356A mutant expressed in CHO cells
ChEMBL 419 15 2 7 2.7 CCOCCOc1ccc(OC[C@@H](O)CNCCc2ccc(OC)c(OC)c2)cc1 10.1021/jm050624l
CHEMBL208185 76925 0 None - 0 Rat 6.1 pKi = 6.1 Functional
Antagonist activity at rat beta-1 adrenergic receptor Y356A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor Y356A mutant expressed in CHO cells
ChEMBL 419 15 2 7 2.7 CCOCCOc1ccc(OC[C@@H](O)CNCCc2ccc(OC)c(OC)c2)cc1 10.1021/jm050624l
5311116 2293 6 None - 3 Rat 4.1 pKi = 4.1 Functional
Antagonist activity at rat beta-1 adrenergic receptor Y356A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor Y356A mutant expressed in CHO cells
ChEMBL 484 15 5 8 2.2 N#Cc1cc(OCCOCC2CC2)ccc1OCC(CNCCNC(=O)Nc1ccc(cc1)O)O 10.1021/jm050624l
544 2293 6 None - 3 Rat 4.1 pKi = 4.1 Functional
Antagonist activity at rat beta-1 adrenergic receptor Y356A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor Y356A mutant expressed in CHO cells
ChEMBL 484 15 5 8 2.2 N#Cc1cc(OCCOCC2CC2)ccc1OCC(CNCCNC(=O)Nc1ccc(cc1)O)O 10.1021/jm050624l
CHEMBL207802 2293 6 None - 3 Rat 4.1 pKi = 4.1 Functional
Antagonist activity at rat beta-1 adrenergic receptor Y356A mutant expressed in CHO cellsAntagonist activity at rat beta-1 adrenergic receptor Y356A mutant expressed in CHO cells
ChEMBL 484 15 5 8 2.2 N#Cc1cc(OCCOCC2CC2)ccc1OCC(CNCCNC(=O)Nc1ccc(cc1)O)O 10.1021/jm050624l
41835 215976 0 None 54 2 Human 7.8 pA2 = 7.8 Functional
NoneNone
Drug Central 372 8 4 6 1.9 CC(CCC1=CC2=C(OCO2)C=C1)NCC(O)C1=CC(C(N)=O)=C(O)C=C1 None
36811 1421 34 None -3 7 Human 8.3 pEC50 = 8.3 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 8.3 pEC50 = 8.3 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 8.3 pEC50 = 8.3 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 8.3 pEC50 = 8.3 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 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 301 7 4 4 3.0 CC(CCc1ccc(cc1)O)NCCc1ccc(c(c1)O)O None
10184665 3916 48 None -44 3 Human 8.2 pEC50 = 8.2 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 8.2 pEC50 = 8.2 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 8.2 pEC50 = 8.2 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 8.2 pEC50 = 8.2 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 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O None
65772 215997 0 None -1 3 Guinea pig 8.2 pEC50 = 8.2 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
443372 10123 23 None -10 8 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta1 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta1 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
Drug Central 211 4 4 4 1.1 CC(C)NC[C@H](O)c1ccc(O)c(O)c1 None
CHEMBL1160723 10123 23 None -10 8 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta1 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta1 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
Drug Central 211 4 4 4 1.1 CC(C)NC[C@H](O)c1ccc(O)c(O)c1 None
CHEMBL2062275 10123 23 None -10 8 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human beta1 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta1 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
Drug Central 211 4 4 4 1.1 CC(C)NC[C@H](O)c1ccc(O)c(O)c1 None
1499 2052 43 None -64 36 Human 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 -64 36 Human 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 -64 36 Human 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 -64 36 Human 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 -64 36 Human 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
12065 621 21 None -6 2 Human 9.2 pEC50 = 9.2 Functional
Determined in an intracellular cAMP accumulation assay in CHO-K1 cells expressing hβ1-ARDetermined in an intracellular cAMP accumulation assay in CHO-K1 cells expressing hβ1-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 9.2 pEC50 = 9.2 Functional
Determined in an intracellular cAMP accumulation assay in CHO-K1 cells expressing hβ1-ARDetermined in an intracellular cAMP accumulation assay in CHO-K1 cells expressing hβ1-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 9.2 pEC50 = 9.2 Functional
Determined in an intracellular cAMP accumulation assay in CHO-K1 cells expressing hβ1-ARDetermined in an intracellular cAMP accumulation assay in CHO-K1 cells expressing hβ1-AR
Guide to Pharmacology 370 6 4 5 2.7 Cc1ccccc1CC(C)(C)NCC(c1c2c(c(cc1)O)NC(=O)CO2)O 19875286
9512 3566 35 None -1000 3 Human 5.4 pEC50 = 5.4 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 -1000 3 Human 5.4 pEC50 = 5.4 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 -1000 3 Human 5.4 pEC50 = 5.4 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 -1000 3 Human 5.4 pEC50 = 5.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 410 9 4 4 4.4 Clc1cccc(c1)[C@H](CNCCNc1cccc(c1)c1cccc(c1)C(=O)O)O 16640337
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
176 394 63 None -10 34 Human 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
2157 394 63 None -10 34 Human 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
2566 394 63 None -10 34 Human 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
CHEMBL633 394 63 None -10 34 Human 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
DB01118 394 63 None -10 34 Human 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
1499 2052 43 None -269 36 Rat 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 -269 36 Rat 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 -269 36 Rat 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 -269 36 Rat 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 -269 36 Rat 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
319 1292 39 None -43 6 Human 8.2 pIC50 = 8.2 Functional
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 -43 6 Human 8.2 pIC50 = 8.2 Functional
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 -43 6 Human 8.2 pIC50 = 8.2 Functional
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 -43 6 Human 8.2 pIC50 = 8.2 Functional
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 -43 6 Human 8.2 pIC50 = 8.2 Functional
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 -43 6 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 None




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
9906822 161476 0 None - 0 Human 9.9 pEC50 = 9.9 Binding
Agonist activity at Homo sapiens (human) beta1 adrenoreceptorAgonist activity at Homo sapiens (human) beta1 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 - 0 Human 9.9 pEC50 = 9.9 Binding
Agonist activity at Homo sapiens (human) beta1 adrenoreceptorAgonist activity at Homo sapiens (human) beta1 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
44396736 66519 0 None - 0 Human 8.9 pEC50 = 8.9 Binding
Agonist activity at Homo sapiens (human) beta1 adrenoreceptorAgonist activity at Homo sapiens (human) beta1 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 - 0 Human 8.9 pEC50 = 8.9 Binding
Agonist activity at Homo sapiens (human) beta1 adrenoreceptorAgonist activity at Homo sapiens (human) beta1 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
44396715 67097 0 None - 0 Human 8.9 pEC50 = 8.9 Binding
Agonist activity at Homo sapiens (human) beta1 adrenoreceptorAgonist activity at Homo sapiens (human) beta1 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 - 0 Human 8.9 pEC50 = 8.9 Binding
Agonist activity at Homo sapiens (human) beta1 adrenoreceptorAgonist activity at Homo sapiens (human) beta1 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
165193 3126 60 None -2 43 Human 8.7 pEC50 = 8.7 Binding
Displacement of [125I]cyanopindolol from human recombinant adrenergic beta-1 receptor expressed in Rex16 cellsDisplacement of [125I]cyanopindolol from human recombinant adrenergic beta-1 receptor expressed in Rex16 cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/np058114h
2303 3126 60 None -2 43 Human 8.7 pEC50 = 8.7 Binding
Displacement of [125I]cyanopindolol from human recombinant adrenergic beta-1 receptor expressed in Rex16 cellsDisplacement of [125I]cyanopindolol from human recombinant adrenergic beta-1 receptor expressed in Rex16 cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/np058114h
4946 3126 60 None -2 43 Human 8.7 pEC50 = 8.7 Binding
Displacement of [125I]cyanopindolol from human recombinant adrenergic beta-1 receptor expressed in Rex16 cellsDisplacement of [125I]cyanopindolol from human recombinant adrenergic beta-1 receptor expressed in Rex16 cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/np058114h
564 3126 60 None -2 43 Human 8.7 pEC50 = 8.7 Binding
Displacement of [125I]cyanopindolol from human recombinant adrenergic beta-1 receptor expressed in Rex16 cellsDisplacement of [125I]cyanopindolol from human recombinant adrenergic beta-1 receptor expressed in Rex16 cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/np058114h
62882 3126 60 None -2 43 Human 8.7 pEC50 = 8.7 Binding
Displacement of [125I]cyanopindolol from human recombinant adrenergic beta-1 receptor expressed in Rex16 cellsDisplacement of [125I]cyanopindolol from human recombinant adrenergic beta-1 receptor expressed in Rex16 cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/np058114h
63 3126 60 None -2 43 Human 8.7 pEC50 = 8.7 Binding
Displacement of [125I]cyanopindolol from human recombinant adrenergic beta-1 receptor expressed in Rex16 cellsDisplacement of [125I]cyanopindolol from human recombinant adrenergic beta-1 receptor expressed in Rex16 cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/np058114h
66366 3126 60 None -2 43 Human 8.7 pEC50 = 8.7 Binding
Displacement of [125I]cyanopindolol from human recombinant adrenergic beta-1 receptor expressed in Rex16 cellsDisplacement of [125I]cyanopindolol from human recombinant adrenergic beta-1 receptor expressed in Rex16 cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/np058114h
91536 3126 60 None -2 43 Human 8.7 pEC50 = 8.7 Binding
Displacement of [125I]cyanopindolol from human recombinant adrenergic beta-1 receptor expressed in Rex16 cellsDisplacement of [125I]cyanopindolol from human recombinant adrenergic beta-1 receptor expressed in Rex16 cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/np058114h
CHEMBL27 3126 60 None -2 43 Human 8.7 pEC50 = 8.7 Binding
Displacement of [125I]cyanopindolol from human recombinant adrenergic beta-1 receptor expressed in Rex16 cellsDisplacement of [125I]cyanopindolol from human recombinant adrenergic beta-1 receptor expressed in Rex16 cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/np058114h
CHEMBL452861 3126 60 None -2 43 Human 8.7 pEC50 = 8.7 Binding
Displacement of [125I]cyanopindolol from human recombinant adrenergic beta-1 receptor expressed in Rex16 cellsDisplacement of [125I]cyanopindolol from human recombinant adrenergic beta-1 receptor expressed in Rex16 cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/np058114h
DB00571 3126 60 None -2 43 Human 8.7 pEC50 = 8.7 Binding
Displacement of [125I]cyanopindolol from human recombinant adrenergic beta-1 receptor expressed in Rex16 cellsDisplacement of [125I]cyanopindolol from human recombinant adrenergic beta-1 receptor expressed in Rex16 cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/np058114h
9927453 96226 0 None - 0 Human 8.7 pEC50 = 8.7 Binding
Agonist activity at Homo sapiens (human) beta1 adrenoreceptorAgonist activity at Homo sapiens (human) beta1 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 - 0 Human 8.7 pEC50 = 8.7 Binding
Agonist activity at Homo sapiens (human) beta1 adrenoreceptorAgonist activity at Homo sapiens (human) beta1 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
44392457 165393 0 None - 0 Human 8.0 pEC50 = 8 Binding
Agonist activity at Homo sapiens (human) beta1 adrenoreceptorAgonist activity at Homo sapiens (human) beta1 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 - 0 Human 8.0 pEC50 = 8 Binding
Agonist activity at Homo sapiens (human) beta1 adrenoreceptorAgonist activity at Homo sapiens (human) beta1 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
44328703 10118 0 None - 2 Human 6.0 pEC50 = 6 Binding
Agonist activity at beta1-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 GRK2 and coelenterazine 400a by BRET assayAgonist activity at beta1-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 GRK2 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 - 2 Human 6.0 pEC50 = 6 Binding
Agonist activity at beta1-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 GRK2 and coelenterazine 400a by BRET assayAgonist activity at beta1-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 GRK2 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
10347461 105786 0 None - 0 Human 6.0 pEC50 = 6 Binding
Agonist activity at human beta1 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta1 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 - 0 Human 6.0 pEC50 = 6 Binding
Agonist activity at human beta1 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta1 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 - 0 Human 6.0 pEC50 = 6 Binding
Agonist activity at human beta1 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta1 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
146025803 175593 0 None - 2 Human 5.0 pEC50 = 5 Binding
Agonist activity at beta1-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 beta1-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 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 - 2 Human 5.0 pEC50 = 5 Binding
Agonist activity at beta1-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 beta1-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 467 14 4 7 3.7 COc1cc(CCNC[C@H](O)COc2ccc(O)c(O)c2)ccc1OCCCc1ccccc1 10.1021/acs.jmedchem.9b00349
76333795 84877 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at Homo sapiens (human) beta1 adrenoreceptorAgonist activity at Homo sapiens (human) beta1 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 - 0 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at Homo sapiens (human) beta1 adrenoreceptorAgonist activity at Homo sapiens (human) beta1 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
10482960 105895 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human beta1 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta1 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 - 0 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human beta1 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta1 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 - 0 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human beta1 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta1 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
567 715 10 None -11 5 Human 5.8 pEC50 = 5.8 Binding
Agonist activity at Homo sapiens (human) beta1 adrenoreceptorAgonist activity at Homo sapiens (human) beta1 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 -11 5 Human 5.8 pEC50 = 5.8 Binding
Agonist activity at Homo sapiens (human) beta1 adrenoreceptorAgonist activity at Homo sapiens (human) beta1 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 -11 5 Human 5.8 pEC50 = 5.8 Binding
Agonist activity at Homo sapiens (human) beta1 adrenoreceptorAgonist activity at Homo sapiens (human) beta1 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
5581 101175 10 None -3 7 Guinea pig 6.8 pEC50 = 6.8 Binding
Inhibitory activity against Beta-1 adrenergic receptor in guinea pig atria after treatment with the compoundInhibitory activity against Beta-1 adrenergic receptor in guinea pig atria 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 -3 7 Guinea pig 6.8 pEC50 = 6.8 Binding
Inhibitory activity against Beta-1 adrenergic receptor in guinea pig atria after treatment with the compoundInhibitory activity against Beta-1 adrenergic receptor in guinea pig atria after treatment with the compound
ChEMBL 345 5 3 6 2.6 COc1cc(CC2NCCc3cc(O)c(O)cc32)cc(OC)c1OC 10.1021/jm00081a007
11432806 65851 0 None -16 3 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at Homo sapiens (human) beta1 adrenoreceptorAgonist activity at Homo sapiens (human) beta1 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 -16 3 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at Homo sapiens (human) beta1 adrenoreceptorAgonist activity at Homo sapiens (human) beta1 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
44396568 66934 0 None -28 3 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at Homo sapiens (human) beta1 adrenoreceptorAgonist activity at Homo sapiens (human) beta1 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 -28 3 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at Homo sapiens (human) beta1 adrenoreceptorAgonist activity at Homo sapiens (human) beta1 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
76315638 84878 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at Homo sapiens (human) beta1 adrenoreceptorAgonist activity at Homo sapiens (human) beta1 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 - 0 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at Homo sapiens (human) beta1 adrenoreceptorAgonist activity at Homo sapiens (human) beta1 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
2419 3394 80 None -162 6 Human 6.7 pEC50 = 6.7 Binding
Agonist activity at beta1-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 GRK5 and coelenterazine 400a by BRET assayAgonist activity at beta1-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 GRK5 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 -162 6 Human 6.7 pEC50 = 6.7 Binding
Agonist activity at beta1-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 GRK5 and coelenterazine 400a by BRET assayAgonist activity at beta1-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 GRK5 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 -162 6 Human 6.7 pEC50 = 6.7 Binding
Agonist activity at beta1-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 GRK5 and coelenterazine 400a by BRET assayAgonist activity at beta1-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 GRK5 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 -162 6 Human 6.7 pEC50 = 6.7 Binding
Agonist activity at beta1-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 GRK5 and coelenterazine 400a by BRET assayAgonist activity at beta1-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 GRK5 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 -162 6 Human 6.7 pEC50 = 6.7 Binding
Agonist activity at beta1-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 GRK5 and coelenterazine 400a by BRET assayAgonist activity at beta1-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 GRK5 and coelenterazine 400a by BRET assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/acs.jmedchem.9b00349
127046950 139502 0 None - 6 Human 5.7 pEC50 = 5.7 Binding
Agonist activity at beta1-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 beta1-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 - 6 Human 5.7 pEC50 = 5.7 Binding
Agonist activity at beta1-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 beta1-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
11318107 105894 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Agonist activity at human beta1 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta1 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 - 0 Human 5.7 pEC50 = 5.7 Binding
Agonist activity at human beta1 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta1 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 - 0 Human 5.7 pEC50 = 5.7 Binding
Agonist activity at human beta1 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta1 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
11318358 105938 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Agonist activity at human beta1 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta1 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 - 0 Human 5.7 pEC50 = 5.7 Binding
Agonist activity at human beta1 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta1 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 - 0 Human 5.7 pEC50 = 5.7 Binding
Agonist activity at human beta1 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta1 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
10393774 120218 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
In vitro activity to increase cAMP levels in Chinese hamster ovary (CHO) cells expressing the cloned human beta 1 Adrenergic receptorIn vitro activity to increase cAMP levels in Chinese hamster ovary (CHO) cells expressing the cloned human beta 1 Adrenergic receptor
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 - 0 Human 5.7 pEC50 = 5.7 Binding
In vitro activity to increase cAMP levels in Chinese hamster ovary (CHO) cells expressing the cloned human beta 1 Adrenergic receptorIn vitro activity to increase cAMP levels in Chinese hamster ovary (CHO) cells expressing the cloned human beta 1 Adrenergic receptor
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
44396532 66408 0 None -3 3 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at Homo sapiens (human) beta1 adrenoreceptorAgonist activity at Homo sapiens (human) beta1 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 -3 3 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at Homo sapiens (human) beta1 adrenoreceptorAgonist activity at Homo sapiens (human) beta1 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
164612037 184785 0 None -1 20 Human 4.7 pEC50 = 4.7 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]CGP12177 from human beta-1 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 4.7 pEC50 = 4.7 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]CGP12177 from human beta-1 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
76315640 84880 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at Homo sapiens (human) beta1 adrenoreceptorAgonist activity at Homo sapiens (human) beta1 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 - 0 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at Homo sapiens (human) beta1 adrenoreceptorAgonist activity at Homo sapiens (human) beta1 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
13720716 62709 0 None -1 2 Guinea pig 6.6 pEC50 = 6.6 Binding
Inhibitory activity against Beta-1 adrenergic receptor in guinea pig atriaInhibitory activity against Beta-1 adrenergic receptor in guinea pig atria
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 6.6 pEC50 = 6.6 Binding
Inhibitory activity against Beta-1 adrenergic receptor in guinea pig atriaInhibitory activity against Beta-1 adrenergic receptor in guinea pig atria
ChEMBL 363 5 3 6 2.7 COc1cc(C[C@@H]2NCCc3cc(O)c(O)c(F)c32)cc(OC)c1OC 10.1021/jm00081a007
443372 10123 23 None - 3 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at beta1-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 beta1-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 - 3 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at beta1-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 beta1-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 - 3 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at beta1-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 beta1-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
10370605 105939 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at human beta1 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta1 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 - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at human beta1 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta1 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 - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at human beta1 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta1 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
146025803 175593 0 None - 2 Human 5.6 pEC50 = 5.6 Binding
Agonist activity at beta1-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 GRK2 and coelenterazine 400a by BRET assayAgonist activity at beta1-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 GRK2 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 - 2 Human 5.6 pEC50 = 5.6 Binding
Agonist activity at beta1-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 GRK2 and coelenterazine 400a by BRET assayAgonist activity at beta1-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 GRK2 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
146025803 175593 0 None - 2 Human 5.6 pEC50 = 5.6 Binding
Agonist activity at beta1-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 beta1-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 - 2 Human 5.6 pEC50 = 5.6 Binding
Agonist activity at beta1-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 beta1-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 5.6 pEC50 = 5.6 Binding
Inhibitory activity against Beta-1 adrenergic receptor in guinea pig atria after treatment with the compoundInhibitory activity against Beta-1 adrenergic receptor in guinea pig atria 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 5.6 pEC50 = 5.6 Binding
Inhibitory activity against Beta-1 adrenergic receptor in guinea pig atria after treatment with the compoundInhibitory activity against Beta-1 adrenergic receptor in guinea pig atria 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
15133334 118067 0 None - 0 Guinea pig 5.5 pEC50 = 5.5 Binding
Inhibitory activity against Beta-1 adrenergic receptor in guinea pig atria after treatment with the compoundInhibitory activity against Beta-1 adrenergic receptor in guinea pig atria 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 5.5 pEC50 = 5.5 Binding
Inhibitory activity against Beta-1 adrenergic receptor in guinea pig atria after treatment with the compoundInhibitory activity against Beta-1 adrenergic receptor in guinea pig atria 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
44583033 184938 0 None - 0 Human 8.5 pEC50 = 8.5 Binding
Binding affinity to beta-1 adrenoceptorBinding affinity to beta-1 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 8.5 pEC50 = 8.5 Binding
Binding affinity to beta-1 adrenoceptorBinding affinity to beta-1 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
44396779 66711 0 None - 0 Human 8.5 pEC50 = 8.5 Binding
Agonist activity at Homo sapiens (human) beta1 adrenoreceptorAgonist activity at Homo sapiens (human) beta1 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 - 0 Human 8.5 pEC50 = 8.5 Binding
Agonist activity at Homo sapiens (human) beta1 adrenoreceptorAgonist activity at Homo sapiens (human) beta1 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
146025802 169000 0 None - 2 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at beta1-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 beta1-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 - 2 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at beta1-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 beta1-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
44328703 10118 0 None - 2 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at beta1-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 GRK5 and coelenterazine 400a by BRET assayAgonist activity at beta1-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 GRK5 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 - 2 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at beta1-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 GRK5 and coelenterazine 400a by BRET assayAgonist activity at beta1-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 GRK5 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
146025802 169000 0 None - 2 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at beta1-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 beta1-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 349 10 4 7 1.5 COc1ccccc1OCCNC[C@H](O)COc1ccc(O)c(O)c1 10.1021/acs.jmedchem.9b00349
CHEMBL4435895 169000 0 None - 2 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at beta1-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 beta1-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 349 10 4 7 1.5 COc1ccccc1OCCNC[C@H](O)COc1ccc(O)c(O)c1 10.1021/acs.jmedchem.9b00349
3931 2208 42 None -3 2 Human 6.5 pEC50 = 6.5 Binding
In vitro activity to increase cAMP levels in Chinese hamster ovary (CHO) cells expressing the cloned human beta 1 Adrenergic receptorIn vitro activity to increase cAMP levels in Chinese hamster ovary (CHO) cells expressing the cloned human beta 1 Adrenergic receptor
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 6.5 pEC50 = 6.5 Binding
In vitro activity to increase cAMP levels in Chinese hamster ovary (CHO) cells expressing the cloned human beta 1 Adrenergic receptorIn vitro activity to increase cAMP levels in Chinese hamster ovary (CHO) cells expressing the cloned human beta 1 Adrenergic receptor
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 6.5 pEC50 = 6.5 Binding
In vitro activity to increase cAMP levels in Chinese hamster ovary (CHO) cells expressing the cloned human beta 1 Adrenergic receptorIn vitro activity to increase cAMP levels in Chinese hamster ovary (CHO) cells expressing the cloned human beta 1 Adrenergic receptor
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
44392558 64909 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at Homo sapiens (human) beta1 adrenoreceptorAgonist activity at Homo sapiens (human) beta1 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 - 0 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at Homo sapiens (human) beta1 adrenoreceptorAgonist activity at Homo sapiens (human) beta1 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
11962616 219 7 None - 0 Human 7.4 pEC50 = 7.4 Binding
Inhibition of 3H]CGP12177 binding to human beta1 adrenoceptor expressed in sf9 cell membranes incubated for 60 mins by scintillation counting methodInhibition of 3H]CGP12177 binding to human beta1 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 7.4 pEC50 = 7.4 Binding
Inhibition of 3H]CGP12177 binding to human beta1 adrenoceptor expressed in sf9 cell membranes incubated for 60 mins by scintillation counting methodInhibition of 3H]CGP12177 binding to human beta1 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 7.4 pEC50 = 7.4 Binding
Inhibition of 3H]CGP12177 binding to human beta1 adrenoceptor expressed in sf9 cell membranes incubated for 60 mins by scintillation counting methodInhibition of 3H]CGP12177 binding to human beta1 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 7.4 pEC50 = 7.4 Binding
Inhibition of 3H]CGP12177 binding to human beta1 adrenoceptor expressed in sf9 cell membranes incubated for 60 mins by scintillation counting methodInhibition of 3H]CGP12177 binding to human beta1 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
127045855 139121 0 None - 6 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at beta1-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 beta1-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 - 6 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at beta1-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 beta1-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
3083544 462 46 None -8 5 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human beta1 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta1 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 -8 5 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human beta1 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta1 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 -8 5 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human beta1 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta1 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 -8 5 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human beta1 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta1 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 -8 5 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human beta1 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta1 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
146025802 169000 0 None - 2 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at beta1-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 GRK2 and coelenterazine 400a by BRET assayAgonist activity at beta1-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 GRK2 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 - 2 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at beta1-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 GRK2 and coelenterazine 400a by BRET assayAgonist activity at beta1-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 GRK2 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
146025802 169000 0 None - 2 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at beta1-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 GRK5 and coelenterazine 400a by BRET assayAgonist activity at beta1-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 GRK5 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 - 2 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at beta1-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 GRK5 and coelenterazine 400a by BRET assayAgonist activity at beta1-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 GRK5 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
10184665 3916 48 None - 0 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at human beta1 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta1 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 - 0 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at human beta1 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta1 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 - 0 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at human beta1 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta1 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 - 0 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at human beta1 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta1 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 - 0 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at human beta1 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta1 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
9917962 167382 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Binding affinity towards human Beta-1 adrenergic receptorBinding affinity towards human Beta-1 adrenergic receptor
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 7.4 pEC50 = 7.4 Binding
Binding affinity towards human Beta-1 adrenergic receptorBinding affinity towards human Beta-1 adrenergic receptor
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
443372 10123 23 None - 3 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at beta1-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 GRK5 and coelenterazine 400a by BRET assayAgonist activity at beta1-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 GRK5 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 - 3 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at beta1-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 GRK5 and coelenterazine 400a by BRET assayAgonist activity at beta1-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 GRK5 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 - 3 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at beta1-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 GRK5 and coelenterazine 400a by BRET assayAgonist activity at beta1-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 GRK5 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
76322965 84881 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at Homo sapiens (human) beta1 adrenoreceptorAgonist activity at Homo sapiens (human) beta1 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 - 0 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at Homo sapiens (human) beta1 adrenoreceptorAgonist activity at Homo sapiens (human) beta1 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
11270071 98520 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at Homo sapiens (human) beta1 adrenoreceptorAgonist activity at Homo sapiens (human) beta1 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 - 0 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at Homo sapiens (human) beta1 adrenoreceptorAgonist activity at Homo sapiens (human) beta1 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
9803765 99173 0 None - 0 Human 4.3 pEC50 = 4.3 Binding
In vitro activity to increase cAMP levels in Chinese hamster ovary (CHO) cells expressing the cloned human beta 1 Adrenergic receptorIn vitro activity to increase cAMP levels in Chinese hamster ovary (CHO) cells expressing the cloned human beta 1 Adrenergic receptor
ChEMBL 449 8 5 7 1.8 CS(=O)(=O)Nc1cc([C@@H](O)CNC2CCN(c3ccc(C(=O)O)cc3)CC2)ccc1O 10.1021/jm000544b
CHEMBL284311 99173 0 None - 0 Human 4.3 pEC50 = 4.3 Binding
In vitro activity to increase cAMP levels in Chinese hamster ovary (CHO) cells expressing the cloned human beta 1 Adrenergic receptorIn vitro activity to increase cAMP levels in Chinese hamster ovary (CHO) cells expressing the cloned human beta 1 Adrenergic receptor
ChEMBL 449 8 5 7 1.8 CS(=O)(=O)Nc1cc([C@@H](O)CNC2CCN(c3ccc(C(=O)O)cc3)CC2)ccc1O 10.1021/jm000544b
168290235 192356 0 None -5 20 Human 4.3 pEC50 = 4.3 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]CGP12177 from human beta-1 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 -5 20 Human 4.3 pEC50 = 4.3 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]CGP12177 from human beta-1 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 -5 20 Human 4.3 pEC50 = 4.3 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]CGP12177 from human beta-1 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
44396531 66486 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Agonist activity at Homo sapiens (human) beta1 adrenoreceptorAgonist activity at Homo sapiens (human) beta1 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 - 0 Human 8.3 pEC50 = 8.3 Binding
Agonist activity at Homo sapiens (human) beta1 adrenoreceptorAgonist activity at Homo sapiens (human) beta1 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 - 3 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at beta1-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 GRK2 and coelenterazine 400a by BRET assayAgonist activity at beta1-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 GRK2 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 - 3 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at beta1-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 GRK2 and coelenterazine 400a by BRET assayAgonist activity at beta1-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 GRK2 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 - 3 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at beta1-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 GRK2 and coelenterazine 400a by BRET assayAgonist activity at beta1-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 GRK2 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
127046950 139502 0 None - 6 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at beta1-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 GRK5 and coelenterazine 400a by BRET assayAgonist activity at beta1-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 GRK5 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 - 6 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at beta1-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 GRK5 and coelenterazine 400a by BRET assayAgonist activity at beta1-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 GRK5 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
10053159 105787 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at human beta1 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta1 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 - 0 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at human beta1 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta1 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 - 0 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at human beta1 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta1 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
10076176 105941 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at human beta1 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta1 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 - 0 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at human beta1 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta1 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 - 0 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at human beta1 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta1 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
10339796 121154 0 None - 0 Guinea pig 6.3 pEC50 = 6.3 Binding
Inhibitory activity against Beta-1 adrenergic receptor in guinea pig atria after treatment with the compoundInhibitory activity against Beta-1 adrenergic receptor in guinea pig atria 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 6.3 pEC50 = 6.3 Binding
Inhibitory activity against Beta-1 adrenergic receptor in guinea pig atria after treatment with the compoundInhibitory activity against Beta-1 adrenergic receptor in guinea pig atria 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
2419 3394 80 None -162 6 Human 5.3 pEC50 = 5.3 Binding
Agonist activity at beta1-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 beta1-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 -162 6 Human 5.3 pEC50 = 5.3 Binding
Agonist activity at beta1-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 beta1-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 -162 6 Human 5.3 pEC50 = 5.3 Binding
Agonist activity at beta1-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 beta1-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 -162 6 Human 5.3 pEC50 = 5.3 Binding
Agonist activity at beta1-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 beta1-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 -162 6 Human 5.3 pEC50 = 5.3 Binding
Agonist activity at beta1-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 beta1-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
127045855 139121 0 None - 6 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at beta1-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 GRK5 and coelenterazine 400a by BRET assayAgonist activity at beta1-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 GRK5 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 - 6 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at beta1-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 GRK5 and coelenterazine 400a by BRET assayAgonist activity at beta1-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 GRK5 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 - 3 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at beta1-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 beta1-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 - 3 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at beta1-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 beta1-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 - 3 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at beta1-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 beta1-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
44396513 66375 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Agonist activity at Homo sapiens (human) beta1 adrenoreceptorAgonist activity at Homo sapiens (human) beta1 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 - 0 Human 8.2 pEC50 = 8.2 Binding
Agonist activity at Homo sapiens (human) beta1 adrenoreceptorAgonist activity at Homo sapiens (human) beta1 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
6916441 98855 1 None - 0 Human 8.2 pEC50 = 8.2 Binding
Agonist activity at Homo sapiens (human) beta1 adrenoreceptorAgonist activity at Homo sapiens (human) beta1 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 - 0 Human 8.2 pEC50 = 8.2 Binding
Agonist activity at Homo sapiens (human) beta1 adrenoreceptorAgonist activity at Homo sapiens (human) beta1 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
44396577 66603 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Agonist activity at Homo sapiens (human) beta1 adrenoreceptorAgonist activity at Homo sapiens (human) beta1 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 - 0 Human 8.2 pEC50 = 8.2 Binding
Agonist activity at Homo sapiens (human) beta1 adrenoreceptorAgonist activity at Homo sapiens (human) beta1 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
44396596 122771 0 None -3 3 Human 8.2 pEC50 = 8.2 Binding
Agonist activity at Homo sapiens (human) beta1 adrenoreceptorAgonist activity at Homo sapiens (human) beta1 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 -3 3 Human 8.2 pEC50 = 8.2 Binding
Agonist activity at Homo sapiens (human) beta1 adrenoreceptorAgonist activity at Homo sapiens (human) beta1 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
76319327 84888 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Agonist activity at Homo sapiens (human) beta1 adrenoreceptorAgonist activity at Homo sapiens (human) beta1 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 - 0 Human 8.2 pEC50 = 8.2 Binding
Agonist activity at Homo sapiens (human) beta1 adrenoreceptorAgonist activity at Homo sapiens (human) beta1 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
13720717 77483 0 None -3 2 Guinea pig 5.2 pEC50 = 5.2 Binding
Inhibitory activity against Beta-1 adrenergic receptor in guinea pig atriaInhibitory activity against Beta-1 adrenergic receptor in guinea pig atria
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 5.2 pEC50 = 5.2 Binding
Inhibitory activity against Beta-1 adrenergic receptor in guinea pig atriaInhibitory activity against Beta-1 adrenergic receptor in guinea pig atria
ChEMBL 363 5 3 6 2.7 COc1cc(C[C@H]2NCCc3cc(O)c(O)c(F)c32)cc(OC)c1OC 10.1021/jm00081a007
127045855 139121 0 None - 6 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at beta1-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 GRK2 and coelenterazine 400a by BRET assayAgonist activity at beta1-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 GRK2 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 - 6 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at beta1-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 GRK2 and coelenterazine 400a by BRET assayAgonist activity at beta1-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 GRK2 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
44328703 10118 0 None - 2 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at beta1-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 beta1-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 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 - 2 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at beta1-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 beta1-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 241 6 4 5 0.8 CC(C)NC[C@H](O)COc1ccc(O)c(O)c1 10.1021/acs.jmedchem.9b00349
44328703 10118 0 None - 2 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at beta1-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 beta1-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 - 2 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at beta1-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 beta1-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
76329060 105942 0 None - 0 Human 5.2 pEC50 = 5.2 Binding
Agonist activity at human beta1 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta1 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 - 0 Human 5.2 pEC50 = 5.2 Binding
Agonist activity at human beta1 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta1 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 - 0 Human 5.2 pEC50 = 5.2 Binding
Agonist activity at human beta1 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta1 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
76315639 84879 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at Homo sapiens (human) beta1 adrenoreceptorAgonist activity at Homo sapiens (human) beta1 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 - 0 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at Homo sapiens (human) beta1 adrenoreceptorAgonist activity at Homo sapiens (human) beta1 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
76315637 84876 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at Homo sapiens (human) beta1 adrenoreceptorAgonist activity at Homo sapiens (human) beta1 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 - 0 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at Homo sapiens (human) beta1 adrenoreceptorAgonist activity at Homo sapiens (human) beta1 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
44396530 66738 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at Homo sapiens (human) beta1 adrenoreceptorAgonist activity at Homo sapiens (human) beta1 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 - 0 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at Homo sapiens (human) beta1 adrenoreceptorAgonist activity at Homo sapiens (human) beta1 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
44392542 65516 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at Homo sapiens (human) beta1 adrenoreceptorAgonist activity at Homo sapiens (human) beta1 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 - 0 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at Homo sapiens (human) beta1 adrenoreceptorAgonist activity at Homo sapiens (human) beta1 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
443372 10123 23 None - 3 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at human beta1 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta1 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 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at human beta1 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta1 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 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at human beta1 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta1 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
127045855 139121 0 None - 6 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at beta1-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 beta1-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 - 6 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at beta1-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 beta1-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
127046950 139502 0 None - 6 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at beta1-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 GRK2 and coelenterazine 400a by BRET assayAgonist activity at beta1-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 GRK2 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 - 6 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at beta1-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 GRK2 and coelenterazine 400a by BRET assayAgonist activity at beta1-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 GRK2 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
127046950 139502 0 None - 6 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at beta1-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 beta1-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 - 6 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at beta1-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 beta1-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 - 2 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at beta1-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 beta1-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 - 2 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at beta1-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 beta1-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
2419 3394 80 None -162 6 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at human beta1 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta1 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 -162 6 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at human beta1 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta1 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 -162 6 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at human beta1 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta1 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 -162 6 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at human beta1 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta1 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 -162 6 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at human beta1 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta1 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
146025803 175593 0 None - 2 Human 5.1 pEC50 = 5.1 Binding
Agonist activity at beta1-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 GRK5 and coelenterazine 400a by BRET assayAgonist activity at beta1-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 GRK5 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 - 2 Human 5.1 pEC50 = 5.1 Binding
Agonist activity at beta1-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 GRK5 and coelenterazine 400a by BRET assayAgonist activity at beta1-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 GRK5 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
44392575 64026 0 None - 0 Human 8.0 pEC50 = 8.0 Binding
Agonist activity at Homo sapiens (human) beta1 adrenoreceptorAgonist activity at Homo sapiens (human) beta1 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 - 0 Human 8.0 pEC50 = 8.0 Binding
Agonist activity at Homo sapiens (human) beta1 adrenoreceptorAgonist activity at Homo sapiens (human) beta1 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
53494950 72738 0 None - 0 Human 10.4 pIC50 = 10.4 Binding
Displacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assayDisplacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assay
ChEMBL 416 12 4 6 2.1 N#Cc1ccccc1OC[C@@H](O)CNCCNC(=O)Nc1cccc(OCCF)c1 10.1021/ml1002458
CHEMBL2011218 72738 0 None - 0 Human 10.4 pIC50 = 10.4 Binding
Displacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assayDisplacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assay
ChEMBL 416 12 4 6 2.1 N#Cc1ccccc1OC[C@@H](O)CNCCNC(=O)Nc1cccc(OCCF)c1 10.1021/ml1002458
70683109 72746 0 None - 0 Human 10.3 pIC50 = 10.3 Binding
Displacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assayDisplacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assay
ChEMBL 481 9 4 6 1.7 N#Cc1ccccc1OC[C@@H](O)CNCCNC(=O)Nc1ccc(I)nc1 10.1021/ml1002458
CHEMBL2011226 72746 0 None - 0 Human 10.3 pIC50 = 10.3 Binding
Displacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assayDisplacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assay
ChEMBL 481 9 4 6 1.7 N#Cc1ccccc1OC[C@@H](O)CNCCNC(=O)Nc1ccc(I)nc1 10.1021/ml1002458
70693600 72747 0 None - 0 Human 10.3 pIC50 = 10.3 Binding
Displacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assayDisplacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assay
ChEMBL 433 9 4 6 1.9 N#Cc1ccccc1OC[C@@H](O)CNCCNC(=O)Nc1ccc(Br)nc1 10.1021/ml1002458
CHEMBL2011227 72747 0 None - 0 Human 10.3 pIC50 = 10.3 Binding
Displacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assayDisplacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assay
ChEMBL 433 9 4 6 1.9 N#Cc1ccccc1OC[C@@H](O)CNCCNC(=O)Nc1ccc(Br)nc1 10.1021/ml1002458
11546170 72736 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assayDisplacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assay
ChEMBL 416 12 4 6 2.1 N#Cc1ccccc1OC[C@@H](O)CNCCNC(=O)Nc1ccc(OCCF)cc1 10.1021/ml1002458
CHEMBL2011216 72736 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assayDisplacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assay
ChEMBL 416 12 4 6 2.1 N#Cc1ccccc1OC[C@@H](O)CNCCNC(=O)Nc1ccc(OCCF)cc1 10.1021/ml1002458
70691507 72735 0 None - 0 Human 10.0 pIC50 = 10 Binding
Displacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assayDisplacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assay
ChEMBL 372 9 4 5 1.8 N#Cc1ccccc1OC[C@@H](O)CNCCNC(=O)Nc1ccc(F)cc1 10.1021/ml1002458
CHEMBL2011215 72735 0 None - 0 Human 10.0 pIC50 = 10 Binding
Displacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assayDisplacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assay
ChEMBL 372 9 4 5 1.8 N#Cc1ccccc1OC[C@@H](O)CNCCNC(=O)Nc1ccc(F)cc1 10.1021/ml1002458
70683108 72744 0 None - 0 Human 10.0 pIC50 = 10 Binding
Displacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assayDisplacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assay
ChEMBL 417 12 4 7 1.5 N#Cc1ccccc1OC[C@@H](O)CNCCNC(=O)Nc1ccc(OCCF)nc1 10.1021/ml1002458
CHEMBL2011224 72744 0 None - 0 Human 10.0 pIC50 = 10 Binding
Displacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assayDisplacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assay
ChEMBL 417 12 4 7 1.5 N#Cc1ccccc1OC[C@@H](O)CNCCNC(=O)Nc1ccc(OCCF)nc1 10.1021/ml1002458
11523842 72733 0 None - 0 Human 10.0 pIC50 = 10.0 Binding
Displacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assayDisplacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assay
ChEMBL 384 10 4 6 1.7 COc1ccc(NC(=O)NCCNC[C@H](O)COc2ccccc2C#N)cc1 10.1021/ml1002458
CHEMBL2011213 72733 0 None - 0 Human 10.0 pIC50 = 10.0 Binding
Displacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assayDisplacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assay
ChEMBL 384 10 4 6 1.7 COc1ccc(NC(=O)NCCNC[C@H](O)COc2ccccc2C#N)cc1 10.1021/ml1002458
70680984 72754 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Displacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assayDisplacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assay
ChEMBL 371 10 3 5 1.4 N#Cc1ccccc1OC[C@@H](O)CNCCNC(=O)Cc1ccc(F)cc1 10.1021/ml1002458
CHEMBL2011235 72754 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Displacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assayDisplacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assay
ChEMBL 371 10 3 5 1.4 N#Cc1ccccc1OC[C@@H](O)CNCCNC(=O)Cc1ccc(F)cc1 10.1021/ml1002458
2585 788 100 None -1 22 Human 9.8 pIC50 = 9.8 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
522 788 100 None -1 22 Human 9.8 pIC50 = 9.8 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
551 788 100 None -1 22 Human 9.8 pIC50 = 9.8 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
CHEMBL723 788 100 None -1 22 Human 9.8 pIC50 = 9.8 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
DB01136 788 100 None -1 22 Human 9.8 pIC50 = 9.8 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
70687345 72734 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assayDisplacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assay
ChEMBL 372 9 4 5 1.8 N#Cc1ccccc1OC[C@@H](O)CNCCNC(=O)Nc1ccccc1F 10.1021/ml1002458
CHEMBL2011214 72734 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assayDisplacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assay
ChEMBL 372 9 4 5 1.8 N#Cc1ccccc1OC[C@@H](O)CNCCNC(=O)Nc1ccccc1F 10.1021/ml1002458
70683106 72737 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assayDisplacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assay
ChEMBL 430 13 4 6 2.4 N#Cc1ccccc1OC[C@@H](O)CNCCNC(=O)Nc1ccc(OCCCF)cc1 10.1021/ml1002458
CHEMBL2011217 72737 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assayDisplacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assay
ChEMBL 430 13 4 6 2.4 N#Cc1ccccc1OC[C@@H](O)CNCCNC(=O)Nc1ccc(OCCCF)cc1 10.1021/ml1002458
70680982 72745 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assayDisplacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assay
ChEMBL 373 9 4 6 1.2 N#Cc1ccccc1OC[C@@H](O)CNCCNC(=O)Nc1ccc(F)nc1 10.1021/ml1002458
CHEMBL2011225 72745 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assayDisplacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assay
ChEMBL 373 9 4 6 1.2 N#Cc1ccccc1OC[C@@H](O)CNCCNC(=O)Nc1ccc(F)nc1 10.1021/ml1002458
70693601 72748 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assayDisplacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assay
ChEMBL 434 9 4 7 1.3 N#Cc1ccccc1OC[C@@H](O)CNCCNC(=O)Nc1cnc(Br)cn1 10.1021/ml1002458
CHEMBL2011228 72748 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assayDisplacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assay
ChEMBL 434 9 4 7 1.3 N#Cc1ccccc1OC[C@@H](O)CNCCNC(=O)Nc1cnc(Br)cn1 10.1021/ml1002458
127 3066 45 None 2 15 Human 9.1 pIC50 = 9.1 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 248 6 3 3 1.9 O[C@H](COc1cccc2c1cc[nH]2)CNC(C)C nan
688095 3066 45 None 2 15 Human 9.1 pIC50 = 9.1 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 248 6 3 3 1.9 O[C@H](COc1cccc2c1cc[nH]2)CNC(C)C nan
CHEMBL117405 3066 45 None 2 15 Human 9.1 pIC50 = 9.1 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 248 6 3 3 1.9 O[C@H](COc1cccc2c1cc[nH]2)CNC(C)C nan
2176 3065 66 None -4 27 Human 9.0 pIC50 = 9.0 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C nan
4828 3065 66 None -4 27 Human 9.0 pIC50 = 9.0 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C nan
91 3065 66 None -4 27 Human 9.0 pIC50 = 9.0 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C nan
CHEMBL500 3065 66 None -4 27 Human 9.0 pIC50 = 9.0 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C nan
DB00960 3065 66 None -4 27 Human 9.0 pIC50 = 9.0 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C nan
70689402 72742 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assayDisplacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assay
ChEMBL 416 10 5 6 1.5 N#Cc1ccccc1OC[C@@H](O)CNCCNC(=O)Nc1ccc(C(=O)O)c(F)c1 10.1021/ml1002458
CHEMBL2011222 72742 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assayDisplacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assay
ChEMBL 416 10 5 6 1.5 N#Cc1ccccc1OC[C@@H](O)CNCCNC(=O)Nc1ccc(C(=O)O)c(F)c1 10.1021/ml1002458
70680981 72739 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assayDisplacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assay
ChEMBL 429 12 5 6 2.5 CC(CF)Nc1ccc(NC(=O)NCCNC[C@H](O)COc2ccccc2C#N)cc1 10.1021/ml1002458
CHEMBL2011219 72739 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assayDisplacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assay
ChEMBL 429 12 5 6 2.5 CC(CF)Nc1ccc(NC(=O)NCCNC[C@H](O)COc2ccccc2C#N)cc1 10.1021/ml1002458
145990586 166279 0 None -1 11 Human 8.8 pIC50 = 8.8 Binding
Displacement of [3H]-CGP-12177 from human beta1-adrenergic receptorDisplacement of [3H]-CGP-12177 from human beta1-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 8.8 pIC50 = 8.8 Binding
Displacement of [3H]-CGP-12177 from human beta1-adrenergic receptorDisplacement of [3H]-CGP-12177 from human beta1-adrenergic receptor
ChEMBL 297 2 2 4 2.6 COc1cc2c3c(c1OC)-c1ccccc1[C@@H](O)[C@@H]3NCC2 10.1039/C7MD00656J
2249 509 106 None -5 12 Human 8.8 pIC50 = 8.8 Binding
Percent inhibition against Beta-1 adrenergic receptor at 1 uMPercent inhibition against Beta-1 adrenergic receptor at 1 uM
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1021/jm058018d
255 509 106 None -5 12 Human 8.8 pIC50 = 8.8 Binding
Percent inhibition against Beta-1 adrenergic receptor at 1 uMPercent inhibition against Beta-1 adrenergic receptor at 1 uM
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1021/jm058018d
548 509 106 None -5 12 Human 8.8 pIC50 = 8.8 Binding
Percent inhibition against Beta-1 adrenergic receptor at 1 uMPercent inhibition against Beta-1 adrenergic receptor at 1 uM
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1021/jm058018d
CHEMBL24 509 106 None -5 12 Human 8.8 pIC50 = 8.8 Binding
Percent inhibition against Beta-1 adrenergic receptor at 1 uMPercent inhibition against Beta-1 adrenergic receptor at 1 uM
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1021/jm058018d
DB00335 509 106 None -5 12 Human 8.8 pIC50 = 8.8 Binding
Percent inhibition against Beta-1 adrenergic receptor at 1 uMPercent inhibition against Beta-1 adrenergic receptor at 1 uM
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1021/jm058018d
165193 3126 60 None -2 43 Human 8.7 pIC50 = 8.7 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
2303 3126 60 None -2 43 Human 8.7 pIC50 = 8.7 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
4946 3126 60 None -2 43 Human 8.7 pIC50 = 8.7 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
564 3126 60 None -2 43 Human 8.7 pIC50 = 8.7 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
62882 3126 60 None -2 43 Human 8.7 pIC50 = 8.7 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
63 3126 60 None -2 43 Human 8.7 pIC50 = 8.7 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
66366 3126 60 None -2 43 Human 8.7 pIC50 = 8.7 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
91536 3126 60 None -2 43 Human 8.7 pIC50 = 8.7 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
CHEMBL27 3126 60 None -2 43 Human 8.7 pIC50 = 8.7 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
CHEMBL452861 3126 60 None -2 43 Human 8.7 pIC50 = 8.7 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
DB00571 3126 60 None -2 43 Human 8.7 pIC50 = 8.7 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
24901416 70001 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of radiolabeled iodocyanopindolol from beta1 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from beta1 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 8.7 pIC50 = 8.7 Binding
Displacement of radiolabeled iodocyanopindolol from beta1 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from beta1 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
44268305 97832 0 None - 0 Human 8.0 pIC50 = 8 Binding
Compound was tested for binding affinity against cloned human beta-1 adrenergic receptor from CHO cells using [125I]-iodocyanopindolol as radioligandCompound was tested for binding affinity against cloned human beta-1 adrenergic receptor from CHO cells using [125I]-iodocyanopindolol as 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 8.0 pIC50 = 8 Binding
Compound was tested for binding affinity against cloned human beta-1 adrenergic receptor from CHO cells using [125I]-iodocyanopindolol as radioligandCompound was tested for binding affinity against cloned human beta-1 adrenergic receptor from CHO cells using [125I]-iodocyanopindolol as 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
1531 2226 64 None -1 15 Human 8.0 pIC50 = 8 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
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 pIC50 = 8 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
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 pIC50 = 8 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
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 pIC50 = 8 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
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 pIC50 = 8 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O nan
70685188 72750 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assayDisplacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assay
ChEMBL 392 11 4 9 -0.3 N#Cc1ccccc1OC[C@@H](O)CNCCNC(=O)Nc1nnn(CCF)n1 10.1021/ml1002458
CHEMBL2011230 72750 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assayDisplacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assay
ChEMBL 392 11 4 9 -0.3 N#Cc1ccccc1OC[C@@H](O)CNCCNC(=O)Nc1nnn(CCF)n1 10.1021/ml1002458
70687347 72752 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assayDisplacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assay
ChEMBL 358 9 3 6 0.9 N#Cc1ccccc1OC[C@@H](O)CNCCNC(=O)c1ccc(F)nc1 10.1021/ml1002458
CHEMBL2011233 72752 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assayDisplacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assay
ChEMBL 358 9 3 6 0.9 N#Cc1ccccc1OC[C@@H](O)CNCCNC(=O)c1ccc(F)nc1 10.1021/ml1002458
24901143 70007 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of radiolabeled iodocyanopindolol from beta1 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from beta1 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 8.0 pIC50 = 8 Binding
Displacement of radiolabeled iodocyanopindolol from beta1 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from beta1 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
24900750 70021 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of radiolabeled iodocyanopindolol from beta1 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from beta1 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 8.0 pIC50 = 8 Binding
Displacement of radiolabeled iodocyanopindolol from beta1 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from beta1 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
16049162 63746 0 None - 0 Human 7.0 pIC50 = 7 Binding
Binding affinity to adrenergic beta1 receptorBinding affinity to adrenergic beta1 receptor
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 - 0 Human 7.0 pIC50 = 7 Binding
Binding affinity to adrenergic beta1 receptorBinding affinity to adrenergic beta1 receptor
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
16049377 63752 0 None - 0 Human 7.0 pIC50 = 7 Binding
Binding affinity to adrenergic beta1 receptorBinding affinity to adrenergic beta1 receptor
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 - 0 Human 7.0 pIC50 = 7 Binding
Binding affinity to adrenergic beta1 receptorBinding affinity to adrenergic beta1 receptor
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
24900751 70022 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of radiolabeled iodocyanopindolol from beta1 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from beta1 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 7.0 pIC50 = 7 Binding
Displacement of radiolabeled iodocyanopindolol from beta1 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from beta1 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
44268277 22093 0 None - 0 Human 7.0 pIC50 = 7 Binding
Tested for binding affinity against cloned human beta-1 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandTested for binding affinity against cloned human beta-1 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 7.0 pIC50 = 7 Binding
Tested for binding affinity against cloned human beta-1 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandTested for binding affinity against cloned human beta-1 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
44281371 99645 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity to recombinant human beta-1 adrenergic receptor expressed in CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-1 adrenergic receptor expressed in 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 6.0 pIC50 = 6 Binding
Binding affinity to recombinant human beta-1 adrenergic receptor expressed in CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-1 adrenergic receptor expressed in 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
44377315 57062 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards human Beta-1 adrenergic receptor expressed in CHO cells, using 125I]iodocyanopindololBinding affinity towards human Beta-1 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-1 adrenergic receptor expressed in CHO cells, using 125I]iodocyanopindololBinding affinity towards human Beta-1 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
44313090 102682 0 None - 0 Human 6.0 pIC50 = 6 Binding
Compound was evaluated for its inhibitory activity against CHO cells expressing the cloned human Beta-1 adrenergic receptor in the presence of [125I]iodocyanopindololCompound was evaluated for its inhibitory activity against CHO cells expressing the cloned human Beta-1 adrenergic receptor in the presence of [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 6.0 pIC50 = 6 Binding
Compound was evaluated for its inhibitory activity against CHO cells expressing the cloned human Beta-1 adrenergic receptor in the presence of [125I]iodocyanopindololCompound was evaluated for its inhibitory activity against CHO cells expressing the cloned human Beta-1 adrenergic receptor in the presence of [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 6.0 pIC50 = 6 Binding
Compound was evaluated for its inhibitory activity against CHO cells expressing the cloned human Beta-1 adrenergic receptor in the presence of [125I]iodocyanopindololCompound was evaluated for its inhibitory activity against CHO cells expressing the cloned human Beta-1 adrenergic receptor in the presence of [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 6.0 pIC50 = 6 Binding
Compound was evaluated for its inhibitory activity against CHO cells expressing the cloned human Beta-1 adrenergic receptor in the presence of [125I]iodocyanopindololCompound was evaluated for its inhibitory activity against CHO cells expressing the cloned human Beta-1 adrenergic receptor in the presence of [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
3038500 9235 8 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [125]I-cyanopindolol from recombinant human beta1 adrenergic receptor after 1 hr by scintillation counting methodDisplacement of [125]I-cyanopindolol from recombinant human beta1 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 6.0 pIC50 = 6 Binding
Displacement of [125]I-cyanopindolol from recombinant human beta1 adrenergic receptor after 1 hr by scintillation counting methodDisplacement of [125]I-cyanopindolol from recombinant human beta1 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
44307007 100298 0 None - 0 Human 6.0 pIC50 = 6 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-1 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-1 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 6.0 pIC50 = 6 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-1 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-1 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
10437614 100462 6 None - 0 Human 6.0 pIC50 = 6 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-1 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-1 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 6.0 pIC50 = 6 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-1 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-1 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
44303198 201459 0 None - 0 Human 6.0 pIC50 = 6 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-1 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-1 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 6.0 pIC50 = 6 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-1 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-1 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
44307065 201632 0 None - 0 Human 6.0 pIC50 = 6 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-1 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-1 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 6.0 pIC50 = 6 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-1 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-1 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
44307064 201635 0 None - 0 Human 6.0 pIC50 = 6 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-1 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-1 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 6.0 pIC50 = 6 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-1 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-1 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
44307343 201900 0 None - 0 Human 6.0 pIC50 = 6 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-1 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-1 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 6.0 pIC50 = 6 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-1 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-1 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
44268572 25446 0 None - 0 Human 6.0 pIC50 = 6 Binding
In vitro affinity at Beta-1 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-1 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-1 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-1 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
44268482 97635 0 None - 0 Human 6.0 pIC50 = 6 Binding
In vitro affinity at Beta-1 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-1 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 6.0 pIC50 = 6 Binding
In vitro affinity at Beta-1 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-1 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
12017016 99690 0 None - 0 Human 6.0 pIC50 = 6 Binding
In vitro binding affinity at beta-1 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-1 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 6.0 pIC50 = 6 Binding
In vitro binding affinity at beta-1 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-1 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
44298497 193022 0 None - 0 Human 6.0 pIC50 = 6 Binding
In vitro binding affinity towards cloned human beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-1 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 6.0 pIC50 = 6 Binding
In vitro binding affinity towards cloned human beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-1 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
44298731 196394 0 None - 0 Human 6.0 pIC50 = 6 Binding
In vitro binding affinity towards cloned human beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-1 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 6.0 pIC50 = 6 Binding
In vitro binding affinity towards cloned human beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-1 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
9799092 47027 0 None - 0 Human 6.0 pIC50 = 6 Binding
Receptor binding assay(Beta-1 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-1 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 6.0 pIC50 = 6 Binding
Receptor binding assay(Beta-1 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-1 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
44268281 16684 0 None - 0 Human 6.0 pIC50 = 6 Binding
Tested for binding affinity against cloned human beta-1 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandTested for binding affinity against cloned human beta-1 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 6.0 pIC50 = 6 Binding
Tested for binding affinity against cloned human beta-1 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandTested for binding affinity against cloned human beta-1 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
44268275 19398 0 None - 0 Human 6.0 pIC50 = 6 Binding
Tested for binding affinity against cloned human beta-1 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandTested for binding affinity against cloned human beta-1 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 6.0 pIC50 = 6 Binding
Tested for binding affinity against cloned human beta-1 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandTested for binding affinity against cloned human beta-1 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
44268254 19798 0 None - 0 Human 6.0 pIC50 = 6 Binding
Tested for binding affinity against cloned human beta-1 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandTested for binding affinity against cloned human beta-1 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 6.0 pIC50 = 6 Binding
Tested for binding affinity against cloned human beta-1 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandTested for binding affinity against cloned human beta-1 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 6.0 pIC50 = 6 Binding
Tested for binding affinity against cloned human beta-1 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandTested for binding affinity against cloned human beta-1 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 6.0 pIC50 = 6 Binding
Tested for binding affinity against cloned human beta-1 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandTested for binding affinity against cloned human beta-1 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
44268324 16590 0 None - 0 Human 6.0 pIC50 = 6 Binding
Tested for binding affinity against cloned human beta-1 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligand.Tested for binding affinity against cloned human beta-1 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 6.0 pIC50 = 6 Binding
Tested for binding affinity against cloned human beta-1 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligand.Tested for binding affinity against cloned human beta-1 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
44268274 18647 0 None - 0 Human 6.0 pIC50 = 6 Binding
Tested for binding affinity against cloned human beta-1 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligand.Tested for binding affinity against cloned human beta-1 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 6.0 pIC50 = 6 Binding
Tested for binding affinity against cloned human beta-1 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligand.Tested for binding affinity against cloned human beta-1 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
44335572 5088 0 None - 0 Human 5.0 pIC50 = 5 Binding
Beta-1 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-1 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 5.0 pIC50 = 5 Binding
Beta-1 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-1 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
44335498 107044 0 None - 0 Human 5.0 pIC50 = 5 Binding
Beta-1 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-1 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 5.0 pIC50 = 5 Binding
Beta-1 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-1 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
44335562 108041 0 None - 0 Human 5.0 pIC50 = 5 Binding
Beta-1 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-1 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 5.0 pIC50 = 5 Binding
Beta-1 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-1 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
44303192 201585 0 None - 0 Human 5.0 pIC50 = 5 Binding
Beta-1 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-1 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 5.0 pIC50 = 5 Binding
Beta-1 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-1 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
12049923 201967 0 None - 0 Human 5.0 pIC50 = 5 Binding
Binding affinity for cloned human Beta-1 adrenergic receptor expressed in CHO cells, tested in the presence of I-iodocyanopindolol.Binding affinity for cloned human Beta-1 adrenergic receptor expressed in CHO cells, tested 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 5.0 pIC50 = 5 Binding
Binding affinity for cloned human Beta-1 adrenergic receptor expressed in CHO cells, tested in the presence of I-iodocyanopindolol.Binding affinity for cloned human Beta-1 adrenergic receptor expressed in CHO cells, tested 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
44461468 105136 0 None - 0 Human 5.0 pIC50 = 5 Binding
Binding affinity towards Beta-1 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindololBinding affinity towards Beta-1 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 5.0 pIC50 = 5 Binding
Binding affinity towards Beta-1 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindololBinding affinity towards Beta-1 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
44377412 119636 0 None - 0 Human 5.0 pIC50 = 5 Binding
Binding affinity towards Beta-1 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindololBinding affinity towards Beta-1 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-1 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindololBinding affinity towards Beta-1 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 cloned human Beta-1 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity towards cloned human Beta-1 adrenergic receptor prepared from CHO cells 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 cloned human Beta-1 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity towards cloned human Beta-1 adrenergic receptor prepared from CHO cells 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
12043158 162666 0 None - 0 Human 5.0 pIC50 = 5 Binding
Binding affinity towards cloned human Beta-1 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity towards cloned human Beta-1 adrenergic receptor prepared from CHO cells 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 5.0 pIC50 = 5 Binding
Binding affinity towards cloned human Beta-1 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity towards cloned human Beta-1 adrenergic receptor prepared from CHO cells 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
44377677 56570 0 None - 0 Human 5.0 pIC50 = 5 Binding
Binding affinity towards human Beta-1 adrenergic receptor expressed in CHO cells, using 125I]iodocyanopindololBinding affinity towards human Beta-1 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 5.0 pIC50 = 5 Binding
Binding affinity towards human Beta-1 adrenergic receptor expressed in CHO cells, using 125I]iodocyanopindololBinding affinity towards human Beta-1 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
44377517 56921 0 None - 0 Human 5.0 pIC50 = 5 Binding
Binding affinity towards human Beta-1 adrenergic receptor expressed in CHO cells, using 125I]iodocyanopindololBinding affinity towards human Beta-1 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 5.0 pIC50 = 5 Binding
Binding affinity towards human Beta-1 adrenergic receptor expressed in CHO cells, using 125I]iodocyanopindololBinding affinity towards human Beta-1 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
44377957 57183 0 None - 0 Human 5.0 pIC50 = 5 Binding
Binding affinity towards human Beta-1 adrenergic receptor expressed in CHO cells, using 125I]iodocyanopindololBinding affinity towards human Beta-1 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 5.0 pIC50 = 5 Binding
Binding affinity towards human Beta-1 adrenergic receptor expressed in CHO cells, using 125I]iodocyanopindololBinding affinity towards human Beta-1 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
44377650 119687 0 None - 0 Human 5.0 pIC50 = 5 Binding
Binding affinity towards human Beta-1 adrenergic receptor expressed in CHO cells, using 125I]iodocyanopindololBinding affinity towards human Beta-1 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 5.0 pIC50 = 5 Binding
Binding affinity towards human Beta-1 adrenergic receptor expressed in CHO cells, using 125I]iodocyanopindololBinding affinity towards human Beta-1 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
44461489 203631 0 None - 0 Human 5.0 pIC50 = 5 Binding
Binding affinity towards human Beta-1 adrenergic receptor expressed in CHO cells, using 125I]iodocyanopindololBinding affinity towards human Beta-1 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 5.0 pIC50 = 5 Binding
Binding affinity towards human Beta-1 adrenergic receptor expressed in CHO cells, using 125I]iodocyanopindololBinding affinity towards human Beta-1 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
44461719 204139 0 None - 0 Human 5.0 pIC50 = 5 Binding
Binding affinity towards human Beta-1 adrenergic receptor expressed in CHO cells, using 125I]iodocyanopindololBinding affinity towards human Beta-1 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 5.0 pIC50 = 5 Binding
Binding affinity towards human Beta-1 adrenergic receptor expressed in CHO cells, using 125I]iodocyanopindololBinding affinity towards human Beta-1 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
44306992 202057 0 None - 0 Human 5.0 pIC50 = 5 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-1 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-1 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 5.0 pIC50 = 5 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-1 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-1 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
44298767 100419 0 None - 0 Human 5.0 pIC50 = 5 Binding
In vitro binding affinity towards cloned human beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-1 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-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-1 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
44298306 101516 0 None - 0 Human 5.0 pIC50 = 5 Binding
In vitro binding affinity towards cloned human beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-1 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 5.0 pIC50 = 5 Binding
In vitro binding affinity towards cloned human beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-1 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
44298752 195173 0 None - 0 Human 5.0 pIC50 = 5 Binding
In vitro binding affinity towards cloned human beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-1 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 5.0 pIC50 = 5 Binding
In vitro binding affinity towards cloned human beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-1 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
44298718 195401 0 None - 0 Human 5.0 pIC50 = 5 Binding
In vitro binding affinity towards cloned human beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-1 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 5.0 pIC50 = 5 Binding
In vitro binding affinity towards cloned human beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-1 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
44335844 4787 0 None - 0 Human 4.0 pIC50 = 4 Binding
Beta-1 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-1 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 4.0 pIC50 = 4 Binding
Beta-1 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-1 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
44335882 4820 0 None - 0 Human 4.0 pIC50 = 4 Binding
Beta-1 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-1 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 4.0 pIC50 = 4 Binding
Beta-1 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-1 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
44335833 5491 0 None - 0 Human 4.0 pIC50 = 4 Binding
Beta-1 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-1 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 4.0 pIC50 = 4 Binding
Beta-1 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-1 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
44301881 100056 0 None - 0 Human 4.0 pIC50 = 4 Binding
Binding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cellsBinding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cells
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 Binding
Binding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cellsBinding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cells
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
44377755 119436 0 None - 0 Human 4.0 pIC50 = 4 Binding
Binding affinity towards human Beta-1 adrenergic receptor expressed in CHO cells, using 125I]iodocyanopindololBinding affinity towards human Beta-1 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 4.0 pIC50 = 4 Binding
Binding affinity towards human Beta-1 adrenergic receptor expressed in CHO cells, using 125I]iodocyanopindololBinding affinity towards human Beta-1 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
44461488 203654 0 None - 0 Human 4.0 pIC50 = 4 Binding
Binding affinity towards human Beta-1 adrenergic receptor expressed in CHO cells, using 125I]iodocyanopindololBinding affinity towards human Beta-1 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-1 adrenergic receptor expressed in CHO cells, using 125I]iodocyanopindololBinding affinity towards human Beta-1 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
44298761 193334 0 None - 0 Human 4.0 pIC50 = 4 Binding
In vitro binding affinity towards cloned human beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-1 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 4.0 pIC50 = 4 Binding
In vitro binding affinity towards cloned human beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-1 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
145947241 167060 0 None -8 2 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [3H]-CGP-12177 from adrenergic beta1 receptor in Wistar rat cortex incubated for 60 mins by microbeta liquid scintillation counting analysisDisplacement of [3H]-CGP-12177 from adrenergic beta1 receptor in Wistar rat cortex incubated for 60 mins by microbeta liquid scintillation counting analysis
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 -8 2 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [3H]-CGP-12177 from adrenergic beta1 receptor in Wistar rat cortex incubated for 60 mins by microbeta liquid scintillation counting analysisDisplacement of [3H]-CGP-12177 from adrenergic beta1 receptor in Wistar rat cortex incubated for 60 mins by microbeta liquid scintillation counting analysis
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 -8 2 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [3H]-CGP-12177 from adrenergic beta1 receptor in Wistar rat cortex incubated for 60 mins by microbeta liquid scintillation counting analysisDisplacement of [3H]-CGP-12177 from adrenergic beta1 receptor in Wistar rat cortex incubated for 60 mins by microbeta liquid scintillation counting analysis
ChEMBL 449 10 2 7 3.5 COc1ccc(CCNCC(O)COc2cccc3c(=O)c4ccccc4oc23)cc1OC 10.1016/j.bmc.2018.04.038
44349588 116449 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity for human Beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity for human Beta-1 adrenergic receptor 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 7.0 pIC50 = 7.0 Binding
Binding affinity for human Beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity for human Beta-1 adrenergic receptor 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
9912580 17886 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Tested for binding affinity against cloned human beta-1 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandTested for binding affinity against cloned human beta-1 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 7.0 pIC50 = 7.0 Binding
Tested for binding affinity against cloned human beta-1 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandTested for binding affinity against cloned human beta-1 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
44301818 201053 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cellsBinding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cells
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 6.0 pIC50 = 6.0 Binding
Binding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cellsBinding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cells
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
14998855 55397 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterolBinding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterol
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 Human 6.0 pIC50 = 6.0 Binding
Binding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterolBinding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterol
ChEMBL 402 6 2 5 1.3 CN(c1ccc(C(=O)NCC2CN(c3ccccc3)CCN2)cc1)S(C)(=O)=O 10.1021/jm00082a016
14998858 119528 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterolBinding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterol
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 Human 6.0 pIC50 = 6.0 Binding
Binding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterolBinding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterol
ChEMBL 422 6 3 5 1.9 CS(=O)(=O)Nc1ccc(C(=O)NCC2CN(c3cccc(Cl)c3)CCN2)cc1 10.1021/jm00082a016
44349378 18324 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity for human Beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity for human Beta-1 adrenergic receptor 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 6.0 pIC50 = 6.0 Binding
Binding affinity for human Beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity for human Beta-1 adrenergic receptor 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
46881651 6768 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]cyanopindolol from human beta 1 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 1 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 6.0 pIC50 = 6.0 Binding
Displacement of [125I]cyanopindolol from human beta 1 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 1 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
46881753 7170 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of [125I]cyanopindolol from human beta 1 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 1 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counter
ChEMBL 443 10 3 6 3.4 Cn1c(CCC(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)nc2ccccc21 10.1016/j.bmcl.2010.01.130
CHEMBL1085929 7170 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of [125I]cyanopindolol from human beta 1 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 1 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counter
ChEMBL 443 10 3 6 3.4 Cn1c(CCC(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)nc2ccccc21 10.1016/j.bmcl.2010.01.130
2812 4696 96 None -38 34 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
CHEMBL104 4696 96 None -38 34 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
5806 102690 16 None - 3 Guinea pig 6.9 pIC50 = 6.9 Binding
Inhibitory concentration against beta-1-adrenergic receptor in isolated guinea pig atriaInhibitory concentration against beta-1-adrenergic receptor in isolated guinea pig atria
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 6.9 pIC50 = 6.9 Binding
Inhibitory concentration against beta-1-adrenergic receptor in isolated guinea pig atriaInhibitory concentration against beta-1-adrenergic receptor in isolated guinea pig atria
ChEMBL 247 4 2 2 3.0 CC(C)NCC(O)c1ccc(Cl)c(Cl)c1 10.1021/jm00036a018
24901141 70180 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of radiolabeled iodocyanopindolol from beta1 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from beta1 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 7.9 pIC50 = 7.9 Binding
Displacement of radiolabeled iodocyanopindolol from beta1 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from beta1 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
12582 935 40 None -3 5 Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
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 -3 5 Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
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 -3 5 Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
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 -3 5 Human 6.9 pIC50 = 6.9 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 276 3 3 3 3.0 CC(C)(C)NCC(C1=CC(=C(C(=C1)Cl)N)Cl)O nan
44338637 109024 0 None - 0 Guinea pig 5.9 pIC50 = 5.9 Binding
Beta-1 adrenergic receptor blocking was assessed from 50% inhibition of the isoproterenol submaximal response on isolated Guinea pig atria(IA)Beta-1 adrenergic receptor blocking was assessed from 50% inhibition of the isoproterenol submaximal response on isolated Guinea pig atria(IA)
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 5.9 pIC50 = 5.9 Binding
Beta-1 adrenergic receptor blocking was assessed from 50% inhibition of the isoproterenol submaximal response on isolated Guinea pig atria(IA)Beta-1 adrenergic receptor blocking was assessed from 50% inhibition of the isoproterenol submaximal response on isolated Guinea pig atria(IA)
ChEMBL 346 7 2 5 2.8 COC12CCCCC1c1ccccc1/C2=N/OCC(O)CNC(C)C 10.1021/jm00122a008
10416656 18407 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity for human Beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity for human Beta-1 adrenergic receptor 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 5.9 pIC50 = 5.9 Binding
Binding affinity for human Beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity for human Beta-1 adrenergic receptor 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
9831168 202986 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Compound was evaluated for its inhibitory activity against CHO cells expressing the cloned human Beta-1 adrenergic receptor in the presence of [125I]iodocyanopindololCompound was evaluated for its inhibitory activity against CHO cells expressing the cloned human Beta-1 adrenergic receptor in the presence of [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 5.9 pIC50 = 5.9 Binding
Compound was evaluated for its inhibitory activity against CHO cells expressing the cloned human Beta-1 adrenergic receptor in the presence of [125I]iodocyanopindololCompound was evaluated for its inhibitory activity against CHO cells expressing the cloned human Beta-1 adrenergic receptor in the presence of [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
12017012 99348 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
In vitro binding affinity at beta-1 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-1 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 5.9 pIC50 = 5.9 Binding
In vitro binding affinity at beta-1 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-1 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
44338131 108165 0 None - 0 Guinea pig 4.9 pIC50 = 4.9 Binding
Beta-1 adrenergic receptor blocking was assessed from 50% inhibition of the isoproterenol submaximal response on isolated Guinea pig atria(IA)Beta-1 adrenergic receptor blocking was assessed from 50% inhibition of the isoproterenol submaximal response on isolated Guinea pig atria(IA)
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 4.9 pIC50 = 4.9 Binding
Beta-1 adrenergic receptor blocking was assessed from 50% inhibition of the isoproterenol submaximal response on isolated Guinea pig atria(IA)Beta-1 adrenergic receptor blocking was assessed from 50% inhibition of the isoproterenol submaximal response on isolated Guinea pig atria(IA)
ChEMBL 360 6 2 5 3.2 COC12CCCCC1c1ccccc1/C2=N/OCC(O)CNC(C)(C)C 10.1021/jm00122a008
83111 57061 78 None - 0 Human 4.9 pIC50 = 4.9 Binding
Binding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterolBinding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterol
ChEMBL 176 1 1 2 1.4 Cc1cccc(N2CCNCC2)c1 10.1021/jm00082a016
CHEMBL165175 57061 78 None - 0 Human 4.9 pIC50 = 4.9 Binding
Binding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterolBinding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterol
ChEMBL 176 1 1 2 1.4 Cc1cccc(N2CCNCC2)c1 10.1021/jm00082a016
415628 206441 89 None - 5 Human 4.9 pIC50 = 4.9 Binding
Binding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterolBinding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterol
ChEMBL 196 1 1 2 1.8 Clc1ccccc1N1CCNCC1 10.1021/jm00082a016
CHEMBL9841 206441 89 None - 5 Human 4.9 pIC50 = 4.9 Binding
Binding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterolBinding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterol
ChEMBL 196 1 1 2 1.8 Clc1ccccc1N1CCNCC1 10.1021/jm00082a016
46881981 5648 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of [125I]cyanopindolol from human beta 1 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 1 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 4.9 pIC50 = 4.9 Binding
Displacement of [125I]cyanopindolol from human beta 1 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 1 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
46845698 5690 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of [125I]cyanopindolol from human beta 1 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 1 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 4.9 pIC50 = 4.9 Binding
Displacement of [125I]cyanopindolol from human beta 1 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 1 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
10464801 11094 0 None - 2 Guinea pig 4.9 pIC50 = 4.9 Binding
Inhibitory concentration against beta-1-adrenergic receptor in isolated guinea pig atriaInhibitory concentration against beta-1-adrenergic receptor in isolated guinea pig atria
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 4.9 pIC50 = 4.9 Binding
Inhibitory concentration against beta-1-adrenergic receptor in isolated guinea pig atriaInhibitory concentration against beta-1-adrenergic receptor in isolated guinea pig atria
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 4.9 pIC50 = 4.9 Binding
Inhibitory concentration against beta-1-adrenergic receptor in isolated guinea pig atriaInhibitory concentration against beta-1-adrenergic receptor in isolated guinea pig atria
ChEMBL 174 6 2 4 0.4 CCO/N=C/C(O)CNC(C)C 10.1021/jm00036a018
16049160 63745 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to adrenergic beta1 receptorBinding affinity to adrenergic beta1 receptor
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 - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to adrenergic beta1 receptorBinding affinity to adrenergic beta1 receptor
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
16049234 63748 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to adrenergic beta1 receptorBinding affinity to adrenergic beta1 receptor
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 - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to adrenergic beta1 receptorBinding affinity to adrenergic beta1 receptor
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
16049374 63753 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to adrenergic beta1 receptorBinding affinity to adrenergic beta1 receptor
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 - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to adrenergic beta1 receptorBinding affinity to adrenergic beta1 receptor
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
24900811 70006 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of radiolabeled iodocyanopindolol from beta1 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from beta1 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 5.9 pIC50 = 5.9 Binding
Displacement of radiolabeled iodocyanopindolol from beta1 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from beta1 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
57401436 70043 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of radiolabeled iodocyanopindolol from beta1 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from beta1 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 5.9 pIC50 = 5.9 Binding
Displacement of radiolabeled iodocyanopindolol from beta1 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from beta1 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
4189 205185 91 None -38 34 Human 4.9 pIC50 = 4.9 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL1559 205185 91 None -38 34 Human 4.9 pIC50 = 4.9 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL91 205185 91 None -38 34 Human 4.9 pIC50 = 4.9 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
3198 203792 73 None -38 34 Human 4.9 pIC50 = 4.9 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL1201049 203792 73 None -38 34 Human 4.9 pIC50 = 4.9 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL808 203792 73 None -38 34 Human 4.9 pIC50 = 4.9 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
10054896 113627 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity to recombinant human beta-1 adrenergic receptor expressed in CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-1 adrenergic receptor expressed in 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 5.9 pIC50 = 5.9 Binding
Binding affinity to recombinant human beta-1 adrenergic receptor expressed in CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-1 adrenergic receptor expressed in 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
12049918 101727 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity for cloned human Beta-1 adrenergic receptor expressed in CHO cells, tested in the presence of I-iodocyanopindolol.Binding affinity for cloned human Beta-1 adrenergic receptor expressed in CHO cells, tested 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 5.9 pIC50 = 5.9 Binding
Binding affinity for cloned human Beta-1 adrenergic receptor expressed in CHO cells, tested in the presence of I-iodocyanopindolol.Binding affinity for cloned human Beta-1 adrenergic receptor expressed in CHO cells, tested 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
44307379 201942 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-1 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-1 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 5.9 pIC50 = 5.9 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-1 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-1 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
44307378 202094 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-1 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-1 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 5.9 pIC50 = 5.9 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-1 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-1 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
44338562 9322 0 None - 0 Guinea pig 4.9 pIC50 = 4.9 Binding
Beta-1 adrenergic receptor blocking was assessed from 50% inhibition of the isoproterenol submaximal response on isolated Guinea pig atria(IA)Beta-1 adrenergic receptor blocking was assessed from 50% inhibition of the isoproterenol submaximal response on isolated Guinea pig atria(IA)
ChEMBL 482 11 2 7 4.1 COc1cc(CCNCC(O)CO/N=C2/c3ccccc3C3CCCCCC23OC)cc(OC)c1 10.1021/jm00122a008
CHEMBL111706 9322 0 None - 0 Guinea pig 4.9 pIC50 = 4.9 Binding
Beta-1 adrenergic receptor blocking was assessed from 50% inhibition of the isoproterenol submaximal response on isolated Guinea pig atria(IA)Beta-1 adrenergic receptor blocking was assessed from 50% inhibition of the isoproterenol submaximal response on isolated Guinea pig atria(IA)
ChEMBL 482 11 2 7 4.1 COc1cc(CCNCC(O)CO/N=C2/c3ccccc3C3CCCCCC23OC)cc(OC)c1 10.1021/jm00122a008
44301842 197183 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Binding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cellsBinding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cells
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 4.9 pIC50 = 4.9 Binding
Binding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cellsBinding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cells
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
80447 56917 113 None - 0 Human 4.9 pIC50 = 4.9 Binding
Binding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterolBinding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterol
ChEMBL 207 2 1 4 1.0 O=[N+]([O-])c1ccc(N2CCNCC2)cc1 10.1021/jm00082a016
CHEMBL165012 56917 113 None - 0 Human 4.9 pIC50 = 4.9 Binding
Binding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterolBinding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterol
ChEMBL 207 2 1 4 1.0 O=[N+]([O-])c1ccc(N2CCNCC2)cc1 10.1021/jm00082a016
46881899 7690 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of [125I]cyanopindolol from human beta 1 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 1 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)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2010.01.130
CHEMBL1089395 7690 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of [125I]cyanopindolol from human beta 1 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 1 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)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2010.01.130
2249 509 106 None -5 12 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C nan
255 509 106 None -5 12 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C nan
548 509 106 None -5 12 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C nan
CHEMBL24 509 106 None -5 12 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C nan
DB00335 509 106 None -5 12 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C nan
76332892 105421 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of [125I]-cyanopindolol from recombinant human beta-1 adrenergic receptor expressed in CHO cell membranes after 1 hr by scintillation counting analysisDisplacement of [125I]-cyanopindolol from recombinant human beta-1 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 4.9 pIC50 = 4.9 Binding
Displacement of [125I]-cyanopindolol from recombinant human beta-1 adrenergic receptor expressed in CHO cell membranes after 1 hr by scintillation counting analysisDisplacement of [125I]-cyanopindolol from recombinant human beta-1 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
10375227 11098 0 None - 2 Guinea pig 4.9 pIC50 = 4.9 Binding
Inhibitory concentration against beta-1-adrenergic receptor in isolated guinea pig atriaInhibitory concentration against beta-1-adrenergic receptor in isolated guinea pig atria
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 4.9 pIC50 = 4.9 Binding
Inhibitory concentration against beta-1-adrenergic receptor in isolated guinea pig atriaInhibitory concentration against beta-1-adrenergic receptor in isolated guinea pig atria
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 4.9 pIC50 = 4.9 Binding
Inhibitory concentration against beta-1-adrenergic receptor in isolated guinea pig atriaInhibitory concentration against beta-1-adrenergic receptor in isolated guinea pig atria
ChEMBL 188 5 2 4 0.8 C/C=N/OCC(O)CNC(C)(C)C 10.1021/jm00036a018
10012704 11102 0 None - 2 Guinea pig 4.9 pIC50 = 4.9 Binding
Inhibitory concentration against beta-1-adrenergic receptor in isolated guinea pig atriaInhibitory concentration against beta-1-adrenergic receptor in isolated guinea pig atria
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 4.9 pIC50 = 4.9 Binding
Inhibitory concentration against beta-1-adrenergic receptor in isolated guinea pig atriaInhibitory concentration against beta-1-adrenergic receptor in isolated guinea pig atria
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 4.9 pIC50 = 4.9 Binding
Inhibitory concentration against beta-1-adrenergic receptor in isolated guinea pig atriaInhibitory concentration against beta-1-adrenergic receptor in isolated guinea pig atria
ChEMBL 188 5 2 4 0.8 CCO/N=C/C(O)CNC(C)(C)C 10.1021/jm00036a018
44268308 17910 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Tested for binding affinity against cloned human beta-1 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligand.Tested for binding affinity against cloned human beta-1 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 6.9 pIC50 = 6.9 Binding
Tested for binding affinity against cloned human beta-1 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligand.Tested for binding affinity against cloned human beta-1 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
46881698 7074 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]cyanopindolol from human beta 1 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 1 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 5.9 pIC50 = 5.9 Binding
Displacement of [125I]cyanopindolol from human beta 1 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 1 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
44298288 101099 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
In vitro binding affinity towards cloned human beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-1 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 5.9 pIC50 = 5.9 Binding
In vitro binding affinity towards cloned human beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-1 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
44298515 194165 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
In vitro binding affinity towards cloned human beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-1 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 5.9 pIC50 = 5.9 Binding
In vitro binding affinity towards cloned human beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-1 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
44457929 84339 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibitory activity against cloned human Beta-1 adrenergic receptor in the presence of [125I]iodocyanopindolol in CHO cells by receptor binding assayInhibitory activity against cloned human Beta-1 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 5.9 pIC50 = 5.9 Binding
Inhibitory activity against cloned human Beta-1 adrenergic receptor in the presence of [125I]iodocyanopindolol in CHO cells by receptor binding assayInhibitory activity against cloned human Beta-1 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
91965 206280 88 None - 2 Human 4.9 pIC50 = 4.9 Binding
Binding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterolBinding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterol
ChEMBL 176 1 1 2 1.4 Cc1ccccc1N1CCNCC1 10.1021/jm00082a016
CHEMBL9746 206280 88 None - 2 Human 4.9 pIC50 = 4.9 Binding
Binding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterolBinding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterol
ChEMBL 176 1 1 2 1.4 Cc1ccccc1N1CCNCC1 10.1021/jm00082a016
145946965 167024 0 None - 1 Rat 5.9 pIC50 = 5.9 Binding
Displacement of [3H]-CGP-12177 from adrenergic beta1 receptor in Wistar rat cortex incubated for 60 mins by microbeta liquid scintillation counting analysisDisplacement of [3H]-CGP-12177 from adrenergic beta1 receptor in Wistar rat cortex incubated for 60 mins by microbeta liquid scintillation counting analysis
ChEMBL 431 6 1 7 2.9 O=c1c2ccccc2oc2c(OCC(O)CN3CCN(c4ccccn4)CC3)cccc12 10.1016/j.bmc.2018.04.038
CHEMBL4126588 167024 0 None - 1 Rat 5.9 pIC50 = 5.9 Binding
Displacement of [3H]-CGP-12177 from adrenergic beta1 receptor in Wistar rat cortex incubated for 60 mins by microbeta liquid scintillation counting analysisDisplacement of [3H]-CGP-12177 from adrenergic beta1 receptor in Wistar rat cortex incubated for 60 mins by microbeta liquid scintillation counting analysis
ChEMBL 431 6 1 7 2.9 O=c1c2ccccc2oc2c(OCC(O)CN3CCN(c4ccccn4)CC3)cccc12 10.1016/j.bmc.2018.04.038
CHEMBL4300897 167024 0 None - 1 Rat 5.9 pIC50 = 5.9 Binding
Displacement of [3H]-CGP-12177 from adrenergic beta1 receptor in Wistar rat cortex incubated for 60 mins by microbeta liquid scintillation counting analysisDisplacement of [3H]-CGP-12177 from adrenergic beta1 receptor in Wistar rat cortex incubated for 60 mins by microbeta liquid scintillation counting analysis
ChEMBL 431 6 1 7 2.9 O=c1c2ccccc2oc2c(OCC(O)CN3CCN(c4ccccn4)CC3)cccc12 10.1016/j.bmc.2018.04.038
2464 3570 52 None -2 6 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C nan
5253 3570 52 None -2 6 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C nan
7297 3570 52 None -2 6 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C nan
CHEMBL471 3570 52 None -2 6 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C nan
DB00489 3570 52 None -2 6 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C nan
44268249 19299 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Tested for binding affinity against cloned human beta-1 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandTested for binding affinity against cloned human beta-1 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 7.8 pIC50 = 7.8 Binding
Tested for binding affinity against cloned human beta-1 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandTested for binding affinity against cloned human beta-1 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
44268495 24811 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
In vitro affinity at Beta-1 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-1 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-1 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-1 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
44268496 97910 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
In vitro affinity at Beta-1 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-1 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 6.8 pIC50 = 6.8 Binding
In vitro affinity at Beta-1 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-1 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
44268320 18227 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Tested for binding affinity against cloned human beta-1 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligand.Tested for binding affinity against cloned human beta-1 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
Tested for binding affinity against cloned human beta-1 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligand.Tested for binding affinity against cloned human beta-1 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
44301618 197393 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cellsBinding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cells
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 5.8 pIC50 = 5.8 Binding
Binding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cellsBinding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cells
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
46881618 7917 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]cyanopindolol from human beta 1 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 1 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 1 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 1 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
44298769 195421 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
In vitro binding affinity towards cloned human beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-1 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 5.8 pIC50 = 5.8 Binding
In vitro binding affinity towards cloned human beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-1 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
97478 9821 96 None - 0 Human 4.8 pIC50 = 4.8 Binding
Binding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterolBinding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterol
ChEMBL 196 1 1 2 1.8 Clc1ccc(N2CCNCC2)cc1 10.1021/jm00082a016
CHEMBL114478 9821 96 None - 0 Human 4.8 pIC50 = 4.8 Binding
Binding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterolBinding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterol
ChEMBL 196 1 1 2 1.8 Clc1ccc(N2CCNCC2)cc1 10.1021/jm00082a016
10103956 11081 0 None - 2 Guinea pig 4.8 pIC50 = 4.8 Binding
Inhibitory concentration against beta-1-adrenergic receptor in isolated guinea pig atriaInhibitory concentration against beta-1-adrenergic receptor in isolated guinea pig atria
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 4.8 pIC50 = 4.8 Binding
Inhibitory concentration against beta-1-adrenergic receptor in isolated guinea pig atriaInhibitory concentration against beta-1-adrenergic receptor in isolated guinea pig atria
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 4.8 pIC50 = 4.8 Binding
Inhibitory concentration against beta-1-adrenergic receptor in isolated guinea pig atriaInhibitory concentration against beta-1-adrenergic receptor in isolated guinea pig atria
ChEMBL 188 7 2 4 0.8 CC/C=N/OCC(O)CNC(C)C 10.1021/jm00036a018
9990035 11901 0 None - 2 Guinea pig 4.8 pIC50 = 4.8 Binding
Inhibitory concentration against beta-1-adrenergic receptor in isolated guinea pig atriaInhibitory concentration against beta-1-adrenergic receptor in isolated guinea pig atria
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 4.8 pIC50 = 4.8 Binding
Inhibitory concentration against beta-1-adrenergic receptor in isolated guinea pig atriaInhibitory concentration against beta-1-adrenergic receptor in isolated guinea pig atria
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 4.8 pIC50 = 4.8 Binding
Inhibitory concentration against beta-1-adrenergic receptor in isolated guinea pig atriaInhibitory concentration against beta-1-adrenergic receptor in isolated guinea pig atria
ChEMBL 188 7 2 4 0.8 CCCO/N=C/C(O)CNC(C)C 10.1021/jm00036a018
16049450 63747 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to adrenergic beta1 receptorBinding affinity to adrenergic beta1 receptor
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 - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to adrenergic beta1 receptorBinding affinity to adrenergic beta1 receptor
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
56670158 63750 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to adrenergic beta1 receptorBinding affinity to adrenergic beta1 receptor
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 - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to adrenergic beta1 receptorBinding affinity to adrenergic beta1 receptor
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
24901210 69970 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of radiolabeled iodocyanopindolol from beta1 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from beta1 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 6.8 pIC50 = 6.8 Binding
Displacement of radiolabeled iodocyanopindolol from beta1 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from beta1 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
24900685 69999 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of radiolabeled iodocyanopindolol from beta1 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from beta1 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 6.8 pIC50 = 6.8 Binding
Displacement of radiolabeled iodocyanopindolol from beta1 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from beta1 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
24901283 70024 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of radiolabeled iodocyanopindolol from beta1 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from beta1 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 6.8 pIC50 = 6.8 Binding
Displacement of radiolabeled iodocyanopindolol from beta1 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from beta1 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
10282871 16357 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity for human Beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity for human Beta-1 adrenergic receptor 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 7.8 pIC50 = 7.8 Binding
Binding affinity for human Beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity for human Beta-1 adrenergic receptor 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
44335534 4743 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Beta-1 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-1 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 6.8 pIC50 = 6.8 Binding
Beta-1 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-1 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
44338543 5849 0 None - 0 Guinea pig 6.8 pIC50 = 6.8 Binding
Beta-1 adrenergic receptor blocking was assessed from 50% inhibition of the isoproterenol submaximal response on isolated Guinea pig atria(IA)Beta-1 adrenergic receptor blocking was assessed from 50% inhibition of the isoproterenol submaximal response on isolated Guinea pig atria(IA)
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 6.8 pIC50 = 6.8 Binding
Beta-1 adrenergic receptor blocking was assessed from 50% inhibition of the isoproterenol submaximal response on isolated Guinea pig atria(IA)Beta-1 adrenergic receptor blocking was assessed from 50% inhibition of the isoproterenol submaximal response on isolated Guinea pig atria(IA)
ChEMBL 374 6 2 5 3.6 COC12CCCCCC1c1ccccc1/C2=N/OCC(O)CNC(C)(C)C 10.1021/jm00122a008
131847 55771 7 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterolBinding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterol
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 Human 6.8 pIC50 = 6.8 Binding
Binding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterolBinding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterol
ChEMBL 388 6 3 5 1.3 CS(=O)(=O)Nc1ccc(C(=O)NCC2CN(c3ccccc3)CCN2)cc1 10.1021/jm00082a016
44301819 100580 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cellsBinding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cells
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 5.8 pIC50 = 5.8 Binding
Binding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cellsBinding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cells
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
208932 13431 8 None - 0 Human 5.8 pIC50 = 5.8 Binding
Tested for Beta-1 adrenergic receptor selectivity in canine cardiac tissue in anesthetized dogsTested for Beta-1 adrenergic receptor selectivity in canine cardiac 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 - 0 Human 5.8 pIC50 = 5.8 Binding
Tested for Beta-1 adrenergic receptor selectivity in canine cardiac tissue in anesthetized dogsTested for Beta-1 adrenergic receptor selectivity in canine cardiac 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 - 0 Human 5.8 pIC50 = 5.8 Binding
Tested for Beta-1 adrenergic receptor selectivity in canine cardiac tissue in anesthetized dogsTested for Beta-1 adrenergic receptor selectivity in canine cardiac 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
44281531 100043 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Binding affinity to recombinant human beta-1 adrenergic receptor expressed in CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-1 adrenergic receptor expressed in 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 4.8 pIC50 = 4.8 Binding
Binding affinity to recombinant human beta-1 adrenergic receptor expressed in CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-1 adrenergic receptor expressed in 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
46881796 5507 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [125I]cyanopindolol from human beta 1 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 1 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 4.8 pIC50 = 4.8 Binding
Displacement of [125I]cyanopindolol from human beta 1 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 1 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
2249 509 106 None -5 12 Human 5.8 pIC50 = 5.8 Binding
Inhibition of human alpha1 adrenoceptorInhibition of human alpha1 adrenoceptor
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1016/j.bmc.2010.07.034
255 509 106 None -5 12 Human 5.8 pIC50 = 5.8 Binding
Inhibition of human alpha1 adrenoceptorInhibition of human alpha1 adrenoceptor
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1016/j.bmc.2010.07.034
548 509 106 None -5 12 Human 5.8 pIC50 = 5.8 Binding
Inhibition of human alpha1 adrenoceptorInhibition of human alpha1 adrenoceptor
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1016/j.bmc.2010.07.034
CHEMBL24 509 106 None -5 12 Human 5.8 pIC50 = 5.8 Binding
Inhibition of human alpha1 adrenoceptorInhibition of human alpha1 adrenoceptor
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1016/j.bmc.2010.07.034
DB00335 509 106 None -5 12 Human 5.8 pIC50 = 5.8 Binding
Inhibition of human alpha1 adrenoceptorInhibition of human alpha1 adrenoceptor
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1016/j.bmc.2010.07.034
16118894 2203 3 None - 0 Human 6.8 pIC50 = 6.8 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-1 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-1 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 6.8 pIC50 = 6.8 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-1 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-1 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 6.8 pIC50 = 6.8 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-1 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-1 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
16118894 2203 3 None - 0 Human 6.8 pIC50 = 6.8 Binding
Tested for binding affinity against cloned human beta-1 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandTested for binding affinity against cloned human beta-1 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 6.8 pIC50 = 6.8 Binding
Tested for binding affinity against cloned human beta-1 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandTested for binding affinity against cloned human beta-1 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 6.8 pIC50 = 6.8 Binding
Tested for binding affinity against cloned human beta-1 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandTested for binding affinity against cloned human beta-1 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
11758172 100454 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cellsBinding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cells
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 (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cellsBinding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cells
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
14998849 56206 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterolBinding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterol
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 Human 5.8 pIC50 = 5.8 Binding
Binding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterolBinding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterol
ChEMBL 418 7 3 6 1.3 COc1cccc(N2CCNC(CNC(=O)c3ccc(NS(C)(=O)=O)cc3)C2)c1 10.1021/jm00082a016
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-1 adrenergic receptor in the presence of [125I]- iodocyanopindolol.Binding affinity was evaluated on chinese hamster ovary (CHO) cells expressing the cloned human beta-1 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-1 adrenergic receptor in the presence of [125I]- iodocyanopindolol.Binding affinity was evaluated on chinese hamster ovary (CHO) cells expressing the cloned human beta-1 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
46881983 5675 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]cyanopindolol from human beta 1 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 1 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counter
ChEMBL 477 9 4 5 4.7 O=C(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccccc1-c1nc2ccccc2[nH]1 10.1016/j.bmcl.2010.01.130
CHEMBL1078575 5675 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]cyanopindolol from human beta 1 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 1 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counter
ChEMBL 477 9 4 5 4.7 O=C(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccccc1-c1nc2ccccc2[nH]1 10.1016/j.bmcl.2010.01.130
208932 13431 8 None - 0 Human 5.8 pIC50 = 5.8 Binding
In vitro Beta-1 adrenergic receptor affinity in partially purified membrane fractions from canine cardiac tissue using [SH]dihydroalprenolol (4.5 nM)In vitro Beta-1 adrenergic receptor affinity in partially purified membrane fractions from canine cardiac 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 Human 5.8 pIC50 = 5.8 Binding
In vitro Beta-1 adrenergic receptor affinity in partially purified membrane fractions from canine cardiac tissue using [SH]dihydroalprenolol (4.5 nM)In vitro Beta-1 adrenergic receptor affinity in partially purified membrane fractions from canine cardiac 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 Human 5.8 pIC50 = 5.8 Binding
In vitro Beta-1 adrenergic receptor affinity in partially purified membrane fractions from canine cardiac tissue using [SH]dihydroalprenolol (4.5 nM)In vitro Beta-1 adrenergic receptor affinity in partially purified membrane fractions from canine cardiac 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
71612644 132829 0 None 2 2 Human 4.8 pIC50 = 4.8 Binding
Inhibition Assay: Human recombinant adrenergic β1 receptors expressed in CHO-K1 cells are used in modified Tris-HCl buffer pH 7.4. A 25 aliquot is incubated with 0.03 nM [125I]Cyanopindolol for 120 minutes at 25° C. Non-specific binding is estimated in the presence of 100 μM S(−)-Propranolol. Receptors are filtered and washed, the filters are then counted to determine [125I]Cyanopindolol specifically bound. Compounds are screened at 10 μM.Inhibition Assay: Human recombinant adrenergic β1 receptors expressed in CHO-K1 cells are used in modified Tris-HCl buffer pH 7.4. A 25 aliquot is incubated with 0.03 nM [125I]Cyanopindolol for 120 minutes at 25° C. Non-specific binding is estimated in the presence of 100 μM S(−)-Propranolol. Receptors are filtered and washed, the filters are then counted to determine [125I]Cyanopindolol 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 4.8 pIC50 = 4.8 Binding
Inhibition Assay: Human recombinant adrenergic β1 receptors expressed in CHO-K1 cells are used in modified Tris-HCl buffer pH 7.4. A 25 aliquot is incubated with 0.03 nM [125I]Cyanopindolol for 120 minutes at 25° C. Non-specific binding is estimated in the presence of 100 μM S(−)-Propranolol. Receptors are filtered and washed, the filters are then counted to determine [125I]Cyanopindolol specifically bound. Compounds are screened at 10 μM.Inhibition Assay: Human recombinant adrenergic β1 receptors expressed in CHO-K1 cells are used in modified Tris-HCl buffer pH 7.4. A 25 aliquot is incubated with 0.03 nM [125I]Cyanopindolol for 120 minutes at 25° C. Non-specific binding is estimated in the presence of 100 μM S(−)-Propranolol. Receptors are filtered and washed, the filters are then counted to determine [125I]Cyanopindolol specifically bound. Compounds are screened at 10 μM.
ChEMBL 303 7 2 5 0.5 N#CC1CCCN1C(=O)CNCC(O)COc1ccccc1 nan
1016 3678 75 None -43 35 Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2561 3678 75 None -43 35 Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2733526 3678 75 None -43 35 Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
5384 3678 75 None -43 35 Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
CHEMBL83 3678 75 None -43 35 Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
DB00675 3678 75 None -43 35 Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2247 502 77 None -128 42 Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
249 502 77 None -128 42 Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
2603 502 77 None -128 42 Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
CHEMBL296419 502 77 None -128 42 Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
DB00637 502 77 None -128 42 Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
2249 509 106 None -5 12 Human 5.8 pIC50 = 5.8 Binding
Inhibition of human beta 1 adrenergic receptorInhibition of human beta 1 adrenergic receptor
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1021/jm701575k
255 509 106 None -5 12 Human 5.8 pIC50 = 5.8 Binding
Inhibition of human beta 1 adrenergic receptorInhibition of human beta 1 adrenergic receptor
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1021/jm701575k
548 509 106 None -5 12 Human 5.8 pIC50 = 5.8 Binding
Inhibition of human beta 1 adrenergic receptorInhibition of human beta 1 adrenergic receptor
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1021/jm701575k
CHEMBL24 509 106 None -5 12 Human 5.8 pIC50 = 5.8 Binding
Inhibition of human beta 1 adrenergic receptorInhibition of human beta 1 adrenergic receptor
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1021/jm701575k
DB00335 509 106 None -5 12 Human 5.8 pIC50 = 5.8 Binding
Inhibition of human beta 1 adrenergic receptorInhibition of human beta 1 adrenergic receptor
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1021/jm701575k
1786 2474 79 None -1 11 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O nan
4171 2474 79 None -1 11 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O nan
553 2474 79 None -1 11 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O nan
CHEMBL13 2474 79 None -1 11 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O nan
DB00264 2474 79 None -1 11 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O nan
145946488 166965 0 None -46 2 Rat 6.8 pIC50 = 6.8 Binding
Displacement of [3H]-CGP-12177 from adrenergic beta1 receptor in Wistar rat cortex incubated for 60 mins by microbeta liquid scintillation counting analysisDisplacement of [3H]-CGP-12177 from adrenergic beta1 receptor in Wistar rat cortex incubated for 60 mins by microbeta liquid scintillation counting analysis
ChEMBL 435 10 2 7 3.4 COc1ccccc1OCCNCC(O)COc1cccc2c(=O)c3ccccc3oc12 10.1016/j.bmc.2018.04.038
CHEMBL4127540 166965 0 None -46 2 Rat 6.8 pIC50 = 6.8 Binding
Displacement of [3H]-CGP-12177 from adrenergic beta1 receptor in Wistar rat cortex incubated for 60 mins by microbeta liquid scintillation counting analysisDisplacement of [3H]-CGP-12177 from adrenergic beta1 receptor in Wistar rat cortex incubated for 60 mins by microbeta liquid scintillation counting analysis
ChEMBL 435 10 2 7 3.4 COc1ccccc1OCCNCC(O)COc1cccc2c(=O)c3ccccc3oc12 10.1016/j.bmc.2018.04.038
CHEMBL4300195 166965 0 None -46 2 Rat 6.8 pIC50 = 6.8 Binding
Displacement of [3H]-CGP-12177 from adrenergic beta1 receptor in Wistar rat cortex incubated for 60 mins by microbeta liquid scintillation counting analysisDisplacement of [3H]-CGP-12177 from adrenergic beta1 receptor in Wistar rat cortex incubated for 60 mins by microbeta liquid scintillation counting analysis
ChEMBL 435 10 2 7 3.4 COc1ccccc1OCCNCC(O)COc1cccc2c(=O)c3ccccc3oc12 10.1016/j.bmc.2018.04.038
145947665 167110 0 None 10 2 Rat 6.8 pIC50 = 6.8 Binding
Displacement of [3H]-CGP-12177 from adrenergic beta1 receptor in Wistar rat cortex incubated for 60 mins by microbeta liquid scintillation counting analysisDisplacement of [3H]-CGP-12177 from adrenergic beta1 receptor in Wistar rat cortex incubated for 60 mins by microbeta liquid scintillation counting analysis
ChEMBL 405 8 2 6 3.5 COc1ccccc1CNCC(O)COc1cccc2c(=O)c3ccccc3oc12 10.1016/j.bmc.2018.04.038
CHEMBL4128794 167110 0 None 10 2 Rat 6.8 pIC50 = 6.8 Binding
Displacement of [3H]-CGP-12177 from adrenergic beta1 receptor in Wistar rat cortex incubated for 60 mins by microbeta liquid scintillation counting analysisDisplacement of [3H]-CGP-12177 from adrenergic beta1 receptor in Wistar rat cortex incubated for 60 mins by microbeta liquid scintillation counting analysis
ChEMBL 405 8 2 6 3.5 COc1ccccc1CNCC(O)COc1cccc2c(=O)c3ccccc3oc12 10.1016/j.bmc.2018.04.038
CHEMBL4302144 167110 0 None 10 2 Rat 6.8 pIC50 = 6.8 Binding
Displacement of [3H]-CGP-12177 from adrenergic beta1 receptor in Wistar rat cortex incubated for 60 mins by microbeta liquid scintillation counting analysisDisplacement of [3H]-CGP-12177 from adrenergic beta1 receptor in Wistar rat cortex incubated for 60 mins by microbeta liquid scintillation counting analysis
ChEMBL 405 8 2 6 3.5 COc1ccccc1CNCC(O)COc1cccc2c(=O)c3ccccc3oc12 10.1016/j.bmc.2018.04.038
165193 3126 60 None -2 43 Human 7.8 pIC50 = 7.8 Binding
Tested for Beta-1 adrenergic receptor selectivity in canine cardiac tissue in anesthetized dogsTested for Beta-1 adrenergic receptor selectivity in canine cardiac tissue in anesthetized dogs
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00172a033
2303 3126 60 None -2 43 Human 7.8 pIC50 = 7.8 Binding
Tested for Beta-1 adrenergic receptor selectivity in canine cardiac tissue in anesthetized dogsTested for Beta-1 adrenergic receptor selectivity in canine cardiac tissue in anesthetized dogs
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00172a033
4946 3126 60 None -2 43 Human 7.8 pIC50 = 7.8 Binding
Tested for Beta-1 adrenergic receptor selectivity in canine cardiac tissue in anesthetized dogsTested for Beta-1 adrenergic receptor selectivity in canine cardiac tissue in anesthetized dogs
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00172a033
564 3126 60 None -2 43 Human 7.8 pIC50 = 7.8 Binding
Tested for Beta-1 adrenergic receptor selectivity in canine cardiac tissue in anesthetized dogsTested for Beta-1 adrenergic receptor selectivity in canine cardiac tissue in anesthetized dogs
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00172a033
62882 3126 60 None -2 43 Human 7.8 pIC50 = 7.8 Binding
Tested for Beta-1 adrenergic receptor selectivity in canine cardiac tissue in anesthetized dogsTested for Beta-1 adrenergic receptor selectivity in canine cardiac tissue in anesthetized dogs
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00172a033
63 3126 60 None -2 43 Human 7.8 pIC50 = 7.8 Binding
Tested for Beta-1 adrenergic receptor selectivity in canine cardiac tissue in anesthetized dogsTested for Beta-1 adrenergic receptor selectivity in canine cardiac tissue in anesthetized dogs
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00172a033
66366 3126 60 None -2 43 Human 7.8 pIC50 = 7.8 Binding
Tested for Beta-1 adrenergic receptor selectivity in canine cardiac tissue in anesthetized dogsTested for Beta-1 adrenergic receptor selectivity in canine cardiac tissue in anesthetized dogs
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00172a033
91536 3126 60 None -2 43 Human 7.8 pIC50 = 7.8 Binding
Tested for Beta-1 adrenergic receptor selectivity in canine cardiac tissue in anesthetized dogsTested for Beta-1 adrenergic receptor selectivity in canine cardiac tissue in anesthetized dogs
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00172a033
CHEMBL27 3126 60 None -2 43 Human 7.8 pIC50 = 7.8 Binding
Tested for Beta-1 adrenergic receptor selectivity in canine cardiac tissue in anesthetized dogsTested for Beta-1 adrenergic receptor selectivity in canine cardiac tissue in anesthetized dogs
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00172a033
CHEMBL452861 3126 60 None -2 43 Human 7.8 pIC50 = 7.8 Binding
Tested for Beta-1 adrenergic receptor selectivity in canine cardiac tissue in anesthetized dogsTested for Beta-1 adrenergic receptor selectivity in canine cardiac tissue in anesthetized dogs
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00172a033
DB00571 3126 60 None -2 43 Human 7.8 pIC50 = 7.8 Binding
Tested for Beta-1 adrenergic receptor selectivity in canine cardiac tissue in anesthetized dogsTested for Beta-1 adrenergic receptor selectivity in canine cardiac tissue in anesthetized dogs
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00172a033
9933039 162483 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Tested for binding affinity against cloned human beta-1 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandTested for binding affinity against cloned human beta-1 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 6.8 pIC50 = 6.8 Binding
Tested for binding affinity against cloned human beta-1 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandTested for binding affinity against cloned human beta-1 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
44349356 116470 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity for human Beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity for human Beta-1 adrenergic receptor 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 5.8 pIC50 = 5.8 Binding
Binding affinity for human Beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity for human Beta-1 adrenergic receptor 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
10627736 116482 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-1 adrenergic receptor in the presence of [125I]- iodocyanopindolol.Binding affinity was evaluated on chinese hamster ovary (CHO) cells expressing the cloned human beta-1 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 5.8 pIC50 = 5.8 Binding
Binding affinity was evaluated on chinese hamster ovary (CHO) cells expressing the cloned human beta-1 adrenergic receptor in the presence of [125I]- iodocyanopindolol.Binding affinity was evaluated on chinese hamster ovary (CHO) cells expressing the cloned human beta-1 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
44312924 164263 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Compound was evaluated for its inhibitory activity against CHO cells expressing the cloned human beta-1 adrenergic receptor (AR) in the presence of [125I]-iodocyanopindololCompound was evaluated for its inhibitory activity against CHO cells expressing the cloned human beta-1 adrenergic receptor (AR) in the presence of [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 5.8 pIC50 = 5.8 Binding
Compound was evaluated for its inhibitory activity against CHO cells expressing the cloned human beta-1 adrenergic receptor (AR) in the presence of [125I]-iodocyanopindololCompound was evaluated for its inhibitory activity against CHO cells expressing the cloned human beta-1 adrenergic receptor (AR) in the presence of [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
9826638 201599 1 None - 0 Human 5.8 pIC50 = 5.8 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-1 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-1 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 5.8 pIC50 = 5.8 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-1 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-1 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
44298695 100455 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
In vitro binding affinity towards cloned human beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-1 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 5.8 pIC50 = 5.8 Binding
In vitro binding affinity towards cloned human beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-1 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
44298843 194978 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
In vitro binding affinity towards cloned human beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-1 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 5.8 pIC50 = 5.8 Binding
In vitro binding affinity towards cloned human beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-1 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
10347866 84569 1 None - 0 Human 4.8 pIC50 = 4.8 Binding
Binding affinity towards Beta-1 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindololBinding affinity towards Beta-1 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 4.8 pIC50 = 4.8 Binding
Binding affinity towards Beta-1 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindololBinding affinity towards Beta-1 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
10347866 84569 1 None - 0 Human 4.8 pIC50 = 4.8 Binding
Binding affinity towards human Beta-1 adrenergic receptor expressed in CHO cells, using 125I]iodocyanopindololBinding affinity towards human Beta-1 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 4.8 pIC50 = 4.8 Binding
Binding affinity towards human Beta-1 adrenergic receptor expressed in CHO cells, using 125I]iodocyanopindololBinding affinity towards human Beta-1 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
14664347 13505 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
In vitro Beta-1 adrenergic receptor affinity in partially purified membrane fractions from canine cardiac tissue using [SH]dihydroalprenolol (4.5 nM)In vitro Beta-1 adrenergic receptor affinity in partially purified membrane fractions from canine cardiac tissue using [SH]dihydroalprenolol (4.5 nM)
ChEMBL 474 12 2 8 2.0 Cc1nccn1-c1ccc(OCCNCC(O)COc2ccc(N(C)S(C)(=O)=O)cc2)cc1 10.1021/jm00166a002
CHEMBL11944 13505 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
In vitro Beta-1 adrenergic receptor affinity in partially purified membrane fractions from canine cardiac tissue using [SH]dihydroalprenolol (4.5 nM)In vitro Beta-1 adrenergic receptor affinity in partially purified membrane fractions from canine cardiac tissue using [SH]dihydroalprenolol (4.5 nM)
ChEMBL 474 12 2 8 2.0 Cc1nccn1-c1ccc(OCCNCC(O)COc2ccc(N(C)S(C)(=O)=O)cc2)cc1 10.1021/jm00166a002
44276727 96852 0 None - 3 Human 6.7 pIC50 = 6.7 Binding
Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-1 adrenergic receptor in dog heart.Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-1 adrenergic receptor in dog heart.
ChEMBL 263 6 2 3 2.2 Cc1ccc(OCC(O)CNC(C)C)c2c1CCC2 10.1021/jm00350a009
CHEMBL26917 96852 0 None - 3 Human 6.7 pIC50 = 6.7 Binding
Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-1 adrenergic receptor in dog heart.Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-1 adrenergic receptor in dog heart.
ChEMBL 263 6 2 3 2.2 Cc1ccc(OCC(O)CNC(C)C)c2c1CCC2 10.1021/jm00350a009
24900426 70003 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of radiolabeled iodocyanopindolol from beta1 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from beta1 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 7.7 pIC50 = 7.7 Binding
Displacement of radiolabeled iodocyanopindolol from beta1 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from beta1 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
24901285 70029 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of radiolabeled iodocyanopindolol from beta1 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from beta1 adrenoceptor
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 - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of radiolabeled iodocyanopindolol from beta1 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from beta1 adrenoceptor
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
44268464 19198 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
In vitro affinity at Beta-1 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-1 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 6.7 pIC50 = 6.7 Binding
In vitro affinity at Beta-1 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-1 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
44268520 21024 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
In vitro affinity at Beta-1 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-1 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 6.7 pIC50 = 6.7 Binding
In vitro affinity at Beta-1 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-1 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
10746499 113947 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity was evaluated on chinese hamster ovary (CHO) cells expressing the cloned human beta-1 adrenergic receptor in the presence of [125I]- iodocyanopindolol.Binding affinity was evaluated on chinese hamster ovary (CHO) cells expressing the cloned human beta-1 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 5.7 pIC50 = 5.7 Binding
Binding affinity was evaluated on chinese hamster ovary (CHO) cells expressing the cloned human beta-1 adrenergic receptor in the presence of [125I]- iodocyanopindolol.Binding affinity was evaluated on chinese hamster ovary (CHO) cells expressing the cloned human beta-1 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
46882084 5689 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]cyanopindolol from human beta 1 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 1 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 5.7 pIC50 = 5.7 Binding
Displacement of [125I]cyanopindolol from human beta 1 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 1 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
46881901 7748 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]cyanopindolol from human beta 1 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 1 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 5.7 pIC50 = 5.7 Binding
Displacement of [125I]cyanopindolol from human beta 1 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 1 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
12017007 157821 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
In vitro binding affinity at beta-1 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-1 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-1 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-1 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
44338579 162739 0 None - 0 Guinea pig 4.7 pIC50 = 4.7 Binding
Beta-1 adrenergic receptor blocking was assessed from 50% inhibition of the isoproterenol submaximal response on isolated Guinea pig atria(IA)Beta-1 adrenergic receptor blocking was assessed from 50% inhibition of the isoproterenol submaximal response on isolated Guinea pig atria(IA)
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 4.7 pIC50 = 4.7 Binding
Beta-1 adrenergic receptor blocking was assessed from 50% inhibition of the isoproterenol submaximal response on isolated Guinea pig atria(IA)Beta-1 adrenergic receptor blocking was assessed from 50% inhibition of the isoproterenol submaximal response on isolated Guinea pig atria(IA)
ChEMBL 364 7 2 5 3.0 COC12CCCCC1c1ccc(F)cc1/C2=N/OCC(O)CNC(C)C 10.1021/jm00122a008
44301979 100382 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Binding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cellsBinding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cells
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 4.7 pIC50 = 4.7 Binding
Binding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cellsBinding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cells
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
7096 205735 111 None -21 4 Human 4.7 pIC50 = 4.7 Binding
Binding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterolBinding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterol
ChEMBL 162 1 1 2 1.1 c1ccc(N2CCNCC2)cc1 10.1021/jm00082a016
CHEMBL9434 205735 111 None -21 4 Human 4.7 pIC50 = 4.7 Binding
Binding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterolBinding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterol
ChEMBL 162 1 1 2 1.1 c1ccc(N2CCNCC2)cc1 10.1021/jm00082a016
46845699 5712 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Displacement of [125I]cyanopindolol from human beta 1 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 1 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 4.7 pIC50 = 4.7 Binding
Displacement of [125I]cyanopindolol from human beta 1 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 1 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
46881573 8174 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Displacement of [125I]cyanopindolol from human beta 1 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 1 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 4.7 pIC50 = 4.7 Binding
Displacement of [125I]cyanopindolol from human beta 1 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 1 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
14739897 206585 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Tested for Beta-1 adrenergic receptor selectivity in canine cardiac tissue in anesthetized dogsTested for Beta-1 adrenergic receptor selectivity in canine cardiac 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 Human 4.7 pIC50 = 4.7 Binding
Tested for Beta-1 adrenergic receptor selectivity in canine cardiac tissue in anesthetized dogsTested for Beta-1 adrenergic receptor selectivity in canine cardiac 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
36811 1421 34 None -93 7 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 301 7 4 4 3.0 CC(CCc1ccc(cc1)O)NCCc1ccc(c(c1)O)O nan
535 1421 34 None -93 7 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 301 7 4 4 3.0 CC(CCc1ccc(cc1)O)NCCc1ccc(c(c1)O)O nan
937 1421 34 None -93 7 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 301 7 4 4 3.0 CC(CCc1ccc(cc1)O)NCCc1ccc(c(c1)O)O nan
CHEMBL926 1421 34 None -93 7 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 301 7 4 4 3.0 CC(CCc1ccc(cc1)O)NCCc1ccc(c(c1)O)O nan
DB00841 1421 34 None -93 7 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 301 7 4 4 3.0 CC(CCc1ccc(cc1)O)NCCc1ccc(c(c1)O)O nan
1054 1549 49 None -1 3 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 295 9 2 5 1.5 COC(=O)CCc1ccc(cc1)OCC(CNC(C)C)O nan
59768 1549 49 None -1 3 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 295 9 2 5 1.5 COC(=O)CCc1ccc(cc1)OCC(CNC(C)C)O nan
7178 1549 49 None -1 3 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 295 9 2 5 1.5 COC(=O)CCc1ccc(cc1)OCC(CNC(C)C)O nan
CHEMBL768 1549 49 None -1 3 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 295 9 2 5 1.5 COC(=O)CCc1ccc(cc1)OCC(CNC(C)C)O nan
DB00187 1549 49 None -1 3 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 295 9 2 5 1.5 COC(=O)CCc1ccc(cc1)OCC(CNC(C)C)O nan
12043157 116237 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity towards cloned human Beta-1 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity towards cloned human Beta-1 adrenergic receptor prepared from CHO cells 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 5.7 pIC50 = 5.7 Binding
Binding affinity towards cloned human Beta-1 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity towards cloned human Beta-1 adrenergic receptor prepared from CHO cells 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
24900749 70023 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of radiolabeled iodocyanopindolol from beta1 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from beta1 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 6.7 pIC50 = 6.7 Binding
Displacement of radiolabeled iodocyanopindolol from beta1 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from beta1 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
57400229 70030 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of radiolabeled iodocyanopindolol from beta1 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from beta1 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 6.7 pIC50 = 6.7 Binding
Displacement of radiolabeled iodocyanopindolol from beta1 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from beta1 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
10346448 119312 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Receptor binding assay(Beta-1 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-1 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 5.7 pIC50 = 5.7 Binding
Receptor binding assay(Beta-1 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-1 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
70683107 72741 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assayDisplacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assay
ChEMBL 416 10 5 6 1.5 N#Cc1ccc(F)cc1OC[C@@H](O)CNCCNC(=O)Nc1ccc(C(=O)O)cc1 10.1021/ml1002458
CHEMBL2011221 72741 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assayDisplacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assay
ChEMBL 416 10 5 6 1.5 N#Cc1ccc(F)cc1OC[C@@H](O)CNCCNC(=O)Nc1ccc(C(=O)O)cc1 10.1021/ml1002458
70693599 72743 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assayDisplacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assay
ChEMBL 416 11 4 6 2.2 CCOc1ccc(NC(=O)NCCNC[C@H](O)COc2cccc(F)c2C#N)cc1 10.1021/ml1002458
CHEMBL2011223 72743 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assayDisplacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assay
ChEMBL 416 11 4 6 2.2 CCOc1ccc(NC(=O)NCCNC[C@H](O)COc2cccc(F)c2C#N)cc1 10.1021/ml1002458
165193 3126 60 None -2 43 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Cynopindolol from human recombinant beta1 adrenergic receptor expressed in CHOK1 cells after 2 hrsDisplacement of [125I]Cynopindolol from human recombinant beta1 adrenergic receptor expressed in CHOK1 cells after 2 hrs
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmcl.2013.01.025
2303 3126 60 None -2 43 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Cynopindolol from human recombinant beta1 adrenergic receptor expressed in CHOK1 cells after 2 hrsDisplacement of [125I]Cynopindolol from human recombinant beta1 adrenergic receptor expressed in CHOK1 cells after 2 hrs
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmcl.2013.01.025
4946 3126 60 None -2 43 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Cynopindolol from human recombinant beta1 adrenergic receptor expressed in CHOK1 cells after 2 hrsDisplacement of [125I]Cynopindolol from human recombinant beta1 adrenergic receptor expressed in CHOK1 cells after 2 hrs
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmcl.2013.01.025
564 3126 60 None -2 43 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Cynopindolol from human recombinant beta1 adrenergic receptor expressed in CHOK1 cells after 2 hrsDisplacement of [125I]Cynopindolol from human recombinant beta1 adrenergic receptor expressed in CHOK1 cells after 2 hrs
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmcl.2013.01.025
62882 3126 60 None -2 43 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Cynopindolol from human recombinant beta1 adrenergic receptor expressed in CHOK1 cells after 2 hrsDisplacement of [125I]Cynopindolol from human recombinant beta1 adrenergic receptor expressed in CHOK1 cells after 2 hrs
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmcl.2013.01.025
63 3126 60 None -2 43 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Cynopindolol from human recombinant beta1 adrenergic receptor expressed in CHOK1 cells after 2 hrsDisplacement of [125I]Cynopindolol from human recombinant beta1 adrenergic receptor expressed in CHOK1 cells after 2 hrs
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmcl.2013.01.025
66366 3126 60 None -2 43 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Cynopindolol from human recombinant beta1 adrenergic receptor expressed in CHOK1 cells after 2 hrsDisplacement of [125I]Cynopindolol from human recombinant beta1 adrenergic receptor expressed in CHOK1 cells after 2 hrs
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmcl.2013.01.025
91536 3126 60 None -2 43 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Cynopindolol from human recombinant beta1 adrenergic receptor expressed in CHOK1 cells after 2 hrsDisplacement of [125I]Cynopindolol from human recombinant beta1 adrenergic receptor expressed in CHOK1 cells after 2 hrs
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmcl.2013.01.025
CHEMBL27 3126 60 None -2 43 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Cynopindolol from human recombinant beta1 adrenergic receptor expressed in CHOK1 cells after 2 hrsDisplacement of [125I]Cynopindolol from human recombinant beta1 adrenergic receptor expressed in CHOK1 cells after 2 hrs
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmcl.2013.01.025
CHEMBL452861 3126 60 None -2 43 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Cynopindolol from human recombinant beta1 adrenergic receptor expressed in CHOK1 cells after 2 hrsDisplacement of [125I]Cynopindolol from human recombinant beta1 adrenergic receptor expressed in CHOK1 cells after 2 hrs
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmcl.2013.01.025
DB00571 3126 60 None -2 43 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Cynopindolol from human recombinant beta1 adrenergic receptor expressed in CHOK1 cells after 2 hrsDisplacement of [125I]Cynopindolol from human recombinant beta1 adrenergic receptor expressed in CHOK1 cells after 2 hrs
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmcl.2013.01.025
165193 3126 60 None -2 43 Human 8.6 pIC50 = 8.6 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
2303 3126 60 None -2 43 Human 8.6 pIC50 = 8.6 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
4946 3126 60 None -2 43 Human 8.6 pIC50 = 8.6 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
564 3126 60 None -2 43 Human 8.6 pIC50 = 8.6 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
62882 3126 60 None -2 43 Human 8.6 pIC50 = 8.6 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
63 3126 60 None -2 43 Human 8.6 pIC50 = 8.6 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
66366 3126 60 None -2 43 Human 8.6 pIC50 = 8.6 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
91536 3126 60 None -2 43 Human 8.6 pIC50 = 8.6 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
CHEMBL27 3126 60 None -2 43 Human 8.6 pIC50 = 8.6 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
CHEMBL452861 3126 60 None -2 43 Human 8.6 pIC50 = 8.6 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
DB00571 3126 60 None -2 43 Human 8.6 pIC50 = 8.6 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
33624 3749 29 None -7 9 Human 8.6 pIC50 = 8.6 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C nan
4061 3749 29 None -7 9 Human 8.6 pIC50 = 8.6 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C nan
565 3749 29 None -7 9 Human 8.6 pIC50 = 8.6 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C nan
CHEMBL499 3749 29 None -7 9 Human 8.6 pIC50 = 8.6 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C nan
DB00373 3749 29 None -7 9 Human 8.6 pIC50 = 8.6 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C nan
70680983 72751 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assayDisplacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assay
ChEMBL 348 8 3 6 -0.1 N#Cc1ccccc1OC[C@@H](O)CNCCNC(=O)N1CCOCC1 10.1021/ml1002458
CHEMBL2011232 72751 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assayDisplacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assay
ChEMBL 348 8 3 6 -0.1 N#Cc1ccccc1OC[C@@H](O)CNCCNC(=O)N1CCOCC1 10.1021/ml1002458
3931 2208 42 None -3 2 Human 6.7 pIC50 = 6.7 Binding
In vitro affinity at Beta-1 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-1 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-1 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-1 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-1 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-1 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
44268604 36379 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
In vitro affinity at Beta-1 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-1 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-1 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-1 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
44285529 150373 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
In vitro binding affinity at beta-1 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-1 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 6.7 pIC50 = 6.7 Binding
In vitro binding affinity at beta-1 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-1 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
44335618 4704 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Beta-1 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-1 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 5.7 pIC50 = 5.7 Binding
Beta-1 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-1 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
44335560 5228 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Beta-1 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-1 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 5.7 pIC50 = 5.7 Binding
Beta-1 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-1 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
44335589 108887 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Beta-1 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-1 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindolol
ChEMBL 540 15 4 7 4.9 CCCCCCOC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(98)00571-x
CHEMBL321957 108887 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Beta-1 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-1 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindolol
ChEMBL 540 15 4 7 4.9 CCCCCCOC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(98)00571-x
1346 83 108 None - 9 Human 5.7 pIC50 = 5.7 Binding
Binding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterolBinding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterol
ChEMBL 192 2 1 3 1.1 COc1ccccc1N1CCNCC1 10.1021/jm00082a016
280 83 108 None - 9 Human 5.7 pIC50 = 5.7 Binding
Binding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterolBinding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterol
ChEMBL 192 2 1 3 1.1 COc1ccccc1N1CCNCC1 10.1021/jm00082a016
9899402 83 108 None - 9 Human 5.7 pIC50 = 5.7 Binding
Binding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterolBinding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterol
ChEMBL 192 2 1 3 1.1 COc1ccccc1N1CCNCC1 10.1021/jm00082a016
CHEMBL9666 83 108 None - 9 Human 5.7 pIC50 = 5.7 Binding
Binding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterolBinding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterol
ChEMBL 192 2 1 3 1.1 COc1ccccc1N1CCNCC1 10.1021/jm00082a016
1355 1972 82 None - 16 Human 5.7 pIC50 = 5.7 Binding
Binding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterolBinding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterol
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm00082a016
142 1972 82 None - 16 Human 5.7 pIC50 = 5.7 Binding
Binding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterolBinding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterol
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm00082a016
CHEMBL478 1972 82 None - 16 Human 5.7 pIC50 = 5.7 Binding
Binding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterolBinding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterol
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm00082a016
DB12110 1972 82 None - 16 Human 5.7 pIC50 = 5.7 Binding
Binding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterolBinding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterol
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm00082a016
10438390 201702 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity for cloned human Beta-1 adrenergic receptor expressed in CHO cells, tested in the presence of I-iodocyanopindolol.Binding affinity for cloned human Beta-1 adrenergic receptor expressed in CHO cells, tested 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 5.7 pIC50 = 5.7 Binding
Binding affinity for cloned human Beta-1 adrenergic receptor expressed in CHO cells, tested in the presence of I-iodocyanopindolol.Binding affinity for cloned human Beta-1 adrenergic receptor expressed in CHO cells, tested 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
44281344 99369 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity to recombinant human beta-1 adrenergic receptor expressed in CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-1 adrenergic receptor expressed in 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 5.7 pIC50 = 5.7 Binding
Binding affinity to recombinant human beta-1 adrenergic receptor expressed in CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-1 adrenergic receptor expressed in 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
44281255 114982 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity to recombinant human beta-1 adrenergic receptor expressed in CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-1 adrenergic receptor expressed in 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 5.7 pIC50 = 5.7 Binding
Binding affinity to recombinant human beta-1 adrenergic receptor expressed in CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-1 adrenergic receptor expressed in 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
44281384 118794 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity to recombinant human beta-1 adrenergic receptor expressed in CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-1 adrenergic receptor expressed in 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 5.7 pIC50 = 5.7 Binding
Binding affinity to recombinant human beta-1 adrenergic receptor expressed in CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-1 adrenergic receptor expressed in 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
44281467 118848 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity to recombinant human beta-1 adrenergic receptor expressed in CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-1 adrenergic receptor expressed in 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 5.7 pIC50 = 5.7 Binding
Binding affinity to recombinant human beta-1 adrenergic receptor expressed in CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-1 adrenergic receptor expressed in 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
44281468 161322 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity to recombinant human beta-1 adrenergic receptor expressed in CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-1 adrenergic receptor expressed in 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-1 adrenergic receptor expressed in CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-1 adrenergic receptor expressed in 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-1 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindololBinding affinity towards Beta-1 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-1 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindololBinding affinity towards Beta-1 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
44461717 105187 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity towards Beta-1 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindololBinding affinity towards Beta-1 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 5.7 pIC50 = 5.7 Binding
Binding affinity towards Beta-1 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindololBinding affinity towards Beta-1 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 5.7 pIC50 = 5.7 Binding
Binding affinity towards Beta-1 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindololBinding affinity towards Beta-1 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 5.7 pIC50 = 5.7 Binding
Binding affinity towards Beta-1 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindololBinding affinity towards Beta-1 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
44281276 99344 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity towards cloned human Beta-1 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity towards cloned human Beta-1 adrenergic receptor prepared from CHO cells 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 5.7 pIC50 = 5.7 Binding
Binding affinity towards cloned human Beta-1 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity towards cloned human Beta-1 adrenergic receptor prepared from CHO cells 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
44281277 99702 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity towards cloned human Beta-1 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity towards cloned human Beta-1 adrenergic receptor prepared from CHO cells 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 5.7 pIC50 = 5.7 Binding
Binding affinity towards cloned human Beta-1 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity towards cloned human Beta-1 adrenergic receptor prepared from CHO cells 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
44377637 55228 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity towards human Beta-1 adrenergic receptor expressed in CHO cells, using 125I]iodocyanopindololBinding affinity towards human Beta-1 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-1 adrenergic receptor expressed in CHO cells, using 125I]iodocyanopindololBinding affinity towards human Beta-1 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
10841426 116359 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity was evaluated on chinese hamster ovary (CHO) cells expressing the cloned human beta-1 adrenergic receptor in the presence of [125I]- iodocyanopindolol.Binding affinity was evaluated on chinese hamster ovary (CHO) cells expressing the cloned human beta-1 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 5.7 pIC50 = 5.7 Binding
Binding affinity was evaluated on chinese hamster ovary (CHO) cells expressing the cloned human beta-1 adrenergic receptor in the presence of [125I]- iodocyanopindolol.Binding affinity was evaluated on chinese hamster ovary (CHO) cells expressing the cloned human beta-1 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
9832011 104989 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Compound was evaluated for its inhibitory activity against CHO cells expressing the cloned human Beta-1 adrenergic receptor in the presence of [125I]iodocyanopindololCompound was evaluated for its inhibitory activity against CHO cells expressing the cloned human Beta-1 adrenergic receptor 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 - 0 Human 5.7 pIC50 = 5.7 Binding
Compound was evaluated for its inhibitory activity against CHO cells expressing the cloned human Beta-1 adrenergic receptor in the presence of [125I]iodocyanopindololCompound was evaluated for its inhibitory activity against CHO cells expressing the cloned human Beta-1 adrenergic receptor 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
44307063 201634 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-1 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-1 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 5.7 pIC50 = 5.7 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-1 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-1 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
44306979 201991 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-1 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-1 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 5.7 pIC50 = 5.7 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-1 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-1 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
44306985 202015 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-1 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-1 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 5.7 pIC50 = 5.7 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-1 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-1 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
12017005 99792 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
In vitro binding affinity at beta-1 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-1 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 5.7 pIC50 = 5.7 Binding
In vitro binding affinity at beta-1 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-1 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
12017014 99836 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
In vitro binding affinity at beta-1 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-1 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 5.7 pIC50 = 5.7 Binding
In vitro binding affinity at beta-1 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-1 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
44285225 153030 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
In vitro binding affinity at beta-1 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-1 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 5.7 pIC50 = 5.7 Binding
In vitro binding affinity at beta-1 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-1 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
44268327 97834 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Tested for binding affinity against cloned human beta-1 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandTested for binding affinity against cloned human beta-1 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 5.7 pIC50 = 5.7 Binding
Tested for binding affinity against cloned human beta-1 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandTested for binding affinity against cloned human beta-1 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
44335497 4739 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Beta-1 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-1 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 4.7 pIC50 = 4.7 Binding
Beta-1 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-1 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
10416448 201693 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Binding affinity for cloned human Beta-1 adrenergic receptor expressed in CHO cells, tested in the presence of I-iodocyanopindolol.Binding affinity for cloned human Beta-1 adrenergic receptor expressed in CHO cells, tested 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 4.7 pIC50 = 4.7 Binding
Binding affinity for cloned human Beta-1 adrenergic receptor expressed in CHO cells, tested in the presence of I-iodocyanopindolol.Binding affinity for cloned human Beta-1 adrenergic receptor expressed in CHO cells, tested 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
70693598 72740 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assayDisplacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assay
ChEMBL 416 10 5 6 1.5 N#Cc1c(F)cccc1OC[C@@H](O)CNCCNC(=O)Nc1ccc(C(=O)O)cc1 10.1021/ml1002458
CHEMBL2011220 72740 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assayDisplacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assay
ChEMBL 416 10 5 6 1.5 N#Cc1c(F)cccc1OC[C@@H](O)CNCCNC(=O)Nc1ccc(C(=O)O)cc1 10.1021/ml1002458
2249 509 106 None -5 12 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H](-)CGP12177 from human recombinant Beta-1 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H](-)CGP12177 from human recombinant Beta-1 adrenergic receptor expressed in HEK293 cells
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1016/j.bmc.2016.03.006
255 509 106 None -5 12 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H](-)CGP12177 from human recombinant Beta-1 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H](-)CGP12177 from human recombinant Beta-1 adrenergic receptor expressed in HEK293 cells
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1016/j.bmc.2016.03.006
548 509 106 None -5 12 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H](-)CGP12177 from human recombinant Beta-1 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H](-)CGP12177 from human recombinant Beta-1 adrenergic receptor expressed in HEK293 cells
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1016/j.bmc.2016.03.006
CHEMBL24 509 106 None -5 12 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H](-)CGP12177 from human recombinant Beta-1 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H](-)CGP12177 from human recombinant Beta-1 adrenergic receptor expressed in HEK293 cells
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1016/j.bmc.2016.03.006
DB00335 509 106 None -5 12 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H](-)CGP12177 from human recombinant Beta-1 adrenergic receptor expressed in HEK293 cellsDisplacement of [3H](-)CGP12177 from human recombinant Beta-1 adrenergic receptor expressed in HEK293 cells
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1016/j.bmc.2016.03.006
2249 509 106 None -5 12 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]CGP 12177 from human recombinant beta1 adrenergic receptor expressed in HEK293 cells measured after 60 mins by scintillation counting methodDisplacement of [3H]CGP 12177 from human recombinant beta1 adrenergic receptor expressed in HEK293 cells measured after 60 mins by scintillation counting method
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1016/j.bmc.2016.11.014
255 509 106 None -5 12 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]CGP 12177 from human recombinant beta1 adrenergic receptor expressed in HEK293 cells measured after 60 mins by scintillation counting methodDisplacement of [3H]CGP 12177 from human recombinant beta1 adrenergic receptor expressed in HEK293 cells measured after 60 mins by scintillation counting method
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1016/j.bmc.2016.11.014
548 509 106 None -5 12 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]CGP 12177 from human recombinant beta1 adrenergic receptor expressed in HEK293 cells measured after 60 mins by scintillation counting methodDisplacement of [3H]CGP 12177 from human recombinant beta1 adrenergic receptor expressed in HEK293 cells measured after 60 mins by scintillation counting method
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1016/j.bmc.2016.11.014
CHEMBL24 509 106 None -5 12 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]CGP 12177 from human recombinant beta1 adrenergic receptor expressed in HEK293 cells measured after 60 mins by scintillation counting methodDisplacement of [3H]CGP 12177 from human recombinant beta1 adrenergic receptor expressed in HEK293 cells measured after 60 mins by scintillation counting method
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1016/j.bmc.2016.11.014
DB00335 509 106 None -5 12 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]CGP 12177 from human recombinant beta1 adrenergic receptor expressed in HEK293 cells measured after 60 mins by scintillation counting methodDisplacement of [3H]CGP 12177 from human recombinant beta1 adrenergic receptor expressed in HEK293 cells measured after 60 mins by scintillation counting method
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1016/j.bmc.2016.11.014
44280904 99486 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity to recombinant human beta-1 adrenergic receptor expressed in CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-1 adrenergic receptor expressed in 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 5.7 pIC50 = 5.7 Binding
Binding affinity to recombinant human beta-1 adrenergic receptor expressed in CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-1 adrenergic receptor expressed in 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
12017006 99918 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
In vitro binding affinity at beta-1 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-1 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 5.7 pIC50 = 5.7 Binding
In vitro binding affinity at beta-1 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-1 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
10483845 201374 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Binding affinity for cloned human Beta-1 adrenergic receptor expressed in CHO cells, tested in the presence of I-iodocyanopindolol.Binding affinity for cloned human Beta-1 adrenergic receptor expressed in CHO cells, tested 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 cloned human Beta-1 adrenergic receptor expressed in CHO cells, tested in the presence of I-iodocyanopindolol.Binding affinity for cloned human Beta-1 adrenergic receptor expressed in CHO cells, tested 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
14664345 13127 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
In vitro Beta-1 adrenergic receptor affinity in partially purified membrane fractions from canine cardiac tissue using [SH]dihydroalprenolol (4.5 nM)In vitro Beta-1 adrenergic receptor affinity in partially purified membrane fractions from canine cardiac tissue using [SH]dihydroalprenolol (4.5 nM)
ChEMBL 460 12 2 8 1.7 CN(c1ccc(OCC(O)CNCCOc2ccc(-n3ccnc3)cc2)cc1)S(C)(=O)=O 10.1021/jm00166a002
CHEMBL1191442 13127 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
In vitro Beta-1 adrenergic receptor affinity in partially purified membrane fractions from canine cardiac tissue using [SH]dihydroalprenolol (4.5 nM)In vitro Beta-1 adrenergic receptor affinity in partially purified membrane fractions from canine cardiac tissue using [SH]dihydroalprenolol (4.5 nM)
ChEMBL 460 12 2 8 1.7 CN(c1ccc(OCC(O)CNCCOc2ccc(-n3ccnc3)cc2)cc1)S(C)(=O)=O 10.1021/jm00166a002
CHEMBL542544 13127 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
In vitro Beta-1 adrenergic receptor affinity in partially purified membrane fractions from canine cardiac tissue using [SH]dihydroalprenolol (4.5 nM)In vitro Beta-1 adrenergic receptor affinity in partially purified membrane fractions from canine cardiac tissue using [SH]dihydroalprenolol (4.5 nM)
ChEMBL 460 12 2 8 1.7 CN(c1ccc(OCC(O)CNCCOc2ccc(-n3ccnc3)cc2)cc1)S(C)(=O)=O 10.1021/jm00166a002
44268534 19153 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
In vitro affinity at Beta-1 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-1 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 6.7 pIC50 = 6.7 Binding
In vitro affinity at Beta-1 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-1 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
44268478 162252 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
In vitro affinity at Beta-1 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-1 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 6.7 pIC50 = 6.7 Binding
In vitro affinity at Beta-1 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-1 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
44298851 100075 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
In vitro binding affinity towards cloned human beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-1 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 6.7 pIC50 = 6.7 Binding
In vitro binding affinity towards cloned human beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-1 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
448537 159691 86 None -50 25 Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 nan
CHEMBL411 159691 86 None -50 25 Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 nan
14998850 119475 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterolBinding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterol
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 Human 6.6 pIC50 = 6.6 Binding
Binding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterolBinding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterol
ChEMBL 418 7 3 6 1.3 COc1ccccc1N1CCNC(CNC(=O)c2ccc(NS(C)(=O)=O)cc2)C1 10.1021/jm00082a016
9871525 16715 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity for human Beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity for human Beta-1 adrenergic receptor 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 6.6 pIC50 = 6.6 Binding
Binding affinity for human Beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity for human Beta-1 adrenergic receptor 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
14998852 55374 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterolBinding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterol
ChEMBL 360 6 3 5 1.9 CS(=O)(=O)Nc1ccc(NCC2CN(c3ccccc3)CCN2)cc1 10.1021/jm00082a016
CHEMBL162182 55374 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterolBinding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterol
ChEMBL 360 6 3 5 1.9 CS(=O)(=O)Nc1ccc(NCC2CN(c3ccccc3)CCN2)cc1 10.1021/jm00082a016
9810596 16605 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity for human Beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity for human Beta-1 adrenergic receptor 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 5.6 pIC50 = 5.6 Binding
Binding affinity for human Beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity for human Beta-1 adrenergic receptor 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
10371216 99273 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity to recombinant human beta-1 adrenergic receptor expressed in CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-1 adrenergic receptor expressed in 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 5.6 pIC50 = 5.6 Binding
Binding affinity to recombinant human beta-1 adrenergic receptor expressed in CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-1 adrenergic receptor expressed in 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
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-1 adrenergic receptor in the presence of [125I]- iodocyanopindolol.Binding affinity was evaluated on chinese hamster ovary (CHO) cells expressing the cloned human beta-1 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-1 adrenergic receptor in the presence of [125I]- iodocyanopindolol.Binding affinity was evaluated on chinese hamster ovary (CHO) cells expressing the cloned human beta-1 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 1 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 1 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 1 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 1 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
25020250 15247 8 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of beta-1 adrenoceptor ( assessed as residual activity at 1 uM )Inhibition of beta-1 adrenoceptor ( assessed as residual activity at 1 uM )
ChEMBL 388 4 2 6 3.8 c1cc2c(N3CCNCC3)nc(-c3ccnc(NC4CCCCC4)c3)cc2cn1 10.1021/jm100075z
CHEMBL1214998 15247 8 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of beta-1 adrenoceptor ( assessed as residual activity at 1 uM )Inhibition of beta-1 adrenoceptor ( assessed as residual activity at 1 uM )
ChEMBL 388 4 2 6 3.8 c1cc2c(N3CCNCC3)nc(-c3ccnc(NC4CCCCC4)c3)cc2cn1 10.1021/jm100075z
10206782 16661 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity for human Beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity for human Beta-1 adrenergic receptor 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 6.6 pIC50 = 6.6 Binding
Binding affinity for human Beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity for human Beta-1 adrenergic receptor 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
44268479 20674 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
In vitro affinity at Beta-1 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-1 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 6.6 pIC50 = 6.6 Binding
In vitro affinity at Beta-1 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-1 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
10054165 84338 1 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity towards human Beta-1 adrenergic receptor expressed in CHO cells, using 125I]iodocyanopindololBinding affinity towards human Beta-1 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 5.6 pIC50 = 5.6 Binding
Binding affinity towards human Beta-1 adrenergic receptor expressed in CHO cells, using 125I]iodocyanopindololBinding affinity towards human Beta-1 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
31101 719 39 None -245 36 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 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 nan
35 719 39 None -245 36 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 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 nan
403 719 39 None -245 36 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 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 nan
CHEMBL493 719 39 None -245 36 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 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 nan
DB01200 719 39 None -245 36 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 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 nan
46881982 5660 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]cyanopindolol from human beta 1 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 1 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 5.6 pIC50 = 5.6 Binding
Displacement of [125I]cyanopindolol from human beta 1 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 1 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
130400 206634 9 None - 0 Human 5.6 pIC50 = 5.6 Binding
In vitro Beta-1 adrenergic receptor affinity in partially purified membrane fractions from canine cardiac tissue using [SH]dihydroalprenolol (4.5 nM)In vitro Beta-1 adrenergic receptor affinity in partially purified membrane fractions from canine cardiac 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 Human 5.6 pIC50 = 5.6 Binding
In vitro Beta-1 adrenergic receptor affinity in partially purified membrane fractions from canine cardiac tissue using [SH]dihydroalprenolol (4.5 nM)In vitro Beta-1 adrenergic receptor affinity in partially purified membrane fractions from canine cardiac 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 Human 5.6 pIC50 = 5.6 Binding
In vitro Beta-1 adrenergic receptor affinity in partially purified membrane fractions from canine cardiac tissue using [SH]dihydroalprenolol (4.5 nM)In vitro Beta-1 adrenergic receptor affinity in partially purified membrane fractions from canine cardiac 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
12017011 99887 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
In vitro binding affinity at beta-1 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-1 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 5.6 pIC50 = 5.6 Binding
In vitro binding affinity at beta-1 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-1 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
14739889 206024 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Tested for Beta-1 adrenergic receptor selectivity in canine cardiac tissue in anesthetized dogsTested for Beta-1 adrenergic receptor selectivity in canine cardiac 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 Human 5.6 pIC50 = 5.6 Binding
Tested for Beta-1 adrenergic receptor selectivity in canine cardiac tissue in anesthetized dogsTested for Beta-1 adrenergic receptor selectivity in canine cardiac tissue in anesthetized dogs
ChEMBL 364 9 3 5 1.9 Cc1cccc(OCC(O)CNCc2ccc(NS(C)(=O)=O)cc2)c1 10.1021/jm00172a033
130400 206634 9 None - 0 Human 5.6 pIC50 = 5.6 Binding
Tested for Beta-1 adrenergic receptor selectivity in canine cardiac tissue in anesthetized dogsTested for Beta-1 adrenergic receptor selectivity in canine cardiac 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 - 0 Human 5.6 pIC50 = 5.6 Binding
Tested for Beta-1 adrenergic receptor selectivity in canine cardiac tissue in anesthetized dogsTested for Beta-1 adrenergic receptor selectivity in canine cardiac 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 - 0 Human 5.6 pIC50 = 5.6 Binding
Tested for Beta-1 adrenergic receptor selectivity in canine cardiac tissue in anesthetized dogsTested for Beta-1 adrenergic receptor selectivity in canine cardiac tissue in anesthetized dogs
ChEMBL 446 12 3 8 1.7 CS(=O)(=O)Nc1ccc(OCC(O)CNCCOc2ccc(-n3ccnc3)cc2)cc1 10.1021/jm00172a033
44281424 99829 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity to recombinant human beta-1 adrenergic receptor expressed in CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-1 adrenergic receptor expressed in 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 5.6 pIC50 = 5.6 Binding
Binding affinity to recombinant human beta-1 adrenergic receptor expressed in CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-1 adrenergic receptor expressed in 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
44268367 20622 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Tested for binding affinity against cloned human beta-1 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandTested for binding affinity against cloned human beta-1 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 7.6 pIC50 = 7.6 Binding
Tested for binding affinity against cloned human beta-1 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandTested for binding affinity against cloned human beta-1 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
44268556 23916 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
In vitro affinity at Beta-1 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-1 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 6.6 pIC50 = 6.6 Binding
In vitro affinity at Beta-1 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-1 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
11342656 200963 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cellsBinding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cells
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 5.6 pIC50 = 5.6 Binding
Binding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cellsBinding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cells
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
12049920 102146 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity for cloned human Beta-1 adrenergic receptor expressed in CHO cells, tested in the presence of I-iodocyanopindolol.Binding affinity for cloned human Beta-1 adrenergic receptor expressed in CHO cells, tested 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 5.6 pIC50 = 5.6 Binding
Binding affinity for cloned human Beta-1 adrenergic receptor expressed in CHO cells, tested in the presence of I-iodocyanopindolol.Binding affinity for cloned human Beta-1 adrenergic receptor expressed in CHO cells, tested 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
10258518 101468 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity for human Beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity for human Beta-1 adrenergic receptor 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 5.6 pIC50 = 5.6 Binding
Binding affinity for human Beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity for human Beta-1 adrenergic receptor 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
44281372 99643 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity to recombinant human beta-1 adrenergic receptor expressed in CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-1 adrenergic receptor expressed in 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 5.6 pIC50 = 5.6 Binding
Binding affinity to recombinant human beta-1 adrenergic receptor expressed in CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-1 adrenergic receptor expressed in 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
44461705 204130 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity towards Beta-1 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindololBinding affinity towards Beta-1 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 5.6 pIC50 = 5.6 Binding
Binding affinity towards Beta-1 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindololBinding affinity towards Beta-1 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
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-1 adrenergic receptor in the presence of [125I]- iodocyanopindolol.Binding affinity was evaluated on chinese hamster ovary (CHO) cells expressing the cloned human beta-1 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-1 adrenergic receptor in the presence of [125I]- iodocyanopindolol.Binding affinity was evaluated on chinese hamster ovary (CHO) cells expressing the cloned human beta-1 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
44298823 100796 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
In vitro binding affinity towards cloned human beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-1 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 5.6 pIC50 = 5.6 Binding
In vitro binding affinity towards cloned human beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-1 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
44281074 114618 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Binding affinity towards cloned human Beta-1 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity towards cloned human Beta-1 adrenergic receptor prepared from CHO cells 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 4.6 pIC50 = 4.6 Binding
Binding affinity towards cloned human Beta-1 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity towards cloned human Beta-1 adrenergic receptor prepared from CHO cells 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
16049090 63743 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to adrenergic beta1 receptorBinding affinity to adrenergic beta1 receptor
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 - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to adrenergic beta1 receptorBinding affinity to adrenergic beta1 receptor
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
24901211 69973 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of radiolabeled iodocyanopindolol from beta1 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from beta1 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 6.6 pIC50 = 6.6 Binding
Displacement of radiolabeled iodocyanopindolol from beta1 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from beta1 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
2810 67245 50 None -1 2 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 213 4 2 2 2.4 CC(C)NCC(O)c1ccccc1Cl nan
CHEMBL1902627 67245 50 None -1 2 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 213 4 2 2 2.4 CC(C)NCC(O)c1ccccc1Cl nan
70691508 72749 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assayDisplacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assay
ChEMBL 361 9 4 7 1.2 N#Cc1ccccc1OC[C@@H](O)CNCCNC(=O)Nc1nccs1 10.1021/ml1002458
CHEMBL2011229 72749 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assayDisplacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assay
ChEMBL 361 9 4 7 1.2 N#Cc1ccccc1OC[C@@H](O)CNCCNC(=O)Nc1nccs1 10.1021/ml1002458
2249 509 106 None -5 12 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to human adrenergic beta1 receptor by radioligand displacement assayBinding affinity to human adrenergic beta1 receptor by radioligand displacement assay
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1016/j.ejmech.2013.01.044
255 509 106 None -5 12 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to human adrenergic beta1 receptor by radioligand displacement assayBinding affinity to human adrenergic beta1 receptor by radioligand displacement assay
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1016/j.ejmech.2013.01.044
548 509 106 None -5 12 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to human adrenergic beta1 receptor by radioligand displacement assayBinding affinity to human adrenergic beta1 receptor by radioligand displacement assay
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1016/j.ejmech.2013.01.044
CHEMBL24 509 106 None -5 12 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to human adrenergic beta1 receptor by radioligand displacement assayBinding affinity to human adrenergic beta1 receptor by radioligand displacement assay
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1016/j.ejmech.2013.01.044
DB00335 509 106 None -5 12 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to human adrenergic beta1 receptor by radioligand displacement assayBinding affinity to human adrenergic beta1 receptor by radioligand displacement assay
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1016/j.ejmech.2013.01.044
44268571 24412 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
In vitro affinity at Beta-1 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-1 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 6.6 pIC50 = 6.6 Binding
In vitro affinity at Beta-1 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-1 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
12049922 102255 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity for cloned human Beta-1 adrenergic receptor expressed in CHO cells, tested in the presence of I-iodocyanopindolol.Binding affinity for cloned human Beta-1 adrenergic receptor expressed in CHO cells, tested 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 5.6 pIC50 = 5.6 Binding
Binding affinity for cloned human Beta-1 adrenergic receptor expressed in CHO cells, tested in the presence of I-iodocyanopindolol.Binding affinity for cloned human Beta-1 adrenergic receptor expressed in CHO cells, tested 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
12049916 201296 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity for cloned human Beta-1 adrenergic receptor expressed in CHO cells, tested in the presence of I-iodocyanopindolol.Binding affinity for cloned human Beta-1 adrenergic receptor expressed in CHO cells, tested 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 5.6 pIC50 = 5.6 Binding
Binding affinity for cloned human Beta-1 adrenergic receptor expressed in CHO cells, tested in the presence of I-iodocyanopindolol.Binding affinity for cloned human Beta-1 adrenergic receptor expressed in CHO cells, tested 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
44281408 112802 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity to recombinant human beta-1 adrenergic receptor expressed in CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-1 adrenergic receptor expressed in 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 5.6 pIC50 = 5.6 Binding
Binding affinity to recombinant human beta-1 adrenergic receptor expressed in CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-1 adrenergic receptor expressed in 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
10651078 17745 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-1 adrenergic receptor in the presence of [125I]- iodocyanopindolol.Binding affinity was evaluated on chinese hamster ovary (CHO) cells expressing the cloned human beta-1 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 5.6 pIC50 = 5.6 Binding
Binding affinity was evaluated on chinese hamster ovary (CHO) cells expressing the cloned human beta-1 adrenergic receptor in the presence of [125I]- iodocyanopindolol.Binding affinity was evaluated on chinese hamster ovary (CHO) cells expressing the cloned human beta-1 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
14664348 12726 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
In vitro Beta-1 adrenergic receptor affinity in partially purified membrane fractions from canine cardiac tissue using [SH]dihydroalprenolol (4.5 nM)In vitro Beta-1 adrenergic receptor affinity in partially purified membrane fractions from canine cardiac 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 Human 5.6 pIC50 = 5.6 Binding
In vitro Beta-1 adrenergic receptor affinity in partially purified membrane fractions from canine cardiac tissue using [SH]dihydroalprenolol (4.5 nM)In vitro Beta-1 adrenergic receptor affinity in partially purified membrane fractions from canine cardiac 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 Human 5.6 pIC50 = 5.6 Binding
In vitro Beta-1 adrenergic receptor affinity in partially purified membrane fractions from canine cardiac tissue using [SH]dihydroalprenolol (4.5 nM)In vitro Beta-1 adrenergic receptor affinity in partially purified membrane fractions from canine cardiac 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
44298533 193324 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
In vitro binding affinity towards cloned human beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-1 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 5.6 pIC50 = 5.6 Binding
In vitro binding affinity towards cloned human beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-1 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
14998853 119608 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Binding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterolBinding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterol
ChEMBL 360 6 3 5 1.9 CS(=O)(=O)Nc1ccc(NCC2CNCCN2c2ccccc2)cc1 10.1021/jm00082a016
CHEMBL351183 119608 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Binding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterolBinding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterol
ChEMBL 360 6 3 5 1.9 CS(=O)(=O)Nc1ccc(NCC2CNCCN2c2ccccc2)cc1 10.1021/jm00082a016
12043155 99268 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Binding affinity towards cloned human Beta-1 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity towards cloned human Beta-1 adrenergic receptor prepared from CHO cells 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 4.6 pIC50 = 4.6 Binding
Binding affinity towards cloned human Beta-1 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity towards cloned human Beta-1 adrenergic receptor prepared from CHO cells 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
10081581 11080 0 None - 2 Guinea pig 4.6 pIC50 = 4.6 Binding
Inhibitory concentration against beta-1-adrenergic receptor in isolated guinea pig atriaInhibitory concentration against beta-1-adrenergic receptor in isolated guinea pig atria
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 4.6 pIC50 = 4.6 Binding
Inhibitory concentration against beta-1-adrenergic receptor in isolated guinea pig atriaInhibitory concentration against beta-1-adrenergic receptor in isolated guinea pig atria
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 4.6 pIC50 = 4.6 Binding
Inhibitory concentration against beta-1-adrenergic receptor in isolated guinea pig atriaInhibitory concentration against beta-1-adrenergic receptor in isolated guinea pig atria
ChEMBL 202 6 2 4 1.1 CC/C=N/OCC(O)CNC(C)(C)C 10.1021/jm00036a018
44377753 119412 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Binding affinity towards human Beta-1 adrenergic receptor expressed in CHO cells, using 125I]iodocyanopindololBinding affinity towards human Beta-1 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 4.6 pIC50 = 4.6 Binding
Binding affinity towards human Beta-1 adrenergic receptor expressed in CHO cells, using 125I]iodocyanopindololBinding affinity towards human Beta-1 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
44338499 108136 0 None - 0 Guinea pig 5.6 pIC50 = 5.6 Binding
Beta-1 adrenergic receptor blocking was assessed from 50% inhibition of the isoproterenol submaximal response on isolated Guinea pig atria(IA)Beta-1 adrenergic receptor blocking was assessed from 50% inhibition of the isoproterenol submaximal response on isolated Guinea pig atria(IA)
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 5.6 pIC50 = 5.6 Binding
Beta-1 adrenergic receptor blocking was assessed from 50% inhibition of the isoproterenol submaximal response on isolated Guinea pig atria(IA)Beta-1 adrenergic receptor blocking was assessed from 50% inhibition of the isoproterenol submaximal response on isolated Guinea pig atria(IA)
ChEMBL 346 5 3 5 2.6 CC(C)(C)NCC(O)CO/N=C1/c2ccccc2C2CCCCC12O 10.1021/jm00122a008
14664343 10987 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
In vitro Beta-1 adrenergic receptor affinity in partially purified membrane fractions from canine cardiac tissue using [SH]dihydroalprenolol (4.5 nM)In vitro Beta-1 adrenergic receptor affinity in partially purified membrane fractions from canine cardiac 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 Human 5.6 pIC50 = 5.6 Binding
In vitro Beta-1 adrenergic receptor affinity in partially purified membrane fractions from canine cardiac tissue using [SH]dihydroalprenolol (4.5 nM)In vitro Beta-1 adrenergic receptor affinity in partially purified membrane fractions from canine cardiac 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 Human 5.6 pIC50 = 5.6 Binding
In vitro Beta-1 adrenergic receptor affinity in partially purified membrane fractions from canine cardiac tissue using [SH]dihydroalprenolol (4.5 nM)In vitro Beta-1 adrenergic receptor affinity in partially purified membrane fractions from canine cardiac 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
12049921 201874 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Binding affinity for cloned human Beta-1 adrenergic receptor expressed in CHO cells, tested in the presence of I-iodocyanopindolol.Binding affinity for cloned human Beta-1 adrenergic receptor expressed in CHO cells, tested 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 4.6 pIC50 = 4.6 Binding
Binding affinity for cloned human Beta-1 adrenergic receptor expressed in CHO cells, tested in the presence of I-iodocyanopindolol.Binding affinity for cloned human Beta-1 adrenergic receptor expressed in CHO cells, tested 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
2447484 102282 2 None - 2 Human 7.5 pIC50 = 7.5 Binding
Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-1 adrenergic receptor in dog heart.Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-1 adrenergic receptor in dog heart.
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 Human 7.5 pIC50 = 7.5 Binding
Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-1 adrenergic receptor in dog heart.Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-1 adrenergic receptor in dog heart.
ChEMBL 324 5 2 4 3.2 CC(C)(C)NC[C@H](O)CON=C1c2ccccc2-c2ccccc21 10.1021/jm00350a009
10205362 116441 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity for human Beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity for human Beta-1 adrenergic receptor 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 6.5 pIC50 = 6.5 Binding
Binding affinity for human Beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity for human Beta-1 adrenergic receptor 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
44306956 201647 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-1 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-1 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 6.5 pIC50 = 6.5 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-1 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-1 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
72548703 161007 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H](-)CGP 12177 from human beta1 adrenoceptor after 60 mins by scintillation counting analysisDisplacement of [3H](-)CGP 12177 from human beta1 adrenoceptor after 60 mins by scintillation counting analysis
ChEMBL 583 8 3 6 5.8 CC(C)(C)NS(=O)(=O)c1ccc(-c2sc(C(=O)N[C@H]3C[C@H](C(=O)O)C3)nc2CC2CCCCC2)c2ccccc12 10.1016/j.bmcl.2018.03.093
CHEMBL4128926 161007 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H](-)CGP 12177 from human beta1 adrenoceptor after 60 mins by scintillation counting analysisDisplacement of [3H](-)CGP 12177 from human beta1 adrenoceptor after 60 mins by scintillation counting analysis
ChEMBL 583 8 3 6 5.8 CC(C)(C)NS(=O)(=O)c1ccc(-c2sc(C(=O)N[C@H]3C[C@H](C(=O)O)C3)nc2CC2CCCCC2)c2ccccc12 10.1016/j.bmcl.2018.03.093
70695718 72753 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assayDisplacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assay
ChEMBL 372 10 3 6 1.8 N#Cc1ccccc1OC[C@@H](O)CNCCCC(=O)Nc1ccc(F)nc1 10.1021/ml1002458
CHEMBL2011234 72753 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assayDisplacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assay
ChEMBL 372 10 3 6 1.8 N#Cc1ccccc1OC[C@@H](O)CNCCCC(=O)Nc1ccc(F)nc1 10.1021/ml1002458
16049026 63741 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to adrenergic beta1 receptorBinding affinity to adrenergic beta1 receptor
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 - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to adrenergic beta1 receptorBinding affinity to adrenergic beta1 receptor
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 - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to adrenergic beta1 receptorBinding affinity to adrenergic beta1 receptor
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 - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to adrenergic beta1 receptorBinding affinity to adrenergic beta1 receptor
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
16049028 63739 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding affinity to adrenergic beta1 receptorBinding affinity to adrenergic beta1 receptor
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 - 0 Human 8.4 pIC50 = 8.4 Binding
Binding affinity to adrenergic beta1 receptorBinding affinity to adrenergic beta1 receptor
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
44268568 24716 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro affinity at Beta-1 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-1 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-1 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-1 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
44338529 108135 0 None - 0 Guinea pig 5.5 pIC50 = 5.5 Binding
Beta-1 adrenergic receptor blocking was assessed from 50% inhibition of the isoproterenol submaximal response on isolated Guinea pig atria(IA)Beta-1 adrenergic receptor blocking was assessed from 50% inhibition of the isoproterenol submaximal response on isolated Guinea pig atria(IA)
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 5.5 pIC50 = 5.5 Binding
Beta-1 adrenergic receptor blocking was assessed from 50% inhibition of the isoproterenol submaximal response on isolated Guinea pig atria(IA)Beta-1 adrenergic receptor blocking was assessed from 50% inhibition of the isoproterenol submaximal response on isolated Guinea pig atria(IA)
ChEMBL 360 7 2 5 3.2 COC12CCCCCC1c1ccccc1/C2=N/OCC(O)CNC(C)C 10.1021/jm00122a008
44301803 167232 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cellsBinding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cells
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 5.5 pIC50 = 5.5 Binding
Binding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cellsBinding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cells
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
14998846 56076 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterolBinding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterol
ChEMBL 374 7 3 5 1.6 CS(=O)(=O)Nc1ccc(CNCC2CN(c3ccccc3)CCN2)cc1 10.1021/jm00082a016
CHEMBL163153 56076 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterolBinding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterol
ChEMBL 374 7 3 5 1.6 CS(=O)(=O)Nc1ccc(CNCC2CN(c3ccccc3)CCN2)cc1 10.1021/jm00082a016
12049919 201401 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity for cloned human Beta-1 adrenergic receptor expressed in CHO cells, tested in the presence of I-iodocyanopindolol.Binding affinity for cloned human Beta-1 adrenergic receptor expressed in CHO cells, tested 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 5.5 pIC50 = 5.5 Binding
Binding affinity for cloned human Beta-1 adrenergic receptor expressed in CHO cells, tested in the presence of I-iodocyanopindolol.Binding affinity for cloned human Beta-1 adrenergic receptor expressed in CHO cells, tested 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
44349323 16602 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity for human Beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity for human Beta-1 adrenergic receptor 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 5.5 pIC50 = 5.5 Binding
Binding affinity for human Beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity for human Beta-1 adrenergic receptor 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
44281530 99346 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity to recombinant human beta-1 adrenergic receptor expressed in CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-1 adrenergic receptor expressed in 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 5.5 pIC50 = 5.5 Binding
Binding affinity to recombinant human beta-1 adrenergic receptor expressed in CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-1 adrenergic receptor expressed in 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
9938030 99550 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity to recombinant human beta-1 adrenergic receptor expressed in CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-1 adrenergic receptor expressed in 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 5.5 pIC50 = 5.5 Binding
Binding affinity to recombinant human beta-1 adrenergic receptor expressed in CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-1 adrenergic receptor expressed in 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
44281425 99830 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity to recombinant human beta-1 adrenergic receptor expressed in CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-1 adrenergic receptor expressed in 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 5.5 pIC50 = 5.5 Binding
Binding affinity to recombinant human beta-1 adrenergic receptor expressed in CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-1 adrenergic receptor expressed in 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
44377687 57128 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity towards human Beta-1 adrenergic receptor expressed in CHO cells, using 125I]iodocyanopindololBinding affinity towards human Beta-1 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 5.5 pIC50 = 5.5 Binding
Binding affinity towards human Beta-1 adrenergic receptor expressed in CHO cells, using 125I]iodocyanopindololBinding affinity towards human Beta-1 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
46881700 6770 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]cyanopindolol from human beta 1 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 1 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counter
ChEMBL 443 9 3 7 2.3 O=C(Cn1c(=O)ncc2ccccc21)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/j.bmcl.2010.01.130
CHEMBL1084144 6770 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]cyanopindolol from human beta 1 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 1 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counter
ChEMBL 443 9 3 7 2.3 O=C(Cn1c(=O)ncc2ccccc21)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/j.bmcl.2010.01.130
46881529 7167 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]cyanopindolol from human beta 1 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 1 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counter
ChEMBL 375 9 3 4 3.1 O=C(Cc1ccccc1)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/j.bmcl.2010.01.130
CHEMBL1085898 7167 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]cyanopindolol from human beta 1 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 1 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counter
ChEMBL 375 9 3 4 3.1 O=C(Cc1ccccc1)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/j.bmcl.2010.01.130
12017001 146500 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
In vitro binding affinity at beta-1 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-1 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-1 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-1 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
44298850 167609 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
In vitro binding affinity towards cloned human beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-1 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 5.5 pIC50 = 5.5 Binding
In vitro binding affinity towards cloned human beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-1 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
44298281 193051 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
In vitro binding affinity towards cloned human beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-1 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 5.5 pIC50 = 5.5 Binding
In vitro binding affinity towards cloned human beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-1 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
44335499 4908 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Beta-1 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-1 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 4.5 pIC50 = 4.5 Binding
Beta-1 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-1 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
44335651 108059 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Beta-1 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-1 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 4.5 pIC50 = 4.5 Binding
Beta-1 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-1 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
44302005 100082 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Binding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cellsBinding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cells
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 4.5 pIC50 = 4.5 Binding
Binding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cellsBinding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cells
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
44280957 112046 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Binding affinity towards cloned human Beta-1 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity towards cloned human Beta-1 adrenergic receptor prepared from CHO cells 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 4.5 pIC50 = 4.5 Binding
Binding affinity towards cloned human Beta-1 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity towards cloned human Beta-1 adrenergic receptor prepared from CHO cells 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
11819522 11896 0 None - 2 Guinea pig 4.5 pIC50 = 4.5 Binding
Inhibitory concentration against beta-1-adrenergic receptor in isolated guinea pig atriaInhibitory concentration against beta-1-adrenergic receptor in isolated guinea pig atria
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 4.5 pIC50 = 4.5 Binding
Inhibitory concentration against beta-1-adrenergic receptor in isolated guinea pig atriaInhibitory concentration against beta-1-adrenergic receptor in isolated guinea pig atria
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 4.5 pIC50 = 4.5 Binding
Inhibitory concentration against beta-1-adrenergic receptor in isolated guinea pig atriaInhibitory concentration against beta-1-adrenergic receptor in isolated guinea pig atria
ChEMBL 174 6 2 4 0.4 C/C=N/OCC(O)CNC(C)C 10.1021/jm00036a018
46881574 7686 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]cyanopindolol from human beta 1 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 1 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(Cn1cc2ccccc2n1)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/j.bmcl.2010.01.130
CHEMBL1089386 7686 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]cyanopindolol from human beta 1 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 1 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(Cn1cc2ccccc2n1)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/j.bmcl.2010.01.130
14998847 55276 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Binding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterolBinding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterol
ChEMBL 388 6 3 5 1.3 CS(=O)(=O)Nc1ccc(C(=O)NCC2CNCCN2c2ccccc2)cc1 10.1021/jm00082a016
CHEMBL162095 55276 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Binding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterolBinding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterol
ChEMBL 388 6 3 5 1.3 CS(=O)(=O)Nc1ccc(C(=O)NCC2CNCCN2c2ccccc2)cc1 10.1021/jm00082a016
12017003 141386 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
In vitro binding affinity at beta-1 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-1 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 4.5 pIC50 = 4.5 Binding
In vitro binding affinity at beta-1 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-1 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
319 1292 39 None -154 9 Human 6.5 pIC50 = 6.5 Binding
Binding affinity to adrenergic beta1 receptorBinding affinity to adrenergic beta1 receptor
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 -154 9 Human 6.5 pIC50 = 6.5 Binding
Binding affinity to adrenergic beta1 receptorBinding affinity to adrenergic beta1 receptor
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 -154 9 Human 6.5 pIC50 = 6.5 Binding
Binding affinity to adrenergic beta1 receptorBinding affinity to adrenergic beta1 receptor
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 -154 9 Human 6.5 pIC50 = 6.5 Binding
Binding affinity to adrenergic beta1 receptorBinding affinity to adrenergic beta1 receptor
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 -154 9 Human 6.5 pIC50 = 6.5 Binding
Binding affinity to adrenergic beta1 receptorBinding affinity to adrenergic beta1 receptor
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 -154 9 Human 6.5 pIC50 = 6.5 Binding
Binding affinity to adrenergic beta1 receptorBinding affinity to adrenergic beta1 receptor
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
4183 1986 62 None -2 3 Human 6.5 pIC50 = 6.5 Binding
Binding affinity to beta1 adrenoceptorBinding affinity to beta1 adrenoceptor
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 -2 3 Human 6.5 pIC50 = 6.5 Binding
Binding affinity to beta1 adrenoceptorBinding affinity to beta1 adrenoceptor
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 -2 3 Human 6.5 pIC50 = 6.5 Binding
Binding affinity to beta1 adrenoceptorBinding affinity to beta1 adrenoceptor
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 -2 3 Human 6.5 pIC50 = 6.5 Binding
Binding affinity to beta1 adrenoceptorBinding affinity to beta1 adrenoceptor
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 -2 3 Human 6.5 pIC50 = 6.5 Binding
Binding affinity to beta1 adrenoceptorBinding affinity to beta1 adrenoceptor
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
24901351 69974 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of radiolabeled iodocyanopindolol from beta1 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from beta1 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 6.5 pIC50 = 6.5 Binding
Displacement of radiolabeled iodocyanopindolol from beta1 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from beta1 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
24901413 69998 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of radiolabeled iodocyanopindolol from beta1 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from beta1 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 6.5 pIC50 = 6.5 Binding
Displacement of radiolabeled iodocyanopindolol from beta1 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from beta1 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
24900937 70026 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of radiolabeled iodocyanopindolol from beta1 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from beta1 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 6.5 pIC50 = 6.5 Binding
Displacement of radiolabeled iodocyanopindolol from beta1 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from beta1 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
57401435 70042 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of radiolabeled iodocyanopindolol from beta1 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from beta1 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 5.5 pIC50 = 5.5 Binding
Displacement of radiolabeled iodocyanopindolol from beta1 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from beta1 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
44298314 100678 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro binding affinity towards cloned human beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-1 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 6.5 pIC50 = 6.5 Binding
In vitro binding affinity towards cloned human beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-1 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
11556330 162648 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cellsBinding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cells
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 5.5 pIC50 = 5.5 Binding
Binding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cellsBinding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cells
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
14998851 119542 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterolBinding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterol
ChEMBL 361 6 2 5 1.9 CS(=O)(=O)Nc1ccc(OCC2CN(c3ccccc3)CCN2)cc1 10.1021/jm00082a016
CHEMBL350581 119542 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterolBinding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterol
ChEMBL 361 6 2 5 1.9 CS(=O)(=O)Nc1ccc(OCC2CN(c3ccccc3)CCN2)cc1 10.1021/jm00082a016
567 715 10 None - 5 Rat 5.5 pIC50 = 5.5 Binding
Compound was evaluated for its binding affinity towards Beta-1 adrenergic receptor in rat heart membrane by displacing [125I]- iodocyanopindololCompound was evaluated for its binding affinity towards Beta-1 adrenergic receptor in rat heart membrane by displacing [125I]- iodocyanopindolol
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 5.5 pIC50 = 5.5 Binding
Compound was evaluated for its binding affinity towards Beta-1 adrenergic receptor in rat heart membrane by displacing [125I]- iodocyanopindololCompound was evaluated for its binding affinity towards Beta-1 adrenergic receptor in rat heart membrane by displacing [125I]- iodocyanopindolol
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 5.5 pIC50 = 5.5 Binding
Compound was evaluated for its binding affinity towards Beta-1 adrenergic receptor in rat heart membrane by displacing [125I]- iodocyanopindololCompound was evaluated for its binding affinity towards Beta-1 adrenergic receptor in rat heart membrane by displacing [125I]- iodocyanopindolol
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
14739901 205991 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Tested for Beta-1 adrenergic receptor selectivity in canine cardiac tissue in anesthetized dogsTested for Beta-1 adrenergic receptor selectivity in canine cardiac 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 Human 5.5 pIC50 = 5.5 Binding
Tested for Beta-1 adrenergic receptor selectivity in canine cardiac tissue in anesthetized dogsTested for Beta-1 adrenergic receptor selectivity in canine cardiac tissue in anesthetized dogs
ChEMBL 419 8 2 6 1.9 Cc1ccccc1OCC(O)CN1CCN(c2ccc(NS(C)(=O)=O)cc2)CC1 10.1021/jm00172a033
14739893 4198 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Tested for Beta-1 adrenergic receptor selectivity in canine cardiac tissue in anesthetized dogsTested for Beta-1 adrenergic receptor selectivity in canine cardiac 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 Human 4.5 pIC50 = 4.5 Binding
Tested for Beta-1 adrenergic receptor selectivity in canine cardiac tissue in anesthetized dogsTested for Beta-1 adrenergic receptor selectivity in canine cardiac tissue in anesthetized dogs
ChEMBL 416 10 3 7 1.8 CS(=O)(=O)Nc1ccc(OCC(O)CNCc2ccc(-n3ccnc3)cc2)cc1 10.1021/jm00172a033
1499 2052 43 None -46 17 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C nan
3779 2052 43 None -46 17 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C nan
536 2052 43 None -46 17 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C nan
CHEMBL434 2052 43 None -46 17 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C nan
DB01064 2052 43 None -46 17 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C nan
12828562 109205 0 None - 2 Guinea pig 4.5 pIC50 = 4.5 Binding
Inhibitory activity against beta-1 adrenergic receptor in guinea pig atria is determinedInhibitory activity against beta-1 adrenergic receptor in guinea pig atria 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 4.5 pIC50 = 4.5 Binding
Inhibitory activity against beta-1 adrenergic receptor in guinea pig atria is determinedInhibitory activity against beta-1 adrenergic receptor in guinea pig atria is determined
ChEMBL 237 3 3 4 1.7 CC(C)NCC1OCCc2cc(O)c(O)cc21 10.1021/jm00073a006
165193 3126 60 None -7 43 Guinea pig 7.5 pIC50 = 7.5 Binding
Inhibitory activity against beta-1 adrenergic receptor in guinea pig atria is determinedInhibitory activity against beta-1 adrenergic receptor in guinea pig atria is determined
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00073a006
2303 3126 60 None -7 43 Guinea pig 7.5 pIC50 = 7.5 Binding
Inhibitory activity against beta-1 adrenergic receptor in guinea pig atria is determinedInhibitory activity against beta-1 adrenergic receptor in guinea pig atria is determined
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00073a006
4946 3126 60 None -7 43 Guinea pig 7.5 pIC50 = 7.5 Binding
Inhibitory activity against beta-1 adrenergic receptor in guinea pig atria is determinedInhibitory activity against beta-1 adrenergic receptor in guinea pig atria is determined
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00073a006
564 3126 60 None -7 43 Guinea pig 7.5 pIC50 = 7.5 Binding
Inhibitory activity against beta-1 adrenergic receptor in guinea pig atria is determinedInhibitory activity against beta-1 adrenergic receptor in guinea pig atria is determined
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00073a006
62882 3126 60 None -7 43 Guinea pig 7.5 pIC50 = 7.5 Binding
Inhibitory activity against beta-1 adrenergic receptor in guinea pig atria is determinedInhibitory activity against beta-1 adrenergic receptor in guinea pig atria is determined
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00073a006
63 3126 60 None -7 43 Guinea pig 7.5 pIC50 = 7.5 Binding
Inhibitory activity against beta-1 adrenergic receptor in guinea pig atria is determinedInhibitory activity against beta-1 adrenergic receptor in guinea pig atria is determined
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00073a006
66366 3126 60 None -7 43 Guinea pig 7.5 pIC50 = 7.5 Binding
Inhibitory activity against beta-1 adrenergic receptor in guinea pig atria is determinedInhibitory activity against beta-1 adrenergic receptor in guinea pig atria is determined
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00073a006
91536 3126 60 None -7 43 Guinea pig 7.5 pIC50 = 7.5 Binding
Inhibitory activity against beta-1 adrenergic receptor in guinea pig atria is determinedInhibitory activity against beta-1 adrenergic receptor in guinea pig atria is determined
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00073a006
CHEMBL27 3126 60 None -7 43 Guinea pig 7.5 pIC50 = 7.5 Binding
Inhibitory activity against beta-1 adrenergic receptor in guinea pig atria is determinedInhibitory activity against beta-1 adrenergic receptor in guinea pig atria is determined
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00073a006
CHEMBL452861 3126 60 None -7 43 Guinea pig 7.5 pIC50 = 7.5 Binding
Inhibitory activity against beta-1 adrenergic receptor in guinea pig atria is determinedInhibitory activity against beta-1 adrenergic receptor in guinea pig atria is determined
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00073a006
DB00571 3126 60 None -7 43 Guinea pig 7.5 pIC50 = 7.5 Binding
Inhibitory activity against beta-1 adrenergic receptor in guinea pig atria is determinedInhibitory activity against beta-1 adrenergic receptor in guinea pig atria is determined
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00073a006
44338613 110876 0 None - 0 Guinea pig 6.5 pIC50 = 6.5 Binding
Beta-1 adrenergic receptor blocking was assessed from 50% inhibition of the isoproterenol submaximal response on isolated Guinea pig atria(IA)Beta-1 adrenergic receptor blocking was assessed from 50% inhibition of the isoproterenol submaximal response on isolated Guinea pig atria(IA)
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 6.5 pIC50 = 6.5 Binding
Beta-1 adrenergic receptor blocking was assessed from 50% inhibition of the isoproterenol submaximal response on isolated Guinea pig atria(IA)Beta-1 adrenergic receptor blocking was assessed from 50% inhibition of the isoproterenol submaximal response on isolated Guinea pig atria(IA)
ChEMBL 360 5 3 5 2.9 CC(C)(C)NCC(O)CO/N=C1/c2ccccc2C2CCCCCC12O 10.1021/jm00122a008
44268563 96724 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro affinity at Beta-1 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-1 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 6.5 pIC50 = 6.5 Binding
In vitro affinity at Beta-1 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-1 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
46881699 5502 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]cyanopindolol from human beta 1 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 1 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counter
ChEMBL 443 9 3 7 2.3 O=C(Cn1cnc2ccccc2c1=O)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/j.bmcl.2010.01.130
CHEMBL1077238 5502 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]cyanopindolol from human beta 1 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 1 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counter
ChEMBL 443 9 3 7 2.3 O=C(Cn1cnc2ccccc2c1=O)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/j.bmcl.2010.01.130
9873257 84507 12 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibitory activity against cloned human Beta-1 adrenergic receptor in the presence of [125I]iodocyanopindolol expressed in CHO cells by receptor binding assayInhibitory activity against cloned human Beta-1 adrenergic receptor in the presence of [125I]iodocyanopindolol expressed 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 5.5 pIC50 = 5.5 Binding
Inhibitory activity against cloned human Beta-1 adrenergic receptor in the presence of [125I]iodocyanopindolol expressed in CHO cells by receptor binding assayInhibitory activity against cloned human Beta-1 adrenergic receptor in the presence of [125I]iodocyanopindolol expressed 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
44268632 24008 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro affinity at Beta-1 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-1 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 6.5 pIC50 = 6.5 Binding
In vitro affinity at Beta-1 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-1 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
44285634 99929 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro binding affinity at beta-1 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-1 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 6.5 pIC50 = 6.5 Binding
In vitro binding affinity at beta-1 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-1 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
44281097 114222 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity to recombinant human beta-1 adrenergic receptor expressed in CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-1 adrenergic receptor expressed in 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-1 adrenergic receptor expressed in CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-1 adrenergic receptor expressed in 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
2291 3123 52 None -11 12 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O nan
2561 3123 52 None -11 12 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O nan
4932 3123 52 None -11 12 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O nan
CHEMBL631 3123 52 None -11 12 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O nan
DB01182 3123 52 None -11 12 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O nan
11811722 9955 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity against beta-1 adrenergic receptorBinding affinity against beta-1 adrenergic receptor
ChEMBL 413 5 1 4 4.4 O=C1NCN(c2ccccc2)C12CCN(Cc1cccc(Oc3ccccc3)c1)CC2 10.1021/jm010878g
CHEMBL115280 9955 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity against beta-1 adrenergic receptorBinding affinity against beta-1 adrenergic receptor
ChEMBL 413 5 1 4 4.4 O=C1NCN(c2ccccc2)C12CCN(Cc1cccc(Oc3ccccc3)c1)CC2 10.1021/jm010878g
46881701 6771 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]cyanopindolol from human beta 1 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 1 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 5.4 pIC50 = 5.4 Binding
Displacement of [125I]cyanopindolol from human beta 1 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 1 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
44281400 109857 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Binding affinity to recombinant human beta-1 adrenergic receptor expressed in CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-1 adrenergic receptor expressed in 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 5.4 pIC50 = 5.4 Binding
Binding affinity to recombinant human beta-1 adrenergic receptor expressed in CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-1 adrenergic receptor expressed in 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
2369 615 75 None 5 8 Human 7.4 pIC50 = 7.4 Binding
Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-1 adrenergic receptor in dog heartCompound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-1 adrenergic receptor in dog heart
ChEMBL 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C 10.1021/jm00350a009
356 615 75 None 5 8 Human 7.4 pIC50 = 7.4 Binding
Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-1 adrenergic receptor in dog heartCompound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-1 adrenergic receptor in dog heart
ChEMBL 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C 10.1021/jm00350a009
549 615 75 None 5 8 Human 7.4 pIC50 = 7.4 Binding
Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-1 adrenergic receptor in dog heartCompound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-1 adrenergic receptor in dog heart
ChEMBL 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C 10.1021/jm00350a009
CHEMBL423 615 75 None 5 8 Human 7.4 pIC50 = 7.4 Binding
Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-1 adrenergic receptor in dog heartCompound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-1 adrenergic receptor in dog heart
ChEMBL 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C 10.1021/jm00350a009
DB00195 615 75 None 5 8 Human 7.4 pIC50 = 7.4 Binding
Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-1 adrenergic receptor in dog heartCompound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-1 adrenergic receptor in dog heart
ChEMBL 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C 10.1021/jm00350a009
121848 130175 4 None - 2 Human 7.4 pIC50 = 7.4 Binding
Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-1 adrenergic receptor in dog heart.Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-1 adrenergic receptor in dog heart.
ChEMBL 324 5 2 4 3.2 CC(C)(C)NCC(O)CON=C1c2ccccc2-c2ccccc21 10.1021/jm00350a009
CHEMBL368457 130175 4 None - 2 Human 7.4 pIC50 = 7.4 Binding
Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-1 adrenergic receptor in dog heart.Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-1 adrenergic receptor in dog heart.
ChEMBL 324 5 2 4 3.2 CC(C)(C)NCC(O)CON=C1c2ccccc2-c2ccccc21 10.1021/jm00350a009
21138 97986 34 None -4 7 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 259 6 2 3 2.6 CC(C)NC[C@@H](O)COc1cccc2ccccc12 nan
CHEMBL275742 97986 34 None -4 7 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 259 6 2 3 2.6 CC(C)NC[C@@H](O)COc1cccc2ccccc12 nan
44301832 199380 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Binding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cellsBinding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cells
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 5.4 pIC50 = 5.4 Binding
Binding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cellsBinding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cells
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
44285692 136690 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
In vitro binding affinity at beta-1 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-1 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 4.4 pIC50 = 4.4 Binding
In vitro binding affinity at beta-1 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-1 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
44267518 13198 1 None - 0 Human 4.4 pIC50 = 4.4 Binding
Tested for Beta-1 adrenergic receptor selectivity in canine cardiac tissue in anesthetized dogsTested for Beta-1 adrenergic receptor selectivity in canine cardiac 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 - 0 Human 4.4 pIC50 = 4.4 Binding
Tested for Beta-1 adrenergic receptor selectivity in canine cardiac tissue in anesthetized dogsTested for Beta-1 adrenergic receptor selectivity in canine cardiac 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 - 0 Human 4.4 pIC50 = 4.4 Binding
Tested for Beta-1 adrenergic receptor selectivity in canine cardiac tissue in anesthetized dogsTested for Beta-1 adrenergic receptor selectivity in canine cardiac 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
44349367 16725 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Binding affinity for human Beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity for human Beta-1 adrenergic receptor 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 5.4 pIC50 = 5.4 Binding
Binding affinity for human Beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity for human Beta-1 adrenergic receptor 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
83113 57118 86 None - 0 Human 4.4 pIC50 = 4.4 Binding
Binding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterolBinding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterol
ChEMBL 176 1 1 2 1.4 Cc1ccc(N2CCNCC2)cc1 10.1021/jm00082a016
CHEMBL165462 57118 86 None - 0 Human 4.4 pIC50 = 4.4 Binding
Binding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterolBinding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterol
ChEMBL 176 1 1 2 1.4 Cc1ccc(N2CCNCC2)cc1 10.1021/jm00082a016
269722 198288 103 None - 1 Human 4.4 pIC50 = 4.4 Binding
Binding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterolBinding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterol
ChEMBL 192 2 1 3 1.1 COc1ccc(N2CCNCC2)cc1 10.1021/jm00082a016
CHEMBL59517 198288 103 None - 1 Human 4.4 pIC50 = 4.4 Binding
Binding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterolBinding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterol
ChEMBL 192 2 1 3 1.1 COc1ccc(N2CCNCC2)cc1 10.1021/jm00082a016
44267518 13198 1 None - 0 Human 4.4 pIC50 = 4.4 Binding
In vitro Beta-1 adrenergic receptor affinity in partially purified membrane fractions from canine cardiac tissue using [SH]dihydroalprenolol (4.5 nM)In vitro Beta-1 adrenergic receptor affinity in partially purified membrane fractions from canine cardiac 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
CHEMBL1192069 13198 1 None - 0 Human 4.4 pIC50 = 4.4 Binding
In vitro Beta-1 adrenergic receptor affinity in partially purified membrane fractions from canine cardiac tissue using [SH]dihydroalprenolol (4.5 nM)In vitro Beta-1 adrenergic receptor affinity in partially purified membrane fractions from canine cardiac 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
CHEMBL543251 13198 1 None - 0 Human 4.4 pIC50 = 4.4 Binding
In vitro Beta-1 adrenergic receptor affinity in partially purified membrane fractions from canine cardiac tissue using [SH]dihydroalprenolol (4.5 nM)In vitro Beta-1 adrenergic receptor affinity in partially purified membrane fractions from canine cardiac 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
16049309 63754 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to adrenergic beta1 receptorBinding affinity to adrenergic beta1 receptor
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 - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to adrenergic beta1 receptorBinding affinity to adrenergic beta1 receptor
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
56670092 63758 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity to adrenergic beta1 receptorBinding affinity to adrenergic beta1 receptor
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 - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity to adrenergic beta1 receptorBinding affinity to adrenergic beta1 receptor
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
24901348 69969 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of radiolabeled iodocyanopindolol from beta1 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from beta1 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 6.4 pIC50 = 6.4 Binding
Displacement of radiolabeled iodocyanopindolol from beta1 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from beta1 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
24901349 69972 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of radiolabeled iodocyanopindolol from beta1 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from beta1 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 6.4 pIC50 = 6.4 Binding
Displacement of radiolabeled iodocyanopindolol from beta1 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from beta1 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
24901347 69975 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of radiolabeled iodocyanopindolol from beta1 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from beta1 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 6.4 pIC50 = 6.4 Binding
Displacement of radiolabeled iodocyanopindolol from beta1 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from beta1 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
137 367 47 None -19 12 Human 8.3 pIC50 = 8.3 Binding
Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-1 adrenergic receptor in dog heart.Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-1 adrenergic receptor in dog heart.
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1021/jm00350a009
2119 367 47 None -19 12 Human 8.3 pIC50 = 8.3 Binding
Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-1 adrenergic receptor in dog heart.Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-1 adrenergic receptor in dog heart.
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1021/jm00350a009
563 367 47 None -19 12 Human 8.3 pIC50 = 8.3 Binding
Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-1 adrenergic receptor in dog heart.Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-1 adrenergic receptor in dog heart.
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1021/jm00350a009
66368 367 47 None -19 12 Human 8.3 pIC50 = 8.3 Binding
Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-1 adrenergic receptor in dog heart.Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-1 adrenergic receptor in dog heart.
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1021/jm00350a009
CHEMBL266195 367 47 None -19 12 Human 8.3 pIC50 = 8.3 Binding
Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-1 adrenergic receptor in dog heart.Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-1 adrenergic receptor in dog heart.
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1021/jm00350a009
DB00866 367 47 None -19 12 Human 8.3 pIC50 = 8.3 Binding
Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-1 adrenergic receptor in dog heart.Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-1 adrenergic receptor in dog heart.
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1021/jm00350a009
15483883 99755 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Binding affinity to recombinant human beta-1 adrenergic receptor expressed in CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-1 adrenergic receptor expressed in 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 5.4 pIC50 = 5.4 Binding
Binding affinity to recombinant human beta-1 adrenergic receptor expressed in CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-1 adrenergic receptor expressed in 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
44281219 111509 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Binding affinity to recombinant human beta-1 adrenergic receptor expressed in CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-1 adrenergic receptor expressed in 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 5.4 pIC50 = 5.4 Binding
Binding affinity to recombinant human beta-1 adrenergic receptor expressed in CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-1 adrenergic receptor expressed in 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
15523861 57206 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Binding affinity towards human Beta-1 adrenergic receptor expressed in CHO cells, using 125I]iodocyanopindololBinding affinity towards human Beta-1 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 5.4 pIC50 = 5.4 Binding
Binding affinity towards human Beta-1 adrenergic receptor expressed in CHO cells, using 125I]iodocyanopindololBinding affinity towards human Beta-1 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
44377316 119544 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Binding affinity towards human Beta-1 adrenergic receptor expressed in CHO cells, using 125I]iodocyanopindololBinding affinity towards human Beta-1 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 5.4 pIC50 = 5.4 Binding
Binding affinity towards human Beta-1 adrenergic receptor expressed in CHO cells, using 125I]iodocyanopindololBinding affinity towards human Beta-1 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
46882031 5703 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]cyanopindolol from human beta 1 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 1 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 5.4 pIC50 = 5.4 Binding
Displacement of [125I]cyanopindolol from human beta 1 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 1 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
44298290 167632 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
In vitro binding affinity towards cloned human beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-1 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 5.4 pIC50 = 5.4 Binding
In vitro binding affinity towards cloned human beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-1 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
44298822 193316 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
In vitro binding affinity towards cloned human beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-1 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 5.4 pIC50 = 5.4 Binding
In vitro binding affinity towards cloned human beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-1 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
44298516 193906 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
In vitro binding affinity towards cloned human beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-1 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 5.4 pIC50 = 5.4 Binding
In vitro binding affinity towards cloned human beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-1 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
44301764 100152 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
Binding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cellsBinding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cells
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 4.4 pIC50 = 4.4 Binding
Binding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cellsBinding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cells
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
12049915 102353 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
Binding affinity for cloned human Beta-1 adrenergic receptor expressed in CHO cells, tested in the presence of I-iodocyanopindolol.Binding affinity for cloned human Beta-1 adrenergic receptor expressed in CHO cells, tested 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 4.4 pIC50 = 4.4 Binding
Binding affinity for cloned human Beta-1 adrenergic receptor expressed in CHO cells, tested in the presence of I-iodocyanopindolol.Binding affinity for cloned human Beta-1 adrenergic receptor expressed in CHO cells, tested 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
44298728 193105 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
In vitro binding affinity towards cloned human beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-1 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-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-1 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
44190762 176296 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of radioligand from adrenergic beta-1 receptorDisplacement of radioligand from adrenergic beta-1 receptor
ChEMBL 531 8 1 5 6.6 Cc1c(C(=O)c2ccc(Cl)cc2)c2ccc(OC(F)(F)F)cc2n1Cc1cccc(O[C@H](C)C(=O)O)c1 10.1016/j.bmcl.2008.07.103
CHEMBL461571 176296 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of radioligand from adrenergic beta-1 receptorDisplacement of radioligand from adrenergic beta-1 receptor
ChEMBL 531 8 1 5 6.6 Cc1c(C(=O)c2ccc(Cl)cc2)c2ccc(OC(F)(F)F)cc2n1Cc1cccc(O[C@H](C)C(=O)O)c1 10.1016/j.bmcl.2008.07.103
46882030 5676 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]cyanopindolol from human beta 1 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 1 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 5.4 pIC50 = 5.4 Binding
Displacement of [125I]cyanopindolol from human beta 1 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 1 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
1043 1545 13 None -26302 29 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
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 -26302 29 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
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 -26302 29 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
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 -26302 29 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
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 -26302 29 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
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
44298821 193315 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
In vitro binding affinity towards cloned human beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-1 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 5.4 pIC50 = 5.4 Binding
In vitro binding affinity towards cloned human beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-1 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
12017018 141794 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
In vitro binding affinity at beta-1 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-1 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 4.4 pIC50 = 4.4 Binding
In vitro binding affinity at beta-1 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-1 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
145947927 167178 0 None -16 2 Rat 6.4 pIC50 = 6.4 Binding
Displacement of [3H]-CGP-12177 from adrenergic beta1 receptor in Wistar rat cortex incubated for 60 mins by microbeta liquid scintillation counting analysisDisplacement of [3H]-CGP-12177 from adrenergic beta1 receptor in Wistar rat cortex incubated for 60 mins by microbeta liquid scintillation counting analysis
ChEMBL 419 9 2 6 3.5 COc1ccccc1CCNCC(O)COc1cccc2c(=O)c3ccccc3oc12 10.1016/j.bmc.2018.04.038
CHEMBL4130151 167178 0 None -16 2 Rat 6.4 pIC50 = 6.4 Binding
Displacement of [3H]-CGP-12177 from adrenergic beta1 receptor in Wistar rat cortex incubated for 60 mins by microbeta liquid scintillation counting analysisDisplacement of [3H]-CGP-12177 from adrenergic beta1 receptor in Wistar rat cortex incubated for 60 mins by microbeta liquid scintillation counting analysis
ChEMBL 419 9 2 6 3.5 COc1ccccc1CCNCC(O)COc1cccc2c(=O)c3ccccc3oc12 10.1016/j.bmc.2018.04.038
CHEMBL4302997 167178 0 None -16 2 Rat 6.4 pIC50 = 6.4 Binding
Displacement of [3H]-CGP-12177 from adrenergic beta1 receptor in Wistar rat cortex incubated for 60 mins by microbeta liquid scintillation counting analysisDisplacement of [3H]-CGP-12177 from adrenergic beta1 receptor in Wistar rat cortex incubated for 60 mins by microbeta liquid scintillation counting analysis
ChEMBL 419 9 2 6 3.5 COc1ccccc1CCNCC(O)COc1cccc2c(=O)c3ccccc3oc12 10.1016/j.bmc.2018.04.038
2447486 62716 1 None - 2 Human 7.4 pIC50 = 7.4 Binding
Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-1 adrenergic receptor in dog heart.Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-1 adrenergic receptor in dog heart.
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 Human 7.4 pIC50 = 7.4 Binding
Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-1 adrenergic receptor in dog heart.Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-1 adrenergic receptor in dog heart.
ChEMBL 324 5 2 4 3.2 CC(C)(C)NC[C@@H](O)CON=C1c2ccccc2-c2ccccc21 10.1021/jm00350a009
76322045 105420 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-cyanopindolol from recombinant human beta-1 adrenergic receptor expressed in CHO cell membranes after 1 hr by scintillation counting analysisDisplacement of [125I]-cyanopindolol from recombinant human beta-1 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 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-cyanopindolol from recombinant human beta-1 adrenergic receptor expressed in CHO cell membranes after 1 hr by scintillation counting analysisDisplacement of [125I]-cyanopindolol from recombinant human beta-1 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
176 394 63 None -660 31 Human 4.4 pIC50 = 4.4 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2157 394 63 None -660 31 Human 4.4 pIC50 = 4.4 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2566 394 63 None -660 31 Human 4.4 pIC50 = 4.4 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
CHEMBL633 394 63 None -660 31 Human 4.4 pIC50 = 4.4 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
DB01118 394 63 None -660 31 Human 4.4 pIC50 = 4.4 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
44307340 102109 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-1 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-1 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 6.4 pIC50 = 6.4 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-1 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-1 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
44281218 155158 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Binding affinity to recombinant human beta-1 adrenergic receptor expressed in CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-1 adrenergic receptor expressed in 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 5.4 pIC50 = 5.4 Binding
Binding affinity to recombinant human beta-1 adrenergic receptor expressed in CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-1 adrenergic receptor expressed in 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
44112 120764 41 None -2 7 Human 7.3 pIC50 = 7.3 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 380 7 2 4 4.5 Cc1cc2c(OCC(CNC(C)(C)C)OC(=O)c3ccccc3)cccc2[nH]1 nan
CHEMBL357995 120764 41 None -2 7 Human 7.3 pIC50 = 7.3 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 380 7 2 4 4.5 Cc1cc2c(OCC(CNC(C)(C)C)OC(=O)c3ccccc3)cccc2[nH]1 nan
44307196 201884 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-1 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-1 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 6.3 pIC50 = 6.3 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-1 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-1 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
12017010 162638 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
In vitro binding affinity at beta-1 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-1 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 5.3 pIC50 = 5.3 Binding
In vitro binding affinity at beta-1 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-1 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
10138809 168508 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity for human Beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity for human Beta-1 adrenergic receptor 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 6.3 pIC50 = 6.3 Binding
Binding affinity for human Beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity for human Beta-1 adrenergic receptor 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
10099346 140529 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
In vitro binding affinity at beta-1 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-1 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 5.3 pIC50 = 5.3 Binding
In vitro binding affinity at beta-1 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-1 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
46881900 7691 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]cyanopindolol from human beta 1 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 1 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 5.3 pIC50 = 5.3 Binding
Displacement of [125I]cyanopindolol from human beta 1 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 1 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
70687348 72755 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assayDisplacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assay
ChEMBL 393 10 3 6 1.0 N#Cc1ccccc1OC[C@@H](O)CNCCNS(=O)(=O)c1ccccc1F 10.1021/ml1002458
CHEMBL2011236 72755 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assayDisplacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assay
ChEMBL 393 10 3 6 1.0 N#Cc1ccccc1OC[C@@H](O)CNCCNS(=O)(=O)c1ccccc1F 10.1021/ml1002458
16049158 63744 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity to adrenergic beta1 receptorBinding affinity to adrenergic beta1 receptor
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 - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity to adrenergic beta1 receptorBinding affinity to adrenergic beta1 receptor
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
56673609 63757 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity to adrenergic beta1 receptorBinding affinity to adrenergic beta1 receptor
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 - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity to adrenergic beta1 receptorBinding affinity to adrenergic beta1 receptor
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
24900689 70005 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of radiolabeled iodocyanopindolol from beta1 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from beta1 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 7.3 pIC50 = 7.3 Binding
Displacement of radiolabeled iodocyanopindolol from beta1 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from beta1 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
44268268 18449 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Tested for binding affinity against cloned human beta-1 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligand.Tested for binding affinity against cloned human beta-1 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 6.3 pIC50 = 6.3 Binding
Tested for binding affinity against cloned human beta-1 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligand.Tested for binding affinity against cloned human beta-1 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
567 715 10 None -11 5 Human 5.3 pIC50 = 5.3 Binding
Beta-1 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-1 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 -11 5 Human 5.3 pIC50 = 5.3 Binding
Beta-1 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-1 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 -11 5 Human 5.3 pIC50 = 5.3 Binding
Beta-1 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-1 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
15483880 99138 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity to recombinant human beta-1 adrenergic receptor expressed in CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-1 adrenergic receptor expressed in 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 5.3 pIC50 = 5.3 Binding
Binding affinity to recombinant human beta-1 adrenergic receptor expressed in CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-1 adrenergic receptor expressed in 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
44281469 99642 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity to recombinant human beta-1 adrenergic receptor expressed in CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-1 adrenergic receptor expressed in 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 5.3 pIC50 = 5.3 Binding
Binding affinity to recombinant human beta-1 adrenergic receptor expressed in CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-1 adrenergic receptor expressed in 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
44308088 201894 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity towards Beta-1 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindololBinding affinity towards Beta-1 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-1 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindololBinding affinity towards Beta-1 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
10099459 203973 1 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity towards Beta-1 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindololBinding affinity towards Beta-1 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 5.3 pIC50 = 5.3 Binding
Binding affinity towards Beta-1 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindololBinding affinity towards Beta-1 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
44377636 119580 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity towards human Beta-1 adrenergic receptor expressed in CHO cells, using 125I]iodocyanopindololBinding affinity towards human Beta-1 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 5.3 pIC50 = 5.3 Binding
Binding affinity towards human Beta-1 adrenergic receptor expressed in CHO cells, using 125I]iodocyanopindololBinding affinity towards human Beta-1 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
10099459 203973 1 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity towards human Beta-1 adrenergic receptor expressed in CHO cells, using 125I]iodocyanopindololBinding affinity towards human Beta-1 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 5.3 pIC50 = 5.3 Binding
Binding affinity towards human Beta-1 adrenergic receptor expressed in CHO cells, using 125I]iodocyanopindololBinding affinity towards human Beta-1 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
46881937 6671 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]cyanopindolol from human beta 1 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 1 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counter
ChEMBL 494 9 3 6 5.5 O=C(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccccc1-c1nc2ccccc2s1 10.1016/j.bmcl.2010.01.130
CHEMBL1083831 6671 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]cyanopindolol from human beta 1 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 1 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counter
ChEMBL 494 9 3 6 5.5 O=C(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccccc1-c1nc2ccccc2s1 10.1016/j.bmcl.2010.01.130
44458134 84395 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibitory activity against cloned human Beta-1 adrenergic receptor in the presence of [125I]iodocyanopindolol in CHO cells by receptor binding assayInhibitory activity against cloned human Beta-1 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 5.3 pIC50 = 5.3 Binding
Inhibitory activity against cloned human Beta-1 adrenergic receptor in the presence of [125I]iodocyanopindolol in CHO cells by receptor binding assayInhibitory activity against cloned human Beta-1 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
44301886 100597 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Binding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cellsBinding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cells
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 4.3 pIC50 = 4.3 Binding
Binding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cellsBinding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cells
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
44377665 167759 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Binding affinity towards human Beta-1 adrenergic receptor expressed in CHO cells, using 125I]iodocyanopindololBinding affinity towards human Beta-1 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-1 adrenergic receptor expressed in CHO cells, using 125I]iodocyanopindololBinding affinity towards human Beta-1 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
2419 3394 80 None -162 6 Human 6.3 pIC50 = 6.3 Binding
Binding affinity to adrenergic beta1 receptorBinding affinity to adrenergic beta1 receptor
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.05.097
5152 3394 80 None -162 6 Human 6.3 pIC50 = 6.3 Binding
Binding affinity to adrenergic beta1 receptorBinding affinity to adrenergic beta1 receptor
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.05.097
559 3394 80 None -162 6 Human 6.3 pIC50 = 6.3 Binding
Binding affinity to adrenergic beta1 receptorBinding affinity to adrenergic beta1 receptor
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.05.097
CHEMBL1263 3394 80 None -162 6 Human 6.3 pIC50 = 6.3 Binding
Binding affinity to adrenergic beta1 receptorBinding affinity to adrenergic beta1 receptor
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.05.097
DB00938 3394 80 None -162 6 Human 6.3 pIC50 = 6.3 Binding
Binding affinity to adrenergic beta1 receptorBinding affinity to adrenergic beta1 receptor
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.05.097
2419 3394 80 None -162 6 Human 6.3 pIC50 = 6.3 Binding
Binding affinity to beta1 adrenoceptorBinding affinity to beta1 adrenoceptor
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.10.049
5152 3394 80 None -162 6 Human 6.3 pIC50 = 6.3 Binding
Binding affinity to beta1 adrenoceptorBinding affinity to beta1 adrenoceptor
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.10.049
559 3394 80 None -162 6 Human 6.3 pIC50 = 6.3 Binding
Binding affinity to beta1 adrenoceptorBinding affinity to beta1 adrenoceptor
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.10.049
CHEMBL1263 3394 80 None -162 6 Human 6.3 pIC50 = 6.3 Binding
Binding affinity to beta1 adrenoceptorBinding affinity to beta1 adrenoceptor
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.10.049
DB00938 3394 80 None -162 6 Human 6.3 pIC50 = 6.3 Binding
Binding affinity to beta1 adrenoceptorBinding affinity to beta1 adrenoceptor
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.10.049
57398562 70002 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of radiolabeled iodocyanopindolol from beta1 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from beta1 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 6.3 pIC50 = 6.3 Binding
Displacement of radiolabeled iodocyanopindolol from beta1 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from beta1 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
9984028 119208 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Receptor binding assay(Beta-1 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-1 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 5.3 pIC50 = 5.3 Binding
Receptor binding assay(Beta-1 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-1 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
44268498 97882 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
In vitro affinity at Beta-1 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-1 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 6.3 pIC50 = 6.3 Binding
In vitro affinity at Beta-1 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-1 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
10075383 96645 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Tested for binding affinity against cloned human beta-1 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandTested for binding affinity against cloned human beta-1 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 6.3 pIC50 = 6.3 Binding
Tested for binding affinity against cloned human beta-1 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandTested for binding affinity against cloned human beta-1 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
44301617 197028 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Binding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cellsBinding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cells
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 4.3 pIC50 = 4.3 Binding
Binding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cellsBinding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cells
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
44268470 24651 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
In vitro affinity at Beta-1 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-1 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 6.3 pIC50 = 6.3 Binding
In vitro affinity at Beta-1 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-1 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
44377754 119432 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity towards human Beta-1 adrenergic receptor expressed in CHO cells, using 125I]iodocyanopindololBinding affinity towards human Beta-1 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 5.3 pIC50 = 5.3 Binding
Binding affinity towards human Beta-1 adrenergic receptor expressed in CHO cells, using 125I]iodocyanopindololBinding affinity towards human Beta-1 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
44306959 201385 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-1 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-1 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 5.3 pIC50 = 5.3 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-1 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-1 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
14998848 119569 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterolBinding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterol
ChEMBL 361 5 2 5 2.1 O=C(NCC1CN(c2ccccc2)CCN1)c1ccc(-n2ccnc2)cc1 10.1021/jm00082a016
CHEMBL350847 119569 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterolBinding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterol
ChEMBL 361 5 2 5 2.1 O=C(NCC1CN(c2ccccc2)CCN1)c1ccc(-n2ccnc2)cc1 10.1021/jm00082a016
44268605 97949 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
In vitro affinity at Beta-1 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-1 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-1 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-1 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
44280903 99485 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity to recombinant human beta-1 adrenergic receptor expressed in CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-1 adrenergic receptor expressed in 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 6.3 pIC50 = 6.3 Binding
Binding affinity to recombinant human beta-1 adrenergic receptor expressed in CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-1 adrenergic receptor expressed in 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
44461718 204138 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity towards Beta-1 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindololBinding affinity towards Beta-1 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 5.3 pIC50 = 5.3 Binding
Binding affinity towards Beta-1 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindololBinding affinity towards Beta-1 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
10007337 116187 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity towards cloned human Beta-1 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity towards cloned human Beta-1 adrenergic receptor prepared from CHO cells 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 5.3 pIC50 = 5.3 Binding
Binding affinity towards cloned human Beta-1 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity towards cloned human Beta-1 adrenergic receptor prepared from CHO cells 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
12043156 167575 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity towards cloned human Beta-1 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity towards cloned human Beta-1 adrenergic receptor prepared from CHO cells 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 5.3 pIC50 = 5.3 Binding
Binding affinity towards cloned human Beta-1 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity towards cloned human Beta-1 adrenergic receptor prepared from CHO cells 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
44461718 204138 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity towards human Beta-1 adrenergic receptor expressed in CHO cells, using 125I]iodocyanopindololBinding affinity towards human Beta-1 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 5.3 pIC50 = 5.3 Binding
Binding affinity towards human Beta-1 adrenergic receptor expressed in CHO cells, using 125I]iodocyanopindololBinding affinity towards human Beta-1 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
44307333 201970 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-1 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-1 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 5.3 pIC50 = 5.3 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-1 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-1 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
44280860 99439 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Binding affinity towards cloned human Beta-1 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity towards cloned human Beta-1 adrenergic receptor prepared from CHO cells 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 4.3 pIC50 = 4.3 Binding
Binding affinity towards cloned human Beta-1 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity towards cloned human Beta-1 adrenergic receptor prepared from CHO cells 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
1588 2284 24 None -218 44 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
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 -218 44 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
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 -218 44 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
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 -218 44 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
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 -218 44 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
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
12049917 201328 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity for cloned human Beta-1 adrenergic receptor expressed in CHO cells, tested in the presence of I-iodocyanopindolol.Binding affinity for cloned human Beta-1 adrenergic receptor expressed in CHO cells, tested 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 5.3 pIC50 = 5.3 Binding
Binding affinity for cloned human Beta-1 adrenergic receptor expressed in CHO cells, tested in the presence of I-iodocyanopindolol.Binding affinity for cloned human Beta-1 adrenergic receptor expressed in CHO cells, tested 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
44281073 118688 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Binding affinity towards cloned human Beta-1 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity towards cloned human Beta-1 adrenergic receptor prepared from CHO cells 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 4.3 pIC50 = 4.3 Binding
Binding affinity towards cloned human Beta-1 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity towards cloned human Beta-1 adrenergic receptor prepared from CHO cells 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
45482789 197237 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of adrenergic beta-1 receptorInhibition of adrenergic beta-1 receptor
ChEMBL 428 4 2 2 4.5 CCN(CC)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1 10.1016/j.bmcl.2009.09.002
CHEMBL584554 197237 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of adrenergic beta-1 receptorInhibition of adrenergic beta-1 receptor
ChEMBL 428 4 2 2 4.5 CCN(CC)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1 10.1016/j.bmcl.2009.09.002
15523859 204207 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity towards Beta-1 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindololBinding affinity towards Beta-1 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 6.2 pIC50 = 6.2 Binding
Binding affinity towards Beta-1 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindololBinding affinity towards Beta-1 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 6.2 pIC50 = 6.2 Binding
Binding affinity towards human Beta-1 adrenergic receptor expressed in CHO cells, using 125I]iodocyanopindololBinding affinity towards human Beta-1 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 6.2 pIC50 = 6.2 Binding
Binding affinity towards human Beta-1 adrenergic receptor expressed in CHO cells, using 125I]iodocyanopindololBinding affinity towards human Beta-1 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
44298315 192685 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
In vitro binding affinity towards cloned human beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-1 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 6.2 pIC50 = 6.2 Binding
In vitro binding affinity towards cloned human beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-1 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
14823035 141019 2 None - 3 Rat 7.2 pIC50 = 7.2 Binding
Compound was evaluated for its binding affinity towards Beta-1 adrenergic receptor in rat heart membrane by displacing [125I]- iodocyanopindololCompound was evaluated for its binding affinity towards Beta-1 adrenergic receptor in rat heart membrane by displacing [125I]- iodocyanopindolol
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 7.2 pIC50 = 7.2 Binding
Compound was evaluated for its binding affinity towards Beta-1 adrenergic receptor in rat heart membrane by displacing [125I]- iodocyanopindololCompound was evaluated for its binding affinity towards Beta-1 adrenergic receptor in rat heart membrane by displacing [125I]- iodocyanopindolol
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
10112732 16618 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity for human Beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity for human Beta-1 adrenergic receptor 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 6.2 pIC50 = 6.2 Binding
Binding affinity for human Beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity for human Beta-1 adrenergic receptor 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
44307186 202063 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-1 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-1 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 6.2 pIC50 = 6.2 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-1 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-1 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
24900813 70008 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of radiolabeled iodocyanopindolol from beta1 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from beta1 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 8.2 pIC50 = 8.2 Binding
Displacement of radiolabeled iodocyanopindolol from beta1 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from beta1 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
44268365 98104 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Tested for binding affinity against cloned human beta-1 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandTested for binding affinity against cloned human beta-1 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 8.2 pIC50 = 8.2 Binding
Tested for binding affinity against cloned human beta-1 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandTested for binding affinity against cloned human beta-1 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
39468 2270 33 None -3 7 Human 8.2 pIC50 = 8.2 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 291 5 2 4 2.3 O[C@H](COc1cccc2c1CCCC2=O)CNC(C)(C)C nan
431 2270 33 None -3 7 Human 8.2 pIC50 = 8.2 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 291 5 2 4 2.3 O[C@H](COc1cccc2c1CCCC2=O)CNC(C)(C)C nan
570 2270 33 None -3 7 Human 8.2 pIC50 = 8.2 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 291 5 2 4 2.3 O[C@H](COc1cccc2c1CCCC2=O)CNC(C)(C)C nan
CHEMBL1201237 2270 33 None -3 7 Human 8.2 pIC50 = 8.2 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 291 5 2 4 2.3 O[C@H](COc1cccc2c1CCCC2=O)CNC(C)(C)C nan
DB01210 2270 33 None -3 7 Human 8.2 pIC50 = 8.2 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 291 5 2 4 2.3 O[C@H](COc1cccc2c1CCCC2=O)CNC(C)(C)C nan
44268349 20361 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Tested for binding affinity against cloned human beta-1 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandTested for binding affinity against cloned human beta-1 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 7.2 pIC50 = 7.2 Binding
Tested for binding affinity against cloned human beta-1 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandTested for binding affinity against cloned human beta-1 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
1499 2052 43 None -33 17 Rat 6.2 pIC50 = 6.2 Binding
Compound was evaluated for its binding affinity towards beta-1 adrenergic receptor in rat heart membrane by displacing [125I]- iodocyanopindololCompound was evaluated for its binding affinity towards beta-1 adrenergic receptor in rat heart membrane by displacing [125I]- iodocyanopindolol
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm00094a025
3779 2052 43 None -33 17 Rat 6.2 pIC50 = 6.2 Binding
Compound was evaluated for its binding affinity towards beta-1 adrenergic receptor in rat heart membrane by displacing [125I]- iodocyanopindololCompound was evaluated for its binding affinity towards beta-1 adrenergic receptor in rat heart membrane by displacing [125I]- iodocyanopindolol
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm00094a025
536 2052 43 None -33 17 Rat 6.2 pIC50 = 6.2 Binding
Compound was evaluated for its binding affinity towards beta-1 adrenergic receptor in rat heart membrane by displacing [125I]- iodocyanopindololCompound was evaluated for its binding affinity towards beta-1 adrenergic receptor in rat heart membrane by displacing [125I]- iodocyanopindolol
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm00094a025
CHEMBL434 2052 43 None -33 17 Rat 6.2 pIC50 = 6.2 Binding
Compound was evaluated for its binding affinity towards beta-1 adrenergic receptor in rat heart membrane by displacing [125I]- iodocyanopindololCompound was evaluated for its binding affinity towards beta-1 adrenergic receptor in rat heart membrane by displacing [125I]- iodocyanopindolol
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm00094a025
DB01064 2052 43 None -33 17 Rat 6.2 pIC50 = 6.2 Binding
Compound was evaluated for its binding affinity towards beta-1 adrenergic receptor in rat heart membrane by displacing [125I]- iodocyanopindololCompound was evaluated for its binding affinity towards beta-1 adrenergic receptor in rat heart membrane by displacing [125I]- iodocyanopindolol
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm00094a025
46881576 7747 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]cyanopindolol from human beta 1 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 1 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 6.2 pIC50 = 6.2 Binding
Displacement of [125I]cyanopindolol from human beta 1 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 1 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
2249 509 106 None -5 12 Human 6.2 pIC50 = 6.2 Binding
Displacement of radiolabeled atenolol from human adrenergic beta-1 receptorDisplacement of radiolabeled atenolol from human adrenergic beta-1 receptor
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1021/jm8007618
255 509 106 None -5 12 Human 6.2 pIC50 = 6.2 Binding
Displacement of radiolabeled atenolol from human adrenergic beta-1 receptorDisplacement of radiolabeled atenolol from human adrenergic beta-1 receptor
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1021/jm8007618
548 509 106 None -5 12 Human 6.2 pIC50 = 6.2 Binding
Displacement of radiolabeled atenolol from human adrenergic beta-1 receptorDisplacement of radiolabeled atenolol from human adrenergic beta-1 receptor
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1021/jm8007618
CHEMBL24 509 106 None -5 12 Human 6.2 pIC50 = 6.2 Binding
Displacement of radiolabeled atenolol from human adrenergic beta-1 receptorDisplacement of radiolabeled atenolol from human adrenergic beta-1 receptor
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1021/jm8007618
DB00335 509 106 None -5 12 Human 6.2 pIC50 = 6.2 Binding
Displacement of radiolabeled atenolol from human adrenergic beta-1 receptorDisplacement of radiolabeled atenolol from human adrenergic beta-1 receptor
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1021/jm8007618
44307144 201906 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-1 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-1 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 6.2 pIC50 = 6.2 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-1 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-1 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
44298256 195426 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
In vitro binding affinity towards cloned human beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-1 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 6.2 pIC50 = 6.2 Binding
In vitro binding affinity towards cloned human beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-1 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
44301806 100240 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Binding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cellsBinding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cells
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 5.2 pIC50 = 5.2 Binding
Binding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cellsBinding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cells
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
46881938 6672 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I]cyanopindolol from human beta 1 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 1 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 5.2 pIC50 = 5.2 Binding
Displacement of [125I]cyanopindolol from human beta 1 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 1 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
44285226 99373 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
In vitro binding affinity at beta-1 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-1 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 5.2 pIC50 = 5.2 Binding
In vitro binding affinity at beta-1 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-1 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
44335628 4752 0 None - 0 Human 4.2 pIC50 = 4.2 Binding
Beta-1 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-1 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 4.2 pIC50 = 4.2 Binding
Beta-1 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-1 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
44335588 5186 0 None - 0 Human 4.2 pIC50 = 4.2 Binding
Beta-1 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-1 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 4.2 pIC50 = 4.2 Binding
Beta-1 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-1 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
44268273 96620 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Tested for binding affinity against cloned human beta-1 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandTested for binding affinity against cloned human beta-1 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 6.2 pIC50 = 6.2 Binding
Tested for binding affinity against cloned human beta-1 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandTested for binding affinity against cloned human beta-1 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
44349645 113006 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity for human Beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity for human Beta-1 adrenergic receptor 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 for human Beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity for human Beta-1 adrenergic receptor 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
12049926 201384 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Binding affinity for cloned human Beta-1 adrenergic receptor expressed in CHO cells, tested in the presence of I-iodocyanopindolol.Binding affinity for cloned human Beta-1 adrenergic receptor expressed in CHO cells, tested 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 5.2 pIC50 = 5.2 Binding
Binding affinity for cloned human Beta-1 adrenergic receptor expressed in CHO cells, tested in the presence of I-iodocyanopindolol.Binding affinity for cloned human Beta-1 adrenergic receptor expressed in CHO cells, tested 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
56663238 63756 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to adrenergic beta1 receptorBinding affinity to adrenergic beta1 receptor
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 - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to adrenergic beta1 receptorBinding affinity to adrenergic beta1 receptor
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
24901144 69971 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of radiolabeled iodocyanopindolol from beta1 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from beta1 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 7.2 pIC50 = 7.2 Binding
Displacement of radiolabeled iodocyanopindolol from beta1 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from beta1 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 7.2 pIC50 = 7.2 Binding
Displacement of radiolabeled iodocyanopindolol from beta1 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from beta1 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 7.2 pIC50 = 7.2 Binding
Displacement of radiolabeled iodocyanopindolol from beta1 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from beta1 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
57391554 70010 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of radiolabeled iodocyanopindolol from beta1 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from beta1 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 7.2 pIC50 = 7.2 Binding
Displacement of radiolabeled iodocyanopindolol from beta1 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from beta1 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
24900942 70031 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of radiolabeled iodocyanopindolol from beta1 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from beta1 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 7.2 pIC50 = 7.2 Binding
Displacement of radiolabeled iodocyanopindolol from beta1 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from beta1 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
44306991 201978 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-1 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-1 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 5.2 pIC50 = 5.2 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-1 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-1 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
9917962 167382 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity for human Beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity for human Beta-1 adrenergic receptor 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 7.2 pIC50 = 7.2 Binding
Binding affinity for human Beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity for human Beta-1 adrenergic receptor 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
44298787 193071 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
In vitro binding affinity towards cloned human beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-1 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 6.2 pIC50 = 6.2 Binding
In vitro binding affinity towards cloned human beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-1 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
44301804 167607 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Binding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cellsBinding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cells
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 5.2 pIC50 = 5.2 Binding
Binding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cellsBinding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cells
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
44313161 103286 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Compound was evaluated for its inhibitory activity against CHO cells expressing the cloned human Beta-1 adrenergic receptor in the presence of [125I]iodocyanopindololCompound was evaluated for its inhibitory activity against CHO cells expressing the cloned human Beta-1 adrenergic receptor in the presence of [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 5.2 pIC50 = 5.2 Binding
Compound was evaluated for its inhibitory activity against CHO cells expressing the cloned human Beta-1 adrenergic receptor in the presence of [125I]iodocyanopindololCompound was evaluated for its inhibitory activity against CHO cells expressing the cloned human Beta-1 adrenergic receptor in the presence of [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
12017017 126946 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
In vitro binding affinity at beta-1 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-1 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 5.2 pIC50 = 5.2 Binding
In vitro binding affinity at beta-1 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-1 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
12017013 135745 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
In vitro binding affinity at beta-1 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-1 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 5.2 pIC50 = 5.2 Binding
In vitro binding affinity at beta-1 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-1 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
12017002 141155 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
In vitro binding affinity at beta-1 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-1 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 5.2 pIC50 = 5.2 Binding
In vitro binding affinity at beta-1 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-1 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
44281470 113062 0 None - 0 Human 4.2 pIC50 = 4.2 Binding
Binding affinity to recombinant human beta-1 adrenergic receptor expressed in CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-1 adrenergic receptor expressed in 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 4.2 pIC50 = 4.2 Binding
Binding affinity to recombinant human beta-1 adrenergic receptor expressed in CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-1 adrenergic receptor expressed in 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
13864381 206593 3 None - 4 Guinea pig 4.2 pIC50 = 4.2 Binding
Inhibitory activity against beta-1 adrenergic receptor in guinea pig atria is determinedInhibitory activity against beta-1 adrenergic receptor in guinea pig atria is determined
ChEMBL 195 1 3 4 0.7 NCC1OCCc2c1ccc(O)c2O 10.1021/jm00073a006
CHEMBL542683 206593 3 None - 4 Guinea pig 4.2 pIC50 = 4.2 Binding
Inhibitory activity against beta-1 adrenergic receptor in guinea pig atria is determinedInhibitory activity against beta-1 adrenergic receptor in guinea pig atria is determined
ChEMBL 195 1 3 4 0.7 NCC1OCCc2c1ccc(O)c2O 10.1021/jm00073a006
CHEMBL99361 206593 3 None - 4 Guinea pig 4.2 pIC50 = 4.2 Binding
Inhibitory activity against beta-1 adrenergic receptor in guinea pig atria is determinedInhibitory activity against beta-1 adrenergic receptor in guinea pig atria is determined
ChEMBL 195 1 3 4 0.7 NCC1OCCc2c1ccc(O)c2O 10.1021/jm00073a006
13864389 4982 2 None - 2 Guinea pig 5.2 pIC50 = 5.2 Binding
Inhibitory activity against beta-1 adrenergic receptor in guinea pig atria is determinedInhibitory activity against beta-1 adrenergic receptor in guinea pig atria is determined
ChEMBL 195 1 3 4 0.7 NCC1OCCc2cc(O)c(O)cc21 10.1021/jm00073a006
CHEMBL105383 4982 2 None - 2 Guinea pig 5.2 pIC50 = 5.2 Binding
Inhibitory activity against beta-1 adrenergic receptor in guinea pig atria is determinedInhibitory activity against beta-1 adrenergic receptor in guinea pig atria is determined
ChEMBL 195 1 3 4 0.7 NCC1OCCc2cc(O)c(O)cc21 10.1021/jm00073a006
15123375 57174 3 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterolBinding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterol
ChEMBL 295 4 2 3 1.9 O=C(NCC1CN(c2ccccc2)CCN1)c1ccccc1 10.1021/jm00082a016
CHEMBL165901 57174 3 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterolBinding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterol
ChEMBL 295 4 2 3 1.9 O=C(NCC1CN(c2ccccc2)CCN1)c1ccccc1 10.1021/jm00082a016
16049087 63737 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to adrenergic beta1 receptorBinding affinity to adrenergic beta1 receptor
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 - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to adrenergic beta1 receptorBinding affinity to adrenergic beta1 receptor
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
16049088 63738 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to adrenergic beta1 receptorBinding affinity to adrenergic beta1 receptor
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 - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to adrenergic beta1 receptorBinding affinity to adrenergic beta1 receptor
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
16049024 63740 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to adrenergic beta1 receptorBinding affinity to adrenergic beta1 receptor
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 - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to adrenergic beta1 receptorBinding affinity to adrenergic beta1 receptor
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
24901284 70028 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of radiolabeled iodocyanopindolol from beta1 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from beta1 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 8.1 pIC50 = 8.1 Binding
Displacement of radiolabeled iodocyanopindolol from beta1 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from beta1 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
46881872 7650 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]cyanopindolol from human beta 1 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 1 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 6.2 pIC50 = 6.2 Binding
Displacement of [125I]cyanopindolol from human beta 1 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 1 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
44298849 194768 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
In vitro binding affinity towards cloned human beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-1 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 6.2 pIC50 = 6.2 Binding
In vitro binding affinity towards cloned human beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-1 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
44335663 4707 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Beta-1 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-1 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 5.2 pIC50 = 5.2 Binding
Beta-1 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-1 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
44335496 4718 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Beta-1 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-1 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 5.2 pIC50 = 5.2 Binding
Beta-1 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-1 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
44301831 100482 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Binding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cellsBinding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cells
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 5.2 pIC50 = 5.2 Binding
Binding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cellsBinding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cells
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 5.2 pIC50 = 5.2 Binding
Binding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cellsBinding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cells
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 5.2 pIC50 = 5.2 Binding
Binding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cellsBinding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cells
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
44281407 99828 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Binding affinity to recombinant human beta-1 adrenergic receptor expressed in CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-1 adrenergic receptor expressed in 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 5.2 pIC50 = 5.2 Binding
Binding affinity to recombinant human beta-1 adrenergic receptor expressed in CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-1 adrenergic receptor expressed in 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
44461706 204197 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Binding affinity towards Beta-1 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindololBinding affinity towards Beta-1 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 5.2 pIC50 = 5.2 Binding
Binding affinity towards Beta-1 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindololBinding affinity towards Beta-1 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
44285685 99739 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
In vitro binding affinity at beta-1 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-1 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 5.2 pIC50 = 5.2 Binding
In vitro binding affinity at beta-1 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-1 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
12043159 99538 0 None - 0 Human 4.2 pIC50 = 4.2 Binding
Binding affinity towards cloned human Beta-1 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity towards cloned human Beta-1 adrenergic receptor prepared from CHO cells 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 cloned human Beta-1 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity towards cloned human Beta-1 adrenergic receptor prepared from CHO cells 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
44281396 99484 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity to recombinant human beta-1 adrenergic receptor expressed in CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-1 adrenergic receptor expressed in 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 6.2 pIC50 = 6.2 Binding
Binding affinity to recombinant human beta-1 adrenergic receptor expressed in CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-1 adrenergic receptor expressed in 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
10119061 17759 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity for human Beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity for human Beta-1 adrenergic receptor 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 6.1 pIC50 = 6.1 Binding
Binding affinity for human Beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity for human Beta-1 adrenergic receptor 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
44268539 20212 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro affinity at Beta-1 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-1 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 6.1 pIC50 = 6.1 Binding
In vitro affinity at Beta-1 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-1 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
14739891 205986 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Tested for Beta-1 adrenergic receptor selectivity in canine cardiac tissue in anesthetized dogsTested for Beta-1 adrenergic receptor selectivity in canine cardiac 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 Human 5.1 pIC50 = 5.1 Binding
Tested for Beta-1 adrenergic receptor selectivity in canine cardiac tissue in anesthetized dogsTested for Beta-1 adrenergic receptor selectivity in canine cardiac tissue in anesthetized dogs
ChEMBL 408 12 3 6 1.8 COCCc1ccc(OCC(O)CNCc2ccc(NS(C)(=O)=O)cc2)cc1 10.1021/jm00172a033
1978 248 54 None -16 6 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 336 10 3 5 3.0 CCCC(=Nc1ccc(c(c1)C(=O)C)OCC(CNC(C)C)O)O nan
40 248 54 None -16 6 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 336 10 3 5 3.0 CCCC(=Nc1ccc(c(c1)C(=O)C)OCC(CNC(C)C)O)O nan
7107 248 54 None -16 6 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 336 10 3 5 3.0 CCCC(=Nc1ccc(c(c1)C(=O)C)OCC(CNC(C)C)O)O nan
CHEMBL642 248 54 None -16 6 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 336 10 3 5 3.0 CCCC(=Nc1ccc(c(c1)C(=O)C)OCC(CNC(C)C)O)O nan
DB01193 248 54 None -16 6 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 336 10 3 5 3.0 CCCC(=Nc1ccc(c(c1)C(=O)C)OCC(CNC(C)C)O)O nan
44349646 16675 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity for human Beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity for human Beta-1 adrenergic receptor 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 7.1 pIC50 = 7.1 Binding
Binding affinity for human Beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity for human Beta-1 adrenergic receptor 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
44349629 18323 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity for human Beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity for human Beta-1 adrenergic receptor 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 6.1 pIC50 = 6.1 Binding
Binding affinity for human Beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity for human Beta-1 adrenergic receptor 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
44268569 97729 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro affinity at Beta-1 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-1 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 6.1 pIC50 = 6.1 Binding
In vitro affinity at Beta-1 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-1 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
12017004 99680 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
In vitro binding affinity at beta-1 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-1 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 5.1 pIC50 = 5.1 Binding
In vitro binding affinity at beta-1 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-1 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
46881575 7687 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]cyanopindolol from human beta 1 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 1 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 5.1 pIC50 = 5.1 Binding
Displacement of [125I]cyanopindolol from human beta 1 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 1 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
9958539 102618 0 None -1 3 Human 6.1 pIC50 = 6.1 Binding
Compound was evaluated for its inhibitory activity against CHO cells expressing the cloned human Beta-1 adrenergic receptor in the presence of [125I]iodocyanopindololCompound was evaluated for its inhibitory activity against CHO cells expressing the cloned human Beta-1 adrenergic receptor in the presence of [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 6.1 pIC50 = 6.1 Binding
Compound was evaluated for its inhibitory activity against CHO cells expressing the cloned human Beta-1 adrenergic receptor in the presence of [125I]iodocyanopindololCompound was evaluated for its inhibitory activity against CHO cells expressing the cloned human Beta-1 adrenergic receptor in the presence of [125I]iodocyanopindolol
ChEMBL 527 3 2 5 3.4 COc1c(I)cc(CC2NCCc3nc(N)sc32)cc1I 10.1016/s0960-894x(00)00459-5
145947596 167127 0 None - 1 Rat 6.1 pIC50 = 6.1 Binding
Displacement of [3H]-CGP-12177 from adrenergic beta1 receptor in Wistar rat cortex incubated for 60 mins by microbeta liquid scintillation counting analysisDisplacement of [3H]-CGP-12177 from adrenergic beta1 receptor in Wistar rat cortex incubated for 60 mins by microbeta liquid scintillation counting analysis
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 Rat 6.1 pIC50 = 6.1 Binding
Displacement of [3H]-CGP-12177 from adrenergic beta1 receptor in Wistar rat cortex incubated for 60 mins by microbeta liquid scintillation counting analysisDisplacement of [3H]-CGP-12177 from adrenergic beta1 receptor in Wistar rat cortex incubated for 60 mins by microbeta liquid scintillation counting analysis
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 Rat 6.1 pIC50 = 6.1 Binding
Displacement of [3H]-CGP-12177 from adrenergic beta1 receptor in Wistar rat cortex incubated for 60 mins by microbeta liquid scintillation counting analysisDisplacement of [3H]-CGP-12177 from adrenergic beta1 receptor in Wistar rat cortex incubated for 60 mins by microbeta liquid scintillation counting analysis
ChEMBL 355 5 2 5 3.4 Cc1cccc2c(=O)c3ccc(OCC(O)CNC(C)(C)C)cc3oc12 10.1016/j.bmc.2018.04.038
16049448 63749 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to adrenergic beta1 receptorBinding affinity to adrenergic beta1 receptor
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 - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to adrenergic beta1 receptorBinding affinity to adrenergic beta1 receptor
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 - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to adrenergic beta1 receptorBinding affinity to adrenergic beta1 receptor
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 - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to adrenergic beta1 receptorBinding affinity to adrenergic beta1 receptor
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
24901209 69997 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of radiolabeled iodocyanopindolol from beta1 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from beta1 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 7.1 pIC50 = 7.1 Binding
Displacement of radiolabeled iodocyanopindolol from beta1 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from beta1 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
24900812 70009 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of radiolabeled iodocyanopindolol from beta1 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from beta1 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 7.1 pIC50 = 7.1 Binding
Displacement of radiolabeled iodocyanopindolol from beta1 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from beta1 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
44349379 18327 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity for human Beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity for human Beta-1 adrenergic receptor 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 6.1 pIC50 = 6.1 Binding
Binding affinity for human Beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity for human Beta-1 adrenergic receptor 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
56673674 63751 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity to adrenergic beta1 receptorBinding affinity to adrenergic beta1 receptor
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 - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity to adrenergic beta1 receptorBinding affinity to adrenergic beta1 receptor
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
24900874 70025 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of radiolabeled iodocyanopindolol from beta1 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from beta1 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 6.1 pIC50 = 6.1 Binding
Displacement of radiolabeled iodocyanopindolol from beta1 adrenoceptorDisplacement of radiolabeled iodocyanopindolol from beta1 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
44307113 168806 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-1 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-1 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 7.1 pIC50 = 7.1 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-1 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-1 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
44268570 97730 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro affinity at Beta-1 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-1 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-1 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-1 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
14739892 206499 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Tested for Beta-1 adrenergic receptor selectivity in canine cardiac tissue in anesthetized dogsTested for Beta-1 adrenergic receptor selectivity in canine cardiac tissue in anesthetized dogs
ChEMBL 337 8 2 5 2.7 Cc1ccccc1OCC(O)CNCc1ccc(-n2ccnc2)cc1 10.1021/jm00172a033
CHEMBL98773 206499 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Tested for Beta-1 adrenergic receptor selectivity in canine cardiac tissue in anesthetized dogsTested for Beta-1 adrenergic receptor selectivity in canine cardiac tissue in anesthetized dogs
ChEMBL 337 8 2 5 2.7 Cc1ccccc1OCC(O)CNCc1ccc(-n2ccnc2)cc1 10.1021/jm00172a033
44335603 106933 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Beta-1 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-1 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 5.1 pIC50 = 5.1 Binding
Beta-1 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-1 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
9915238 196479 1 None - 0 Human 5.1 pIC50 = 5.1 Binding
Beta-1 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-1 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 5.1 pIC50 = 5.1 Binding
Beta-1 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-1 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
81430 198400 100 None - 1 Human 5.1 pIC50 = 5.1 Binding
Binding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterolBinding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterol
ChEMBL 192 2 1 3 1.1 COc1cccc(N2CCNCC2)c1 10.1021/jm00082a016
CHEMBL59597 198400 100 None - 1 Human 5.1 pIC50 = 5.1 Binding
Binding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterolBinding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterol
ChEMBL 192 2 1 3 1.1 COc1cccc(N2CCNCC2)c1 10.1021/jm00082a016
15483879 99309 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity to recombinant human beta-1 adrenergic receptor expressed in CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-1 adrenergic receptor expressed in 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 5.1 pIC50 = 5.1 Binding
Binding affinity to recombinant human beta-1 adrenergic receptor expressed in CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-1 adrenergic receptor expressed in 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
44281395 99455 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity to recombinant human beta-1 adrenergic receptor expressed in CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-1 adrenergic receptor expressed in 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 5.1 pIC50 = 5.1 Binding
Binding affinity to recombinant human beta-1 adrenergic receptor expressed in CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-1 adrenergic receptor expressed in 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
12017015 122565 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
In vitro binding affinity at beta-1 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-1 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 5.1 pIC50 = 5.1 Binding
In vitro binding affinity at beta-1 adrenergic receptors in the presence of [125I]iodocyanopindolol.In vitro binding affinity at beta-1 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
9915238 196479 1 None - 0 Human 5.1 pIC50 = 5.1 Binding
In vitro binding affinity towards cloned human beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-1 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 5.1 pIC50 = 5.1 Binding
In vitro binding affinity towards cloned human beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-1 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
9896742 203226 0 None - 0 Human 4.1 pIC50 = 4.1 Binding
Compound was evaluated for its inhibitory activity against CHO cells expressing the cloned human Beta-1 adrenergic receptor in the presence of [125I]iodocyanopindololCompound was evaluated for its inhibitory activity against CHO cells expressing the cloned human Beta-1 adrenergic receptor in the presence of [125I]iodocyanopindolol
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 - 0 Human 4.1 pIC50 = 4.1 Binding
Compound was evaluated for its inhibitory activity against CHO cells expressing the cloned human Beta-1 adrenergic receptor in the presence of [125I]iodocyanopindololCompound was evaluated for its inhibitory activity against CHO cells expressing the cloned human Beta-1 adrenergic receptor in the presence of [125I]iodocyanopindolol
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
44268266 17809 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Tested for binding affinity against cloned human beta-1 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandTested for binding affinity against cloned human beta-1 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
Tested for binding affinity against cloned human beta-1 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandTested for binding affinity against cloned human beta-1 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
44349357 159350 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity for human Beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity for human Beta-1 adrenergic receptor 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 6.1 pIC50 = 6.1 Binding
Binding affinity for human Beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity for human Beta-1 adrenergic receptor 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
44338578 110073 0 None - 0 Guinea pig 6.1 pIC50 = 6.1 Binding
Beta-1 adrenergic receptor blocking was assessed from 50% inhibition of the isoproterenol submaximal response on isolated Guinea pig atria(IA)Beta-1 adrenergic receptor blocking was assessed from 50% inhibition of the isoproterenol submaximal response on isolated Guinea pig atria(IA)
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 6.1 pIC50 = 6.1 Binding
Beta-1 adrenergic receptor blocking was assessed from 50% inhibition of the isoproterenol submaximal response on isolated Guinea pig atria(IA)Beta-1 adrenergic receptor blocking was assessed from 50% inhibition of the isoproterenol submaximal response on isolated Guinea pig atria(IA)
ChEMBL 378 6 2 5 3.4 COC12CCCCC1c1ccc(F)cc1/C2=N/OCC(O)CNC(C)(C)C 10.1021/jm00122a008
44349237 162875 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity for human Beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity for human Beta-1 adrenergic receptor 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 6.1 pIC50 = 6.1 Binding
Binding affinity for human Beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity for human Beta-1 adrenergic receptor 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
44268352 15349 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Tested for binding affinity against cloned human beta-1 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandTested for binding affinity against cloned human beta-1 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 6.1 pIC50 = 6.1 Binding
Tested for binding affinity against cloned human beta-1 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandTested for binding affinity against cloned human beta-1 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
46881617 7846 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]cyanopindolol from human beta 1 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 1 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 1 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 1 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
46901383 15248 18 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of beta-1 adrenoceptorInhibition of beta-1 adrenoceptor
ChEMBL 380 5 3 6 2.4 NC(=O)c1cc(-c2ccnc(NC3CCCCC3)c2)nc(N2CCNCC2)c1 10.1021/jm100076w
CHEMBL1214999 15248 18 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of beta-1 adrenoceptorInhibition of beta-1 adrenoceptor
ChEMBL 380 5 3 6 2.4 NC(=O)c1cc(-c2ccnc(NC3CCCCC3)c2)nc(N2CCNCC2)c1 10.1021/jm100076w
10442852 11095 0 None - 2 Guinea pig 5.1 pIC50 = 5.1 Binding
Inhibitory concentration against beta-1-adrenergic receptor in isolated guinea pig atriaInhibitory concentration against beta-1-adrenergic receptor in isolated guinea pig atria
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 5.1 pIC50 = 5.1 Binding
Inhibitory concentration against beta-1-adrenergic receptor in isolated guinea pig atriaInhibitory concentration against beta-1-adrenergic receptor in isolated guinea pig atria
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 5.1 pIC50 = 5.1 Binding
Inhibitory concentration against beta-1-adrenergic receptor in isolated guinea pig atriaInhibitory concentration against beta-1-adrenergic receptor in isolated guinea pig atria
ChEMBL 202 6 2 4 1.1 CCCO/N=C/C(O)CNC(C)(C)C 10.1021/jm00036a018
10076885 99310 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity towards cloned human Beta-1 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity towards cloned human Beta-1 adrenergic receptor prepared from CHO cells 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 5.1 pIC50 = 5.1 Binding
Binding affinity towards cloned human Beta-1 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity towards cloned human Beta-1 adrenergic receptor prepared from CHO cells 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
46881752 7169 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]cyanopindolol from human beta 1 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 1 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counter
ChEMBL 431 9 4 6 3.6 O=C(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)OCc1nc2ccccc2[nH]1 10.1016/j.bmcl.2010.01.130
CHEMBL1085928 7169 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]cyanopindolol from human beta 1 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 1 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counter
ChEMBL 431 9 4 6 3.6 O=C(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)OCc1nc2ccccc2[nH]1 10.1016/j.bmcl.2010.01.130
10101116 14348 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity for human Beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity for human Beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand in CHO cells
ChEMBL 684 11 4 9 6.8 N#CN/C(=N\c1cccc2c1CCN2c1nc(-c2ccc(OC(F)(F)F)cc2)cs1)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/s0960-894x(00)00669-7
CHEMBL120238 14348 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity for human Beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity for human Beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand in CHO cells
ChEMBL 684 11 4 9 6.8 N#CN/C(=N\c1cccc2c1CCN2c1nc(-c2ccc(OC(F)(F)F)cc2)cs1)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/s0960-894x(00)00669-7
10722793 112835 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity was evaluated on chinese hamster ovary (CHO) cells expressing the cloned human beta-1 adrenergic receptor in the presence of [125I]- iodocyanopindolol.Binding affinity was evaluated on chinese hamster ovary (CHO) cells expressing the cloned human beta-1 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 5.1 pIC50 = 5.1 Binding
Binding affinity was evaluated on chinese hamster ovary (CHO) cells expressing the cloned human beta-1 adrenergic receptor in the presence of [125I]- iodocyanopindolol.Binding affinity was evaluated on chinese hamster ovary (CHO) cells expressing the cloned human beta-1 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
44338127 7564 0 None - 0 Guinea pig 6.1 pIC50 = 6.1 Binding
Beta-1 adrenergic receptor blocking was assessed from 50% inhibition of the isoproterenol submaximal response on isolated Guinea pig atria(IA)Beta-1 adrenergic receptor blocking was assessed from 50% inhibition of the isoproterenol submaximal response on isolated Guinea pig atria(IA)
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 6.1 pIC50 = 6.1 Binding
Beta-1 adrenergic receptor blocking was assessed from 50% inhibition of the isoproterenol submaximal response on isolated Guinea pig atria(IA)Beta-1 adrenergic receptor blocking was assessed from 50% inhibition of the isoproterenol submaximal response on isolated Guinea pig atria(IA)
ChEMBL 390 8 3 6 2.6 CC(C)(C)NCC(O)CO/N=C1/c2ccccc2C2CCCCC12OCCO 10.1021/jm00122a008
44301866 100096 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cellsBinding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cells
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 6.1 pIC50 = 6.1 Binding
Binding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cellsBinding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cells
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
44377514 56205 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity towards Beta-1 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindololBinding affinity towards Beta-1 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-1 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindololBinding affinity towards Beta-1 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
44461486 203642 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity towards Beta-1 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindololBinding affinity towards Beta-1 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 5.1 pIC50 = 5.1 Binding
Binding affinity towards Beta-1 adrenergic receptor in CHO cells expressing the cloned human receptor using 125I]iodocyanopindololBinding affinity towards Beta-1 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
44280795 112072 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity towards cloned human Beta-1 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity towards cloned human Beta-1 adrenergic receptor prepared from CHO cells 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 cloned human Beta-1 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity towards cloned human Beta-1 adrenergic receptor prepared from CHO cells 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
15523860 119653 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity towards human Beta-1 adrenergic receptor expressed in CHO cells, using 125I]iodocyanopindololBinding affinity towards human Beta-1 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 5.1 pIC50 = 5.1 Binding
Binding affinity towards human Beta-1 adrenergic receptor expressed in CHO cells, using 125I]iodocyanopindololBinding affinity towards human Beta-1 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
44307396 202046 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-1 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-1 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 6.1 pIC50 = 6.1 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-1 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-1 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
46881750 7130 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]cyanopindolol from human beta 1 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 1 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 5.1 pIC50 = 5.1 Binding
Displacement of [125I]cyanopindolol from human beta 1 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 1 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
12049914 201890 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity for cloned human Beta-1 adrenergic receptor expressed in CHO cells, tested in the presence of I-iodocyanopindolol.Binding affinity for cloned human Beta-1 adrenergic receptor expressed in CHO cells, tested 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 cloned human Beta-1 adrenergic receptor expressed in CHO cells, tested in the presence of I-iodocyanopindolol.Binding affinity for cloned human Beta-1 adrenergic receptor expressed in CHO cells, tested 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
44268509 19208 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro affinity at Beta-1 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-1 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 6.1 pIC50 = 6.1 Binding
In vitro affinity at Beta-1 adrenergic receptor in the presence of [125I]iodocyanopindolol.In vitro affinity at Beta-1 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
44338133 9127 0 None - 0 Guinea pig 6.1 pIC50 = 6.1 Binding
Beta-1 adrenergic receptor blocking was assessed from 50% inhibition of the isoproterenol submaximal response on isolated Guinea pig atria(IA)Beta-1 adrenergic receptor blocking was assessed from 50% inhibition of the isoproterenol submaximal response on isolated Guinea pig atria(IA)
ChEMBL 346 6 3 5 2.6 CC(C)NCC(O)CO/N=C1/c2ccccc2C2CCCCCC12O 10.1021/jm00122a008
CHEMBL110659 9127 0 None - 0 Guinea pig 6.1 pIC50 = 6.1 Binding
Beta-1 adrenergic receptor blocking was assessed from 50% inhibition of the isoproterenol submaximal response on isolated Guinea pig atria(IA)Beta-1 adrenergic receptor blocking was assessed from 50% inhibition of the isoproterenol submaximal response on isolated Guinea pig atria(IA)
ChEMBL 346 6 3 5 2.6 CC(C)NCC(O)CO/N=C1/c2ccccc2C2CCCCCC12O 10.1021/jm00122a008
2464 3570 52 None -2 6 Human 5.1 pIC50 = 5.1 Binding
Tested for Beta-1 adrenergic receptor selectivity in canine cardiac tissue in anesthetized dogsTested for Beta-1 adrenergic receptor selectivity in canine cardiac 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 -2 6 Human 5.1 pIC50 = 5.1 Binding
Tested for Beta-1 adrenergic receptor selectivity in canine cardiac tissue in anesthetized dogsTested for Beta-1 adrenergic receptor selectivity in canine cardiac 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 -2 6 Human 5.1 pIC50 = 5.1 Binding
Tested for Beta-1 adrenergic receptor selectivity in canine cardiac tissue in anesthetized dogsTested for Beta-1 adrenergic receptor selectivity in canine cardiac 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 -2 6 Human 5.1 pIC50 = 5.1 Binding
Tested for Beta-1 adrenergic receptor selectivity in canine cardiac tissue in anesthetized dogsTested for Beta-1 adrenergic receptor selectivity in canine cardiac 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 -2 6 Human 5.1 pIC50 = 5.1 Binding
Tested for Beta-1 adrenergic receptor selectivity in canine cardiac tissue in anesthetized dogsTested for Beta-1 adrenergic receptor selectivity in canine cardiac tissue in anesthetized dogs
ChEMBL 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C 10.1021/jm00172a033
44307205 202110 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-1 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-1 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 6.1 pIC50 = 6.1 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-1 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-1 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
44298852 101260 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro binding affinity towards cloned human beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-1 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 6.1 pIC50 = 6.1 Binding
In vitro binding affinity towards cloned human beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-1 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
44268322 18768 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Tested for binding affinity against cloned human beta-1 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandTested for binding affinity against cloned human beta-1 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 6.1 pIC50 = 6.1 Binding
Tested for binding affinity against cloned human beta-1 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligandTested for binding affinity against cloned human beta-1 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
44301843 197917 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cellsBinding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cells
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 5.1 pIC50 = 5.1 Binding
Binding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cellsBinding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cells
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
2464 3570 52 None -2 6 Human 5.1 pIC50 = 5.1 Binding
Binding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterolBinding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterol
ChEMBL 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C 10.1021/jm00082a016
5253 3570 52 None -2 6 Human 5.1 pIC50 = 5.1 Binding
Binding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterolBinding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterol
ChEMBL 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C 10.1021/jm00082a016
7297 3570 52 None -2 6 Human 5.1 pIC50 = 5.1 Binding
Binding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterolBinding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterol
ChEMBL 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C 10.1021/jm00082a016
CHEMBL471 3570 52 None -2 6 Human 5.1 pIC50 = 5.1 Binding
Binding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterolBinding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterol
ChEMBL 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C 10.1021/jm00082a016
DB00489 3570 52 None -2 6 Human 5.1 pIC50 = 5.1 Binding
Binding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterolBinding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterol
ChEMBL 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C 10.1021/jm00082a016
44281343 109867 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity to recombinant human beta-1 adrenergic receptor expressed in CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-1 adrenergic receptor expressed in 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-1 adrenergic receptor expressed in CHO cells in the presence of [125I]iodocyanopindololBinding affinity to recombinant human beta-1 adrenergic receptor expressed in 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
44280858 99339 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity towards cloned human Beta-1 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity towards cloned human Beta-1 adrenergic receptor prepared from CHO cells 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 5.1 pIC50 = 5.1 Binding
Binding affinity towards cloned human Beta-1 adrenergic receptor prepared from CHO cells in the presence of [125I]iodocyanopindololBinding affinity towards cloned human Beta-1 adrenergic receptor prepared from CHO cells 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
2464 3570 52 None -2 6 Human 5.1 pIC50 = 5.1 Binding
In vitro Beta-1 adrenergic receptor affinity in partially purified membrane fractions from canine cardiac tissue using [SH]dihydroalprenolol (4.5 nM)In vitro Beta-1 adrenergic receptor affinity in partially purified membrane fractions from canine cardiac 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 -2 6 Human 5.1 pIC50 = 5.1 Binding
In vitro Beta-1 adrenergic receptor affinity in partially purified membrane fractions from canine cardiac tissue using [SH]dihydroalprenolol (4.5 nM)In vitro Beta-1 adrenergic receptor affinity in partially purified membrane fractions from canine cardiac 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 -2 6 Human 5.1 pIC50 = 5.1 Binding
In vitro Beta-1 adrenergic receptor affinity in partially purified membrane fractions from canine cardiac tissue using [SH]dihydroalprenolol (4.5 nM)In vitro Beta-1 adrenergic receptor affinity in partially purified membrane fractions from canine cardiac 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 -2 6 Human 5.1 pIC50 = 5.1 Binding
In vitro Beta-1 adrenergic receptor affinity in partially purified membrane fractions from canine cardiac tissue using [SH]dihydroalprenolol (4.5 nM)In vitro Beta-1 adrenergic receptor affinity in partially purified membrane fractions from canine cardiac 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 -2 6 Human 5.1 pIC50 = 5.1 Binding
In vitro Beta-1 adrenergic receptor affinity in partially purified membrane fractions from canine cardiac tissue using [SH]dihydroalprenolol (4.5 nM)In vitro Beta-1 adrenergic receptor affinity in partially purified membrane fractions from canine cardiac 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
44298700 101463 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
In vitro binding affinity towards cloned human beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-1 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 5.1 pIC50 = 5.1 Binding
In vitro binding affinity towards cloned human beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-1 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
44268341 22541 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Tested for binding affinity against cloned human beta-1 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligand.Tested for binding affinity against cloned human beta-1 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 5.1 pIC50 = 5.1 Binding
Tested for binding affinity against cloned human beta-1 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligand.Tested for binding affinity against cloned human beta-1 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
44301880 196952 0 None - 0 Human 4.1 pIC50 = 4.1 Binding
Binding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cellsBinding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cells
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 4.1 pIC50 = 4.1 Binding
Binding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cellsBinding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cells
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
44307166 102235 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-1 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-1 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 6.0 pIC50 = 6.0 Binding
Evaluated for its agonist activity and the binding affinity against human Beta-1 adrenergic receptor in membranes from chinese hamster ovary cellEvaluated for its agonist activity and the binding affinity against human Beta-1 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
12049925 98228 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity for cloned human Beta-1 adrenergic receptor expressed in CHO cells, tested in the presence of I-iodocyanopindolol.Binding affinity for cloned human Beta-1 adrenergic receptor expressed in CHO cells, tested 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 6.0 pIC50 = 6.0 Binding
Binding affinity for cloned human Beta-1 adrenergic receptor expressed in CHO cells, tested in the presence of I-iodocyanopindolol.Binding affinity for cloned human Beta-1 adrenergic receptor expressed in CHO cells, tested 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
12049924 202091 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity for cloned human Beta-1 adrenergic receptor expressed in CHO cells, tested in the presence of I-iodocyanopindolol.Binding affinity for cloned human Beta-1 adrenergic receptor expressed in CHO cells, tested 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 6.0 pIC50 = 6.0 Binding
Binding affinity for cloned human Beta-1 adrenergic receptor expressed in CHO cells, tested in the presence of I-iodocyanopindolol.Binding affinity for cloned human Beta-1 adrenergic receptor expressed in CHO cells, tested 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
44301867 100097 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cellsBinding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cells
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 6.0 pIC50 = 6.0 Binding
Binding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cellsBinding affinity (measured using [125I]iodocyanopindolol) against human Beta-1 adrenergic receptor expressed in CHO cells
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
46881531 6896 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of [125I]cyanopindolol from human beta 1 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 1 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(Cc1n[nH]c2ccccc12)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/j.bmcl.2010.01.130
CHEMBL1084667 6896 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of [125I]cyanopindolol from human beta 1 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 1 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(Cc1n[nH]c2ccccc12)Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1 10.1016/j.bmcl.2010.01.130
44335548 109264 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Beta-1 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-1 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 6.0 pIC50 = 6.0 Binding
Beta-1 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindololBeta-1 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
44298781 100214 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
In vitro binding affinity towards cloned human beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-1 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 = 6.0 Binding
In vitro binding affinity towards cloned human beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand to stimulate increase in cAMP in CHO cellsIn vitro binding affinity towards cloned human beta-1 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
10160636 112986 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity for human Beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity for human Beta-1 adrenergic receptor 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 6.0 pIC50 = 6.0 Binding
Binding affinity for human Beta-1 adrenergic receptor using [125I]iodocyanopindolol as radioligand in CHO cellsBinding affinity for human Beta-1 adrenergic receptor 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
46882028 5666 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of [125I]cyanopindolol from human beta 1 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 1 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 5.0 pIC50 = 5.0 Binding
Displacement of [125I]cyanopindolol from human beta 1 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counterDisplacement of [125I]cyanopindolol from human beta 1 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
164612037 184785 0 None -1 20 Human 10.1 pKd = 10.1 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]CGP12177 from human beta-1 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 10.1 pKd = 10.1 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]CGP12177 from human beta-1 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 -5 20 Human 10.1 pKd = 10.1 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]CGP12177 from human beta-1 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 -5 20 Human 10.1 pKd = 10.1 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]CGP12177 from human beta-1 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 -5 20 Human 10.1 pKd = 10.1 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]CGP12177 from human beta-1 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 10.1 pKd = 10.1 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]CGP12177 from human beta-1 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 10.1 pKd = 10.1 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]CGP12177 from human beta-1 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 10.1 pKd = 10.1 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]CGP12177 from human beta-1 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 10.1 pKd = 10.1 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]CGP12177 from human beta-1 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 10.1 pKd = 10.1 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]CGP12177 from human beta-1 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 10.1 pKd = 10.1 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenergic receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysisDisplacement of [3H]CGP12177 from human beta-1 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
21595418 102153 0 None -2 2 Guinea pig 9.8 pKd = 9.8 Binding
Beta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atriumBeta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atrium
ChEMBL 271 4 2 3 2.7 O[C@H](COc1cccc2ccccc12)[C@@H]1CCCCN1 10.1021/jm00119a011
CHEMBL304344 102153 0 None -2 2 Guinea pig 9.8 pKd = 9.8 Binding
Beta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atriumBeta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atrium
ChEMBL 271 4 2 3 2.7 O[C@H](COc1cccc2ccccc12)[C@@H]1CCCCN1 10.1021/jm00119a011
33624 3749 29 None -3 9 Guinea pig 9.4 pKd = 9.4 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C 10.1021/jm00361a004
4061 3749 29 None -3 9 Guinea pig 9.4 pKd = 9.4 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C 10.1021/jm00361a004
565 3749 29 None -3 9 Guinea pig 9.4 pKd = 9.4 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C 10.1021/jm00361a004
CHEMBL499 3749 29 None -3 9 Guinea pig 9.4 pKd = 9.4 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C 10.1021/jm00361a004
DB00373 3749 29 None -3 9 Guinea pig 9.4 pKd = 9.4 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C 10.1021/jm00361a004
33624 3749 29 None -3 9 Guinea pig 9.4 pKd = 9.4 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C 10.1021/jm00156a028
4061 3749 29 None -3 9 Guinea pig 9.4 pKd = 9.4 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C 10.1021/jm00156a028
565 3749 29 None -3 9 Guinea pig 9.4 pKd = 9.4 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C 10.1021/jm00156a028
CHEMBL499 3749 29 None -3 9 Guinea pig 9.4 pKd = 9.4 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C 10.1021/jm00156a028
DB00373 3749 29 None -3 9 Guinea pig 9.4 pKd = 9.4 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C 10.1021/jm00156a028
12179890 94184 1 None 3 2 Human 9.4 pKd = 9.4 Binding
Binding affinity to beta-1 adrenergic receptorBinding affinity to beta-1 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 9.4 pKd = 9.4 Binding
Binding affinity to beta-1 adrenergic receptorBinding affinity to beta-1 adrenergic receptor
ChEMBL 223 6 2 3 1.7 Cc1cccc(OC[C@@H](O)CNC(C)C)c1 10.1021/jm800227h
12878481 59659 0 None 169 2 Guinea pig 9.1 pKd = 9.1 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
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 9.1 pKd = 9.1 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
ChEMBL 341 7 3 4 2.6 OC(CNC1CC1)COc1ccc(-c2nc(C(F)(F)F)c[nH]2)cc1 10.1021/jm00361a004
13157386 62832 1 None 138 2 Guinea pig 9.1 pKd = 9.1 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
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 9.1 pKd = 9.1 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
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 9.1 pKd = 9.1 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
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 9.1 pKd = 9.1 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
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 9.1 pKd = 9.1 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
ChEMBL 479 12 3 7 4.4 COc1ccc(CCNCC(O)COc2ccc(-c3nc(-c4cccs4)c[nH]3)cc2)cc1OC 10.1021/jm00156a028
12878477 103046 0 None 10 2 Guinea pig 9.1 pKd = 9.1 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
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 9.1 pKd = 9.1 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
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
123686 1942 44 None 1 9 Guinea pig 9.0 pKd = 9.0 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
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 1 9 Guinea pig 9.0 pKd = 9.0 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
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 1 9 Guinea pig 9.0 pKd = 9.0 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
ChEMBL 354 9 4 5 1.7 C1=CC=C(C=C1)NC(=O)NCCNCC(COC2=CC=CC=C2C#N)O 10.1021/jm00156a028
25271869 158073 2 None -38 2 Human 9.0 pKd = 9.0 Binding
Displacement of [3H](-)CGP12177 from human beta1-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting methodDisplacement of [3H](-)CGP12177 from human beta1-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 9.0 pKd = 9.0 Binding
Displacement of [3H](-)CGP12177 from human beta1-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting methodDisplacement of [3H](-)CGP12177 from human beta1-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
2685 875 15 None -1 7 Human 9.0 pKd = 9.0 Binding
Displacement of [3H](-)CGP12177 from human beta1-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting methodDisplacement of [3H](-)CGP12177 from human beta1-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 -1 7 Human 9.0 pKd = 9.0 Binding
Displacement of [3H](-)CGP12177 from human beta1-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting methodDisplacement of [3H](-)CGP12177 from human beta1-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 -1 7 Human 9.0 pKd = 9.0 Binding
Displacement of [3H](-)CGP12177 from human beta1-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting methodDisplacement of [3H](-)CGP12177 from human beta1-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
13157406 9324 0 None 144 2 Guinea pig 8.9 pKd = 8.9 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
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 8.9 pKd = 8.9 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
ChEMBL 357 8 3 5 3.5 CC(C)NCC(O)COc1ccc(-c2nc(-c3cccs3)c[nH]2)cc1 10.1021/jm00361a004
13157406 9324 0 None 144 2 Guinea pig 8.9 pKd = 8.9 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
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 8.9 pKd = 8.9 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
ChEMBL 357 8 3 5 3.5 CC(C)NCC(O)COc1ccc(-c2nc(-c3cccs3)c[nH]2)cc1 10.1021/jm00156a028
13157406 9324 0 None 144 2 Guinea pig 8.9 pKd = 8.9 Binding
Activity at beta-1 adrenergic receptorActivity at beta-1 adrenergic receptor
ChEMBL 357 8 3 5 3.5 CC(C)NCC(O)COc1ccc(-c2nc(-c3cccs3)c[nH]2)cc1 10.1021/jm00103a004
CHEMBL11171 9324 0 None 144 2 Guinea pig 8.9 pKd = 8.9 Binding
Activity at beta-1 adrenergic receptorActivity at beta-1 adrenergic receptor
ChEMBL 357 8 3 5 3.5 CC(C)NCC(O)COc1ccc(-c2nc(-c3cccs3)c[nH]2)cc1 10.1021/jm00103a004
13621703 9278 0 None - 1 Guinea pig 8.8 pKd = 8.8 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
ChEMBL 439 12 3 6 3.8 COc1ccc(CCNCC(O)COc2ccc(-c3nc(C(C)C)c[nH]3)cc2)cc1OC 10.1021/jm00156a028
CHEMBL11145 9278 0 None - 1 Guinea pig 8.8 pKd = 8.8 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
ChEMBL 439 12 3 6 3.8 COc1ccc(CCNCC(O)COc2ccc(-c3nc(C(C)C)c[nH]3)cc2)cc1OC 10.1021/jm00156a028
13040879 23636 0 None -1 2 Guinea pig 8.8 pKd = 8.8 Binding
Ability to block Beta-1 adrenergic receptor in guinea pig right atria preparationAbility to block Beta-1 adrenergic receptor in guinea pig right atria 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 8.8 pKd = 8.8 Binding
Ability to block Beta-1 adrenergic receptor in guinea pig right atria preparationAbility to block Beta-1 adrenergic receptor in guinea pig right atria preparation
ChEMBL 281 6 2 5 1.6 COC(=O)c1ccccc1OCC(O)CNC(C)(C)C 10.1021/jm00354a003
2369 615 75 None 5 8 Human 8.8 pKd = 8.8 Binding
Antagonist activity against beta-1 adrenergic receptor (unknown origin)Antagonist activity against beta-1 adrenergic receptor (unknown origin)
ChEMBL 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C 10.1021/acs.jmedchem.5b00201
356 615 75 None 5 8 Human 8.8 pKd = 8.8 Binding
Antagonist activity against beta-1 adrenergic receptor (unknown origin)Antagonist activity against beta-1 adrenergic receptor (unknown origin)
ChEMBL 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C 10.1021/acs.jmedchem.5b00201
549 615 75 None 5 8 Human 8.8 pKd = 8.8 Binding
Antagonist activity against beta-1 adrenergic receptor (unknown origin)Antagonist activity against beta-1 adrenergic receptor (unknown origin)
ChEMBL 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C 10.1021/acs.jmedchem.5b00201
CHEMBL423 615 75 None 5 8 Human 8.8 pKd = 8.8 Binding
Antagonist activity against beta-1 adrenergic receptor (unknown origin)Antagonist activity against beta-1 adrenergic receptor (unknown origin)
ChEMBL 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C 10.1021/acs.jmedchem.5b00201
DB00195 615 75 None 5 8 Human 8.8 pKd = 8.8 Binding
Antagonist activity against beta-1 adrenergic receptor (unknown origin)Antagonist activity against beta-1 adrenergic receptor (unknown origin)
ChEMBL 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C 10.1021/acs.jmedchem.5b00201
12521601 128111 0 None 20 2 Guinea pig 8.8 pKd = 8.8 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
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 8.8 pKd = 8.8 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
ChEMBL 371 7 3 5 3.9 CC(C)(C)NCC(O)COc1ccc(-c2nc(-c3cccs3)c[nH]2)cc1 10.1021/jm00361a004
2685 875 15 None -1 7 Human 8.8 pKd = 8.8 Binding
Displacement of [3H]-CGP12177 from human beta1 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta1 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 -1 7 Human 8.8 pKd = 8.8 Binding
Displacement of [3H]-CGP12177 from human beta1 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta1 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 -1 7 Human 8.8 pKd = 8.8 Binding
Displacement of [3H]-CGP12177 from human beta1 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta1 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
3123920 2774 79 None 2 6 Guinea pig 8.8 pKd = 8.8 Binding
Beta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atriumBeta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atrium
ChEMBL 209 6 2 3 1.4 OC(COc1ccccc1)CNC(C)C 10.1021/jm00119a011
546 2774 79 None 2 6 Guinea pig 8.8 pKd = 8.8 Binding
Beta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atriumBeta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atrium
ChEMBL 209 6 2 3 1.4 OC(COc1ccccc1)CNC(C)C 10.1021/jm00119a011
CHEMBL7154 2774 79 None 2 6 Guinea pig 8.8 pKd = 8.8 Binding
Beta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atriumBeta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atrium
ChEMBL 209 6 2 3 1.4 OC(COc1ccccc1)CNC(C)C 10.1021/jm00119a011
2369 615 75 None -13 8 Guinea pig 8.8 pKd = 8.8 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
ChEMBL 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C 10.1021/jm00361a004
356 615 75 None -13 8 Guinea pig 8.8 pKd = 8.8 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
ChEMBL 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C 10.1021/jm00361a004
549 615 75 None -13 8 Guinea pig 8.8 pKd = 8.8 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
ChEMBL 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C 10.1021/jm00361a004
CHEMBL423 615 75 None -13 8 Guinea pig 8.8 pKd = 8.8 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
ChEMBL 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C 10.1021/jm00361a004
DB00195 615 75 None -13 8 Guinea pig 8.8 pKd = 8.8 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
ChEMBL 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C 10.1021/jm00361a004
165193 3126 60 None -7 43 Guinea pig 8.8 pKd = 8.8 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00361a004
2303 3126 60 None -7 43 Guinea pig 8.8 pKd = 8.8 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00361a004
4946 3126 60 None -7 43 Guinea pig 8.8 pKd = 8.8 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00361a004
564 3126 60 None -7 43 Guinea pig 8.8 pKd = 8.8 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00361a004
62882 3126 60 None -7 43 Guinea pig 8.8 pKd = 8.8 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00361a004
63 3126 60 None -7 43 Guinea pig 8.8 pKd = 8.8 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00361a004
66366 3126 60 None -7 43 Guinea pig 8.8 pKd = 8.8 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00361a004
91536 3126 60 None -7 43 Guinea pig 8.8 pKd = 8.8 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00361a004
CHEMBL27 3126 60 None -7 43 Guinea pig 8.8 pKd = 8.8 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00361a004
CHEMBL452861 3126 60 None -7 43 Guinea pig 8.8 pKd = 8.8 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00361a004
DB00571 3126 60 None -7 43 Guinea pig 8.8 pKd = 8.8 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00361a004
2369 615 75 None -13 8 Guinea pig 8.8 pKd = 8.8 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
ChEMBL 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C 10.1021/jm00156a028
356 615 75 None -13 8 Guinea pig 8.8 pKd = 8.8 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
ChEMBL 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C 10.1021/jm00156a028
549 615 75 None -13 8 Guinea pig 8.8 pKd = 8.8 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
ChEMBL 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C 10.1021/jm00156a028
CHEMBL423 615 75 None -13 8 Guinea pig 8.8 pKd = 8.8 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
ChEMBL 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C 10.1021/jm00156a028
DB00195 615 75 None -13 8 Guinea pig 8.8 pKd = 8.8 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
ChEMBL 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C 10.1021/jm00156a028
165193 3126 60 None -7 43 Guinea pig 8.8 pKd = 8.8 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00156a028
2303 3126 60 None -7 43 Guinea pig 8.8 pKd = 8.8 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00156a028
4946 3126 60 None -7 43 Guinea pig 8.8 pKd = 8.8 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00156a028
564 3126 60 None -7 43 Guinea pig 8.8 pKd = 8.8 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00156a028
62882 3126 60 None -7 43 Guinea pig 8.8 pKd = 8.8 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00156a028
63 3126 60 None -7 43 Guinea pig 8.8 pKd = 8.8 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00156a028
66366 3126 60 None -7 43 Guinea pig 8.8 pKd = 8.8 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00156a028
91536 3126 60 None -7 43 Guinea pig 8.8 pKd = 8.8 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00156a028
CHEMBL27 3126 60 None -7 43 Guinea pig 8.8 pKd = 8.8 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00156a028
CHEMBL452861 3126 60 None -7 43 Guinea pig 8.8 pKd = 8.8 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00156a028
DB00571 3126 60 None -7 43 Guinea pig 8.8 pKd = 8.8 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00156a028
18047 201915 18 None 2 5 Guinea pig 8.8 pKd = 8.8 Binding
Beta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atriumBeta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atrium
ChEMBL 223 6 2 3 1.7 Cc1cccc(OCC(O)CNC(C)C)c1 10.1021/jm00119a011
CHEMBL67096 201915 18 None 2 5 Guinea pig 8.8 pKd = 8.8 Binding
Beta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atriumBeta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atrium
ChEMBL 223 6 2 3 1.7 Cc1cccc(OCC(O)CNC(C)C)c1 10.1021/jm00119a011
13267804 202297 0 None -1 2 Guinea pig 8.8 pKd = 8.8 Binding
Beta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atriumBeta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atrium
ChEMBL 271 4 2 3 2.7 O[C@H](COc1cccc2ccccc12)[C@H]1CCCCN1 10.1021/jm00119a011
CHEMBL69635 202297 0 None -1 2 Guinea pig 8.8 pKd = 8.8 Binding
Beta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atriumBeta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atrium
ChEMBL 271 4 2 3 2.7 O[C@H](COc1cccc2ccccc12)[C@H]1CCCCN1 10.1021/jm00119a011
123686 1942 44 None -1 9 Human 8.8 pKd = 8.8 Binding
Displacement of [3H]-CGP12177 from human beta1 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta1 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 -1 9 Human 8.8 pKd = 8.8 Binding
Displacement of [3H]-CGP12177 from human beta1 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta1 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 -1 9 Human 8.8 pKd = 8.8 Binding
Displacement of [3H]-CGP12177 from human beta1 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta1 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
13157364 77598 0 None 30 2 Guinea pig 8.7 pKd = 8.7 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
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 8.7 pKd = 8.7 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
ChEMBL 341 7 3 4 2.6 O[C@@H](CNC1CC1)COc1ccc(-c2nc(C(F)(F)F)c[nH]2)cc1 10.1021/jm00361a004
13621676 9112 0 None 1122 2 Guinea pig 8.7 pKd = 8.7 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
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 8.7 pKd = 8.7 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
ChEMBL 475 11 3 6 3.4 COc1ccc(CCNCC(O)COc2ccc(-c3nc(Br)c[nH]3)cc2)cc1OC 10.1021/jm00156a028
165193 3126 60 None -7 43 Guinea pig 8.7 pKd = 8.7 Binding
Ability to block Beta-1 adrenergic receptor in guinea pig right atria preparationAbility to block Beta-1 adrenergic receptor in guinea pig right atria preparation
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00354a003
2303 3126 60 None -7 43 Guinea pig 8.7 pKd = 8.7 Binding
Ability to block Beta-1 adrenergic receptor in guinea pig right atria preparationAbility to block Beta-1 adrenergic receptor in guinea pig right atria preparation
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00354a003
4946 3126 60 None -7 43 Guinea pig 8.7 pKd = 8.7 Binding
Ability to block Beta-1 adrenergic receptor in guinea pig right atria preparationAbility to block Beta-1 adrenergic receptor in guinea pig right atria preparation
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00354a003
564 3126 60 None -7 43 Guinea pig 8.7 pKd = 8.7 Binding
Ability to block Beta-1 adrenergic receptor in guinea pig right atria preparationAbility to block Beta-1 adrenergic receptor in guinea pig right atria preparation
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00354a003
62882 3126 60 None -7 43 Guinea pig 8.7 pKd = 8.7 Binding
Ability to block Beta-1 adrenergic receptor in guinea pig right atria preparationAbility to block Beta-1 adrenergic receptor in guinea pig right atria preparation
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00354a003
63 3126 60 None -7 43 Guinea pig 8.7 pKd = 8.7 Binding
Ability to block Beta-1 adrenergic receptor in guinea pig right atria preparationAbility to block Beta-1 adrenergic receptor in guinea pig right atria preparation
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00354a003
66366 3126 60 None -7 43 Guinea pig 8.7 pKd = 8.7 Binding
Ability to block Beta-1 adrenergic receptor in guinea pig right atria preparationAbility to block Beta-1 adrenergic receptor in guinea pig right atria preparation
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00354a003
91536 3126 60 None -7 43 Guinea pig 8.7 pKd = 8.7 Binding
Ability to block Beta-1 adrenergic receptor in guinea pig right atria preparationAbility to block Beta-1 adrenergic receptor in guinea pig right atria preparation
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00354a003
CHEMBL27 3126 60 None -7 43 Guinea pig 8.7 pKd = 8.7 Binding
Ability to block Beta-1 adrenergic receptor in guinea pig right atria preparationAbility to block Beta-1 adrenergic receptor in guinea pig right atria preparation
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00354a003
CHEMBL452861 3126 60 None -7 43 Guinea pig 8.7 pKd = 8.7 Binding
Ability to block Beta-1 adrenergic receptor in guinea pig right atria preparationAbility to block Beta-1 adrenergic receptor in guinea pig right atria preparation
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00354a003
DB00571 3126 60 None -7 43 Guinea pig 8.7 pKd = 8.7 Binding
Ability to block Beta-1 adrenergic receptor in guinea pig right atria preparationAbility to block Beta-1 adrenergic receptor in guinea pig right atria preparation
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00354a003
165193 3126 60 None -7 43 Guinea pig 8.7 pKd = 8.7 Binding
Antagonist activity at beta1 adrenoceptor in guinea pig atrium assessed as inhibition of isoproterenol-induced response after 20 minsAntagonist activity at beta1 adrenoceptor in guinea pig atrium 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 -7 43 Guinea pig 8.7 pKd = 8.7 Binding
Antagonist activity at beta1 adrenoceptor in guinea pig atrium assessed as inhibition of isoproterenol-induced response after 20 minsAntagonist activity at beta1 adrenoceptor in guinea pig atrium 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 -7 43 Guinea pig 8.7 pKd = 8.7 Binding
Antagonist activity at beta1 adrenoceptor in guinea pig atrium assessed as inhibition of isoproterenol-induced response after 20 minsAntagonist activity at beta1 adrenoceptor in guinea pig atrium 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 -7 43 Guinea pig 8.7 pKd = 8.7 Binding
Antagonist activity at beta1 adrenoceptor in guinea pig atrium assessed as inhibition of isoproterenol-induced response after 20 minsAntagonist activity at beta1 adrenoceptor in guinea pig atrium 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 -7 43 Guinea pig 8.7 pKd = 8.7 Binding
Antagonist activity at beta1 adrenoceptor in guinea pig atrium assessed as inhibition of isoproterenol-induced response after 20 minsAntagonist activity at beta1 adrenoceptor in guinea pig atrium 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 -7 43 Guinea pig 8.7 pKd = 8.7 Binding
Antagonist activity at beta1 adrenoceptor in guinea pig atrium assessed as inhibition of isoproterenol-induced response after 20 minsAntagonist activity at beta1 adrenoceptor in guinea pig atrium 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 -7 43 Guinea pig 8.7 pKd = 8.7 Binding
Antagonist activity at beta1 adrenoceptor in guinea pig atrium assessed as inhibition of isoproterenol-induced response after 20 minsAntagonist activity at beta1 adrenoceptor in guinea pig atrium 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 -7 43 Guinea pig 8.7 pKd = 8.7 Binding
Antagonist activity at beta1 adrenoceptor in guinea pig atrium assessed as inhibition of isoproterenol-induced response after 20 minsAntagonist activity at beta1 adrenoceptor in guinea pig atrium 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 -7 43 Guinea pig 8.7 pKd = 8.7 Binding
Antagonist activity at beta1 adrenoceptor in guinea pig atrium assessed as inhibition of isoproterenol-induced response after 20 minsAntagonist activity at beta1 adrenoceptor in guinea pig atrium 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 -7 43 Guinea pig 8.7 pKd = 8.7 Binding
Antagonist activity at beta1 adrenoceptor in guinea pig atrium assessed as inhibition of isoproterenol-induced response after 20 minsAntagonist activity at beta1 adrenoceptor in guinea pig atrium 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 -7 43 Guinea pig 8.7 pKd = 8.7 Binding
Antagonist activity at beta1 adrenoceptor in guinea pig atrium assessed as inhibition of isoproterenol-induced response after 20 minsAntagonist activity at beta1 adrenoceptor in guinea pig atrium 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
105110 99655 6 None -1 2 Guinea pig 8.7 pKd = 8.7 Binding
In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.
ChEMBL 273 7 2 3 2.8 CC(C)CNCC(O)COc1cccc2ccccc12 10.1021/jm00354a002
CHEMBL287651 99655 6 None -1 2 Guinea pig 8.7 pKd = 8.7 Binding
In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.
ChEMBL 273 7 2 3 2.8 CC(C)CNCC(O)COc1cccc2ccccc12 10.1021/jm00354a002
13040919 105574 0 None -19 2 Guinea pig 8.0 pKd = 8 Binding
Ability to block Beta-1 adrenergic receptor in guinea pig right atria preparationAbility to block Beta-1 adrenergic receptor in guinea pig right atria 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 8.0 pKd = 8 Binding
Ability to block Beta-1 adrenergic receptor in guinea pig right atria preparationAbility to block Beta-1 adrenergic receptor in guinea pig right atria preparation
ChEMBL 339 9 2 7 1.1 CCOC(=O)C(C)(C)NCC(O)COc1ccccc1C(=O)OC 10.1021/jm00354a003
12462222 112131 0 None 39 2 Guinea pig 8.0 pKd = 8 Binding
Antagonist activity at beta1 adrenoceptor in guinea pig atrium assessed as inhibition of isoproterenol-induced response after 20 minsAntagonist activity at beta1 adrenoceptor in guinea pig atrium 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 8.0 pKd = 8 Binding
Antagonist activity at beta1 adrenoceptor in guinea pig atrium assessed as inhibition of isoproterenol-induced response after 20 minsAntagonist activity at beta1 adrenoceptor in guinea pig atrium 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 8.0 pKd = 8 Binding
Antagonist activity at beta1 adrenoceptor in guinea pig atrium assessed as inhibition of isoproterenol-induced response after 20 minsAntagonist activity at beta1 adrenoceptor in guinea pig atrium 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
235055 106926 8 None 3 2 Guinea pig 8.0 pKd = 8 Binding
In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.
ChEMBL 223 7 2 3 1.7 CC(C)CNCC(O)COc1ccccc1 10.1021/jm00354a002
CHEMBL31811 106926 8 None 3 2 Guinea pig 8.0 pKd = 8 Binding
In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.
ChEMBL 223 7 2 3 1.7 CC(C)CNCC(O)COc1ccccc1 10.1021/jm00354a002
13621706 8955 0 None 154 2 Guinea pig 8.0 pKd = 8 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
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 8.0 pKd = 8 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
ChEMBL 317 8 3 4 2.9 CC(C)NCC(O)COc1ccc(-c2nc(C(C)C)c[nH]2)cc1 10.1021/jm00156a028
5464103 91091 16 None 1 2 Guinea pig 8.0 pKd = 8.0 Binding
Beta-1 adrenergic receptor blocking activity in atria of guinea pig.Beta-1 adrenergic receptor blocking activity in atria 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 8.0 pKd = 8.0 Binding
Beta-1 adrenergic receptor blocking activity in atria of guinea pig.Beta-1 adrenergic receptor blocking activity in atria 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 8.0 pKd = 8.0 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor determined as pA2 in guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor determined as pA2 in guinea pig atria
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 8.0 pKd = 8.0 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor determined as pA2 in guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor determined as pA2 in guinea pig atria
ChEMBL 228 6 2 4 1.5 C/C(=N\OCC(O)CNC(C)(C)C)C1CC1 10.1021/jm00145a008
6917762 9219 7 None -1 2 Guinea pig 8.0 pKd = 8.0 Binding
The compound was tested for beta-adrenergic activity against Beta-1 adrenergic receptor from guinea pig left atriaThe compound was tested for beta-adrenergic activity against Beta-1 adrenergic receptor from guinea pig left atria
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 8.0 pKd = 8.0 Binding
The compound was tested for beta-adrenergic activity against Beta-1 adrenergic receptor from guinea pig left atriaThe compound was tested for beta-adrenergic activity against Beta-1 adrenergic receptor from guinea pig left atria
ChEMBL 228 6 2 4 1.5 C/C(=N\OCC(O)CNC(C)(C)C)C1CC1 10.1021/jm00115a008
6917762 9219 7 None -1 2 Guinea pig 8.0 pKd = 8.0 Binding
The compound was tested for beta-adrenergic activity against Beta-1 adrenergic receptor from guinea pig right atriaThe compound was tested for beta-adrenergic activity against Beta-1 adrenergic receptor from guinea pig right atria
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 8.0 pKd = 8.0 Binding
The compound was tested for beta-adrenergic activity against Beta-1 adrenergic receptor from guinea pig right atriaThe compound was tested for beta-adrenergic activity against Beta-1 adrenergic receptor from guinea pig right atria
ChEMBL 228 6 2 4 1.5 C/C(=N\OCC(O)CNC(C)(C)C)C1CC1 10.1021/jm00115a008
13157371 59711 0 None 3235 2 Guinea pig 8.0 pKd = 8.0 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
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 8.0 pKd = 8.0 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
ChEMBL 397 11 3 6 2.7 COc1ccc(CCNCC(O)COc2ccc(-c3ncc[nH]3)cc2)cc1OC 10.1021/jm00361a004
13621757 201739 0 None - 1 Guinea pig 8.0 pKd = 8.0 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
ChEMBL 453 13 3 7 2.8 COc1ccc(CCNC[C@H](O)COc2ccc(Cc3nc(C(C)=O)c[nH]3)cc2)cc1OC 10.1021/jm00156a028
CHEMBL65774 201739 0 None - 1 Guinea pig 8.0 pKd = 8.0 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
ChEMBL 453 13 3 7 2.8 COc1ccc(CCNC[C@H](O)COc2ccc(Cc3nc(C(C)=O)c[nH]3)cc2)cc1OC 10.1021/jm00156a028
13621651 9036 0 None - 1 Guinea pig 8.0 pKd = 8.0 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
ChEMBL 441 13 3 7 2.8 COCc1c[nH]c(-c2ccc(OCC(O)CNCCc3ccc(OC)c(OC)c3)cc2)n1 10.1021/jm00156a028
CHEMBL10998 9036 0 None - 1 Guinea pig 8.0 pKd = 8.0 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
ChEMBL 441 13 3 7 2.8 COCc1c[nH]c(-c2ccc(OCC(O)CNCCc3ccc(OC)c(OC)c3)cc2)n1 10.1021/jm00156a028
1054 1549 49 None 1 3 Guinea pig 7.0 pKd = 7 Binding
Ability to block Beta-1 adrenergic receptor in guinea pig right atria preparationAbility to block Beta-1 adrenergic receptor in guinea pig right atria preparation
ChEMBL 295 9 2 5 1.5 COC(=O)CCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm00354a003
59768 1549 49 None 1 3 Guinea pig 7.0 pKd = 7 Binding
Ability to block Beta-1 adrenergic receptor in guinea pig right atria preparationAbility to block Beta-1 adrenergic receptor in guinea pig right atria preparation
ChEMBL 295 9 2 5 1.5 COC(=O)CCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm00354a003
7178 1549 49 None 1 3 Guinea pig 7.0 pKd = 7 Binding
Ability to block Beta-1 adrenergic receptor in guinea pig right atria preparationAbility to block Beta-1 adrenergic receptor in guinea pig right atria preparation
ChEMBL 295 9 2 5 1.5 COC(=O)CCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm00354a003
CHEMBL768 1549 49 None 1 3 Guinea pig 7.0 pKd = 7 Binding
Ability to block Beta-1 adrenergic receptor in guinea pig right atria preparationAbility to block Beta-1 adrenergic receptor in guinea pig right atria preparation
ChEMBL 295 9 2 5 1.5 COC(=O)CCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm00354a003
DB00187 1549 49 None 1 3 Guinea pig 7.0 pKd = 7 Binding
Ability to block Beta-1 adrenergic receptor in guinea pig right atria preparationAbility to block Beta-1 adrenergic receptor in guinea pig right atria preparation
ChEMBL 295 9 2 5 1.5 COC(=O)CCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm00354a003
1054 1549 49 None 1 3 Guinea pig 7.0 pKd = 7 Binding
Activity at beta-1 adrenergic receptorActivity at beta-1 adrenergic receptor
ChEMBL 295 9 2 5 1.5 COC(=O)CCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm00103a004
59768 1549 49 None 1 3 Guinea pig 7.0 pKd = 7 Binding
Activity at beta-1 adrenergic receptorActivity at beta-1 adrenergic receptor
ChEMBL 295 9 2 5 1.5 COC(=O)CCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm00103a004
7178 1549 49 None 1 3 Guinea pig 7.0 pKd = 7 Binding
Activity at beta-1 adrenergic receptorActivity at beta-1 adrenergic receptor
ChEMBL 295 9 2 5 1.5 COC(=O)CCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm00103a004
CHEMBL768 1549 49 None 1 3 Guinea pig 7.0 pKd = 7 Binding
Activity at beta-1 adrenergic receptorActivity at beta-1 adrenergic receptor
ChEMBL 295 9 2 5 1.5 COC(=O)CCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm00103a004
DB00187 1549 49 None 1 3 Guinea pig 7.0 pKd = 7 Binding
Activity at beta-1 adrenergic receptorActivity at beta-1 adrenergic receptor
ChEMBL 295 9 2 5 1.5 COC(=O)CCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm00103a004
44307782 201857 3 None 2 2 Guinea pig 7.0 pKd = 7 Binding
Beta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atriumBeta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atrium
ChEMBL 223 6 1 3 1.8 CC(C)N(C)CC(O)COc1ccccc1 10.1021/jm00119a011
CHEMBL66662 201857 3 None 2 2 Guinea pig 7.0 pKd = 7 Binding
Beta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atriumBeta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atrium
ChEMBL 223 6 1 3 1.8 CC(C)N(C)CC(O)COc1ccccc1 10.1021/jm00119a011
44279341 99624 0 None - 1 Guinea pig 7.0 pKd = 7 Binding
In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.
ChEMBL 403 13 2 7 2.2 COc1ccc(CCOC(=O)CCNCC(O)COc2ccccc2)cc1OC 10.1021/jm00354a002
CHEMBL287452 99624 0 None - 1 Guinea pig 7.0 pKd = 7 Binding
In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.
ChEMBL 403 13 2 7 2.2 COc1ccc(CCOC(=O)CCNCC(O)COc2ccccc2)cc1OC 10.1021/jm00354a002
3486 3096 51 None -6 11 Guinea pig 6.0 pKd = 6 Binding
Activity at beta-1 adrenergic receptorActivity at beta-1 adrenergic receptor
ChEMBL 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C 10.1021/jm00103a004
4883 3096 51 None -6 11 Guinea pig 6.0 pKd = 6 Binding
Activity at beta-1 adrenergic receptorActivity at beta-1 adrenergic receptor
ChEMBL 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C 10.1021/jm00103a004
555 3096 51 None -6 11 Guinea pig 6.0 pKd = 6 Binding
Activity at beta-1 adrenergic receptorActivity at beta-1 adrenergic receptor
ChEMBL 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C 10.1021/jm00103a004
CHEMBL6995 3096 51 None -6 11 Guinea pig 6.0 pKd = 6 Binding
Activity at beta-1 adrenergic receptorActivity at beta-1 adrenergic receptor
ChEMBL 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C 10.1021/jm00103a004
DB01297 3096 51 None -6 11 Guinea pig 6.0 pKd = 6 Binding
Activity at beta-1 adrenergic receptorActivity at beta-1 adrenergic receptor
ChEMBL 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C 10.1021/jm00103a004
12484287 109215 0 None -2 2 Guinea pig 6.0 pKd = 6 Binding
Competitive antagonist activity at beta-1 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced atrial beat rateCompetitive antagonist activity at beta-1 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced atrial beat rate
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 6.0 pKd = 6 Binding
Competitive antagonist activity at beta-1 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced atrial beat rateCompetitive antagonist activity at beta-1 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced atrial beat rate
ChEMBL 249 6 3 4 1.3 CC(C)NCC(O)COc1ccc2[nH]cnc2c1 10.1021/jm00188a019
214809 109966 5 None 1 2 Rat 5.0 pKd = 5 Binding
Antagonist activity at beta1 adrenergic receptor in isolated rat atriaAntagonist activity at beta1 adrenergic receptor in isolated rat atria
ChEMBL 252 7 3 4 0.5 CC(C)NCC(O)COc1ccc(C(N)=O)cc1 10.1021/jm00207a025
CHEMBL3247302 109966 5 None 1 2 Rat 5.0 pKd = 5 Binding
Antagonist activity at beta1 adrenergic receptor in isolated rat atriaAntagonist activity at beta1 adrenergic receptor in isolated rat atria
ChEMBL 252 7 3 4 0.5 CC(C)NCC(O)COc1ccc(C(N)=O)cc1 10.1021/jm00207a025
44383643 165071 1 None -15 2 Guinea pig 4.0 pKd = 4 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor determined as pA2 in guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor determined as pA2 in guinea pig atria
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 4.0 pKd = 4 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor determined as pA2 in guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor determined as pA2 in guinea pig atria
ChEMBL 238 7 1 3 3.0 CC(C)(C)NCCCON=C(C1CC1)C1CC1 10.1021/jm00145a008
56597178 87817 0 None 10 2 Human 7.0 pKd = 7.0 Binding
Displacement of [3H]-CGP12177 from human beta1 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta1 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 7.0 pKd = 7.0 Binding
Displacement of [3H]-CGP12177 from human beta1 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta1 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
13974078 9319 0 None - 1 Guinea pig 6.0 pKd = 6.0 Binding
The compound was tested for beta-adrenergic activity against Beta-1 adrenergic receptor from guinea pig right atriaThe compound was tested for beta-adrenergic activity against Beta-1 adrenergic receptor from guinea pig right atria
ChEMBL 388 7 4 6 2.5 CC(C)(C)NCC(O)COCC1CN=C(Nc2c(Cl)cccc2Cl)N1 10.1021/jm00115a008
CHEMBL111697 9319 0 None - 1 Guinea pig 6.0 pKd = 6.0 Binding
The compound was tested for beta-adrenergic activity against Beta-1 adrenergic receptor from guinea pig right atriaThe compound was tested for beta-adrenergic activity against Beta-1 adrenergic receptor from guinea pig right atria
ChEMBL 388 7 4 6 2.5 CC(C)(C)NCC(O)COCC1CN=C(Nc2c(Cl)cccc2Cl)N1 10.1021/jm00115a008
3486 3096 51 None -6 11 Guinea pig 7.0 pKd = 7.0 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
ChEMBL 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C 10.1021/jm00361a004
4883 3096 51 None -6 11 Guinea pig 7.0 pKd = 7.0 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
ChEMBL 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C 10.1021/jm00361a004
555 3096 51 None -6 11 Guinea pig 7.0 pKd = 7.0 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
ChEMBL 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C 10.1021/jm00361a004
CHEMBL6995 3096 51 None -6 11 Guinea pig 7.0 pKd = 7.0 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
ChEMBL 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C 10.1021/jm00361a004
DB01297 3096 51 None -6 11 Guinea pig 7.0 pKd = 7.0 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
ChEMBL 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C 10.1021/jm00361a004
551640 201813 19 None 1 2 Guinea pig 6.0 pKd = 6.0 Binding
Beta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atriumBeta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atrium
ChEMBL 223 7 2 3 1.6 CC(C)NCC(O)COCc1ccccc1 10.1021/jm00119a011
CHEMBL66331 201813 19 None 1 2 Guinea pig 6.0 pKd = 6.0 Binding
Beta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atriumBeta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atrium
ChEMBL 223 7 2 3 1.6 CC(C)NCC(O)COCc1ccccc1 10.1021/jm00119a011
137 367 47 None -19 12 Human 8.0 pKd = 8.0 Binding
Displacement of [3H]-CGP 12177 from human beta-1 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-1 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 -19 12 Human 8.0 pKd = 8.0 Binding
Displacement of [3H]-CGP 12177 from human beta-1 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-1 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 -19 12 Human 8.0 pKd = 8.0 Binding
Displacement of [3H]-CGP 12177 from human beta-1 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-1 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 -19 12 Human 8.0 pKd = 8.0 Binding
Displacement of [3H]-CGP 12177 from human beta-1 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-1 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 -19 12 Human 8.0 pKd = 8.0 Binding
Displacement of [3H]-CGP 12177 from human beta-1 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-1 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 -19 12 Human 8.0 pKd = 8.0 Binding
Displacement of [3H]-CGP 12177 from human beta-1 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-1 adrenergic receptor expressed in CHOK1 cells
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1021/jm2008562
71662249 87810 0 None 109 2 Human 8.0 pKd = 8.0 Binding
Displacement of [3H]-CGP12177 from human beta1 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta1 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 8.0 pKd = 8.0 Binding
Displacement of [3H]-CGP12177 from human beta1 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta1 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
13621642 6113 0 None 2754 2 Guinea pig 7.9 pKd = 7.9 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
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 7.9 pKd = 7.9 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
ChEMBL 453 12 3 7 3.2 COc1ccc(CCNCC(O)COc2ccc(-c3nc(C(C)=O)c(C)[nH]3)cc2)cc1OC 10.1021/jm00156a028
13590033 9729 0 None 19 2 Guinea pig 6.0 pKd = 6.0 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
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 6.0 pKd = 6.0 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
ChEMBL 398 11 2 7 2.9 COc1ccc(CCNCC(O)COc2ccc(-c3ncco3)cc2)cc1OC 10.1021/jm00156a028
71662410 87814 0 None 12 2 Human 6.9 pKd = 6.9 Binding
Displacement of [3H]-CGP12177 from human beta1 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta1 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 6.9 pKd = 6.9 Binding
Displacement of [3H]-CGP12177 from human beta1 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta1 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
13621767 9224 0 None - 1 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 503 13 3 6 3.5 COc1ccc(CCNCC(O)COc2ccc(CCc3nc(Br)c[nH]3)cc2)cc1OC 10.1021/jm00156a028
CHEMBL11112 9224 0 None - 1 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 503 13 3 6 3.5 COc1ccc(CCNCC(O)COc2ccc(CCc3nc(Br)c[nH]3)cc2)cc1OC 10.1021/jm00156a028
71662409 87812 0 None 85 2 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]-CGP12177 from human beta1 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta1 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 7.9 pKd = 7.9 Binding
Displacement of [3H]-CGP12177 from human beta1 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta1 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
70695511 77492 1 None 1 2 Guinea pig 7.9 pKd = 7.9 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor determined as pA2 in guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor determined as pA2 in guinea pig atria
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-1 adrenergic receptor determined as pA2 in guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor determined as pA2 in guinea pig atria
ChEMBL 254 7 2 4 1.9 CC(C)(C)NC[C@H](O)CON=C(C1CC1)C1CC1 10.1021/jm00145a008
56598967 87819 0 None 275 2 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]-CGP12177 from human beta1 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta1 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 7.9 pKd = 7.9 Binding
Displacement of [3H]-CGP12177 from human beta1 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta1 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
13040886 99261 0 None -1 2 Guinea pig 7.9 pKd = 7.9 Binding
The compound was tested in vitro for its ability to block Beta-1 adrenergic receptor in guinea pig right atria preparationThe compound was tested in vitro for its ability to block Beta-1 adrenergic receptor in guinea pig right atria 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
The compound was tested in vitro for its ability to block Beta-1 adrenergic receptor in guinea pig right atria preparationThe compound was tested in vitro for its ability to block Beta-1 adrenergic receptor in guinea pig right atria preparation
ChEMBL 279 8 2 5 1.7 C=COC(=O)c1ccccc1OCC(O)CNC(C)C 10.1021/jm00354a003
66653395 87818 0 None 109 2 Human 7.9 pKd = 7.9 Binding
Displacement of [3H]-CGP12177 from human beta1 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta1 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 7.9 pKd = 7.9 Binding
Displacement of [3H]-CGP12177 from human beta1 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta1 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
13621715 5050 0 None 436 2 Guinea pig 7.9 pKd = 7.9 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
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 7.9 pKd = 7.9 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
ChEMBL 387 11 3 6 3.2 CCOCCNCC(O)COc1ccc(-c2nc(-c3cccs3)c[nH]2)cc1 10.1021/jm00156a028
13621721 161566 0 None 2630 2 Guinea pig 7.9 pKd = 7.9 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
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 7.9 pKd = 7.9 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
ChEMBL 420 10 3 6 3.8 OC(CNCCc1ccncc1)COc1ccc(-c2nc(-c3cccs3)c[nH]2)cc1 10.1021/jm00156a028
9816183 100068 5 None -5 2 Human 6.9 pKd = 6.9 Binding
Compound was tested for its binding affinity to human Beta-1 adrenergic receptor by using the radioligand [3H]CGP-12177Compound was tested for its binding affinity to human Beta-1 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 6.9 pKd = 6.9 Binding
Compound was tested for its binding affinity to human Beta-1 adrenergic receptor by using the radioligand [3H]CGP-12177Compound was tested for its binding affinity to human Beta-1 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
44459582 93112 0 None -13 2 Guinea pig 6.9 pKd = 6.9 Binding
Beta-1 adrenergic receptor blocking activity in atria of guinea pig.Beta-1 adrenergic receptor blocking activity in atria 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 6.9 pKd = 6.9 Binding
Beta-1 adrenergic receptor blocking activity in atria of guinea pig.Beta-1 adrenergic receptor blocking activity in atria 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
192962 109940 12 None 2 2 Guinea pig 6.9 pKd = 6.9 Binding
Antagonist activity at beta1 adrenoceptor in guinea pig atrium assessed as inhibition of isoproterenol-induced response after 20 minsAntagonist activity at beta1 adrenoceptor in guinea pig atrium 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 6.9 pKd = 6.9 Binding
Antagonist activity at beta1 adrenoceptor in guinea pig atrium assessed as inhibition of isoproterenol-induced response after 20 minsAntagonist activity at beta1 adrenoceptor in guinea pig atrium 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
2725073 98675 52 None 10 2 Guinea pig 6.9 pKd = 6.9 Binding
In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.
ChEMBL 167 4 2 3 0.4 NCC(O)COc1ccccc1 10.1021/jm00354a002
CHEMBL281109 98675 52 None 10 2 Guinea pig 6.9 pKd = 6.9 Binding
In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.
ChEMBL 167 4 2 3 0.4 NCC(O)COc1ccccc1 10.1021/jm00354a002
15569840 162730 0 None - 1 Guinea pig 6.9 pKd = 6.9 Binding
In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.
ChEMBL 329 8 2 5 2.3 COC(=O)c1ccc(CNCC(O)COc2ccccc2C)cc1 10.1021/jm00354a002
CHEMBL418770 162730 0 None - 1 Guinea pig 6.9 pKd = 6.9 Binding
In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.
ChEMBL 329 8 2 5 2.3 COC(=O)c1ccc(CNCC(O)COc2ccccc2C)cc1 10.1021/jm00354a002
13040888 106372 0 None -1 2 Guinea pig 6.9 pKd = 6.9 Binding
The compound was tested in vitro for its ability to block Beta-1 adrenergic receptor in guinea pig right atria preparationThe compound was tested in vitro for its ability to block Beta-1 adrenergic receptor in guinea pig right atria 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 6.9 pKd = 6.9 Binding
The compound was tested in vitro for its ability to block Beta-1 adrenergic receptor in guinea pig right atria preparationThe compound was tested in vitro for its ability to block Beta-1 adrenergic receptor in guinea pig right atria preparation
ChEMBL 279 8 2 5 1.7 C=COC(=O)c1cccc(OCC(O)CNC(C)C)c1 10.1021/jm00354a003
13040905 106057 0 None 10 2 Guinea pig 5.9 pKd = 5.9 Binding
Ability to block Beta-1 adrenergic receptor in guinea pig right atria preparationAbility to block Beta-1 adrenergic receptor in guinea pig right atria 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 5.9 pKd = 5.9 Binding
Ability to block Beta-1 adrenergic receptor in guinea pig right atria preparationAbility to block Beta-1 adrenergic receptor in guinea pig right atria preparation
ChEMBL 343 10 2 5 2.3 COC(=O)CCc1ccc(OCC(O)CNCc2ccccc2)cc1 10.1021/jm00354a003
13040911 106737 0 None - 1 Guinea pig 5.9 pKd = 5.9 Binding
Ability to block Beta-1 adrenergic receptor in guinea pig right atria preparationAbility to block Beta-1 adrenergic receptor in guinea pig right atria preparation
ChEMBL 353 12 2 7 1.1 CCOC(=O)CCNCC(O)COc1ccc(CCC(=O)OC)cc1 10.1021/jm00354a003
CHEMBL31677 106737 0 None - 1 Guinea pig 5.9 pKd = 5.9 Binding
Ability to block Beta-1 adrenergic receptor in guinea pig right atria preparationAbility to block Beta-1 adrenergic receptor in guinea pig right atria preparation
ChEMBL 353 12 2 7 1.1 CCOC(=O)CCNCC(O)COc1ccc(CCC(=O)OC)cc1 10.1021/jm00354a003
15578602 98899 2 None -1 2 Guinea pig 5.9 pKd = 5.9 Binding
In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.
ChEMBL 267 8 2 5 0.9 CCOC(=O)CNCC(O)COc1ccccc1C 10.1021/jm00354a002
CHEMBL282537 98899 2 None -1 2 Guinea pig 5.9 pKd = 5.9 Binding
In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.
ChEMBL 267 8 2 5 0.9 CCOC(=O)CNCC(O)COc1ccccc1C 10.1021/jm00354a002
15578567 106476 0 None - 1 Guinea pig 5.9 pKd = 5.9 Binding
In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.
ChEMBL 339 10 2 7 0.8 CCOC(=O)C(NCC(O)COc1ccccc1C)C(=O)OCC 10.1021/jm00354a002
CHEMBL31508 106476 0 None - 1 Guinea pig 5.9 pKd = 5.9 Binding
In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.
ChEMBL 339 10 2 7 0.8 CCOC(=O)C(NCC(O)COc1ccccc1C)C(=O)OCC 10.1021/jm00354a002
15578620 106597 0 None - 1 Guinea pig 5.9 pKd = 5.9 Binding
The compound was tested in vitro for its ability to block Beta-1 adrenergic receptor n guinea pig tracheaThe compound was tested in vitro for its ability to block Beta-1 adrenergic receptor n guinea pig trachea
ChEMBL 343 9 2 5 2.7 CCOC(=O)c1ccc(CNCC(O)COc2ccccc2C)cc1 10.1021/jm00354a002
CHEMBL31591 106597 0 None - 1 Guinea pig 5.9 pKd = 5.9 Binding
The compound was tested in vitro for its ability to block Beta-1 adrenergic receptor n guinea pig tracheaThe compound was tested in vitro for its ability to block Beta-1 adrenergic receptor n guinea pig trachea
ChEMBL 343 9 2 5 2.7 CCOC(=O)c1ccc(CNCC(O)COc2ccccc2C)cc1 10.1021/jm00354a002
44459632 95993 0 None -2 2 Guinea pig 4.9 pKd = 4.9 Binding
Beta-1 adrenergic receptor blocking activity in atria of guinea pig.Beta-1 adrenergic receptor blocking activity in atria 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 4.9 pKd = 4.9 Binding
Beta-1 adrenergic receptor blocking activity in atria of guinea pig.Beta-1 adrenergic receptor blocking activity in atria of guinea pig.
ChEMBL 230 7 3 4 1.1 CC(NOCC(O)CNC(C)(C)C)C1CC1 10.1021/jm00376a011
13621656 9187 0 None 1348 2 Guinea pig 7.9 pKd = 7.9 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
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 7.9 pKd = 7.9 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
ChEMBL 455 14 3 7 3.2 CCOCc1c[nH]c(-c2ccc(OCC(O)CNCCc3ccc(OC)c(OC)c3)cc2)n1 10.1021/jm00156a028
5487795 92831 2 None -79 2 Guinea pig 5.9 pKd = 5.9 Binding
Beta-1 adrenergic receptor blocking activity in atria of guinea pig.Beta-1 adrenergic receptor blocking activity in atria 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 5.9 pKd = 5.9 Binding
Beta-1 adrenergic receptor blocking activity in atria of guinea pig.Beta-1 adrenergic receptor blocking activity in atria 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
12606686 92413 3 None -31 2 Guinea pig 4.9 pKd = 4.9 Binding
Beta-1 adrenergic receptor blocking activity in atria of guinea pig.Beta-1 adrenergic receptor blocking activity in atria 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 4.9 pKd = 4.9 Binding
Beta-1 adrenergic receptor blocking activity in atria of guinea pig.Beta-1 adrenergic receptor blocking activity in atria 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 4.9 pKd = 4.9 Binding
Beta-1 adrenergic receptor blocking activity in atria of guinea pig.Beta-1 adrenergic receptor blocking activity in atria of guinea pig.
ChEMBL 189 5 2 3 1.2 CC(C)OCC(O)CNC(C)(C)C 10.1021/jm00376a011
5473526 157786 2 None -2 2 Human 4.9 pKd = 4.9 Binding
Displacement of [3H](-)CGP12177 from human beta1-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting methodDisplacement of [3H](-)CGP12177 from human beta1-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 4.9 pKd = 4.9 Binding
Displacement of [3H](-)CGP12177 from human beta1-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting methodDisplacement of [3H](-)CGP12177 from human beta1-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
165193 3126 60 None -7 43 Guinea pig 7.9 pKd = 7.9 Binding
Competitive antagonist activity at beta-1 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced atrial contractile forceCompetitive antagonist activity at beta-1 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced atrial contractile force
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00188a019
2303 3126 60 None -7 43 Guinea pig 7.9 pKd = 7.9 Binding
Competitive antagonist activity at beta-1 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced atrial contractile forceCompetitive antagonist activity at beta-1 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced atrial contractile force
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00188a019
4946 3126 60 None -7 43 Guinea pig 7.9 pKd = 7.9 Binding
Competitive antagonist activity at beta-1 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced atrial contractile forceCompetitive antagonist activity at beta-1 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced atrial contractile force
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00188a019
564 3126 60 None -7 43 Guinea pig 7.9 pKd = 7.9 Binding
Competitive antagonist activity at beta-1 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced atrial contractile forceCompetitive antagonist activity at beta-1 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced atrial contractile force
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00188a019
62882 3126 60 None -7 43 Guinea pig 7.9 pKd = 7.9 Binding
Competitive antagonist activity at beta-1 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced atrial contractile forceCompetitive antagonist activity at beta-1 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced atrial contractile force
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00188a019
63 3126 60 None -7 43 Guinea pig 7.9 pKd = 7.9 Binding
Competitive antagonist activity at beta-1 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced atrial contractile forceCompetitive antagonist activity at beta-1 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced atrial contractile force
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00188a019
66366 3126 60 None -7 43 Guinea pig 7.9 pKd = 7.9 Binding
Competitive antagonist activity at beta-1 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced atrial contractile forceCompetitive antagonist activity at beta-1 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced atrial contractile force
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00188a019
91536 3126 60 None -7 43 Guinea pig 7.9 pKd = 7.9 Binding
Competitive antagonist activity at beta-1 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced atrial contractile forceCompetitive antagonist activity at beta-1 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced atrial contractile force
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00188a019
CHEMBL27 3126 60 None -7 43 Guinea pig 7.9 pKd = 7.9 Binding
Competitive antagonist activity at beta-1 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced atrial contractile forceCompetitive antagonist activity at beta-1 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced atrial contractile force
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00188a019
CHEMBL452861 3126 60 None -7 43 Guinea pig 7.9 pKd = 7.9 Binding
Competitive antagonist activity at beta-1 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced atrial contractile forceCompetitive antagonist activity at beta-1 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced atrial contractile force
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00188a019
DB00571 3126 60 None -7 43 Guinea pig 7.9 pKd = 7.9 Binding
Competitive antagonist activity at beta-1 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced atrial contractile forceCompetitive antagonist activity at beta-1 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced atrial contractile force
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00188a019
1786 2474 79 None -2 11 Guinea pig 7.8 pKd = 7.8 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm00361a004
4171 2474 79 None -2 11 Guinea pig 7.8 pKd = 7.8 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm00361a004
553 2474 79 None -2 11 Guinea pig 7.8 pKd = 7.8 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm00361a004
CHEMBL13 2474 79 None -2 11 Guinea pig 7.8 pKd = 7.8 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm00361a004
DB00264 2474 79 None -2 11 Guinea pig 7.8 pKd = 7.8 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm00361a004
1786 2474 79 None -2 11 Guinea pig 7.8 pKd = 7.8 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm00156a028
4171 2474 79 None -2 11 Guinea pig 7.8 pKd = 7.8 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm00156a028
553 2474 79 None -2 11 Guinea pig 7.8 pKd = 7.8 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm00156a028
CHEMBL13 2474 79 None -2 11 Guinea pig 7.8 pKd = 7.8 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm00156a028
DB00264 2474 79 None -2 11 Guinea pig 7.8 pKd = 7.8 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm00156a028
13621620 8885 0 None 1174 2 Guinea pig 7.8 pKd = 7.8 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
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 7.8 pKd = 7.8 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
ChEMBL 425 11 3 6 3.3 COc1ccc(CCNCC(O)COc2ccc(-c3nc(C)c(C)[nH]3)cc2)cc1OC 10.1021/jm00156a028
15112598 9216 0 None 2 3 Guinea pig 5.8 pKd = 5.8 Binding
The compound was tested for beta-adrenergic activity against Beta-1 adrenergic receptor from guinea pig left atriaThe compound was tested for beta-adrenergic activity against Beta-1 adrenergic receptor from guinea pig left atria
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 2 3 Guinea pig 5.8 pKd = 5.8 Binding
The compound was tested for beta-adrenergic activity against Beta-1 adrenergic receptor from guinea pig left atriaThe compound was tested for beta-adrenergic activity against Beta-1 adrenergic receptor from guinea pig left atria
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
12462220 112104 2 None -1 2 Guinea pig 5.8 pKd = 5.8 Binding
Antagonist activity at beta1 adrenoceptor in guinea pig atrium assessed as inhibition of isoproterenol-induced response after 20 minsAntagonist activity at beta1 adrenoceptor in guinea pig atrium 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 5.8 pKd = 5.8 Binding
Antagonist activity at beta1 adrenoceptor in guinea pig atrium assessed as inhibition of isoproterenol-induced response after 20 minsAntagonist activity at beta1 adrenoceptor in guinea pig atrium 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 5.8 pKd = 5.8 Binding
Antagonist activity at beta1 adrenoceptor in guinea pig atrium assessed as inhibition of isoproterenol-induced response after 20 minsAntagonist activity at beta1 adrenoceptor in guinea pig atrium 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
15112598 9216 0 None 2 3 Guinea pig 5.8 pKd = 5.8 Binding
The compound was tested for beta-adrenergic activity against Beta-1 adrenergic receptor from guinea pig right atriaThe compound was tested for beta-adrenergic activity against Beta-1 adrenergic receptor from guinea pig right atria
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 2 3 Guinea pig 5.8 pKd = 5.8 Binding
The compound was tested for beta-adrenergic activity against Beta-1 adrenergic receptor from guinea pig right atriaThe compound was tested for beta-adrenergic activity against Beta-1 adrenergic receptor from guinea pig right atria
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
71662248 87805 0 None 75 2 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-CGP12177 from human beta1 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta1 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 7.8 pKd = 7.8 Binding
Displacement of [3H]-CGP12177 from human beta1 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta1 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
1786 2474 79 None -1 11 Human 7.8 pKd = 7.8 Binding
Antagonist activity against beta-1 adrenergic receptor (unknown origin)Antagonist activity against beta-1 adrenergic receptor (unknown origin)
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/acs.jmedchem.5b00201
4171 2474 79 None -1 11 Human 7.8 pKd = 7.8 Binding
Antagonist activity against beta-1 adrenergic receptor (unknown origin)Antagonist activity against beta-1 adrenergic receptor (unknown origin)
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/acs.jmedchem.5b00201
553 2474 79 None -1 11 Human 7.8 pKd = 7.8 Binding
Antagonist activity against beta-1 adrenergic receptor (unknown origin)Antagonist activity against beta-1 adrenergic receptor (unknown origin)
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/acs.jmedchem.5b00201
CHEMBL13 2474 79 None -1 11 Human 7.8 pKd = 7.8 Binding
Antagonist activity against beta-1 adrenergic receptor (unknown origin)Antagonist activity against beta-1 adrenergic receptor (unknown origin)
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/acs.jmedchem.5b00201
DB00264 2474 79 None -1 11 Human 7.8 pKd = 7.8 Binding
Antagonist activity against beta-1 adrenergic receptor (unknown origin)Antagonist activity against beta-1 adrenergic receptor (unknown origin)
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/acs.jmedchem.5b00201
56599097 87804 0 None 87 2 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-CGP12177 from human beta1 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta1 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 7.8 pKd = 7.8 Binding
Displacement of [3H]-CGP12177 from human beta1 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta1 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
15578610 111649 0 None 2 2 Guinea pig 7.8 pKd = 7.8 Binding
In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.
ChEMBL 309 11 2 5 2.1 CCOC(=O)CCCCNCC(O)COc1ccccc1C 10.1021/jm00354a002
CHEMBL32902 111649 0 None 2 2 Guinea pig 7.8 pKd = 7.8 Binding
In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.
ChEMBL 309 11 2 5 2.1 CCOC(=O)CCCCNCC(O)COc1ccccc1C 10.1021/jm00354a002
13621720 97837 0 None 407 2 Guinea pig 7.8 pKd = 7.8 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
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 7.8 pKd = 7.8 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
ChEMBL 357 9 3 5 3.5 CCCNCC(O)COc1ccc(-c2nc(-c3cccs3)c[nH]2)cc1 10.1021/jm00156a028
2892936 95461 5 None -15 2 Guinea pig 5.8 pKd = 5.8 Binding
Beta-1 adrenergic receptor blocking activity in atria of guinea pig.Beta-1 adrenergic receptor blocking activity in atria 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 5.8 pKd = 5.8 Binding
Beta-1 adrenergic receptor blocking activity in atria of guinea pig.Beta-1 adrenergic receptor blocking activity in atria of guinea pig.
ChEMBL 271 5 2 3 3.0 CC1CC(OCC(O)CNC(C)(C)C)CC(C)(C)C1 10.1021/jm00376a011
12238214 25252 8 None 19 2 Guinea pig 6.8 pKd = 6.8 Binding
Ability to block Beta-1 adrenergic receptor in guinea pig right atria preparationAbility to block Beta-1 adrenergic receptor in guinea pig right atria 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 6.8 pKd = 6.8 Binding
Ability to block Beta-1 adrenergic receptor in guinea pig right atria preparationAbility to block Beta-1 adrenergic receptor in guinea pig right atria preparation
ChEMBL 267 7 2 5 1.2 COC(=O)c1ccc(OCC(O)CNC(C)C)cc1 10.1021/jm00354a003
13040900 106861 3 None - 1 Guinea pig 6.8 pKd = 6.8 Binding
Ability to block Beta-1 adrenergic receptor in guinea pig right atria preparationAbility to block Beta-1 adrenergic receptor in guinea pig right atria preparation
ChEMBL 322 10 3 4 1.9 CC(C)NCC(O)COc1ccc(CCC(=O)NC(C)C)cc1 10.1021/jm00354a003
CHEMBL31768 106861 3 None - 1 Guinea pig 6.8 pKd = 6.8 Binding
Ability to block Beta-1 adrenergic receptor in guinea pig right atria preparationAbility to block Beta-1 adrenergic receptor in guinea pig right atria preparation
ChEMBL 322 10 3 4 1.9 CC(C)NCC(O)COc1ccc(CCC(=O)NC(C)C)cc1 10.1021/jm00354a003
2249 509 106 None 2 12 Guinea pig 6.8 pKd = 6.8 Binding
Activity at beta-1 adrenergic receptorActivity at beta-1 adrenergic receptor
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1021/jm00103a004
255 509 106 None 2 12 Guinea pig 6.8 pKd = 6.8 Binding
Activity at beta-1 adrenergic receptorActivity at beta-1 adrenergic receptor
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1021/jm00103a004
548 509 106 None 2 12 Guinea pig 6.8 pKd = 6.8 Binding
Activity at beta-1 adrenergic receptorActivity at beta-1 adrenergic receptor
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1021/jm00103a004
CHEMBL24 509 106 None 2 12 Guinea pig 6.8 pKd = 6.8 Binding
Activity at beta-1 adrenergic receptorActivity at beta-1 adrenergic receptor
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1021/jm00103a004
DB00335 509 106 None 2 12 Guinea pig 6.8 pKd = 6.8 Binding
Activity at beta-1 adrenergic receptorActivity at beta-1 adrenergic receptor
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1021/jm00103a004
62773144 109938 3 None 1 2 Guinea pig 6.8 pKd = 6.8 Binding
Antagonist activity at beta1 adrenoceptor in guinea pig atrium assessed as inhibition of isoproterenol-induced response after 20 minsAntagonist activity at beta1 adrenoceptor in guinea pig atrium 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 6.8 pKd = 6.8 Binding
Antagonist activity at beta1 adrenoceptor in guinea pig atrium assessed as inhibition of isoproterenol-induced response after 20 minsAntagonist activity at beta1 adrenoceptor in guinea pig atrium 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
14201557 201865 0 None -1 2 Guinea pig 6.8 pKd = 6.8 Binding
Beta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atriumBeta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atrium
ChEMBL 235 4 1 3 1.9 CN1CCCC[C@@H]1[C@H](O)COc1ccccc1 10.1021/jm00119a011
CHEMBL66724 201865 0 None -1 2 Guinea pig 6.8 pKd = 6.8 Binding
Beta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atriumBeta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atrium
ChEMBL 235 4 1 3 1.9 CN1CCCC[C@@H]1[C@H](O)COc1ccccc1 10.1021/jm00119a011
15578598 99754 2 None 7 2 Guinea pig 5.8 pKd = 5.8 Binding
In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.
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 5.8 pKd = 5.8 Binding
In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.
ChEMBL 297 10 2 6 1.0 CCOC(=O)CCNCC(O)COc1ccc(OC)cc1 10.1021/jm00354a002
3025067 98910 58 None -812 15 Human 4.8 pKd = 4.8 Binding
Binding affinity to His-tagged human beta1 adrenergic receptor expressed in HEK293 cell membranes by surface plasmon resonance analysisBinding affinity to His-tagged human beta1 adrenergic receptor expressed in HEK293 cell membranes by surface plasmon resonance analysis
ChEMBL 220 1 1 4 0.9 c1cc2c(c(N3CCNCC3)c1)OCCO2 10.1021/jm400140q
65853 98910 58 None -812 15 Human 4.8 pKd = 4.8 Binding
Binding affinity to His-tagged human beta1 adrenergic receptor expressed in HEK293 cell membranes by surface plasmon resonance analysisBinding affinity to His-tagged human beta1 adrenergic receptor expressed in HEK293 cell membranes by surface plasmon resonance analysis
ChEMBL 220 1 1 4 0.9 c1cc2c(c(N3CCNCC3)c1)OCCO2 10.1021/jm400140q
CHEMBL282614 98910 58 None -812 15 Human 4.8 pKd = 4.8 Binding
Binding affinity to His-tagged human beta1 adrenergic receptor expressed in HEK293 cell membranes by surface plasmon resonance analysisBinding affinity to His-tagged human beta1 adrenergic receptor expressed in HEK293 cell membranes by surface plasmon resonance analysis
ChEMBL 220 1 1 4 0.9 c1cc2c(c(N3CCNCC3)c1)OCCO2 10.1021/jm400140q
13621774 98015 0 None 208 2 Guinea pig 7.8 pKd = 7.8 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
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 7.8 pKd = 7.8 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
ChEMBL 427 13 3 7 2.6 COc1ccc(CCNCC(O)COc2ccc(OCc3ncc[nH]3)cc2)cc1OC 10.1021/jm00156a028
56599231 87813 0 None 81 2 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-CGP12177 from human beta1 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta1 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 7.8 pKd = 7.8 Binding
Displacement of [3H]-CGP12177 from human beta1 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta1 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 7.8 pKd = 7.8 Binding
Displacement of [3H]-CGP12177 from human beta1 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta1 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 7.8 pKd = 7.8 Binding
Displacement of [3H]-CGP12177 from human beta1 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta1 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
13621653 75579 0 None 2238 2 Guinea pig 7.8 pKd = 7.8 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
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 7.8 pKd = 7.8 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
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
3025067 98910 58 None -812 15 Human 4.8 pKd = 4.8 Binding
Binding affinity to His-tagged human beta1 adrenergic receptor expressed in HEK293 cell membranes by surface plasmon resonance analysisBinding affinity to His-tagged human beta1 adrenergic receptor expressed in HEK293 cell membranes by surface plasmon resonance analysis
ChEMBL 220 1 1 4 0.9 c1cc2c(c(N3CCNCC3)c1)OCCO2 10.1021/jm400140q
65853 98910 58 None -812 15 Human 4.8 pKd = 4.8 Binding
Binding affinity to His-tagged human beta1 adrenergic receptor expressed in HEK293 cell membranes by surface plasmon resonance analysisBinding affinity to His-tagged human beta1 adrenergic receptor expressed in HEK293 cell membranes by surface plasmon resonance analysis
ChEMBL 220 1 1 4 0.9 c1cc2c(c(N3CCNCC3)c1)OCCO2 10.1021/jm400140q
CHEMBL282614 98910 58 None -812 15 Human 4.8 pKd = 4.8 Binding
Binding affinity to His-tagged human beta1 adrenergic receptor expressed in HEK293 cell membranes by surface plasmon resonance analysisBinding affinity to His-tagged human beta1 adrenergic receptor expressed in HEK293 cell membranes by surface plasmon resonance analysis
ChEMBL 220 1 1 4 0.9 c1cc2c(c(N3CCNCC3)c1)OCCO2 10.1021/jm400140q
54669764 65146 0 None -37 3 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-CGP 12177 from human beta-1 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-1 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 7.8 pKd = 7.8 Binding
Displacement of [3H]-CGP 12177 from human beta-1 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-1 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
56599099 87822 0 None 91 2 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-CGP12177 from human beta1 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta1 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 7.8 pKd = 7.8 Binding
Displacement of [3H]-CGP12177 from human beta1 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta1 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
71662247 87824 0 None 51 2 Human 7.8 pKd = 7.8 Binding
Displacement of [3H]-CGP12177 from human beta1 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta1 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 7.8 pKd = 7.8 Binding
Displacement of [3H]-CGP12177 from human beta1 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta1 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
13621700 201340 0 None 3630 2 Guinea pig 7.8 pKd = 7.8 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
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 7.8 pKd = 7.8 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
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
12398051 110032 0 None -43 2 Guinea pig 4.8 pKd = 4.8 Binding
Inhibition of beta1-adrenergic receptor in guinea pig auricle assessed as reversal of isoproterenol-induced effectInhibition of beta1-adrenergic receptor in guinea pig auricle assessed as reversal of isoproterenol-induced effect
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 4.8 pKd = 4.8 Binding
Inhibition of beta1-adrenergic receptor in guinea pig auricle assessed as reversal of isoproterenol-induced effectInhibition of beta1-adrenergic receptor in guinea pig auricle assessed as reversal of isoproterenol-induced effect
ChEMBL 245 2 2 2 2.8 CC1(C)NC1C(O)c1ccc(Cl)c(Cl)c1 10.1021/jm00199a012
13621671 168851 1 None 234 2 Guinea pig 7.7 pKd = 7.7 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
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 7.7 pKd = 7.7 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
ChEMBL 496 13 3 8 2.5 COc1ccc(CCNCC(O)COc2ccc(-c3nc(CN4CCOCC4)c[nH]3)cc2)cc1OC 10.1021/jm00156a028
44459891 95704 0 None -7 2 Guinea pig 6.7 pKd = 6.7 Binding
Beta-1 adrenergic receptor blocking activity in atria of guinea pig.Beta-1 adrenergic receptor blocking activity in atria 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 6.7 pKd = 6.7 Binding
Beta-1 adrenergic receptor blocking activity in atria of guinea pig.Beta-1 adrenergic receptor blocking activity in atria of guinea pig.
ChEMBL 217 5 2 3 1.8 CC(C)(C)COCC(O)CNC(C)(C)C 10.1021/jm00376a011
5311179 1935 18 None -85 3 Human 6.7 pKd = 6.7 Binding
Displacement of [3H](-)CGP12177 from human beta1-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting methodDisplacement of [3H](-)CGP12177 from human beta1-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 6.7 pKd = 6.7 Binding
Displacement of [3H](-)CGP12177 from human beta1-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting methodDisplacement of [3H](-)CGP12177 from human beta1-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 6.7 pKd = 6.7 Binding
Displacement of [3H](-)CGP12177 from human beta1-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting methodDisplacement of [3H](-)CGP12177 from human beta1-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 6.7 pKd = 6.7 Binding
Displacement of [3H](-)CGP12177 from human beta1-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting methodDisplacement of [3H](-)CGP12177 from human beta1-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 6.7 pKd = 6.7 Binding
Displacement of [3H](-)CGP12177 from human beta1-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting methodDisplacement of [3H](-)CGP12177 from human beta1-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
90672832 109968 0 None 2 2 Rat 4.7 pKd = 4.7 Binding
Antagonist activity at beta1 adrenergic receptor in isolated rat atriaAntagonist activity at beta1 adrenergic receptor in isolated rat atria
ChEMBL 294 6 3 5 0.5 CC(C)NCC(O)COc1ccc2c(c1)OCCNC2=O 10.1021/jm00207a025
CHEMBL3247304 109968 0 None 2 2 Rat 4.7 pKd = 4.7 Binding
Antagonist activity at beta1 adrenergic receptor in isolated rat atriaAntagonist activity at beta1 adrenergic receptor in isolated rat atria
ChEMBL 294 6 3 5 0.5 CC(C)NCC(O)COc1ccc2c(c1)OCCNC2=O 10.1021/jm00207a025
54756928 65142 0 None -57 3 Human 6.7 pKd = 6.7 Binding
Displacement of [3H]-CGP 12177 from human beta-1 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-1 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 -57 3 Human 6.7 pKd = 6.7 Binding
Displacement of [3H]-CGP 12177 from human beta-1 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-1 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
13157407 59954 0 None 245 2 Guinea pig 6.7 pKd = 6.7 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
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 6.7 pKd = 6.7 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
ChEMBL 419 10 3 5 4.4 OC(CNCCc1ccccc1)COc1ccc(-c2nc(-c3cccs3)c[nH]2)cc1 10.1021/jm00361a004
13621761 9263 0 None 10 2 Guinea pig 7.7 pKd = 7.7 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
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 7.7 pKd = 7.7 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
ChEMBL 385 8 3 5 3.9 CC(C)(C)NCC(O)COc1ccc(Cc2nc(-c3cccs3)c[nH]2)cc1 10.1021/jm00156a028
2769826 202113 22 None -1 2 Guinea pig 7.7 pKd = 7.7 Binding
Beta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atriumBeta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atrium
ChEMBL 259 6 2 3 2.6 CC(C)NCC(O)COc1ccc2ccccc2c1 10.1021/jm00119a011
CHEMBL68419 202113 22 None -1 2 Guinea pig 7.7 pKd = 7.7 Binding
Beta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atriumBeta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atrium
ChEMBL 259 6 2 3 2.6 CC(C)NCC(O)COc1ccc2ccccc2c1 10.1021/jm00119a011
56599102 87807 0 None 60 2 Human 7.7 pKd = 7.7 Binding
Displacement of [3H]-CGP12177 from human beta1 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta1 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 7.7 pKd = 7.7 Binding
Displacement of [3H]-CGP12177 from human beta1 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta1 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
56599233 87816 0 None 87 2 Human 7.7 pKd = 7.7 Binding
Displacement of [3H]-CGP12177 from human beta1 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta1 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 7.7 pKd = 7.7 Binding
Displacement of [3H]-CGP12177 from human beta1 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta1 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
13621712 75581 0 None 1288 2 Guinea pig 7.7 pKd = 7.7 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
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 7.7 pKd = 7.7 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
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
54757027 65145 0 None -53 3 Human 6.7 pKd = 6.7 Binding
Displacement of [3H]-CGP 12177 from human beta-1 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-1 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 -53 3 Human 6.7 pKd = 6.7 Binding
Displacement of [3H]-CGP 12177 from human beta-1 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-1 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
157736 98496 8 None 31 2 Guinea pig 6.7 pKd = 6.7 Binding
Ability to block Beta-1 adrenergic receptor in guinea pig right atria preparationAbility to block Beta-1 adrenergic receptor in guinea pig right atria 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 6.7 pKd = 6.7 Binding
Ability to block Beta-1 adrenergic receptor in guinea pig right atria preparationAbility to block Beta-1 adrenergic receptor in guinea pig right atria preparation
ChEMBL 309 10 2 5 1.9 CCOC(=O)CCc1ccc(OCC(O)CNC(C)C)cc1 10.1021/jm00354a003
90672835 109970 0 None -10 2 Rat 6.7 pKd = 6.7 Binding
Antagonist activity at beta1 adrenergic receptor in isolated rat atriaAntagonist activity at beta1 adrenergic receptor in isolated rat atria
ChEMBL 279 8 2 4 2.5 C/C=C\c1ccc(OCC(O)CNC(C)C)c(OC)c1 10.1021/jm00207a025
CHEMBL3247309 109970 0 None -10 2 Rat 6.7 pKd = 6.7 Binding
Antagonist activity at beta1 adrenergic receptor in isolated rat atriaAntagonist activity at beta1 adrenergic receptor in isolated rat atria
ChEMBL 279 8 2 4 2.5 C/C=C\c1ccc(OCC(O)CNC(C)C)c(OC)c1 10.1021/jm00207a025
15578594 106567 2 None 1 2 Guinea pig 6.7 pKd = 6.7 Binding
In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.
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 6.7 pKd = 6.7 Binding
In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.
ChEMBL 281 9 2 5 1.3 CCOC(=O)CCNCC(O)COc1cccc(C)c1 10.1021/jm00354a002
15569840 162730 0 None - 1 Guinea pig 6.7 pKd = 6.7 Binding
The compound was tested in vitro for its ability to block Beta-1 adrenergic receptor in guinea pig tracheaThe compound was tested in vitro for its ability to block Beta-1 adrenergic receptor in guinea pig trachea
ChEMBL 329 8 2 5 2.3 COC(=O)c1ccc(CNCC(O)COc2ccccc2C)cc1 10.1021/jm00354a002
CHEMBL418770 162730 0 None - 1 Guinea pig 6.7 pKd = 6.7 Binding
The compound was tested in vitro for its ability to block Beta-1 adrenergic receptor in guinea pig tracheaThe compound was tested in vitro for its ability to block Beta-1 adrenergic receptor in guinea pig trachea
ChEMBL 329 8 2 5 2.3 COC(=O)c1ccc(CNCC(O)COc2ccccc2C)cc1 10.1021/jm00354a002
15578618 102327 0 None - 1 Guinea pig 5.7 pKd = 5.7 Binding
In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.
ChEMBL 321 9 2 5 1.5 O=C(CCNCC(O)COc1ccccc1)OCC(F)(F)F 10.1021/jm00354a002
CHEMBL30538 102327 0 None - 1 Guinea pig 5.7 pKd = 5.7 Binding
In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.
ChEMBL 321 9 2 5 1.5 O=C(CCNCC(O)COc1ccccc1)OCC(F)(F)F 10.1021/jm00354a002
15578555 105854 3 None 1 2 Guinea pig 5.7 pKd = 5.7 Binding
In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.
ChEMBL 253 8 2 5 0.6 CCOC(=O)CNCC(O)COc1ccccc1 10.1021/jm00354a002
CHEMBL31392 105854 3 None 1 2 Guinea pig 5.7 pKd = 5.7 Binding
In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.
ChEMBL 253 8 2 5 0.6 CCOC(=O)CNCC(O)COc1ccccc1 10.1021/jm00354a002
15578616 104103 0 None - 1 Guinea pig 5.7 pKd = 5.7 Binding
The compound was tested in vitro for its ability to block Beta-1 adrenergic receptor in guinea pig right atriaThe compound was tested in vitro for its ability to block Beta-1 adrenergic receptor in guinea pig right atria
ChEMBL 333 9 2 5 2.2 O=C(CCNCC(O)COc1ccccc1)Oc1ccc(F)cc1 10.1021/jm00354a002
CHEMBL31047 104103 0 None - 1 Guinea pig 5.7 pKd = 5.7 Binding
The compound was tested in vitro for its ability to block Beta-1 adrenergic receptor in guinea pig right atriaThe compound was tested in vitro for its ability to block Beta-1 adrenergic receptor in guinea pig right atria
ChEMBL 333 9 2 5 2.2 O=C(CCNCC(O)COc1ccccc1)Oc1ccc(F)cc1 10.1021/jm00354a002
133620 203274 17 None - 1 Guinea pig 4.7 pKd = 4.7 Binding
Ability to block Beta-1 adrenergic receptor in guinea pig right atria preparationAbility to block Beta-1 adrenergic receptor in guinea pig right atria preparation
ChEMBL 281 9 3 4 1.4 CC(C)NCC(O)COc1ccc(CCC(=O)O)cc1 10.1021/jm00354a003
CHEMBL767 203274 17 None - 1 Guinea pig 4.7 pKd = 4.7 Binding
Ability to block Beta-1 adrenergic receptor in guinea pig right atria preparationAbility to block Beta-1 adrenergic receptor in guinea pig right atria preparation
ChEMBL 281 9 3 4 1.4 CC(C)NCC(O)COc1ccc(CCC(=O)O)cc1 10.1021/jm00354a003
13621680 161561 0 None 446 2 Guinea pig 8.7 pKd = 8.7 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
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 8.7 pKd = 8.7 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
ChEMBL 431 11 3 6 3.3 COc1ccc(CCNCC(O)COc2ccc(-c3nc(Cl)c[nH]3)cc2)cc1OC 10.1021/jm00156a028
165193 3126 60 None -7 43 Guinea pig 8.6 pKd = 8.6 Binding
Beta-1 adrenergic receptor blocking activity in atria of guinea pig.Beta-1 adrenergic receptor blocking activity in atria of guinea pig.
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00376a011
2303 3126 60 None -7 43 Guinea pig 8.6 pKd = 8.6 Binding
Beta-1 adrenergic receptor blocking activity in atria of guinea pig.Beta-1 adrenergic receptor blocking activity in atria of guinea pig.
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00376a011
4946 3126 60 None -7 43 Guinea pig 8.6 pKd = 8.6 Binding
Beta-1 adrenergic receptor blocking activity in atria of guinea pig.Beta-1 adrenergic receptor blocking activity in atria of guinea pig.
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00376a011
564 3126 60 None -7 43 Guinea pig 8.6 pKd = 8.6 Binding
Beta-1 adrenergic receptor blocking activity in atria of guinea pig.Beta-1 adrenergic receptor blocking activity in atria of guinea pig.
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00376a011
62882 3126 60 None -7 43 Guinea pig 8.6 pKd = 8.6 Binding
Beta-1 adrenergic receptor blocking activity in atria of guinea pig.Beta-1 adrenergic receptor blocking activity in atria of guinea pig.
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00376a011
63 3126 60 None -7 43 Guinea pig 8.6 pKd = 8.6 Binding
Beta-1 adrenergic receptor blocking activity in atria of guinea pig.Beta-1 adrenergic receptor blocking activity in atria of guinea pig.
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00376a011
66366 3126 60 None -7 43 Guinea pig 8.6 pKd = 8.6 Binding
Beta-1 adrenergic receptor blocking activity in atria of guinea pig.Beta-1 adrenergic receptor blocking activity in atria of guinea pig.
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00376a011
91536 3126 60 None -7 43 Guinea pig 8.6 pKd = 8.6 Binding
Beta-1 adrenergic receptor blocking activity in atria of guinea pig.Beta-1 adrenergic receptor blocking activity in atria of guinea pig.
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00376a011
CHEMBL27 3126 60 None -7 43 Guinea pig 8.6 pKd = 8.6 Binding
Beta-1 adrenergic receptor blocking activity in atria of guinea pig.Beta-1 adrenergic receptor blocking activity in atria of guinea pig.
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00376a011
CHEMBL452861 3126 60 None -7 43 Guinea pig 8.6 pKd = 8.6 Binding
Beta-1 adrenergic receptor blocking activity in atria of guinea pig.Beta-1 adrenergic receptor blocking activity in atria of guinea pig.
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00376a011
DB00571 3126 60 None -7 43 Guinea pig 8.6 pKd = 8.6 Binding
Beta-1 adrenergic receptor blocking activity in atria of guinea pig.Beta-1 adrenergic receptor blocking activity in atria of guinea pig.
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00376a011
165193 3126 60 None -7 43 Guinea pig 8.6 pKd = 8.6 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor determined as pA2 in guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor determined as pA2 in guinea pig atria
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00145a008
2303 3126 60 None -7 43 Guinea pig 8.6 pKd = 8.6 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor determined as pA2 in guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor determined as pA2 in guinea pig atria
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00145a008
4946 3126 60 None -7 43 Guinea pig 8.6 pKd = 8.6 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor determined as pA2 in guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor determined as pA2 in guinea pig atria
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00145a008
564 3126 60 None -7 43 Guinea pig 8.6 pKd = 8.6 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor determined as pA2 in guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor determined as pA2 in guinea pig atria
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00145a008
62882 3126 60 None -7 43 Guinea pig 8.6 pKd = 8.6 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor determined as pA2 in guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor determined as pA2 in guinea pig atria
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00145a008
63 3126 60 None -7 43 Guinea pig 8.6 pKd = 8.6 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor determined as pA2 in guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor determined as pA2 in guinea pig atria
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00145a008
66366 3126 60 None -7 43 Guinea pig 8.6 pKd = 8.6 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor determined as pA2 in guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor determined as pA2 in guinea pig atria
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00145a008
91536 3126 60 None -7 43 Guinea pig 8.6 pKd = 8.6 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor determined as pA2 in guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor determined as pA2 in guinea pig atria
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00145a008
CHEMBL27 3126 60 None -7 43 Guinea pig 8.6 pKd = 8.6 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor determined as pA2 in guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor determined as pA2 in guinea pig atria
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00145a008
CHEMBL452861 3126 60 None -7 43 Guinea pig 8.6 pKd = 8.6 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor determined as pA2 in guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor determined as pA2 in guinea pig atria
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00145a008
DB00571 3126 60 None -7 43 Guinea pig 8.6 pKd = 8.6 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor determined as pA2 in guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor determined as pA2 in guinea pig atria
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00145a008
9904228 98818 0 None -1 2 Guinea pig 8.6 pKd = 8.6 Binding
Ability to block Beta-1 adrenergic receptor in guinea pig right atria preparationAbility to block Beta-1 adrenergic receptor in guinea pig right atria 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 8.6 pKd = 8.6 Binding
Ability to block Beta-1 adrenergic receptor in guinea pig right atria preparationAbility to block Beta-1 adrenergic receptor in guinea pig right atria preparation
ChEMBL 295 9 2 5 1.5 COC(=O)CCc1ccccc1OCC(O)CNC(C)C 10.1021/jm00354a003
165193 3126 60 None -7 43 Guinea pig 8.6 pKd = 8.6 Binding
Beta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atriumBeta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atrium
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00119a011
2303 3126 60 None -7 43 Guinea pig 8.6 pKd = 8.6 Binding
Beta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atriumBeta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atrium
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00119a011
4946 3126 60 None -7 43 Guinea pig 8.6 pKd = 8.6 Binding
Beta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atriumBeta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atrium
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00119a011
564 3126 60 None -7 43 Guinea pig 8.6 pKd = 8.6 Binding
Beta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atriumBeta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atrium
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00119a011
62882 3126 60 None -7 43 Guinea pig 8.6 pKd = 8.6 Binding
Beta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atriumBeta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atrium
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00119a011
63 3126 60 None -7 43 Guinea pig 8.6 pKd = 8.6 Binding
Beta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atriumBeta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atrium
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00119a011
66366 3126 60 None -7 43 Guinea pig 8.6 pKd = 8.6 Binding
Beta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atriumBeta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atrium
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00119a011
91536 3126 60 None -7 43 Guinea pig 8.6 pKd = 8.6 Binding
Beta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atriumBeta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atrium
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00119a011
CHEMBL27 3126 60 None -7 43 Guinea pig 8.6 pKd = 8.6 Binding
Beta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atriumBeta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atrium
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00119a011
CHEMBL452861 3126 60 None -7 43 Guinea pig 8.6 pKd = 8.6 Binding
Beta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atriumBeta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atrium
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00119a011
DB00571 3126 60 None -7 43 Guinea pig 8.6 pKd = 8.6 Binding
Beta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atriumBeta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atrium
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00119a011
44279657 103884 1 None 2 2 Guinea pig 8.6 pKd = 8.6 Binding
In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.
ChEMBL 237 7 2 3 2.0 Cc1ccccc1OCC(O)CNCC(C)C 10.1021/jm00354a002
CHEMBL31021 103884 1 None 2 2 Guinea pig 8.6 pKd = 8.6 Binding
In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.
ChEMBL 237 7 2 3 2.0 Cc1ccccc1OCC(O)CNCC(C)C 10.1021/jm00354a002
2176 3065 66 None -4 27 Human 8.6 pKd = 8.6 Binding
Displacement of [3H]-CGP 12177 from human beta-1 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-1 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 -4 27 Human 8.6 pKd = 8.6 Binding
Displacement of [3H]-CGP 12177 from human beta-1 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-1 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 -4 27 Human 8.6 pKd = 8.6 Binding
Displacement of [3H]-CGP 12177 from human beta-1 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-1 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 -4 27 Human 8.6 pKd = 8.6 Binding
Displacement of [3H]-CGP 12177 from human beta-1 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-1 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 -4 27 Human 8.6 pKd = 8.6 Binding
Displacement of [3H]-CGP 12177 from human beta-1 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-1 adrenergic receptor expressed in CHOK1 cells
ChEMBL 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C 10.1021/jm2008562
13621767 9224 0 None - 1 Guinea pig 8.5 pKd = 8.5 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
ChEMBL 503 13 3 6 3.5 COc1ccc(CCNCC(O)COc2ccc(CCc3nc(Br)c[nH]3)cc2)cc1OC 10.1021/jm00156a028
CHEMBL11112 9224 0 None - 1 Guinea pig 8.5 pKd = 8.5 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
ChEMBL 503 13 3 6 3.5 COc1ccc(CCNCC(O)COc2ccc(CCc3nc(Br)c[nH]3)cc2)cc1OC 10.1021/jm00156a028
13621749 9390 0 None - 1 Guinea pig 8.5 pKd = 8.5 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
ChEMBL 493 13 3 7 4.3 COc1ccc(CCNCC(O)COc2ccc(Cc3nc(-c4cccs4)c[nH]3)cc2)cc1OC 10.1021/jm00156a028
CHEMBL11205 9390 0 None - 1 Guinea pig 8.5 pKd = 8.5 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
ChEMBL 493 13 3 7 4.3 COc1ccc(CCNCC(O)COc2ccc(Cc3nc(-c4cccs4)c[nH]3)cc2)cc1OC 10.1021/jm00156a028
2369 615 75 None -5 8 Rat 8.5 pKd = 8.5 Binding
Antagonist activity at rat beta1 adrenoceptorAntagonist activity at rat beta1 adrenoceptor
ChEMBL 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C 10.1021/acs.jmedchem.6b00472
356 615 75 None -5 8 Rat 8.5 pKd = 8.5 Binding
Antagonist activity at rat beta1 adrenoceptorAntagonist activity at rat beta1 adrenoceptor
ChEMBL 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C 10.1021/acs.jmedchem.6b00472
549 615 75 None -5 8 Rat 8.5 pKd = 8.5 Binding
Antagonist activity at rat beta1 adrenoceptorAntagonist activity at rat beta1 adrenoceptor
ChEMBL 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C 10.1021/acs.jmedchem.6b00472
CHEMBL423 615 75 None -5 8 Rat 8.5 pKd = 8.5 Binding
Antagonist activity at rat beta1 adrenoceptorAntagonist activity at rat beta1 adrenoceptor
ChEMBL 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C 10.1021/acs.jmedchem.6b00472
DB00195 615 75 None -5 8 Rat 8.5 pKd = 8.5 Binding
Antagonist activity at rat beta1 adrenoceptorAntagonist activity at rat beta1 adrenoceptor
ChEMBL 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C 10.1021/acs.jmedchem.6b00472
13157374 77597 0 None 1412 2 Guinea pig 7.7 pKd = 7.7 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
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 7.7 pKd = 7.7 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
ChEMBL 397 11 3 6 2.7 COc1ccc(CCNC[C@H](O)COc2ccc(-c3ncc[nH]3)cc2)cc1OC 10.1021/jm00361a004
13621752 96891 0 None 144 2 Guinea pig 7.7 pKd = 7.7 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
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 7.7 pKd = 7.7 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
ChEMBL 425 12 3 6 2.9 COc1ccc(CCNCC(O)COc2ccc(Cc3nc(C)c[nH]3)cc2)cc1OC 10.1021/jm00156a028
3486 3096 51 None -6 11 Guinea pig 6.7 pKd = 6.7 Binding
Antagonist activity at beta1 adrenoceptor in guinea pig atrium assessed as inhibition of isoproterenol-induced response after 20 minsAntagonist activity at beta1 adrenoceptor in guinea pig atrium 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 -6 11 Guinea pig 6.7 pKd = 6.7 Binding
Antagonist activity at beta1 adrenoceptor in guinea pig atrium assessed as inhibition of isoproterenol-induced response after 20 minsAntagonist activity at beta1 adrenoceptor in guinea pig atrium 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 -6 11 Guinea pig 6.7 pKd = 6.7 Binding
Antagonist activity at beta1 adrenoceptor in guinea pig atrium assessed as inhibition of isoproterenol-induced response after 20 minsAntagonist activity at beta1 adrenoceptor in guinea pig atrium 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 -6 11 Guinea pig 6.7 pKd = 6.7 Binding
Antagonist activity at beta1 adrenoceptor in guinea pig atrium assessed as inhibition of isoproterenol-induced response after 20 minsAntagonist activity at beta1 adrenoceptor in guinea pig atrium 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 -6 11 Guinea pig 6.7 pKd = 6.7 Binding
Antagonist activity at beta1 adrenoceptor in guinea pig atrium assessed as inhibition of isoproterenol-induced response after 20 minsAntagonist activity at beta1 adrenoceptor in guinea pig atrium 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
54757232 65170 0 None -30 3 Human 7.7 pKd = 7.7 Binding
Displacement of [3H]-CGP 12177 from human beta-1 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-1 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 7.7 pKd = 7.7 Binding
Displacement of [3H]-CGP 12177 from human beta-1 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-1 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
13621710 9194 0 None 478 2 Guinea pig 7.7 pKd = 7.7 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
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 7.7 pKd = 7.7 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
ChEMBL 453 11 3 6 4.0 COc1ccc(CCNCC(O)COc2ccc(-c3nc(C(C)(C)C)c[nH]3)cc2)cc1OC 10.1021/jm00156a028
1786 2474 79 None -21 11 Rat 7.6 pKd = 7.6 Binding
Antagonist activity at rat beta1 adrenoceptorAntagonist activity at rat beta1 adrenoceptor
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/acs.jmedchem.6b00472
4171 2474 79 None -21 11 Rat 7.6 pKd = 7.6 Binding
Antagonist activity at rat beta1 adrenoceptorAntagonist activity at rat beta1 adrenoceptor
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/acs.jmedchem.6b00472
553 2474 79 None -21 11 Rat 7.6 pKd = 7.6 Binding
Antagonist activity at rat beta1 adrenoceptorAntagonist activity at rat beta1 adrenoceptor
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/acs.jmedchem.6b00472
CHEMBL13 2474 79 None -21 11 Rat 7.6 pKd = 7.6 Binding
Antagonist activity at rat beta1 adrenoceptorAntagonist activity at rat beta1 adrenoceptor
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/acs.jmedchem.6b00472
DB00264 2474 79 None -21 11 Rat 7.6 pKd = 7.6 Binding
Antagonist activity at rat beta1 adrenoceptorAntagonist activity at rat beta1 adrenoceptor
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1021/acs.jmedchem.6b00472
2030 3602 7 None -316 10 Human 6.7 pKd = 6.7 Binding
Binding affinity to human adrenergic beta-1 receptorBinding affinity to human adrenergic beta-1 receptor
ChEMBL 464 4 0 6 3.0 COc1cccc2c1C[C@H]1C[C@H](CN([C@@H]1C2)C)C(=O)N1CCN(CC1)c1ccc(cc1)[N+](=O)[O-] 10.1016/j.bmcl.2007.04.086
5311377 3602 7 None -316 10 Human 6.7 pKd = 6.7 Binding
Binding affinity to human adrenergic beta-1 receptorBinding affinity to human adrenergic beta-1 receptor
ChEMBL 464 4 0 6 3.0 COc1cccc2c1C[C@H]1C[C@H](CN([C@@H]1C2)C)C(=O)N1CCN(CC1)c1ccc(cc1)[N+](=O)[O-] 10.1016/j.bmcl.2007.04.086
CHEMBL251541 3602 7 None -316 10 Human 6.7 pKd = 6.7 Binding
Binding affinity to human adrenergic beta-1 receptorBinding affinity to human adrenergic beta-1 receptor
ChEMBL 464 4 0 6 3.0 COc1cccc2c1C[C@H]1C[C@H](CN([C@@H]1C2)C)C(=O)N1CCN(CC1)c1ccc(cc1)[N+](=O)[O-] 10.1016/j.bmcl.2007.04.086
6917762 9219 7 None -1 2 Guinea pig 7.6 pKd = 7.6 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor determined as pA2 in guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor determined as pA2 in guinea pig atria
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 7.6 pKd = 7.6 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor determined as pA2 in guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor determined as pA2 in guinea pig atria
ChEMBL 228 6 2 4 1.5 C/C(=N\OCC(O)CNC(C)(C)C)C1CC1 10.1021/jm00145a008
13621722 96859 5 None 229 2 Guinea pig 7.6 pKd = 7.6 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
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 7.6 pKd = 7.6 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
ChEMBL 275 7 3 4 1.8 CC(C)NCC(O)COc1ccc(-c2ncc[nH]2)cc1 10.1021/jm00156a028
2249 509 106 None 2 12 Guinea pig 7.6 pKd = 7.6 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1021/jm00361a004
255 509 106 None 2 12 Guinea pig 7.6 pKd = 7.6 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1021/jm00361a004
548 509 106 None 2 12 Guinea pig 7.6 pKd = 7.6 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1021/jm00361a004
CHEMBL24 509 106 None 2 12 Guinea pig 7.6 pKd = 7.6 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1021/jm00361a004
DB00335 509 106 None 2 12 Guinea pig 7.6 pKd = 7.6 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1021/jm00361a004
13157412 59918 0 None - 1 Guinea pig 7.6 pKd = 7.6 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
ChEMBL 411 11 3 6 3.0 COc1ccc(CCNCC(O)COc2ccc(-c3nc(C)c[nH]3)cc2)cc1OC 10.1021/jm00361a004
CHEMBL174106 59918 0 None - 1 Guinea pig 7.6 pKd = 7.6 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
ChEMBL 411 11 3 6 3.0 COc1ccc(CCNCC(O)COc2ccc(-c3nc(C)c[nH]3)cc2)cc1OC 10.1021/jm00361a004
2249 509 106 None 2 12 Guinea pig 7.6 pKd = 7.6 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1021/jm00156a028
255 509 106 None 2 12 Guinea pig 7.6 pKd = 7.6 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1021/jm00156a028
548 509 106 None 2 12 Guinea pig 7.6 pKd = 7.6 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1021/jm00156a028
CHEMBL24 509 106 None 2 12 Guinea pig 7.6 pKd = 7.6 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1021/jm00156a028
DB00335 509 106 None 2 12 Guinea pig 7.6 pKd = 7.6 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1021/jm00156a028
3682 188837 7 None -229 8 Human 6.6 pKd = 6.6 Binding
Displacement of [3H]-CGP12177 from human beta1 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta1 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 -229 8 Human 6.6 pKd = 6.6 Binding
Displacement of [3H]-CGP12177 from human beta1 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta1 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 -229 8 Human 6.6 pKd = 6.6 Binding
Displacement of [3H]-CGP12177 from human beta1 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta1 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
13621638 9756 0 None 2137 2 Guinea pig 7.6 pKd = 7.6 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
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 7.6 pKd = 7.6 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
ChEMBL 455 13 3 7 3.1 COCc1[nH]c(-c2ccc(OCC(O)CNCCc3ccc(OC)c(OC)c3)cc2)nc1C 10.1021/jm00156a028
13621722 96859 5 None 229 2 Guinea pig 7.6 pKd = 7.6 Binding
Activity at beta-1 adrenergic receptorActivity at beta-1 adrenergic receptor
ChEMBL 275 7 3 4 1.8 CC(C)NCC(O)COc1ccc(-c2ncc[nH]2)cc1 10.1021/jm00103a004
CHEMBL269219 96859 5 None 229 2 Guinea pig 7.6 pKd = 7.6 Binding
Activity at beta-1 adrenergic receptorActivity at beta-1 adrenergic receptor
ChEMBL 275 7 3 4 1.8 CC(C)NCC(O)COc1ccc(-c2ncc[nH]2)cc1 10.1021/jm00103a004
2834366 112150 5 None 6 2 Rat 7.6 pKd = 7.6 Binding
Antagonist activity at beta1 adrenergic receptor in isolated rat atriaAntagonist activity at beta1 adrenergic receptor in isolated rat atria
ChEMBL 251 8 2 3 2.4 CCCc1ccc(OCC(O)CNC(C)C)cc1 10.1021/jm00207a025
CHEMBL3247307 112150 5 None 6 2 Rat 7.6 pKd = 7.6 Binding
Antagonist activity at beta1 adrenergic receptor in isolated rat atriaAntagonist activity at beta1 adrenergic receptor in isolated rat atria
ChEMBL 251 8 2 3 2.4 CCCc1ccc(OCC(O)CNC(C)C)cc1 10.1021/jm00207a025
CHEMBL3303501 112150 5 None 6 2 Rat 7.6 pKd = 7.6 Binding
Antagonist activity at beta1 adrenergic receptor in isolated rat atriaAntagonist activity at beta1 adrenergic receptor in isolated rat atria
ChEMBL 251 8 2 3 2.4 CCCc1ccc(OCC(O)CNC(C)C)cc1 10.1021/jm00207a025
3486 3096 51 None -6 11 Guinea pig 6.6 pKd = 6.6 Binding
Ability to block Beta-1 adrenergic receptor in guinea pig right atria preparationAbility to block Beta-1 adrenergic receptor in guinea pig right atria preparation
ChEMBL 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C 10.1021/jm00354a003
4883 3096 51 None -6 11 Guinea pig 6.6 pKd = 6.6 Binding
Ability to block Beta-1 adrenergic receptor in guinea pig right atria preparationAbility to block Beta-1 adrenergic receptor in guinea pig right atria preparation
ChEMBL 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C 10.1021/jm00354a003
555 3096 51 None -6 11 Guinea pig 6.6 pKd = 6.6 Binding
Ability to block Beta-1 adrenergic receptor in guinea pig right atria preparationAbility to block Beta-1 adrenergic receptor in guinea pig right atria preparation
ChEMBL 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C 10.1021/jm00354a003
CHEMBL6995 3096 51 None -6 11 Guinea pig 6.6 pKd = 6.6 Binding
Ability to block Beta-1 adrenergic receptor in guinea pig right atria preparationAbility to block Beta-1 adrenergic receptor in guinea pig right atria preparation
ChEMBL 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C 10.1021/jm00354a003
DB01297 3096 51 None -6 11 Guinea pig 6.6 pKd = 6.6 Binding
Ability to block Beta-1 adrenergic receptor in guinea pig right atria preparationAbility to block Beta-1 adrenergic receptor in guinea pig right atria preparation
ChEMBL 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C 10.1021/jm00354a003
13040894 99554 0 None 12 2 Guinea pig 6.6 pKd = 6.6 Binding
Ability to block Beta-1 adrenergic receptor in guinea pig right atria preparationAbility to block Beta-1 adrenergic receptor in guinea pig right atria 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 6.6 pKd = 6.6 Binding
Ability to block Beta-1 adrenergic receptor in guinea pig right atria preparationAbility to block Beta-1 adrenergic receptor in guinea pig right atria preparation
ChEMBL 309 10 2 5 1.9 COC(=O)CCCc1ccc(OCC(O)CNC(C)C)cc1 10.1021/jm00354a003
13040915 102446 0 None 50 2 Guinea pig 6.6 pKd = 6.6 Binding
Ability to block Beta-1 adrenergic receptor in guinea pig right atria preparationAbility to block Beta-1 adrenergic receptor in guinea pig right atria 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-1 adrenergic receptor in guinea pig right atria preparationAbility to block Beta-1 adrenergic receptor in guinea pig right atria preparation
ChEMBL 325 10 2 7 0.8 CCOC(=O)CCNCC(O)COc1ccccc1C(=O)OC 10.1021/jm00354a003
12797747 201834 2 None -2 2 Guinea pig 6.6 pKd = 6.6 Binding
Beta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atriumBeta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atrium
ChEMBL 251 9 2 3 2.0 CC(C)NCC(O)COCCCc1ccccc1 10.1021/jm00119a011
CHEMBL66449 201834 2 None -2 2 Guinea pig 6.6 pKd = 6.6 Binding
Beta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atriumBeta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atrium
ChEMBL 251 9 2 3 2.0 CC(C)NCC(O)COCCCc1ccccc1 10.1021/jm00119a011
15578575 99248 2 None 3 2 Guinea pig 6.6 pKd = 6.6 Binding
In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.
ChEMBL 281 10 2 5 1.4 CCOC(=O)CCCNCC(O)COc1ccccc1 10.1021/jm00354a002
CHEMBL284808 99248 2 None 3 2 Guinea pig 6.6 pKd = 6.6 Binding
In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.
ChEMBL 281 10 2 5 1.4 CCOC(=O)CCCNCC(O)COc1ccccc1 10.1021/jm00354a002
15578620 106597 0 None - 1 Guinea pig 6.6 pKd = 6.6 Binding
In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.
ChEMBL 343 9 2 5 2.7 CCOC(=O)c1ccc(CNCC(O)COc2ccccc2C)cc1 10.1021/jm00354a002
CHEMBL31591 106597 0 None - 1 Guinea pig 6.6 pKd = 6.6 Binding
In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.
ChEMBL 343 9 2 5 2.7 CCOC(=O)c1ccc(CNCC(O)COc2ccccc2C)cc1 10.1021/jm00354a002
44279341 99624 0 None - 1 Guinea pig 6.6 pKd = 6.6 Binding
The compound was tested in vitro for its ability to block beta-2-adrenergic receptor in guinea pig tracheaThe compound was tested in vitro for its ability to block beta-2-adrenergic receptor in guinea pig trachea
ChEMBL 403 13 2 7 2.2 COc1ccc(CCOC(=O)CCNCC(O)COc2ccccc2)cc1OC 10.1021/jm00354a002
CHEMBL287452 99624 0 None - 1 Guinea pig 6.6 pKd = 6.6 Binding
The compound was tested in vitro for its ability to block beta-2-adrenergic receptor in guinea pig tracheaThe compound was tested in vitro for its ability to block beta-2-adrenergic receptor in guinea pig trachea
ChEMBL 403 13 2 7 2.2 COc1ccc(CCOC(=O)CCNCC(O)COc2ccccc2)cc1OC 10.1021/jm00354a002
12462226 112129 1 None -1 2 Guinea pig 5.6 pKd = 5.6 Binding
Antagonist activity at beta1 adrenoceptor in guinea pig atrium assessed as inhibition of isoproterenol-induced response after 20 minsAntagonist activity at beta1 adrenoceptor in guinea pig atrium 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 beta1 adrenoceptor in guinea pig atrium assessed as inhibition of isoproterenol-induced response after 20 minsAntagonist activity at beta1 adrenoceptor in guinea pig atrium 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 beta1 adrenoceptor in guinea pig atrium assessed as inhibition of isoproterenol-induced response after 20 minsAntagonist activity at beta1 adrenoceptor in guinea pig atrium 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
14348818 109273 0 None -5 3 Guinea pig 4.6 pKd = 4.6 Binding
The compound was tested for beta-adrenergic activity against Beta-1 adrenergic receptor from guinea pig left atriaThe compound was tested for beta-adrenergic activity against Beta-1 adrenergic receptor from guinea pig left atria
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 -5 3 Guinea pig 4.6 pKd = 4.6 Binding
The compound was tested for beta-adrenergic activity against Beta-1 adrenergic receptor from guinea pig left atriaThe compound was tested for beta-adrenergic activity against Beta-1 adrenergic receptor from guinea pig left atria
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
165193 3126 60 None -7 43 Guinea pig 6.6 pKd = 6.6 Binding
Inhibition of beta1-adrenergic receptor in guinea pig auricle assessed as reversal of isoproterenol-induced effectInhibition of beta1-adrenergic receptor in guinea pig auricle assessed as reversal of isoproterenol-induced effect
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00199a012
2303 3126 60 None -7 43 Guinea pig 6.6 pKd = 6.6 Binding
Inhibition of beta1-adrenergic receptor in guinea pig auricle assessed as reversal of isoproterenol-induced effectInhibition of beta1-adrenergic receptor in guinea pig auricle assessed as reversal of isoproterenol-induced effect
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00199a012
4946 3126 60 None -7 43 Guinea pig 6.6 pKd = 6.6 Binding
Inhibition of beta1-adrenergic receptor in guinea pig auricle assessed as reversal of isoproterenol-induced effectInhibition of beta1-adrenergic receptor in guinea pig auricle assessed as reversal of isoproterenol-induced effect
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00199a012
564 3126 60 None -7 43 Guinea pig 6.6 pKd = 6.6 Binding
Inhibition of beta1-adrenergic receptor in guinea pig auricle assessed as reversal of isoproterenol-induced effectInhibition of beta1-adrenergic receptor in guinea pig auricle assessed as reversal of isoproterenol-induced effect
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00199a012
62882 3126 60 None -7 43 Guinea pig 6.6 pKd = 6.6 Binding
Inhibition of beta1-adrenergic receptor in guinea pig auricle assessed as reversal of isoproterenol-induced effectInhibition of beta1-adrenergic receptor in guinea pig auricle assessed as reversal of isoproterenol-induced effect
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00199a012
63 3126 60 None -7 43 Guinea pig 6.6 pKd = 6.6 Binding
Inhibition of beta1-adrenergic receptor in guinea pig auricle assessed as reversal of isoproterenol-induced effectInhibition of beta1-adrenergic receptor in guinea pig auricle assessed as reversal of isoproterenol-induced effect
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00199a012
66366 3126 60 None -7 43 Guinea pig 6.6 pKd = 6.6 Binding
Inhibition of beta1-adrenergic receptor in guinea pig auricle assessed as reversal of isoproterenol-induced effectInhibition of beta1-adrenergic receptor in guinea pig auricle assessed as reversal of isoproterenol-induced effect
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00199a012
91536 3126 60 None -7 43 Guinea pig 6.6 pKd = 6.6 Binding
Inhibition of beta1-adrenergic receptor in guinea pig auricle assessed as reversal of isoproterenol-induced effectInhibition of beta1-adrenergic receptor in guinea pig auricle assessed as reversal of isoproterenol-induced effect
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00199a012
CHEMBL27 3126 60 None -7 43 Guinea pig 6.6 pKd = 6.6 Binding
Inhibition of beta1-adrenergic receptor in guinea pig auricle assessed as reversal of isoproterenol-induced effectInhibition of beta1-adrenergic receptor in guinea pig auricle assessed as reversal of isoproterenol-induced effect
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00199a012
CHEMBL452861 3126 60 None -7 43 Guinea pig 6.6 pKd = 6.6 Binding
Inhibition of beta1-adrenergic receptor in guinea pig auricle assessed as reversal of isoproterenol-induced effectInhibition of beta1-adrenergic receptor in guinea pig auricle assessed as reversal of isoproterenol-induced effect
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00199a012
DB00571 3126 60 None -7 43 Guinea pig 6.6 pKd = 6.6 Binding
Inhibition of beta1-adrenergic receptor in guinea pig auricle assessed as reversal of isoproterenol-induced effectInhibition of beta1-adrenergic receptor in guinea pig auricle assessed as reversal of isoproterenol-induced effect
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00199a012
29057685 158275 12 None -1 2 Human 4.6 pKd = 4.6 Binding
Displacement of [3H](-)CGP12177 from human beta1-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting methodDisplacement of [3H](-)CGP12177 from human beta1-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 4.6 pKd = 4.6 Binding
Displacement of [3H](-)CGP12177 from human beta1-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting methodDisplacement of [3H](-)CGP12177 from human beta1-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 4.6 pKd = 4.6 Binding
Displacement of [3H](-)CGP12177 from human beta1-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting methodDisplacement of [3H](-)CGP12177 from human beta1-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
44383465 120230 1 None -2 2 Guinea pig 7.6 pKd = 7.6 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor determined as pA2 in guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor determined as pA2 in guinea pig atria
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 7.6 pKd = 7.6 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor determined as pA2 in guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor determined as pA2 in guinea pig atria
ChEMBL 228 6 2 4 1.5 C/C(=N\OC[C@@H](O)CNC(C)(C)C)C1CC1 10.1021/jm00145a008
21595423 201812 0 None -10 2 Guinea pig 6.6 pKd = 6.6 Binding
Beta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atriumBeta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atrium
ChEMBL 263 7 2 3 2.1 O[C@H](COCCCc1ccccc1)[C@@H]1CCCCN1 10.1021/jm00119a011
CHEMBL66324 201812 0 None -10 2 Guinea pig 6.6 pKd = 6.6 Binding
Beta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atriumBeta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atrium
ChEMBL 263 7 2 3 2.1 O[C@H](COCCCc1ccccc1)[C@@H]1CCCCN1 10.1021/jm00119a011
2297435 55302 6 None -10 2 Human 4.6 pKd = 4.6 Binding
Displacement of [3H](-)CGP12177 from human beta1-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting methodDisplacement of [3H](-)CGP12177 from human beta1-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 4.6 pKd = 4.6 Binding
Displacement of [3H](-)CGP12177 from human beta1-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting methodDisplacement of [3H](-)CGP12177 from human beta1-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
13157386 62832 1 None 138 2 Guinea pig 7.5 pKd = 7.5 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
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 7.5 pKd = 7.5 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
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 7.5 pKd = 7.5 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
ChEMBL 479 12 3 7 4.4 COc1ccc(CCNC[C@H](O)COc2ccc(-c3nc(-c4cccs4)c[nH]3)cc2)cc1OC 10.1021/jm00156a028
13621764 161459 0 None 1288 2 Guinea pig 8.5 pKd = 8.5 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
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 8.5 pKd = 8.5 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
ChEMBL 507 14 3 7 4.5 COc1ccc(CCNCC(O)COc2ccc(CCc3nc(-c4cccs4)c[nH]3)cc2)cc1OC 10.1021/jm00156a028
13040881 98704 0 None -1 2 Guinea pig 8.5 pKd = 8.5 Binding
Ability to block Beta-1 adrenergic receptor in guinea pig right atria preparationAbility to block Beta-1 adrenergic receptor in guinea pig right atria 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 8.5 pKd = 8.5 Binding
Ability to block Beta-1 adrenergic receptor in guinea pig right atria preparationAbility to block Beta-1 adrenergic receptor in guinea pig right atria preparation
ChEMBL 295 7 2 5 2.0 CCOC(=O)c1ccccc1OCC(O)CNC(C)(C)C 10.1021/jm00354a003
56598832 87826 0 None 588 3 Human 8.5 pKd = 8.5 Binding
Displacement of [3H]-CGP12177 from human beta1 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta1 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 8.5 pKd = 8.5 Binding
Displacement of [3H]-CGP12177 from human beta1 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta1 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
15578565 106505 0 None 2 2 Guinea pig 8.5 pKd = 8.5 Binding
In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.
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 8.5 pKd = 8.5 Binding
In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.
ChEMBL 309 9 2 5 2.1 CCOC(=O)CC(C)(C)NCC(O)COc1ccccc1C 10.1021/jm00354a002
13621770 9244 0 None 7 2 Guinea pig 8.5 pKd = 8.5 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor was measured by the inhibition of the positive chronotropic effect of isoproterenolin in isolated guinea pig atria.In vitro inhibitory activity against beta-1 adrenergic receptor was measured by the inhibition of the positive chronotropic effect of isoproterenolin in isolated guinea pig atria.
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 8.5 pKd = 8.5 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor was measured by the inhibition of the positive chronotropic effect of isoproterenolin in isolated guinea pig atria.In vitro inhibitory activity against beta-1 adrenergic receptor was measured by the inhibition of the positive chronotropic effect of isoproterenolin in isolated guinea pig atria.
ChEMBL 367 8 3 4 2.5 CC(C)NCC(O)COc1ccc(Cc2nc(Br)c[nH]2)cc1 10.1021/jm00156a028
13621602 9721 0 None 1096 2 Guinea pig 8.5 pKd = 8.5 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
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 8.5 pKd = 8.5 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
ChEMBL 493 12 3 7 4.7 COc1ccc(CCNCC(O)COc2ccc(-c3nc(-c4cccs4)c[nH]3)cc2C)cc1OC 10.1021/jm00156a028
2840793 201926 27 None 1 2 Guinea pig 8.4 pKd = 8.4 Binding
Beta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atriumBeta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atrium
ChEMBL 223 6 2 3 1.7 Cc1ccc(OCC(O)CNC(C)C)cc1 10.1021/jm00119a011
CHEMBL67151 201926 27 None 1 2 Guinea pig 8.4 pKd = 8.4 Binding
Beta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atriumBeta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atrium
ChEMBL 223 6 2 3 1.7 Cc1ccc(OCC(O)CNC(C)C)cc1 10.1021/jm00119a011
12484297 109216 0 None -15 2 Guinea pig 7.5 pKd = 7.5 Binding
Competitive antagonist activity at beta-1 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced atrial contractile forceCompetitive antagonist activity at beta-1 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced atrial contractile force
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 7.5 pKd = 7.5 Binding
Competitive antagonist activity at beta-1 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced atrial contractile forceCompetitive antagonist activity at beta-1 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced atrial contractile force
ChEMBL 249 6 3 4 1.3 CC(C)NCC(O)COc1cccc2[nH]cnc12 10.1021/jm00188a019
13621690 9777 0 None 1318 2 Guinea pig 7.5 pKd = 7.5 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
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 7.5 pKd = 7.5 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
ChEMBL 440 12 4 7 1.8 COc1ccc(CCNCC(O)COc2ccc(-c3nc(C(N)=O)c[nH]3)cc2)cc1OC 10.1021/jm00156a028
13621631 9584 0 None 169 2 Guinea pig 7.5 pKd = 7.5 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-1 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 7.5 pKd = 7.5 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig tracheaIn vitro inhibitory activity against beta-1 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
12606706 92788 0 None -13 2 Guinea pig 6.5 pKd = 6.5 Binding
Beta-1 adrenergic receptor blocking activity in atria of guinea pig.Beta-1 adrenergic receptor blocking activity in atria 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 6.5 pKd = 6.5 Binding
Beta-1 adrenergic receptor blocking activity in atria of guinea pig.Beta-1 adrenergic receptor blocking activity in atria 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 6.5 pKd = 6.5 Binding
Beta-1 adrenergic receptor blocking activity in atria of guinea pig.Beta-1 adrenergic receptor blocking activity in atria of guinea pig.
ChEMBL 202 5 2 4 1.1 CC(C)=NOCC(O)CNC(C)(C)C 10.1021/jm00376a011
3869259 156899 3 None -3 2 Human 5.5 pKd = 5.5 Binding
Displacement of [3H](-)CGP12177 from human beta1-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting methodDisplacement of [3H](-)CGP12177 from human beta1-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 5.5 pKd = 5.5 Binding
Displacement of [3H](-)CGP12177 from human beta1-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting methodDisplacement of [3H](-)CGP12177 from human beta1-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 5.5 pKd = 5.5 Binding
Displacement of [3H](-)CGP12177 from human beta1-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting methodDisplacement of [3H](-)CGP12177 from human beta1-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 5.5 pKd = 5.5 Binding
Displacement of [3H](-)CGP12177 from human beta1-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting methodDisplacement of [3H](-)CGP12177 from human beta1-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
21296271 96474 3 None -1 2 Guinea pig 4.5 pKd = 4.5 Binding
Beta-1 adrenergic receptor blocking activity in atria of guinea pig.Beta-1 adrenergic receptor blocking activity in atria 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-1 adrenergic receptor blocking activity in atria of guinea pig.Beta-1 adrenergic receptor blocking activity in atria of guinea pig.
ChEMBL 241 7 2 3 1.9 CC(C)(C)NCC(O)COC(C1CC1)C1CC1 10.1021/jm00376a011
54757331 65171 0 None -39 3 Human 7.5 pKd = 7.5 Binding
Displacement of [3H]-CGP 12177 from human beta-1 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-1 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 7.5 pKd = 7.5 Binding
Displacement of [3H]-CGP 12177 from human beta-1 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-1 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
15578592 99028 2 None 1 2 Guinea pig 7.5 pKd = 7.5 Binding
In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.
ChEMBL 281 9 2 5 1.3 CCOC(=O)CCNCC(O)COc1ccccc1C 10.1021/jm00354a002
CHEMBL283289 99028 2 None 1 2 Guinea pig 7.5 pKd = 7.5 Binding
In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.
ChEMBL 281 9 2 5 1.3 CCOC(=O)CCNCC(O)COc1ccccc1C 10.1021/jm00354a002
15578606 107467 2 None 3 2 Guinea pig 7.5 pKd = 7.5 Binding
In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.
ChEMBL 267 8 2 5 0.9 COC(=O)CCNCC(O)COc1ccccc1C 10.1021/jm00354a002
CHEMBL31938 107467 2 None 3 2 Guinea pig 7.5 pKd = 7.5 Binding
In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.
ChEMBL 267 8 2 5 0.9 COC(=O)CCNCC(O)COc1ccccc1C 10.1021/jm00354a002
559935 103307 7 None 12 2 Guinea pig 6.5 pKd = 6.5 Binding
Ability to block Beta-1 adrenergic receptor in guinea pig right atria preparationAbility to block Beta-1 adrenergic receptor in guinea pig right atria 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 6.5 pKd = 6.5 Binding
Ability to block Beta-1 adrenergic receptor in guinea pig right atria preparationAbility to block Beta-1 adrenergic receptor in guinea pig right atria preparation
ChEMBL 281 6 2 5 1.6 COC(=O)c1ccc(OCC(O)CNC(C)(C)C)cc1 10.1021/jm00354a003
11722868 103887 0 None 7 2 Guinea pig 6.5 pKd = 6.5 Binding
Ability to block Beta-1 adrenergic receptor in guinea pig right atria preparationAbility to block Beta-1 adrenergic receptor in guinea pig right atria 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 6.5 pKd = 6.5 Binding
Ability to block Beta-1 adrenergic receptor in guinea pig right atria preparationAbility to block Beta-1 adrenergic receptor in guinea pig right atria preparation
ChEMBL 309 8 2 5 1.9 COC(=O)CCc1ccc(OCC(O)CNC(C)(C)C)cc1 10.1021/jm00354a003
12238216 106626 0 None 2 2 Guinea pig 6.5 pKd = 6.5 Binding
Ability to block Beta-1 adrenergic receptor in guinea pig right atria preparationAbility to block Beta-1 adrenergic receptor in guinea pig right atria 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 6.5 pKd = 6.5 Binding
Ability to block Beta-1 adrenergic receptor in guinea pig right atria preparationAbility to block Beta-1 adrenergic receptor in guinea pig right atria preparation
ChEMBL 281 8 2 5 1.6 CCOC(=O)c1ccc(OCC(O)CNC(C)C)cc1 10.1021/jm00354a003
13040909 106675 0 None 19 2 Guinea pig 6.5 pKd = 6.5 Binding
Ability to block Beta-1 adrenergic receptor in guinea pig right atria preparationAbility to block Beta-1 adrenergic receptor in guinea pig right atria 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 6.5 pKd = 6.5 Binding
Ability to block Beta-1 adrenergic receptor in guinea pig right atria preparationAbility to block Beta-1 adrenergic receptor in guinea pig right atria preparation
ChEMBL 417 13 2 7 2.4 COC(=O)CCc1ccc(OCC(O)CNCCc2ccc(OC)c(OC)c2)cc1 10.1021/jm00354a003
12238216 106626 0 None 2 2 Guinea pig 6.5 pKd = 6.5 Binding
Activity at beta-1 adrenergic receptorActivity at beta-1 adrenergic receptor
ChEMBL 281 8 2 5 1.6 CCOC(=O)c1ccc(OCC(O)CNC(C)C)cc1 10.1021/jm00103a004
CHEMBL31608 106626 0 None 2 2 Guinea pig 6.5 pKd = 6.5 Binding
Activity at beta-1 adrenergic receptorActivity at beta-1 adrenergic receptor
ChEMBL 281 8 2 5 1.6 CCOC(=O)c1ccc(OCC(O)CNC(C)C)cc1 10.1021/jm00103a004
159899 107056 28 None 1 2 Guinea pig 6.5 pKd = 6.5 Binding
In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.
ChEMBL 217 4 2 3 1.5 NCC(O)COc1cccc2ccccc12 10.1021/jm00354a002
CHEMBL31888 107056 28 None 1 2 Guinea pig 6.5 pKd = 6.5 Binding
In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.
ChEMBL 217 4 2 3 1.5 NCC(O)COc1cccc2ccccc12 10.1021/jm00354a002
13040917 99307 0 None - 1 Guinea pig 5.5 pKd = 5.5 Binding
Ability to block Beta-1 adrenergic receptor in guinea pig right atria preparationAbility to block Beta-1 adrenergic receptor in guinea pig right atria preparation
ChEMBL 383 11 2 9 0.3 CCOC(=O)C(NCC(O)COc1ccccc1C(=O)OC)C(=O)OCC 10.1021/jm00354a003
CHEMBL285233 99307 0 None - 1 Guinea pig 5.5 pKd = 5.5 Binding
Ability to block Beta-1 adrenergic receptor in guinea pig right atria preparationAbility to block Beta-1 adrenergic receptor in guinea pig right atria preparation
ChEMBL 383 11 2 9 0.3 CCOC(=O)C(NCC(O)COc1ccccc1C(=O)OC)C(=O)OCC 10.1021/jm00354a003
15578604 106607 1 None -1 2 Guinea pig 5.5 pKd = 5.5 Binding
In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.
ChEMBL 253 7 2 5 0.5 COC(=O)CNCC(O)COc1ccccc1C 10.1021/jm00354a002
CHEMBL31598 106607 1 None -1 2 Guinea pig 5.5 pKd = 5.5 Binding
In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.
ChEMBL 253 7 2 5 0.5 COC(=O)CNCC(O)COc1ccccc1C 10.1021/jm00354a002
56598831 88699 0 None 295 2 Human 7.5 pKd = 7.5 Binding
Displacement of [3H]-CGP12177 from human beta1 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta1 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 459 15 5 7 2.3 O=C(NCCNCC(O)COc1ccc(OCCOCC2CC2)cc1)Nc1ccc(O)cc1 10.1021/jm400348g
CHEMBL2348220 88699 0 None 295 2 Human 7.5 pKd = 7.5 Binding
Displacement of [3H]-CGP12177 from human beta1 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta1 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 459 15 5 7 2.3 O=C(NCCNCC(O)COc1ccc(OCCOCC2CC2)cc1)Nc1ccc(O)cc1 10.1021/jm400348g
CHEMBL2365796 88699 0 None 295 2 Human 7.5 pKd = 7.5 Binding
Displacement of [3H]-CGP12177 from human beta1 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta1 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 459 15 5 7 2.3 O=C(NCCNCC(O)COc1ccc(OCCOCC2CC2)cc1)Nc1ccc(O)cc1 10.1021/jm400348g
54756927 65141 0 None -97 3 Human 7.5 pKd = 7.5 Binding
Displacement of [3H]-CGP 12177 from human beta-1 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-1 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 7.5 pKd = 7.5 Binding
Displacement of [3H]-CGP 12177 from human beta-1 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-1 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
54579961 62717 1 None -3 2 Guinea pig 7.5 pKd = 7.5 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor determined as pA2 in guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor determined as pA2 in guinea pig atria
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 7.5 pKd = 7.5 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor determined as pA2 in guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor determined as pA2 in guinea pig atria
ChEMBL 254 7 2 4 1.9 CC(C)(C)NC[C@@H](O)CON=C(C1CC1)C1CC1 10.1021/jm00145a008
3486 3096 51 None -1 11 Rat 6.5 pKd = 6.5 Binding
Antagonist activity at beta1 adrenergic receptor in isolated rat atriaAntagonist activity at beta1 adrenergic receptor in isolated rat atria
ChEMBL 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C 10.1021/jm00207a025
4883 3096 51 None -1 11 Rat 6.5 pKd = 6.5 Binding
Antagonist activity at beta1 adrenergic receptor in isolated rat atriaAntagonist activity at beta1 adrenergic receptor in isolated rat atria
ChEMBL 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C 10.1021/jm00207a025
555 3096 51 None -1 11 Rat 6.5 pKd = 6.5 Binding
Antagonist activity at beta1 adrenergic receptor in isolated rat atriaAntagonist activity at beta1 adrenergic receptor in isolated rat atria
ChEMBL 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C 10.1021/jm00207a025
CHEMBL6995 3096 51 None -1 11 Rat 6.5 pKd = 6.5 Binding
Antagonist activity at beta1 adrenergic receptor in isolated rat atriaAntagonist activity at beta1 adrenergic receptor in isolated rat atria
ChEMBL 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C 10.1021/jm00207a025
DB01297 3096 51 None -1 11 Rat 6.5 pKd = 6.5 Binding
Antagonist activity at beta1 adrenergic receptor in isolated rat atriaAntagonist activity at beta1 adrenergic receptor in isolated rat atria
ChEMBL 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C 10.1021/jm00207a025
44274622 99318 0 None -3 2 Guinea pig 5.5 pKd = 5.5 Binding
Beta-1 adrenergic receptor blocking activity in atria of guinea pig.Beta-1 adrenergic receptor blocking activity in atria 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 5.5 pKd = 5.5 Binding
Beta-1 adrenergic receptor blocking activity in atria of guinea pig.Beta-1 adrenergic receptor blocking activity in atria of guinea pig.
ChEMBL 215 6 2 3 1.6 CC(OCC(O)CNC(C)(C)C)C1CC1 10.1021/jm00376a011
29072430 158911 12 None -6 2 Human 4.5 pKd = 4.5 Binding
Displacement of [3H](-)CGP12177 from human beta1-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting methodDisplacement of [3H](-)CGP12177 from human beta1-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 4.5 pKd = 4.5 Binding
Displacement of [3H](-)CGP12177 from human beta1-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting methodDisplacement of [3H](-)CGP12177 from human beta1-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 4.5 pKd = 4.5 Binding
Displacement of [3H](-)CGP12177 from human beta1-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting methodDisplacement of [3H](-)CGP12177 from human beta1-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
54758417 65140 0 None -38 3 Human 7.4 pKd = 7.4 Binding
Displacement of [3H]-CGP 12177 from human beta-1 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-1 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 7.4 pKd = 7.4 Binding
Displacement of [3H]-CGP 12177 from human beta-1 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-1 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
214004 109965 4 None - 1 Rat 5.4 pKd = 5.4 Binding
Antagonist activity at beta1 adrenergic receptor in isolated rat atriaAntagonist activity at beta1 adrenergic receptor in isolated rat atria
ChEMBL 266 7 3 4 0.8 CNC(=O)c1ccc(OCC(O)CNC(C)C)cc1 10.1021/jm00207a025
CHEMBL3247301 109965 4 None - 1 Rat 5.4 pKd = 5.4 Binding
Antagonist activity at beta1 adrenergic receptor in isolated rat atriaAntagonist activity at beta1 adrenergic receptor in isolated rat atria
ChEMBL 266 7 3 4 0.8 CNC(=O)c1ccc(OCC(O)CNC(C)C)cc1 10.1021/jm00207a025
3067050 92973 1 None -3 2 Guinea pig 4.4 pKd = 4.4 Binding
Beta-1 adrenergic receptor blocking activity in atria of guinea pig.Beta-1 adrenergic receptor blocking activity in atria 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 4.4 pKd = 4.4 Binding
Beta-1 adrenergic receptor blocking activity in atria of guinea pig.Beta-1 adrenergic receptor blocking activity in atria of guinea pig.
ChEMBL 215 6 2 3 1.7 C=CC(C)(C)OCC(O)CNC(C)(C)C 10.1021/jm00376a011
14201550 101679 0 None - 1 Guinea pig 6.4 pKd = 6.4 Binding
Beta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atriumBeta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atrium
ChEMBL 263 7 2 3 2.1 O[C@H](COCCCc1ccccc1)[C@H]1CCCCN1 10.1021/jm00119a011
CHEMBL302605 101679 0 None - 1 Guinea pig 6.4 pKd = 6.4 Binding
Beta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atriumBeta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atrium
ChEMBL 263 7 2 3 2.1 O[C@H](COCCCc1ccccc1)[C@H]1CCCCN1 10.1021/jm00119a011
16415941 158506 12 None -2 2 Human 4.4 pKd = 4.4 Binding
Displacement of [3H](-)CGP12177 from human beta1-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting methodDisplacement of [3H](-)CGP12177 from human beta1-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 4.4 pKd = 4.4 Binding
Displacement of [3H](-)CGP12177 from human beta1-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting methodDisplacement of [3H](-)CGP12177 from human beta1-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 4.4 pKd = 4.4 Binding
Displacement of [3H](-)CGP12177 from human beta1-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting methodDisplacement of [3H](-)CGP12177 from human beta1-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
12484297 109216 0 None -15 2 Guinea pig 7.4 pKd = 7.4 Binding
Competitive antagonist activity at beta-1 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced atrial beat rateCompetitive antagonist activity at beta-1 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced atrial beat rate
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 7.4 pKd = 7.4 Binding
Competitive antagonist activity at beta-1 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced atrial beat rateCompetitive antagonist activity at beta-1 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced atrial beat rate
ChEMBL 249 6 3 4 1.3 CC(C)NCC(O)COc1cccc2[nH]cnc12 10.1021/jm00188a019
2369 615 75 None -13 8 Guinea pig 7.4 pKd = 7.4 Binding
Compound was tested for the biological activity at the Beta-1 adrenergic receptorCompound was tested for the biological activity at the Beta-1 adrenergic receptor
ChEMBL 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C 10.1021/jm00103a004
356 615 75 None -13 8 Guinea pig 7.4 pKd = 7.4 Binding
Compound was tested for the biological activity at the Beta-1 adrenergic receptorCompound was tested for the biological activity at the Beta-1 adrenergic receptor
ChEMBL 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C 10.1021/jm00103a004
549 615 75 None -13 8 Guinea pig 7.4 pKd = 7.4 Binding
Compound was tested for the biological activity at the Beta-1 adrenergic receptorCompound was tested for the biological activity at the Beta-1 adrenergic receptor
ChEMBL 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C 10.1021/jm00103a004
CHEMBL423 615 75 None -13 8 Guinea pig 7.4 pKd = 7.4 Binding
Compound was tested for the biological activity at the Beta-1 adrenergic receptorCompound was tested for the biological activity at the Beta-1 adrenergic receptor
ChEMBL 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C 10.1021/jm00103a004
DB00195 615 75 None -13 8 Guinea pig 7.4 pKd = 7.4 Binding
Compound was tested for the biological activity at the Beta-1 adrenergic receptorCompound was tested for the biological activity at the Beta-1 adrenergic receptor
ChEMBL 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C 10.1021/jm00103a004
15578563 99598 0 None 1 2 Guinea pig 7.4 pKd = 7.4 Binding
In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.
ChEMBL 317 9 2 5 2.1 CCOC(=O)CCNCC(O)COc1cccc2ccccc12 10.1021/jm00354a002
CHEMBL287242 99598 0 None 1 2 Guinea pig 7.4 pKd = 7.4 Binding
In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.
ChEMBL 317 9 2 5 2.1 CCOC(=O)CCNCC(O)COc1cccc2ccccc12 10.1021/jm00354a002
15578588 103637 2 None 6 2 Guinea pig 7.4 pKd = 7.4 Binding
In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.
ChEMBL 301 9 2 5 1.6 CCOC(=O)CCNCC(O)COc1ccccc1Cl 10.1021/jm00354a002
CHEMBL30942 103637 2 None 6 2 Guinea pig 7.4 pKd = 7.4 Binding
In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.
ChEMBL 301 9 2 5 1.6 CCOC(=O)CCNCC(O)COc1ccccc1Cl 10.1021/jm00354a002
15578608 107000 2 None 5 2 Guinea pig 7.4 pKd = 7.4 Binding
In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.
ChEMBL 295 10 2 5 1.7 CCOC(=O)CCCNCC(O)COc1ccccc1C 10.1021/jm00354a002
CHEMBL31857 107000 2 None 5 2 Guinea pig 7.4 pKd = 7.4 Binding
In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.
ChEMBL 295 10 2 5 1.7 CCOC(=O)CCCNCC(O)COc1ccccc1C 10.1021/jm00354a002
15578590 161490 2 None 5 2 Guinea pig 7.4 pKd = 7.4 Binding
In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.
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 7.4 pKd = 7.4 Binding
In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.
ChEMBL 301 9 2 5 1.6 CCOC(=O)CCNCC(O)COc1cccc(Cl)c1 10.1021/jm00354a002
12941056 101733 0 None 10 2 Guinea pig 6.4 pKd = 6.4 Binding
Ability to block Beta-1 adrenergic receptor in guinea pig right atria preparationAbility to block Beta-1 adrenergic receptor in guinea pig right atria 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 6.4 pKd = 6.4 Binding
Ability to block Beta-1 adrenergic receptor in guinea pig right atria preparationAbility to block Beta-1 adrenergic receptor in guinea pig right atria preparation
ChEMBL 281 8 2 5 1.1 COC(=O)Cc1ccc(OCC(O)CNC(C)C)cc1 10.1021/jm00354a003
193122 1871 6 None -3 2 Guinea pig 6.4 pKd = 6.4 Binding
Compound was tested for the biological activity at the Beta-1 adrenergic receptorCompound was tested for the biological activity at the Beta-1 adrenergic receptor
ChEMBL 283 10 2 5 1.5 COCCOc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm00103a004
542 1871 6 None -3 2 Guinea pig 6.4 pKd = 6.4 Binding
Compound was tested for the biological activity at the Beta-1 adrenergic receptorCompound was tested for the biological activity at the Beta-1 adrenergic receptor
ChEMBL 283 10 2 5 1.5 COCCOc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm00103a004
CHEMBL142773 1871 6 None -3 2 Guinea pig 6.4 pKd = 6.4 Binding
Compound was tested for the biological activity at the Beta-1 adrenergic receptorCompound was tested for the biological activity at the Beta-1 adrenergic receptor
ChEMBL 283 10 2 5 1.5 COCCOc1ccc(cc1)OCC(CNC(C)C)O 10.1021/jm00103a004
15569837 106050 2 None 6 2 Guinea pig 6.4 pKd = 6.4 Binding
In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.
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 6.4 pKd = 6.4 Binding
In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.
ChEMBL 301 9 2 5 1.6 CCOC(=O)CCNCC(O)COc1ccc(Cl)cc1 10.1021/jm00354a002
15578596 110922 2 None -1 2 Guinea pig 6.4 pKd = 6.4 Binding
In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.
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 6.4 pKd = 6.4 Binding
In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.
ChEMBL 297 10 2 6 1.0 CCOC(=O)CCNCC(O)COc1cccc(OC)c1 10.1021/jm00354a002
15578614 102358 0 None - 1 Guinea pig 6.4 pKd = 6.4 Binding
The compound was tested in vitro for its ability to block Beta-1 adrenergic receptor in guinea pig right atriaThe compound was tested in vitro for its ability to block Beta-1 adrenergic receptor in guinea pig right atria
ChEMBL 315 9 2 5 2.0 O=C(CCNCC(O)COc1ccccc1)Oc1ccccc1 10.1021/jm00354a002
CHEMBL30558 102358 0 None - 1 Guinea pig 6.4 pKd = 6.4 Binding
The compound was tested in vitro for its ability to block Beta-1 adrenergic receptor in guinea pig right atriaThe compound was tested in vitro for its ability to block Beta-1 adrenergic receptor in guinea pig right atria
ChEMBL 315 9 2 5 2.0 O=C(CCNCC(O)COc1ccccc1)Oc1ccccc1 10.1021/jm00354a002
13040902 104395 0 None 1 2 Guinea pig 5.4 pKd = 5.4 Binding
Ability to block Beta-1 adrenergic receptor in guinea pig right atria preparationAbility to block Beta-1 adrenergic receptor in guinea pig right atria 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 5.4 pKd = 5.4 Binding
Ability to block Beta-1 adrenergic receptor in guinea pig right atria preparationAbility to block Beta-1 adrenergic receptor in guinea pig right atria preparation
ChEMBL 323 11 2 5 2.3 CCCOC(=O)CCc1ccc(OCC(O)CNC(C)C)cc1 10.1021/jm00354a003
14348818 109273 0 None -5 3 Guinea pig 4.4 pKd = 4.4 Binding
The compound was tested for beta-adrenergic activity against Beta-1 adrenergic receptor from guinea pig left atriaThe compound was tested for beta-adrenergic activity against Beta-1 adrenergic receptor from guinea pig left atria
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 -5 3 Guinea pig 4.4 pKd = 4.4 Binding
The compound was tested for beta-adrenergic activity against Beta-1 adrenergic receptor from guinea pig left atriaThe compound was tested for beta-adrenergic activity against Beta-1 adrenergic receptor from guinea pig left atria
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
2803 939 53 None -134 19 Guinea pig 4.4 pKd = 4.4 Binding
The compound was tested for beta-adrenergic activity against Beta-1 adrenergic receptor from guinea pig right atriaThe compound was tested for beta-adrenergic activity against Beta-1 adrenergic receptor from guinea pig right atria
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1021/jm00115a008
516 939 53 None -134 19 Guinea pig 4.4 pKd = 4.4 Binding
The compound was tested for beta-adrenergic activity against Beta-1 adrenergic receptor from guinea pig right atriaThe compound was tested for beta-adrenergic activity against Beta-1 adrenergic receptor from guinea pig right atria
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1021/jm00115a008
704 939 53 None -134 19 Guinea pig 4.4 pKd = 4.4 Binding
The compound was tested for beta-adrenergic activity against Beta-1 adrenergic receptor from guinea pig right atriaThe compound was tested for beta-adrenergic activity against Beta-1 adrenergic receptor from guinea pig right atria
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1021/jm00115a008
CHEMBL134 939 53 None -134 19 Guinea pig 4.4 pKd = 4.4 Binding
The compound was tested for beta-adrenergic activity against Beta-1 adrenergic receptor from guinea pig right atriaThe compound was tested for beta-adrenergic activity against Beta-1 adrenergic receptor from guinea pig right atria
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1021/jm00115a008
DB00575 939 53 None -134 19 Guinea pig 4.4 pKd = 4.4 Binding
The compound was tested for beta-adrenergic activity against Beta-1 adrenergic receptor from guinea pig right atriaThe compound was tested for beta-adrenergic activity against Beta-1 adrenergic receptor from guinea pig right atria
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1021/jm00115a008
14348818 109273 0 None -5 3 Guinea pig 4.4 pKd = 4.4 Binding
The compound was tested for beta-adrenergic activity against Beta-1 adrenergic receptor from guinea pig right atriaThe compound was tested for beta-adrenergic activity against Beta-1 adrenergic receptor from guinea pig right atria
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 -5 3 Guinea pig 4.4 pKd = 4.4 Binding
The compound was tested for beta-adrenergic activity against Beta-1 adrenergic receptor from guinea pig right atriaThe compound was tested for beta-adrenergic activity against Beta-1 adrenergic receptor from guinea pig right atria
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
135079 10387 1 None 9772 2 Guinea pig 8.4 pKd = 8.4 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
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 8.4 pKd = 8.4 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
ChEMBL 479 12 3 7 4.4 COc1ccc(CCNCC(O)COc2ccc(-c3nc(-c4cccs4)c[nH]3)cc2)cc1OC 10.1021/jm00361a004
14201539 201820 0 None 1 2 Guinea pig 7.4 pKd = 7.4 Binding
Beta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atriumBeta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atrium
ChEMBL 271 4 2 3 2.7 O[C@H](COc1ccc2ccccc2c1)[C@H]1CCCCN1 10.1021/jm00119a011
CHEMBL66384 201820 0 None 1 2 Guinea pig 7.4 pKd = 7.4 Binding
Beta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atriumBeta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atrium
ChEMBL 271 4 2 3 2.7 O[C@H](COc1ccc2ccccc2c1)[C@H]1CCCCN1 10.1021/jm00119a011
2249 509 106 None 2 12 Guinea pig 7.4 pKd = 7.4 Binding
Antagonist activity at beta1 adrenoceptor in guinea pig atrium assessed as inhibition of isoproterenol-induced response after 20 minsAntagonist activity at beta1 adrenoceptor in guinea pig atrium 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 2 12 Guinea pig 7.4 pKd = 7.4 Binding
Antagonist activity at beta1 adrenoceptor in guinea pig atrium assessed as inhibition of isoproterenol-induced response after 20 minsAntagonist activity at beta1 adrenoceptor in guinea pig atrium 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 2 12 Guinea pig 7.4 pKd = 7.4 Binding
Antagonist activity at beta1 adrenoceptor in guinea pig atrium assessed as inhibition of isoproterenol-induced response after 20 minsAntagonist activity at beta1 adrenoceptor in guinea pig atrium 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 2 12 Guinea pig 7.4 pKd = 7.4 Binding
Antagonist activity at beta1 adrenoceptor in guinea pig atrium assessed as inhibition of isoproterenol-induced response after 20 minsAntagonist activity at beta1 adrenoceptor in guinea pig atrium 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 2 12 Guinea pig 7.4 pKd = 7.4 Binding
Antagonist activity at beta1 adrenoceptor in guinea pig atrium assessed as inhibition of isoproterenol-induced response after 20 minsAntagonist activity at beta1 adrenoceptor in guinea pig atrium 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
13621723 9844 0 None 1698 2 Guinea pig 7.4 pKd = 7.4 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
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 7.4 pKd = 7.4 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
ChEMBL 395 10 5 5 2.2 O=C(NCCNCC(O)COc1ccc(-c2ncc[nH]2)cc1)Nc1ccccc1 10.1021/jm00156a028
13621665 98032 0 None 1412 2 Guinea pig 7.4 pKd = 7.4 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
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 7.4 pKd = 7.4 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
ChEMBL 455 14 3 7 2.9 COCCc1c[nH]c(-c2ccc(OCC(O)CNCCc3ccc(OC)c(OC)c3)cc2)n1 10.1021/jm00156a028
328583 110031 1 None -676 2 Guinea pig 4.4 pKd = 4.4 Binding
Inhibition of beta1-adrenergic receptor in guinea pig auricle assessed as reversal of isoproterenol-induced effectInhibition of beta1-adrenergic receptor in guinea pig auricle assessed as reversal of isoproterenol-induced effect
ChEMBL 177 2 2 2 1.5 CC1(C)NC1C(O)c1ccccc1 10.1021/jm00199a012
CHEMBL3251298 110031 1 None -676 2 Guinea pig 4.4 pKd = 4.4 Binding
Inhibition of beta1-adrenergic receptor in guinea pig auricle assessed as reversal of isoproterenol-induced effectInhibition of beta1-adrenergic receptor in guinea pig auricle assessed as reversal of isoproterenol-induced effect
ChEMBL 177 2 2 2 1.5 CC1(C)NC1C(O)c1ccccc1 10.1021/jm00199a012
29074692 159180 13 None -2 2 Human 4.4 pKd = 4.4 Binding
Displacement of [3H](-)CGP12177 from human beta1-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting methodDisplacement of [3H](-)CGP12177 from human beta1-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 4.4 pKd = 4.4 Binding
Displacement of [3H](-)CGP12177 from human beta1-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting methodDisplacement of [3H](-)CGP12177 from human beta1-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 4.4 pKd = 4.4 Binding
Displacement of [3H](-)CGP12177 from human beta1-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting methodDisplacement of [3H](-)CGP12177 from human beta1-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
2184756 55591 3 None -12 2 Human 4.3 pKd = 4.3 Binding
Displacement of [3H](-)CGP12177 from human beta1-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting methodDisplacement of [3H](-)CGP12177 from human beta1-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 4.3 pKd = 4.3 Binding
Displacement of [3H](-)CGP12177 from human beta1-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting methodDisplacement of [3H](-)CGP12177 from human beta1-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
71662246 87820 0 None 11 2 Human 7.3 pKd = 7.3 Binding
Displacement of [3H]-CGP12177 from human beta1 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta1 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 7.3 pKd = 7.3 Binding
Displacement of [3H]-CGP12177 from human beta1 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta1 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
29057664 157568 13 None -1 2 Human 4.3 pKd = 4.3 Binding
Displacement of [3H](-)CGP12177 from human beta1-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting methodDisplacement of [3H](-)CGP12177 from human beta1-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 4.3 pKd = 4.3 Binding
Displacement of [3H](-)CGP12177 from human beta1-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting methodDisplacement of [3H](-)CGP12177 from human beta1-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 4.3 pKd = 4.3 Binding
Displacement of [3H](-)CGP12177 from human beta1-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting methodDisplacement of [3H](-)CGP12177 from human beta1-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
44459922 96352 0 None 4 2 Guinea pig 7.3 pKd = 7.3 Binding
Beta-1 adrenergic receptor blocking activity in atria of guinea pig.Beta-1 adrenergic receptor blocking activity in atria 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 7.3 pKd = 7.3 Binding
Beta-1 adrenergic receptor blocking activity in atria of guinea pig.Beta-1 adrenergic receptor blocking activity in atria 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
13302060 12711 0 None 112 2 Guinea pig 6.3 pKd = 6.3 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
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 6.3 pKd = 6.3 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
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 6.3 pKd = 6.3 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
ChEMBL 411 11 2 7 2.7 COc1ccc(CCNCC(O)COc2ccc(-c3nccn3C)cc2)cc1OC 10.1021/jm00156a028
21595422 101735 0 None 2 2 Guinea pig 7.3 pKd = 7.3 Binding
Beta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atriumBeta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atrium
ChEMBL 235 5 2 3 1.7 O[C@H](COCc1ccccc1)[C@@H]1CCCCN1 10.1021/jm00119a011
CHEMBL302935 101735 0 None 2 2 Guinea pig 7.3 pKd = 7.3 Binding
Beta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atriumBeta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atrium
ChEMBL 235 5 2 3 1.7 O[C@H](COCc1ccccc1)[C@@H]1CCCCN1 10.1021/jm00119a011
12606684 95615 3 None -15 2 Guinea pig 6.3 pKd = 6.3 Binding
Beta-1 adrenergic receptor blocking activity in atria of guinea pig.Beta-1 adrenergic receptor blocking activity in atria 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 6.3 pKd = 6.3 Binding
Beta-1 adrenergic receptor blocking activity in atria of guinea pig.Beta-1 adrenergic receptor blocking activity in atria 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 6.3 pKd = 6.3 Binding
Beta-1 adrenergic receptor blocking activity in atria of guinea pig.Beta-1 adrenergic receptor blocking activity in atria of guinea pig.
ChEMBL 203 6 2 3 1.4 CC(C)COCC(O)CNC(C)(C)C 10.1021/jm00376a011
12548683 22625 0 None 2 2 Guinea pig 8.3 pKd = 8.3 Binding
Ability to block Beta-1 adrenergic receptor in guinea pig right atria preparationAbility to block Beta-1 adrenergic receptor in guinea pig right atria 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 8.3 pKd = 8.3 Binding
Ability to block Beta-1 adrenergic receptor in guinea pig right atria preparationAbility to block Beta-1 adrenergic receptor in guinea pig right atria preparation
ChEMBL 267 7 2 5 1.2 COC(=O)c1ccccc1OCC(O)CNC(C)C 10.1021/jm00354a003
10467512 99413 0 None -2 2 Guinea pig 8.3 pKd = 8.3 Binding
Beta-1 adrenergic receptor blocking activity in atria of guinea pig.Beta-1 adrenergic receptor blocking activity in atria 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 8.3 pKd = 8.3 Binding
Beta-1 adrenergic receptor blocking activity in atria of guinea pig.Beta-1 adrenergic receptor blocking activity in atria of guinea pig.
ChEMBL 254 7 2 4 1.9 CC(C)(C)NCC(O)CON=C(C1CC1)C1CC1 10.1021/jm00376a011
13621599 9789 0 None 3981 2 Guinea pig 8.3 pKd = 8.3 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
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 8.3 pKd = 8.3 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
ChEMBL 513 12 3 7 5.0 COc1ccc(CCNCC(O)COc2ccc(-c3nc(-c4cccs4)c[nH]3)cc2Cl)cc1OC 10.1021/jm00156a028
13040884 23563 0 None 15 2 Guinea pig 8.3 pKd = 8.3 Binding
The compound was tested in vitro for its ability to block Beta-1 adrenergic receptor in guinea pig right atriaThe compound was tested in vitro for its ability to block Beta-1 adrenergic receptor in guinea pig right atria
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 8.3 pKd = 8.3 Binding
The compound was tested in vitro for its ability to block Beta-1 adrenergic receptor in guinea pig right atriaThe compound was tested in vitro for its ability to block Beta-1 adrenergic receptor in guinea pig right atria
ChEMBL 389 11 2 7 2.1 COC(=O)c1ccccc1OCC(O)CNCCc1ccc(OC)c(OC)c1 10.1021/jm00354a003
13621796 9342 0 None 1659 2 Guinea pig 8.3 pKd = 8.3 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
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 8.3 pKd = 8.3 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
ChEMBL 480 12 3 8 3.8 COc1ccc(CCNCC(O)COc2ccc(-c3nc(-c4cccs4)c[nH]3)cn2)cc1OC 10.1021/jm00156a028
13157365 127274 0 None 239 2 Guinea pig 8.3 pKd = 8.3 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
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 8.3 pKd = 8.3 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
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 8.2 pKd = 8.2 Binding
Antagonist activity at beta1 adrenoceptor in guinea pig atrium assessed as inhibition of isoproterenol-induced response after 20 minsAntagonist activity at beta1 adrenoceptor in guinea pig atrium 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 8.2 pKd = 8.2 Binding
Antagonist activity at beta1 adrenoceptor in guinea pig atrium assessed as inhibition of isoproterenol-induced response after 20 minsAntagonist activity at beta1 adrenoceptor in guinea pig atrium 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 8.2 pKd = 8.2 Binding
Antagonist activity at beta1 adrenoceptor in guinea pig atrium assessed as inhibition of isoproterenol-induced response after 20 minsAntagonist activity at beta1 adrenoceptor in guinea pig atrium 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
13040883 98705 0 None -1 2 Guinea pig 7.3 pKd = 7.3 Binding
Ability to block Beta-1 adrenergic receptor in guinea pig right atria preparationAbility to block Beta-1 adrenergic receptor in guinea pig right atria 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 7.3 pKd = 7.3 Binding
Ability to block Beta-1 adrenergic receptor in guinea pig right atria preparationAbility to block Beta-1 adrenergic receptor in guinea pig right atria preparation
ChEMBL 297 8 3 6 0.6 COC(=O)c1ccccc1OCC(O)CNC(C)(C)CO 10.1021/jm00354a003
13040896 101725 1 None 15 2 Guinea pig 7.3 pKd = 7.3 Binding
Ability to block Beta-1 adrenergic receptor in guinea pig right atria preparationAbility to block Beta-1 adrenergic receptor in guinea pig right atria 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 7.3 pKd = 7.3 Binding
Ability to block Beta-1 adrenergic receptor in guinea pig right atria preparationAbility to block Beta-1 adrenergic receptor in guinea pig right atria preparation
ChEMBL 293 8 2 5 1.6 COC(=O)/C=C/c1ccc(OCC(O)CNC(C)C)cc1 10.1021/jm00354a003
9970852 109969 0 None 25 2 Rat 7.3 pKd = 7.3 Binding
Antagonist activity at beta1 adrenergic receptor in isolated rat atriaAntagonist activity at beta1 adrenergic receptor in isolated rat atria
ChEMBL 279 8 2 4 2.5 C/C=C/c1ccc(OCC(O)CNC(C)C)c(OC)c1 10.1021/jm00207a025
CHEMBL3247308 109969 0 None 25 2 Rat 7.3 pKd = 7.3 Binding
Antagonist activity at beta1 adrenergic receptor in isolated rat atriaAntagonist activity at beta1 adrenergic receptor in isolated rat atria
ChEMBL 279 8 2 4 2.5 C/C=C/c1ccc(OCC(O)CNC(C)C)c(OC)c1 10.1021/jm00207a025
15578573 106865 2 None 25 2 Guinea pig 7.3 pKd = 7.3 Binding
In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.
ChEMBL 267 9 2 5 1.0 CCOC(=O)CCNCC(O)COc1ccccc1 10.1021/jm00354a002
CHEMBL31772 106865 2 None 25 2 Guinea pig 7.3 pKd = 7.3 Binding
In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.
ChEMBL 267 9 2 5 1.0 CCOC(=O)CCNCC(O)COc1ccccc1 10.1021/jm00354a002
13621595 7498 0 None 575 2 Guinea pig 7.3 pKd = 7.3 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
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 7.3 pKd = 7.3 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
ChEMBL 489 11 3 6 3.7 COc1ccc(CCNCC(O)COc2ccc(-c3nc(C)c[nH]3)cc2Br)cc1OC 10.1021/jm00156a028
13040890 103922 0 None 3 2 Guinea pig 6.3 pKd = 6.3 Binding
Activity at beta-1 adrenergic receptorActivity at beta-1 adrenergic receptor
ChEMBL 279 8 2 5 1.7 C=COC(=O)c1ccc(OCC(O)CNC(C)C)cc1 10.1021/jm00103a004
CHEMBL31036 103922 0 None 3 2 Guinea pig 6.3 pKd = 6.3 Binding
Activity at beta-1 adrenergic receptorActivity at beta-1 adrenergic receptor
ChEMBL 279 8 2 5 1.7 C=COC(=O)c1ccc(OCC(O)CNC(C)C)cc1 10.1021/jm00103a004
13040890 103922 0 None 3 2 Guinea pig 6.3 pKd = 6.3 Binding
The compound was tested in vitro for its ability to block Beta-1 adrenergic receptor in guinea pig right atria preparationThe compound was tested in vitro for its ability to block Beta-1 adrenergic receptor in guinea pig right atria 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 6.3 pKd = 6.3 Binding
The compound was tested in vitro for its ability to block Beta-1 adrenergic receptor in guinea pig right atria preparationThe compound was tested in vitro for its ability to block Beta-1 adrenergic receptor in guinea pig right atria preparation
ChEMBL 279 8 2 5 1.7 C=COC(=O)c1ccc(OCC(O)CNC(C)C)cc1 10.1021/jm00354a003
14348818 109273 0 None -5 3 Guinea pig 4.3 pKd = 4.3 Binding
The compound was tested for beta-adrenergic activity against Beta-1 adrenergic receptor from guinea pig left atriaThe compound was tested for beta-adrenergic activity against Beta-1 adrenergic receptor from guinea pig left atria
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 -5 3 Guinea pig 4.3 pKd = 4.3 Binding
The compound was tested for beta-adrenergic activity against Beta-1 adrenergic receptor from guinea pig left atriaThe compound was tested for beta-adrenergic activity against Beta-1 adrenergic receptor from guinea pig left atria
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
14348819 9318 0 None - 1 Guinea pig 4.3 pKd = 4.3 Binding
The compound was tested for beta-adrenergic activity against Beta-1 adrenergic receptor from guinea pig right atriaThe compound was tested for beta-adrenergic activity against Beta-1 adrenergic receptor from guinea pig right atria
ChEMBL 374 6 4 6 2.5 CC(C)(C)NCC(O)COc1cc(Cl)c(NC2=NCCN2)c(Cl)c1 10.1021/jm00115a008
CHEMBL111694 9318 0 None - 1 Guinea pig 4.3 pKd = 4.3 Binding
The compound was tested for beta-adrenergic activity against Beta-1 adrenergic receptor from guinea pig right atriaThe compound was tested for beta-adrenergic activity against Beta-1 adrenergic receptor from guinea pig right atria
ChEMBL 374 6 4 6 2.5 CC(C)(C)NCC(O)COc1cc(Cl)c(NC2=NCCN2)c(Cl)c1 10.1021/jm00115a008
14348818 109273 0 None -5 3 Guinea pig 4.3 pKd = 4.3 Binding
The compound was tested for beta-adrenergic activity against Beta-1 adrenergic receptor from guinea pig right atriaThe compound was tested for beta-adrenergic activity against Beta-1 adrenergic receptor from guinea pig right atria
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 -5 3 Guinea pig 4.3 pKd = 4.3 Binding
The compound was tested for beta-adrenergic activity against Beta-1 adrenergic receptor from guinea pig right atriaThe compound was tested for beta-adrenergic activity against Beta-1 adrenergic receptor from guinea pig right atria
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
13157384 77921 0 None - 1 Guinea pig 7.3 pKd = 7.3 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
ChEMBL 479 12 3 7 4.4 COc1ccc(CCNC[C@@H](O)COc2ccc(-c3nc(-c4cccs4)c[nH]3)cc2)cc1OC 10.1021/jm00361a004
CHEMBL2093062 77921 0 None - 1 Guinea pig 7.3 pKd = 7.3 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
ChEMBL 479 12 3 7 4.4 COc1ccc(CCNC[C@@H](O)COc2ccc(-c3nc(-c4cccs4)c[nH]3)cc2)cc1OC 10.1021/jm00361a004
CHEMBL2109975 77921 0 None - 1 Guinea pig 7.3 pKd = 7.3 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
ChEMBL 479 12 3 7 4.4 COc1ccc(CCNC[C@@H](O)COc2ccc(-c3nc(-c4cccs4)c[nH]3)cc2)cc1OC 10.1021/jm00361a004
54757229 65169 0 None -33 3 Human 7.3 pKd = 7.3 Binding
Displacement of [3H]-CGP 12177 from human beta-1 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-1 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 -33 3 Human 7.3 pKd = 7.3 Binding
Displacement of [3H]-CGP 12177 from human beta-1 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-1 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
44307572 201356 0 None 1 2 Guinea pig 7.3 pKd = 7.3 Binding
Beta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atriumBeta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atrium
ChEMBL 235 4 1 3 1.9 CN1CCCC[C@H]1[C@H](O)COc1ccccc1 10.1021/jm00119a011
CHEMBL63582 201356 0 None 1 2 Guinea pig 7.3 pKd = 7.3 Binding
Beta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atriumBeta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atrium
ChEMBL 235 4 1 3 1.9 CN1CCCC[C@H]1[C@H](O)COc1ccccc1 10.1021/jm00119a011
54757026 65144 0 None -74 3 Human 7.3 pKd = 7.3 Binding
Displacement of [3H]-CGP 12177 from human beta-1 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-1 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 7.3 pKd = 7.3 Binding
Displacement of [3H]-CGP 12177 from human beta-1 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-1 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
173 3199 88 None -69 23 Human 5.3 pKd = 5.3 Binding
Binding affinity to His-tagged human beta1 adrenergic receptor expressed in HEK293 cell membranes by surface plasmon resonance analysisBinding affinity to His-tagged human beta1 adrenergic receptor expressed in HEK293 cell membranes by surface plasmon resonance analysis
ChEMBL 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 10.1021/jm400140q
5011 3199 88 None -69 23 Human 5.3 pKd = 5.3 Binding
Binding affinity to His-tagged human beta1 adrenergic receptor expressed in HEK293 cell membranes by surface plasmon resonance analysisBinding affinity to His-tagged human beta1 adrenergic receptor expressed in HEK293 cell membranes by surface plasmon resonance analysis
ChEMBL 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 10.1021/jm400140q
CHEMBL18772 3199 88 None -69 23 Human 5.3 pKd = 5.3 Binding
Binding affinity to His-tagged human beta1 adrenergic receptor expressed in HEK293 cell membranes by surface plasmon resonance analysisBinding affinity to His-tagged human beta1 adrenergic receptor expressed in HEK293 cell membranes by surface plasmon resonance analysis
ChEMBL 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 10.1021/jm400140q
173 3199 88 None -69 23 Human 5.3 pKd = 5.3 Binding
Binding affinity to His-tagged human beta1 adrenergic receptor expressed in HEK293 cell membranes by surface plasmon resonance analysisBinding affinity to His-tagged human beta1 adrenergic receptor expressed in HEK293 cell membranes by surface plasmon resonance analysis
ChEMBL 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 10.1021/jm400140q
5011 3199 88 None -69 23 Human 5.3 pKd = 5.3 Binding
Binding affinity to His-tagged human beta1 adrenergic receptor expressed in HEK293 cell membranes by surface plasmon resonance analysisBinding affinity to His-tagged human beta1 adrenergic receptor expressed in HEK293 cell membranes by surface plasmon resonance analysis
ChEMBL 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 10.1021/jm400140q
CHEMBL18772 3199 88 None -69 23 Human 5.3 pKd = 5.3 Binding
Binding affinity to His-tagged human beta1 adrenergic receptor expressed in HEK293 cell membranes by surface plasmon resonance analysisBinding affinity to His-tagged human beta1 adrenergic receptor expressed in HEK293 cell membranes by surface plasmon resonance analysis
ChEMBL 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 10.1021/jm400140q
21595420 202008 0 None -1 2 Guinea pig 7.2 pKd = 7.2 Binding
Beta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atriumBeta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atrium
ChEMBL 235 4 2 3 1.9 Cc1ccc(OC[C@@H](O)[C@@H]2CCCCN2)cc1 10.1021/jm00119a011
CHEMBL67631 202008 0 None -1 2 Guinea pig 7.2 pKd = 7.2 Binding
Beta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atriumBeta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atrium
ChEMBL 235 4 2 3 1.9 Cc1ccc(OC[C@@H](O)[C@@H]2CCCCN2)cc1 10.1021/jm00119a011
13590031 9295 0 None - 1 Guinea pig 7.2 pKd = 7.2 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
ChEMBL 414 11 2 7 3.4 COc1ccc(CCNCC(O)COc2ccc(-c3nccs3)cc2)cc1OC 10.1021/jm00156a028
CHEMBL11155 9295 0 None - 1 Guinea pig 7.2 pKd = 7.2 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
ChEMBL 414 11 2 7 3.4 COc1ccc(CCNCC(O)COc2ccc(-c3nccs3)cc2)cc1OC 10.1021/jm00156a028
165193 3126 60 None -2 43 Human 8.2 pKd = 8.2 Binding
Displacement of [3H]-CGP 12177 from human beta-1 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-1 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 -2 43 Human 8.2 pKd = 8.2 Binding
Displacement of [3H]-CGP 12177 from human beta-1 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-1 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 -2 43 Human 8.2 pKd = 8.2 Binding
Displacement of [3H]-CGP 12177 from human beta-1 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-1 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 -2 43 Human 8.2 pKd = 8.2 Binding
Displacement of [3H]-CGP 12177 from human beta-1 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-1 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 -2 43 Human 8.2 pKd = 8.2 Binding
Displacement of [3H]-CGP 12177 from human beta-1 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-1 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 -2 43 Human 8.2 pKd = 8.2 Binding
Displacement of [3H]-CGP 12177 from human beta-1 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-1 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 -2 43 Human 8.2 pKd = 8.2 Binding
Displacement of [3H]-CGP 12177 from human beta-1 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-1 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 -2 43 Human 8.2 pKd = 8.2 Binding
Displacement of [3H]-CGP 12177 from human beta-1 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-1 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 -2 43 Human 8.2 pKd = 8.2 Binding
Displacement of [3H]-CGP 12177 from human beta-1 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-1 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 -2 43 Human 8.2 pKd = 8.2 Binding
Displacement of [3H]-CGP 12177 from human beta-1 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-1 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 -2 43 Human 8.2 pKd = 8.2 Binding
Displacement of [3H]-CGP 12177 from human beta-1 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-1 adrenergic receptor expressed in CHOK1 cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm2008562
13157380 61793 0 None 2041 2 Guinea pig 8.2 pKd = 8.2 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
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 8.2 pKd = 8.2 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
ChEMBL 493 12 3 7 4.8 COc1ccc(CC(C)NCC(O)COc2ccc(-c3nc(-c4cccs4)c[nH]3)cc2)cc1OC 10.1021/jm00361a004
13621686 9739 0 None 575 2 Guinea pig 8.2 pKd = 8.2 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
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 8.2 pKd = 8.2 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
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
66653268 87809 0 None 426 3 Human 8.2 pKd = 8.2 Binding
Displacement of [3H]-CGP12177 from human beta1 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta1 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 8.2 pKd = 8.2 Binding
Displacement of [3H]-CGP12177 from human beta1 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta1 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
13157405 77596 0 None 141 2 Guinea pig 8.2 pKd = 8.2 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
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 8.2 pKd = 8.2 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
ChEMBL 355 8 3 5 3.3 O[C@@H](CNC1CC1)COc1ccc(-c2nc(-c3cccs3)c[nH]2)cc1 10.1021/jm00361a004
135817 167718 11 None - 1 Guinea pig 8.2 pKd = 8.2 Binding
Activity at beta-1 adrenergic receptorActivity at beta-1 adrenergic receptor
ChEMBL 391 13 2 5 3.2 CC(C)NCC(O)COc1ccc(OCCOCCc2ccc(F)cc2)cc1 10.1021/jm00103a004
CHEMBL43405 167718 11 None - 1 Guinea pig 8.2 pKd = 8.2 Binding
Activity at beta-1 adrenergic receptorActivity at beta-1 adrenergic receptor
ChEMBL 391 13 2 5 3.2 CC(C)NCC(O)COc1ccc(OCCOCCc2ccc(F)cc2)cc1 10.1021/jm00103a004
13157402 167772 0 None 398 2 Guinea pig 8.2 pKd = 8.2 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
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 8.2 pKd = 8.2 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
ChEMBL 355 8 3 5 3.3 OC(CNC1CC1)COc1ccc(-c2nc(-c3cccs3)c[nH]2)cc1 10.1021/jm00361a004
13621716 75580 0 None 165 2 Guinea pig 8.2 pKd = 8.2 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
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 8.2 pKd = 8.2 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
ChEMBL 387 11 3 6 3.2 CCOCCNC[C@H](O)COc1ccc(-c2nc(-c3cccs3)c[nH]2)cc1 10.1021/jm00156a028
56599101 87806 0 None 42 2 Human 8.2 pKd = 8.2 Binding
Displacement of [3H]-CGP12177 from human beta1 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta1 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 8.2 pKd = 8.2 Binding
Displacement of [3H]-CGP12177 from human beta1 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta1 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
10467512 99413 0 None -2 2 Guinea pig 8.2 pKd = 8.2 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor determined as pA2 in guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor determined as pA2 in guinea pig atria
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 8.2 pKd = 8.2 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor determined as pA2 in guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor determined as pA2 in guinea pig atria
ChEMBL 254 7 2 4 1.9 CC(C)(C)NCC(O)CON=C(C1CC1)C1CC1 10.1021/jm00145a008
13621772 9158 0 None 301 2 Guinea pig 8.2 pKd = 8.2 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
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 8.2 pKd = 8.2 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
ChEMBL 441 14 3 7 2.7 COc1ccc(CCNCC(O)COc2ccc(COCc3ncc[nH]3)cc2)cc1OC 10.1021/jm00156a028
12521588 60047 0 None 10 2 Guinea pig 7.2 pKd = 7.2 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
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 7.2 pKd = 7.2 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
ChEMBL 289 6 3 4 2.2 CC(C)(C)NCC(O)COc1ccc(-c2ncc[nH]2)cc1 10.1021/jm00361a004
13157410 127801 0 None 446 2 Guinea pig 7.2 pKd = 7.2 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
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 7.2 pKd = 7.2 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
ChEMBL 287 7 3 4 1.9 Cc1c[nH]c(-c2ccc(OCC(O)CNC3CC3)cc2)n1 10.1021/jm00361a004
12521605 165775 0 None 9 2 Guinea pig 7.2 pKd = 7.2 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
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 7.2 pKd = 7.2 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
ChEMBL 303 6 3 4 2.5 Cc1c[nH]c(-c2ccc(OCC(O)CNC(C)(C)C)cc2)n1 10.1021/jm00361a004
13621758 9676 0 None 3 2 Guinea pig 7.2 pKd = 7.2 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
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 7.2 pKd = 7.2 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
ChEMBL 317 7 3 4 2.4 Cc1c[nH]c(Cc2ccc(OCC(O)CNC(C)(C)C)cc2)n1 10.1021/jm00156a028
24208809 109937 34 None -5 2 Guinea pig 6.2 pKd = 6.2 Binding
Antagonist activity at beta1 adrenoceptor in guinea pig atrium assessed as inhibition of isoproterenol-induced response after 20 minsAntagonist activity at beta1 adrenoceptor in guinea pig atrium 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 6.2 pKd = 6.2 Binding
Antagonist activity at beta1 adrenoceptor in guinea pig atrium assessed as inhibition of isoproterenol-induced response after 20 minsAntagonist activity at beta1 adrenoceptor in guinea pig atrium 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
2834364 34910 19 None -1 3 Guinea pig 7.2 pKd = 7.2 Binding
Activity at beta-1 adrenergic receptorActivity at beta-1 adrenergic receptor
ChEMBL 237 7 2 3 2.0 CCc1ccc(OCC(O)CNC(C)C)cc1 10.1021/jm00103a004
CHEMBL143467 34910 19 None -1 3 Guinea pig 7.2 pKd = 7.2 Binding
Activity at beta-1 adrenergic receptorActivity at beta-1 adrenergic receptor
ChEMBL 237 7 2 3 2.0 CCc1ccc(OCC(O)CNC(C)C)cc1 10.1021/jm00103a004
2834364 34910 19 None -1 3 Rat 7.2 pKd = 7.2 Binding
Antagonist activity at beta1 adrenergic receptor in isolated rat atriaAntagonist activity at beta1 adrenergic receptor in isolated rat atria
ChEMBL 237 7 2 3 2.0 CCc1ccc(OCC(O)CNC(C)C)cc1 10.1021/jm00207a025
CHEMBL143467 34910 19 None -1 3 Rat 7.2 pKd = 7.2 Binding
Antagonist activity at beta1 adrenergic receptor in isolated rat atriaAntagonist activity at beta1 adrenergic receptor in isolated rat atria
ChEMBL 237 7 2 3 2.0 CCc1ccc(OCC(O)CNC(C)C)cc1 10.1021/jm00207a025
60903220 109939 2 None 1 2 Guinea pig 6.2 pKd = 6.2 Binding
Antagonist activity at beta1 adrenoceptor in guinea pig atrium assessed as inhibition of isoproterenol-induced response after 20 minsAntagonist activity at beta1 adrenoceptor in guinea pig atrium 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 6.2 pKd = 6.2 Binding
Antagonist activity at beta1 adrenoceptor in guinea pig atrium assessed as inhibition of isoproterenol-induced response after 20 minsAntagonist activity at beta1 adrenoceptor in guinea pig atrium 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
15578561 104367 0 None -1 2 Guinea pig 6.2 pKd = 6.2 Binding
In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.
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-1 adrenergic receptor in guinea pig right atria.In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.
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-1 adrenergic receptor in guinea pig right atria.In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.
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-1 adrenergic receptor in guinea pig right atria.In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.
ChEMBL 303 8 2 5 1.7 CCOC(=O)CNCC(O)COc1cccc2ccccc12 10.1021/jm00354a002
15578570 99410 0 None - 1 Guinea pig 5.2 pKd = 5.2 Binding
In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.
ChEMBL 329 8 2 5 3.0 CCOC(=O)c1cccc(NCC(O)COc2ccccc2C)c1 10.1021/jm00354a002
CHEMBL285958 99410 0 None - 1 Guinea pig 5.2 pKd = 5.2 Binding
In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.
ChEMBL 329 8 2 5 3.0 CCOC(=O)c1cccc(NCC(O)COc2ccccc2C)c1 10.1021/jm00354a002
2803 939 53 None -134 19 Guinea pig 4.2 pKd = 4.2 Binding
The compound was tested for beta-adrenergic activity against Beta-1 adrenergic receptor from guinea pig left atriaThe compound was tested for beta-adrenergic activity against Beta-1 adrenergic receptor from guinea pig left atria
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1021/jm00115a008
516 939 53 None -134 19 Guinea pig 4.2 pKd = 4.2 Binding
The compound was tested for beta-adrenergic activity against Beta-1 adrenergic receptor from guinea pig left atriaThe compound was tested for beta-adrenergic activity against Beta-1 adrenergic receptor from guinea pig left atria
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1021/jm00115a008
704 939 53 None -134 19 Guinea pig 4.2 pKd = 4.2 Binding
The compound was tested for beta-adrenergic activity against Beta-1 adrenergic receptor from guinea pig left atriaThe compound was tested for beta-adrenergic activity against Beta-1 adrenergic receptor from guinea pig left atria
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1021/jm00115a008
CHEMBL134 939 53 None -134 19 Guinea pig 4.2 pKd = 4.2 Binding
The compound was tested for beta-adrenergic activity against Beta-1 adrenergic receptor from guinea pig left atriaThe compound was tested for beta-adrenergic activity against Beta-1 adrenergic receptor from guinea pig left atria
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1021/jm00115a008
DB00575 939 53 None -134 19 Guinea pig 4.2 pKd = 4.2 Binding
The compound was tested for beta-adrenergic activity against Beta-1 adrenergic receptor from guinea pig left atriaThe compound was tested for beta-adrenergic activity against Beta-1 adrenergic receptor from guinea pig left atria
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1021/jm00115a008
13157369 59404 2 None - 1 Guinea pig 6.2 pKd = 6.2 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
ChEMBL 273 7 3 4 1.6 OC(CNC1CC1)COc1ccc(-c2ncc[nH]2)cc1 10.1021/jm00361a004
CHEMBL172431 59404 2 None - 1 Guinea pig 6.2 pKd = 6.2 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
ChEMBL 273 7 3 4 1.6 OC(CNC1CC1)COc1ccc(-c2ncc[nH]2)cc1 10.1021/jm00361a004
56597179 87827 0 None 501 2 Human 8.1 pKd = 8.1 Binding
Displacement of [3H]-CGP12177 from human beta1 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta1 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 8.1 pKd = 8.1 Binding
Displacement of [3H]-CGP12177 from human beta1 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta1 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
13621593 9185 0 None 204 2 Guinea pig 8.1 pKd = 8.1 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
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 8.1 pKd = 8.1 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
ChEMBL 509 11 3 6 4.1 COc1ccc(CCNCC(O)COc2ccc(-c3nc(Br)c[nH]3)cc2Cl)cc1OC 10.1021/jm00156a028
13621626 9427 0 None 741 2 Guinea pig 8.1 pKd = 8.1 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
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 8.1 pKd = 8.1 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
ChEMBL 445 11 3 6 3.6 COc1ccc(CCNCC(O)COc2ccc(-c3nc(C)c(Cl)[nH]3)cc2)cc1OC 10.1021/jm00156a028
54757126 65147 0 None -57 3 Human 7.1 pKd = 7.1 Binding
Displacement of [3H]-CGP 12177 from human beta-1 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-1 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 7.1 pKd = 7.1 Binding
Displacement of [3H]-CGP 12177 from human beta-1 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-1 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
56599229 87808 0 None 37 2 Human 7.1 pKd = 7.1 Binding
Displacement of [3H]-CGP12177 from human beta1 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta1 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 7.1 pKd = 7.1 Binding
Displacement of [3H]-CGP12177 from human beta1 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta1 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
56599230 87811 0 None 10 2 Human 7.1 pKd = 7.1 Binding
Displacement of [3H]-CGP12177 from human beta1 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta1 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 7.1 pKd = 7.1 Binding
Displacement of [3H]-CGP12177 from human beta1 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta1 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
15578577 171993 0 None 1 2 Guinea pig 7.1 pKd = 7.1 Binding
In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.
ChEMBL 303 8 2 5 1.7 COC(=O)CCNCC(O)COc1cccc2ccccc12 10.1021/jm00354a002
CHEMBL448775 171993 0 None 1 2 Guinea pig 7.1 pKd = 7.1 Binding
In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.
ChEMBL 303 8 2 5 1.7 COC(=O)CCNCC(O)COc1cccc2ccccc12 10.1021/jm00354a002
13040907 106582 0 None 19 2 Guinea pig 6.1 pKd = 6.1 Binding
Ability to block Beta-1 adrenergic receptor in guinea pig right atria preparationAbility to block Beta-1 adrenergic receptor in guinea pig right atria 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 6.1 pKd = 6.1 Binding
Ability to block Beta-1 adrenergic receptor in guinea pig right atria preparationAbility to block Beta-1 adrenergic receptor in guinea pig right atria preparation
ChEMBL 371 12 2 5 2.8 COC(=O)CCc1ccc(OCC(O)CNCCCc2ccccc2)cc1 10.1021/jm00354a003
59373811 109941 5 None 2 2 Guinea pig 6.1 pKd = 6.1 Binding
Antagonist activity at beta1 adrenoceptor in guinea pig atrium assessed as inhibition of isoproterenol-induced response after 20 minsAntagonist activity at beta1 adrenoceptor in guinea pig atrium 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 6.1 pKd = 6.1 Binding
Antagonist activity at beta1 adrenoceptor in guinea pig atrium assessed as inhibition of isoproterenol-induced response after 20 minsAntagonist activity at beta1 adrenoceptor in guinea pig atrium 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
44279490 104156 0 None 1 2 Guinea pig 6.1 pKd = 6.1 Binding
The compound was tested in vitro for its ability to block Beta-1 adrenergic receptor in guinea pig right atriaThe compound was tested in vitro for its ability to block Beta-1 adrenergic receptor in guinea pig right atria
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 6.1 pKd = 6.1 Binding
The compound was tested in vitro for its ability to block Beta-1 adrenergic receptor in guinea pig right atriaThe compound was tested in vitro for its ability to block Beta-1 adrenergic receptor in guinea pig right atria
ChEMBL 297 9 2 5 1.8 CCOC(=O)CCNCC(O)COC1=CC=CCC1(C)C 10.1021/jm00354a002
15578569 110035 0 None - 1 Guinea pig 5.1 pKd = 5.1 Binding
In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.
ChEMBL 329 8 2 5 3.0 CCOC(=O)c1ccc(NCC(O)COc2ccccc2C)cc1 10.1021/jm00354a002
CHEMBL32514 110035 0 None - 1 Guinea pig 5.1 pKd = 5.1 Binding
In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.In vitro ability to block beta-1 adrenergic receptor in guinea pig right atria.
ChEMBL 329 8 2 5 3.0 CCOC(=O)c1ccc(NCC(O)COc2ccccc2C)cc1 10.1021/jm00354a002
9576814 59095 4 None 2 2 Guinea pig 8.1 pKd = 8.1 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor determined as pA2 in guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor determined as pA2 in guinea pig atria
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 8.1 pKd = 8.1 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor determined as pA2 in guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor determined as pA2 in guinea pig atria
ChEMBL 228 6 2 4 1.5 C/C(=N\OC[C@H](O)CNC(C)(C)C)C1CC1 10.1021/jm00145a008
21595419 101632 0 None 1 2 Guinea pig 8.1 pKd = 8.1 Binding
Beta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atriumBeta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atrium
ChEMBL 271 4 2 3 2.7 O[C@H](COc1ccc2ccccc2c1)[C@@H]1CCCCN1 10.1021/jm00119a011
CHEMBL302339 101632 0 None 1 2 Guinea pig 8.1 pKd = 8.1 Binding
Beta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atriumBeta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atrium
ChEMBL 271 4 2 3 2.7 O[C@H](COc1ccc2ccccc2c1)[C@@H]1CCCCN1 10.1021/jm00119a011
14201547 201862 0 None -2 2 Guinea pig 7.1 pKd = 7.1 Binding
Beta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atriumBeta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atrium
ChEMBL 235 5 2 3 1.7 O[C@H](COCc1ccccc1)[C@H]1CCCCN1 10.1021/jm00119a011
CHEMBL66702 201862 0 None -2 2 Guinea pig 7.1 pKd = 7.1 Binding
Beta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atriumBeta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atrium
ChEMBL 235 5 2 3 1.7 O[C@H](COCc1ccccc1)[C@H]1CCCCN1 10.1021/jm00119a011
44274623 96355 3 None 7 2 Guinea pig 7.1 pKd = 7.1 Binding
Beta-1 adrenergic receptor blocking activity in atria of guinea pig.Beta-1 adrenergic receptor blocking activity in atria 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 7.1 pKd = 7.1 Binding
Beta-1 adrenergic receptor blocking activity in atria of guinea pig.Beta-1 adrenergic receptor blocking activity in atria of guinea pig.
ChEMBL 201 6 2 3 1.2 CC(C)(C)NCC(O)COCC1CC1 10.1021/jm00376a011
155774 4021 33 None 5 3 Human 7.1 pKd = 7.1 Binding
Displacement of [3H]-CGP12177 from human beta1 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta1 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 7.1 pKd = 7.1 Binding
Displacement of [3H]-CGP12177 from human beta1 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta1 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 7.1 pKd = 7.1 Binding
Displacement of [3H]-CGP12177 from human beta1 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta1 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 7.1 pKd = 7.1 Binding
Displacement of [3H]-CGP12177 from human beta1 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta1 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 7.1 pKd = 7.1 Binding
Displacement of [3H]-CGP12177 from human beta1 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta1 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
44459541 95684 0 None -1 2 Guinea pig 7.1 pKd = 7.1 Binding
Beta-1 adrenergic receptor blocking activity in atria of guinea pig.Beta-1 adrenergic receptor blocking activity in atria 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 7.1 pKd = 7.1 Binding
Beta-1 adrenergic receptor blocking activity in atria of guinea pig.Beta-1 adrenergic receptor blocking activity in atria of guinea pig.
ChEMBL 242 7 2 4 1.9 C/C(CC1CC1)=N/OCC(O)CNC(C)(C)C 10.1021/jm00376a011
12484287 109215 0 None -2 2 Guinea pig 6.1 pKd = 6.1 Binding
Competitive antagonist activity at beta-1 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced atrial contractile forceCompetitive antagonist activity at beta-1 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced atrial contractile force
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 6.1 pKd = 6.1 Binding
Competitive antagonist activity at beta-1 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced atrial contractile forceCompetitive antagonist activity at beta-1 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced atrial contractile force
ChEMBL 249 6 3 4 1.3 CC(C)NCC(O)COc1ccc2[nH]cnc2c1 10.1021/jm00188a019
54758320 65172 0 None -13 3 Human 6.1 pKd = 6.1 Binding
Displacement of [3H]-CGP 12177 from human beta-1 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-1 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 -13 3 Human 6.1 pKd = 6.1 Binding
Displacement of [3H]-CGP 12177 from human beta-1 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-1 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
54756929 65143 0 None -50 3 Human 7.1 pKd = 7.1 Binding
Displacement of [3H]-CGP 12177 from human beta-1 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-1 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 -50 3 Human 7.1 pKd = 7.1 Binding
Displacement of [3H]-CGP 12177 from human beta-1 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-1 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
5311116 2293 6 None 54 3 Human 8.0 pKd = 8.0 Binding
Displacement of [3H]-CGP12177 from human beta1 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta1 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 54 3 Human 8.0 pKd = 8.0 Binding
Displacement of [3H]-CGP12177 from human beta1 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta1 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 54 3 Human 8.0 pKd = 8.0 Binding
Displacement of [3H]-CGP12177 from human beta1 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta1 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
56599098 87821 0 None 95 2 Human 8.0 pKd = 8.0 Binding
Displacement of [3H]-CGP12177 from human beta1 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta1 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 8.0 pKd = 8.0 Binding
Displacement of [3H]-CGP12177 from human beta1 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta1 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
13157382 61916 0 None 3981 2 Guinea pig 8.0 pKd = 8.0 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
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 8.0 pKd = 8.0 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
ChEMBL 507 12 3 7 5.2 COc1ccc(CC(C)(C)NCC(O)COc2ccc(-c3nc(-c4cccs4)c[nH]3)cc2)cc1OC 10.1021/jm00361a004
165193 3126 60 None -7 43 Guinea pig 8.0 pKd = 8.0 Binding
Competitive antagonist activity at beta-1 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced atrial beat rateCompetitive antagonist activity at beta-1 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced atrial beat rate
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00188a019
2303 3126 60 None -7 43 Guinea pig 8.0 pKd = 8.0 Binding
Competitive antagonist activity at beta-1 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced atrial beat rateCompetitive antagonist activity at beta-1 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced atrial beat rate
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00188a019
4946 3126 60 None -7 43 Guinea pig 8.0 pKd = 8.0 Binding
Competitive antagonist activity at beta-1 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced atrial beat rateCompetitive antagonist activity at beta-1 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced atrial beat rate
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00188a019
564 3126 60 None -7 43 Guinea pig 8.0 pKd = 8.0 Binding
Competitive antagonist activity at beta-1 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced atrial beat rateCompetitive antagonist activity at beta-1 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced atrial beat rate
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00188a019
62882 3126 60 None -7 43 Guinea pig 8.0 pKd = 8.0 Binding
Competitive antagonist activity at beta-1 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced atrial beat rateCompetitive antagonist activity at beta-1 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced atrial beat rate
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00188a019
63 3126 60 None -7 43 Guinea pig 8.0 pKd = 8.0 Binding
Competitive antagonist activity at beta-1 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced atrial beat rateCompetitive antagonist activity at beta-1 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced atrial beat rate
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00188a019
66366 3126 60 None -7 43 Guinea pig 8.0 pKd = 8.0 Binding
Competitive antagonist activity at beta-1 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced atrial beat rateCompetitive antagonist activity at beta-1 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced atrial beat rate
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00188a019
91536 3126 60 None -7 43 Guinea pig 8.0 pKd = 8.0 Binding
Competitive antagonist activity at beta-1 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced atrial beat rateCompetitive antagonist activity at beta-1 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced atrial beat rate
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00188a019
CHEMBL27 3126 60 None -7 43 Guinea pig 8.0 pKd = 8.0 Binding
Competitive antagonist activity at beta-1 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced atrial beat rateCompetitive antagonist activity at beta-1 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced atrial beat rate
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00188a019
CHEMBL452861 3126 60 None -7 43 Guinea pig 8.0 pKd = 8.0 Binding
Competitive antagonist activity at beta-1 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced atrial beat rateCompetitive antagonist activity at beta-1 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced atrial beat rate
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00188a019
DB00571 3126 60 None -7 43 Guinea pig 8.0 pKd = 8.0 Binding
Competitive antagonist activity at beta-1 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced atrial beat rateCompetitive antagonist activity at beta-1 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced atrial beat rate
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00188a019
44459890 99534 0 None 8 2 Guinea pig 8.0 pKd = 8.0 Binding
Beta-1 adrenergic receptor blocking activity in atria of guinea pig.Beta-1 adrenergic receptor blocking activity in atria 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 8.0 pKd = 8.0 Binding
Beta-1 adrenergic receptor blocking activity in atria of guinea pig.Beta-1 adrenergic receptor blocking activity in atria of guinea pig.
ChEMBL 214 6 2 4 1.1 CC(C)(C)NCC(O)CO/N=C\C1CC1 10.1021/jm00376a011
54757129 65148 0 None -29 3 Human 7.0 pKd = 7.0 Binding
Displacement of [3H]-CGP 12177 from human beta-1 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-1 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 -29 3 Human 7.0 pKd = 7.0 Binding
Displacement of [3H]-CGP 12177 from human beta-1 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-1 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
56598833 87825 0 None - 1 Human 7.0 pKd = 7.0 Binding
Displacement of [3H]-CGP12177 from human beta1 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta1 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 433 14 5 7 2.0 CCOCCOc1ccc(OCC(O)CNCCNC(=O)Nc2ccc(O)cc2)cc1 10.1021/jm400348g
CHEMBL2348217 87825 0 None - 1 Human 7.0 pKd = 7.0 Binding
Displacement of [3H]-CGP12177 from human beta1 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta1 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
ChEMBL 433 14 5 7 2.0 CCOCCOc1ccc(OCC(O)CNCCNC(=O)Nc2ccc(O)cc2)cc1 10.1021/jm400348g
13621725 9416 0 None - 1 Guinea pig 7.0 pKd = 7.0 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
ChEMBL 389 12 5 5 1.8 CCCCNC(=O)NCCNCC(O)COc1ccc(-c2nc(C)c[nH]2)cc1 10.1021/jm00156a028
CHEMBL11219 9416 0 None - 1 Guinea pig 7.0 pKd = 7.0 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria
ChEMBL 389 12 5 5 1.8 CCCCNC(=O)NCCNCC(O)COc1ccc(-c2nc(C)c[nH]2)cc1 10.1021/jm00156a028
21595421 162904 0 None -28 2 Guinea pig 7.0 pKd = 7.0 Binding
Beta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atriumBeta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atrium
ChEMBL 235 4 2 3 1.9 Cc1cccc(OC[C@@H](O)[C@@H]2CCCCN2)c1 10.1021/jm00119a011
CHEMBL419994 162904 0 None -28 2 Guinea pig 7.0 pKd = 7.0 Binding
Beta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atriumBeta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atrium
ChEMBL 235 4 2 3 1.9 Cc1cccc(OC[C@@H](O)[C@@H]2CCCCN2)c1 10.1021/jm00119a011
56599100 87823 0 None 12 2 Human 7.0 pKd = 7.0 Binding
Displacement of [3H]-CGP12177 from human beta1 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta1 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 7.0 pKd = 7.0 Binding
Displacement of [3H]-CGP12177 from human beta1 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]-CGP12177 from human beta1 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
6917762 9219 7 None -1 2 Guinea pig 7.0 pKd = 7.0 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor determined as pA2 in guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor determined as pA2 in guinea pig atria
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 7.0 pKd = 7.0 Binding
In vitro inhibitory activity against beta-1 adrenergic receptor determined as pA2 in guinea pig atriaIn vitro inhibitory activity against beta-1 adrenergic receptor determined as pA2 in guinea pig atria
ChEMBL 228 6 2 4 1.5 C/C(=N\OCC(O)CNC(C)(C)C)C1CC1 10.1021/jm00145a008
54758415 65173 0 None -6 3 Human 7.0 pKd = 7.0 Binding
Displacement of [3H]-CGP 12177 from human beta-1 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-1 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 7.0 pKd = 7.0 Binding
Displacement of [3H]-CGP 12177 from human beta-1 adrenergic receptor expressed in CHOK1 cellsDisplacement of [3H]-CGP 12177 from human beta-1 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
20986823 156302 7 None -4 2 Human 4.0 pKd = 4.0 Binding
Displacement of [3H](-)CGP12177 from human beta1-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting methodDisplacement of [3H](-)CGP12177 from human beta1-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 4.0 pKd = 4.0 Binding
Displacement of [3H](-)CGP12177 from human beta1-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting methodDisplacement of [3H](-)CGP12177 from human beta1-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
9849699 72902 9 None -1 2 Human 10.6 pKi = 10.6 Binding
Displacement of [125I]Iodocyanopindolol from human adrenergic beta1 receptor expressed in insect sf9 cells by scintillation countingDisplacement of [125I]Iodocyanopindolol from human adrenergic beta1 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 10.6 pKi = 10.6 Binding
Displacement of [125I]Iodocyanopindolol from human adrenergic beta1 receptor expressed in insect sf9 cells by scintillation countingDisplacement of [125I]Iodocyanopindolol from human adrenergic beta1 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 10.6 pKi = 10.6 Binding
Displacement of [125I]Iodocyanopindolol from human adrenergic beta1 receptor expressed in insect sf9 cells by scintillation countingDisplacement of [125I]Iodocyanopindolol from human adrenergic beta1 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 10.6 pKi = 10.6 Binding
Displacement of [125I]Iodocyanopindolol from human adrenergic beta1 receptor expressed in insect sf9 cells by scintillation countingDisplacement of [125I]Iodocyanopindolol from human adrenergic beta1 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
487 779 65 None -4 6 Mouse 10.1 pKi = 10.1 Binding
Displacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T 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 Mouse 10.1 pKi = 10.1 Binding
Displacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T 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 Mouse 10.1 pKi = 10.1 Binding
Displacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T 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 Mouse 10.1 pKi = 10.1 Binding
Displacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T 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
46889772 6902 0 None 79 3 Human 10.0 pKi = 10 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta-1 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta-1 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 10.0 pKi = 10 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta-1 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta-1 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
2585 788 100 None -1 22 Human 10.0 pKi = 10.0 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
522 788 100 None -1 22 Human 10.0 pKi = 10.0 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
551 788 100 None -1 22 Human 10.0 pKi = 10.0 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
CHEMBL723 788 100 None -1 22 Human 10.0 pKi = 10.0 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
DB01136 788 100 None -1 22 Human 10.0 pKi = 10.0 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
185395 139303 37 None -6 3 Mouse 9.7 pKi = 9.7 Binding
Displacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T 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 Mouse 9.7 pKi = 9.7 Binding
Displacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T 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
6603756 122376 3 None -2 2 Human 9.6 pKi = 9.6 Binding
Inhibition of I-iodocyanopindolol binding to human beta 1 adrenergic receptorsInhibition of I-iodocyanopindolol binding to human beta 1 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 9.6 pKi = 9.6 Binding
Inhibition of I-iodocyanopindolol binding to human beta 1 adrenergic receptorsInhibition of I-iodocyanopindolol binding to human beta 1 adrenergic receptors
ChEMBL 279 5 4 5 1.4 CC(C)(C)NC[C@H](O)COc1cccc2[nH]c(O)nc12 10.1021/jm000544b
127 3066 45 None 2 15 Human 9.4 pKi = 9.4 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 248 6 3 3 1.9 O[C@H](COc1cccc2c1cc[nH]2)CNC(C)C nan
688095 3066 45 None 2 15 Human 9.4 pKi = 9.4 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 248 6 3 3 1.9 O[C@H](COc1cccc2c1cc[nH]2)CNC(C)C nan
CHEMBL117405 3066 45 None 2 15 Human 9.4 pKi = 9.4 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 248 6 3 3 1.9 O[C@H](COc1cccc2c1cc[nH]2)CNC(C)C nan
155548437 173189 0 None -3 2 Mouse 9.3 pKi = 9.3 Binding
Displacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T 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 Mouse 9.3 pKi = 9.3 Binding
Displacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranes
ChEMBL 502 16 3 8 4.1 COc1cc(CCNC[C@H](O)COc2cccc3ccccc23)ccc1OCCSSCCN 10.1016/j.bmc.2019.05.034
2176 3065 66 None -4 27 Human 9.3 pKi = 9.3 Binding
Binding affinity at human adrenergic beta-1 receptorBinding affinity at human adrenergic beta-1 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 -4 27 Human 9.3 pKi = 9.3 Binding
Binding affinity at human adrenergic beta-1 receptorBinding affinity at human adrenergic beta-1 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 -4 27 Human 9.3 pKi = 9.3 Binding
Binding affinity at human adrenergic beta-1 receptorBinding affinity at human adrenergic beta-1 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 -4 27 Human 9.3 pKi = 9.3 Binding
Binding affinity at human adrenergic beta-1 receptorBinding affinity at human adrenergic beta-1 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 -4 27 Human 9.3 pKi = 9.3 Binding
Binding affinity at human adrenergic beta-1 receptorBinding affinity at human adrenergic beta-1 receptor
ChEMBL 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C 10.1016/j.bmcl.2007.07.086
2176 3065 66 None -4 27 Human 9.3 pKi = 9.3 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C nan
4828 3065 66 None -4 27 Human 9.3 pKi = 9.3 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C nan
91 3065 66 None -4 27 Human 9.3 pKi = 9.3 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C nan
CHEMBL500 3065 66 None -4 27 Human 9.3 pKi = 9.3 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C nan
DB00960 3065 66 None -4 27 Human 9.3 pKi = 9.3 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C nan
118710940 113238 0 None -1 3 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 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 9.1 pKi = 9.1 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 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
2585 788 100 None -4 22 Rat 9.1 pKi = 9.1 Binding
Displacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation methodDisplacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation method
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1016/j.ejmech.2008.05.019
522 788 100 None -4 22 Rat 9.1 pKi = 9.1 Binding
Displacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation methodDisplacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation method
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1016/j.ejmech.2008.05.019
551 788 100 None -4 22 Rat 9.1 pKi = 9.1 Binding
Displacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation methodDisplacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation method
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1016/j.ejmech.2008.05.019
CHEMBL723 788 100 None -4 22 Rat 9.1 pKi = 9.1 Binding
Displacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation methodDisplacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation method
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1016/j.ejmech.2008.05.019
DB01136 788 100 None -4 22 Rat 9.1 pKi = 9.1 Binding
Displacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation methodDisplacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation method
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1016/j.ejmech.2008.05.019
49864395 15446 0 None -1 2 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 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 9.1 pKi = 9.1 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 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
46889812 6363 0 None -10 3 Human 9.0 pKi = 9 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta-1 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta-1 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 9.0 pKi = 9 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta-1 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta-1 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
155525244 170418 0 None -15 2 Mouse 9.0 pKi = 9.0 Binding
Displacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T 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 Mouse 9.0 pKi = 9.0 Binding
Displacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranes
ChEMBL 516 17 3 8 4.5 COc1cc(CCNC[C@H](O)COc2cccc3ccccc23)ccc1OCCCSSCCN 10.1016/j.bmc.2019.05.034
165193 3126 60 None -2 43 Human 9.0 pKi = 9.0 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
2303 3126 60 None -2 43 Human 9.0 pKi = 9.0 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
4946 3126 60 None -2 43 Human 9.0 pKi = 9.0 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
564 3126 60 None -2 43 Human 9.0 pKi = 9.0 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
62882 3126 60 None -2 43 Human 9.0 pKi = 9.0 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
63 3126 60 None -2 43 Human 9.0 pKi = 9.0 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
66366 3126 60 None -2 43 Human 9.0 pKi = 9.0 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
91536 3126 60 None -2 43 Human 9.0 pKi = 9.0 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
CHEMBL27 3126 60 None -2 43 Human 9.0 pKi = 9.0 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
CHEMBL452861 3126 60 None -2 43 Human 9.0 pKi = 9.0 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
DB00571 3126 60 None -2 43 Human 9.0 pKi = 9.0 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
2685 875 15 None -1 7 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]CGP12177 from human beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from human beta1 adrenoceptor expressed in HEK293T 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 -1 7 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]CGP12177 from human beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from human beta1 adrenoceptor expressed in HEK293T 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 -1 7 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]CGP12177 from human beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from human beta1 adrenoceptor expressed in HEK293T 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
165193 3126 60 None -2 43 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]Cynopindolol from human recombinant beta1 adrenergic receptor expressed in CHOK1 cells after 2 hrsDisplacement of [125I]Cynopindolol from human recombinant beta1 adrenergic receptor expressed in CHOK1 cells after 2 hrs
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmcl.2013.01.025
2303 3126 60 None -2 43 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]Cynopindolol from human recombinant beta1 adrenergic receptor expressed in CHOK1 cells after 2 hrsDisplacement of [125I]Cynopindolol from human recombinant beta1 adrenergic receptor expressed in CHOK1 cells after 2 hrs
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmcl.2013.01.025
4946 3126 60 None -2 43 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]Cynopindolol from human recombinant beta1 adrenergic receptor expressed in CHOK1 cells after 2 hrsDisplacement of [125I]Cynopindolol from human recombinant beta1 adrenergic receptor expressed in CHOK1 cells after 2 hrs
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmcl.2013.01.025
564 3126 60 None -2 43 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]Cynopindolol from human recombinant beta1 adrenergic receptor expressed in CHOK1 cells after 2 hrsDisplacement of [125I]Cynopindolol from human recombinant beta1 adrenergic receptor expressed in CHOK1 cells after 2 hrs
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmcl.2013.01.025
62882 3126 60 None -2 43 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]Cynopindolol from human recombinant beta1 adrenergic receptor expressed in CHOK1 cells after 2 hrsDisplacement of [125I]Cynopindolol from human recombinant beta1 adrenergic receptor expressed in CHOK1 cells after 2 hrs
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmcl.2013.01.025
63 3126 60 None -2 43 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]Cynopindolol from human recombinant beta1 adrenergic receptor expressed in CHOK1 cells after 2 hrsDisplacement of [125I]Cynopindolol from human recombinant beta1 adrenergic receptor expressed in CHOK1 cells after 2 hrs
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmcl.2013.01.025
66366 3126 60 None -2 43 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]Cynopindolol from human recombinant beta1 adrenergic receptor expressed in CHOK1 cells after 2 hrsDisplacement of [125I]Cynopindolol from human recombinant beta1 adrenergic receptor expressed in CHOK1 cells after 2 hrs
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmcl.2013.01.025
91536 3126 60 None -2 43 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]Cynopindolol from human recombinant beta1 adrenergic receptor expressed in CHOK1 cells after 2 hrsDisplacement of [125I]Cynopindolol from human recombinant beta1 adrenergic receptor expressed in CHOK1 cells after 2 hrs
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmcl.2013.01.025
CHEMBL27 3126 60 None -2 43 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]Cynopindolol from human recombinant beta1 adrenergic receptor expressed in CHOK1 cells after 2 hrsDisplacement of [125I]Cynopindolol from human recombinant beta1 adrenergic receptor expressed in CHOK1 cells after 2 hrs
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmcl.2013.01.025
CHEMBL452861 3126 60 None -2 43 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]Cynopindolol from human recombinant beta1 adrenergic receptor expressed in CHOK1 cells after 2 hrsDisplacement of [125I]Cynopindolol from human recombinant beta1 adrenergic receptor expressed in CHOK1 cells after 2 hrs
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmcl.2013.01.025
DB00571 3126 60 None -2 43 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]Cynopindolol from human recombinant beta1 adrenergic receptor expressed in CHOK1 cells after 2 hrsDisplacement of [125I]Cynopindolol from human recombinant beta1 adrenergic receptor expressed in CHOK1 cells after 2 hrs
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmcl.2013.01.025
49864380 15442 0 None 1 2 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 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 8.9 pKi = 8.9 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 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
165193 3126 60 None -2 43 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]CGP12177 from human beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from human beta1 adrenoceptor expressed in HEK293T 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 -2 43 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]CGP12177 from human beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from human beta1 adrenoceptor expressed in HEK293T 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 -2 43 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]CGP12177 from human beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from human beta1 adrenoceptor expressed in HEK293T 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 -2 43 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]CGP12177 from human beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from human beta1 adrenoceptor expressed in HEK293T 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 -2 43 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]CGP12177 from human beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from human beta1 adrenoceptor expressed in HEK293T 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 -2 43 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]CGP12177 from human beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from human beta1 adrenoceptor expressed in HEK293T 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 -2 43 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]CGP12177 from human beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from human beta1 adrenoceptor expressed in HEK293T 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 -2 43 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]CGP12177 from human beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from human beta1 adrenoceptor expressed in HEK293T 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 -2 43 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]CGP12177 from human beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from human beta1 adrenoceptor expressed in HEK293T 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 -2 43 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]CGP12177 from human beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from human beta1 adrenoceptor expressed in HEK293T 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 -2 43 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]CGP12177 from human beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from human beta1 adrenoceptor expressed in HEK293T cell membranes
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmc.2019.05.034
2685 875 15 None 1 7 Mouse 8.9 pKi = 8.9 Binding
Displacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T 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 1 7 Mouse 8.9 pKi = 8.9 Binding
Displacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T 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 1 7 Mouse 8.9 pKi = 8.9 Binding
Displacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T 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
10075766 99943 0 None - 1 Human 8.9 pKi = 8.9 Binding
Inhibition of [3H]dihydroalprenolol binding to beta 1 adrenoceptor from turkey erythrocyte membranes.Inhibition of [3H]dihydroalprenolol binding to beta 1 adrenoceptor from turkey erythrocyte membranes.
ChEMBL 532 11 5 8 0.2 NS(=O)(=O)c1cc(S(=O)(=O)NCCNCC(O)COc2cccc3c2CCC(=O)N3)ccc1Cl 10.1021/jm00053a020
CHEMBL290313 99943 0 None - 1 Human 8.9 pKi = 8.9 Binding
Inhibition of [3H]dihydroalprenolol binding to beta 1 adrenoceptor from turkey erythrocyte membranes.Inhibition of [3H]dihydroalprenolol binding to beta 1 adrenoceptor from turkey erythrocyte membranes.
ChEMBL 532 11 5 8 0.2 NS(=O)(=O)c1cc(S(=O)(=O)NCCNCC(O)COc2cccc3c2CCC(=O)N3)ccc1Cl 10.1021/jm00053a020
165193 3126 60 None -2 43 Human 8.8 pKi = 8.8 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
2303 3126 60 None -2 43 Human 8.8 pKi = 8.8 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
4946 3126 60 None -2 43 Human 8.8 pKi = 8.8 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
564 3126 60 None -2 43 Human 8.8 pKi = 8.8 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
62882 3126 60 None -2 43 Human 8.8 pKi = 8.8 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
63 3126 60 None -2 43 Human 8.8 pKi = 8.8 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
66366 3126 60 None -2 43 Human 8.8 pKi = 8.8 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
91536 3126 60 None -2 43 Human 8.8 pKi = 8.8 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
CHEMBL27 3126 60 None -2 43 Human 8.8 pKi = 8.8 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
CHEMBL452861 3126 60 None -2 43 Human 8.8 pKi = 8.8 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
DB00571 3126 60 None -2 43 Human 8.8 pKi = 8.8 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C nan
49864333 15422 0 None -1 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 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 8.8 pKi = 8.8 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 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
33624 3749 29 None -7 9 Human 8.8 pKi = 8.8 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C nan
4061 3749 29 None -7 9 Human 8.8 pKi = 8.8 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C nan
565 3749 29 None -7 9 Human 8.8 pKi = 8.8 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C nan
CHEMBL499 3749 29 None -7 9 Human 8.8 pKi = 8.8 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C nan
DB00373 3749 29 None -7 9 Human 8.8 pKi = 8.8 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C nan
49864460 15460 0 None 1 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 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 8.8 pKi = 8.8 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 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
11617407 15433 0 None -4 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 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 8.7 pKi = 8.7 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 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
11625619 77251 0 None -4 2 Human 8.7 pKi = 8.7 Binding
Binding affinity to human beta1-adrenoceptor by radioligand binding assayBinding affinity to human beta1-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 8.7 pKi = 8.7 Binding
Binding affinity to human beta1-adrenoceptor by radioligand binding assayBinding affinity to human beta1-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
2583 204168 46 None 2 2 Human 8.7 pKi = 8.7 Binding
Inhibition of [3H]dihydroalprenolol binding to beta 1 adrenoceptor from turkey erythrocyte membranes.Inhibition of [3H]dihydroalprenolol binding to beta 1 adrenoceptor from turkey erythrocyte membranes.
ChEMBL 292 5 3 4 1.7 CC(C)(C)NCC(O)COc1cccc2c1CCC(=O)N2 10.1021/jm00053a020
CHEMBL839 204168 46 None 2 2 Human 8.7 pKi = 8.7 Binding
Inhibition of [3H]dihydroalprenolol binding to beta 1 adrenoceptor from turkey erythrocyte membranes.Inhibition of [3H]dihydroalprenolol binding to beta 1 adrenoceptor from turkey erythrocyte membranes.
ChEMBL 292 5 3 4 1.7 CC(C)(C)NCC(O)COc1cccc2c1CCC(=O)N2 10.1021/jm00053a020
145947665 167110 0 None 10 2 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]-CGP-12177 from adrenergic beta1 receptor in Wistar rat cortex incubated for 60 mins by microbeta liquid scintillation counting analysisDisplacement of [3H]-CGP-12177 from adrenergic beta1 receptor in Wistar rat cortex incubated for 60 mins by microbeta liquid scintillation counting analysis
ChEMBL 405 8 2 6 3.5 COc1ccccc1CNCC(O)COc1cccc2c(=O)c3ccccc3oc12 10.1016/j.bmc.2018.04.038
CHEMBL4128794 167110 0 None 10 2 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]-CGP-12177 from adrenergic beta1 receptor in Wistar rat cortex incubated for 60 mins by microbeta liquid scintillation counting analysisDisplacement of [3H]-CGP-12177 from adrenergic beta1 receptor in Wistar rat cortex incubated for 60 mins by microbeta liquid scintillation counting analysis
ChEMBL 405 8 2 6 3.5 COc1ccccc1CNCC(O)COc1cccc2c(=O)c3ccccc3oc12 10.1016/j.bmc.2018.04.038
CHEMBL4302144 167110 0 None 10 2 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]-CGP-12177 from adrenergic beta1 receptor in Wistar rat cortex incubated for 60 mins by microbeta liquid scintillation counting analysisDisplacement of [3H]-CGP-12177 from adrenergic beta1 receptor in Wistar rat cortex incubated for 60 mins by microbeta liquid scintillation counting analysis
ChEMBL 405 8 2 6 3.5 COc1ccccc1CNCC(O)COc1cccc2c(=O)c3ccccc3oc12 10.1016/j.bmc.2018.04.038
52948805 17558 0 None -10 3 Human 7.0 pKi = 7 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta-1 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 -10 3 Human 7.0 pKi = 7 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta-1 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
10132882 94060 0 None 1 2 Human 7.0 pKi = 7 Binding
Displacement of [125I]iodocyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human adrenergic beta-1 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 7.0 pKi = 7 Binding
Displacement of [125I]iodocyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human adrenergic beta-1 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
10201549 94061 1 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]iodocyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human adrenergic beta-1 receptor expressed in CHO cells
ChEMBL 409 8 2 6 3.9 O[C@@H](CNCCOc1ccc(-c2csc(C(F)(F)F)n2)cc1)c1cccnc1 10.1016/j.bmcl.2007.06.072
CHEMBL251600 94061 1 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]iodocyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human adrenergic beta-1 receptor expressed in CHO cells
ChEMBL 409 8 2 6 3.9 O[C@@H](CNCCOc1ccc(-c2csc(C(F)(F)F)n2)cc1)c1cccnc1 10.1016/j.bmcl.2007.06.072
155519891 169814 0 None -3 6 Human 6.0 pKi = 6 Binding
Displacement of [125I]-pindolol from human recombinant adrenergic Beta1 receptor expressed in Flp-In CHO cells after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-pindolol from human recombinant adrenergic Beta1 receptor expressed in Flp-In CHO 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 -3 6 Human 6.0 pKi = 6 Binding
Displacement of [125I]-pindolol from human recombinant adrenergic Beta1 receptor expressed in Flp-In CHO cells after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-pindolol from human recombinant adrenergic Beta1 receptor expressed in Flp-In CHO 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
3687256 6741 6 None -12 3 Human 6.0 pKi = 6 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta-1 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta-1 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 -12 3 Human 6.0 pKi = 6 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta-1 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta-1 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
44444185 154208 0 None -112 3 Human 6.0 pKi = 6 Binding
Displacement of [125I]iodocyanopindolol from human cloned adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human cloned adrenergic beta-1 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 -112 3 Human 6.0 pKi = 6 Binding
Displacement of [125I]iodocyanopindolol from human cloned adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human cloned adrenergic beta-1 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
681 1432 65 None -44 39 Rat 5.0 pKi = 5 Binding
Binding of [3H]dihydroalprenolol to beta-1 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-1 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 -44 39 Rat 5.0 pKi = 5 Binding
Binding of [3H]dihydroalprenolol to beta-1 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-1 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 -44 39 Rat 5.0 pKi = 5 Binding
Binding of [3H]dihydroalprenolol to beta-1 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-1 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 -44 39 Rat 5.0 pKi = 5 Binding
Binding of [3H]dihydroalprenolol to beta-1 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-1 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 -44 39 Rat 5.0 pKi = 5 Binding
Binding of [3H]dihydroalprenolol to beta-1 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-1 adrenergic receptor of rat cerebral cortical membranes
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm990599h
9892481 69875 11 None -3162 2 Human 5.0 pKi = 5 Binding
Displacement of [3H]dihydroalprenolol from beta1 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta1 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 5.0 pKi = 5 Binding
Displacement of [3H]dihydroalprenolol from beta1 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta1 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
59119466 111763 0 None -39 2 Human 5.0 pKi = 5 Binding
Displacement of [3H]dihydroalprenolol from beta1 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta1 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 5.0 pKi = 5 Binding
Displacement of [3H]dihydroalprenolol from beta1 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta1 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
2247 502 77 None -128 42 Human 5.0 pKi = 5 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
249 502 77 None -128 42 Human 5.0 pKi = 5 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
2603 502 77 None -128 42 Human 5.0 pKi = 5 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
CHEMBL296419 502 77 None -128 42 Human 5.0 pKi = 5 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
DB00637 502 77 None -128 42 Human 5.0 pKi = 5 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
16735274 159476 0 None -1 2 Rat 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 Rat 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
1786 2474 79 None -1 11 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O nan
4171 2474 79 None -1 11 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O nan
553 2474 79 None -1 11 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O nan
CHEMBL13 2474 79 None -1 11 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O nan
DB00264 2474 79 None -1 11 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O nan
44424578 165482 0 None -1 2 Rat 5.0 pKi = 5.0 Binding
Displacement of [3H]CGP-12177 from beta-1 adrenergic receptor in Sprague-Dawley rat cortical membraneDisplacement of [3H]CGP-12177 from beta-1 adrenergic receptor in Sprague-Dawley rat cortical membrane
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 Rat 5.0 pKi = 5.0 Binding
Displacement of [3H]CGP-12177 from beta-1 adrenergic receptor in Sprague-Dawley rat cortical membraneDisplacement of [3H]CGP-12177 from beta-1 adrenergic receptor in Sprague-Dawley rat cortical membrane
ChEMBL 253 7 4 4 2.3 CCCC[C@@H](C)NC[C@H](O)c1cc(O)cc(O)c1 10.1021/jm070030d
137640201 156407 2 None -8128 13 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]CGP12177 from human recombinant beta1 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by beta counting methodDisplacement of [3H]CGP12177 from human recombinant beta1 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 -8128 13 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]CGP12177 from human recombinant beta1 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by beta counting methodDisplacement of [3H]CGP12177 from human recombinant beta1 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
44350012 17825 0 None -6 3 Guinea pig 5.0 pKi = 5.0 Binding
Binding affinity at Beta-1 adrenergic receptor in guinea pigs by [125I]CYP displacementBinding affinity at Beta-1 adrenergic receptor in guinea pigs by [125I]CYP displacement
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 -6 3 Guinea pig 5.0 pKi = 5.0 Binding
Binding affinity at Beta-1 adrenergic receptor in guinea pigs by [125I]CYP displacementBinding affinity at Beta-1 adrenergic receptor in guinea pigs by [125I]CYP displacement
ChEMBL 363 4 3 7 0.4 CC1CN=C2C(N3CCNCC3)=NC=CN21.O=C(O)C/C=C\CC(=O)O 10.1021/jm00099a012
10464801 11094 0 None 3 2 Rat 6.0 pKi = 6.0 Binding
Binding affinity against beta-1-adrenergic receptor in rat brainBinding affinity against beta-1-adrenergic receptor in rat brain
ChEMBL 174 6 2 4 0.4 CCO/N=C/C(O)CNC(C)C 10.1021/jm00036a018
CHEMBL1178754 11094 0 None 3 2 Rat 6.0 pKi = 6.0 Binding
Binding affinity against beta-1-adrenergic receptor in rat brainBinding affinity against beta-1-adrenergic receptor in rat brain
ChEMBL 174 6 2 4 0.4 CCO/N=C/C(O)CNC(C)C 10.1021/jm00036a018
CHEMBL39682 11094 0 None 3 2 Rat 6.0 pKi = 6.0 Binding
Binding affinity against beta-1-adrenergic receptor in rat brainBinding affinity against beta-1-adrenergic receptor in rat brain
ChEMBL 174 6 2 4 0.4 CCO/N=C/C(O)CNC(C)C 10.1021/jm00036a018
145946294 166933 0 None 3 2 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-CGP12177 from human beta1 ADR expressed in HEK293T cell membranes after 90 mins by scintillation countingDisplacement of [3H]-CGP12177 from human beta1 ADR expressed in HEK293T cell membranes 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 5.0 pKi = 5.0 Binding
Displacement of [3H]-CGP12177 from human beta1 ADR expressed in HEK293T cell membranes after 90 mins by scintillation countingDisplacement of [3H]-CGP12177 from human beta1 ADR expressed in HEK293T cell membranes 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 5.0 pKi = 5.0 Binding
Displacement of [3H]-CGP12177 from human beta1 ADR expressed in HEK293T cell membranes after 90 mins by scintillation countingDisplacement of [3H]-CGP12177 from human beta1 ADR expressed in HEK293T cell membranes 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
24936882 17385 0 None -52 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta-1 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 -52 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta-1 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
46889699 6555 0 None -26 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta-1 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta-1 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 6.0 pKi = 6.0 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta-1 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta-1 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
44444195 94087 0 None -87 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]iodocyanopindolol from human cloned adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human cloned adrenergic beta-1 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 -87 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]iodocyanopindolol from human cloned adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human cloned adrenergic beta-1 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
49864413 15452 0 None -2 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 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 6.0 pKi = 6.0 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 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
10527469 155712 1 None -22908 16 Human 5.0 pKi = 5.0 Binding
Binding affinity against Beta-1 adrenergic receptor using [3H]DHA as radioligandBinding affinity against Beta-1 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 -22908 16 Human 5.0 pKi = 5.0 Binding
Binding affinity against Beta-1 adrenergic receptor using [3H]DHA as radioligandBinding affinity against Beta-1 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
11647002 15447 0 None -22 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 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 7.0 pKi = 7.0 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 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
851833 33802 86 None 1 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]dihydroalprenolol from human wild type beta1 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysisDisplacement of [3H]dihydroalprenolol from human wild type beta1 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysis
ChEMBL 230 1 1 2 2.4 Clc1cccc(N2CCNCC2)c1Cl 10.1021/jm400140q
CHEMBL1424807 33802 86 None 1 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]dihydroalprenolol from human wild type beta1 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysisDisplacement of [3H]dihydroalprenolol from human wild type beta1 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysis
ChEMBL 230 1 1 2 2.4 Clc1cccc(N2CCNCC2)c1Cl 10.1021/jm400140q
10012704 11102 0 None 1 2 Rat 6.0 pKi = 6.0 Binding
Binding affinity against beta-1-adrenergic receptor in rat brainBinding affinity against beta-1-adrenergic receptor in rat brain
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 Rat 6.0 pKi = 6.0 Binding
Binding affinity against beta-1-adrenergic receptor in rat brainBinding affinity against beta-1-adrenergic receptor in rat brain
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 Rat 6.0 pKi = 6.0 Binding
Binding affinity against beta-1-adrenergic receptor in rat brainBinding affinity against beta-1-adrenergic receptor in rat brain
ChEMBL 188 5 2 4 0.8 CCO/N=C/C(O)CNC(C)(C)C 10.1021/jm00036a018
25242459 12615 0 None - 1 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation countingDisplacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation counting
ChEMBL 391 7 3 6 2.7 CC(C)(CO)NCC(O)COc1cccc2c(=O)c3ccc(Cl)cc3oc12 10.1016/j.bmc.2008.12.031
CHEMBL1187782 12615 0 None - 1 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation countingDisplacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation counting
ChEMBL 391 7 3 6 2.7 CC(C)(CO)NCC(O)COc1cccc2c(=O)c3ccc(Cl)cc3oc12 10.1016/j.bmc.2008.12.031
CHEMBL520600 12615 0 None - 1 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation countingDisplacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation counting
ChEMBL 391 7 3 6 2.7 CC(C)(CO)NCC(O)COc1cccc2c(=O)c3ccc(Cl)cc3oc12 10.1016/j.bmc.2008.12.031
165193 3126 60 None -2 43 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-CGP12177 from human beta1 ADR expressed in HEK293T cell membranes after 90 mins by scintillation countingDisplacement of [3H]-CGP12177 from human beta1 ADR expressed in HEK293T cell membranes 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 -2 43 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-CGP12177 from human beta1 ADR expressed in HEK293T cell membranes after 90 mins by scintillation countingDisplacement of [3H]-CGP12177 from human beta1 ADR expressed in HEK293T cell membranes 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 -2 43 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-CGP12177 from human beta1 ADR expressed in HEK293T cell membranes after 90 mins by scintillation countingDisplacement of [3H]-CGP12177 from human beta1 ADR expressed in HEK293T cell membranes 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 -2 43 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-CGP12177 from human beta1 ADR expressed in HEK293T cell membranes after 90 mins by scintillation countingDisplacement of [3H]-CGP12177 from human beta1 ADR expressed in HEK293T cell membranes 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 -2 43 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-CGP12177 from human beta1 ADR expressed in HEK293T cell membranes after 90 mins by scintillation countingDisplacement of [3H]-CGP12177 from human beta1 ADR expressed in HEK293T cell membranes 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 -2 43 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-CGP12177 from human beta1 ADR expressed in HEK293T cell membranes after 90 mins by scintillation countingDisplacement of [3H]-CGP12177 from human beta1 ADR expressed in HEK293T cell membranes 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 -2 43 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-CGP12177 from human beta1 ADR expressed in HEK293T cell membranes after 90 mins by scintillation countingDisplacement of [3H]-CGP12177 from human beta1 ADR expressed in HEK293T cell membranes 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 -2 43 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-CGP12177 from human beta1 ADR expressed in HEK293T cell membranes after 90 mins by scintillation countingDisplacement of [3H]-CGP12177 from human beta1 ADR expressed in HEK293T cell membranes 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 -2 43 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-CGP12177 from human beta1 ADR expressed in HEK293T cell membranes after 90 mins by scintillation countingDisplacement of [3H]-CGP12177 from human beta1 ADR expressed in HEK293T cell membranes 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 -2 43 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-CGP12177 from human beta1 ADR expressed in HEK293T cell membranes after 90 mins by scintillation countingDisplacement of [3H]-CGP12177 from human beta1 ADR expressed in HEK293T cell membranes 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 -2 43 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-CGP12177 from human beta1 ADR expressed in HEK293T cell membranes after 90 mins by scintillation countingDisplacement of [3H]-CGP12177 from human beta1 ADR expressed in HEK293T cell membranes after 90 mins by scintillation counting
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/acs.jmedchem.8b00625
44396532 66408 0 None -3 3 Human 7.0 pKi = 7.0 Binding
Binding inhibition constant was determined by inhibition of [125I]iodocyanopindolol binding to Beta-1 adrenergic receptorBinding inhibition constant was determined by inhibition of [125I]iodocyanopindolol binding to Beta-1 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 -3 3 Human 7.0 pKi = 7.0 Binding
Binding inhibition constant was determined by inhibition of [125I]iodocyanopindolol binding to Beta-1 adrenergic receptorBinding inhibition constant was determined by inhibition of [125I]iodocyanopindolol binding to Beta-1 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
72544566 92685 0 None -5 5 Pig 7.0 pKi = 7.0 Binding
Displacement of [3H]-prazosin from alpha1-adrenergic receptor in pig cerebral cortexDisplacement of [3H]-prazosin from alpha1-adrenergic receptor in pig cerebral cortex
ChEMBL 375 10 0 6 3.1 COc1ccccc1N1CCN(Cc2cn(CCCCCCF)nn2)CC1 10.1016/j.bmcl.2013.09.026
CHEMBL2443009 92685 0 None -5 5 Pig 7.0 pKi = 7.0 Binding
Displacement of [3H]-prazosin from alpha1-adrenergic receptor in pig cerebral cortexDisplacement of [3H]-prazosin from alpha1-adrenergic receptor in pig cerebral cortex
ChEMBL 375 10 0 6 3.1 COc1ccccc1N1CCN(Cc2cn(CCCCCCF)nn2)CC1 10.1016/j.bmcl.2013.09.026
1028 287 69 None -66 30 Rat 6.0 pKi = 6.0 Binding
Binding of [3H]dihydroalprenolol to beta-1 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-1 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 -66 30 Rat 6.0 pKi = 6.0 Binding
Binding of [3H]dihydroalprenolol to beta-1 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-1 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 -66 30 Rat 6.0 pKi = 6.0 Binding
Binding of [3H]dihydroalprenolol to beta-1 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-1 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 -66 30 Rat 6.0 pKi = 6.0 Binding
Binding of [3H]dihydroalprenolol to beta-1 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-1 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 -66 30 Rat 6.0 pKi = 6.0 Binding
Binding of [3H]dihydroalprenolol to beta-1 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-1 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 -66 30 Rat 6.0 pKi = 6.0 Binding
Binding of [3H]dihydroalprenolol to beta-1 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-1 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
44423644 84970 0 None -13 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]CYP from human adrenergic beta 1 receptor transfected in CHO cells in presence of 100 uM GTPDisplacement of [125I]CYP from human adrenergic beta 1 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 6.0 pKi = 6.0 Binding
Displacement of [125I]CYP from human adrenergic beta 1 receptor transfected in CHO cells in presence of 100 uM GTPDisplacement of [125I]CYP from human adrenergic beta 1 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
49864377 15439 0 None -12 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 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 7.0 pKi = 7.0 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 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
36811 1421 34 None -93 7 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 301 7 4 4 3.0 CC(CCc1ccc(cc1)O)NCCc1ccc(c(c1)O)O nan
535 1421 34 None -93 7 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 301 7 4 4 3.0 CC(CCc1ccc(cc1)O)NCCc1ccc(c(c1)O)O nan
937 1421 34 None -93 7 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 301 7 4 4 3.0 CC(CCc1ccc(cc1)O)NCCc1ccc(c(c1)O)O nan
CHEMBL926 1421 34 None -93 7 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 301 7 4 4 3.0 CC(CCc1ccc(cc1)O)NCCc1ccc(c(c1)O)O nan
DB00841 1421 34 None -93 7 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 301 7 4 4 3.0 CC(CCc1ccc(cc1)O)NCCc1ccc(c(c1)O)O nan
1054 1549 49 None -1 3 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 295 9 2 5 1.5 COC(=O)CCc1ccc(cc1)OCC(CNC(C)C)O nan
59768 1549 49 None -1 3 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 295 9 2 5 1.5 COC(=O)CCc1ccc(cc1)OCC(CNC(C)C)O nan
7178 1549 49 None -1 3 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 295 9 2 5 1.5 COC(=O)CCc1ccc(cc1)OCC(CNC(C)C)O nan
CHEMBL768 1549 49 None -1 3 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 295 9 2 5 1.5 COC(=O)CCc1ccc(cc1)OCC(CNC(C)C)O nan
DB00187 1549 49 None -1 3 Human 6.9 pKi = 6.9 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 295 9 2 5 1.5 COC(=O)CCc1ccc(cc1)OCC(CNC(C)C)O nan
567 715 10 None -11 5 Human 6.0 pKi = 6.0 Binding
Ability to bind to human Beta-1 adrenergic receptor using membranes of stably transfected CHO cellsAbility to bind to human Beta-1 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 -11 5 Human 6.0 pKi = 6.0 Binding
Ability to bind to human Beta-1 adrenergic receptor using membranes of stably transfected CHO cellsAbility to bind to human Beta-1 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 -11 5 Human 6.0 pKi = 6.0 Binding
Ability to bind to human Beta-1 adrenergic receptor using membranes of stably transfected CHO cellsAbility to bind to human Beta-1 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 -11 5 Human 5.0 pKi = 5.0 Binding
Compound was tested for its binding affinity against Beta-1 adrenergic receptor in CHO cell membrane using [125I]iodocyanopindolol as the radioligand.Compound was tested for its binding affinity against Beta-1 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 -11 5 Human 5.0 pKi = 5.0 Binding
Compound was tested for its binding affinity against Beta-1 adrenergic receptor in CHO cell membrane using [125I]iodocyanopindolol as the radioligand.Compound was tested for its binding affinity against Beta-1 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 -11 5 Human 5.0 pKi = 5.0 Binding
Compound was tested for its binding affinity against Beta-1 adrenergic receptor in CHO cell membrane using [125I]iodocyanopindolol as the radioligand.Compound was tested for its binding affinity against Beta-1 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
52948056 17322 0 None -6 3 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta-1 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 -6 3 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta-1 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
2769774 6625 16 None -16 3 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta-1 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta-1 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 6.9 pKi = 6.9 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta-1 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta-1 receptor expressed in CHOK1 cells
ChEMBL 277 7 1 4 1.5 C=CCc1ccccc1OCC(O)CN1CCOCC1 10.1016/j.bmcl.2010.04.009
13720717 77483 0 None -3 2 Guinea pig 5.9 pKi = 5.9 Binding
Binding affinity against Beta-1 adrenergic receptor in guinea pig left ventricleBinding affinity against Beta-1 adrenergic receptor in guinea pig left ventricle
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 5.9 pKi = 5.9 Binding
Binding affinity against Beta-1 adrenergic receptor in guinea pig left ventricleBinding affinity against Beta-1 adrenergic receptor in guinea pig left ventricle
ChEMBL 363 5 3 6 2.7 COc1cc(C[C@H]2NCCc3cc(O)c(O)c(F)c32)cc(OC)c1OC 10.1021/jm00081a007
4080436 6626 3 None -10 3 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta-1 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta-1 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 7.9 pKi = 7.9 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta-1 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta-1 receptor expressed in CHOK1 cells
ChEMBL 279 6 1 4 1.9 CC(C)c1ccccc1OCC(O)CN1CCOCC1 10.1016/j.bmcl.2010.04.009
146025802 169000 0 None 1 2 Mouse 7.9 pKi = 7.9 Binding
Displacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T 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 Mouse 7.9 pKi = 7.9 Binding
Displacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T 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
559926 96546 5 None - 1 Rat 6.9 pKi = 6.9 Binding
Compound was evaluated for the inhibition of binding of [3H]dihydroalprenolol from beta-1 adrenergic receptor of rat cerebral cortical membranesCompound was evaluated for the inhibition of binding of [3H]dihydroalprenolol from beta-1 adrenergic receptor of rat cerebral cortical membranes
ChEMBL 255 5 4 5 1.2 CC(C)(C)NCC(O)COc1ccc(O)c(O)c1 10.1021/jm00107a027
CHEMBL266619 96546 5 None - 1 Rat 6.9 pKi = 6.9 Binding
Compound was evaluated for the inhibition of binding of [3H]dihydroalprenolol from beta-1 adrenergic receptor of rat cerebral cortical membranesCompound was evaluated for the inhibition of binding of [3H]dihydroalprenolol from beta-1 adrenergic receptor of rat cerebral cortical membranes
ChEMBL 255 5 4 5 1.2 CC(C)(C)NCC(O)COc1ccc(O)c(O)c1 10.1021/jm00107a027
44444378 93807 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]iodocyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human adrenergic beta-1 receptor expressed in CHO cells
ChEMBL 418 9 2 7 4.0 O[C@@H](CNCCOc1ccc(-c2csc(-c3cccnc3)n2)cc1)c1cccnc1 10.1016/j.bmcl.2007.06.072
CHEMBL250146 93807 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]iodocyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human adrenergic beta-1 receptor expressed in CHO cells
ChEMBL 418 9 2 7 4.0 O[C@@H](CNCCOc1ccc(-c2csc(-c3cccnc3)n2)cc1)c1cccnc1 10.1016/j.bmcl.2007.06.072
72545011 92680 0 None -8 5 Pig 6.9 pKi = 6.9 Binding
Displacement of [3H]-prazosin from alpha1-adrenergic receptor in pig cerebral cortexDisplacement of [3H]-prazosin from alpha1-adrenergic receptor in pig cerebral cortex
ChEMBL 411 8 0 7 2.9 COc1ccccc1N1CCN(Cc2cn(-c3ccc(OCCF)cc3)nn2)CC1 10.1016/j.bmcl.2013.09.026
CHEMBL2443004 92680 0 None -8 5 Pig 6.9 pKi = 6.9 Binding
Displacement of [3H]-prazosin from alpha1-adrenergic receptor in pig cerebral cortexDisplacement of [3H]-prazosin from alpha1-adrenergic receptor in pig cerebral cortex
ChEMBL 411 8 0 7 2.9 COc1ccccc1N1CCN(Cc2cn(-c3ccc(OCCF)cc3)nn2)CC1 10.1016/j.bmcl.2013.09.026
72545239 92682 0 None -1 5 Pig 6.9 pKi = 6.9 Binding
Displacement of [3H]-prazosin from alpha1-adrenergic receptor in pig cerebral cortexDisplacement of [3H]-prazosin from alpha1-adrenergic receptor in pig cerebral cortex
ChEMBL 499 14 0 9 3.0 COc1ccccc1N1CCN(Cc2cn(-c3ccc(OCCOCCOCCF)cc3)nn2)CC1 10.1016/j.bmcl.2013.09.026
CHEMBL2443006 92682 0 None -1 5 Pig 6.9 pKi = 6.9 Binding
Displacement of [3H]-prazosin from alpha1-adrenergic receptor in pig cerebral cortexDisplacement of [3H]-prazosin from alpha1-adrenergic receptor in pig cerebral cortex
ChEMBL 499 14 0 9 3.0 COc1ccccc1N1CCN(Cc2cn(-c3ccc(OCCOCCOCCF)cc3)nn2)CC1 10.1016/j.bmcl.2013.09.026
155512924 169121 0 None -1 2 Mouse 5.9 pKi = 5.9 Binding
Displacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T 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 Mouse 5.9 pKi = 5.9 Binding
Displacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T 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
1028 287 69 None -66 30 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]dihydroalprenolol from adrenergic beta 1 receptor of rat cerebral cortical membranesDisplacement of [3H]dihydroalprenolol from adrenergic beta 1 receptor of rat cerebral cortical membranes
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00076a024
139148732 287 69 None -66 30 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]dihydroalprenolol from adrenergic beta 1 receptor of rat cerebral cortical membranesDisplacement of [3H]dihydroalprenolol from adrenergic beta 1 receptor of rat cerebral cortical membranes
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00076a024
479 287 69 None -66 30 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]dihydroalprenolol from adrenergic beta 1 receptor of rat cerebral cortical membranesDisplacement of [3H]dihydroalprenolol from adrenergic beta 1 receptor of rat cerebral cortical membranes
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00076a024
5816 287 69 None -66 30 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]dihydroalprenolol from adrenergic beta 1 receptor of rat cerebral cortical membranesDisplacement of [3H]dihydroalprenolol from adrenergic beta 1 receptor of rat cerebral cortical membranes
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00076a024
CHEMBL679 287 69 None -66 30 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]dihydroalprenolol from adrenergic beta 1 receptor of rat cerebral cortical membranesDisplacement of [3H]dihydroalprenolol from adrenergic beta 1 receptor of rat cerebral cortical membranes
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00076a024
DB00668 287 69 None -66 30 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]dihydroalprenolol from adrenergic beta 1 receptor of rat cerebral cortical membranesDisplacement of [3H]dihydroalprenolol from adrenergic beta 1 receptor of rat cerebral cortical membranes
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00076a024
49864416 15455 0 None -30 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 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 6.9 pKi = 6.9 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 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
9990035 11901 0 None 4 2 Rat 5.9 pKi = 5.9 Binding
Binding affinity against beta-1-adrenergic receptor in rat brainBinding affinity against beta-1-adrenergic receptor in rat brain
ChEMBL 188 7 2 4 0.8 CCCO/N=C/C(O)CNC(C)C 10.1021/jm00036a018
CHEMBL1183337 11901 0 None 4 2 Rat 5.9 pKi = 5.9 Binding
Binding affinity against beta-1-adrenergic receptor in rat brainBinding affinity against beta-1-adrenergic receptor in rat brain
ChEMBL 188 7 2 4 0.8 CCCO/N=C/C(O)CNC(C)C 10.1021/jm00036a018
CHEMBL291115 11901 0 None 4 2 Rat 5.9 pKi = 5.9 Binding
Binding affinity against beta-1-adrenergic receptor in rat brainBinding affinity against beta-1-adrenergic receptor in rat brain
ChEMBL 188 7 2 4 0.8 CCCO/N=C/C(O)CNC(C)C 10.1021/jm00036a018
44286965 159850 0 None -4 3 Human 5.9 pKi = 5.9 Binding
Ability to bind to human Beta-1 adrenergic receptor using membranes of stably transfected CHO cellsAbility to bind to human Beta-1 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 5.9 pKi = 5.9 Binding
Ability to bind to human Beta-1 adrenergic receptor using membranes of stably transfected CHO cellsAbility to bind to human Beta-1 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
11178830 147582 0 None -794 9 Human 5.9 pKi = 5.9 Binding
Binding affinity at adrenergic beta 1 receptorBinding affinity at adrenergic beta 1 receptor
ChEMBL 467 6 1 5 4.5 Cc1ccc2c(OCCN3CCC(Cc4ccc5c(c4F)NC(=O)CO5)CC3)cc(F)cc2n1 10.1016/j.bmcl.2006.11.031
CHEMBL393539 147582 0 None -794 9 Human 5.9 pKi = 5.9 Binding
Binding affinity at adrenergic beta 1 receptorBinding affinity at adrenergic beta 1 receptor
ChEMBL 467 6 1 5 4.5 Cc1ccc2c(OCCN3CCC(Cc4ccc5c(c4F)NC(=O)CO5)CC3)cc(F)cc2n1 10.1016/j.bmcl.2006.11.031
770558 87093 56 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]dihydroalprenolol from human wild type beta1 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysisDisplacement of [3H]dihydroalprenolol from human wild type beta1 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysis
ChEMBL 298 1 1 2 3.1 FC(F)(F)c1cc(N2CCNCC2)cc(C(F)(F)F)c1 10.1021/jm400140q
CHEMBL2335162 87093 56 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]dihydroalprenolol from human wild type beta1 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysisDisplacement of [3H]dihydroalprenolol from human wild type beta1 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysis
ChEMBL 298 1 1 2 3.1 FC(F)(F)c1cc(N2CCNCC2)cc(C(F)(F)F)c1 10.1021/jm400140q
59119467 111749 0 None -39 2 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]dihydroalprenolol from beta1 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta1 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 4.9 pKi = 4.9 Binding
Displacement of [3H]dihydroalprenolol from beta1 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta1 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 4.9 pKi = 4.9 Binding
Displacement of [3H]dihydroalprenolol from beta1 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta1 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 4.9 pKi = 4.9 Binding
Displacement of [3H]dihydroalprenolol from beta1 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta1 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 4.9 pKi = 4.9 Binding
Displacement of [3H]dihydroalprenolol from beta1 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta1 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 4.9 pKi = 4.9 Binding
Displacement of [3H]dihydroalprenolol from beta1 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta1 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
59119455 111757 0 None -19 2 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]dihydroalprenolol from beta1 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta1 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 4.9 pKi = 4.9 Binding
Displacement of [3H]dihydroalprenolol from beta1 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta1 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
1960 2805 64 None -144 26 Rat 6.9 pKi = 6.9 Binding
Compound was evaluated for beta adrenergic binding affinity towards Beta-1 adrenergic receptor of rat brainCompound was evaluated for beta adrenergic binding affinity towards Beta-1 adrenergic receptor of rat brain
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00084a006
439260 2805 64 None -144 26 Rat 6.9 pKi = 6.9 Binding
Compound was evaluated for beta adrenergic binding affinity towards Beta-1 adrenergic receptor of rat brainCompound was evaluated for beta adrenergic binding affinity towards Beta-1 adrenergic receptor of rat brain
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00084a006
505 2805 64 None -144 26 Rat 6.9 pKi = 6.9 Binding
Compound was evaluated for beta adrenergic binding affinity towards Beta-1 adrenergic receptor of rat brainCompound was evaluated for beta adrenergic binding affinity towards Beta-1 adrenergic receptor of rat brain
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00084a006
CHEMBL1437 2805 64 None -144 26 Rat 6.9 pKi = 6.9 Binding
Compound was evaluated for beta adrenergic binding affinity towards Beta-1 adrenergic receptor of rat brainCompound was evaluated for beta adrenergic binding affinity towards Beta-1 adrenergic receptor of rat brain
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00084a006
DB00368 2805 64 None -144 26 Rat 6.9 pKi = 6.9 Binding
Compound was evaluated for beta adrenergic binding affinity towards Beta-1 adrenergic receptor of rat brainCompound was evaluated for beta adrenergic binding affinity towards Beta-1 adrenergic receptor of rat brain
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00084a006
1960 2805 64 None -144 26 Rat 6.9 pKi = 6.9 Binding
Tested for binding affinity against beta-1 adrenergic receptor in rat brain using [3H]-CGP- 26505 as radioligandTested for binding affinity against beta-1 adrenergic receptor in rat brain using [3H]-CGP- 26505 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 -144 26 Rat 6.9 pKi = 6.9 Binding
Tested for binding affinity against beta-1 adrenergic receptor in rat brain using [3H]-CGP- 26505 as radioligandTested for binding affinity against beta-1 adrenergic receptor in rat brain using [3H]-CGP- 26505 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 -144 26 Rat 6.9 pKi = 6.9 Binding
Tested for binding affinity against beta-1 adrenergic receptor in rat brain using [3H]-CGP- 26505 as radioligandTested for binding affinity against beta-1 adrenergic receptor in rat brain using [3H]-CGP- 26505 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 -144 26 Rat 6.9 pKi = 6.9 Binding
Tested for binding affinity against beta-1 adrenergic receptor in rat brain using [3H]-CGP- 26505 as radioligandTested for binding affinity against beta-1 adrenergic receptor in rat brain using [3H]-CGP- 26505 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 -144 26 Rat 6.9 pKi = 6.9 Binding
Tested for binding affinity against beta-1 adrenergic receptor in rat brain using [3H]-CGP- 26505 as radioligandTested for binding affinity against beta-1 adrenergic receptor in rat brain using [3H]-CGP- 26505 as radioligand
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00073a006
448537 159691 86 None -50 25 Human 4.9 pKi = 4.9 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 nan
CHEMBL411 159691 86 None -50 25 Human 4.9 pKi = 4.9 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 nan
24936492 17352 0 None -4 3 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta-1 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 -4 3 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta-1 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
46889853 6440 0 None -64 3 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta-1 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta-1 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 7.9 pKi = 7.9 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta-1 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta-1 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
118710949 113249 0 None -3 3 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 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 7.9 pKi = 7.9 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 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
10352428 100623 1 None -1 4 Rat 6.9 pKi = 6.9 Binding
Binding of [3H]dihydroalprenolol to beta-1 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-1 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 Rat 6.9 pKi = 6.9 Binding
Binding of [3H]dihydroalprenolol to beta-1 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-1 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
10136220 154274 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]iodocyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human adrenergic beta-1 receptor expressed in CHO cells
ChEMBL 409 9 2 6 4.6 O[C@@H](CNCCOc1ccc(-c2csc(C3CCCC3)n2)cc1)c1cccnc1 10.1016/j.bmcl.2007.06.072
CHEMBL400392 154274 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]iodocyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human adrenergic beta-1 receptor expressed in CHO cells
ChEMBL 409 9 2 6 4.6 O[C@@H](CNCCOc1ccc(-c2csc(C3CCCC3)n2)cc1)c1cccnc1 10.1016/j.bmcl.2007.06.072
72545238 92681 0 None -25 5 Pig 6.9 pKi = 6.9 Binding
Displacement of [3H]-prazosin from alpha1-adrenergic receptor in pig cerebral cortexDisplacement of [3H]-prazosin from alpha1-adrenergic receptor in pig cerebral cortex
ChEMBL 425 9 0 7 3.3 COc1ccccc1N1CCN(Cc2cn(-c3ccc(OCCCF)cc3)nn2)CC1 10.1016/j.bmcl.2013.09.026
CHEMBL2443005 92681 0 None -25 5 Pig 6.9 pKi = 6.9 Binding
Displacement of [3H]-prazosin from alpha1-adrenergic receptor in pig cerebral cortexDisplacement of [3H]-prazosin from alpha1-adrenergic receptor in pig cerebral cortex
ChEMBL 425 9 0 7 3.3 COc1ccccc1N1CCN(Cc2cn(-c3ccc(OCCCF)cc3)nn2)CC1 10.1016/j.bmcl.2013.09.026
1960 2805 64 None -144 26 Rat 5.9 pKi = 5.9 Binding
Binding of [3H]dihydroalprenolol to beta-1 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-1 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 -144 26 Rat 5.9 pKi = 5.9 Binding
Binding of [3H]dihydroalprenolol to beta-1 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-1 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 -144 26 Rat 5.9 pKi = 5.9 Binding
Binding of [3H]dihydroalprenolol to beta-1 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-1 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 -144 26 Rat 5.9 pKi = 5.9 Binding
Binding of [3H]dihydroalprenolol to beta-1 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-1 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 -144 26 Rat 5.9 pKi = 5.9 Binding
Binding of [3H]dihydroalprenolol to beta-1 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-1 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
9821129 202725 0 None -1 3 Human 5.9 pKi = 5.9 Binding
Compound was tested for its binding affinity against Beta-1 adrenergic receptor in CHO cell membrane using [125I]iodocyanopindolol as the radioligand.Compound was tested for its binding affinity against Beta-1 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 -1 3 Human 5.9 pKi = 5.9 Binding
Compound was tested for its binding affinity against Beta-1 adrenergic receptor in CHO cell membrane using [125I]iodocyanopindolol as the radioligand.Compound was tested for its binding affinity against Beta-1 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
72545008 92677 0 None -1 5 Pig 5.9 pKi = 5.9 Binding
Displacement of [3H]-prazosin from alpha1-adrenergic receptor in pig cerebral cortexDisplacement of [3H]-prazosin from alpha1-adrenergic receptor in pig cerebral cortex
ChEMBL 451 15 0 9 1.6 COc1ccccc1N1CCN(Cc2cn(CCOCCOCCOCCF)nn2)CC1 10.1016/j.bmcl.2013.09.026
CHEMBL2443001 92677 0 None -1 5 Pig 5.9 pKi = 5.9 Binding
Displacement of [3H]-prazosin from alpha1-adrenergic receptor in pig cerebral cortexDisplacement of [3H]-prazosin from alpha1-adrenergic receptor in pig cerebral cortex
ChEMBL 451 15 0 9 1.6 COc1ccccc1N1CCN(Cc2cn(CCOCCOCCOCCF)nn2)CC1 10.1016/j.bmcl.2013.09.026
247704 288 26 None -12 5 Rat 4.9 pKi = 4.9 Binding
Binding of [3H]dihydroalprenolol to beta-1 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-1 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 -12 5 Rat 4.9 pKi = 4.9 Binding
Binding of [3H]dihydroalprenolol to beta-1 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-1 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 -12 5 Rat 4.9 pKi = 4.9 Binding
Binding of [3H]dihydroalprenolol to beta-1 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-1 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
155515982 169432 0 None -51286 17 Human 4.9 pKi = 4.9 Binding
Displacement of [3H] CGP12177 from beta1 adrenergic receptor (unknown origin)Displacement of [3H] CGP12177 from beta1 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 -51286 17 Human 4.9 pKi = 4.9 Binding
Displacement of [3H] CGP12177 from beta1 adrenergic receptor (unknown origin)Displacement of [3H] CGP12177 from beta1 adrenergic receptor (unknown origin)
ChEMBL 473 10 2 5 4.1 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2)c2ccccc2)CC1 10.1021/acs.jmedchem.9b01085
2146 3039 63 None -36 8 Rat 4.9 pKi = 4.9 Binding
Displacement of [3H]dihydroalprenolol from adrenergic beta 1 receptor of rat cerebral cortical membranesDisplacement of [3H]dihydroalprenolol from adrenergic beta 1 receptor of rat cerebral cortical membranes
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1021/jm00076a024
485 3039 63 None -36 8 Rat 4.9 pKi = 4.9 Binding
Displacement of [3H]dihydroalprenolol from adrenergic beta 1 receptor of rat cerebral cortical membranesDisplacement of [3H]dihydroalprenolol from adrenergic beta 1 receptor of rat cerebral cortical membranes
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1021/jm00076a024
6041 3039 63 None -36 8 Rat 4.9 pKi = 4.9 Binding
Displacement of [3H]dihydroalprenolol from adrenergic beta 1 receptor of rat cerebral cortical membranesDisplacement of [3H]dihydroalprenolol from adrenergic beta 1 receptor of rat cerebral cortical membranes
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1021/jm00076a024
CHEMBL1215 3039 63 None -36 8 Rat 4.9 pKi = 4.9 Binding
Displacement of [3H]dihydroalprenolol from adrenergic beta 1 receptor of rat cerebral cortical membranesDisplacement of [3H]dihydroalprenolol from adrenergic beta 1 receptor of rat cerebral cortical membranes
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1021/jm00076a024
DB00388 3039 63 None -36 8 Rat 4.9 pKi = 4.9 Binding
Displacement of [3H]dihydroalprenolol from adrenergic beta 1 receptor of rat cerebral cortical membranesDisplacement of [3H]dihydroalprenolol from adrenergic beta 1 receptor of rat cerebral cortical membranes
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1021/jm00076a024
11188590 77252 0 None -1 2 Human 6.9 pKi = 6.9 Binding
Binding affinity to human beta1-adrenoceptor by radioligand binding assayBinding affinity to human beta1-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 6.9 pKi = 6.9 Binding
Binding affinity to human beta1-adrenoceptor by radioligand binding assayBinding affinity to human beta1-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
7096 205735 111 None -21 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]dihydroalprenolol from human wild type beta1 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysisDisplacement of [3H]dihydroalprenolol from human wild type beta1 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysis
ChEMBL 162 1 1 2 1.1 c1ccc(N2CCNCC2)cc1 10.1021/jm400140q
CHEMBL9434 205735 111 None -21 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]dihydroalprenolol from human wild type beta1 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysisDisplacement of [3H]dihydroalprenolol from human wild type beta1 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysis
ChEMBL 162 1 1 2 1.1 c1ccc(N2CCNCC2)cc1 10.1021/jm400140q
145946710 166985 0 None -2 2 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]-CGP12177 from human beta1 ADR expressed in HEK293T cell membranes after 90 mins by scintillation countingDisplacement of [3H]-CGP12177 from human beta1 ADR expressed in HEK293T cell membranes 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 4.9 pKi = 4.9 Binding
Displacement of [3H]-CGP12177 from human beta1 ADR expressed in HEK293T cell membranes after 90 mins by scintillation countingDisplacement of [3H]-CGP12177 from human beta1 ADR expressed in HEK293T cell membranes 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 4.9 pKi = 4.9 Binding
Displacement of [3H]-CGP12177 from human beta1 ADR expressed in HEK293T cell membranes after 90 mins by scintillation countingDisplacement of [3H]-CGP12177 from human beta1 ADR expressed in HEK293T cell membranes 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
4143663 6799 12 None -1 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta-1 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta-1 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 -1 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta-1 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta-1 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
31101 719 39 None -245 36 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 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 nan
35 719 39 None -245 36 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 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 nan
403 719 39 None -245 36 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 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 nan
CHEMBL493 719 39 None -245 36 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 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 nan
DB01200 719 39 None -245 36 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 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 nan
46889810 7320 0 None -28 3 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta-1 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta-1 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 7.9 pKi = 7.9 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta-1 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta-1 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
44328703 10118 0 None -1 2 Mouse 7.9 pKi = 7.9 Binding
Displacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T 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 Mouse 7.9 pKi = 7.9 Binding
Displacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T 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
1621 2386 16 None -102 45 Human 6.9 pKi = 6.9 Binding
Binding affinity towards Beta-1 adrenergic receptorBinding affinity towards Beta-1 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 -102 45 Human 6.9 pKi = 6.9 Binding
Binding affinity towards Beta-1 adrenergic receptorBinding affinity towards Beta-1 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 -102 45 Human 6.9 pKi = 6.9 Binding
Binding affinity towards Beta-1 adrenergic receptorBinding affinity towards Beta-1 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 -102 45 Human 6.9 pKi = 6.9 Binding
Binding affinity towards Beta-1 adrenergic receptorBinding affinity towards Beta-1 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 -102 45 Human 6.9 pKi = 6.9 Binding
Binding affinity towards Beta-1 adrenergic receptorBinding affinity towards Beta-1 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
10291064 94031 0 None -14 2 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]iodocyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human adrenergic beta-1 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 6.9 pKi = 6.9 Binding
Displacement of [125I]iodocyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human adrenergic beta-1 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
10436455 155370 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibition of [3H]dihydroalprenolol binding to beta 1 adrenoceptor from turkey erythrocyte membranes.Inhibition of [3H]dihydroalprenolol binding to beta 1 adrenoceptor from turkey erythrocyte membranes.
ChEMBL 512 7 3 8 1.6 NS(=O)(=O)c1cc(N2CCN(CC(O)COc3cccc4c3SCC(=O)N4)CC2)ccc1Cl 10.1021/jm00053a020
CHEMBL40609 155370 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibition of [3H]dihydroalprenolol binding to beta 1 adrenoceptor from turkey erythrocyte membranes.Inhibition of [3H]dihydroalprenolol binding to beta 1 adrenoceptor from turkey erythrocyte membranes.
ChEMBL 512 7 3 8 1.6 NS(=O)(=O)c1cc(N2CCN(CC(O)COc3cccc4c3SCC(=O)N4)CC2)ccc1Cl 10.1021/jm00053a020
52946430 17628 0 None -4 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta-1 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 -4 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta-1 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
25266786 181107 0 None - 1 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation methodDisplacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation method
ChEMBL 356 10 3 5 2.6 COc1ccccc1OCCNC[C@@H](O)COc1cccc2[nH]ccc12 10.1016/j.ejmech.2008.05.019
CHEMBL477672 181107 0 None - 1 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation methodDisplacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation method
ChEMBL 356 10 3 5 2.6 COc1ccccc1OCCNC[C@@H](O)COc1cccc2[nH]ccc12 10.1016/j.ejmech.2008.05.019
4376990 192397 4 None -588 11 Human 5.8 pKi = 5.8 Binding
Binding affinity to beta1 receptor (unknown origin) assessed as inhibition constantBinding affinity to beta1 receptor (unknown origin) assessed as inhibition constant
ChEMBL 372 4 2 4 4.1 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(Cl)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5207529 192397 4 None -588 11 Human 5.8 pKi = 5.8 Binding
Binding affinity to beta1 receptor (unknown origin) assessed as inhibition constantBinding affinity to beta1 receptor (unknown origin) assessed as inhibition constant
ChEMBL 372 4 2 4 4.1 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(Cl)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5222754 192397 4 None -588 11 Human 5.8 pKi = 5.8 Binding
Binding affinity to beta1 receptor (unknown origin) assessed as inhibition constantBinding affinity to beta1 receptor (unknown origin) assessed as inhibition constant
ChEMBL 372 4 2 4 4.1 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(Cl)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
688468 141788 7 None -190 2 Rat 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 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 Rat 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 303 6 5 5 2.1 C[C@H](Cc1ccc(O)cc1)NC[C@H](O)c1cc(O)cc(O)c1 nan
11819522 11896 0 None 4 2 Rat 5.8 pKi = 5.8 Binding
Binding affinity against beta-1-adrenergic receptor in rat brainBinding affinity against beta-1-adrenergic receptor in rat brain
ChEMBL 174 6 2 4 0.4 C/C=N/OCC(O)CNC(C)C 10.1021/jm00036a018
CHEMBL1183318 11896 0 None 4 2 Rat 5.8 pKi = 5.8 Binding
Binding affinity against beta-1-adrenergic receptor in rat brainBinding affinity against beta-1-adrenergic receptor in rat brain
ChEMBL 174 6 2 4 0.4 C/C=N/OCC(O)CNC(C)C 10.1021/jm00036a018
CHEMBL290153 11896 0 None 4 2 Rat 5.8 pKi = 5.8 Binding
Binding affinity against beta-1-adrenergic receptor in rat brainBinding affinity against beta-1-adrenergic receptor in rat brain
ChEMBL 174 6 2 4 0.4 C/C=N/OCC(O)CNC(C)C 10.1021/jm00036a018
24937014 17211 0 None -58 3 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta-1 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 -58 3 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta-1 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
688468 141788 7 None -190 2 Rat 4.8 pKi = 4.8 Binding
Displacement of [3H]CGP-12177 from beta-1 adrenergic receptor in Sprague-Dawley rat cortical membraneDisplacement of [3H]CGP-12177 from beta-1 adrenergic receptor in Sprague-Dawley rat cortical membrane
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 Rat 4.8 pKi = 4.8 Binding
Displacement of [3H]CGP-12177 from beta-1 adrenergic receptor in Sprague-Dawley rat cortical membraneDisplacement of [3H]CGP-12177 from beta-1 adrenergic receptor in Sprague-Dawley rat cortical membrane
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
56677231 63293 0 None -234 2 Rat 4.8 pKi = 4.8 Binding
Displacement of [3H]CGP-12177 from beta1-adrenergic receptor in Sprague-Dawley rat cortical membrane after 2 hrsDisplacement of [3H]CGP-12177 from beta1-adrenergic receptor in Sprague-Dawley rat cortical membrane after 2 hrs
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 Rat 4.8 pKi = 4.8 Binding
Displacement of [3H]CGP-12177 from beta1-adrenergic receptor in Sprague-Dawley rat cortical membrane after 2 hrsDisplacement of [3H]CGP-12177 from beta1-adrenergic receptor in Sprague-Dawley rat cortical membrane after 2 hrs
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
12828562 109205 0 None 3 2 Rat 5.8 pKi = 5.8 Binding
Tested for binding affinity against beta-1 adrenergic receptor in rat brain using [3H]-CGP- 26505 as radioligandTested for binding affinity against beta-1 adrenergic receptor in rat brain using [3H]-CGP- 26505 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 Rat 5.8 pKi = 5.8 Binding
Tested for binding affinity against beta-1 adrenergic receptor in rat brain using [3H]-CGP- 26505 as radioligandTested for binding affinity against beta-1 adrenergic receptor in rat brain using [3H]-CGP- 26505 as radioligand
ChEMBL 237 3 3 4 1.7 CC(C)NCC1OCCc2cc(O)c(O)cc21 10.1021/jm00073a006
2810 67245 50 None -1 2 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 213 4 2 2 2.4 CC(C)NCC(O)c1ccccc1Cl nan
CHEMBL1902627 67245 50 None -1 2 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 213 4 2 2 2.4 CC(C)NCC(O)c1ccccc1Cl nan
165193 3126 60 None -18 43 Rat 7.8 pKi = 7.8 Binding
Displacement of [3H]-CGP-12177 from beta1-adrenergic receptor in rat brain cortex after 1 hr by Microbeta scintillation counting methodDisplacement of [3H]-CGP-12177 from beta1-adrenergic receptor in rat brain cortex after 1 hr by Microbeta scintillation counting method
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.ejmech.2018.01.093
2303 3126 60 None -18 43 Rat 7.8 pKi = 7.8 Binding
Displacement of [3H]-CGP-12177 from beta1-adrenergic receptor in rat brain cortex after 1 hr by Microbeta scintillation counting methodDisplacement of [3H]-CGP-12177 from beta1-adrenergic receptor in rat brain cortex after 1 hr by Microbeta scintillation counting method
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.ejmech.2018.01.093
4946 3126 60 None -18 43 Rat 7.8 pKi = 7.8 Binding
Displacement of [3H]-CGP-12177 from beta1-adrenergic receptor in rat brain cortex after 1 hr by Microbeta scintillation counting methodDisplacement of [3H]-CGP-12177 from beta1-adrenergic receptor in rat brain cortex after 1 hr by Microbeta scintillation counting method
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.ejmech.2018.01.093
564 3126 60 None -18 43 Rat 7.8 pKi = 7.8 Binding
Displacement of [3H]-CGP-12177 from beta1-adrenergic receptor in rat brain cortex after 1 hr by Microbeta scintillation counting methodDisplacement of [3H]-CGP-12177 from beta1-adrenergic receptor in rat brain cortex after 1 hr by Microbeta scintillation counting method
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.ejmech.2018.01.093
62882 3126 60 None -18 43 Rat 7.8 pKi = 7.8 Binding
Displacement of [3H]-CGP-12177 from beta1-adrenergic receptor in rat brain cortex after 1 hr by Microbeta scintillation counting methodDisplacement of [3H]-CGP-12177 from beta1-adrenergic receptor in rat brain cortex after 1 hr by Microbeta scintillation counting method
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.ejmech.2018.01.093
63 3126 60 None -18 43 Rat 7.8 pKi = 7.8 Binding
Displacement of [3H]-CGP-12177 from beta1-adrenergic receptor in rat brain cortex after 1 hr by Microbeta scintillation counting methodDisplacement of [3H]-CGP-12177 from beta1-adrenergic receptor in rat brain cortex after 1 hr by Microbeta scintillation counting method
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.ejmech.2018.01.093
66366 3126 60 None -18 43 Rat 7.8 pKi = 7.8 Binding
Displacement of [3H]-CGP-12177 from beta1-adrenergic receptor in rat brain cortex after 1 hr by Microbeta scintillation counting methodDisplacement of [3H]-CGP-12177 from beta1-adrenergic receptor in rat brain cortex after 1 hr by Microbeta scintillation counting method
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.ejmech.2018.01.093
91536 3126 60 None -18 43 Rat 7.8 pKi = 7.8 Binding
Displacement of [3H]-CGP-12177 from beta1-adrenergic receptor in rat brain cortex after 1 hr by Microbeta scintillation counting methodDisplacement of [3H]-CGP-12177 from beta1-adrenergic receptor in rat brain cortex after 1 hr by Microbeta scintillation counting method
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.ejmech.2018.01.093
CHEMBL27 3126 60 None -18 43 Rat 7.8 pKi = 7.8 Binding
Displacement of [3H]-CGP-12177 from beta1-adrenergic receptor in rat brain cortex after 1 hr by Microbeta scintillation counting methodDisplacement of [3H]-CGP-12177 from beta1-adrenergic receptor in rat brain cortex after 1 hr by Microbeta scintillation counting method
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.ejmech.2018.01.093
CHEMBL452861 3126 60 None -18 43 Rat 7.8 pKi = 7.8 Binding
Displacement of [3H]-CGP-12177 from beta1-adrenergic receptor in rat brain cortex after 1 hr by Microbeta scintillation counting methodDisplacement of [3H]-CGP-12177 from beta1-adrenergic receptor in rat brain cortex after 1 hr by Microbeta scintillation counting method
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.ejmech.2018.01.093
DB00571 3126 60 None -18 43 Rat 7.8 pKi = 7.8 Binding
Displacement of [3H]-CGP-12177 from beta1-adrenergic receptor in rat brain cortex after 1 hr by Microbeta scintillation counting methodDisplacement of [3H]-CGP-12177 from beta1-adrenergic receptor in rat brain cortex after 1 hr by Microbeta scintillation counting method
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.ejmech.2018.01.093
49864379 15441 0 None -8 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 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 7.8 pKi = 7.8 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 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
10049403 154749 0 None - 1 Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]dihydroalprenolol binding to beta 1 adrenoceptor from turkey erythrocyte membranes.Inhibition of [3H]dihydroalprenolol binding to beta 1 adrenoceptor from turkey erythrocyte membranes.
ChEMBL 449 10 4 6 2.6 NS(=O)(=O)c1cc(NCCNCC(O)COc2cccc3ccccc23)ccc1Cl 10.1021/jm00053a020
CHEMBL40297 154749 0 None - 1 Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]dihydroalprenolol binding to beta 1 adrenoceptor from turkey erythrocyte membranes.Inhibition of [3H]dihydroalprenolol binding to beta 1 adrenoceptor from turkey erythrocyte membranes.
ChEMBL 449 10 4 6 2.6 NS(=O)(=O)c1cc(NCCNCC(O)COc2cccc3ccccc23)ccc1Cl 10.1021/jm00053a020
10082625 13666 0 None 1 3 Guinea pig 6.8 pKi = 6.8 Binding
Binding affinity at Beta-1 adrenergic receptor in guinea pigs by [125I]CYP displacementBinding affinity at Beta-1 adrenergic receptor in guinea pigs by [125I]CYP displacement
ChEMBL 231 1 1 5 0.8 Cc1cn2c(C)cnc2c(N2CCNCC2)n1 10.1021/jm00099a012
CHEMBL1195526 13666 0 None 1 3 Guinea pig 6.8 pKi = 6.8 Binding
Binding affinity at Beta-1 adrenergic receptor in guinea pigs by [125I]CYP displacementBinding affinity at Beta-1 adrenergic receptor in guinea pigs by [125I]CYP displacement
ChEMBL 231 1 1 5 0.8 Cc1cn2c(C)cnc2c(N2CCNCC2)n1 10.1021/jm00099a012
CHEMBL554785 13666 0 None 1 3 Guinea pig 6.8 pKi = 6.8 Binding
Binding affinity at Beta-1 adrenergic receptor in guinea pigs by [125I]CYP displacementBinding affinity at Beta-1 adrenergic receptor in guinea pigs by [125I]CYP displacement
ChEMBL 231 1 1 5 0.8 Cc1cn2c(C)cnc2c(N2CCNCC2)n1 10.1021/jm00099a012
2249 509 106 None -5 12 Human 6.8 pKi = 6.8 Binding
Binding affinity to human adrenergic beta1 receptor by radioligand displacement assayBinding affinity to human adrenergic beta1 receptor by radioligand displacement assay
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1016/j.ejmech.2013.01.044
255 509 106 None -5 12 Human 6.8 pKi = 6.8 Binding
Binding affinity to human adrenergic beta1 receptor by radioligand displacement assayBinding affinity to human adrenergic beta1 receptor by radioligand displacement assay
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1016/j.ejmech.2013.01.044
548 509 106 None -5 12 Human 6.8 pKi = 6.8 Binding
Binding affinity to human adrenergic beta1 receptor by radioligand displacement assayBinding affinity to human adrenergic beta1 receptor by radioligand displacement assay
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1016/j.ejmech.2013.01.044
CHEMBL24 509 106 None -5 12 Human 6.8 pKi = 6.8 Binding
Binding affinity to human adrenergic beta1 receptor by radioligand displacement assayBinding affinity to human adrenergic beta1 receptor by radioligand displacement assay
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1016/j.ejmech.2013.01.044
DB00335 509 106 None -5 12 Human 6.8 pKi = 6.8 Binding
Binding affinity to human adrenergic beta1 receptor by radioligand displacement assayBinding affinity to human adrenergic beta1 receptor by radioligand displacement assay
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1016/j.ejmech.2013.01.044
52943919 17524 0 None -25 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta-1 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 -25 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta-1 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
10273469 93806 0 None 3 2 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]iodocyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human adrenergic beta-1 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 6.8 pKi = 6.8 Binding
Displacement of [125I]iodocyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human adrenergic beta-1 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
155521165 169980 0 None 14 2 Mouse 6.8 pKi = 6.8 Binding
Displacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T 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 Mouse 6.8 pKi = 6.8 Binding
Displacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T 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
127046949 139366 0 None -23 6 Mouse 6.8 pKi = 6.8 Binding
Displacement of [3H]CGP12177 from mouse beta1 receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from mouse beta1 receptor expressed in HEK293 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 -23 6 Mouse 6.8 pKi = 6.8 Binding
Displacement of [3H]CGP12177 from mouse beta1 receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from mouse beta1 receptor expressed in HEK293 cells
ChEMBL 472 12 3 5 4.6 COc1cc(CCNCCc2ccc(O)c3[nH]c(=O)ccc23)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
6603820 95317 13 None -162 13 Human 5.8 pKi = 5.8 Binding
Binding affinity against Beta-1 adrenergic receptorBinding affinity against Beta-1 adrenergic receptor
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1021/jm00018a002
CHEMBL25856 95317 13 None -162 13 Human 5.8 pKi = 5.8 Binding
Binding affinity against Beta-1 adrenergic receptorBinding affinity against Beta-1 adrenergic receptor
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1021/jm00018a002
44444179 93695 0 None -39 3 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]iodocyanopindolol from human cloned adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human cloned adrenergic beta-1 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 -39 3 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]iodocyanopindolol from human cloned adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human cloned adrenergic beta-1 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
127047221 139387 0 None -6 6 Mouse 5.8 pKi = 5.8 Binding
Displacement of [3H]CGP12177 from mouse beta1 receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from mouse beta1 receptor expressed in HEK293 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 -6 6 Mouse 5.8 pKi = 5.8 Binding
Displacement of [3H]CGP12177 from mouse beta1 receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from mouse beta1 receptor expressed in HEK293 cells
ChEMBL 319 8 4 6 1.8 COc1ccccc1OCCNC[C@@H](O)c1ccc(O)c(O)c1 10.1016/j.bmc.2016.04.028
594115 19164 2 None 3 2 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]dihydroalprenolol from adrenergic beta 1 receptor of rat cerebral cortical membranesDisplacement of [3H]dihydroalprenolol from adrenergic beta 1 receptor of rat cerebral cortical 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 5.8 pKi = 5.8 Binding
Displacement of [3H]dihydroalprenolol from adrenergic beta 1 receptor of rat cerebral cortical membranesDisplacement of [3H]dihydroalprenolol from adrenergic beta 1 receptor of rat cerebral cortical membranes
ChEMBL 187 2 4 4 0.2 NCC(O)c1cc(O)c(O)c(F)c1 10.1021/jm00076a024
3042920 203289 10 None -1 2 Rat 4.8 pKi = 4.8 Binding
Compound was evaluated for beta adrenergic binding affinity towards beta-1 receptor of rat brainCompound was evaluated for beta adrenergic binding affinity towards beta-1 receptor of rat brain
ChEMBL 195 1 3 4 0.8 Oc1ccc(C2CNCCO2)cc1O 10.1021/jm00084a006
CHEMBL7681 203289 10 None -1 2 Rat 4.8 pKi = 4.8 Binding
Compound was evaluated for beta adrenergic binding affinity towards beta-1 receptor of rat brainCompound was evaluated for beta adrenergic binding affinity towards beta-1 receptor of rat brain
ChEMBL 195 1 3 4 0.8 Oc1ccc(C2CNCCO2)cc1O 10.1021/jm00084a006
49864414 15453 0 None -37 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 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 5.8 pKi = 5.8 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 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
2249 509 106 None -5 12 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-CGP12177 from human beta1 ADR expressed in HEK293T cell membranes after 90 mins by scintillation countingDisplacement of [3H]-CGP12177 from human beta1 ADR expressed in HEK293T cell membranes 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 -5 12 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-CGP12177 from human beta1 ADR expressed in HEK293T cell membranes after 90 mins by scintillation countingDisplacement of [3H]-CGP12177 from human beta1 ADR expressed in HEK293T cell membranes 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 -5 12 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-CGP12177 from human beta1 ADR expressed in HEK293T cell membranes after 90 mins by scintillation countingDisplacement of [3H]-CGP12177 from human beta1 ADR expressed in HEK293T cell membranes 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 -5 12 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-CGP12177 from human beta1 ADR expressed in HEK293T cell membranes after 90 mins by scintillation countingDisplacement of [3H]-CGP12177 from human beta1 ADR expressed in HEK293T cell membranes 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 -5 12 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-CGP12177 from human beta1 ADR expressed in HEK293T cell membranes after 90 mins by scintillation countingDisplacement of [3H]-CGP12177 from human beta1 ADR expressed in HEK293T cell membranes 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
145946991 167039 0 None 1 2 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]-CGP12177 from human beta1 ADR expressed in HEK293T cell membranes after 90 mins by scintillation countingDisplacement of [3H]-CGP12177 from human beta1 ADR expressed in HEK293T cell membranes 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 4.8 pKi = 4.8 Binding
Displacement of [3H]-CGP12177 from human beta1 ADR expressed in HEK293T cell membranes after 90 mins by scintillation countingDisplacement of [3H]-CGP12177 from human beta1 ADR expressed in HEK293T cell membranes 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 4.8 pKi = 4.8 Binding
Displacement of [3H]-CGP12177 from human beta1 ADR expressed in HEK293T cell membranes after 90 mins by scintillation countingDisplacement of [3H]-CGP12177 from human beta1 ADR expressed in HEK293T cell membranes 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
44444393 165851 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]iodocyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human adrenergic beta-1 receptor expressed in CHO cells
ChEMBL 353 8 2 6 3.1 Cc1nc(-c2ccc(OCCNC[C@H](O)c3cccnc3)cc2)c(C)o1 10.1016/j.bmcl.2007.06.072
CHEMBL427711 165851 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]iodocyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human adrenergic beta-1 receptor expressed in CHO cells
ChEMBL 353 8 2 6 3.1 Cc1nc(-c2ccc(OCCNC[C@H](O)c3cccnc3)cc2)c(C)o1 10.1016/j.bmcl.2007.06.072
145947060 167047 0 None - 1 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]-CGP-12177 from adrenergic beta1 receptor in Wistar rat cortex incubated for 60 mins by microbeta liquid scintillation counting analysisDisplacement of [3H]-CGP-12177 from adrenergic beta1 receptor in Wistar rat cortex incubated for 60 mins by microbeta liquid scintillation counting analysis
ChEMBL 431 6 1 7 2.9 O=c1c2ccccc2oc2cc(OCC(O)CN3CCN(c4ccccn4)CC3)ccc12 10.1016/j.bmc.2018.04.038
CHEMBL4126157 167047 0 None - 1 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]-CGP-12177 from adrenergic beta1 receptor in Wistar rat cortex incubated for 60 mins by microbeta liquid scintillation counting analysisDisplacement of [3H]-CGP-12177 from adrenergic beta1 receptor in Wistar rat cortex incubated for 60 mins by microbeta liquid scintillation counting analysis
ChEMBL 431 6 1 7 2.9 O=c1c2ccccc2oc2cc(OCC(O)CN3CCN(c4ccccn4)CC3)ccc12 10.1016/j.bmc.2018.04.038
CHEMBL4301323 167047 0 None - 1 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]-CGP-12177 from adrenergic beta1 receptor in Wistar rat cortex incubated for 60 mins by microbeta liquid scintillation counting analysisDisplacement of [3H]-CGP-12177 from adrenergic beta1 receptor in Wistar rat cortex incubated for 60 mins by microbeta liquid scintillation counting analysis
ChEMBL 431 6 1 7 2.9 O=c1c2ccccc2oc2cc(OCC(O)CN3CCN(c4ccccn4)CC3)ccc12 10.1016/j.bmc.2018.04.038
16735272 85371 0 None -46 2 Rat 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 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 Rat 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 337 6 4 4 3.5 C[C@@H](Cc1cccc2ccccc12)NC[C@H](O)c1cc(O)cc(O)c1 nan
16735272 85371 0 None -46 2 Rat 4.8 pKi = 4.8 Binding
Displacement of [3H]CGP-12177 from beta-1 adrenergic receptor in Sprague-Dawley rat cortical membraneDisplacement of [3H]CGP-12177 from beta-1 adrenergic receptor in Sprague-Dawley rat cortical membrane
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 Rat 4.8 pKi = 4.8 Binding
Displacement of [3H]CGP-12177 from beta-1 adrenergic receptor in Sprague-Dawley rat cortical membraneDisplacement of [3H]CGP-12177 from beta-1 adrenergic receptor in Sprague-Dawley rat cortical membrane
ChEMBL 337 6 4 4 3.5 C[C@@H](Cc1cccc2ccccc12)NC[C@H](O)c1cc(O)cc(O)c1 10.1021/jm070030d
1499 2052 43 None -46 17 Human 5.8 pKi = 5.8 Binding
Binding Affinity against human Beta-1 adrenergic receptor expressed in Chinese hamster ovary(CHO) cells was measured by using [125I]ICYP radioligandBinding Affinity against human Beta-1 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 -46 17 Human 5.8 pKi = 5.8 Binding
Binding Affinity against human Beta-1 adrenergic receptor expressed in Chinese hamster ovary(CHO) cells was measured by using [125I]ICYP radioligandBinding Affinity against human Beta-1 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 -46 17 Human 5.8 pKi = 5.8 Binding
Binding Affinity against human Beta-1 adrenergic receptor expressed in Chinese hamster ovary(CHO) cells was measured by using [125I]ICYP radioligandBinding Affinity against human Beta-1 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 -46 17 Human 5.8 pKi = 5.8 Binding
Binding Affinity against human Beta-1 adrenergic receptor expressed in Chinese hamster ovary(CHO) cells was measured by using [125I]ICYP radioligandBinding Affinity against human Beta-1 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 -46 17 Human 5.8 pKi = 5.8 Binding
Binding Affinity against human Beta-1 adrenergic receptor expressed in Chinese hamster ovary(CHO) cells was measured by using [125I]ICYP radioligandBinding Affinity against human Beta-1 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
44439167 90112 0 None -158 10 Human 5.8 pKi = 5.8 Binding
Binding affinity at adrenergic beta 1 receptorBinding affinity at adrenergic beta 1 receptor
ChEMBL 483 6 1 5 5.0 Cc1ccc2c(OCCN3CCC(Cc4cc(F)c5c(c4)NC(=O)CO5)CC3)cc(Cl)cc2n1 10.1016/j.bmcl.2006.11.031
CHEMBL238732 90112 0 None -158 10 Human 5.8 pKi = 5.8 Binding
Binding affinity at adrenergic beta 1 receptorBinding affinity at adrenergic beta 1 receptor
ChEMBL 483 6 1 5 5.0 Cc1ccc2c(OCCN3CCC(Cc4cc(F)c5c(c4)NC(=O)CO5)CC3)cc(Cl)cc2n1 10.1016/j.bmcl.2006.11.031
2736205 87094 70 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]dihydroalprenolol from human wild type beta1 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysisDisplacement of [3H]dihydroalprenolol from human wild type beta1 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysis
ChEMBL 222 3 1 4 1.1 COc1cc(OC)cc(N2CCNCC2)c1 10.1021/jm400140q
CHEMBL2335163 87094 70 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]dihydroalprenolol from human wild type beta1 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysisDisplacement of [3H]dihydroalprenolol from human wild type beta1 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysis
ChEMBL 222 3 1 4 1.1 COc1cc(OC)cc(N2CCNCC2)c1 10.1021/jm400140q
702318 87096 67 None -19 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]dihydroalprenolol from human wild type beta1 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysisDisplacement of [3H]dihydroalprenolol from human wild type beta1 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysis
ChEMBL 227 1 1 3 2.0 Cc1cc(N2CCNCC2)c2ccccc2n1 10.1021/jm400140q
CHEMBL2335165 87096 67 None -19 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]dihydroalprenolol from human wild type beta1 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysisDisplacement of [3H]dihydroalprenolol from human wild type beta1 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysis
ChEMBL 227 1 1 3 2.0 Cc1cc(N2CCNCC2)c2ccccc2n1 10.1021/jm400140q
59119410 111760 0 None -158 2 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]dihydroalprenolol from beta1 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta1 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 4.8 pKi = 4.8 Binding
Displacement of [3H]dihydroalprenolol from beta1 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta1 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
24885648 16940 0 None -17 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta-1 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 -17 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta-1 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
46889852 6439 0 None -79 3 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta-1 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta-1 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 7.8 pKi = 7.8 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta-1 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta-1 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
127045855 139121 0 None -1 6 Mouse 6.8 pKi = 6.8 Binding
Displacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T 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 Mouse 6.8 pKi = 6.8 Binding
Displacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T 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 Mouse 6.8 pKi = 6.8 Binding
Displacement of [3H]CGP12177 from mouse beta1 receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from mouse beta1 receptor expressed in HEK293 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 Mouse 6.8 pKi = 6.8 Binding
Displacement of [3H]CGP12177 from mouse beta1 receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from mouse beta1 receptor expressed in HEK293 cells
ChEMBL 319 8 4 6 1.8 COc1ccccc1OCCNC[C@H](O)c1ccc(O)c(O)c1 10.1016/j.bmc.2016.04.028
10459124 167419 0 None - 1 Human 6.8 pKi = 6.8 Binding
Inhibition of [3H]dihydroalprenolol binding to beta 1 adrenoceptor from turkey erythrocyte membranes.Inhibition of [3H]dihydroalprenolol binding to beta 1 adrenoceptor from turkey erythrocyte membranes.
ChEMBL 513 11 4 7 1.4 NS(=O)(=O)c1cc(S(=O)(=O)NCCNCC(O)COc2cccc3ccccc23)ccc1Cl 10.1021/jm00053a020
CHEMBL43196 167419 0 None - 1 Human 6.8 pKi = 6.8 Binding
Inhibition of [3H]dihydroalprenolol binding to beta 1 adrenoceptor from turkey erythrocyte membranes.Inhibition of [3H]dihydroalprenolol binding to beta 1 adrenoceptor from turkey erythrocyte membranes.
ChEMBL 513 11 4 7 1.4 NS(=O)(=O)c1cc(S(=O)(=O)NCCNCC(O)COc2cccc3ccccc23)ccc1Cl 10.1021/jm00053a020
1960 2805 64 None -144 26 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]dihydroalprenolol from adrenergic beta 1 receptor of rat cerebral cortical membranesDisplacement of [3H]dihydroalprenolol from adrenergic beta 1 receptor of rat cerebral cortical membranes
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00076a024
439260 2805 64 None -144 26 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]dihydroalprenolol from adrenergic beta 1 receptor of rat cerebral cortical membranesDisplacement of [3H]dihydroalprenolol from adrenergic beta 1 receptor of rat cerebral cortical membranes
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00076a024
505 2805 64 None -144 26 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]dihydroalprenolol from adrenergic beta 1 receptor of rat cerebral cortical membranesDisplacement of [3H]dihydroalprenolol from adrenergic beta 1 receptor of rat cerebral cortical membranes
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00076a024
CHEMBL1437 2805 64 None -144 26 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]dihydroalprenolol from adrenergic beta 1 receptor of rat cerebral cortical membranesDisplacement of [3H]dihydroalprenolol from adrenergic beta 1 receptor of rat cerebral cortical membranes
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00076a024
DB00368 2805 64 None -144 26 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]dihydroalprenolol from adrenergic beta 1 receptor of rat cerebral cortical membranesDisplacement of [3H]dihydroalprenolol from adrenergic beta 1 receptor of rat cerebral cortical membranes
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00076a024
53379897 63300 0 None -40 2 Rat 4.8 pKi = 4.8 Binding
Displacement of [3H]CGP-12177 from beta1-adrenergic receptor in Sprague-Dawley rat cortical membrane after 2 hrsDisplacement of [3H]CGP-12177 from beta1-adrenergic receptor in Sprague-Dawley rat cortical membrane after 2 hrs
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 Rat 4.8 pKi = 4.8 Binding
Displacement of [3H]CGP-12177 from beta1-adrenergic receptor in Sprague-Dawley rat cortical membrane after 2 hrsDisplacement of [3H]CGP-12177 from beta1-adrenergic receptor in Sprague-Dawley rat cortical membrane after 2 hrs
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
49864332 15421 0 None -6 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 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 6.8 pKi = 6.8 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 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
49864396 15448 0 None -25 3 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 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 7.8 pKi = 7.8 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 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 7.8 pKi = 7.8 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 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 7.8 pKi = 7.8 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 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
49864441 15458 0 None -4 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 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 7.8 pKi = 7.8 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 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
14823035 141019 2 None -52 3 Human 6.8 pKi = 6.8 Binding
Ability to bind to human Beta-1 adrenergic receptor using membranes of stably transfected CHO cellsAbility to bind to human Beta-1 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 6.8 pKi = 6.8 Binding
Ability to bind to human Beta-1 adrenergic receptor using membranes of stably transfected CHO cellsAbility to bind to human Beta-1 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
10379016 16300 2 None 1 3 Guinea pig 6.8 pKi = 6.8 Binding
Binding affinity at Beta-1 adrenergic receptor in guinea pigs by [125I]CYP displacementBinding affinity at Beta-1 adrenergic receptor in guinea pigs by [125I]CYP displacement
ChEMBL 281 1 1 5 0.9 Brc1cnc(N2CCNCC2)c2nccn12 10.1021/jm00099a012
CHEMBL123566 16300 2 None 1 3 Guinea pig 6.8 pKi = 6.8 Binding
Binding affinity at Beta-1 adrenergic receptor in guinea pigs by [125I]CYP displacementBinding affinity at Beta-1 adrenergic receptor in guinea pigs by [125I]CYP displacement
ChEMBL 281 1 1 5 0.9 Brc1cnc(N2CCNCC2)c2nccn12 10.1021/jm00099a012
90469115 185250 2 None -56 17 Human 6.8 pKi = 6.8 Binding
Binding affinity to human adrenergic beta1 receptorBinding affinity to human adrenergic beta1 receptor
ChEMBL 410 3 1 6 3.0 O=S(=O)(c1cccc(F)c1)n1ccc2c(N3CCNCC3)nc3ccccc3c21 10.1021/acs.jmedchem.1c00224
CHEMBL4867565 185250 2 None -56 17 Human 6.8 pKi = 6.8 Binding
Binding affinity to human adrenergic beta1 receptorBinding affinity to human adrenergic beta1 receptor
ChEMBL 410 3 1 6 3.0 O=S(=O)(c1cccc(F)c1)n1ccc2c(N3CCNCC3)nc3ccccc3c21 10.1021/acs.jmedchem.1c00224
46889701 6983 0 None -1 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta-1 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta-1 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 6.8 pKi = 6.8 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta-1 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta-1 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
10131985 154091 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]iodocyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human adrenergic beta-1 receptor expressed in CHO cells
ChEMBL 339 8 2 6 2.7 Cc1ocnc1-c1ccc(OCCNC[C@H](O)c2cccnc2)cc1 10.1016/j.bmcl.2007.06.072
CHEMBL399440 154091 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]iodocyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human adrenergic beta-1 receptor expressed in CHO cells
ChEMBL 339 8 2 6 2.7 Cc1ocnc1-c1ccc(OCCNC[C@H](O)c2cccnc2)cc1 10.1016/j.bmcl.2007.06.072
2249 509 106 None -5 12 Human 6.8 pKi = 6.8 Binding
Displacement of [3H](-)-CGP12177 from human adrenergic beta1 receptorDisplacement of [3H](-)-CGP12177 from human adrenergic beta1 receptor
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1021/jm2006782
255 509 106 None -5 12 Human 6.8 pKi = 6.8 Binding
Displacement of [3H](-)-CGP12177 from human adrenergic beta1 receptorDisplacement of [3H](-)-CGP12177 from human adrenergic beta1 receptor
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1021/jm2006782
548 509 106 None -5 12 Human 6.8 pKi = 6.8 Binding
Displacement of [3H](-)-CGP12177 from human adrenergic beta1 receptorDisplacement of [3H](-)-CGP12177 from human adrenergic beta1 receptor
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1021/jm2006782
CHEMBL24 509 106 None -5 12 Human 6.8 pKi = 6.8 Binding
Displacement of [3H](-)-CGP12177 from human adrenergic beta1 receptorDisplacement of [3H](-)-CGP12177 from human adrenergic beta1 receptor
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1021/jm2006782
DB00335 509 106 None -5 12 Human 6.8 pKi = 6.8 Binding
Displacement of [3H](-)-CGP12177 from human adrenergic beta1 receptorDisplacement of [3H](-)-CGP12177 from human adrenergic beta1 receptor
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1021/jm2006782
16736094 85343 0 None -9 2 Rat 4.8 pKi = 4.8 Binding
Displacement of [3H]CGP-12177 from beta-1 adrenergic receptor in Sprague-Dawley rat cortical membraneDisplacement of [3H]CGP-12177 from beta-1 adrenergic receptor in Sprague-Dawley rat cortical membrane
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 Rat 4.8 pKi = 4.8 Binding
Displacement of [3H]CGP-12177 from beta-1 adrenergic receptor in Sprague-Dawley rat cortical membraneDisplacement of [3H]CGP-12177 from beta-1 adrenergic receptor in Sprague-Dawley rat cortical membrane
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 Rat 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 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 Rat 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 302 6 5 5 1.9 C[C@H](Cc1cccc(N)c1)NC[C@H](O)c1cc(O)cc(O)c1 nan
118710936 113234 0 None -29 3 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 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 7.8 pKi = 7.8 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 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
319 1292 39 None -154 9 Human 6.8 pKi = 6.8 Binding
Binding affinity to human beta1-adrenoceptor by radioligand binding assayBinding affinity to human beta1-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 -154 9 Human 6.8 pKi = 6.8 Binding
Binding affinity to human beta1-adrenoceptor by radioligand binding assayBinding affinity to human beta1-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 -154 9 Human 6.8 pKi = 6.8 Binding
Binding affinity to human beta1-adrenoceptor by radioligand binding assayBinding affinity to human beta1-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 -154 9 Human 6.8 pKi = 6.8 Binding
Binding affinity to human beta1-adrenoceptor by radioligand binding assayBinding affinity to human beta1-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 -154 9 Human 6.8 pKi = 6.8 Binding
Binding affinity to human beta1-adrenoceptor by radioligand binding assayBinding affinity to human beta1-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 -154 9 Human 6.8 pKi = 6.8 Binding
Binding affinity to human beta1-adrenoceptor by radioligand binding assayBinding affinity to human beta1-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
127045854 139021 0 None -13 6 Mouse 6.8 pKi = 6.8 Binding
Displacement of [3H]CGP12177 from mouse beta1 receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from mouse beta1 receptor expressed in HEK293 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 Mouse 6.8 pKi = 6.8 Binding
Displacement of [3H]CGP12177 from mouse beta1 receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from mouse beta1 receptor expressed in HEK293 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
10420352 168164 10 None -6 4 Guinea pig 5.8 pKi = 5.8 Binding
Binding affinity against beta-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of Dihydro-[3H]-alprenololBinding affinity against beta-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of Dihydro-[3H]-alprenolol
ChEMBL 201 3 4 4 0.5 CNCC(O)c1ccc(O)c(O)c1F 10.1021/jm00118a019
CHEMBL43711 168164 10 None -6 4 Guinea pig 5.8 pKi = 5.8 Binding
Binding affinity against beta-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of Dihydro-[3H]-alprenololBinding affinity against beta-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of Dihydro-[3H]-alprenolol
ChEMBL 201 3 4 4 0.5 CNCC(O)c1ccc(O)c(O)c1F 10.1021/jm00118a019
10420352 168164 10 None -6 4 Rat 5.8 pKi = 5.8 Binding
Binding of [3H]dihydroalprenolol to beta-1 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-1 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 Rat 5.8 pKi = 5.8 Binding
Binding of [3H]dihydroalprenolol to beta-1 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-1 adrenergic receptor of rat cerebral cortical membranes
ChEMBL 201 3 4 4 0.5 CNCC(O)c1ccc(O)c(O)c1F 10.1021/jm990599h
10420352 168164 10 None -6 4 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]dihydroalprenolol from adrenergic beta 1 receptor of rat cerebral cortical membranesDisplacement of [3H]dihydroalprenolol from adrenergic beta 1 receptor of rat cerebral cortical membranes
ChEMBL 201 3 4 4 0.5 CNCC(O)c1ccc(O)c(O)c1F 10.1021/jm00076a024
CHEMBL43711 168164 10 None -6 4 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]dihydroalprenolol from adrenergic beta 1 receptor of rat cerebral cortical membranesDisplacement of [3H]dihydroalprenolol from adrenergic beta 1 receptor of rat cerebral cortical membranes
ChEMBL 201 3 4 4 0.5 CNCC(O)c1ccc(O)c(O)c1F 10.1021/jm00076a024
10051943 16134 0 None -602 3 Human 6.7 pKi = 6.7 Binding
Binding affinity for human Beta-1 adrenergic receptor expressed in CHO cells by radioligand competition binding assays using [125I]iodocyanopindolol (ICYP).) PR = potency ratio relative to TMQBinding affinity for human Beta-1 adrenergic receptor expressed in CHO cells by radioligand competition binding assays using [125I]iodocyanopindolol (ICYP).) PR = potency ratio relative to TMQ
ChEMBL 507 2 3 3 3.7 Oc1cc2c(cc1O)C(Cc1cc(I)cc(I)c1)NCC2 10.1021/jm960208o
CHEMBL122757 16134 0 None -602 3 Human 6.7 pKi = 6.7 Binding
Binding affinity for human Beta-1 adrenergic receptor expressed in CHO cells by radioligand competition binding assays using [125I]iodocyanopindolol (ICYP).) PR = potency ratio relative to TMQBinding affinity for human Beta-1 adrenergic receptor expressed in CHO cells by radioligand competition binding assays using [125I]iodocyanopindolol (ICYP).) PR = potency ratio relative to TMQ
ChEMBL 507 2 3 3 3.7 Oc1cc2c(cc1O)C(Cc1cc(I)cc(I)c1)NCC2 10.1021/jm960208o
70684846 77246 9 None -4 2 Human 6.7 pKi = 6.7 Binding
Binding affinity to human beta1-adrenoceptor by radioligand binding assayBinding affinity to human beta1-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 6.7 pKi = 6.7 Binding
Binding affinity to human beta1-adrenoceptor by radioligand binding assayBinding affinity to human beta1-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
49864440 15457 0 None -29 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 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 6.7 pKi = 6.7 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 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
127035062 135915 0 None -66 19 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]CGP12177 human recombinant beta 1 adrenergic recptor expressed in CHO Flp-In cells after 90 mins by scintillation counting methodDisplacement of [3H]CGP12177 human recombinant beta 1 adrenergic recptor expressed in CHO Flp-In cells after 90 mins by scintillation counting method
ChEMBL 447 12 0 5 5.2 COc1ccc(CCN(CCCc2ccccc2)CCc2ccc3c(c2)OCO3)cc1OC 10.1039/C4MD00418C
CHEMBL3735756 135915 0 None -66 19 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]CGP12177 human recombinant beta 1 adrenergic recptor expressed in CHO Flp-In cells after 90 mins by scintillation counting methodDisplacement of [3H]CGP12177 human recombinant beta 1 adrenergic recptor expressed in CHO Flp-In cells after 90 mins by scintillation counting method
ChEMBL 447 12 0 5 5.2 COc1ccc(CCN(CCCc2ccccc2)CCc2ccc3c(c2)OCO3)cc1OC 10.1039/C4MD00418C
688467 85357 2 None -14 2 Rat 4.7 pKi = 4.7 Binding
Displacement of [3H]CGP-12177 from beta-1 adrenergic receptor in Sprague-Dawley rat cortical membraneDisplacement of [3H]CGP-12177 from beta-1 adrenergic receptor in Sprague-Dawley rat cortical membrane
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 Rat 4.7 pKi = 4.7 Binding
Displacement of [3H]CGP-12177 from beta-1 adrenergic receptor in Sprague-Dawley rat cortical membraneDisplacement of [3H]CGP-12177 from beta-1 adrenergic receptor in Sprague-Dawley rat cortical membrane
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 Rat 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 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 Rat 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 303 6 5 5 2.1 C[C@@H](Cc1ccc(O)cc1)NC[C@H](O)c1cc(O)cc(O)c1 nan
132060734 162562 0 None -6 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-Pindolol from human adrenergic beta1 receptor expressed in Flp-In CHO cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-Pindolol from human adrenergic beta1 receptor expressed in Flp-In CHO cells after 90 mins by microbeta scintillation counting method
ChEMBL 391 5 0 4 4.0 C=C(C)CN1CCN(c2ccc3c(c2)CN(C(=O)OCc2ccccc2)C3)CC1 10.1016/j.ejmech.2018.02.024
CHEMBL4177497 162562 0 None -6 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-Pindolol from human adrenergic beta1 receptor expressed in Flp-In CHO cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-Pindolol from human adrenergic beta1 receptor expressed in Flp-In CHO cells after 90 mins by microbeta scintillation counting method
ChEMBL 391 5 0 4 4.0 C=C(C)CN1CCN(c2ccc3c(c2)CN(C(=O)OCc2ccccc2)C3)CC1 10.1016/j.ejmech.2018.02.024
145990586 166279 0 None -1 11 Human 7.7 pKi = 7.7 Binding
Binding affinity to andrenergic beta1 receptor (unknown origin) assessed as inhibition of radioligand binding by radioligand competition binding assayBinding affinity to andrenergic beta1 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 7.7 pKi = 7.7 Binding
Binding affinity to andrenergic beta1 receptor (unknown origin) assessed as inhibition of radioligand binding by radioligand competition binding assayBinding affinity to andrenergic beta1 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
46889729 6984 0 None -3 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta-1 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta-1 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 6.7 pKi = 6.7 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta-1 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta-1 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
205951 154679 18 None - 1 Rat 4.7 pKi = 4.7 Binding
Binding of [3H]dihydroalprenolol to beta-1 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-1 adrenergic receptor of rat cerebral cortical membranes
ChEMBL 171 2 3 3 0.7 NCCc1ccc(O)c(O)c1F 10.1021/jm990599h
CHEMBL40268 154679 18 None - 1 Rat 4.7 pKi = 4.7 Binding
Binding of [3H]dihydroalprenolol to beta-1 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-1 adrenergic receptor of rat cerebral cortical membranes
ChEMBL 171 2 3 3 0.7 NCCc1ccc(O)c(O)c1F 10.1021/jm990599h
1499 2052 43 None -46 17 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C nan
3779 2052 43 None -46 17 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C nan
536 2052 43 None -46 17 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C nan
CHEMBL434 2052 43 None -46 17 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C nan
DB01064 2052 43 None -46 17 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C nan
8029710 87097 10 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]dihydroalprenolol from human wild type beta1 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysisDisplacement of [3H]dihydroalprenolol from human wild type beta1 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysis
ChEMBL 320 2 1 6 2.7 CSc1nc(N2CCNCC2)c2sc3c(c2n1)CCCC3 10.1021/jm400140q
CHEMBL2335166 87097 10 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]dihydroalprenolol from human wild type beta1 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysisDisplacement of [3H]dihydroalprenolol from human wild type beta1 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysis
ChEMBL 320 2 1 6 2.7 CSc1nc(N2CCNCC2)c2sc3c(c2n1)CCCC3 10.1021/jm400140q
1239 1639 46 None -63 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]dihydroalprenolol from beta1 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta1 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 5.7 pKi = 5.7 Binding
Displacement of [3H]dihydroalprenolol from beta1 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta1 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 5.7 pKi = 5.7 Binding
Displacement of [3H]dihydroalprenolol from beta1 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta1 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 5.7 pKi = 5.7 Binding
Displacement of [3H]dihydroalprenolol from beta1 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta1 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 5.7 pKi = 5.7 Binding
Displacement of [3H]dihydroalprenolol from beta1 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta1 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
10311070 111755 0 None -316 2 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]dihydroalprenolol from beta1 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta1 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 4.7 pKi = 4.7 Binding
Displacement of [3H]dihydroalprenolol from beta1 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta1 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
25266787 181050 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Displacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation methodDisplacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation method
ChEMBL 356 10 3 5 2.6 COc1ccccc1OCCNC[C@H](O)COc1cccc2[nH]ccc12 10.1016/j.ejmech.2008.05.019
CHEMBL477466 181050 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Displacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation methodDisplacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation method
ChEMBL 356 10 3 5 2.6 COc1ccccc1OCCNC[C@H](O)COc1cccc2[nH]ccc12 10.1016/j.ejmech.2008.05.019
49864358 15432 0 None -1 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 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 8.7 pKi = 8.7 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 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
9871887 102712 0 None -6 4 Human 8.7 pKi = 8.7 Binding
Binding affinity for human Beta-1 adrenergic receptor expressed in CHO cells by radioligand competition binding assays using [125I]iodocyanopindolol (ICYP).) PR = potency ratio relative to TMQBinding affinity for human Beta-1 adrenergic receptor expressed in CHO cells by radioligand competition binding assays using [125I]iodocyanopindolol (ICYP).) PR = potency ratio relative to TMQ
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-1 adrenergic receptor expressed in CHO cells by radioligand competition binding assays using [125I]iodocyanopindolol (ICYP).) PR = potency ratio relative to TMQBinding affinity for human Beta-1 adrenergic receptor expressed in CHO cells by radioligand competition binding assays using [125I]iodocyanopindolol (ICYP).) PR = potency ratio relative to TMQ
ChEMBL 537 3 3 4 3.7 COc1c(I)cc(CC2NCCc3cc(O)c(O)cc32)cc1I 10.1021/jm960208o
165193 3126 60 None -2 43 Human 8.6 pKi = 8.6 Binding
Inhibition of [3H]dihydroalprenolol binding to beta 1 adrenoceptor from turkey erythrocyte membranes.Inhibition of [3H]dihydroalprenolol binding to beta 1 adrenoceptor from turkey erythrocyte membranes.
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00053a020
2303 3126 60 None -2 43 Human 8.6 pKi = 8.6 Binding
Inhibition of [3H]dihydroalprenolol binding to beta 1 adrenoceptor from turkey erythrocyte membranes.Inhibition of [3H]dihydroalprenolol binding to beta 1 adrenoceptor from turkey erythrocyte membranes.
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00053a020
4946 3126 60 None -2 43 Human 8.6 pKi = 8.6 Binding
Inhibition of [3H]dihydroalprenolol binding to beta 1 adrenoceptor from turkey erythrocyte membranes.Inhibition of [3H]dihydroalprenolol binding to beta 1 adrenoceptor from turkey erythrocyte membranes.
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00053a020
564 3126 60 None -2 43 Human 8.6 pKi = 8.6 Binding
Inhibition of [3H]dihydroalprenolol binding to beta 1 adrenoceptor from turkey erythrocyte membranes.Inhibition of [3H]dihydroalprenolol binding to beta 1 adrenoceptor from turkey erythrocyte membranes.
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00053a020
62882 3126 60 None -2 43 Human 8.6 pKi = 8.6 Binding
Inhibition of [3H]dihydroalprenolol binding to beta 1 adrenoceptor from turkey erythrocyte membranes.Inhibition of [3H]dihydroalprenolol binding to beta 1 adrenoceptor from turkey erythrocyte membranes.
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00053a020
63 3126 60 None -2 43 Human 8.6 pKi = 8.6 Binding
Inhibition of [3H]dihydroalprenolol binding to beta 1 adrenoceptor from turkey erythrocyte membranes.Inhibition of [3H]dihydroalprenolol binding to beta 1 adrenoceptor from turkey erythrocyte membranes.
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00053a020
66366 3126 60 None -2 43 Human 8.6 pKi = 8.6 Binding
Inhibition of [3H]dihydroalprenolol binding to beta 1 adrenoceptor from turkey erythrocyte membranes.Inhibition of [3H]dihydroalprenolol binding to beta 1 adrenoceptor from turkey erythrocyte membranes.
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00053a020
91536 3126 60 None -2 43 Human 8.6 pKi = 8.6 Binding
Inhibition of [3H]dihydroalprenolol binding to beta 1 adrenoceptor from turkey erythrocyte membranes.Inhibition of [3H]dihydroalprenolol binding to beta 1 adrenoceptor from turkey erythrocyte membranes.
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00053a020
CHEMBL27 3126 60 None -2 43 Human 8.6 pKi = 8.6 Binding
Inhibition of [3H]dihydroalprenolol binding to beta 1 adrenoceptor from turkey erythrocyte membranes.Inhibition of [3H]dihydroalprenolol binding to beta 1 adrenoceptor from turkey erythrocyte membranes.
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00053a020
CHEMBL452861 3126 60 None -2 43 Human 8.6 pKi = 8.6 Binding
Inhibition of [3H]dihydroalprenolol binding to beta 1 adrenoceptor from turkey erythrocyte membranes.Inhibition of [3H]dihydroalprenolol binding to beta 1 adrenoceptor from turkey erythrocyte membranes.
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00053a020
DB00571 3126 60 None -2 43 Human 8.6 pKi = 8.6 Binding
Inhibition of [3H]dihydroalprenolol binding to beta 1 adrenoceptor from turkey erythrocyte membranes.Inhibition of [3H]dihydroalprenolol binding to beta 1 adrenoceptor from turkey erythrocyte membranes.
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00053a020
9860739 147717 1 None 1 3 Human 8.6 pKi = 8.6 Binding
Binding affinity at human adrenergic beta-1 receptorBinding affinity at human adrenergic beta-1 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 8.6 pKi = 8.6 Binding
Binding affinity at human adrenergic beta-1 receptorBinding affinity at human adrenergic beta-1 receptor
ChEMBL 288 6 3 3 2.8 O[C@@H](CNC1CCCCC1)COc1cccc2[nH]ccc12 10.1016/j.bmcl.2007.07.086
165193 3126 60 None -4 43 Mouse 8.6 pKi = 8.6 Binding
Displacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T 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 -4 43 Mouse 8.6 pKi = 8.6 Binding
Displacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T 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 -4 43 Mouse 8.6 pKi = 8.6 Binding
Displacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T 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 -4 43 Mouse 8.6 pKi = 8.6 Binding
Displacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T 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 -4 43 Mouse 8.6 pKi = 8.6 Binding
Displacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T 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 -4 43 Mouse 8.6 pKi = 8.6 Binding
Displacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T 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 -4 43 Mouse 8.6 pKi = 8.6 Binding
Displacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T 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 -4 43 Mouse 8.6 pKi = 8.6 Binding
Displacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T 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 -4 43 Mouse 8.6 pKi = 8.6 Binding
Displacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T 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 -4 43 Mouse 8.6 pKi = 8.6 Binding
Displacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T 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 -4 43 Mouse 8.6 pKi = 8.6 Binding
Displacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranes
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmc.2019.05.034
155512746 169094 0 None 19 2 Mouse 8.6 pKi = 8.6 Binding
Displacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T 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 Mouse 8.6 pKi = 8.6 Binding
Displacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T 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
131645 31922 7 None 1 2 Rat 7.7 pKi = 7.7 Binding
Compound was evaluated for its Beta-1 adrenergic receptor binding affinity by measuring the displacement of [3H]dihydroalprenolol binding in rat heartCompound was evaluated for its Beta-1 adrenergic receptor binding affinity by measuring the displacement of [3H]dihydroalprenolol binding in rat heart
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 Rat 7.7 pKi = 7.7 Binding
Compound was evaluated for its Beta-1 adrenergic receptor binding affinity by measuring the displacement of [3H]dihydroalprenolol binding in rat heartCompound was evaluated for its Beta-1 adrenergic receptor binding affinity by measuring the displacement of [3H]dihydroalprenolol binding in rat heart
ChEMBL 310 5 3 5 1.9 CC(C)(C)NCC(O)COc1cccc2c1SCC(=O)N2 10.1016/s0960-894x(00)00016-0
9858463 93687 0 None -19 2 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]iodocyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human adrenergic beta-1 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 6.7 pKi = 6.7 Binding
Displacement of [125I]iodocyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human adrenergic beta-1 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
52943969 17598 0 None -23 3 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta-1 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 -23 3 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta-1 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
2291 3123 52 None -11 12 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O nan
2561 3123 52 None -11 12 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O nan
4932 3123 52 None -11 12 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O nan
CHEMBL631 3123 52 None -11 12 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O nan
DB01182 3123 52 None -11 12 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O nan
46889728 6624 0 None -5 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta-1 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta-1 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 6.7 pKi = 6.7 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta-1 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta-1 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
118710951 113251 0 None 1 2 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 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 7.7 pKi = 7.7 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 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
172745 99648 7 None -5 6 Rat 6.7 pKi = 6.7 Binding
Binding of [3H]dihydroalprenolol to beta-1 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-1 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 -5 6 Rat 6.7 pKi = 6.7 Binding
Binding of [3H]dihydroalprenolol to beta-1 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-1 adrenergic receptor of rat cerebral cortical membranes
ChEMBL 187 2 4 4 0.2 NCC(O)c1ccc(O)c(O)c1F 10.1021/jm990599h
10155942 93867 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]iodocyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human adrenergic beta-1 receptor expressed in CHO cells
ChEMBL 369 10 2 7 2.6 COCc1nc(-c2ccc(OCCNC[C@H](O)c3cccnc3)cc2)co1 10.1016/j.bmcl.2007.06.072
CHEMBL250559 93867 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]iodocyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human adrenergic beta-1 receptor expressed in CHO cells
ChEMBL 369 10 2 7 2.6 COCc1nc(-c2ccc(OCCNC[C@H](O)c3cccnc3)cc2)co1 10.1016/j.bmcl.2007.06.072
72544787 92684 0 None -6 5 Pig 6.7 pKi = 6.7 Binding
Displacement of [3H]-prazosin from alpha1-adrenergic receptor in pig cerebral cortexDisplacement of [3H]-prazosin from alpha1-adrenergic receptor in pig cerebral cortex
ChEMBL 587 12 3 12 1.2 COc1ccccc1N1CCN(Cc2cn(-c3ccc(OCCCOC4O[C@H](CO)[C@@H](O)[C@H](O)[C@H]4F)cc3)nn2)CC1 10.1016/j.bmcl.2013.09.026
CHEMBL2443008 92684 0 None -6 5 Pig 6.7 pKi = 6.7 Binding
Displacement of [3H]-prazosin from alpha1-adrenergic receptor in pig cerebral cortexDisplacement of [3H]-prazosin from alpha1-adrenergic receptor in pig cerebral cortex
ChEMBL 587 12 3 12 1.2 COc1ccccc1N1CCN(Cc2cn(-c3ccc(OCCCOC4O[C@H](CO)[C@@H](O)[C@H](O)[C@H]4F)cc3)nn2)CC1 10.1016/j.bmcl.2013.09.026
72544789 92686 0 None -9 5 Pig 6.7 pKi = 6.7 Binding
Displacement of [3H]-prazosin from alpha1-adrenergic receptor in pig cerebral cortexDisplacement of [3H]-prazosin from alpha1-adrenergic receptor in pig cerebral cortex
ChEMBL 363 9 0 7 1.6 COc1ccccc1N1CCN(Cc2cn(CCOCCF)nn2)CC1 10.1016/j.bmcl.2013.09.026
CHEMBL2443010 92686 0 None -9 5 Pig 6.7 pKi = 6.7 Binding
Displacement of [3H]-prazosin from alpha1-adrenergic receptor in pig cerebral cortexDisplacement of [3H]-prazosin from alpha1-adrenergic receptor in pig cerebral cortex
ChEMBL 363 9 0 7 1.6 COc1ccccc1N1CCN(Cc2cn(CCOCCF)nn2)CC1 10.1016/j.bmcl.2013.09.026
1028 287 69 None -66 30 Rat 5.7 pKi = 5.7 Binding
Binding of [3H]dihydroalprenolol to beta-1 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-1 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 -66 30 Rat 5.7 pKi = 5.7 Binding
Binding of [3H]dihydroalprenolol to beta-1 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-1 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 -66 30 Rat 5.7 pKi = 5.7 Binding
Binding of [3H]dihydroalprenolol to beta-1 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-1 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 -66 30 Rat 5.7 pKi = 5.7 Binding
Binding of [3H]dihydroalprenolol to beta-1 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-1 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 -66 30 Rat 5.7 pKi = 5.7 Binding
Binding of [3H]dihydroalprenolol to beta-1 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-1 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 -66 30 Rat 5.7 pKi = 5.7 Binding
Binding of [3H]dihydroalprenolol to beta-1 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-1 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
145946965 167024 0 None - 1 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]-CGP-12177 from adrenergic beta1 receptor in Wistar rat cortex incubated for 60 mins by microbeta liquid scintillation counting analysisDisplacement of [3H]-CGP-12177 from adrenergic beta1 receptor in Wistar rat cortex incubated for 60 mins by microbeta liquid scintillation counting analysis
ChEMBL 431 6 1 7 2.9 O=c1c2ccccc2oc2c(OCC(O)CN3CCN(c4ccccn4)CC3)cccc12 10.1016/j.bmc.2018.04.038
CHEMBL4126588 167024 0 None - 1 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]-CGP-12177 from adrenergic beta1 receptor in Wistar rat cortex incubated for 60 mins by microbeta liquid scintillation counting analysisDisplacement of [3H]-CGP-12177 from adrenergic beta1 receptor in Wistar rat cortex incubated for 60 mins by microbeta liquid scintillation counting analysis
ChEMBL 431 6 1 7 2.9 O=c1c2ccccc2oc2c(OCC(O)CN3CCN(c4ccccn4)CC3)cccc12 10.1016/j.bmc.2018.04.038
CHEMBL4300897 167024 0 None - 1 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]-CGP-12177 from adrenergic beta1 receptor in Wistar rat cortex incubated for 60 mins by microbeta liquid scintillation counting analysisDisplacement of [3H]-CGP-12177 from adrenergic beta1 receptor in Wistar rat cortex incubated for 60 mins by microbeta liquid scintillation counting analysis
ChEMBL 431 6 1 7 2.9 O=c1c2ccccc2oc2c(OCC(O)CN3CCN(c4ccccn4)CC3)cccc12 10.1016/j.bmc.2018.04.038
93601 87089 96 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]dihydroalprenolol from human wild type beta1 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysisDisplacement of [3H]dihydroalprenolol from human wild type beta1 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysis
ChEMBL 230 1 1 2 2.4 Clc1ccc(N2CCNCC2)cc1Cl 10.1021/jm400140q
CHEMBL2335159 87089 96 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]dihydroalprenolol from human wild type beta1 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysisDisplacement of [3H]dihydroalprenolol from human wild type beta1 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysis
ChEMBL 230 1 1 2 2.4 Clc1ccc(N2CCNCC2)cc1Cl 10.1021/jm400140q
21138 97986 34 None -4 7 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 259 6 2 3 2.6 CC(C)NC[C@@H](O)COc1cccc2ccccc12 nan
CHEMBL275742 97986 34 None -4 7 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 259 6 2 3 2.6 CC(C)NC[C@@H](O)COc1cccc2ccccc12 nan
52949488 17349 0 None -19 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta-1 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 -19 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta-1 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
44423646 84800 0 None -4 3 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]CYP from human adrenergic beta 1 receptor transfected in CHO cells in presence of 100 uM GTPDisplacement of [125I]CYP from human adrenergic beta 1 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 5.7 pKi = 5.7 Binding
Displacement of [125I]CYP from human adrenergic beta 1 receptor transfected in CHO cells in presence of 100 uM GTPDisplacement of [125I]CYP from human adrenergic beta 1 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
16735257 85290 0 None -151 2 Rat 4.7 pKi = 4.7 Binding
Displacement of [3H]CGP-12177 from beta-1 adrenergic receptor in Sprague-Dawley rat cortical membraneDisplacement of [3H]CGP-12177 from beta-1 adrenergic receptor in Sprague-Dawley rat cortical membrane
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 Rat 4.7 pKi = 4.7 Binding
Displacement of [3H]CGP-12177 from beta-1 adrenergic receptor in Sprague-Dawley rat cortical membraneDisplacement of [3H]CGP-12177 from beta-1 adrenergic receptor in Sprague-Dawley rat cortical membrane
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
16735257 85290 0 None -151 2 Rat 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 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 Rat 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 317 7 4 5 2.4 COc1ccc(C[C@@H](C)NC[C@H](O)c2cc(O)cc(O)c2)cc1 nan
155561031 174413 0 None -1 2 Mouse 7.7 pKi = 7.7 Binding
Displacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T 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 Mouse 7.7 pKi = 7.7 Binding
Displacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T 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
10465942 13419 0 None -1 3 Guinea pig 6.7 pKi = 6.7 Binding
Binding affinity at Beta-1 adrenergic receptor in guinea pigs by [125I]CYP displacementBinding affinity at Beta-1 adrenergic receptor in guinea pigs by [125I]CYP displacement
ChEMBL 217 1 1 5 0.4 Cc1cn2ccnc2c(N2CCNCC2)n1 10.1021/jm00099a012
CHEMBL1193821 13419 0 None -1 3 Guinea pig 6.7 pKi = 6.7 Binding
Binding affinity at Beta-1 adrenergic receptor in guinea pigs by [125I]CYP displacementBinding affinity at Beta-1 adrenergic receptor in guinea pigs by [125I]CYP displacement
ChEMBL 217 1 1 5 0.4 Cc1cn2ccnc2c(N2CCNCC2)n1 10.1021/jm00099a012
CHEMBL545289 13419 0 None -1 3 Guinea pig 6.7 pKi = 6.7 Binding
Binding affinity at Beta-1 adrenergic receptor in guinea pigs by [125I]CYP displacementBinding affinity at Beta-1 adrenergic receptor in guinea pigs by [125I]CYP displacement
ChEMBL 217 1 1 5 0.4 Cc1cn2ccnc2c(N2CCNCC2)n1 10.1021/jm00099a012
598754 48601 59 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to beta1 adrenergic receptor (unknown origin)Binding affinity to beta1 adrenergic receptor (unknown origin)
ChEMBL 227 1 1 3 2.0 Cc1cc(N2CCNCC2)nc2ccccc12 10.1021/jm400561w
CHEMBL1559535 48601 59 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to beta1 adrenergic receptor (unknown origin)Binding affinity to beta1 adrenergic receptor (unknown origin)
ChEMBL 227 1 1 3 2.0 Cc1cc(N2CCNCC2)nc2ccccc12 10.1021/jm400561w
443372 10123 23 None -1 3 Mouse 6.7 pKi = 6.7 Binding
Displacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T 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 Mouse 6.7 pKi = 6.7 Binding
Displacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T 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 Mouse 6.7 pKi = 6.7 Binding
Displacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T 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
155536406 171581 0 None 1 2 Mouse 6.7 pKi = 6.7 Binding
Displacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T 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 Mouse 6.7 pKi = 6.7 Binding
Displacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T 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
1499 2052 43 None -5 17 Mouse 6.7 pKi = 6.7 Binding
Displacement of [3H]CGP12177 from mouse beta1 receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from mouse beta1 receptor expressed in HEK293 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 -5 17 Mouse 6.7 pKi = 6.7 Binding
Displacement of [3H]CGP12177 from mouse beta1 receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from mouse beta1 receptor expressed in HEK293 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 -5 17 Mouse 6.7 pKi = 6.7 Binding
Displacement of [3H]CGP12177 from mouse beta1 receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from mouse beta1 receptor expressed in HEK293 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 -5 17 Mouse 6.7 pKi = 6.7 Binding
Displacement of [3H]CGP12177 from mouse beta1 receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from mouse beta1 receptor expressed in HEK293 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 -5 17 Mouse 6.7 pKi = 6.7 Binding
Displacement of [3H]CGP12177 from mouse beta1 receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from mouse beta1 receptor expressed in HEK293 cells
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2016.04.028
10103956 11081 0 None 2 2 Rat 5.7 pKi = 5.7 Binding
Binding affinity against beta-1-adrenergic receptor in rat brainBinding affinity against beta-1-adrenergic receptor in rat brain
ChEMBL 188 7 2 4 0.8 CC/C=N/OCC(O)CNC(C)C 10.1021/jm00036a018
CHEMBL1178707 11081 0 None 2 2 Rat 5.7 pKi = 5.7 Binding
Binding affinity against beta-1-adrenergic receptor in rat brainBinding affinity against beta-1-adrenergic receptor in rat brain
ChEMBL 188 7 2 4 0.8 CC/C=N/OCC(O)CNC(C)C 10.1021/jm00036a018
CHEMBL38114 11081 0 None 2 2 Rat 5.7 pKi = 5.7 Binding
Binding affinity against beta-1-adrenergic receptor in rat brainBinding affinity against beta-1-adrenergic receptor in rat brain
ChEMBL 188 7 2 4 0.8 CC/C=N/OCC(O)CNC(C)C 10.1021/jm00036a018
2389 3267 114 None -1023 68 Rat 4.7 pKi = 4.7 Binding
Binding affinity measured at the Beta-1 adrenergic receptor by the inhibition of [3H]DHA binding to rat cortex using unlabeled isoprenalin for nonspecific binding.Binding affinity measured at the Beta-1 adrenergic receptor by the inhibition of [3H]DHA binding to rat cortex using unlabeled isoprenalin for nonspecific binding.
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm9810396
5073 3267 114 None -1023 68 Rat 4.7 pKi = 4.7 Binding
Binding affinity measured at the Beta-1 adrenergic receptor by the inhibition of [3H]DHA binding to rat cortex using unlabeled isoprenalin for nonspecific binding.Binding affinity measured at the Beta-1 adrenergic receptor by the inhibition of [3H]DHA binding to rat cortex using unlabeled isoprenalin for nonspecific binding.
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm9810396
96 3267 114 None -1023 68 Rat 4.7 pKi = 4.7 Binding
Binding affinity measured at the Beta-1 adrenergic receptor by the inhibition of [3H]DHA binding to rat cortex using unlabeled isoprenalin for nonspecific binding.Binding affinity measured at the Beta-1 adrenergic receptor by the inhibition of [3H]DHA binding to rat cortex using unlabeled isoprenalin for nonspecific binding.
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm9810396
CHEMBL85 3267 114 None -1023 68 Rat 4.7 pKi = 4.7 Binding
Binding affinity measured at the Beta-1 adrenergic receptor by the inhibition of [3H]DHA binding to rat cortex using unlabeled isoprenalin for nonspecific binding.Binding affinity measured at the Beta-1 adrenergic receptor by the inhibition of [3H]DHA binding to rat cortex using unlabeled isoprenalin for nonspecific binding.
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm9810396
DB00734 3267 114 None -1023 68 Rat 4.7 pKi = 4.7 Binding
Binding affinity measured at the Beta-1 adrenergic receptor by the inhibition of [3H]DHA binding to rat cortex using unlabeled isoprenalin for nonspecific binding.Binding affinity measured at the Beta-1 adrenergic receptor by the inhibition of [3H]DHA binding to rat cortex using unlabeled isoprenalin for nonspecific binding.
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm9810396
598754 48601 59 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]dihydroalprenolol from human wild type beta1 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysisDisplacement of [3H]dihydroalprenolol from human wild type beta1 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysis
ChEMBL 227 1 1 3 2.0 Cc1cc(N2CCNCC2)nc2ccccc12 10.1021/jm400140q
CHEMBL1559535 48601 59 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]dihydroalprenolol from human wild type beta1 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysisDisplacement of [3H]dihydroalprenolol from human wild type beta1 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysis
ChEMBL 227 1 1 3 2.0 Cc1cc(N2CCNCC2)nc2ccccc12 10.1021/jm400140q
9866060 77245 0 None 1 2 Human 6.6 pKi = 6.6 Binding
Binding affinity to human beta1-adrenoceptor by radioligand binding assayBinding affinity to human beta1-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 6.6 pKi = 6.6 Binding
Binding affinity to human beta1-adrenoceptor by radioligand binding assayBinding affinity to human beta1-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
44423643 141512 0 None -8 3 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]CYP from human adrenergic beta 1 receptor transfected in CHO cells in presence of 100 uM GTPDisplacement of [125I]CYP from human adrenergic beta 1 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 7.6 pKi = 7.6 Binding
Displacement of [125I]CYP from human adrenergic beta 1 receptor transfected in CHO cells in presence of 100 uM GTPDisplacement of [125I]CYP from human adrenergic beta 1 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
44396659 67012 0 None -6 3 Human 6.6 pKi = 6.6 Binding
Binding inhibition constant was determined by inhibition of [125I]-iodocyanopindolol binding to Beta-1 adrenergic receptorBinding inhibition constant was determined by inhibition of [125I]-iodocyanopindolol binding to Beta-1 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 6.6 pKi = 6.6 Binding
Binding inhibition constant was determined by inhibition of [125I]-iodocyanopindolol binding to Beta-1 adrenergic receptorBinding inhibition constant was determined by inhibition of [125I]-iodocyanopindolol binding to Beta-1 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
52947060 17386 0 None -2 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta-1 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 -2 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta-1 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
2419 3394 80 None -162 6 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]-CYP from human beta1-adrenergic receptor expressed in COS-7 cells by gamma countingDisplacement of [125I]-CYP from human beta1-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 -162 6 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]-CYP from human beta1-adrenergic receptor expressed in COS-7 cells by gamma countingDisplacement of [125I]-CYP from human beta1-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 -162 6 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]-CYP from human beta1-adrenergic receptor expressed in COS-7 cells by gamma countingDisplacement of [125I]-CYP from human beta1-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 -162 6 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]-CYP from human beta1-adrenergic receptor expressed in COS-7 cells by gamma countingDisplacement of [125I]-CYP from human beta1-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 -162 6 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]-CYP from human beta1-adrenergic receptor expressed in COS-7 cells by gamma countingDisplacement of [125I]-CYP from human beta1-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
10431900 63294 0 None -10 2 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]-CYP from human beta1-adrenergic receptor expressed in COS-7 cells by gamma countingDisplacement of [125I]-CYP from human beta1-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 5.6 pKi = 5.6 Binding
Displacement of [125I]-CYP from human beta1-adrenergic receptor expressed in COS-7 cells by gamma countingDisplacement of [125I]-CYP from human beta1-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
53387674 64817 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]-Iodopindolol from beta1-adrenergic receptor after 1.5 hrs by liquid scintillation countingDisplacement of [125I]-Iodopindolol from beta1-adrenergic receptor after 1.5 hrs by liquid scintillation counting
ChEMBL 415 9 2 7 2.3 COc1ccc2nc(-c3ccc(OCC(O)CNC(C)CF)cc3)n(C)c(=O)c2c1 10.1016/j.bmcl.2011.06.106
CHEMBL1824265 64817 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]-Iodopindolol from beta1-adrenergic receptor after 1.5 hrs by liquid scintillation countingDisplacement of [125I]-Iodopindolol from beta1-adrenergic receptor after 1.5 hrs by liquid scintillation counting
ChEMBL 415 9 2 7 2.3 COc1ccc2nc(-c3ccc(OCC(O)CNC(C)CF)cc3)n(C)c(=O)c2c1 10.1016/j.bmcl.2011.06.106
127046952 139558 0 None -190 6 Mouse 5.6 pKi = 5.6 Binding
Displacement of [3H]CGP12177 from mouse beta1 receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from mouse beta1 receptor expressed in HEK293 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 -190 6 Mouse 5.6 pKi = 5.6 Binding
Displacement of [3H]CGP12177 from mouse beta1 receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from mouse beta1 receptor expressed in HEK293 cells
ChEMBL 421 12 3 5 4.5 COc1cc(CCNCCc2ccc(O)c(O)c2)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
541614 17815 1 None -3 2 Rat 5.6 pKi = 5.6 Binding
Displacement of [3H]dihydroalprenolol from adrenergic beta 1 receptor of rat cerebral cortical membranesDisplacement of [3H]dihydroalprenolol from adrenergic beta 1 receptor of rat cerebral cortical 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 5.6 pKi = 5.6 Binding
Displacement of [3H]dihydroalprenolol from adrenergic beta 1 receptor of rat cerebral cortical membranesDisplacement of [3H]dihydroalprenolol from adrenergic beta 1 receptor of rat cerebral cortical membranes
ChEMBL 219 3 4 4 0.6 CNCC(O)c1cc(F)c(O)c(O)c1F 10.1021/jm00076a024
11218492 87086 44 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]dihydroalprenolol from human wild type beta1 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysisDisplacement of [3H]dihydroalprenolol from human wild type beta1 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysis
ChEMBL 231 1 1 3 1.5 FC(F)(F)c1ccnc(N2CCNCC2)c1 10.1021/jm400140q
CHEMBL2335156 87086 44 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]dihydroalprenolol from human wild type beta1 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysisDisplacement of [3H]dihydroalprenolol from human wild type beta1 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysis
ChEMBL 231 1 1 3 1.5 FC(F)(F)c1ccnc(N2CCNCC2)c1 10.1021/jm400140q
24937013 17252 0 None -33 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta-1 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 -33 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta-1 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
56645363 120963 7 None -3 4 Human 5.6 pKi = 5.6 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000313b ADRB1Selectivity interaction (GPCR panel (PDSP screen)) EUB0000313b ADRB1
ChEMBL 311 3 1 4 3.8 CC(C)(O)c1cncc(-c2nc3ccc(F)cc3n2C2CC2)c1 nan
CHEMBL3582478 120963 7 None -3 4 Human 5.6 pKi = 5.6 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000313b ADRB1Selectivity interaction (GPCR panel (PDSP screen)) EUB0000313b ADRB1
ChEMBL 311 3 1 4 3.8 CC(C)(O)c1cncc(-c2nc3ccc(F)cc3n2C2CC2)c1 nan
1043 1545 13 None -26302 29 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
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 -26302 29 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
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 -26302 29 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
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 -26302 29 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
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 -26302 29 Human 5.6 pKi = 5.6 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
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
15461453 172232 0 None -4 2 Mouse 7.6 pKi = 7.6 Binding
Displacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T 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 Mouse 7.6 pKi = 7.6 Binding
Displacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T cells after 60 mins by radioligand competition binding assay
ChEMBL 390 10 2 4 4.8 COc1ccccc1OCCNCCCOc1cccc2[nH]c3ccccc3c12 10.1021/acs.jmedchem.9b00349
44288393 171078 0 None - 1 Human 7.6 pKi = 7.6 Binding
Inhibition of [3H]dihydroalprenolol binding to beta 1 adrenoceptor from turkey erythrocyte membranes.Inhibition of [3H]dihydroalprenolol binding to beta 1 adrenoceptor from turkey erythrocyte membranes.
ChEMBL 310 5 3 5 2.7 CC(C)(C)Nc1cccc2c1SC(OCCCO)C(=O)N2 10.1021/jm00053a020
CHEMBL446609 171078 0 None - 1 Human 7.6 pKi = 7.6 Binding
Inhibition of [3H]dihydroalprenolol binding to beta 1 adrenoceptor from turkey erythrocyte membranes.Inhibition of [3H]dihydroalprenolol binding to beta 1 adrenoceptor from turkey erythrocyte membranes.
ChEMBL 310 5 3 5 2.7 CC(C)(C)Nc1cccc2c1SC(OCCCO)C(=O)N2 10.1021/jm00053a020
10283146 106776 0 None -1 2 Human 6.6 pKi = 6.6 Binding
Binding affinity of compound against Beta-1 adrenergic receptor was determinedBinding affinity of compound against Beta-1 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 6.6 pKi = 6.6 Binding
Binding affinity of compound against Beta-1 adrenergic receptor was determinedBinding affinity of compound against Beta-1 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
68770 44384 49 None 1 2 Human 6.6 pKi = 6.6 Binding
Binding affinity to beta1 adrenergic receptor (unknown origin) by radioligand binding assayBinding affinity to beta1 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 6.6 pKi = 6.6 Binding
Binding affinity to beta1 adrenergic receptor (unknown origin) by radioligand binding assayBinding affinity to beta1 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
46889700 6982 0 None -18 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta-1 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta-1 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 6.6 pKi = 6.6 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta-1 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta-1 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
10082076 13733 0 None -10 3 Guinea pig 5.6 pKi = 5.6 Binding
Binding affinity at Beta-1 adrenergic receptor in guinea pigs by [125I]CYP displacementBinding affinity at Beta-1 adrenergic receptor in guinea pigs by [125I]CYP displacement
ChEMBL 217 1 1 5 0.4 Cc1cnc2c(N3CCNCC3)nccn12 10.1021/jm00099a012
CHEMBL1195953 13733 0 None -10 3 Guinea pig 5.6 pKi = 5.6 Binding
Binding affinity at Beta-1 adrenergic receptor in guinea pigs by [125I]CYP displacementBinding affinity at Beta-1 adrenergic receptor in guinea pigs by [125I]CYP displacement
ChEMBL 217 1 1 5 0.4 Cc1cnc2c(N3CCNCC3)nccn12 10.1021/jm00099a012
CHEMBL555637 13733 0 None -10 3 Guinea pig 5.6 pKi = 5.6 Binding
Binding affinity at Beta-1 adrenergic receptor in guinea pigs by [125I]CYP displacementBinding affinity at Beta-1 adrenergic receptor in guinea pigs by [125I]CYP displacement
ChEMBL 217 1 1 5 0.4 Cc1cnc2c(N3CCNCC3)nccn12 10.1021/jm00099a012
15580747 64816 0 None 2 3 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]-Iodopindolol from beta1-adrenergic receptor after 1.5 hrs by liquid scintillation countingDisplacement of [125I]-Iodopindolol from beta1-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 2 3 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]-Iodopindolol from beta1-adrenergic receptor after 1.5 hrs by liquid scintillation countingDisplacement of [125I]-Iodopindolol from beta1-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
155526662 170610 0 None -3 2 Mouse 5.6 pKi = 5.6 Binding
Displacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T 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 Mouse 5.6 pKi = 5.6 Binding
Displacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T 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
6603724 154780 3 None 1 3 Rat 4.6 pKi = 4.6 Binding
Binding of [3H]dihydroalprenolol to beta-1 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-1 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 Rat 4.6 pKi = 4.6 Binding
Binding of [3H]dihydroalprenolol to beta-1 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-1 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
46889768 6981 0 None -27 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta-1 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta-1 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 6.6 pKi = 6.6 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta-1 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta-1 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
16737411 142657 0 None -8 2 Rat 4.6 pKi = 4.6 Binding
Displacement of [3H]CGP-12177 from beta-1 adrenergic receptor in Sprague-Dawley rat cortical membraneDisplacement of [3H]CGP-12177 from beta-1 adrenergic receptor in Sprague-Dawley rat cortical membrane
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 Rat 4.6 pKi = 4.6 Binding
Displacement of [3H]CGP-12177 from beta-1 adrenergic receptor in Sprague-Dawley rat cortical membraneDisplacement of [3H]CGP-12177 from beta-1 adrenergic receptor in Sprague-Dawley rat cortical membrane
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 Rat 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
CHEMBL389629 142657 0 None -8 2 Rat 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
24321330 6743 0 None -1 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta-1 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta-1 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 beta-1 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta-1 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
46889771 6901 0 None -6 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta-1 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta-1 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 6.6 pKi = 6.6 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta-1 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta-1 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
72545010 92679 0 None -7 5 Pig 5.6 pKi = 5.6 Binding
Displacement of [3H]-prazosin from alpha1-adrenergic receptor in pig cerebral cortexDisplacement of [3H]-prazosin from alpha1-adrenergic receptor in pig cerebral cortex
ChEMBL 437 6 3 10 -0.4 COc1ccccc1N1CCN(Cc2cn([C@@H]3O[C@H](CF)[C@@H](O)[C@H](O)[C@H]3O)nn2)CC1 10.1016/j.bmcl.2013.09.026
CHEMBL2443003 92679 0 None -7 5 Pig 5.6 pKi = 5.6 Binding
Displacement of [3H]-prazosin from alpha1-adrenergic receptor in pig cerebral cortexDisplacement of [3H]-prazosin from alpha1-adrenergic receptor in pig cerebral cortex
ChEMBL 437 6 3 10 -0.4 COc1ccccc1N1CCN(Cc2cn([C@@H]3O[C@H](CF)[C@@H](O)[C@H](O)[C@H]3O)nn2)CC1 10.1016/j.bmcl.2013.09.026
172745 99648 7 None -5 6 Rat 5.6 pKi = 5.6 Binding
Displacement of [3H]dihydroalprenolol from adrenergic beta 1 receptor of rat cerebral cortical membranesDisplacement of [3H]dihydroalprenolol from adrenergic beta 1 receptor of rat cerebral cortical membranes
ChEMBL 187 2 4 4 0.2 NCC(O)c1ccc(O)c(O)c1F 10.1021/jm00076a024
CHEMBL287587 99648 7 None -5 6 Rat 5.6 pKi = 5.6 Binding
Displacement of [3H]dihydroalprenolol from adrenergic beta 1 receptor of rat cerebral cortical membranesDisplacement of [3H]dihydroalprenolol from adrenergic beta 1 receptor of rat cerebral cortical membranes
ChEMBL 187 2 4 4 0.2 NCC(O)c1ccc(O)c(O)c1F 10.1021/jm00076a024
24733400 87095 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]dihydroalprenolol from human wild type beta1 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysisDisplacement of [3H]dihydroalprenolol from human wild type beta1 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysis
ChEMBL 295 2 1 4 3.4 c1csc(-c2cccc3ccc(N4CCNCC4)nc23)c1 10.1021/jm400140q
CHEMBL2335164 87095 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]dihydroalprenolol from human wild type beta1 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysisDisplacement of [3H]dihydroalprenolol from human wild type beta1 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysis
ChEMBL 295 2 1 4 3.4 c1csc(-c2cccc3ccc(N4CCNCC4)nc23)c1 10.1021/jm400140q
10296414 3462 11 None -1995 9 Human 5.6 pKi = 5.6 Binding
Binding affinity at adrenergic beta 1 receptorBinding affinity at adrenergic beta 1 receptor
ChEMBL 431 6 1 5 4.2 O=C1COc2c(N1)cc(cc2)CC1CCN(CC1)CCOc1cccc2c1ccc(n2)C 10.1016/j.bmcl.2006.11.031
76 3462 11 None -1995 9 Human 5.6 pKi = 5.6 Binding
Binding affinity at adrenergic beta 1 receptorBinding affinity at adrenergic beta 1 receptor
ChEMBL 431 6 1 5 4.2 O=C1COc2c(N1)cc(cc2)CC1CCN(CC1)CCOc1cccc2c1ccc(n2)C 10.1016/j.bmcl.2006.11.031
CHEMBL183460 3462 11 None -1995 9 Human 5.6 pKi = 5.6 Binding
Binding affinity at adrenergic beta 1 receptorBinding affinity at adrenergic beta 1 receptor
ChEMBL 431 6 1 5 4.2 O=C1COc2c(N1)cc(cc2)CC1CCN(CC1)CCOc1cccc2c1ccc(n2)C 10.1016/j.bmcl.2006.11.031
44439165 145208 0 None -1000 8 Human 5.6 pKi = 5.6 Binding
Binding affinity at adrenergic beta 1 receptorBinding affinity at adrenergic beta 1 receptor
ChEMBL 483 6 1 5 5.0 Cc1ccc2c(OCCN3CCC(Cc4cc5c(cc4F)OCC(=O)N5)CC3)cc(Cl)cc2n1 10.1016/j.bmcl.2006.11.031
CHEMBL391661 145208 0 None -1000 8 Human 5.6 pKi = 5.6 Binding
Binding affinity at adrenergic beta 1 receptorBinding affinity at adrenergic beta 1 receptor
ChEMBL 483 6 1 5 5.0 Cc1ccc2c(OCCN3CCC(Cc4cc5c(cc4F)OCC(=O)N5)CC3)cc(Cl)cc2n1 10.1016/j.bmcl.2006.11.031
2419 3394 80 None -162 6 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]dihydroalprenolol from beta1 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta1 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 -162 6 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]dihydroalprenolol from beta1 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta1 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 -162 6 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]dihydroalprenolol from beta1 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta1 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 -162 6 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]dihydroalprenolol from beta1 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta1 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 -162 6 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]dihydroalprenolol from beta1 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta1 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
2778334 87087 93 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]dihydroalprenolol from human wild type beta1 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysisDisplacement of [3H]dihydroalprenolol from human wild type beta1 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysis
ChEMBL 232 1 1 4 0.9 FC(F)(F)c1ccnc(N2CCNCC2)n1 10.1021/jm400140q
CHEMBL2335157 87087 93 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]dihydroalprenolol from human wild type beta1 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysisDisplacement of [3H]dihydroalprenolol from human wild type beta1 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysis
ChEMBL 232 1 1 4 0.9 FC(F)(F)c1ccnc(N2CCNCC2)n1 10.1021/jm400140q
59119472 111752 0 None -31 2 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]dihydroalprenolol from beta1 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta1 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 4.6 pKi = 4.6 Binding
Displacement of [3H]dihydroalprenolol from beta1 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta1 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
176 394 63 None -660 31 Human 4.6 pKi = 4.6 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2157 394 63 None -660 31 Human 4.6 pKi = 4.6 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2566 394 63 None -660 31 Human 4.6 pKi = 4.6 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
CHEMBL633 394 63 None -660 31 Human 4.6 pKi = 4.6 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
DB01118 394 63 None -660 31 Human 4.6 pKi = 4.6 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
52943968 17597 0 None -69 3 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta-1 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 -69 3 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta-1 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
70691181 77248 0 None -13 2 Human 6.6 pKi = 6.6 Binding
Binding affinity to human beta1-adrenoceptor by radioligand binding assayBinding affinity to human beta1-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 6.6 pKi = 6.6 Binding
Binding affinity to human beta1-adrenoceptor by radioligand binding assayBinding affinity to human beta1-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
46889769 6627 0 None -109 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta-1 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta-1 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 6.6 pKi = 6.6 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta-1 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta-1 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
72545240 92683 0 None -16 5 Pig 6.6 pKi = 6.6 Binding
Displacement of [3H]-prazosin from alpha1-adrenergic receptor in pig cerebral cortexDisplacement of [3H]-prazosin from alpha1-adrenergic receptor in pig cerebral cortex
ChEMBL 469 12 0 8 3.4 COc1ccccc1N1CCN(Cc2cn(-c3ccc(OCCCOCCF)cc3)nn2)CC1 10.1016/j.bmcl.2013.09.026
CHEMBL2443007 92683 0 None -16 5 Pig 6.6 pKi = 6.6 Binding
Displacement of [3H]-prazosin from alpha1-adrenergic receptor in pig cerebral cortexDisplacement of [3H]-prazosin from alpha1-adrenergic receptor in pig cerebral cortex
ChEMBL 469 12 0 8 3.4 COc1ccccc1N1CCN(Cc2cn(-c3ccc(OCCCOCCF)cc3)nn2)CC1 10.1016/j.bmcl.2013.09.026
9960584 154080 0 None -436 3 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]iodocyanopindolol from human cloned adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human cloned adrenergic beta-1 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 -436 3 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]iodocyanopindolol from human cloned adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human cloned adrenergic beta-1 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
44571262 12453 0 None - 1 Rat 5.6 pKi = 5.6 Binding
Displacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation countingDisplacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation counting
ChEMBL 341 7 2 5 3.1 CC(C)(CO)NCCCOc1cccc2c(=O)c3ccccc3oc12 10.1016/j.bmc.2008.12.031
CHEMBL1186815 12453 0 None - 1 Rat 5.6 pKi = 5.6 Binding
Displacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation countingDisplacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation counting
ChEMBL 341 7 2 5 3.1 CC(C)(CO)NCCCOc1cccc2c(=O)c3ccccc3oc12 10.1016/j.bmc.2008.12.031
CHEMBL479644 12453 0 None - 1 Rat 5.6 pKi = 5.6 Binding
Displacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation countingDisplacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation counting
ChEMBL 341 7 2 5 3.1 CC(C)(CO)NCCCOc1cccc2c(=O)c3ccccc3oc12 10.1016/j.bmc.2008.12.031
135398737 942 89 None -144 92 Rat 4.6 pKi = 4.6 Binding
Binding affinity measured at the Beta-1 adrenergic receptor by the inhibition of [3H]DHA binding to rat cortex using unlabeled isoprenalin for nonspecific binding.Binding affinity measured at the Beta-1 adrenergic receptor by the inhibition of [3H]DHA binding to rat cortex using unlabeled isoprenalin for nonspecific binding.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9810396
38 942 89 None -144 92 Rat 4.6 pKi = 4.6 Binding
Binding affinity measured at the Beta-1 adrenergic receptor by the inhibition of [3H]DHA binding to rat cortex using unlabeled isoprenalin for nonspecific binding.Binding affinity measured at the Beta-1 adrenergic receptor by the inhibition of [3H]DHA binding to rat cortex using unlabeled isoprenalin for nonspecific binding.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9810396
722 942 89 None -144 92 Rat 4.6 pKi = 4.6 Binding
Binding affinity measured at the Beta-1 adrenergic receptor by the inhibition of [3H]DHA binding to rat cortex using unlabeled isoprenalin for nonspecific binding.Binding affinity measured at the Beta-1 adrenergic receptor by the inhibition of [3H]DHA binding to rat cortex using unlabeled isoprenalin for nonspecific binding.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9810396
CHEMBL42 942 89 None -144 92 Rat 4.6 pKi = 4.6 Binding
Binding affinity measured at the Beta-1 adrenergic receptor by the inhibition of [3H]DHA binding to rat cortex using unlabeled isoprenalin for nonspecific binding.Binding affinity measured at the Beta-1 adrenergic receptor by the inhibition of [3H]DHA binding to rat cortex using unlabeled isoprenalin for nonspecific binding.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9810396
DB00363 942 89 None -144 92 Rat 4.6 pKi = 4.6 Binding
Binding affinity measured at the Beta-1 adrenergic receptor by the inhibition of [3H]DHA binding to rat cortex using unlabeled isoprenalin for nonspecific binding.Binding affinity measured at the Beta-1 adrenergic receptor by the inhibition of [3H]DHA binding to rat cortex using unlabeled isoprenalin for nonspecific binding.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9810396
1960 2805 64 None -144 26 Rat 4.6 pKi = 4.6 Binding
Binding of [3H]dihydroalprenolol to beta-1 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-1 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 -144 26 Rat 4.6 pKi = 4.6 Binding
Binding of [3H]dihydroalprenolol to beta-1 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-1 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 -144 26 Rat 4.6 pKi = 4.6 Binding
Binding of [3H]dihydroalprenolol to beta-1 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-1 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 -144 26 Rat 4.6 pKi = 4.6 Binding
Binding of [3H]dihydroalprenolol to beta-1 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-1 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 -144 26 Rat 4.6 pKi = 4.6 Binding
Binding of [3H]dihydroalprenolol to beta-1 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-1 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
24886595 17449 0 None -4 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta-1 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 -4 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta-1 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
145947253 167079 0 None 1 2 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]-CGP12177 from human beta1 ADR expressed in HEK293T cell membranes after 90 mins by scintillation countingDisplacement of [3H]-CGP12177 from human beta1 ADR expressed in HEK293T cell membranes 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 4.6 pKi = 4.6 Binding
Displacement of [3H]-CGP12177 from human beta1 ADR expressed in HEK293T cell membranes after 90 mins by scintillation countingDisplacement of [3H]-CGP12177 from human beta1 ADR expressed in HEK293T cell membranes 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 4.6 pKi = 4.6 Binding
Displacement of [3H]-CGP12177 from human beta1 ADR expressed in HEK293T cell membranes after 90 mins by scintillation countingDisplacement of [3H]-CGP12177 from human beta1 ADR expressed in HEK293T cell membranes 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
44112 120764 41 None -2 7 Human 7.6 pKi = 7.6 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 380 7 2 4 4.5 Cc1cc2c(OCC(CNC(C)(C)C)OC(=O)c3ccccc3)cccc2[nH]1 nan
CHEMBL357995 120764 41 None -2 7 Human 7.6 pKi = 7.6 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 380 7 2 4 4.5 Cc1cc2c(OCC(CNC(C)(C)C)OC(=O)c3ccccc3)cccc2[nH]1 nan
46889643 6557 0 None 4 3 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta-1 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta-1 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 7.6 pKi = 7.6 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta-1 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta-1 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
155555687 173866 0 None 2 2 Mouse 7.6 pKi = 7.6 Binding
Displacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T 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 Mouse 7.6 pKi = 7.6 Binding
Displacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T 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
9924779 93991 0 None -8 2 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]iodocyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human adrenergic beta-1 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 6.6 pKi = 6.6 Binding
Displacement of [125I]iodocyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human adrenergic beta-1 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
44444191 171857 0 None -38 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]iodocyanopindolol from human cloned adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human cloned adrenergic beta-1 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 -38 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]iodocyanopindolol from human cloned adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human cloned adrenergic beta-1 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
1960 2805 64 None -144 26 Rat 5.6 pKi = 5.6 Binding
Binding of [3H]dihydroalprenolol to beta-1 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-1 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 -144 26 Rat 5.6 pKi = 5.6 Binding
Binding of [3H]dihydroalprenolol to beta-1 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-1 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 -144 26 Rat 5.6 pKi = 5.6 Binding
Binding of [3H]dihydroalprenolol to beta-1 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-1 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 -144 26 Rat 5.6 pKi = 5.6 Binding
Binding of [3H]dihydroalprenolol to beta-1 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-1 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 -144 26 Rat 5.6 pKi = 5.6 Binding
Binding of [3H]dihydroalprenolol to beta-1 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-1 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
42629372 63301 0 None -52 2 Rat 4.6 pKi = 4.6 Binding
Displacement of [3H]CGP-12177 from beta1-adrenergic receptor in Sprague-Dawley rat cortical membrane after 2 hrsDisplacement of [3H]CGP-12177 from beta1-adrenergic receptor in Sprague-Dawley rat cortical membrane after 2 hrs
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 Rat 4.6 pKi = 4.6 Binding
Displacement of [3H]CGP-12177 from beta1-adrenergic receptor in Sprague-Dawley rat cortical membrane after 2 hrsDisplacement of [3H]CGP-12177 from beta1-adrenergic receptor in Sprague-Dawley rat cortical membrane after 2 hrs
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
10406968 113245 0 None -1 3 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 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 7.6 pKi = 7.6 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 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
10466448 112371 2 None -34 2 Guinea pig 5.6 pKi = 5.6 Binding
Binding affinity at Beta-1 adrenergic receptor in guinea pigs by [125I]CYP displacementBinding affinity at Beta-1 adrenergic receptor in guinea pigs by [125I]CYP displacement
ChEMBL 231 1 0 5 0.8 Cc1cnc(N2CCN(C)CC2)c2nccn12 10.1021/jm00099a012
CHEMBL330994 112371 2 None -34 2 Guinea pig 5.6 pKi = 5.6 Binding
Binding affinity at Beta-1 adrenergic receptor in guinea pigs by [125I]CYP displacementBinding affinity at Beta-1 adrenergic receptor in guinea pigs by [125I]CYP displacement
ChEMBL 231 1 0 5 0.8 Cc1cnc(N2CCN(C)CC2)c2nccn12 10.1021/jm00099a012
24936763 17419 0 None -30 3 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta-1 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 -30 3 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta-1 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
24936885 17286 0 None -32 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta-1 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 -32 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta-1 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
12828570 4990 0 None -1 2 Rat 4.5 pKi = 4.5 Binding
Tested for binding affinity against beta-1 adrenergic receptor in rat brain using [3H]-CGP- 26505 as radioligandTested for binding affinity against beta-1 adrenergic receptor in rat brain using [3H]-CGP- 26505 as radioligand
ChEMBL 237 3 3 4 1.7 CC(C)NCC1OCCc2c1ccc(O)c2O 10.1021/jm00073a006
CHEMBL105434 4990 0 None -1 2 Rat 4.5 pKi = 4.5 Binding
Tested for binding affinity against beta-1 adrenergic receptor in rat brain using [3H]-CGP- 26505 as radioligandTested for binding affinity against beta-1 adrenergic receptor in rat brain using [3H]-CGP- 26505 as radioligand
ChEMBL 237 3 3 4 1.7 CC(C)NCC1OCCc2c1ccc(O)c2O 10.1021/jm00073a006
52941476 17488 0 None -28 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta-1 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 -28 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta-1 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
155529446 170876 0 None -8 2 Mouse 7.5 pKi = 7.5 Binding
Displacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T 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 Mouse 7.5 pKi = 7.5 Binding
Displacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranes
ChEMBL 502 16 3 8 4.1 COc1cc(CCNC[C@@H](O)COc2cccc3ccccc23)ccc1OCCSSCCN 10.1016/j.bmc.2019.05.034
52941603 17102 0 None -21 3 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta-1 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 -21 3 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta-1 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
52947443 17417 0 None -17 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta-1 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 -17 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta-1 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
2770390 6629 10 None -1 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta-1 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta-1 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 6.5 pKi = 6.5 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta-1 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta-1 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
10083242 13707 0 None -8 3 Guinea pig 5.5 pKi = 5.5 Binding
Binding affinity at Beta-1 adrenergic receptor in guinea pigs by [125I]CYP displacementBinding affinity at Beta-1 adrenergic receptor in guinea pigs by [125I]CYP displacement
ChEMBL 245 2 1 5 1.3 CC(C)c1cnc2c(N3CCNCC3)nccn12 10.1021/jm00099a012
CHEMBL1195814 13707 0 None -8 3 Guinea pig 5.5 pKi = 5.5 Binding
Binding affinity at Beta-1 adrenergic receptor in guinea pigs by [125I]CYP displacementBinding affinity at Beta-1 adrenergic receptor in guinea pigs by [125I]CYP displacement
ChEMBL 245 2 1 5 1.3 CC(C)c1cnc2c(N3CCNCC3)nccn12 10.1021/jm00099a012
CHEMBL555391 13707 0 None -8 3 Guinea pig 5.5 pKi = 5.5 Binding
Binding affinity at Beta-1 adrenergic receptor in guinea pigs by [125I]CYP displacementBinding affinity at Beta-1 adrenergic receptor in guinea pigs by [125I]CYP displacement
ChEMBL 245 2 1 5 1.3 CC(C)c1cnc2c(N3CCNCC3)nccn12 10.1021/jm00099a012
44582475 181049 0 None - 1 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation methodDisplacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation method
ChEMBL 356 10 3 5 2.6 COc1ccccc1OCCNCC(O)COc1cccc2[nH]ccc12 10.1016/j.ejmech.2008.05.019
CHEMBL477465 181049 0 None - 1 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation methodDisplacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation method
ChEMBL 356 10 3 5 2.6 COc1ccccc1OCCNCC(O)COc1cccc2[nH]ccc12 10.1016/j.ejmech.2008.05.019
165193 3126 60 None -18 43 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]CGP12177 from beta1 adrenoreceptor in Rattus norvegicus (rat) cerebral cortex by liquid scintillation countingDisplacement of [3H]CGP12177 from beta1 adrenoreceptor in Rattus norvegicus (rat) cerebral cortex by liquid scintillation counting
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1007/s00044-008-9094-3
2303 3126 60 None -18 43 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]CGP12177 from beta1 adrenoreceptor in Rattus norvegicus (rat) cerebral cortex by liquid scintillation countingDisplacement of [3H]CGP12177 from beta1 adrenoreceptor in Rattus norvegicus (rat) cerebral cortex by liquid scintillation counting
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1007/s00044-008-9094-3
4946 3126 60 None -18 43 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]CGP12177 from beta1 adrenoreceptor in Rattus norvegicus (rat) cerebral cortex by liquid scintillation countingDisplacement of [3H]CGP12177 from beta1 adrenoreceptor in Rattus norvegicus (rat) cerebral cortex by liquid scintillation counting
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1007/s00044-008-9094-3
564 3126 60 None -18 43 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]CGP12177 from beta1 adrenoreceptor in Rattus norvegicus (rat) cerebral cortex by liquid scintillation countingDisplacement of [3H]CGP12177 from beta1 adrenoreceptor in Rattus norvegicus (rat) cerebral cortex by liquid scintillation counting
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1007/s00044-008-9094-3
62882 3126 60 None -18 43 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]CGP12177 from beta1 adrenoreceptor in Rattus norvegicus (rat) cerebral cortex by liquid scintillation countingDisplacement of [3H]CGP12177 from beta1 adrenoreceptor in Rattus norvegicus (rat) cerebral cortex by liquid scintillation counting
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1007/s00044-008-9094-3
63 3126 60 None -18 43 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]CGP12177 from beta1 adrenoreceptor in Rattus norvegicus (rat) cerebral cortex by liquid scintillation countingDisplacement of [3H]CGP12177 from beta1 adrenoreceptor in Rattus norvegicus (rat) cerebral cortex by liquid scintillation counting
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1007/s00044-008-9094-3
66366 3126 60 None -18 43 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]CGP12177 from beta1 adrenoreceptor in Rattus norvegicus (rat) cerebral cortex by liquid scintillation countingDisplacement of [3H]CGP12177 from beta1 adrenoreceptor in Rattus norvegicus (rat) cerebral cortex by liquid scintillation counting
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1007/s00044-008-9094-3
91536 3126 60 None -18 43 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]CGP12177 from beta1 adrenoreceptor in Rattus norvegicus (rat) cerebral cortex by liquid scintillation countingDisplacement of [3H]CGP12177 from beta1 adrenoreceptor in Rattus norvegicus (rat) cerebral cortex by liquid scintillation counting
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1007/s00044-008-9094-3
CHEMBL27 3126 60 None -18 43 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]CGP12177 from beta1 adrenoreceptor in Rattus norvegicus (rat) cerebral cortex by liquid scintillation countingDisplacement of [3H]CGP12177 from beta1 adrenoreceptor in Rattus norvegicus (rat) cerebral cortex by liquid scintillation counting
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1007/s00044-008-9094-3
CHEMBL452861 3126 60 None -18 43 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]CGP12177 from beta1 adrenoreceptor in Rattus norvegicus (rat) cerebral cortex by liquid scintillation countingDisplacement of [3H]CGP12177 from beta1 adrenoreceptor in Rattus norvegicus (rat) cerebral cortex by liquid scintillation counting
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1007/s00044-008-9094-3
DB00571 3126 60 None -18 43 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]CGP12177 from beta1 adrenoreceptor in Rattus norvegicus (rat) cerebral cortex by liquid scintillation countingDisplacement of [3H]CGP12177 from beta1 adrenoreceptor in Rattus norvegicus (rat) cerebral cortex by liquid scintillation counting
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1007/s00044-008-9094-3
46889811 6362 0 None -16 3 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta-1 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta-1 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 8.5 pKi = 8.5 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta-1 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta-1 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
185394 139145 34 None -3 5 Mouse 8.5 pKi = 8.5 Binding
Displacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T 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 Mouse 8.5 pKi = 8.5 Binding
Displacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T 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
49864356 15430 0 None -2 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 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 8.4 pKi = 8.4 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 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
12147227 61648 0 None 1 2 Human 8.4 pKi = 8.4 Binding
Inhibition of 125 I-Iodocyanopindolol binding to Beta-1 adrenergic receptorInhibition of 125 I-Iodocyanopindolol binding to Beta-1 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 8.4 pKi = 8.4 Binding
Inhibition of 125 I-Iodocyanopindolol binding to Beta-1 adrenergic receptorInhibition of 125 I-Iodocyanopindolol binding to Beta-1 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 8.4 pKi = 8.4 Binding
Inhibition of 125 I-Iodocyanopindolol binding to Beta-1 adrenergic receptorInhibition of 125 I-Iodocyanopindolol binding to Beta-1 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 8.4 pKi = 8.4 Binding
Inhibition of 125 I-Iodocyanopindolol binding to Beta-1 adrenergic receptorInhibition of 125 I-Iodocyanopindolol binding to Beta-1 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 8.4 pKi = 8.4 Binding
Inhibition of 125 I-Iodocyanopindolol binding to Beta-1 adrenergic receptorInhibition of 125 I-Iodocyanopindolol binding to Beta-1 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
39468 2270 33 None -3 7 Human 8.4 pKi = 8.4 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 291 5 2 4 2.3 O[C@H](COc1cccc2c1CCCC2=O)CNC(C)(C)C nan
431 2270 33 None -3 7 Human 8.4 pKi = 8.4 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 291 5 2 4 2.3 O[C@H](COc1cccc2c1CCCC2=O)CNC(C)(C)C nan
570 2270 33 None -3 7 Human 8.4 pKi = 8.4 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 291 5 2 4 2.3 O[C@H](COc1cccc2c1CCCC2=O)CNC(C)(C)C nan
CHEMBL1201237 2270 33 None -3 7 Human 8.4 pKi = 8.4 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 291 5 2 4 2.3 O[C@H](COc1cccc2c1CCCC2=O)CNC(C)(C)C nan
DB01210 2270 33 None -3 7 Human 8.4 pKi = 8.4 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 291 5 2 4 2.3 O[C@H](COc1cccc2c1CCCC2=O)CNC(C)(C)C nan
52946537 17526 0 None -2 3 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta-1 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 7.5 pKi = 7.5 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cells
ChEMBL 384 7 2 7 2.7 OC(CNC1CCN(c2ncnc3ccsc23)CC1)COc1ccccc1 10.1016/j.bmcl.2010.08.039
118710941 113239 0 None -5 3 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 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 7.5 pKi = 7.5 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 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
164451 102689 11 None 1 3 Human 6.5 pKi = 6.5 Binding
Compound was tested for its binding affinity against Beta-1 adrenergic receptor in CHO cell membrane using [125I]iodocyanopindolol as the radioligand.Compound was tested for its binding affinity against Beta-1 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 1 3 Human 6.5 pKi = 6.5 Binding
Compound was tested for its binding affinity against Beta-1 adrenergic receptor in CHO cell membrane using [125I]iodocyanopindolol as the radioligand.Compound was tested for its binding affinity against Beta-1 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
46889727 6556 0 None -3 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta-1 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta-1 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 6.5 pKi = 6.5 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta-1 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta-1 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
127046948 139527 0 None -13 6 Mouse 6.5 pKi = 6.5 Binding
Displacement of [3H]CGP12177 from mouse beta1 receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from mouse beta1 receptor expressed in HEK293 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 Mouse 6.5 pKi = 6.5 Binding
Displacement of [3H]CGP12177 from mouse beta1 receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from mouse beta1 receptor expressed in HEK293 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
15077955 154824 0 None - 1 Human 6.5 pKi = 6.5 Binding
Inhibition of [3H]dihydroalprenolol binding to beta 1 adrenoceptor from turkey erythrocyte membranes.Inhibition of [3H]dihydroalprenolol binding to beta 1 adrenoceptor from turkey erythrocyte membranes.
ChEMBL 496 10 5 7 0.6 NS(=O)(=O)c1cc(C(=O)NCCNCC(O)COc2cccc3c2CCC(=O)N3)ccc1Cl 10.1021/jm00053a020
CHEMBL40343 154824 0 None - 1 Human 6.5 pKi = 6.5 Binding
Inhibition of [3H]dihydroalprenolol binding to beta 1 adrenoceptor from turkey erythrocyte membranes.Inhibition of [3H]dihydroalprenolol binding to beta 1 adrenoceptor from turkey erythrocyte membranes.
ChEMBL 496 10 5 7 0.6 NS(=O)(=O)c1cc(C(=O)NCCNCC(O)COc2cccc3c2CCC(=O)N3)ccc1Cl 10.1021/jm00053a020
1028 287 69 None -23 30 Guinea pig 5.5 pKi = 5.5 Binding
Binding affinity against beta-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of Dihydro-[3H]-alprenololBinding affinity against beta-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of Dihydro-[3H]-alprenolol
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00118a019
139148732 287 69 None -23 30 Guinea pig 5.5 pKi = 5.5 Binding
Binding affinity against beta-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of Dihydro-[3H]-alprenololBinding affinity against beta-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of Dihydro-[3H]-alprenolol
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00118a019
479 287 69 None -23 30 Guinea pig 5.5 pKi = 5.5 Binding
Binding affinity against beta-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of Dihydro-[3H]-alprenololBinding affinity against beta-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of Dihydro-[3H]-alprenolol
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00118a019
5816 287 69 None -23 30 Guinea pig 5.5 pKi = 5.5 Binding
Binding affinity against beta-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of Dihydro-[3H]-alprenololBinding affinity against beta-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of Dihydro-[3H]-alprenolol
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00118a019
CHEMBL679 287 69 None -23 30 Guinea pig 5.5 pKi = 5.5 Binding
Binding affinity against beta-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of Dihydro-[3H]-alprenololBinding affinity against beta-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of Dihydro-[3H]-alprenolol
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00118a019
DB00668 287 69 None -23 30 Guinea pig 5.5 pKi = 5.5 Binding
Binding affinity against beta-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of Dihydro-[3H]-alprenololBinding affinity against beta-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of Dihydro-[3H]-alprenolol
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00118a019
53387673 64818 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]-Iodopindolol from beta1-adrenergic receptor after 1.5 hrs by liquid scintillation countingDisplacement of [125I]-Iodopindolol from beta1-adrenergic receptor after 1.5 hrs by liquid scintillation counting
ChEMBL 415 9 2 7 2.3 COc1ccc2nc(-c3ccc(OC[C@@H](O)CNC(C)CF)cc3)n(C)c(=O)c2c1 10.1016/j.bmcl.2011.06.106
CHEMBL1824266 64818 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]-Iodopindolol from beta1-adrenergic receptor after 1.5 hrs by liquid scintillation countingDisplacement of [125I]-Iodopindolol from beta1-adrenergic receptor after 1.5 hrs by liquid scintillation counting
ChEMBL 415 9 2 7 2.3 COc1ccc2nc(-c3ccc(OC[C@@H](O)CNC(C)CF)cc3)n(C)c(=O)c2c1 10.1016/j.bmcl.2011.06.106
16736091 85291 0 None -66 2 Rat 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 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 Rat 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 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 Rat 4.5 pKi = 4.5 Binding
Displacement of [3H]CGP-12177 from beta-1 adrenergic receptor in Sprague-Dawley rat cortical membraneDisplacement of [3H]CGP-12177 from beta-1 adrenergic receptor in Sprague-Dawley rat cortical membrane
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 Rat 4.5 pKi = 4.5 Binding
Displacement of [3H]CGP-12177 from beta-1 adrenergic receptor in Sprague-Dawley rat cortical membraneDisplacement of [3H]CGP-12177 from beta-1 adrenergic receptor in Sprague-Dawley rat cortical membrane
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
25198751 12467 0 None - 1 Rat 4.5 pKi = 4.5 Binding
Displacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation countingDisplacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation counting
ChEMBL 325 7 2 5 2.5 C=CCNCC(O)COc1ccc2oc3ccccc3c(=O)c2c1 10.1016/j.bmc.2008.12.031
CHEMBL1186872 12467 0 None - 1 Rat 4.5 pKi = 4.5 Binding
Displacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation countingDisplacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation counting
ChEMBL 325 7 2 5 2.5 C=CCNCC(O)COc1ccc2oc3ccccc3c(=O)c2c1 10.1016/j.bmc.2008.12.031
CHEMBL481415 12467 0 None - 1 Rat 4.5 pKi = 4.5 Binding
Displacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation countingDisplacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation counting
ChEMBL 325 7 2 5 2.5 C=CCNCC(O)COc1ccc2oc3ccccc3c(=O)c2c1 10.1016/j.bmc.2008.12.031
10457669 160725 0 None - 1 Human 7.5 pKi = 7.5 Binding
Inhibition of [3H]dihydroalprenolol binding to beta 1 adrenoceptor from turkey erythrocyte membranes.Inhibition of [3H]dihydroalprenolol binding to beta 1 adrenoceptor from turkey erythrocyte membranes.
ChEMBL 475 7 2 6 2.7 NS(=O)(=O)c1cc(N2CCN(CC(O)COc3cccc4ccccc34)CC2)ccc1Cl 10.1021/jm00053a020
CHEMBL41214 160725 0 None - 1 Human 7.5 pKi = 7.5 Binding
Inhibition of [3H]dihydroalprenolol binding to beta 1 adrenoceptor from turkey erythrocyte membranes.Inhibition of [3H]dihydroalprenolol binding to beta 1 adrenoceptor from turkey erythrocyte membranes.
ChEMBL 475 7 2 6 2.7 NS(=O)(=O)c1cc(N2CCN(CC(O)COc3cccc4ccccc34)CC2)ccc1Cl 10.1021/jm00053a020
49864461 15461 0 None -1 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 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 7.5 pKi = 7.5 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 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
44287337 150614 0 None -2 3 Human 6.5 pKi = 6.5 Binding
Ability to bind to human Beta-1 adrenergic receptor using membranes of stably transfected CHO cellsAbility to bind to human Beta-1 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 6.5 pKi = 6.5 Binding
Ability to bind to human Beta-1 adrenergic receptor using membranes of stably transfected CHO cellsAbility to bind to human Beta-1 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
11820657 13318 1 None -6 2 Guinea pig 6.5 pKi = 6.5 Binding
Binding affinity at Beta-1 adrenergic receptor in guinea pigs by [125I]CYP displacementBinding affinity at Beta-1 adrenergic receptor in guinea pigs by [125I]CYP displacement
ChEMBL 217 1 1 5 0.4 Cc1cn2ccnc(N3CCNCC3)c2n1 10.1021/jm00099a012
CHEMBL1193017 13318 1 None -6 2 Guinea pig 6.5 pKi = 6.5 Binding
Binding affinity at Beta-1 adrenergic receptor in guinea pigs by [125I]CYP displacementBinding affinity at Beta-1 adrenergic receptor in guinea pigs by [125I]CYP displacement
ChEMBL 217 1 1 5 0.4 Cc1cn2ccnc(N3CCNCC3)c2n1 10.1021/jm00099a012
CHEMBL544354 13318 1 None -6 2 Guinea pig 6.5 pKi = 6.5 Binding
Binding affinity at Beta-1 adrenergic receptor in guinea pigs by [125I]CYP displacementBinding affinity at Beta-1 adrenergic receptor in guinea pigs by [125I]CYP displacement
ChEMBL 217 1 1 5 0.4 Cc1cn2ccnc(N3CCNCC3)c2n1 10.1021/jm00099a012
155534529 171387 0 None -2 2 Mouse 6.5 pKi = 6.5 Binding
Displacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T 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 Mouse 6.5 pKi = 6.5 Binding
Displacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T 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
16737412 85341 0 None -3 2 Rat 4.5 pKi = 4.5 Binding
Displacement of [3H]CGP-12177 from beta-1 adrenergic receptor in Sprague-Dawley rat cortical membraneDisplacement of [3H]CGP-12177 from beta-1 adrenergic receptor in Sprague-Dawley rat cortical membrane
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 Rat 4.5 pKi = 4.5 Binding
Displacement of [3H]CGP-12177 from beta-1 adrenergic receptor in Sprague-Dawley rat cortical membraneDisplacement of [3H]CGP-12177 from beta-1 adrenergic receptor in Sprague-Dawley rat cortical membrane
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 Rat 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
CHEMBL229388 85341 0 None -3 2 Rat 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
16736092 85342 0 None -1 2 Rat 4.5 pKi = 4.5 Binding
Displacement of [3H]CGP-12177 from beta-1 adrenergic receptor in Sprague-Dawley rat cortical membraneDisplacement of [3H]CGP-12177 from beta-1 adrenergic receptor in Sprague-Dawley rat cortical membrane
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 Rat 4.5 pKi = 4.5 Binding
Displacement of [3H]CGP-12177 from beta-1 adrenergic receptor in Sprague-Dawley rat cortical membraneDisplacement of [3H]CGP-12177 from beta-1 adrenergic receptor in Sprague-Dawley rat cortical membrane
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 Rat 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 Rat 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
1239 1639 46 None -63 4 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 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 6.5 pKi = 6.5 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 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 6.5 pKi = 6.5 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 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 6.5 pKi = 6.5 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 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 6.5 pKi = 6.5 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 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
153287553 170528 0 None -501 6 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]-pindolol from human recombinant adrenergic Beta1 receptor expressed in Flp-In CHO cells after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-pindolol from human recombinant adrenergic Beta1 receptor expressed in Flp-In CHO cells after 90 mins by microbeta scintillation counting method
ChEMBL 264 1 1 2 3.7 C[C@@]12CN(c3ccccc3)c3ccccc3[C@@H]1CCN2 10.1021/acsmedchemlett.9b00225
CHEMBL4457754 170528 0 None -501 6 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]-pindolol from human recombinant adrenergic Beta1 receptor expressed in Flp-In CHO cells after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-pindolol from human recombinant adrenergic Beta1 receptor expressed in Flp-In CHO cells after 90 mins by microbeta scintillation counting method
ChEMBL 264 1 1 2 3.7 C[C@@]12CN(c3ccccc3)c3ccccc3[C@@H]1CCN2 10.1021/acsmedchemlett.9b00225
10287658 111750 0 None -25 2 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]dihydroalprenolol from beta1 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta1 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 4.5 pKi = 4.5 Binding
Displacement of [3H]dihydroalprenolol from beta1 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta1 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
90644154 111751 0 None -5 2 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]dihydroalprenolol from beta1 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta1 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 4.5 pKi = 4.5 Binding
Displacement of [3H]dihydroalprenolol from beta1 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta1 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
10310047 111758 0 None -199 2 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]dihydroalprenolol from beta1 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta1 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 4.5 pKi = 4.5 Binding
Displacement of [3H]dihydroalprenolol from beta1 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta1 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
1239 1639 46 None -63 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 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 6.5 pKi = 6.5 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 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 6.5 pKi = 6.5 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 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 6.5 pKi = 6.5 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 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 6.5 pKi = 6.5 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 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
46889854 7212 0 None -104 3 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta-1 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta-1 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 7.5 pKi = 7.5 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta-1 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta-1 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
10140996 154367 0 None -398 3 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]iodocyanopindolol from human cloned adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human cloned adrenergic beta-1 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 -398 3 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]iodocyanopindolol from human cloned adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human cloned adrenergic beta-1 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
1588 2284 24 None -218 44 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
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 -218 44 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
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 -218 44 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
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 -218 44 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
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 -218 44 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
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
5581 101175 10 None -1 7 Human 6.5 pKi = 6.5 Binding
Binding Affinity against human Beta-1 adrenergic receptor expressed in Chinese hamster ovary(CHO) cells was measured by using [125I]ICYP radioligandBinding Affinity against human Beta-1 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 6.5 pKi = 6.5 Binding
Binding Affinity against human Beta-1 adrenergic receptor expressed in Chinese hamster ovary(CHO) cells was measured by using [125I]ICYP radioligandBinding Affinity against human Beta-1 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 6.5 pKi = 6.5 Binding
Binding affinity for human Beta-1 adrenergic receptor expressed in CHO cells by radioligand competition binding assays using [125I]iodocyanopindolol (ICYP).) PR = potency ratio relative to TMQBinding affinity for human Beta-1 adrenergic receptor expressed in CHO cells by radioligand competition binding assays using [125I]iodocyanopindolol (ICYP).) PR = potency ratio relative to TMQ
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 6.5 pKi = 6.5 Binding
Binding affinity for human Beta-1 adrenergic receptor expressed in CHO cells by radioligand competition binding assays using [125I]iodocyanopindolol (ICYP).) PR = potency ratio relative to TMQBinding affinity for human Beta-1 adrenergic receptor expressed in CHO cells by radioligand competition binding assays using [125I]iodocyanopindolol (ICYP).) PR = potency ratio relative to TMQ
ChEMBL 345 5 3 6 2.6 COc1cc(CC2NCCc3cc(O)c(O)cc32)cc(OC)c1OC 10.1021/jm960208o
14925759 157482 6 None -11220 13 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]CGP12177 from human recombinant beta1 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by beta counting methodDisplacement of [3H]CGP12177 from human recombinant beta1 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 -11220 13 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]CGP12177 from human recombinant beta1 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by beta counting methodDisplacement of [3H]CGP12177 from human recombinant beta1 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
52943362 17351 0 None -8 3 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta-1 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 -8 3 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta-1 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
118710945 113243 0 None -2 3 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 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 7.5 pKi = 7.5 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 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
155529870 170929 0 None -30 2 Mouse 7.5 pKi = 7.5 Binding
Displacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T 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 Mouse 7.5 pKi = 7.5 Binding
Displacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranes
ChEMBL 516 17 3 8 4.5 COc1cc(CCNC[C@@H](O)COc2cccc3ccccc23)ccc1OCCCSSCCN 10.1016/j.bmc.2019.05.034
49864381 15443 0 None 1 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 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 7.5 pKi = 7.5 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 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
44361777 118062 0 None -3 2 Rat 6.5 pKi = 6.5 Binding
Compound was evaluated for its Beta-1 adrenergic receptor binding affinity by measuring the displacement of [3H]dihydroalprenolol binding in rat heartCompound was evaluated for its Beta-1 adrenergic receptor binding affinity by measuring the displacement of [3H]dihydroalprenolol binding in rat heart
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 Rat 6.5 pKi = 6.5 Binding
Compound was evaluated for its Beta-1 adrenergic receptor binding affinity by measuring the displacement of [3H]dihydroalprenolol binding in rat heartCompound was evaluated for its Beta-1 adrenergic receptor binding affinity by measuring the displacement of [3H]dihydroalprenolol binding in rat heart
ChEMBL 429 7 2 7 2.3 COc1ccccc1N1CCN(CC(O)COc2cccc3c2SCC(=O)N3)CC1 10.1016/s0960-894x(00)00016-0
155511898 169021 0 None -12 2 Mouse 6.5 pKi = 6.5 Binding
Displacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T 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 Mouse 6.5 pKi = 6.5 Binding
Displacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T cells after 60 mins by radioligand competition binding assay
ChEMBL 360 8 2 3 4.5 COc1ccccc1OCCNCCc1cccc2[nH]c3ccccc3c12 10.1021/acs.jmedchem.9b00349
123133225 144264 0 None -5 2 Rat 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
CHEMBL3909417 144264 0 None -5 2 Rat 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
16735263 85351 0 None -5 2 Rat 4.5 pKi = 4.5 Binding
Displacement of [3H]CGP-12177 from beta-1 adrenergic receptor in Sprague-Dawley rat cortical membraneDisplacement of [3H]CGP-12177 from beta-1 adrenergic receptor in Sprague-Dawley rat cortical membrane
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 Rat 4.5 pKi = 4.5 Binding
Displacement of [3H]CGP-12177 from beta-1 adrenergic receptor in Sprague-Dawley rat cortical membraneDisplacement of [3H]CGP-12177 from beta-1 adrenergic receptor in Sprague-Dawley rat cortical membrane
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
123133222 159488 0 None -6 2 Rat 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 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 Rat 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 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 Rat 4.5 pKi = 4.5 Binding
Displacement of [3H]CGP-12177 from beta-1 adrenergic receptor in Sprague-Dawley rat cortical membraneDisplacement of [3H]CGP-12177 from beta-1 adrenergic receptor in Sprague-Dawley rat cortical membrane
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 Rat 4.5 pKi = 4.5 Binding
Displacement of [3H]CGP-12177 from beta-1 adrenergic receptor in Sprague-Dawley rat cortical membraneDisplacement of [3H]CGP-12177 from beta-1 adrenergic receptor in Sprague-Dawley rat cortical membrane
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
16735495 85345 0 None -14 2 Rat 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 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 Rat 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 337 6 4 4 3.5 C[C@H](Cc1cccc2ccccc12)NC[C@H](O)c1cc(O)cc(O)c1 nan
16735495 85345 0 None -14 2 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]CGP-12177 from beta-1 adrenergic receptor in Sprague-Dawley rat cortical membraneDisplacement of [3H]CGP-12177 from beta-1 adrenergic receptor in Sprague-Dawley rat cortical membrane
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 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]CGP-12177 from beta-1 adrenergic receptor in Sprague-Dawley rat cortical membraneDisplacement of [3H]CGP-12177 from beta-1 adrenergic receptor in Sprague-Dawley rat cortical membrane
ChEMBL 337 6 4 4 3.5 C[C@H](Cc1cccc2ccccc12)NC[C@H](O)c1cc(O)cc(O)c1 10.1021/jm070030d
44396798 168815 0 None -30 3 Human 7.5 pKi = 7.5 Binding
Binding inhibition constant was determined by inhibition of [125I]-iodocyanopindolol binding to Beta-1 adrenergic receptorBinding inhibition constant was determined by inhibition of [125I]-iodocyanopindolol binding to Beta-1 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 -30 3 Human 7.5 pKi = 7.5 Binding
Binding inhibition constant was determined by inhibition of [125I]-iodocyanopindolol binding to Beta-1 adrenergic receptorBinding inhibition constant was determined by inhibition of [125I]-iodocyanopindolol binding to Beta-1 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
155521528 170027 0 None -1 2 Mouse 6.5 pKi = 6.5 Binding
Displacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T 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 Mouse 6.5 pKi = 6.5 Binding
Displacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T 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
118710944 113242 0 None -2 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 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 6.5 pKi = 6.5 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 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
15221053 202880 0 None -2 3 Human 5.5 pKi = 5.5 Binding
Compound was tested for its binding affinity against Beta-1 adrenergic receptor in CHO cell membrane using [125I]iodocyanopindolol as the radioligand.Compound was tested for its binding affinity against Beta-1 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 5.5 pKi = 5.5 Binding
Compound was tested for its binding affinity against Beta-1 adrenergic receptor in CHO cell membrane using [125I]iodocyanopindolol as the radioligand.Compound was tested for its binding affinity against Beta-1 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
24937269 17450 0 None -1949 3 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta-1 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 -1949 3 Human 4.5 pKi = 4.5 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta-1 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
13864389 4982 2 None 8 2 Rat 5.5 pKi = 5.5 Binding
Tested for binding affinity against beta-1 adrenergic receptor in rat brain using [3H]-CGP- 26505 as radioligandTested for binding affinity against beta-1 adrenergic receptor in rat brain using [3H]-CGP- 26505 as radioligand
ChEMBL 195 1 3 4 0.7 NCC1OCCc2cc(O)c(O)cc21 10.1021/jm00073a006
CHEMBL105383 4982 2 None 8 2 Rat 5.5 pKi = 5.5 Binding
Tested for binding affinity against beta-1 adrenergic receptor in rat brain using [3H]-CGP- 26505 as radioligandTested for binding affinity against beta-1 adrenergic receptor in rat brain using [3H]-CGP- 26505 as radioligand
ChEMBL 195 1 3 4 0.7 NCC1OCCc2cc(O)c(O)cc21 10.1021/jm00073a006
16736096 141552 0 None -19 2 Rat 4.5 pKi = 4.5 Binding
Displacement of [3H]CGP-12177 from beta-1 adrenergic receptor in Sprague-Dawley rat cortical membraneDisplacement of [3H]CGP-12177 from beta-1 adrenergic receptor in Sprague-Dawley rat cortical membrane
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 Rat 4.5 pKi = 4.5 Binding
Displacement of [3H]CGP-12177 from beta-1 adrenergic receptor in Sprague-Dawley rat cortical membraneDisplacement of [3H]CGP-12177 from beta-1 adrenergic receptor in Sprague-Dawley rat cortical membrane
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 Rat 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 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 Rat 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 337 6 4 4 3.5 C[C@H](Cc1cccc2ccccc12)NC[C@@H](O)c1cc(O)cc(O)c1 nan
49864355 15429 0 None -1 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 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 7.5 pKi = 7.5 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 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
172745 99648 7 None -2 6 Guinea pig 6.5 pKi = 6.5 Binding
Binding affinity against beta-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of Dihydro-[3H]-alprenololBinding affinity against beta-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of Dihydro-[3H]-alprenolol
ChEMBL 187 2 4 4 0.2 NCC(O)c1ccc(O)c(O)c1F 10.1021/jm00118a019
CHEMBL287587 99648 7 None -2 6 Guinea pig 6.5 pKi = 6.5 Binding
Binding affinity against beta-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of Dihydro-[3H]-alprenololBinding affinity against beta-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of Dihydro-[3H]-alprenolol
ChEMBL 187 2 4 4 0.2 NCC(O)c1ccc(O)c(O)c1F 10.1021/jm00118a019
24936488 17452 0 None -2 3 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta-1 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 -2 3 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta-1 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
145947241 167060 0 None -8 2 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]-CGP-12177 from adrenergic beta1 receptor in Wistar rat cortex incubated for 60 mins by microbeta liquid scintillation counting analysisDisplacement of [3H]-CGP-12177 from adrenergic beta1 receptor in Wistar rat cortex incubated for 60 mins by microbeta liquid scintillation counting analysis
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 -8 2 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]-CGP-12177 from adrenergic beta1 receptor in Wistar rat cortex incubated for 60 mins by microbeta liquid scintillation counting analysisDisplacement of [3H]-CGP-12177 from adrenergic beta1 receptor in Wistar rat cortex incubated for 60 mins by microbeta liquid scintillation counting analysis
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 -8 2 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]-CGP-12177 from adrenergic beta1 receptor in Wistar rat cortex incubated for 60 mins by microbeta liquid scintillation counting analysisDisplacement of [3H]-CGP-12177 from adrenergic beta1 receptor in Wistar rat cortex incubated for 60 mins by microbeta liquid scintillation counting analysis
ChEMBL 449 10 2 7 3.5 COc1ccc(CCNCC(O)COc2cccc3c(=O)c4ccccc4oc23)cc1OC 10.1016/j.bmc.2018.04.038
145947927 167178 0 None -16 2 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]-CGP-12177 from adrenergic beta1 receptor in Wistar rat cortex incubated for 60 mins by microbeta liquid scintillation counting analysisDisplacement of [3H]-CGP-12177 from adrenergic beta1 receptor in Wistar rat cortex incubated for 60 mins by microbeta liquid scintillation counting analysis
ChEMBL 419 9 2 6 3.5 COc1ccccc1CCNCC(O)COc1cccc2c(=O)c3ccccc3oc12 10.1016/j.bmc.2018.04.038
CHEMBL4130151 167178 0 None -16 2 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]-CGP-12177 from adrenergic beta1 receptor in Wistar rat cortex incubated for 60 mins by microbeta liquid scintillation counting analysisDisplacement of [3H]-CGP-12177 from adrenergic beta1 receptor in Wistar rat cortex incubated for 60 mins by microbeta liquid scintillation counting analysis
ChEMBL 419 9 2 6 3.5 COc1ccccc1CCNCC(O)COc1cccc2c(=O)c3ccccc3oc12 10.1016/j.bmc.2018.04.038
CHEMBL4302997 167178 0 None -16 2 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]-CGP-12177 from adrenergic beta1 receptor in Wistar rat cortex incubated for 60 mins by microbeta liquid scintillation counting analysisDisplacement of [3H]-CGP-12177 from adrenergic beta1 receptor in Wistar rat cortex incubated for 60 mins by microbeta liquid scintillation counting analysis
ChEMBL 419 9 2 6 3.5 COc1ccccc1CCNCC(O)COc1cccc2c(=O)c3ccccc3oc12 10.1016/j.bmc.2018.04.038
10376053 13009 0 None -2 3 Guinea pig 6.4 pKi = 6.4 Binding
Binding affinity at Beta-1 adrenergic receptor in guinea pigs by [125I]CYP displacementBinding affinity at Beta-1 adrenergic receptor in guinea pigs by [125I]CYP displacement
ChEMBL 217 1 1 5 0.4 Cc1cnc(N2CCNCC2)c2nccn12 10.1021/jm00099a012
CHEMBL1190547 13009 0 None -2 3 Guinea pig 6.4 pKi = 6.4 Binding
Binding affinity at Beta-1 adrenergic receptor in guinea pigs by [125I]CYP displacementBinding affinity at Beta-1 adrenergic receptor in guinea pigs by [125I]CYP displacement
ChEMBL 217 1 1 5 0.4 Cc1cnc(N2CCNCC2)c2nccn12 10.1021/jm00099a012
CHEMBL541088 13009 0 None -2 3 Guinea pig 6.4 pKi = 6.4 Binding
Binding affinity at Beta-1 adrenergic receptor in guinea pigs by [125I]CYP displacementBinding affinity at Beta-1 adrenergic receptor in guinea pigs by [125I]CYP displacement
ChEMBL 217 1 1 5 0.4 Cc1cnc(N2CCNCC2)c2nccn12 10.1021/jm00099a012
10292413 93830 0 None -7 2 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]iodocyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human adrenergic beta-1 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 6.4 pKi = 6.4 Binding
Displacement of [125I]iodocyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human adrenergic beta-1 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
10162297 153361 0 None -33 3 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]iodocyanopindolol from human cloned adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human cloned adrenergic beta-1 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 -33 3 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]iodocyanopindolol from human cloned adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human cloned adrenergic beta-1 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
9947512 154156 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]iodocyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human adrenergic beta-1 receptor expressed in CHO cells
ChEMBL 369 9 2 6 3.5 CCc1nc(-c2ccc(OCCNC[C@H](O)c3cccnc3)cc2)cs1 10.1016/j.bmcl.2007.06.072
CHEMBL399785 154156 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]iodocyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human adrenergic beta-1 receptor expressed in CHO cells
ChEMBL 369 9 2 6 3.5 CCc1nc(-c2ccc(OCCNC[C@H](O)c3cccnc3)cc2)cs1 10.1016/j.bmcl.2007.06.072
1534 102553 51 None -37 12 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]Iodopindolol from human recombinant adrenergic beta1 receptor expressed in CHO cells coexpressing FLP-IN after 1 to 1.5 hrs by scintillation counting analysisDisplacement of [125I]Iodopindolol from human recombinant adrenergic beta1 receptor expressed in CHO cells coexpressing FLP-IN after 1 to 1.5 hrs by scintillation counting analysis
ChEMBL 174 2 2 1 2.1 CC(N)Cc1c[nH]c2ccccc12 10.1016/j.bmcl.2013.03.066
9287 102553 51 None -37 12 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]Iodopindolol from human recombinant adrenergic beta1 receptor expressed in CHO cells coexpressing FLP-IN after 1 to 1.5 hrs by scintillation counting analysisDisplacement of [125I]Iodopindolol from human recombinant adrenergic beta1 receptor expressed in CHO cells coexpressing FLP-IN after 1 to 1.5 hrs by scintillation counting analysis
ChEMBL 174 2 2 1 2.1 CC(N)Cc1c[nH]c2ccccc12 10.1016/j.bmcl.2013.03.066
CHEMBL30713 102553 51 None -37 12 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]Iodopindolol from human recombinant adrenergic beta1 receptor expressed in CHO cells coexpressing FLP-IN after 1 to 1.5 hrs by scintillation counting analysisDisplacement of [125I]Iodopindolol from human recombinant adrenergic beta1 receptor expressed in CHO cells coexpressing FLP-IN after 1 to 1.5 hrs by scintillation counting analysis
ChEMBL 174 2 2 1 2.1 CC(N)Cc1c[nH]c2ccccc12 10.1016/j.bmcl.2013.03.066
1534 102553 51 None -37 12 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]Iodopindolol from human recombinant adrenergic beta1 receptor expressed in CHO cells coexpressing FLP-IN after 1 to 1.5 hrs by scintillation counting analysisDisplacement of [125I]Iodopindolol from human recombinant adrenergic beta1 receptor expressed in CHO cells coexpressing FLP-IN after 1 to 1.5 hrs by scintillation counting analysis
ChEMBL 174 2 2 1 2.1 CC(N)Cc1c[nH]c2ccccc12 10.1016/j.bmcl.2013.03.066
9287 102553 51 None -37 12 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]Iodopindolol from human recombinant adrenergic beta1 receptor expressed in CHO cells coexpressing FLP-IN after 1 to 1.5 hrs by scintillation counting analysisDisplacement of [125I]Iodopindolol from human recombinant adrenergic beta1 receptor expressed in CHO cells coexpressing FLP-IN after 1 to 1.5 hrs by scintillation counting analysis
ChEMBL 174 2 2 1 2.1 CC(N)Cc1c[nH]c2ccccc12 10.1016/j.bmcl.2013.03.066
CHEMBL30713 102553 51 None -37 12 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]Iodopindolol from human recombinant adrenergic beta1 receptor expressed in CHO cells coexpressing FLP-IN after 1 to 1.5 hrs by scintillation counting analysisDisplacement of [125I]Iodopindolol from human recombinant adrenergic beta1 receptor expressed in CHO cells coexpressing FLP-IN after 1 to 1.5 hrs by scintillation counting analysis
ChEMBL 174 2 2 1 2.1 CC(N)Cc1c[nH]c2ccccc12 10.1016/j.bmcl.2013.03.066
25032872 84913 0 None -112 3 Rat 4.4 pKi = 4.4 Binding
Displacement of [3H]CGP12177 from beta1 adrenoreceptor in Rattus norvegicus (rat) cerebral cortex by liquid scintillation countingDisplacement of [3H]CGP12177 from beta1 adrenoreceptor in Rattus norvegicus (rat) cerebral cortex by liquid scintillation counting
ChEMBL 397 6 1 6 0.9 O=C1C2C3C=CC(C3)C2C(=O)N1OCC(O)CN1CCN(c2ccccc2)CC1 10.1007/s00044-008-9094-3
CHEMBL2261429 84913 0 None -112 3 Rat 4.4 pKi = 4.4 Binding
Displacement of [3H]CGP12177 from beta1 adrenoreceptor in Rattus norvegicus (rat) cerebral cortex by liquid scintillation countingDisplacement of [3H]CGP12177 from beta1 adrenoreceptor in Rattus norvegicus (rat) cerebral cortex by liquid scintillation counting
ChEMBL 397 6 1 6 0.9 O=C1C2C3C=CC(C3)C2C(=O)N1OCC(O)CN1CCN(c2ccccc2)CC1 10.1007/s00044-008-9094-3
49864334 15423 0 None -1 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 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 7.4 pKi = 7.4 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 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
118710938 113236 0 None -6 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 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 -6 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 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
183812 204015 21 None -977 2 Human 5.4 pKi = 5.4 Binding
Binding affinity to human beta1-adrenoceptor by radioligand binding assayBinding affinity to human beta1-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 5.4 pKi = 5.4 Binding
Binding affinity to human beta1-adrenoceptor by radioligand binding assayBinding affinity to human beta1-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
24937137 17561 0 None -23 3 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta-1 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 -23 3 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta-1 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
11248705 89850 0 None -158 10 Human 6.4 pKi = 6.4 Binding
Binding affinity at adrenergic beta 1 receptorBinding affinity at adrenergic beta 1 receptor
ChEMBL 483 6 1 5 5.0 Cc1ccc2c(OCCN3CCC(Cc4ccc5c(c4F)NC(=O)CO5)CC3)cc(Cl)cc2n1 10.1016/j.bmcl.2006.11.031
CHEMBL238519 89850 0 None -158 10 Human 6.4 pKi = 6.4 Binding
Binding affinity at adrenergic beta 1 receptorBinding affinity at adrenergic beta 1 receptor
ChEMBL 483 6 1 5 5.0 Cc1ccc2c(OCCN3CCC(Cc4ccc5c(c4F)NC(=O)CO5)CC3)cc(Cl)cc2n1 10.1016/j.bmcl.2006.11.031
9512 3566 35 None 3 2 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]cyanopindolol from human cloned beta-1 adrenergic receptor expressed in Sf9 cellsDisplacement of [125I]cyanopindolol from human cloned beta-1 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 6.4 pKi = 6.4 Binding
Displacement of [125I]cyanopindolol from human cloned beta-1 adrenergic receptor expressed in Sf9 cellsDisplacement of [125I]cyanopindolol from human cloned beta-1 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 6.4 pKi = 6.4 Binding
Displacement of [125I]cyanopindolol from human cloned beta-1 adrenergic receptor expressed in Sf9 cellsDisplacement of [125I]cyanopindolol from human cloned beta-1 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 6.4 pKi = 6.4 Binding
Displacement of [125I]cyanopindolol from human cloned beta-1 adrenergic receptor expressed in Sf9 cellsDisplacement of [125I]cyanopindolol from human cloned beta-1 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 4.4 pKi = 4.4 Binding
Displacement of [3H]dihydroalprenolol from beta1 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta1 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 4.4 pKi = 4.4 Binding
Displacement of [3H]dihydroalprenolol from beta1 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta1 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
25242457 12475 0 None - 1 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation countingDisplacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation counting
ChEMBL 373 8 4 7 1.0 CC(CO)(CO)NCC(O)COc1cccc2c(=O)c3ccccc3oc12 10.1016/j.bmc.2008.12.031
CHEMBL1186915 12475 0 None - 1 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation countingDisplacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation counting
ChEMBL 373 8 4 7 1.0 CC(CO)(CO)NCC(O)COc1cccc2c(=O)c3ccccc3oc12 10.1016/j.bmc.2008.12.031
CHEMBL482397 12475 0 None - 1 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation countingDisplacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation counting
ChEMBL 373 8 4 7 1.0 CC(CO)(CO)NCC(O)COc1cccc2c(=O)c3ccccc3oc12 10.1016/j.bmc.2008.12.031
118710950 113250 0 None -2 3 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 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 8.4 pKi = 8.4 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 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
118710937 113235 0 None -19 3 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 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 7.4 pKi = 7.4 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 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
49864412 15451 0 None -5 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 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 7.4 pKi = 7.4 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 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
10947658 28475 0 None -363 17 Human 6.4 pKi = 6.4 Binding
Binding affinity against Beta-1 adrenergic receptorBinding affinity against Beta-1 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 -363 17 Human 6.4 pKi = 6.4 Binding
Binding affinity against Beta-1 adrenergic receptorBinding affinity against Beta-1 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
1960 2805 64 None -10 26 Guinea pig 6.4 pKi = 6.4 Binding
Binding affinity against beta-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of Dihydro-[3H]-alprenololBinding affinity against beta-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of Dihydro-[3H]-alprenolol
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00118a019
439260 2805 64 None -10 26 Guinea pig 6.4 pKi = 6.4 Binding
Binding affinity against beta-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of Dihydro-[3H]-alprenololBinding affinity against beta-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of Dihydro-[3H]-alprenolol
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00118a019
505 2805 64 None -10 26 Guinea pig 6.4 pKi = 6.4 Binding
Binding affinity against beta-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of Dihydro-[3H]-alprenololBinding affinity against beta-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of Dihydro-[3H]-alprenolol
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00118a019
CHEMBL1437 2805 64 None -10 26 Guinea pig 6.4 pKi = 6.4 Binding
Binding affinity against beta-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of Dihydro-[3H]-alprenololBinding affinity against beta-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of Dihydro-[3H]-alprenolol
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00118a019
DB00368 2805 64 None -10 26 Guinea pig 6.4 pKi = 6.4 Binding
Binding affinity against beta-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of Dihydro-[3H]-alprenololBinding affinity against beta-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of Dihydro-[3H]-alprenolol
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00118a019
10376607 13234 0 None -1 2 Guinea pig 6.4 pKi = 6.4 Binding
Binding affinity at Beta-1 adrenergic receptor in guinea pigs by [125I]CYP displacementBinding affinity at Beta-1 adrenergic receptor in guinea pigs by [125I]CYP displacement
ChEMBL 231 1 1 5 0.8 Cc1cnc(N2CCNCC2)c2ncc(C)n12 10.1021/jm00099a012
CHEMBL1192423 13234 0 None -1 2 Guinea pig 6.4 pKi = 6.4 Binding
Binding affinity at Beta-1 adrenergic receptor in guinea pigs by [125I]CYP displacementBinding affinity at Beta-1 adrenergic receptor in guinea pigs by [125I]CYP displacement
ChEMBL 231 1 1 5 0.8 Cc1cnc(N2CCNCC2)c2ncc(C)n12 10.1021/jm00099a012
CHEMBL543653 13234 0 None -1 2 Guinea pig 6.4 pKi = 6.4 Binding
Binding affinity at Beta-1 adrenergic receptor in guinea pigs by [125I]CYP displacementBinding affinity at Beta-1 adrenergic receptor in guinea pigs by [125I]CYP displacement
ChEMBL 231 1 1 5 0.8 Cc1cnc(N2CCNCC2)c2ncc(C)n12 10.1021/jm00099a012
131268 112390 24 None -26 3 Guinea pig 6.4 pKi = 6.4 Binding
Binding affinity at Beta-1 adrenergic receptor in guinea pigs by [125I]CYP displacementBinding affinity at Beta-1 adrenergic receptor in guinea pigs by [125I]CYP displacement
ChEMBL 203 1 1 5 0.1 c1cn2ccnc2c(N2CCNCC2)n1 10.1021/jm00099a012
CHEMBL331036 112390 24 None -26 3 Guinea pig 6.4 pKi = 6.4 Binding
Binding affinity at Beta-1 adrenergic receptor in guinea pigs by [125I]CYP displacementBinding affinity at Beta-1 adrenergic receptor in guinea pigs by [125I]CYP displacement
ChEMBL 203 1 1 5 0.1 c1cn2ccnc2c(N2CCNCC2)n1 10.1021/jm00099a012
9967732 93717 0 None -19 2 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]iodocyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human adrenergic beta-1 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 6.4 pKi = 6.4 Binding
Displacement of [125I]iodocyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human adrenergic beta-1 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
9946573 154203 0 None -10 2 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]iodocyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human adrenergic beta-1 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 6.4 pKi = 6.4 Binding
Displacement of [125I]iodocyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human adrenergic beta-1 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
127901 101651 13 None - 1 Rat 5.4 pKi = 5.4 Binding
Displacement of [3H]dihydroalprenolol from adrenergic beta 1 receptor of rat cerebral cortical membranesDisplacement of [3H]dihydroalprenolol from adrenergic beta 1 receptor of rat cerebral cortical membranes
ChEMBL 185 3 3 3 0.8 CNCC(O)c1cccc(O)c1F 10.1021/jm00076a024
CHEMBL302451 101651 13 None - 1 Rat 5.4 pKi = 5.4 Binding
Displacement of [3H]dihydroalprenolol from adrenergic beta 1 receptor of rat cerebral cortical membranesDisplacement of [3H]dihydroalprenolol from adrenergic beta 1 receptor of rat cerebral cortical membranes
ChEMBL 185 3 3 3 0.8 CNCC(O)c1cccc(O)c1F 10.1021/jm00076a024
13864381 206593 3 None -39 4 Rat 4.4 pKi = 4.4 Binding
Tested for binding affinity against beta-1 adrenergic receptor in rat brain using [3H]-CGP- 26505 as radioligandTested for binding affinity against beta-1 adrenergic receptor in rat brain using [3H]-CGP- 26505 as radioligand
ChEMBL 195 1 3 4 0.7 NCC1OCCc2c1ccc(O)c2O 10.1021/jm00073a006
CHEMBL542683 206593 3 None -39 4 Rat 4.4 pKi = 4.4 Binding
Tested for binding affinity against beta-1 adrenergic receptor in rat brain using [3H]-CGP- 26505 as radioligandTested for binding affinity against beta-1 adrenergic receptor in rat brain using [3H]-CGP- 26505 as radioligand
ChEMBL 195 1 3 4 0.7 NCC1OCCc2c1ccc(O)c2O 10.1021/jm00073a006
CHEMBL99361 206593 3 None -39 4 Rat 4.4 pKi = 4.4 Binding
Tested for binding affinity against beta-1 adrenergic receptor in rat brain using [3H]-CGP- 26505 as radioligandTested for binding affinity against beta-1 adrenergic receptor in rat brain using [3H]-CGP- 26505 as radioligand
ChEMBL 195 1 3 4 0.7 NCC1OCCc2c1ccc(O)c2O 10.1021/jm00073a006
122237 162627 16 None - 1 Rat 4.4 pKi = 4.4 Binding
Binding of [3H]dihydroalprenolol to beta-1 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-1 adrenergic receptor of rat cerebral cortical membranes
ChEMBL 171 2 3 3 0.7 NCCc1cc(O)c(O)cc1F 10.1021/jm990599h
CHEMBL41818 162627 16 None - 1 Rat 4.4 pKi = 4.4 Binding
Binding of [3H]dihydroalprenolol to beta-1 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-1 adrenergic receptor of rat cerebral cortical membranes
ChEMBL 171 2 3 3 0.7 NCCc1cc(O)c(O)cc1F 10.1021/jm990599h
44444193 153269 0 None -15 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]iodocyanopindolol from human cloned adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human cloned adrenergic beta-1 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 -15 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]iodocyanopindolol from human cloned adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human cloned adrenergic beta-1 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
11625333 77250 0 None -2 2 Human 6.4 pKi = 6.4 Binding
Binding affinity to human beta1-adrenoceptor by radioligand binding assayBinding affinity to human beta1-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 6.4 pKi = 6.4 Binding
Binding affinity to human beta1-adrenoceptor by radioligand binding assayBinding affinity to human beta1-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
1978 248 54 None -16 6 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 336 10 3 5 3.0 CCCC(=Nc1ccc(c(c1)C(=O)C)OCC(CNC(C)C)O)O nan
40 248 54 None -16 6 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 336 10 3 5 3.0 CCCC(=Nc1ccc(c(c1)C(=O)C)OCC(CNC(C)C)O)O nan
7107 248 54 None -16 6 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 336 10 3 5 3.0 CCCC(=Nc1ccc(c(c1)C(=O)C)OCC(CNC(C)C)O)O nan
CHEMBL642 248 54 None -16 6 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 336 10 3 5 3.0 CCCC(=Nc1ccc(c(c1)C(=O)C)OCC(CNC(C)C)O)O nan
DB01193 248 54 None -16 6 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 336 10 3 5 3.0 CCCC(=Nc1ccc(c(c1)C(=O)C)OCC(CNC(C)C)O)O nan
16737588 85375 0 None -4 2 Rat 4.4 pKi = 4.4 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 273 6 4 4 2.0 Oc1cc(O)cc([C@@H](O)CNCCc2ccccc2)c1 nan
CHEMBL229620 85375 0 None -4 2 Rat 4.4 pKi = 4.4 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 273 6 4 4 2.0 Oc1cc(O)cc([C@@H](O)CNCCc2ccccc2)c1 nan
16737588 85375 0 None -4 2 Rat 4.4 pKi = 4.4 Binding
Displacement of [3H]CGP-12177 from beta-1 adrenergic receptor in Sprague-Dawley rat cortical membraneDisplacement of [3H]CGP-12177 from beta-1 adrenergic receptor in Sprague-Dawley rat cortical membrane
ChEMBL 273 6 4 4 2.0 Oc1cc(O)cc([C@@H](O)CNCCc2ccccc2)c1 10.1021/jm070030d
CHEMBL229620 85375 0 None -4 2 Rat 4.4 pKi = 4.4 Binding
Displacement of [3H]CGP-12177 from beta-1 adrenergic receptor in Sprague-Dawley rat cortical membraneDisplacement of [3H]CGP-12177 from beta-1 adrenergic receptor in Sprague-Dawley rat cortical membrane
ChEMBL 273 6 4 4 2.0 Oc1cc(O)cc([C@@H](O)CNCCc2ccccc2)c1 10.1021/jm070030d
44396596 122771 0 None -3 3 Human 7.4 pKi = 7.4 Binding
Binding inhibition constant was determined by inhibition of [125I]iodocyanopindolol binding to Beta-1 adrenergic receptorBinding inhibition constant was determined by inhibition of [125I]iodocyanopindolol binding to Beta-1 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 -3 3 Human 7.4 pKi = 7.4 Binding
Binding inhibition constant was determined by inhibition of [125I]iodocyanopindolol binding to Beta-1 adrenergic receptorBinding inhibition constant was determined by inhibition of [125I]iodocyanopindolol binding to Beta-1 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
2249 509 106 None -5 12 Human 6.4 pKi = 6.4 Binding
Displacement of radiolabeled atenolol from human adrenergic beta-1 receptorDisplacement of radiolabeled atenolol from human adrenergic beta-1 receptor
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1021/jm8007618
255 509 106 None -5 12 Human 6.4 pKi = 6.4 Binding
Displacement of radiolabeled atenolol from human adrenergic beta-1 receptorDisplacement of radiolabeled atenolol from human adrenergic beta-1 receptor
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1021/jm8007618
548 509 106 None -5 12 Human 6.4 pKi = 6.4 Binding
Displacement of radiolabeled atenolol from human adrenergic beta-1 receptorDisplacement of radiolabeled atenolol from human adrenergic beta-1 receptor
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1021/jm8007618
CHEMBL24 509 106 None -5 12 Human 6.4 pKi = 6.4 Binding
Displacement of radiolabeled atenolol from human adrenergic beta-1 receptorDisplacement of radiolabeled atenolol from human adrenergic beta-1 receptor
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1021/jm8007618
DB00335 509 106 None -5 12 Human 6.4 pKi = 6.4 Binding
Displacement of radiolabeled atenolol from human adrenergic beta-1 receptorDisplacement of radiolabeled atenolol from human adrenergic beta-1 receptor
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 10.1021/jm8007618
52944986 17416 0 None -30 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta-1 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 -30 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta-1 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
118710946 113244 0 None -1 2 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 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 6.4 pKi = 6.4 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 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
44312421 162774 0 None -2 3 Human 6.4 pKi = 6.4 Binding
Compound was tested for its binding affinity against Beta-1 adrenergic receptor in CHO cell membrane using [125I]iodocyanopindolol as the radioligand.Compound was tested for its binding affinity against Beta-1 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 6.4 pKi = 6.4 Binding
Compound was tested for its binding affinity against Beta-1 adrenergic receptor in CHO cell membrane using [125I]iodocyanopindolol as the radioligand.Compound was tested for its binding affinity against Beta-1 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
46889767 6979 0 None -5 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta-1 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta-1 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 6.4 pKi = 6.4 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta-1 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta-1 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
49783415 17481 0 None -5888 13 Rat 5.4 pKi = 5.4 Binding
Binding affinity to rat adrenergic beta-1 receptorBinding affinity to rat adrenergic beta-1 receptor
ChEMBL 320 7 1 5 2.9 CCCCN1CCC(COC(=O)c2ccc(N)c(OC)c2)CC1 10.1021/jm100668r
CHEMBL1258452 17481 0 None -5888 13 Rat 5.4 pKi = 5.4 Binding
Binding affinity to rat adrenergic beta-1 receptorBinding affinity to rat adrenergic beta-1 receptor
ChEMBL 320 7 1 5 2.9 CCCCN1CCC(COC(=O)c2ccc(N)c(OC)c2)CC1 10.1021/jm100668r
10381669 12466 0 None - 1 Rat 4.4 pKi = 4.4 Binding
Displacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation countingDisplacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation counting
ChEMBL 325 7 2 5 2.5 C=CCNCC(O)COc1ccc2c(=O)c3ccccc3oc2c1 10.1016/j.bmc.2008.12.031
CHEMBL1186871 12466 0 None - 1 Rat 4.4 pKi = 4.4 Binding
Displacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation countingDisplacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation counting
ChEMBL 325 7 2 5 2.5 C=CCNCC(O)COc1ccc2c(=O)c3ccccc3oc2c1 10.1016/j.bmc.2008.12.031
CHEMBL481414 12466 0 None - 1 Rat 4.4 pKi = 4.4 Binding
Displacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation countingDisplacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation counting
ChEMBL 325 7 2 5 2.5 C=CCNCC(O)COc1ccc2c(=O)c3ccccc3oc2c1 10.1016/j.bmc.2008.12.031
52949934 17451 0 None -5 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta-1 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 -5 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta-1 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
49864415 15454 0 None -117 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 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 6.4 pKi = 6.4 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 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
1862 161 14 None -52 7 Rat 4.4 pKi = 4.4 Binding
Displacement of [3H]dihydroalprenolol from adrenergic beta 1 receptor of rat cerebral cortical membranesDisplacement of [3H]dihydroalprenolol from adrenergic beta 1 receptor of rat cerebral cortical membranes
ChEMBL 187 2 4 4 0.2 NCC(c1cc(O)c(cc1F)O)O 10.1021/jm00076a024
510 161 14 None -52 7 Rat 4.4 pKi = 4.4 Binding
Displacement of [3H]dihydroalprenolol from adrenergic beta 1 receptor of rat cerebral cortical membranesDisplacement of [3H]dihydroalprenolol from adrenergic beta 1 receptor of rat cerebral cortical membranes
ChEMBL 187 2 4 4 0.2 NCC(c1cc(O)c(cc1F)O)O 10.1021/jm00076a024
CHEMBL281232 161 14 None -52 7 Rat 4.4 pKi = 4.4 Binding
Displacement of [3H]dihydroalprenolol from adrenergic beta 1 receptor of rat cerebral cortical membranesDisplacement of [3H]dihydroalprenolol from adrenergic beta 1 receptor of rat cerebral cortical membranes
ChEMBL 187 2 4 4 0.2 NCC(c1cc(O)c(cc1F)O)O 10.1021/jm00076a024
46889642 6862 0 None -3 3 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta-1 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta-1 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 5.3 pKi = 5.3 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta-1 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta-1 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
4806 3933 85 None -2 13 Human 7.3 pKi = 7.3 Binding
Binding affinity to human beta 1 adrenergic receptorBinding affinity to human beta 1 adrenergic receptor
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
7351 3933 85 None -2 13 Human 7.3 pKi = 7.3 Binding
Binding affinity to human beta 1 adrenergic receptorBinding affinity to human beta 1 adrenergic receptor
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
9966051 3933 85 None -2 13 Human 7.3 pKi = 7.3 Binding
Binding affinity to human beta 1 adrenergic receptorBinding affinity to human beta 1 adrenergic receptor
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
CHEMBL2104993 3933 85 None -2 13 Human 7.3 pKi = 7.3 Binding
Binding affinity to human beta 1 adrenergic receptorBinding affinity to human beta 1 adrenergic receptor
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
DB09068 3933 85 None -2 13 Human 7.3 pKi = 7.3 Binding
Binding affinity to human beta 1 adrenergic receptorBinding affinity to human beta 1 adrenergic receptor
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
52948792 17523 0 None -5 3 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta-1 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 -5 3 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta-1 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
44571264 12470 0 None - 1 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation countingDisplacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation counting
ChEMBL 407 8 4 7 1.7 CC(CO)(CO)NCC(O)COc1cccc2c(=O)c3ccc(Cl)cc3oc12 10.1016/j.bmc.2008.12.031
CHEMBL1186886 12470 0 None - 1 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation countingDisplacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation counting
ChEMBL 407 8 4 7 1.7 CC(CO)(CO)NCC(O)COc1cccc2c(=O)c3ccc(Cl)cc3oc12 10.1016/j.bmc.2008.12.031
CHEMBL481799 12470 0 None - 1 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation countingDisplacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation counting
ChEMBL 407 8 4 7 1.7 CC(CO)(CO)NCC(O)COc1cccc2c(=O)c3ccc(Cl)cc3oc12 10.1016/j.bmc.2008.12.031
10207209 168649 0 None -309 3 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]iodocyanopindolol from human cloned adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human cloned adrenergic beta-1 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 -309 3 Human 4.3 pKi = 4.3 Binding
Displacement of [125I]iodocyanopindolol from human cloned adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human cloned adrenergic beta-1 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
10324985 76413 7 None -354 17 Human 6.3 pKi = 6.3 Binding
Binding affinity to adrenergic beta-1 receptorBinding affinity to adrenergic beta-1 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 -354 17 Human 6.3 pKi = 6.3 Binding
Binding affinity to adrenergic beta-1 receptorBinding affinity to adrenergic beta-1 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 -354 17 Human 6.3 pKi = 6.3 Binding
Binding affinity to adrenergic beta-1 receptorBinding affinity to adrenergic beta-1 receptor
ChEMBL 423 7 0 8 1.7 COc1ccc2cccc(N3CCN(CCCCn4ncc(=O)n(C)c4=O)CC3)c2c1 10.1021/jm050725j
16717791 77247 0 None -1 2 Human 6.3 pKi = 6.3 Binding
Binding affinity to human beta1-adrenoceptor by radioligand binding assayBinding affinity to human beta1-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 6.3 pKi = 6.3 Binding
Binding affinity to human beta1-adrenoceptor by radioligand binding assayBinding affinity to human beta1-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
10236758 115259 3 None -48977 13 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]CGP12177 from human recombinant beta1 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by beta counting methodDisplacement of [3H]CGP12177 from human recombinant beta1 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 -48977 13 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]CGP12177 from human recombinant beta1 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by beta counting methodDisplacement of [3H]CGP12177 from human recombinant beta1 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
44396568 66934 0 None -28 3 Human 6.3 pKi = 6.3 Binding
Binding inhibition constant was determined by inhibition of [125I]iodocyanopindolol binding to Beta-1 adrenergic receptorBinding inhibition constant was determined by inhibition of [125I]iodocyanopindolol binding to Beta-1 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 -28 3 Human 6.3 pKi = 6.3 Binding
Binding inhibition constant was determined by inhibition of [125I]iodocyanopindolol binding to Beta-1 adrenergic receptorBinding inhibition constant was determined by inhibition of [125I]iodocyanopindolol binding to Beta-1 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
360400 96804 2 None -1 2 Rat 4.3 pKi = 4.3 Binding
Compound was evaluated for beta adrenergic binding affinity towards beta-1 receptor of rat brainCompound was evaluated for beta adrenergic binding affinity towards beta-1 receptor of rat brain
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 Rat 4.3 pKi = 4.3 Binding
Compound was evaluated for beta adrenergic binding affinity towards beta-1 receptor of rat brainCompound was evaluated for beta adrenergic binding affinity towards beta-1 receptor of rat brain
ChEMBL 237 2 2 4 1.9 CC(C)N1CCOC(c2ccc(O)c(O)c2)C1 10.1021/jm00084a006
24937389 17251 0 None -478 3 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta-1 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 -478 3 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta-1 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
52948728 17250 0 None -8 3 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta-1 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 -8 3 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta-1 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
1786 2474 79 None 1 11 Mouse 7.3 pKi = 7.3 Binding
Displacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T 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 1 11 Mouse 7.3 pKi = 7.3 Binding
Displacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T 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 1 11 Mouse 7.3 pKi = 7.3 Binding
Displacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T 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 1 11 Mouse 7.3 pKi = 7.3 Binding
Displacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T 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 1 11 Mouse 7.3 pKi = 7.3 Binding
Displacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranes
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1016/j.bmc.2019.05.034
155516656 169549 0 None 40 2 Mouse 7.3 pKi = 7.3 Binding
Displacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T 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 Mouse 7.3 pKi = 7.3 Binding
Displacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T 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
44444189 94047 0 None -8 3 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]iodocyanopindolol from human cloned adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human cloned adrenergic beta-1 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 -8 3 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]iodocyanopindolol from human cloned adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human cloned adrenergic beta-1 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
72545007 92676 0 None -3 5 Pig 6.3 pKi = 6.3 Binding
Displacement of [3H]-prazosin from alpha1-adrenergic receptor in pig cerebral cortexDisplacement of [3H]-prazosin from alpha1-adrenergic receptor in pig cerebral cortex
ChEMBL 407 12 0 8 1.6 COc1ccccc1N1CCN(Cc2cn(CCOCCOCCF)nn2)CC1 10.1016/j.bmcl.2013.09.026
CHEMBL2443000 92676 0 None -3 5 Pig 6.3 pKi = 6.3 Binding
Displacement of [3H]-prazosin from alpha1-adrenergic receptor in pig cerebral cortexDisplacement of [3H]-prazosin from alpha1-adrenergic receptor in pig cerebral cortex
ChEMBL 407 12 0 8 1.6 COc1ccccc1N1CCN(Cc2cn(CCOCCOCCF)nn2)CC1 10.1016/j.bmcl.2013.09.026
72545009 92678 0 None 1 5 Pig 6.3 pKi = 6.3 Binding
Displacement of [3H]-prazosin from alpha1-adrenergic receptor in pig cerebral cortexDisplacement of [3H]-prazosin from alpha1-adrenergic receptor in pig cerebral cortex
ChEMBL 437 6 3 10 -0.4 COc1ccccc1N1CCN(Cc2cn([C@@H]3O[C@H](CO)[C@@H](O)[C@H](O)[C@H]3F)nn2)CC1 10.1016/j.bmcl.2013.09.026
CHEMBL2443002 92678 0 None 1 5 Pig 6.3 pKi = 6.3 Binding
Displacement of [3H]-prazosin from alpha1-adrenergic receptor in pig cerebral cortexDisplacement of [3H]-prazosin from alpha1-adrenergic receptor in pig cerebral cortex
ChEMBL 437 6 3 10 -0.4 COc1ccccc1N1CCN(Cc2cn([C@@H]3O[C@H](CO)[C@@H](O)[C@H](O)[C@H]3F)nn2)CC1 10.1016/j.bmcl.2013.09.026
52946357 17525 0 None -11 3 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta-1 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 -11 3 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta-1 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
127045853 139250 0 None -20 6 Mouse 8.3 pKi = 8.3 Binding
Displacement of [3H]CGP12177 from mouse beta1 receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from mouse beta1 receptor expressed in HEK293 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 Mouse 8.3 pKi = 8.3 Binding
Displacement of [3H]CGP12177 from mouse beta1 receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from mouse beta1 receptor expressed in HEK293 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
11757304 99846 0 None - 1 Human 8.3 pKi = 8.3 Binding
Inhibition of [3H]dihydroalprenolol binding to beta 1 adrenoceptor from turkey erythrocyte membranes.Inhibition of [3H]dihydroalprenolol binding to beta 1 adrenoceptor from turkey erythrocyte membranes.
ChEMBL 550 11 5 9 0.3 NS(=O)(=O)c1cc(S(=O)(=O)NCCNCC(O)COc2cccc3c2SCC(=O)N3)ccc1Cl 10.1021/jm00053a020
CHEMBL289390 99846 0 None - 1 Human 8.3 pKi = 8.3 Binding
Inhibition of [3H]dihydroalprenolol binding to beta 1 adrenoceptor from turkey erythrocyte membranes.Inhibition of [3H]dihydroalprenolol binding to beta 1 adrenoceptor from turkey erythrocyte membranes.
ChEMBL 550 11 5 9 0.3 NS(=O)(=O)c1cc(S(=O)(=O)NCCNCC(O)COc2cccc3c2SCC(=O)N3)ccc1Cl 10.1021/jm00053a020
9984829 34903 0 None -1 2 Rat 8.3 pKi = 8.3 Binding
Compound was evaluated for its Beta-1 adrenergic receptor binding affinity by measuring the displacement of [3H]dihydroalprenolol binding in rat heartCompound was evaluated for its Beta-1 adrenergic receptor binding affinity by measuring the displacement of [3H]dihydroalprenolol binding in rat heart
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 Rat 8.3 pKi = 8.3 Binding
Compound was evaluated for its Beta-1 adrenergic receptor binding affinity by measuring the displacement of [3H]dihydroalprenolol binding in rat heartCompound was evaluated for its Beta-1 adrenergic receptor binding affinity by measuring the displacement of [3H]dihydroalprenolol binding in rat heart
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
2405 658 71 None 1 4 Mouse 8.3 pKi = 8.3 Binding
Displacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T 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 1 4 Mouse 8.3 pKi = 8.3 Binding
Displacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T 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 1 4 Mouse 8.3 pKi = 8.3 Binding
Displacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T 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 1 4 Mouse 8.3 pKi = 8.3 Binding
Displacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T 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 1 4 Mouse 8.3 pKi = 8.3 Binding
Displacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T 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
33624 3749 29 None -7 9 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-CGP12177 from human beta1 ADR expressed in HEK293T cell membranes after 90 mins by scintillation countingDisplacement of [3H]-CGP12177 from human beta1 ADR expressed in HEK293T cell membranes 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 -7 9 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-CGP12177 from human beta1 ADR expressed in HEK293T cell membranes after 90 mins by scintillation countingDisplacement of [3H]-CGP12177 from human beta1 ADR expressed in HEK293T cell membranes 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 -7 9 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-CGP12177 from human beta1 ADR expressed in HEK293T cell membranes after 90 mins by scintillation countingDisplacement of [3H]-CGP12177 from human beta1 ADR expressed in HEK293T cell membranes 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 -7 9 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-CGP12177 from human beta1 ADR expressed in HEK293T cell membranes after 90 mins by scintillation countingDisplacement of [3H]-CGP12177 from human beta1 ADR expressed in HEK293T cell membranes 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 -7 9 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-CGP12177 from human beta1 ADR expressed in HEK293T cell membranes after 90 mins by scintillation countingDisplacement of [3H]-CGP12177 from human beta1 ADR expressed in HEK293T cell membranes 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
145948125 167167 0 None -17 2 Rat 8.3 pKi = 8.3 Binding
Displacement of [3H]-CGP-12177 from adrenergic beta1 receptor in Wistar rat cortex incubated for 60 mins by microbeta liquid scintillation counting analysisDisplacement of [3H]-CGP-12177 from adrenergic beta1 receptor in Wistar rat cortex incubated for 60 mins by microbeta liquid scintillation counting analysis
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 -17 2 Rat 8.3 pKi = 8.3 Binding
Displacement of [3H]-CGP-12177 from adrenergic beta1 receptor in Wistar rat cortex incubated for 60 mins by microbeta liquid scintillation counting analysisDisplacement of [3H]-CGP-12177 from adrenergic beta1 receptor in Wistar rat cortex incubated for 60 mins by microbeta liquid scintillation counting analysis
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 -17 2 Rat 8.3 pKi = 8.3 Binding
Displacement of [3H]-CGP-12177 from adrenergic beta1 receptor in Wistar rat cortex incubated for 60 mins by microbeta liquid scintillation counting analysisDisplacement of [3H]-CGP-12177 from adrenergic beta1 receptor in Wistar rat cortex incubated for 60 mins by microbeta liquid scintillation counting analysis
ChEMBL 341 5 2 5 3.1 CC(C)(C)NCC(O)COc1cccc2c(=O)c3ccccc3oc12 10.1016/j.bmc.2018.04.038
68807656 113246 0 None -1 3 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 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 8.3 pKi = 8.3 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 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
102262219 139516 0 None -12 6 Mouse 8.2 pKi = 8.2 Binding
Displacement of [3H]CGP12177 from mouse beta1 receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from mouse beta1 receptor expressed in HEK293 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 Mouse 8.2 pKi = 8.2 Binding
Displacement of [3H]CGP12177 from mouse beta1 receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from mouse beta1 receptor expressed in HEK293 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
1531 2226 64 None -1 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
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 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
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 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
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 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
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 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O nan
10297331 93917 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]iodocyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human adrenergic beta-1 receptor expressed in CHO cells
ChEMBL 445 12 2 7 4.2 O[C@@H](CNCCOc1ccc(-c2coc(COCc3ccccc3)n2)cc1)c1cccnc1 10.1016/j.bmcl.2007.06.072
CHEMBL250760 93917 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]iodocyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human adrenergic beta-1 receptor expressed in CHO cells
ChEMBL 445 12 2 7 4.2 O[C@@H](CNCCOc1ccc(-c2coc(COCc3ccccc3)n2)cc1)c1cccnc1 10.1016/j.bmcl.2007.06.072
10081581 11080 0 None 2 2 Rat 6.3 pKi = 6.3 Binding
Binding affinity against beta-1-adrenergic receptor in rat brainBinding affinity against beta-1-adrenergic receptor in rat brain
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 Rat 6.3 pKi = 6.3 Binding
Binding affinity against beta-1-adrenergic receptor in rat brainBinding affinity against beta-1-adrenergic receptor in rat brain
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 Rat 6.3 pKi = 6.3 Binding
Binding affinity against beta-1-adrenergic receptor in rat brainBinding affinity against beta-1-adrenergic receptor in rat brain
ChEMBL 202 6 2 4 1.1 CC/C=N/OCC(O)CNC(C)(C)C 10.1021/jm00036a018
10266538 116457 2 None -1 2 Guinea pig 6.3 pKi = 6.3 Binding
Binding affinity at Beta-1 adrenergic receptor in guinea pigs by [125I]CYP displacementBinding affinity at Beta-1 adrenergic receptor in guinea pigs by [125I]CYP displacement
ChEMBL 295 1 0 5 1.2 CN1CCN(c2ncc(Br)n3ccnc23)CC1 10.1021/jm00099a012
CHEMBL338704 116457 2 None -1 2 Guinea pig 6.3 pKi = 6.3 Binding
Binding affinity at Beta-1 adrenergic receptor in guinea pigs by [125I]CYP displacementBinding affinity at Beta-1 adrenergic receptor in guinea pigs by [125I]CYP displacement
ChEMBL 295 1 0 5 1.2 CN1CCN(c2ncc(Br)n3ccnc23)CC1 10.1021/jm00099a012
10059780 12835 0 None -9 3 Guinea pig 5.3 pKi = 5.3 Binding
Binding affinity at Beta-1 adrenergic receptor in guinea pigs by [125I]CYP displacementBinding affinity at Beta-1 adrenergic receptor in guinea pigs by [125I]CYP displacement
ChEMBL 231 2 1 5 0.7 CCc1cnc2c(N3CCNCC3)nccn12 10.1021/jm00099a012
CHEMBL1189347 12835 0 None -9 3 Guinea pig 5.3 pKi = 5.3 Binding
Binding affinity at Beta-1 adrenergic receptor in guinea pigs by [125I]CYP displacementBinding affinity at Beta-1 adrenergic receptor in guinea pigs by [125I]CYP displacement
ChEMBL 231 2 1 5 0.7 CCc1cnc2c(N3CCNCC3)nccn12 10.1021/jm00099a012
CHEMBL538537 12835 0 None -9 3 Guinea pig 5.3 pKi = 5.3 Binding
Binding affinity at Beta-1 adrenergic receptor in guinea pigs by [125I]CYP displacementBinding affinity at Beta-1 adrenergic receptor in guinea pigs by [125I]CYP displacement
ChEMBL 231 2 1 5 0.7 CCc1cnc2c(N3CCNCC3)nccn12 10.1021/jm00099a012
127047996 139103 0 None -1122 6 Mouse 5.3 pKi = 5.3 Binding
Displacement of [3H]CGP12177 from mouse beta1 receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from mouse beta1 receptor expressed in HEK293 cells
ChEMBL 303 8 3 5 2.3 COc1ccccc1OCCNCCc1ccc(O)c(O)c1 10.1016/j.bmc.2016.04.028
CHEMBL3797758 139103 0 None -1122 6 Mouse 5.3 pKi = 5.3 Binding
Displacement of [3H]CGP12177 from mouse beta1 receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from mouse beta1 receptor expressed in HEK293 cells
ChEMBL 303 8 3 5 2.3 COc1ccccc1OCCNCCc1ccc(O)c(O)c1 10.1016/j.bmc.2016.04.028
5806 102690 16 None 1 3 Rat 7.3 pKi = 7.3 Binding
Binding affinity against beta-1-adrenergic receptor in rat brainBinding affinity against beta-1-adrenergic receptor in rat brain
ChEMBL 247 4 2 2 3.0 CC(C)NCC(O)c1ccc(Cl)c(Cl)c1 10.1021/jm00036a018
CHEMBL30816 102690 16 None 1 3 Rat 7.3 pKi = 7.3 Binding
Binding affinity against beta-1-adrenergic receptor in rat brainBinding affinity against beta-1-adrenergic receptor in rat brain
ChEMBL 247 4 2 2 3.0 CC(C)NCC(O)c1ccc(Cl)c(Cl)c1 10.1021/jm00036a018
10773922 156940 0 None -1 2 Rat 4.3 pKi = 4.3 Binding
Binding of [3H]dihydroalprenolol to beta-1 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-1 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 Rat 4.3 pKi = 4.3 Binding
Binding of [3H]dihydroalprenolol to beta-1 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-1 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
16736514 142998 0 None -2 2 Rat 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 273 6 4 4 2.0 Oc1cc(O)cc([C@H](O)CNCCc2ccccc2)c1 nan
CHEMBL389902 142998 0 None -2 2 Rat 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 273 6 4 4 2.0 Oc1cc(O)cc([C@H](O)CNCCc2ccccc2)c1 nan
16736514 142998 0 None -2 2 Rat 4.3 pKi = 4.3 Binding
Displacement of [3H]CGP-12177 from beta-1 adrenergic receptor in Sprague-Dawley rat cortical membraneDisplacement of [3H]CGP-12177 from beta-1 adrenergic receptor in Sprague-Dawley rat cortical membrane
ChEMBL 273 6 4 4 2.0 Oc1cc(O)cc([C@H](O)CNCCc2ccccc2)c1 10.1021/jm070030d
CHEMBL389902 142998 0 None -2 2 Rat 4.3 pKi = 4.3 Binding
Displacement of [3H]CGP-12177 from beta-1 adrenergic receptor in Sprague-Dawley rat cortical membraneDisplacement of [3H]CGP-12177 from beta-1 adrenergic receptor in Sprague-Dawley rat cortical membrane
ChEMBL 273 6 4 4 2.0 Oc1cc(O)cc([C@H](O)CNCCc2ccccc2)c1 10.1021/jm070030d
44424581 142791 0 None 1 2 Rat 4.3 pKi = 4.3 Binding
Displacement of [3H]CGP-12177 from beta-1 adrenergic receptor in Sprague-Dawley rat cortical membraneDisplacement of [3H]CGP-12177 from beta-1 adrenergic receptor in Sprague-Dawley rat cortical membrane
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 Rat 4.3 pKi = 4.3 Binding
Displacement of [3H]CGP-12177 from beta-1 adrenergic receptor in Sprague-Dawley rat cortical membraneDisplacement of [3H]CGP-12177 from beta-1 adrenergic receptor in Sprague-Dawley rat cortical membrane
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 Rat 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 Rat 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
4276762 6861 11 None -1 3 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta-1 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta-1 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 6.3 pKi = 6.3 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta-1 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta-1 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
127046951 139359 0 None -11 6 Mouse 6.3 pKi = 6.3 Binding
Displacement of [3H]CGP12177 from mouse beta1 receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from mouse beta1 receptor expressed in HEK293 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 Mouse 6.3 pKi = 6.3 Binding
Displacement of [3H]CGP12177 from mouse beta1 receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from mouse beta1 receptor expressed in HEK293 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
70541 87092 82 None 1 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]dihydroalprenolol from human wild type beta1 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysisDisplacement of [3H]dihydroalprenolol from human wild type beta1 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysis
ChEMBL 190 1 1 2 1.7 Cc1cccc(N2CCNCC2)c1C 10.1021/jm400140q
CHEMBL2335161 87092 82 None 1 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]dihydroalprenolol from human wild type beta1 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysisDisplacement of [3H]dihydroalprenolol from human wild type beta1 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysis
ChEMBL 190 1 1 2 1.7 Cc1cccc(N2CCNCC2)c1C 10.1021/jm400140q
1786 2474 79 None -1 11 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]CGP12177 from human beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from human beta1 adrenoceptor expressed in HEK293T 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 -1 11 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]CGP12177 from human beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from human beta1 adrenoceptor expressed in HEK293T 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 -1 11 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]CGP12177 from human beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from human beta1 adrenoceptor expressed in HEK293T 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 -1 11 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]CGP12177 from human beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from human beta1 adrenoceptor expressed in HEK293T 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 -1 11 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]CGP12177 from human beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from human beta1 adrenoceptor expressed in HEK293T cell membranes
ChEMBL 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10.1016/j.bmc.2019.05.034
2419 3394 80 None -16 6 Mouse 6.3 pKi = 6.3 Binding
Displacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T 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 Mouse 6.3 pKi = 6.3 Binding
Displacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T 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 Mouse 6.3 pKi = 6.3 Binding
Displacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T 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 Mouse 6.3 pKi = 6.3 Binding
Displacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T 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 Mouse 6.3 pKi = 6.3 Binding
Displacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T 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
10512270 164796 9 None -5 2 Rat 6.3 pKi = 6.3 Binding
Binding of [3H]dihydroalprenolol to beta-1 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-1 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 Rat 6.3 pKi = 6.3 Binding
Binding of [3H]dihydroalprenolol to beta-1 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-1 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
24937390 17418 0 None -2 3 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta-1 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 -2 3 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta-1 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
10207208 153621 0 None -63 3 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]iodocyanopindolol from human cloned adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human cloned adrenergic beta-1 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 -63 3 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]iodocyanopindolol from human cloned adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human cloned adrenergic beta-1 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
24937016 17560 0 None -5 3 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta-1 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 -5 3 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta-1 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
44351358 116428 4 None - 1 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]dihydroalprenolol from adrenergic beta 1 receptor of rat cerebral cortical membranesDisplacement of [3H]dihydroalprenolol from adrenergic beta 1 receptor of rat cerebral cortical membranes
ChEMBL 205 2 4 4 0.4 NCC(O)c1cc(F)c(O)c(O)c1F 10.1021/jm00076a024
CHEMBL338564 116428 4 None - 1 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]dihydroalprenolol from adrenergic beta 1 receptor of rat cerebral cortical membranesDisplacement of [3H]dihydroalprenolol from adrenergic beta 1 receptor of rat cerebral cortical membranes
ChEMBL 205 2 4 4 0.4 NCC(O)c1cc(F)c(O)c(O)c1F 10.1021/jm00076a024
44444188 94046 0 None -2 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]iodocyanopindolol from human cloned adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human cloned adrenergic beta-1 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 -2 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]iodocyanopindolol from human cloned adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human cloned adrenergic beta-1 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
3931 2208 42 None -3 2 Human 6.2 pKi = 6.2 Binding
Inhibition of I-iodocyanopindolol binding to human beta 1 adrenergic receptorsInhibition of I-iodocyanopindolol binding to human beta 1 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 6.2 pKi = 6.2 Binding
Inhibition of I-iodocyanopindolol binding to human beta 1 adrenergic receptorsInhibition of I-iodocyanopindolol binding to human beta 1 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 6.2 pKi = 6.2 Binding
Inhibition of I-iodocyanopindolol binding to human beta 1 adrenergic receptorsInhibition of I-iodocyanopindolol binding to human beta 1 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
118710942 113240 0 None -8 3 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 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 7.2 pKi = 7.2 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 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
49864378 15440 0 None -1 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 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 7.2 pKi = 7.2 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 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
15221055 202700 0 None -5 2 Human 4.2 pKi = 4.2 Binding
Compound was tested for its binding affinity against Beta-1 adrenergic receptor in CHO cell membrane using [125I]iodocyanopindolol as the radioligand.Compound was tested for its binding affinity against Beta-1 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 4.2 pKi = 4.2 Binding
Compound was tested for its binding affinity against Beta-1 adrenergic receptor in CHO cell membrane using [125I]iodocyanopindolol as the radioligand.Compound was tested for its binding affinity against Beta-1 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
44286983 141166 0 None -3 3 Human 6.2 pKi = 6.2 Binding
Ability to bind to human Beta-1 adrenergic receptor using membranes of stably transfected CHO cellsAbility to bind to human Beta-1 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 6.2 pKi = 6.2 Binding
Ability to bind to human Beta-1 adrenergic receptor using membranes of stably transfected CHO cellsAbility to bind to human Beta-1 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
118710947 113247 0 None 1 3 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 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 beta1 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 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
146025803 175593 0 None 1 2 Mouse 8.2 pKi = 8.2 Binding
Displacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T 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 Mouse 8.2 pKi = 8.2 Binding
Displacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T 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
146025801 170054 0 None -1 2 Mouse 8.2 pKi = 8.2 Binding
Displacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T 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 Mouse 8.2 pKi = 8.2 Binding
Displacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T 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
118710935 113233 0 None -9 3 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 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 beta1 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 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 8.2 pKi = 8.2 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 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 8.2 pKi = 8.2 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 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
559929 4816 10 None - 1 Rat 7.2 pKi = 7.2 Binding
Compound was evaluated for the inhibition of binding of [3H]dihydroalprenolol from beta-1 adrenergic receptor of rat cerebral cortical membranesCompound was evaluated for the inhibition of binding of [3H]dihydroalprenolol from beta-1 adrenergic receptor of rat cerebral cortical membranes
ChEMBL 273 5 4 5 1.4 CC(C)(C)NCC(O)COc1ccc(O)c(O)c1F 10.1021/jm00107a027
CHEMBL10453 4816 10 None - 1 Rat 7.2 pKi = 7.2 Binding
Compound was evaluated for the inhibition of binding of [3H]dihydroalprenolol from beta-1 adrenergic receptor of rat cerebral cortical membranesCompound was evaluated for the inhibition of binding of [3H]dihydroalprenolol from beta-1 adrenergic receptor of rat cerebral cortical membranes
ChEMBL 273 5 4 5 1.4 CC(C)(C)NCC(O)COc1ccc(O)c(O)c1F 10.1021/jm00107a027
24936881 17320 0 None -10 3 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta-1 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 -10 3 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta-1 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
9816183 100068 5 None -5 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 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 7.2 pKi = 7.2 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 adrenoceptor
ChEMBL 240 3 4 6 1.0 CNCC(O)c1ccc(O)c2nc(O)sc12 10.1016/j.bmcl.2010.06.136
24936491 17323 0 None -7 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta-1 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 -7 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta-1 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
10140092 94056 0 None -114 3 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]iodocyanopindolol from human cloned adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human cloned adrenergic beta-1 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 -114 3 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]iodocyanopindolol from human cloned adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human cloned adrenergic beta-1 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
13599050 96504 2 None 1 2 Rat 4.2 pKi = 4.2 Binding
Compound was evaluated for beta adrenergic binding affinity towards Beta-1 adrenergic receptor of rat brainCompound was evaluated for beta adrenergic binding affinity towards Beta-1 adrenergic receptor of rat brain
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 Rat 4.2 pKi = 4.2 Binding
Compound was evaluated for beta adrenergic binding affinity towards Beta-1 adrenergic receptor of rat brainCompound was evaluated for beta adrenergic binding affinity towards Beta-1 adrenergic receptor of rat brain
ChEMBL 251 2 3 4 1.8 CC(C)N1CCCC(O)(c2ccc(O)c(O)c2)C1 10.1021/jm00084a006
44423640 141511 0 None -4 3 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]CYP from human adrenergic beta 1 receptor transfected in CHO cells in presence of 100 uM GTPDisplacement of [125I]CYP from human adrenergic beta 1 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 7.2 pKi = 7.2 Binding
Displacement of [125I]CYP from human adrenergic beta 1 receptor transfected in CHO cells in presence of 100 uM GTPDisplacement of [125I]CYP from human adrenergic beta 1 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
16737587 159733 0 None 1 2 Rat 4.2 pKi = 4.2 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 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 Rat 4.2 pKi = 4.2 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 267 8 4 4 2.7 CCCCC[C@@H](C)NC[C@@H](O)c1cc(O)cc(O)c1 nan
44424580 85373 0 None 1 2 Rat 4.2 pKi = 4.2 Binding
Displacement of [3H]CGP-12177 from beta-1 adrenergic receptor in Sprague-Dawley rat cortical membraneDisplacement of [3H]CGP-12177 from beta-1 adrenergic receptor in Sprague-Dawley rat cortical membrane
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 Rat 4.2 pKi = 4.2 Binding
Displacement of [3H]CGP-12177 from beta-1 adrenergic receptor in Sprague-Dawley rat cortical membraneDisplacement of [3H]CGP-12177 from beta-1 adrenergic receptor in Sprague-Dawley rat cortical membrane
ChEMBL 253 7 4 4 2.3 CCCC[C@@H](C)NC[C@@H](O)c1cc(O)cc(O)c1 10.1021/jm070030d
10544781 202969 0 None -10 3 Human 5.2 pKi = 5.2 Binding
Binding Affinity against human Beta-1 adrenergic receptor expressed in Chinese hamster ovary(CHO) cells was measured by using [125I]ICYP radioligandBinding Affinity against human Beta-1 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 5.2 pKi = 5.2 Binding
Binding Affinity against human Beta-1 adrenergic receptor expressed in Chinese hamster ovary(CHO) cells was measured by using [125I]ICYP radioligandBinding Affinity against human Beta-1 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
118710939 113237 0 None -14 3 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 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 7.2 pKi = 7.2 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 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
24936626 17212 0 None -87 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta-1 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 -87 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta-1 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
10316512 16673 2 None 18 2 Guinea pig 6.2 pKi = 6.2 Binding
Binding affinity at Beta-1 adrenergic receptor in guinea pigs by [125I]CYP displacementBinding affinity at Beta-1 adrenergic receptor in guinea pigs by [125I]CYP displacement
ChEMBL 359 1 1 5 1.7 Brc1cnc(N2CCNCC2)c2ncc(Br)n12 10.1021/jm00099a012
CHEMBL124926 16673 2 None 18 2 Guinea pig 6.2 pKi = 6.2 Binding
Binding affinity at Beta-1 adrenergic receptor in guinea pigs by [125I]CYP displacementBinding affinity at Beta-1 adrenergic receptor in guinea pigs by [125I]CYP displacement
ChEMBL 359 1 1 5 1.7 Brc1cnc(N2CCNCC2)c2ncc(Br)n12 10.1021/jm00099a012
11779308 18302 8 None -4 2 Guinea pig 5.2 pKi = 5.2 Binding
Binding affinity at Beta-1 adrenergic receptor in guinea pigs by [125I]CYP displacementBinding affinity at Beta-1 adrenergic receptor in guinea pigs by [125I]CYP displacement
ChEMBL 295 1 0 5 1.2 CN1CCN(c2nccn3c(Br)cnc23)CC1 10.1021/jm00099a012
CHEMBL127318 18302 8 None -4 2 Guinea pig 5.2 pKi = 5.2 Binding
Binding affinity at Beta-1 adrenergic receptor in guinea pigs by [125I]CYP displacementBinding affinity at Beta-1 adrenergic receptor in guinea pigs by [125I]CYP displacement
ChEMBL 295 1 0 5 1.2 CN1CCN(c2nccn3c(Br)cnc23)CC1 10.1021/jm00099a012
541604 164776 10 None -91 4 Guinea pig 4.2 pKi = 4.2 Binding
Binding affinity against beta-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of Dihydro-[3H]-alprenololBinding affinity against beta-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of Dihydro-[3H]-alprenolol
ChEMBL 201 3 4 4 0.5 CNCC(O)c1cc(O)c(O)cc1F 10.1021/jm00118a019
CHEMBL42359 164776 10 None -91 4 Guinea pig 4.2 pKi = 4.2 Binding
Binding affinity against beta-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of Dihydro-[3H]-alprenololBinding affinity against beta-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of Dihydro-[3H]-alprenolol
ChEMBL 201 3 4 4 0.5 CNCC(O)c1cc(O)c(O)cc1F 10.1021/jm00118a019
1862 161 14 None -52 7 Rat 4.2 pKi = 4.2 Binding
Binding of [3H]dihydroalprenolol to beta-1 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-1 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 -52 7 Rat 4.2 pKi = 4.2 Binding
Binding of [3H]dihydroalprenolol to beta-1 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-1 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 -52 7 Rat 4.2 pKi = 4.2 Binding
Binding of [3H]dihydroalprenolol to beta-1 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-1 adrenergic receptor of rat cerebral cortical membranes
ChEMBL 187 2 4 4 0.2 NCC(c1cc(O)c(cc1F)O)O 10.1021/jm990599h
541604 164776 10 None -91 4 Rat 4.2 pKi = 4.2 Binding
Displacement of [3H]dihydroalprenolol from adrenergic beta 1 receptor of rat cerebral cortical membranesDisplacement of [3H]dihydroalprenolol from adrenergic beta 1 receptor of rat cerebral cortical membranes
ChEMBL 201 3 4 4 0.5 CNCC(O)c1cc(O)c(O)cc1F 10.1021/jm00076a024
CHEMBL42359 164776 10 None -91 4 Rat 4.2 pKi = 4.2 Binding
Displacement of [3H]dihydroalprenolol from adrenergic beta 1 receptor of rat cerebral cortical membranesDisplacement of [3H]dihydroalprenolol from adrenergic beta 1 receptor of rat cerebral cortical membranes
ChEMBL 201 3 4 4 0.5 CNCC(O)c1cc(O)c(O)cc1F 10.1021/jm00076a024
90644153 111748 0 None -19 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]dihydroalprenolol from beta1 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta1 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 5.2 pKi = 5.2 Binding
Displacement of [3H]dihydroalprenolol from beta1 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta1 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
173 3199 88 None -69 23 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]dihydroalprenolol from human wild type beta1 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysisDisplacement of [3H]dihydroalprenolol from human wild type beta1 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysis
ChEMBL 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 10.1021/jm400140q
5011 3199 88 None -69 23 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]dihydroalprenolol from human wild type beta1 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysisDisplacement of [3H]dihydroalprenolol from human wild type beta1 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysis
ChEMBL 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 10.1021/jm400140q
CHEMBL18772 3199 88 None -69 23 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]dihydroalprenolol from human wild type beta1 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysisDisplacement of [3H]dihydroalprenolol from human wild type beta1 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysis
ChEMBL 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 10.1021/jm400140q
44312269 202724 0 None 2 3 Human 5.2 pKi = 5.2 Binding
Compound was tested for its binding affinity against Beta-1 adrenergic receptor in CHO cell membrane using [125I]iodocyanopindolol as the radioligand.Compound was tested for its binding affinity against Beta-1 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 5.2 pKi = 5.2 Binding
Compound was tested for its binding affinity against Beta-1 adrenergic receptor in CHO cell membrane using [125I]iodocyanopindolol as the radioligand.Compound was tested for its binding affinity against Beta-1 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
44423641 84959 0 None -12 2 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]CYP from human adrenergic beta 1 receptor transfected in CHO cells in presence of 100 uM GTPDisplacement of [125I]CYP from human adrenergic beta 1 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 5.2 pKi = 5.2 Binding
Displacement of [125I]CYP from human adrenergic beta 1 receptor transfected in CHO cells in presence of 100 uM GTPDisplacement of [125I]CYP from human adrenergic beta 1 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
2812 4696 96 None -38 34 Human 5.2 pKi = 5.2 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
CHEMBL104 4696 96 None -38 34 Human 5.2 pKi = 5.2 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
11432806 65851 0 None -16 3 Human 7.2 pKi = 7.2 Binding
Binding inhibition constant was determined by inhibition of [125I]-iodocyanopindolol binding to Beta-1 adrenergic receptorBinding inhibition constant was determined by inhibition of [125I]-iodocyanopindolol binding to Beta-1 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 -16 3 Human 7.2 pKi = 7.2 Binding
Binding inhibition constant was determined by inhibition of [125I]-iodocyanopindolol binding to Beta-1 adrenergic receptorBinding inhibition constant was determined by inhibition of [125I]-iodocyanopindolol binding to Beta-1 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 -16 3 Human 7.2 pKi = 7.2 Binding
Binding inhibition constant was determined by inhibition of [125I]iodocyanopindolol binding to Beta-1 adrenergic receptorBinding inhibition constant was determined by inhibition of [125I]iodocyanopindolol binding to Beta-1 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 -16 3 Human 7.2 pKi = 7.2 Binding
Binding inhibition constant was determined by inhibition of [125I]iodocyanopindolol binding to Beta-1 adrenergic receptorBinding inhibition constant was determined by inhibition of [125I]iodocyanopindolol binding to Beta-1 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
118710935 113233 0 None -9 3 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 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 7.2 pKi = 7.2 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 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
44423645 84971 0 None -4 3 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]CYP from human adrenergic beta 1 receptor transfected in CHO cells in presence of 100 uM GTPDisplacement of [125I]CYP from human adrenergic beta 1 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 7.2 pKi = 7.2 Binding
Displacement of [125I]CYP from human adrenergic beta 1 receptor transfected in CHO cells in presence of 100 uM GTPDisplacement of [125I]CYP from human adrenergic beta 1 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
145946829 166997 0 None 4 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-CGP12177 from human beta1 ADR expressed in HEK293T cell membranes after 90 mins by scintillation countingDisplacement of [3H]-CGP12177 from human beta1 ADR expressed in HEK293T cell membranes 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 5.2 pKi = 5.2 Binding
Displacement of [3H]-CGP12177 from human beta1 ADR expressed in HEK293T cell membranes after 90 mins by scintillation countingDisplacement of [3H]-CGP12177 from human beta1 ADR expressed in HEK293T cell membranes 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 5.2 pKi = 5.2 Binding
Displacement of [3H]-CGP12177 from human beta1 ADR expressed in HEK293T cell membranes after 90 mins by scintillation countingDisplacement of [3H]-CGP12177 from human beta1 ADR expressed in HEK293T cell membranes 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
49864439 15456 0 None -4 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 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 6.2 pKi = 6.2 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 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
594590 72490 89 None 39 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]dihydroalprenolol from human wild type beta1 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysisDisplacement of [3H]dihydroalprenolol from human wild type beta1 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysis
ChEMBL 201 1 2 2 1.6 c1cc(N2CCNCC2)c2cc[nH]c2c1 10.1021/jm400140q
CHEMBL200234 72490 89 None 39 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]dihydroalprenolol from human wild type beta1 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysisDisplacement of [3H]dihydroalprenolol from human wild type beta1 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysis
ChEMBL 201 1 2 2 1.6 c1cc(N2CCNCC2)c2cc[nH]c2c1 10.1021/jm400140q
1499 2052 43 None -33 17 Rat 6.2 pKi = 6.2 Binding
Compound was evaluated for the inhibition of binding of [3H]dihydroalprenolol from beta-1 adrenergic receptor of rat cerebral cortical membranesCompound was evaluated for the inhibition of binding of [3H]dihydroalprenolol from beta-1 adrenergic receptor of rat cerebral cortical membranes
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm00107a027
3779 2052 43 None -33 17 Rat 6.2 pKi = 6.2 Binding
Compound was evaluated for the inhibition of binding of [3H]dihydroalprenolol from beta-1 adrenergic receptor of rat cerebral cortical membranesCompound was evaluated for the inhibition of binding of [3H]dihydroalprenolol from beta-1 adrenergic receptor of rat cerebral cortical membranes
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm00107a027
536 2052 43 None -33 17 Rat 6.2 pKi = 6.2 Binding
Compound was evaluated for the inhibition of binding of [3H]dihydroalprenolol from beta-1 adrenergic receptor of rat cerebral cortical membranesCompound was evaluated for the inhibition of binding of [3H]dihydroalprenolol from beta-1 adrenergic receptor of rat cerebral cortical membranes
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm00107a027
CHEMBL434 2052 43 None -33 17 Rat 6.2 pKi = 6.2 Binding
Compound was evaluated for the inhibition of binding of [3H]dihydroalprenolol from beta-1 adrenergic receptor of rat cerebral cortical membranesCompound was evaluated for the inhibition of binding of [3H]dihydroalprenolol from beta-1 adrenergic receptor of rat cerebral cortical membranes
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm00107a027
DB01064 2052 43 None -33 17 Rat 6.2 pKi = 6.2 Binding
Compound was evaluated for the inhibition of binding of [3H]dihydroalprenolol from beta-1 adrenergic receptor of rat cerebral cortical membranesCompound was evaluated for the inhibition of binding of [3H]dihydroalprenolol from beta-1 adrenergic receptor of rat cerebral cortical membranes
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm00107a027
44361634 34412 0 None - 1 Rat 5.2 pKi = 5.2 Binding
Compound was evaluated for its Beta-1 adrenergic receptor binding affinity by measuring the displacement of [3H]dihydroalprenolol binding in rat heartCompound was evaluated for its Beta-1 adrenergic receptor binding affinity by measuring the displacement of [3H]dihydroalprenolol binding in rat heart
ChEMBL 417 6 2 6 2.4 O=C1CSc2c(cccc2OCC(O)CN2CCN(c3ccc(F)cc3)CC2)N1 10.1016/s0960-894x(00)00016-0
CHEMBL142995 34412 0 None - 1 Rat 5.2 pKi = 5.2 Binding
Compound was evaluated for its Beta-1 adrenergic receptor binding affinity by measuring the displacement of [3H]dihydroalprenolol binding in rat heartCompound was evaluated for its Beta-1 adrenergic receptor binding affinity by measuring the displacement of [3H]dihydroalprenolol binding in rat heart
ChEMBL 417 6 2 6 2.4 O=C1CSc2c(cccc2OCC(O)CN2CCN(c3ccc(F)cc3)CC2)N1 10.1016/s0960-894x(00)00016-0
24936625 17287 0 None -1 2 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cells
ChEMBL 520 9 4 9 3.8 O=C(O)c1cc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)ccc1O 10.1016/j.bmcl.2010.08.039
CHEMBL1257798 17287 0 None -1 2 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cells
ChEMBL 520 9 4 9 3.8 O=C(O)c1cc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)ccc1O 10.1016/j.bmcl.2010.08.039
3207225 87098 7 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]dihydroalprenolol from human wild type beta1 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysisDisplacement of [3H]dihydroalprenolol from human wild type beta1 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysis
ChEMBL 302 1 1 5 2.5 Cc1nc(N2CCNCC2)c2c3c(sc2n1)CC(C)CC3 10.1021/jm400140q
CHEMBL2335167 87098 7 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]dihydroalprenolol from human wild type beta1 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysisDisplacement of [3H]dihydroalprenolol from human wild type beta1 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysis
ChEMBL 302 1 1 5 2.5 Cc1nc(N2CCNCC2)c2c3c(sc2n1)CC(C)CC3 10.1021/jm400140q
594590 72490 89 None 39 2 Human 7.2 pKi = 7.2 Binding
Binding affinity to beta1 adrenergic receptor (unknown origin)Binding affinity to beta1 adrenergic receptor (unknown origin)
ChEMBL 201 1 2 2 1.6 c1cc(N2CCNCC2)c2cc[nH]c2c1 10.1021/jm400561w
CHEMBL200234 72490 89 None 39 2 Human 7.2 pKi = 7.2 Binding
Binding affinity to beta1 adrenergic receptor (unknown origin)Binding affinity to beta1 adrenergic receptor (unknown origin)
ChEMBL 201 1 2 2 1.6 c1cc(N2CCNCC2)c2cc[nH]c2c1 10.1021/jm400561w
12582 935 40 None -3 5 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
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 -3 5 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
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 -3 5 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
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 -3 5 Human 7.2 pKi = 7.2 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 276 3 3 3 3.0 CC(C)(C)NCC(C1=CC(=C(C(=C1)Cl)N)Cl)O nan
10231679 93866 0 None -36 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]iodocyanopindolol from human cloned adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human cloned adrenergic beta-1 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 -36 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]iodocyanopindolol from human cloned adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human cloned adrenergic beta-1 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
46889670 6919 0 None -2 3 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta-1 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta-1 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 8.2 pKi = 8.2 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta-1 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta-1 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
165193 3126 60 None -18 43 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]CGP-12177 from beta1 adrenergic receptor in rat brain cerebral cortex after 60 mins by microbeta scintillation counting methodDisplacement of [3H]CGP-12177 from beta1 adrenergic receptor in rat brain cerebral cortex after 60 mins by microbeta scintillation counting method
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmcl.2016.09.037
2303 3126 60 None -18 43 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]CGP-12177 from beta1 adrenergic receptor in rat brain cerebral cortex after 60 mins by microbeta scintillation counting methodDisplacement of [3H]CGP-12177 from beta1 adrenergic receptor in rat brain cerebral cortex after 60 mins by microbeta scintillation counting method
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmcl.2016.09.037
4946 3126 60 None -18 43 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]CGP-12177 from beta1 adrenergic receptor in rat brain cerebral cortex after 60 mins by microbeta scintillation counting methodDisplacement of [3H]CGP-12177 from beta1 adrenergic receptor in rat brain cerebral cortex after 60 mins by microbeta scintillation counting method
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmcl.2016.09.037
564 3126 60 None -18 43 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]CGP-12177 from beta1 adrenergic receptor in rat brain cerebral cortex after 60 mins by microbeta scintillation counting methodDisplacement of [3H]CGP-12177 from beta1 adrenergic receptor in rat brain cerebral cortex after 60 mins by microbeta scintillation counting method
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmcl.2016.09.037
62882 3126 60 None -18 43 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]CGP-12177 from beta1 adrenergic receptor in rat brain cerebral cortex after 60 mins by microbeta scintillation counting methodDisplacement of [3H]CGP-12177 from beta1 adrenergic receptor in rat brain cerebral cortex after 60 mins by microbeta scintillation counting method
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmcl.2016.09.037
63 3126 60 None -18 43 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]CGP-12177 from beta1 adrenergic receptor in rat brain cerebral cortex after 60 mins by microbeta scintillation counting methodDisplacement of [3H]CGP-12177 from beta1 adrenergic receptor in rat brain cerebral cortex after 60 mins by microbeta scintillation counting method
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmcl.2016.09.037
66366 3126 60 None -18 43 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]CGP-12177 from beta1 adrenergic receptor in rat brain cerebral cortex after 60 mins by microbeta scintillation counting methodDisplacement of [3H]CGP-12177 from beta1 adrenergic receptor in rat brain cerebral cortex after 60 mins by microbeta scintillation counting method
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmcl.2016.09.037
91536 3126 60 None -18 43 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]CGP-12177 from beta1 adrenergic receptor in rat brain cerebral cortex after 60 mins by microbeta scintillation counting methodDisplacement of [3H]CGP-12177 from beta1 adrenergic receptor in rat brain cerebral cortex after 60 mins by microbeta scintillation counting method
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmcl.2016.09.037
CHEMBL27 3126 60 None -18 43 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]CGP-12177 from beta1 adrenergic receptor in rat brain cerebral cortex after 60 mins by microbeta scintillation counting methodDisplacement of [3H]CGP-12177 from beta1 adrenergic receptor in rat brain cerebral cortex after 60 mins by microbeta scintillation counting method
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmcl.2016.09.037
CHEMBL452861 3126 60 None -18 43 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]CGP-12177 from beta1 adrenergic receptor in rat brain cerebral cortex after 60 mins by microbeta scintillation counting methodDisplacement of [3H]CGP-12177 from beta1 adrenergic receptor in rat brain cerebral cortex after 60 mins by microbeta scintillation counting method
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmcl.2016.09.037
DB00571 3126 60 None -18 43 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]CGP-12177 from beta1 adrenergic receptor in rat brain cerebral cortex after 60 mins by microbeta scintillation counting methodDisplacement of [3H]CGP-12177 from beta1 adrenergic receptor in rat brain cerebral cortex after 60 mins by microbeta scintillation counting method
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmcl.2016.09.037
15077948 141097 0 None - 1 Human 8.1 pKi = 8.1 Binding
Inhibition of [3H]dihydroalprenolol binding to beta 1 adrenoceptor from turkey erythrocyte membranes.Inhibition of [3H]dihydroalprenolol binding to beta 1 adrenoceptor from turkey erythrocyte membranes.
ChEMBL 514 10 5 8 0.8 NS(=O)(=O)c1cc(C(=O)NCCNCC(O)COc2cccc3c2SCC(=O)N3)ccc1Cl 10.1021/jm00053a020
CHEMBL38532 141097 0 None - 1 Human 8.1 pKi = 8.1 Binding
Inhibition of [3H]dihydroalprenolol binding to beta 1 adrenoceptor from turkey erythrocyte membranes.Inhibition of [3H]dihydroalprenolol binding to beta 1 adrenoceptor from turkey erythrocyte membranes.
ChEMBL 514 10 5 8 0.8 NS(=O)(=O)c1cc(C(=O)NCCNCC(O)COc2cccc3c2SCC(=O)N3)ccc1Cl 10.1021/jm00053a020
9982903 168487 0 None - 1 Human 8.1 pKi = 8.1 Binding
Inhibition of [3H]dihydroalprenolol binding to beta 1 adrenoceptor from turkey erythrocyte membranes.Inhibition of [3H]dihydroalprenolol binding to beta 1 adrenoceptor from turkey erythrocyte membranes.
ChEMBL 486 10 5 8 1.5 NS(=O)(=O)c1cc(NCCNCC(O)COc2cccc3c2SCC(=O)N3)ccc1Cl 10.1021/jm00053a020
CHEMBL43968 168487 0 None - 1 Human 8.1 pKi = 8.1 Binding
Inhibition of [3H]dihydroalprenolol binding to beta 1 adrenoceptor from turkey erythrocyte membranes.Inhibition of [3H]dihydroalprenolol binding to beta 1 adrenoceptor from turkey erythrocyte membranes.
ChEMBL 486 10 5 8 1.5 NS(=O)(=O)c1cc(NCCNCC(O)COc2cccc3c2SCC(=O)N3)ccc1Cl 10.1021/jm00053a020
118710948 113248 0 None -5 3 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 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 8.1 pKi = 8.1 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 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
44433250 88634 0 None -1 3 Human 8.1 pKi = 8.1 Binding
Binding affinity at human adrenergic beta-1 receptorBinding affinity at human adrenergic beta-1 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 8.1 pKi = 8.1 Binding
Binding affinity at human adrenergic beta-1 receptorBinding affinity at human adrenergic beta-1 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
11647002 15447 0 None -22 3 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 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 7.2 pKi = 7.2 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 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
52943932 17559 0 None -16 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta-1 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 -16 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta-1 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
155564274 174839 0 None 19 2 Mouse 7.2 pKi = 7.2 Binding
Displacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T 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 Mouse 7.2 pKi = 7.2 Binding
Displacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T 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
52947562 17490 0 None 1 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta-1 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 1 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cells
ChEMBL 384 7 2 7 2.7 OC(CNC1CCN(c2ncnc3sccc23)CC1)COc1ccccc1 10.1016/j.bmcl.2010.08.039
46889730 7035 0 None -42 3 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta-1 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta-1 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 6.1 pKi = 6.1 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta-1 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta-1 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
9958539 102618 0 None -1 3 Human 6.1 pKi = 6.1 Binding
Binding Affinity against human Beta-1 adrenergic receptor expressed in Chinese hamster ovary(CHO) cells was measured by using [125I]ICYP radioligandBinding Affinity against human Beta-1 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 6.1 pKi = 6.1 Binding
Binding Affinity against human Beta-1 adrenergic receptor expressed in Chinese hamster ovary(CHO) cells was measured by using [125I]ICYP radioligandBinding Affinity against human Beta-1 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
4189 205185 91 None -38 34 Human 5.1 pKi = 5.1 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL1559 205185 91 None -38 34 Human 5.1 pKi = 5.1 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL91 205185 91 None -38 34 Human 5.1 pKi = 5.1 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
44444187 94018 0 None -23 3 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]iodocyanopindolol from human cloned adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human cloned adrenergic beta-1 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 -23 3 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]iodocyanopindolol from human cloned adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human cloned adrenergic beta-1 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
5187268 6484 11 None -10 3 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta-1 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta-1 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 6.1 pKi = 6.1 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta-1 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta-1 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
155524756 170427 0 None 1 2 Mouse 6.1 pKi = 6.1 Binding
Displacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T 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 Mouse 6.1 pKi = 6.1 Binding
Displacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T 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
155540000 172302 0 None 1 2 Mouse 5.1 pKi = 5.1 Binding
Displacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T 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 Mouse 5.1 pKi = 5.1 Binding
Displacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T 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
3198 203792 73 None -38 34 Human 5.1 pKi = 5.1 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL1201049 203792 73 None -38 34 Human 5.1 pKi = 5.1 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL808 203792 73 None -38 34 Human 5.1 pKi = 5.1 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
2723782 87091 79 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]dihydroalprenolol from human wild type beta1 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysisDisplacement of [3H]dihydroalprenolol from human wild type beta1 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysis
ChEMBL 190 1 1 2 1.7 Cc1ccc(N2CCNCC2)cc1C 10.1021/jm400140q
CHEMBL2335160 87091 79 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]dihydroalprenolol from human wild type beta1 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysisDisplacement of [3H]dihydroalprenolol from human wild type beta1 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysis
ChEMBL 190 1 1 2 1.7 Cc1ccc(N2CCNCC2)cc1C 10.1021/jm400140q
13720716 62709 0 None -1 2 Guinea pig 7.1 pKi = 7.1 Binding
Binding affinity against Beta-1 adrenergic receptor in guinea pig left ventricleBinding affinity against Beta-1 adrenergic receptor in guinea pig left ventricle
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 7.1 pKi = 7.1 Binding
Binding affinity against Beta-1 adrenergic receptor in guinea pig left ventricleBinding affinity against Beta-1 adrenergic receptor in guinea pig left ventricle
ChEMBL 363 5 3 6 2.7 COc1cc(C[C@@H]2NCCc3cc(O)c(O)c(F)c32)cc(OC)c1OC 10.1021/jm00081a007
2249 509 106 None -5 12 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C nan
255 509 106 None -5 12 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C nan
548 509 106 None -5 12 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C nan
CHEMBL24 509 106 None -5 12 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C nan
DB00335 509 106 None -5 12 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C nan
10472143 118759 0 None -169 17 Human 7.1 pKi = 7.1 Binding
Binding affinity towards Beta-1 adrenergic receptorBinding affinity towards Beta-1 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 -169 17 Human 7.1 pKi = 7.1 Binding
Binding affinity towards Beta-1 adrenergic receptorBinding affinity towards Beta-1 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
46889809 6554 0 None -1 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta-1 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta-1 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 7.1 pKi = 7.1 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta-1 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta-1 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
10375227 11098 0 None 2 2 Rat 6.1 pKi = 6.1 Binding
Binding affinity against beta-1-adrenergic receptor in rat brainBinding affinity against beta-1-adrenergic receptor in rat brain
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 Rat 6.1 pKi = 6.1 Binding
Binding affinity against beta-1-adrenergic receptor in rat brainBinding affinity against beta-1-adrenergic receptor in rat brain
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 Rat 6.1 pKi = 6.1 Binding
Binding affinity against beta-1-adrenergic receptor in rat brainBinding affinity against beta-1-adrenergic receptor in rat brain
ChEMBL 188 5 2 4 0.8 C/C=N/OCC(O)CNC(C)(C)C 10.1021/jm00036a018
12353629 202216 0 None -23 3 Rat 6.1 pKi = 6.1 Binding
Compound was evaluated for beta adrenergic binding affinity towards Beta-1 adrenergic receptor of rat brainCompound was evaluated for beta adrenergic binding affinity towards Beta-1 adrenergic receptor of rat brain
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 -23 3 Rat 6.1 pKi = 6.1 Binding
Compound was evaluated for beta adrenergic binding affinity towards Beta-1 adrenergic receptor of rat brainCompound was evaluated for beta adrenergic binding affinity towards Beta-1 adrenergic receptor of rat brain
ChEMBL 237 2 4 4 1.4 CC(C)N[C@@H]1CCc2c(ccc(O)c2O)[C@H]1O 10.1021/jm00084a006
9908924 141111 0 None -9 3 Human 5.1 pKi = 5.1 Binding
Ability to bind to human Beta-1 adrenergic receptor using membranes of stably transfected CHO cellsAbility to bind to human Beta-1 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 -9 3 Human 5.1 pKi = 5.1 Binding
Ability to bind to human Beta-1 adrenergic receptor using membranes of stably transfected CHO cellsAbility to bind to human Beta-1 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
75201901 165861 14 None -562 24 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]-pindolol from recombinant human beta1 adrenergic receptor expressed in CHO Flp-In cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-pindolol from recombinant human beta1 adrenergic receptor expressed in CHO 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 -562 24 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]-pindolol from recombinant human beta1 adrenergic receptor expressed in CHO Flp-In cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-pindolol from recombinant human beta1 adrenergic receptor expressed in CHO 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
118710943 113241 0 None -5 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 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 7.1 pKi = 7.1 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 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
63180 76425 10 None - 1 Rat 7.1 pKi = 7.1 Binding
Displacement of [3H]-CGP12177 from beta1-adrenergic receptor in rat heart membranesDisplacement of [3H]-CGP12177 from beta1-adrenergic receptor in rat heart membranes
ChEMBL 411 7 2 7 2.7 COc1ccc2nc(-c3ccc(OCC(O)CNC(C)(C)C)cc3)n(C)c(=O)c2c1 10.1016/j.bmcl.2011.06.106
CHEMBL1824263 76425 10 None - 1 Rat 7.1 pKi = 7.1 Binding
Displacement of [3H]-CGP12177 from beta1-adrenergic receptor in rat heart membranesDisplacement of [3H]-CGP12177 from beta1-adrenergic receptor in rat heart membranes
ChEMBL 411 7 2 7 2.7 COc1ccc2nc(-c3ccc(OCC(O)CNC(C)(C)C)cc3)n(C)c(=O)c2c1 10.1016/j.bmcl.2011.06.106
CHEMBL2068824 76425 10 None - 1 Rat 7.1 pKi = 7.1 Binding
Displacement of [3H]-CGP12177 from beta1-adrenergic receptor in rat heart membranesDisplacement of [3H]-CGP12177 from beta1-adrenergic receptor in rat heart membranes
ChEMBL 411 7 2 7 2.7 COc1ccc2nc(-c3ccc(OCC(O)CNC(C)(C)C)cc3)n(C)c(=O)c2c1 10.1016/j.bmcl.2011.06.106
44571260 12611 0 None - 1 Rat 5.1 pKi = 5.1 Binding
Displacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation countingDisplacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation counting
ChEMBL 309 7 1 4 3.5 C=CCNCCCOc1cccc2c(=O)c3ccccc3oc12 10.1016/j.bmc.2008.12.031
CHEMBL1187740 12611 0 None - 1 Rat 5.1 pKi = 5.1 Binding
Displacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation countingDisplacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation counting
ChEMBL 309 7 1 4 3.5 C=CCNCCCOc1cccc2c(=O)c3ccccc3oc12 10.1016/j.bmc.2008.12.031
CHEMBL517532 12611 0 None - 1 Rat 5.1 pKi = 5.1 Binding
Displacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation countingDisplacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation counting
ChEMBL 309 7 1 4 3.5 C=CCNCCCOc1cccc2c(=O)c3ccccc3oc12 10.1016/j.bmc.2008.12.031
16735494 141508 0 None -3 2 Rat 4.1 pKi = 4.1 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
CHEMBL387825 141508 0 None -3 2 Rat 4.1 pKi = 4.1 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
16735494 141508 0 None -3 2 Rat 4.1 pKi = 4.1 Binding
Displacement of [3H]CGP-12177 from beta-1 adrenergic receptor in Sprague-Dawley rat cortical membraneDisplacement of [3H]CGP-12177 from beta-1 adrenergic receptor in Sprague-Dawley rat cortical membrane
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 Rat 4.1 pKi = 4.1 Binding
Displacement of [3H]CGP-12177 from beta-1 adrenergic receptor in Sprague-Dawley rat cortical membraneDisplacement of [3H]CGP-12177 from beta-1 adrenergic receptor in Sprague-Dawley rat cortical membrane
ChEMBL 287 6 4 4 2.4 C[C@H](Cc1ccccc1)NC[C@@H](O)c1cc(O)cc(O)c1 10.1021/jm070030d
11776640 13420 0 None -16 3 Guinea pig 5.1 pKi = 5.1 Binding
Binding affinity at Beta-1 adrenergic receptor in guinea pigs by [125I]CYP displacementBinding affinity at Beta-1 adrenergic receptor in guinea pigs by [125I]CYP displacement
ChEMBL 245 3 1 5 1.1 CCCc1cnc2c(N3CCNCC3)nccn12 10.1021/jm00099a012
CHEMBL1193824 13420 0 None -16 3 Guinea pig 5.1 pKi = 5.1 Binding
Binding affinity at Beta-1 adrenergic receptor in guinea pigs by [125I]CYP displacementBinding affinity at Beta-1 adrenergic receptor in guinea pigs by [125I]CYP displacement
ChEMBL 245 3 1 5 1.1 CCCc1cnc2c(N3CCNCC3)nccn12 10.1021/jm00099a012
CHEMBL545293 13420 0 None -16 3 Guinea pig 5.1 pKi = 5.1 Binding
Binding affinity at Beta-1 adrenergic receptor in guinea pigs by [125I]CYP displacementBinding affinity at Beta-1 adrenergic receptor in guinea pigs by [125I]CYP displacement
ChEMBL 245 3 1 5 1.1 CCCc1cnc2c(N3CCNCC3)nccn12 10.1021/jm00099a012
49864394 15445 0 None -6 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 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 7.1 pKi = 7.1 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 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
2419 3394 80 None -162 6 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 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 -162 6 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 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 -162 6 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 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 -162 6 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 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 -162 6 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 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
127047859 139508 0 None -28 6 Mouse 7.1 pKi = 7.1 Binding
Displacement of [3H]CGP12177 from mouse beta1 receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from mouse beta1 receptor expressed in HEK293 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 -28 6 Mouse 7.1 pKi = 7.1 Binding
Displacement of [3H]CGP12177 from mouse beta1 receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from mouse beta1 receptor expressed in HEK293 cells
ChEMBL 476 12 3 6 4.1 COc1cc(CCNCCc2ccc(O)c3c2OCC(=O)N3)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
9871887 102712 0 None -6 4 Human 7.1 pKi = 7.1 Binding
Binding Affinity against human Beta-1 adrenergic receptor expressed in Chinese hamster ovary(CHO) cells was measured by using [125I]ICYP radioligandBinding Affinity against human Beta-1 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 7.1 pKi = 7.1 Binding
Binding Affinity against human Beta-1 adrenergic receptor expressed in Chinese hamster ovary(CHO) cells was measured by using [125I]ICYP radioligandBinding Affinity against human Beta-1 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 7.1 pKi = 7.1 Binding
Binding affinity for human Beta-1 adrenergic receptor expressed in CHO cells by radioligand competition binding assays using [125I]iodocyanopindolol (ICYP).) PR = potency ratio relative to TMQBinding affinity for human Beta-1 adrenergic receptor expressed in CHO cells by radioligand competition binding assays using [125I]iodocyanopindolol (ICYP).) PR = potency ratio relative to TMQ
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 7.1 pKi = 7.1 Binding
Binding affinity for human Beta-1 adrenergic receptor expressed in CHO cells by radioligand competition binding assays using [125I]iodocyanopindolol (ICYP).) PR = potency ratio relative to TMQBinding affinity for human Beta-1 adrenergic receptor expressed in CHO cells by radioligand competition binding assays using [125I]iodocyanopindolol (ICYP).) PR = potency ratio relative to TMQ
ChEMBL 537 3 3 4 3.7 COc1c(I)cc(CC2NCCc3cc(O)c(O)cc32)cc1I 10.1021/jm960208o
9934284 89851 0 None -1995 10 Human 6.1 pKi = 6.1 Binding
Binding affinity at adrenergic beta 1 receptorBinding affinity at adrenergic beta 1 receptor
ChEMBL 467 6 1 5 4.5 Cc1ccc2c(OCCN3CCC(Cc4cc5c(cc4F)OCC(=O)N5)CC3)cc(F)cc2n1 10.1016/j.bmcl.2006.11.031
CHEMBL238520 89851 0 None -1995 10 Human 6.1 pKi = 6.1 Binding
Binding affinity at adrenergic beta 1 receptorBinding affinity at adrenergic beta 1 receptor
ChEMBL 467 6 1 5 4.5 Cc1ccc2c(OCCN3CCC(Cc4cc5c(cc4F)OCC(=O)N5)CC3)cc(F)cc2n1 10.1016/j.bmcl.2006.11.031
90644139 111759 0 None -100 2 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]dihydroalprenolol from beta1 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta1 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 5.1 pKi = 5.1 Binding
Displacement of [3H]dihydroalprenolol from beta1 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta1 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
90644141 111762 0 None -6 2 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]dihydroalprenolol from beta1 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta1 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 5.1 pKi = 5.1 Binding
Displacement of [3H]dihydroalprenolol from beta1 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta1 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
145946259 166952 0 None - 1 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]-CGP12177 from human beta1 ADR expressed in HEK293T cell membranes after 90 mins by scintillation countingDisplacement of [3H]-CGP12177 from human beta1 ADR expressed in HEK293T cell membranes after 90 mins by scintillation counting
ChEMBL 350 9 3 5 1.1 CNCC(O)COc1ccc(S(=O)(=O)NCc2ccccc2)cc1 10.1021/acs.jmedchem.8b00625
CHEMBL4170536 166952 0 None - 1 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]-CGP12177 from human beta1 ADR expressed in HEK293T cell membranes after 90 mins by scintillation countingDisplacement of [3H]-CGP12177 from human beta1 ADR expressed in HEK293T cell membranes after 90 mins by scintillation counting
ChEMBL 350 9 3 5 1.1 CNCC(O)COc1ccc(S(=O)(=O)NCc2ccccc2)cc1 10.1021/acs.jmedchem.8b00625
CHEMBL4300084 166952 0 None - 1 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]-CGP12177 from human beta1 ADR expressed in HEK293T cell membranes after 90 mins by scintillation countingDisplacement of [3H]-CGP12177 from human beta1 ADR expressed in HEK293T cell membranes after 90 mins by scintillation counting
ChEMBL 350 9 3 5 1.1 CNCC(O)COc1ccc(S(=O)(=O)NCc2ccccc2)cc1 10.1021/acs.jmedchem.8b00625
90644146 111740 0 None -5 2 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]dihydroalprenolol from beta1 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta1 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 4.1 pKi = 4.1 Binding
Displacement of [3H]dihydroalprenolol from beta1 receptor (unknown origin) by liquid scintillation counting and cell based assayDisplacement of [3H]dihydroalprenolol from beta1 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
49864442 15459 0 None -27 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 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 8.1 pKi = 8.1 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 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
1499 2052 43 None -33 17 Rat 7.1 pKi = 7.1 Binding
Compound was evaluated for beta adrenergic binding affinity towards Beta-1 adrenergic receptor of rat brainCompound was evaluated for beta adrenergic binding affinity towards Beta-1 adrenergic receptor of rat brain
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm00084a006
3779 2052 43 None -33 17 Rat 7.1 pKi = 7.1 Binding
Compound was evaluated for beta adrenergic binding affinity towards Beta-1 adrenergic receptor of rat brainCompound was evaluated for beta adrenergic binding affinity towards Beta-1 adrenergic receptor of rat brain
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm00084a006
536 2052 43 None -33 17 Rat 7.1 pKi = 7.1 Binding
Compound was evaluated for beta adrenergic binding affinity towards Beta-1 adrenergic receptor of rat brainCompound was evaluated for beta adrenergic binding affinity towards Beta-1 adrenergic receptor of rat brain
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm00084a006
CHEMBL434 2052 43 None -33 17 Rat 7.1 pKi = 7.1 Binding
Compound was evaluated for beta adrenergic binding affinity towards Beta-1 adrenergic receptor of rat brainCompound was evaluated for beta adrenergic binding affinity towards Beta-1 adrenergic receptor of rat brain
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm00084a006
DB01064 2052 43 None -33 17 Rat 7.1 pKi = 7.1 Binding
Compound was evaluated for beta adrenergic binding affinity towards Beta-1 adrenergic receptor of rat brainCompound was evaluated for beta adrenergic binding affinity towards Beta-1 adrenergic receptor of rat brain
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm00084a006
4421983 7183 5 None 1 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta-1 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta-1 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 beta-1 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta-1 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
1499 2052 43 None -33 17 Rat 7.1 pKi = 7.1 Binding
Tested for binding affinity against beta-1 adrenergic receptor in rat brain using [3H]-CGP- 26505 as radioligandTested for binding affinity against beta-1 adrenergic receptor in rat brain using [3H]-CGP- 26505 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 -33 17 Rat 7.1 pKi = 7.1 Binding
Tested for binding affinity against beta-1 adrenergic receptor in rat brain using [3H]-CGP- 26505 as radioligandTested for binding affinity against beta-1 adrenergic receptor in rat brain using [3H]-CGP- 26505 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 -33 17 Rat 7.1 pKi = 7.1 Binding
Tested for binding affinity against beta-1 adrenergic receptor in rat brain using [3H]-CGP- 26505 as radioligandTested for binding affinity against beta-1 adrenergic receptor in rat brain using [3H]-CGP- 26505 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 -33 17 Rat 7.1 pKi = 7.1 Binding
Tested for binding affinity against beta-1 adrenergic receptor in rat brain using [3H]-CGP- 26505 as radioligandTested for binding affinity against beta-1 adrenergic receptor in rat brain using [3H]-CGP- 26505 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 -33 17 Rat 7.1 pKi = 7.1 Binding
Tested for binding affinity against beta-1 adrenergic receptor in rat brain using [3H]-CGP- 26505 as radioligandTested for binding affinity against beta-1 adrenergic receptor in rat brain using [3H]-CGP- 26505 as radioligand
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm00073a006
129896798 182075 32 None 1 3 Human 6.1 pKi = 6.1 Binding
Binding affinity to beta1 adrenoceptor (unknown origin)Binding affinity to beta1 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 6.1 pKi = 6.1 Binding
Binding affinity to beta1 adrenoceptor (unknown origin)Binding affinity to beta1 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
12353620 202631 1 None -66 2 Rat 5.1 pKi = 5.1 Binding
Compound was evaluated for beta adrenergic binding affinity towards Beta-1 adrenergic receptor of rat brainCompound was evaluated for beta adrenergic binding affinity towards Beta-1 adrenergic receptor of rat brain
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 Rat 5.1 pKi = 5.1 Binding
Compound was evaluated for beta adrenergic binding affinity towards Beta-1 adrenergic receptor of rat brainCompound was evaluated for beta adrenergic binding affinity towards Beta-1 adrenergic receptor of rat brain
ChEMBL 195 0 4 4 0.4 N[C@@H]1CCc2c(ccc(O)c2O)[C@H]1O 10.1021/jm00084a006
2419 3394 80 None -162 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 adrenoceptor
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2010.06.136
5152 3394 80 None -162 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 adrenoceptor
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2010.06.136
559 3394 80 None -162 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 adrenoceptor
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2010.06.136
CHEMBL1263 3394 80 None -162 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 adrenoceptor
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2010.06.136
DB00938 3394 80 None -162 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 adrenoceptor
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2010.06.136
44351377 117289 1 None - 1 Rat 4.1 pKi = 4.1 Binding
Displacement of [3H]dihydroalprenolol from adrenergic beta 1 receptor of rat cerebral cortical membranesDisplacement of [3H]dihydroalprenolol from adrenergic beta 1 receptor of rat cerebral cortical membranes
ChEMBL 203 3 3 3 0.9 CNCC(O)c1c(F)ccc(O)c1F 10.1021/jm00076a024
CHEMBL340189 117289 1 None - 1 Rat 4.1 pKi = 4.1 Binding
Displacement of [3H]dihydroalprenolol from adrenergic beta 1 receptor of rat cerebral cortical membranesDisplacement of [3H]dihydroalprenolol from adrenergic beta 1 receptor of rat cerebral cortical membranes
ChEMBL 203 3 3 3 0.9 CNCC(O)c1c(F)ccc(O)c1F 10.1021/jm00076a024
15077956 168651 0 None - 1 Human 6.1 pKi = 6.1 Binding
Inhibition of [3H]dihydroalprenolol binding to beta 1 adrenoceptor from turkey erythrocyte membranes.Inhibition of [3H]dihydroalprenolol binding to beta 1 adrenoceptor from turkey erythrocyte membranes.
ChEMBL 477 10 4 6 1.9 NS(=O)(=O)c1cc(C(=O)NCCNCC(O)COc2cccc3ccccc23)ccc1Cl 10.1021/jm00053a020
CHEMBL44097 168651 0 None - 1 Human 6.1 pKi = 6.1 Binding
Inhibition of [3H]dihydroalprenolol binding to beta 1 adrenoceptor from turkey erythrocyte membranes.Inhibition of [3H]dihydroalprenolol binding to beta 1 adrenoceptor from turkey erythrocyte membranes.
ChEMBL 477 10 4 6 1.9 NS(=O)(=O)c1cc(C(=O)NCCNCC(O)COc2cccc3ccccc23)ccc1Cl 10.1021/jm00053a020
2464 3570 52 None -2 6 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C nan
5253 3570 52 None -2 6 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C nan
7297 3570 52 None -2 6 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C nan
CHEMBL471 3570 52 None -2 6 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C nan
DB00489 3570 52 None -2 6 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C nan
9928332 96719 4 None -416 10 Rat 6.1 pKi = 6.1 Binding
Compound was evaluated for its binding affinity to beta-1 receptor in rat brain using [3H]- DHA radioligand assayCompound was evaluated for its binding affinity to beta-1 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 -416 10 Rat 6.1 pKi = 6.1 Binding
Compound was evaluated for its binding affinity to beta-1 receptor in rat brain using [3H]- DHA radioligand assayCompound was evaluated for its binding affinity to beta-1 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
44570783 12474 0 None - 1 Rat 7.1 pKi = 7.1 Binding
Displacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation countingDisplacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation counting
ChEMBL 325 7 2 5 2.5 C=CCNCC(O)COc1cccc2c(=O)c3ccccc3oc12 10.1016/j.bmc.2008.12.031
CHEMBL1186914 12474 0 None - 1 Rat 7.1 pKi = 7.1 Binding
Displacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation countingDisplacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation counting
ChEMBL 325 7 2 5 2.5 C=CCNCC(O)COc1cccc2c(=O)c3ccccc3oc12 10.1016/j.bmc.2008.12.031
CHEMBL482396 12474 0 None - 1 Rat 7.1 pKi = 7.1 Binding
Displacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation countingDisplacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation counting
ChEMBL 325 7 2 5 2.5 C=CCNCC(O)COc1cccc2c(=O)c3ccccc3oc12 10.1016/j.bmc.2008.12.031
127046950 139502 0 None -4 6 Mouse 7.1 pKi = 7.1 Binding
Displacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T 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 -4 6 Mouse 7.1 pKi = 7.1 Binding
Displacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T 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 -4 6 Mouse 7.1 pKi = 7.1 Binding
Displacement of [3H]CGP12177 from mouse beta1 receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from mouse beta1 receptor expressed in HEK293 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 -4 6 Mouse 7.1 pKi = 7.1 Binding
Displacement of [3H]CGP12177 from mouse beta1 receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from mouse beta1 receptor expressed in HEK293 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
2736067 87088 67 None 93 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]dihydroalprenolol from human wild type beta1 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysisDisplacement of [3H]dihydroalprenolol from human wild type beta1 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysis
ChEMBL 230 1 1 2 2.4 Clc1cc(Cl)cc(N2CCNCC2)c1 10.1021/jm400140q
CHEMBL2335158 87088 67 None 93 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]dihydroalprenolol from human wild type beta1 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysisDisplacement of [3H]dihydroalprenolol from human wild type beta1 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysis
ChEMBL 230 1 1 2 2.4 Clc1cc(Cl)cc(N2CCNCC2)c1 10.1021/jm400140q
10442852 11095 0 None -1 2 Rat 6.1 pKi = 6.1 Binding
Binding affinity against beta-1-adrenergic receptor in rat brainBinding affinity against beta-1-adrenergic receptor in rat brain
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 Rat 6.1 pKi = 6.1 Binding
Binding affinity against beta-1-adrenergic receptor in rat brainBinding affinity against beta-1-adrenergic receptor in rat brain
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 Rat 6.1 pKi = 6.1 Binding
Binding affinity against beta-1-adrenergic receptor in rat brainBinding affinity against beta-1-adrenergic receptor in rat brain
ChEMBL 202 6 2 4 1.1 CCCO/N=C/C(O)CNC(C)(C)C 10.1021/jm00036a018
146025727 171109 0 None -316 27 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]-pindolol from recombinant human beta1 adrenergic receptor expressed in CHO Flp-In cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-pindolol from recombinant human beta1 adrenergic receptor expressed in CHO 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 -316 27 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]-pindolol from recombinant human beta1 adrenergic receptor expressed in CHO Flp-In cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-pindolol from recombinant human beta1 adrenergic receptor expressed in CHO 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
130442572 171332 0 None -181 24 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]-pindolol from recombinant human beta1 adrenergic receptor expressed in CHO Flp-In cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-pindolol from recombinant human beta1 adrenergic receptor expressed in CHO 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 [125I]-pindolol from recombinant human beta1 adrenergic receptor expressed in CHO Flp-In cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-pindolol from recombinant human beta1 adrenergic receptor expressed in CHO 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
145946488 166965 0 None -46 2 Rat 6.1 pKi = 6.1 Binding
Displacement of [3H]-CGP-12177 from adrenergic beta1 receptor in Wistar rat cortex incubated for 60 mins by microbeta liquid scintillation counting analysisDisplacement of [3H]-CGP-12177 from adrenergic beta1 receptor in Wistar rat cortex incubated for 60 mins by microbeta liquid scintillation counting analysis
ChEMBL 435 10 2 7 3.4 COc1ccccc1OCCNCC(O)COc1cccc2c(=O)c3ccccc3oc12 10.1016/j.bmc.2018.04.038
CHEMBL4127540 166965 0 None -46 2 Rat 6.1 pKi = 6.1 Binding
Displacement of [3H]-CGP-12177 from adrenergic beta1 receptor in Wistar rat cortex incubated for 60 mins by microbeta liquid scintillation counting analysisDisplacement of [3H]-CGP-12177 from adrenergic beta1 receptor in Wistar rat cortex incubated for 60 mins by microbeta liquid scintillation counting analysis
ChEMBL 435 10 2 7 3.4 COc1ccccc1OCCNCC(O)COc1cccc2c(=O)c3ccccc3oc12 10.1016/j.bmc.2018.04.038
CHEMBL4300195 166965 0 None -46 2 Rat 6.1 pKi = 6.1 Binding
Displacement of [3H]-CGP-12177 from adrenergic beta1 receptor in Wistar rat cortex incubated for 60 mins by microbeta liquid scintillation counting analysisDisplacement of [3H]-CGP-12177 from adrenergic beta1 receptor in Wistar rat cortex incubated for 60 mins by microbeta liquid scintillation counting analysis
ChEMBL 435 10 2 7 3.4 COc1ccccc1OCCNCC(O)COc1cccc2c(=O)c3ccccc3oc12 10.1016/j.bmc.2018.04.038
52943770 17170 0 None -9 3 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta-1 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 -9 3 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta-1 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
181743 177987 3 None -4265 22 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]Iodopindolol from human adrenergic beta-1 receptorDisplacement of [125I]Iodopindolol from human adrenergic beta-1 receptor
ChEMBL 339 2 0 5 3.2 COc1cc2c3c(c1OC)-c1cc4c(cc1CC3N(C)CC2)OCO4 10.1016/j.bmcl.2009.11.053
CHEMBL467094 177987 3 None -4265 22 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]Iodopindolol from human adrenergic beta-1 receptorDisplacement of [125I]Iodopindolol from human adrenergic beta-1 receptor
ChEMBL 339 2 0 5 3.2 COc1cc2c3c(c1OC)-c1cc4c(cc1CC3N(C)CC2)OCO4 10.1016/j.bmcl.2009.11.053
155513731 169215 0 None -2 2 Mouse 6.1 pKi = 6.1 Binding
Displacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T 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 Mouse 6.1 pKi = 6.1 Binding
Displacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T 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
25120700 80813 0 None -5 2 Human 6.1 pKi = 6.1 Binding
Binding affinity to alpha1 adrenoceptorBinding affinity to alpha1 adrenoceptor
ChEMBL 369 7 1 5 3.0 COc1ccc(N2CCN(CC[C@@H](OC(N)=O)c3ccccc3)CC2)cc1 10.1016/j.bmcl.2012.02.023
CHEMBL2158704 80813 0 None -5 2 Human 6.1 pKi = 6.1 Binding
Binding affinity to alpha1 adrenoceptorBinding affinity to alpha1 adrenoceptor
ChEMBL 369 7 1 5 3.0 COc1ccc(N2CCN(CC[C@@H](OC(N)=O)c3ccccc3)CC2)cc1 10.1016/j.bmcl.2012.02.023
5581 101175 10 None -3 7 Guinea pig 7.1 pKi = 7.1 Binding
Binding affinity against Beta-1 adrenergic receptor in guinea pig left ventricleBinding affinity against Beta-1 adrenergic receptor in guinea pig left ventricle
ChEMBL 345 5 3 6 2.6 COc1cc(CC2NCCc3cc(O)c(O)cc32)cc(OC)c1OC 10.1021/jm00081a007
CHEMBL299175 101175 10 None -3 7 Guinea pig 7.1 pKi = 7.1 Binding
Binding affinity against Beta-1 adrenergic receptor in guinea pig left ventricleBinding affinity against Beta-1 adrenergic receptor in guinea pig left ventricle
ChEMBL 345 5 3 6 2.6 COc1cc(CC2NCCc3cc(O)c(O)cc32)cc(OC)c1OC 10.1021/jm00081a007
131487 4897 12 None - 1 Rat 4.1 pKi = 4.1 Binding
Compound was evaluated for the inhibition of binding of [3H]dihydroalprenolol from beta-1 adrenergic receptor of rat cerebral cortical membranesCompound was evaluated for the inhibition of binding of [3H]dihydroalprenolol from beta-1 adrenergic receptor of rat cerebral cortical membranes
ChEMBL 273 5 4 5 1.4 CC(C)(C)NCC(O)COc1cc(O)c(O)cc1F 10.1021/jm00107a027
CHEMBL10494 4897 12 None - 1 Rat 4.1 pKi = 4.1 Binding
Compound was evaluated for the inhibition of binding of [3H]dihydroalprenolol from beta-1 adrenergic receptor of rat cerebral cortical membranesCompound was evaluated for the inhibition of binding of [3H]dihydroalprenolol from beta-1 adrenergic receptor of rat cerebral cortical membranes
ChEMBL 273 5 4 5 1.4 CC(C)(C)NCC(O)COc1cc(O)c(O)cc1F 10.1021/jm00107a027
44396729 66513 0 None -34 3 Human 7.1 pKi = 7.1 Binding
Binding inhibition constant was determined by inhibition of [125I]-iodocyanopindolol binding to Beta-1 adrenergic receptorBinding inhibition constant was determined by inhibition of [125I]-iodocyanopindolol binding to Beta-1 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 -34 3 Human 7.1 pKi = 7.1 Binding
Binding inhibition constant was determined by inhibition of [125I]-iodocyanopindolol binding to Beta-1 adrenergic receptorBinding inhibition constant was determined by inhibition of [125I]-iodocyanopindolol binding to Beta-1 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
46889770 6628 0 None -5 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta-1 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta-1 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 7.1 pKi = 7.1 Binding
Displacement of [125I]cyanopindolol from human adrenergic beta-1 receptor expressed in CHOK1 cellsDisplacement of [125I]cyanopindolol from human adrenergic beta-1 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
49864335 15424 0 None -4 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 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 8.0 pKi = 8.0 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 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
49864357 15431 0 None -45 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 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 6.0 pKi = 6.0 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 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
4183 1986 62 None -2 3 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 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 7.0 pKi = 7.0 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 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 7.0 pKi = 7.0 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 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 7.0 pKi = 7.0 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 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 7.0 pKi = 7.0 Binding
Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assayDisplacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 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 7.0 pKi = 7.0 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 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 7.0 pKi = 7.0 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 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 7.0 pKi = 7.0 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 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 7.0 pKi = 7.0 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 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 7.0 pKi = 7.0 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 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
9894801 120212 0 None -4 2 Human 5.0 pKi = 5.0 Binding
Inhibition of 125 I-Iodocyanopindolol binding to Beta-1 adrenergic receptorInhibition of 125 I-Iodocyanopindolol binding to Beta-1 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 5.0 pKi = 5.0 Binding
Inhibition of 125 I-Iodocyanopindolol binding to Beta-1 adrenergic receptorInhibition of 125 I-Iodocyanopindolol binding to Beta-1 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
24936627 17489 0 None -41 3 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta-1 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 -41 3 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta-1 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
52949489 17350 0 None -30 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta-1 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 -30 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta-1 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
9827999 130369 0 None 7 2 Human 5.0 pKi = 5.0 Binding
Inhibition of 125 I-Iodocyanopindolol binding to Beta-1 adrenergic receptorInhibition of 125 I-Iodocyanopindolol binding to Beta-1 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 5.0 pKi = 5.0 Binding
Inhibition of 125 I-Iodocyanopindolol binding to Beta-1 adrenergic receptorInhibition of 125 I-Iodocyanopindolol binding to Beta-1 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
130442480 174688 0 None -117 24 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]-pindolol from recombinant human beta1 adrenergic receptor expressed in CHO Flp-In cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-pindolol from recombinant human beta1 adrenergic receptor expressed in CHO Flp-In cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 410 3 0 6 5.7 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1C(F)(F)F 10.1021/acs.jmedchem.9b00351
CHEMBL4572614 174688 0 None -117 24 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]-pindolol from recombinant human beta1 adrenergic receptor expressed in CHO Flp-In cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-pindolol from recombinant human beta1 adrenergic receptor expressed in CHO Flp-In cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 410 3 0 6 5.7 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1C(F)(F)F 10.1021/acs.jmedchem.9b00351
4407909 192254 1 None -16 10 Human 6.0 pKi = 6.0 Binding
Binding affinity to beta1 receptor (unknown origin) assessed as inhibition constantBinding affinity to beta1 receptor (unknown origin) assessed as inhibition constant
ChEMBL 356 4 2 4 3.6 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(F)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5182943 192254 1 None -16 10 Human 6.0 pKi = 6.0 Binding
Binding affinity to beta1 receptor (unknown origin) assessed as inhibition constantBinding affinity to beta1 receptor (unknown origin) assessed as inhibition constant
ChEMBL 356 4 2 4 3.6 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(F)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5221893 192254 1 None -16 10 Human 6.0 pKi = 6.0 Binding
Binding affinity to beta1 receptor (unknown origin) assessed as inhibition constantBinding affinity to beta1 receptor (unknown origin) assessed as inhibition constant
ChEMBL 356 4 2 4 3.6 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(F)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
10112744 154105 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]iodocyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human adrenergic beta-1 receptor expressed in CHO cells
ChEMBL 418 9 2 7 4.0 O[C@@H](CNCCOc1ccc(-c2csc(-c3ccncc3)n2)cc1)c1cccnc1 10.1016/j.bmcl.2007.06.072
CHEMBL399522 154105 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]iodocyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]iodocyanopindolol from human adrenergic beta-1 receptor expressed in CHO cells
ChEMBL 418 9 2 7 4.0 O[C@@H](CNCCOc1ccc(-c2csc(-c3ccncc3)n2)cc1)c1cccnc1 10.1016/j.bmcl.2007.06.072
128658 33738 7 None -11 5 Guinea pig 7.0 pKi = 7.0 Binding
Binding affinity against beta-1 adrenergic receptor in guinea pig left ventricleBinding affinity against beta-1 adrenergic receptor in guinea pig left ventricle
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 -11 5 Guinea pig 7.0 pKi = 7.0 Binding
Binding affinity against beta-1 adrenergic receptor in guinea pig left ventricleBinding affinity against beta-1 adrenergic receptor in guinea pig left ventricle
ChEMBL 363 5 3 6 2.7 COc1cc(CC2NCCc3cc(O)c(O)c(F)c32)cc(OC)c1OC 10.1021/jm00081a007
165193 3126 60 None -18 43 Rat 5.0 pKi = 5.0 Binding
Displacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation countingDisplacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation counting
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmc.2008.12.031
2303 3126 60 None -18 43 Rat 5.0 pKi = 5.0 Binding
Displacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation countingDisplacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation counting
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmc.2008.12.031
4946 3126 60 None -18 43 Rat 5.0 pKi = 5.0 Binding
Displacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation countingDisplacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation counting
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmc.2008.12.031
564 3126 60 None -18 43 Rat 5.0 pKi = 5.0 Binding
Displacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation countingDisplacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation counting
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmc.2008.12.031
62882 3126 60 None -18 43 Rat 5.0 pKi = 5.0 Binding
Displacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation countingDisplacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation counting
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmc.2008.12.031
63 3126 60 None -18 43 Rat 5.0 pKi = 5.0 Binding
Displacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation countingDisplacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation counting
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmc.2008.12.031
66366 3126 60 None -18 43 Rat 5.0 pKi = 5.0 Binding
Displacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation countingDisplacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation counting
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmc.2008.12.031
91536 3126 60 None -18 43 Rat 5.0 pKi = 5.0 Binding
Displacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation countingDisplacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation counting
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmc.2008.12.031
CHEMBL27 3126 60 None -18 43 Rat 5.0 pKi = 5.0 Binding
Displacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation countingDisplacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation counting
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmc.2008.12.031
CHEMBL452861 3126 60 None -18 43 Rat 5.0 pKi = 5.0 Binding
Displacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation countingDisplacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation counting
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmc.2008.12.031
DB00571 3126 60 None -18 43 Rat 5.0 pKi = 5.0 Binding
Displacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation countingDisplacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation counting
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1016/j.bmc.2008.12.031
24936489 17321 0 None -12 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta-1 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 -12 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta-1 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
71612644 132829 0 None 2 2 Human 5.0 pKi = 5.0 Binding
Inhibition Assay: Human recombinant adrenergic β1 receptors expressed in CHO-K1 cells are used in modified Tris-HCl buffer pH 7.4. A 25 aliquot is incubated with 0.03 nM [125I]Cyanopindolol for 120 minutes at 25° C. Non-specific binding is estimated in the presence of 100 μM S(−)-Propranolol. Receptors are filtered and washed, the filters are then counted to determine [125I]Cyanopindolol specifically bound. Compounds are screened at 10 μM.Inhibition Assay: Human recombinant adrenergic β1 receptors expressed in CHO-K1 cells are used in modified Tris-HCl buffer pH 7.4. A 25 aliquot is incubated with 0.03 nM [125I]Cyanopindolol for 120 minutes at 25° C. Non-specific binding is estimated in the presence of 100 μM S(−)-Propranolol. Receptors are filtered and washed, the filters are then counted to determine [125I]Cyanopindolol 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 5.0 pKi = 5.0 Binding
Inhibition Assay: Human recombinant adrenergic β1 receptors expressed in CHO-K1 cells are used in modified Tris-HCl buffer pH 7.4. A 25 aliquot is incubated with 0.03 nM [125I]Cyanopindolol for 120 minutes at 25° C. Non-specific binding is estimated in the presence of 100 μM S(−)-Propranolol. Receptors are filtered and washed, the filters are then counted to determine [125I]Cyanopindolol specifically bound. Compounds are screened at 10 μM.Inhibition Assay: Human recombinant adrenergic β1 receptors expressed in CHO-K1 cells are used in modified Tris-HCl buffer pH 7.4. A 25 aliquot is incubated with 0.03 nM [125I]Cyanopindolol for 120 minutes at 25° C. Non-specific binding is estimated in the presence of 100 μM S(−)-Propranolol. Receptors are filtered and washed, the filters are then counted to determine [125I]Cyanopindolol specifically bound. Compounds are screened at 10 μM.
ChEMBL 303 7 2 5 0.5 N#CC1CCCN1C(=O)CNCC(O)COc1ccccc1 nan
52943383 17384 0 None -16 3 Human 6.0 pKi = 6 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta-1 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 -16 3 Human 6.0 pKi = 6 Binding
Displacement of [125I]-cyanopindolol from human adrenergic beta-1 receptor expressed in CHO cellsDisplacement of [125I]-cyanopindolol from human adrenergic beta-1 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
1016 3678 75 None -43 35 Human 5.0 pKi = 5 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2561 3678 75 None -43 35 Human 5.0 pKi = 5 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2733526 3678 75 None -43 35 Human 5.0 pKi = 5 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
5384 3678 75 None -43 35 Human 5.0 pKi = 5 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
CHEMBL83 3678 75 None -43 35 Human 5.0 pKi = 5 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
DB00675 3678 75 None -43 35 Human 5.0 pKi = 5 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
11962616 219 7 None - 0 Human 7.4 pIC50 = 7.4 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 7.4 pIC50 = 7.4 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 7.4 pIC50 = 7.4 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 7.4 pIC50 = 7.4 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
2803 939 53 None -134 19 Guinea pig 8.4 pKd = 8.4 Binding
The compound was tested for beta-adrenergic activity against Beta-1 adrenergic receptor from guinea pig right atriaThe compound was tested for beta-adrenergic activity against Beta-1 adrenergic receptor from guinea pig right atria
Drug Central 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
516 939 53 None -134 19 Guinea pig 8.4 pKd = 8.4 Binding
The compound was tested for beta-adrenergic activity against Beta-1 adrenergic receptor from guinea pig right atriaThe compound was tested for beta-adrenergic activity against Beta-1 adrenergic receptor from guinea pig right atria
Drug Central 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
704 939 53 None -134 19 Guinea pig 8.4 pKd = 8.4 Binding
The compound was tested for beta-adrenergic activity against Beta-1 adrenergic receptor from guinea pig right atriaThe compound was tested for beta-adrenergic activity against Beta-1 adrenergic receptor from guinea pig right atria
Drug Central 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
CHEMBL134 939 53 None -134 19 Guinea pig 8.4 pKd = 8.4 Binding
The compound was tested for beta-adrenergic activity against Beta-1 adrenergic receptor from guinea pig right atriaThe compound was tested for beta-adrenergic activity against Beta-1 adrenergic receptor from guinea pig right atria
Drug Central 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
DB00575 939 53 None -134 19 Guinea pig 8.4 pKd = 8.4 Binding
The compound was tested for beta-adrenergic activity against Beta-1 adrenergic receptor from guinea pig right atriaThe compound was tested for beta-adrenergic activity against Beta-1 adrenergic receptor from guinea pig right atria
Drug Central 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
3486 3096 51 None -1 11 Rat 8.2 pKd = 8.2 Binding
Antagonist activity at beta1 adrenergic receptor in isolated rat atriaAntagonist activity at beta1 adrenergic receptor in isolated rat atria
Drug Central 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C None
4883 3096 51 None -1 11 Rat 8.2 pKd = 8.2 Binding
Antagonist activity at beta1 adrenergic receptor in isolated rat atriaAntagonist activity at beta1 adrenergic receptor in isolated rat atria
Drug Central 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C None
555 3096 51 None -1 11 Rat 8.2 pKd = 8.2 Binding
Antagonist activity at beta1 adrenergic receptor in isolated rat atriaAntagonist activity at beta1 adrenergic receptor in isolated rat atria
Drug Central 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C None
CHEMBL6995 3096 51 None -1 11 Rat 8.2 pKd = 8.2 Binding
Antagonist activity at beta1 adrenergic receptor in isolated rat atriaAntagonist activity at beta1 adrenergic receptor in isolated rat atria
Drug Central 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C None
DB01297 3096 51 None -1 11 Rat 8.2 pKd = 8.2 Binding
Antagonist activity at beta1 adrenergic receptor in isolated rat atriaAntagonist activity at beta1 adrenergic receptor in isolated rat atria
Drug Central 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C None
3083544 462 46 None -8 5 Human 8.2 pKd = 8.2 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 -8 5 Human 8.2 pKd = 8.2 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 -8 5 Human 8.2 pKd = 8.2 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 -8 5 Human 8.2 pKd = 8.2 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 -8 5 Human 8.2 pKd = 8.2 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
3486 3096 51 None -6 11 Guinea pig 8.2 pKd = 8.2 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
Drug Central 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C None
4883 3096 51 None -6 11 Guinea pig 8.2 pKd = 8.2 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
Drug Central 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C None
555 3096 51 None -6 11 Guinea pig 8.2 pKd = 8.2 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
Drug Central 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C None
CHEMBL6995 3096 51 None -6 11 Guinea pig 8.2 pKd = 8.2 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
Drug Central 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C None
DB01297 3096 51 None -6 11 Guinea pig 8.2 pKd = 8.2 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
Drug Central 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C None
1054 1549 49 None 1 3 Guinea pig 8.2 pKd = 8.2 Binding
Ability to block Beta-1 adrenergic receptor in guinea pig right atria preparationAbility to block Beta-1 adrenergic receptor in guinea pig right atria preparation
Drug Central 295 9 2 5 1.5 COC(=O)CCc1ccc(cc1)OCC(CNC(C)C)O None
59768 1549 49 None 1 3 Guinea pig 8.2 pKd = 8.2 Binding
Ability to block Beta-1 adrenergic receptor in guinea pig right atria preparationAbility to block Beta-1 adrenergic receptor in guinea pig right atria preparation
Drug Central 295 9 2 5 1.5 COC(=O)CCc1ccc(cc1)OCC(CNC(C)C)O None
7178 1549 49 None 1 3 Guinea pig 8.2 pKd = 8.2 Binding
Ability to block Beta-1 adrenergic receptor in guinea pig right atria preparationAbility to block Beta-1 adrenergic receptor in guinea pig right atria preparation
Drug Central 295 9 2 5 1.5 COC(=O)CCc1ccc(cc1)OCC(CNC(C)C)O None
CHEMBL768 1549 49 None 1 3 Guinea pig 8.2 pKd = 8.2 Binding
Ability to block Beta-1 adrenergic receptor in guinea pig right atria preparationAbility to block Beta-1 adrenergic receptor in guinea pig right atria preparation
Drug Central 295 9 2 5 1.5 COC(=O)CCc1ccc(cc1)OCC(CNC(C)C)O None
DB00187 1549 49 None 1 3 Guinea pig 8.2 pKd = 8.2 Binding
Ability to block Beta-1 adrenergic receptor in guinea pig right atria preparationAbility to block Beta-1 adrenergic receptor in guinea pig right atria preparation
Drug Central 295 9 2 5 1.5 COC(=O)CCc1ccc(cc1)OCC(CNC(C)C)O None
2249 509 106 None 2 12 Guinea pig 8.1 pKd = 8.1 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
Drug Central 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C None
255 509 106 None 2 12 Guinea pig 8.1 pKd = 8.1 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
Drug Central 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C None
548 509 106 None 2 12 Guinea pig 8.1 pKd = 8.1 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
Drug Central 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C None
CHEMBL24 509 106 None 2 12 Guinea pig 8.1 pKd = 8.1 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
Drug Central 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C None
DB00335 509 106 None 2 12 Guinea pig 8.1 pKd = 8.1 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
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 8.1 pKd = 8.1 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
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 8.1 pKd = 8.1 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
Drug Central 266 8 3 4 0.5 CC(C)NC[C@H](O)COc1ccc(CC(N)=O)cc1 None
155774 4021 33 None 5 3 Human 8.1 pKd = 8.1 Binding
Antagonist activity at human beta1 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 beta1 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 8.1 pKd = 8.1 Binding
Antagonist activity at human beta1 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 beta1 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 8.1 pKd = 8.1 Binding
Antagonist activity at human beta1 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 beta1 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 8.1 pKd = 8.1 Binding
Antagonist activity at human beta1 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 beta1 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 8.1 pKd = 8.1 Binding
Antagonist activity at human beta1 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 beta1 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
1786 2474 79 None -2 11 Guinea pig 8.1 pKd = 8.1 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
Drug Central 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O None
4171 2474 79 None -2 11 Guinea pig 8.1 pKd = 8.1 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
Drug Central 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O None
553 2474 79 None -2 11 Guinea pig 8.1 pKd = 8.1 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
Drug Central 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O None
CHEMBL13 2474 79 None -2 11 Guinea pig 8.1 pKd = 8.1 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
Drug Central 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O None
DB00264 2474 79 None -2 11 Guinea pig 8.1 pKd = 8.1 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
Drug Central 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O None
2369 615 75 None -5 8 Rat 8.1 pKd = 8.1 Binding
Antagonist activity at rat beta1 adrenoceptorAntagonist activity at rat beta1 adrenoceptor
Drug Central 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C None
356 615 75 None -5 8 Rat 8.1 pKd = 8.1 Binding
Antagonist activity at rat beta1 adrenoceptorAntagonist activity at rat beta1 adrenoceptor
Drug Central 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C None
549 615 75 None -5 8 Rat 8.1 pKd = 8.1 Binding
Antagonist activity at rat beta1 adrenoceptorAntagonist activity at rat beta1 adrenoceptor
Drug Central 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C None
CHEMBL423 615 75 None -5 8 Rat 8.1 pKd = 8.1 Binding
Antagonist activity at rat beta1 adrenoceptorAntagonist activity at rat beta1 adrenoceptor
Drug Central 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C None
DB00195 615 75 None -5 8 Rat 8.1 pKd = 8.1 Binding
Antagonist activity at rat beta1 adrenoceptorAntagonist activity at rat beta1 adrenoceptor
Drug Central 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C None
18047 201915 18 None 2 5 Guinea pig 8.1 pKd = 8.1 Binding
Beta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atriumBeta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atrium
Drug Central 223 6 2 3 1.7 Cc1cccc(OCC(O)CNC(C)C)c1 None
CHEMBL67096 201915 18 None 2 5 Guinea pig 8.1 pKd = 8.1 Binding
Beta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atriumBeta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atrium
Drug Central 223 6 2 3 1.7 Cc1cccc(OCC(O)CNC(C)C)c1 None
2369 615 75 None -13 8 Guinea pig 8.1 pKd = 8.1 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
Drug Central 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C None
356 615 75 None -13 8 Guinea pig 8.1 pKd = 8.1 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
Drug Central 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C None
549 615 75 None -13 8 Guinea pig 8.1 pKd = 8.1 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
Drug Central 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C None
CHEMBL423 615 75 None -13 8 Guinea pig 8.1 pKd = 8.1 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
Drug Central 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C None
DB00195 615 75 None -13 8 Guinea pig 8.1 pKd = 8.1 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
Drug Central 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C None
165193 3126 60 None -7 43 Guinea pig 8.1 pKd = 8.1 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
2303 3126 60 None -7 43 Guinea pig 8.1 pKd = 8.1 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
4946 3126 60 None -7 43 Guinea pig 8.1 pKd = 8.1 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
564 3126 60 None -7 43 Guinea pig 8.1 pKd = 8.1 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
62882 3126 60 None -7 43 Guinea pig 8.1 pKd = 8.1 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
63 3126 60 None -7 43 Guinea pig 8.1 pKd = 8.1 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
66366 3126 60 None -7 43 Guinea pig 8.1 pKd = 8.1 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
91536 3126 60 None -7 43 Guinea pig 8.1 pKd = 8.1 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
CHEMBL27 3126 60 None -7 43 Guinea pig 8.1 pKd = 8.1 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
CHEMBL452861 3126 60 None -7 43 Guinea pig 8.1 pKd = 8.1 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
DB00571 3126 60 None -7 43 Guinea pig 8.1 pKd = 8.1 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
2369 615 75 None 5 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 5 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 5 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 5 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 5 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 -2 5 Human 8.0 pKd = 8.0 Binding
Binding affinity to beta-1 adrenergic receptorBinding affinity to beta-1 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 8.0 pKd = 8.0 Binding
Binding affinity to beta-1 adrenergic receptorBinding affinity to beta-1 adrenergic receptor
Drug Central 223 6 2 3 1.7 Cc1cccc(OCC(O)CNC(C)C)c1 None
33624 3749 29 None -3 9 Guinea pig 8.0 pKd = 8.0 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
Drug Central 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C None
4061 3749 29 None -3 9 Guinea pig 8.0 pKd = 8.0 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
Drug Central 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C None
565 3749 29 None -3 9 Guinea pig 8.0 pKd = 8.0 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
Drug Central 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C None
CHEMBL499 3749 29 None -3 9 Guinea pig 8.0 pKd = 8.0 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
Drug Central 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C None
DB00373 3749 29 None -3 9 Guinea pig 8.0 pKd = 8.0 Binding
In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparationsIn vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations
Drug Central 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C None
137 367 47 None -19 12 Human 8.0 pKd = 8.0 Binding
radioligand [3H]CGP12177 0.15nM competition binding; human recombinant beta-adrenoreceptors in Sf9 cellsradioligand [3H]CGP12177 0.15nM competition binding; human recombinant beta-adrenoreceptors in Sf9 cells
Drug Central 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
2119 367 47 None -19 12 Human 8.0 pKd = 8.0 Binding
radioligand [3H]CGP12177 0.15nM competition binding; human recombinant beta-adrenoreceptors in Sf9 cellsradioligand [3H]CGP12177 0.15nM competition binding; human recombinant beta-adrenoreceptors in Sf9 cells
Drug Central 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
563 367 47 None -19 12 Human 8.0 pKd = 8.0 Binding
radioligand [3H]CGP12177 0.15nM competition binding; human recombinant beta-adrenoreceptors in Sf9 cellsradioligand [3H]CGP12177 0.15nM competition binding; human recombinant beta-adrenoreceptors in Sf9 cells
Drug Central 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
66368 367 47 None -19 12 Human 8.0 pKd = 8.0 Binding
radioligand [3H]CGP12177 0.15nM competition binding; human recombinant beta-adrenoreceptors in Sf9 cellsradioligand [3H]CGP12177 0.15nM competition binding; human recombinant beta-adrenoreceptors in Sf9 cells
Drug Central 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
CHEMBL266195 367 47 None -19 12 Human 8.0 pKd = 8.0 Binding
radioligand [3H]CGP12177 0.15nM competition binding; human recombinant beta-adrenoreceptors in Sf9 cellsradioligand [3H]CGP12177 0.15nM competition binding; human recombinant beta-adrenoreceptors in Sf9 cells
Drug Central 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
DB00866 367 47 None -19 12 Human 8.0 pKd = 8.0 Binding
radioligand [3H]CGP12177 0.15nM competition binding; human recombinant beta-adrenoreceptors in Sf9 cellsradioligand [3H]CGP12177 0.15nM competition binding; human recombinant beta-adrenoreceptors in Sf9 cells
Drug Central 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
165193 3126 60 125I-ICYP -2 43 Human 10.7 pKi = 10.7 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
2303 3126 60 125I-ICYP -2 43 Human 10.7 pKi = 10.7 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
4946 3126 60 125I-ICYP -2 43 Human 10.7 pKi = 10.7 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
564 3126 60 125I-ICYP -2 43 Human 10.7 pKi = 10.7 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
62882 3126 60 125I-ICYP -2 43 Human 10.7 pKi = 10.7 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
63 3126 60 125I-ICYP -2 43 Human 10.7 pKi = 10.7 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
66366 3126 60 125I-ICYP -2 43 Human 10.7 pKi = 10.7 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
91536 3126 60 125I-ICYP -2 43 Human 10.7 pKi = 10.7 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
CHEMBL27 3126 60 125I-ICYP -2 43 Human 10.7 pKi = 10.7 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
CHEMBL452861 3126 60 125I-ICYP -2 43 Human 10.7 pKi = 10.7 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
DB00571 3126 60 125I-ICYP -2 43 Human 10.7 pKi = 10.7 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 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
None 214731 0 125I-ICYP 3 3 Rat 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase None None None None None
None 214476 0 125I-Pindolol -2 30 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 316 7 3 3 3.0 CC(CF)NCC(COC1=CC=CC2=C1C3=CC=CC=C3N2)O None
2176 3065 66 UNDEFINED -4 27 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
4828 3065 66 UNDEFINED -4 27 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
91 3065 66 UNDEFINED -4 27 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
CHEMBL500 3065 66 UNDEFINED -4 27 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
DB00960 3065 66 UNDEFINED -4 27 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
2176 3065 66 125I-ICYP -2 27 Rat 9.2 pKi = 9.2 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 9.2 pKi = 9.2 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 9.2 pKi = 9.2 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 9.2 pKi = 9.2 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 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
165193 3126 60 125I-ICYP -18 43 Rat 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 -18 43 Rat 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 -18 43 Rat 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 -18 43 Rat 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 -18 43 Rat 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 -18 43 Rat 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 -18 43 Rat 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 -18 43 Rat 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 -18 43 Rat 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 -18 43 Rat 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 -18 43 Rat 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
137 367 47 3H-DHA -3 12 Rat 9.0 pKi = 9.0 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 9.0 pKi = 9.0 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 9.0 pKi = 9.0 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 9.0 pKi = 9.0 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 9.0 pKi = 9.0 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 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
2585 788 100 125I-CYP -1 22 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
522 788 100 125I-CYP -1 22 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
551 788 100 125I-CYP -1 22 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
CHEMBL723 788 100 125I-CYP -1 22 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
DB01136 788 100 125I-CYP -1 22 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
123686 1942 44 125I-Pindolol -1 9 Rat 8.7 pKi = 8.7 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 -1 9 Rat 8.7 pKi = 8.7 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 -1 9 Rat 8.7 pKi = 8.7 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
165193 3126 60 125I-CYP -2 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 125I-CYP -2 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 125I-CYP -2 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 125I-CYP -2 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 125I-CYP -2 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 125I-CYP -2 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 125I-CYP -2 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 125I-CYP -2 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 125I-CYP -2 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 125I-CYP -2 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 125I-CYP -2 43 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
2176 3065 66 125I-ICYP -4 27 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
4828 3065 66 125I-ICYP -4 27 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
91 3065 66 125I-ICYP -4 27 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
CHEMBL500 3065 66 125I-ICYP -4 27 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
DB00960 3065 66 125I-ICYP -4 27 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
487 779 65 None -4 6 Mouse 8.0 pKi = 8 Binding
Displacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T cells after 60 mins by radioligand competition binding assay
Drug Central 298 6 3 3 3.1 OC(COc1cccc2c1c1ccccc1[nH]2)CNC(C)C None
569 779 65 None -4 6 Mouse 8.0 pKi = 8 Binding
Displacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T cells after 60 mins by radioligand competition binding assay
Drug Central 298 6 3 3 3.1 OC(COc1cccc2c1c1ccccc1[nH]2)CNC(C)C None
71739 779 65 None -4 6 Mouse 8.0 pKi = 8 Binding
Displacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T cells after 60 mins by radioligand competition binding assay
Drug Central 298 6 3 3 3.1 OC(COc1cccc2c1c1ccccc1[nH]2)CNC(C)C None
CHEMBL324665 779 65 None -4 6 Mouse 8.0 pKi = 8 Binding
Displacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T cells after 60 mins by radioligand competition binding assay
Drug Central 298 6 3 3 3.1 OC(COc1cccc2c1c1ccccc1[nH]2)CNC(C)C 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
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
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
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
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
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
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
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
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
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
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
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
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
135398737 942 89 125I-Pindolol -269 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 125I-Pindolol -269 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 125I-Pindolol -269 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 125I-Pindolol -269 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 125I-Pindolol -269 92 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
1155 1592 45 125I-CYP -57 5 Human 5.0 pKi = 5 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 -57 5 Human 5.0 pKi = 5 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 -57 5 Human 5.0 pKi = 5 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 -57 5 Human 5.0 pKi = 5 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 -57 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 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
1353 1872 85 125I-Pindolol -6918 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 125I-Pindolol -6918 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 125I-Pindolol -6918 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 125I-Pindolol -6918 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 125I-Pindolol -6918 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
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
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
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
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
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
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
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
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
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
119570 3098 90 125I-Pindolol -7585 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 -7585 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 -7585 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 -7585 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 -7585 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 -7585 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 -7585 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 -7585 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 -7585 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 -7585 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
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 -2089 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 -2089 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 -2089 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
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
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
2598 3707 52 125I-ICYP -67 5 Guinea pig 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 125I-CYP -67 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-ICYP -67 5 Guinea pig 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 -67 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-ICYP -67 5 Guinea pig 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 -67 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-ICYP -67 5 Guinea pig 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 -67 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-ICYP -67 5 Guinea pig 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 -67 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
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
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
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
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
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
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
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
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
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
2865 4064 67 125I-Pindolol -1071 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 -1071 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 -1071 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 -1071 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 -1071 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 -501 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 -501 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 -501 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 -501 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 -501 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
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
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
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
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
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
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
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
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
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
104911 214239 0 125I-Pindolol -41686 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
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
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
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
3337 214431 0 125I-Pindolol -58 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 -58 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 -58 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 -58 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 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 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 214640 0 125I-CYP -23 3 Human 5.0 pKi = 5 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
None 214693 0 UNDEFINED -660 28 Guinea pig 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 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 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
3337 214431 0 125I-Pindolol -58 41 Human 6.0 pKi = 6 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 -58 41 Human 6.0 pKi = 6 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 -58 41 Human 6.0 pKi = 6 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 -58 41 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
5581 101175 10 125I-ICYP -4 7 Guinea pig 7.0 pKi = 7.0 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 -4 7 Guinea pig 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 345 5 3 6 2.6 COc1cc(CC2NCCc3cc(O)c(O)cc32)cc(OC)c1OC None
1531 2226 64 125I-ICYP -1 15 Rat 7.9 pKi = 7.9 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 -1 15 Rat 7.9 pKi = 7.9 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 -1 15 Rat 7.9 pKi = 7.9 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 -1 15 Rat 7.9 pKi = 7.9 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 -1 15 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O None
2369 615 75 125I-ICYP -5 8 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C None
356 615 75 125I-ICYP -5 8 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C None
549 615 75 125I-ICYP -5 8 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C None
CHEMBL423 615 75 125I-ICYP -5 8 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C None
DB00195 615 75 125I-ICYP -5 8 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C None
1978 248 54 125I-ICYP -19 6 Rat 6.9 pKi = 6.9 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 -19 6 Rat 6.9 pKi = 6.9 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 -19 6 Rat 6.9 pKi = 6.9 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 -19 6 Rat 6.9 pKi = 6.9 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 -19 6 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 336 10 3 5 3.0 CCCC(=Nc1ccc(c(c1)C(=O)C)OCC(CNC(C)C)O)O 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
3682 188837 7 125I-ICYP -229 8 Human 6.9 pKi = 6.9 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 -229 8 Human 6.9 pKi = 6.9 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 -229 8 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 277 6 2 3 2.6 Cc1ccc(OCC(O)C(C)NC(C)C)c2c1CCC2 None
1621 2386 16 125I-Pindolol -457 45 Rat 6.9 pKi = 6.9 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 -457 45 Rat 6.9 pKi = 6.9 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 -457 45 Rat 6.9 pKi = 6.9 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 -457 45 Rat 6.9 pKi = 6.9 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 -457 45 Rat 6.9 pKi = 6.9 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
242 467 117 125I-Pindolol -22 52 Human 6.9 pKi = 6.9 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 -22 52 Human 6.9 pKi = 6.9 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 -22 52 Human 6.9 pKi = 6.9 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 -22 52 Human 6.9 pKi = 6.9 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 -22 52 Human 6.9 pKi = 6.9 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 -22 52 Human 6.9 pKi = 6.9 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 -22 52 Human 6.9 pKi = 6.9 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 -22 52 Human 6.9 pKi = 6.9 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 -22 52 Human 6.9 pKi = 6.9 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 -22 52 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
3682 188837 7 125I-Pindolol -1047 8 Rat 5.8 pKi = 5.8 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 -1047 8 Rat 5.8 pKi = 5.8 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 -1047 8 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 277 6 2 3 2.6 Cc1ccc(OCC(O)C(C)NC(C)C)c2c1CCC2 None
2419 3394 80 125I-CYP -162 6 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O None
5152 3394 80 125I-CYP -162 6 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O None
559 3394 80 125I-CYP -162 6 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O None
CHEMBL1263 3394 80 125I-CYP -162 6 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O None
DB00938 3394 80 125I-CYP -162 6 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O None
3083544 462 46 125I-CYP -8 5 Human 5.8 pKi = 5.8 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 -8 5 Human 5.8 pKi = 5.8 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 -8 5 Human 5.8 pKi = 5.8 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 -8 5 Human 5.8 pKi = 5.8 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 -8 5 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O None
3682 188837 7 125I-ICYP -1047 8 Rat 6.7 pKi = 6.7 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 -1047 8 Rat 6.7 pKi = 6.7 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 -1047 8 Rat 6.7 pKi = 6.7 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 -1047 8 Rat 6.7 pKi = 6.7 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 -1047 8 Rat 6.7 pKi = 6.7 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 -1047 8 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 277 6 2 3 2.6 Cc1ccc(OCC(O)C(C)NC(C)C)c2c1CCC2 None
124433 150887 10 UNDEFINED 1 3 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 288 6 3 3 2.8 OC(CNC1CCCCC1)COc1cccc2[nH]ccc12 None
CHEMBL396185 150887 10 UNDEFINED 1 3 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 288 6 3 3 2.8 OC(CNC1CCCCC1)COc1cccc2[nH]ccc12 None
2176 3065 66 125I-CYP -4 27 Human 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-CYP -4 27 Human 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-CYP -4 27 Human 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-CYP -4 27 Human 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-CYP -4 27 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
165193 3126 60 125I-ICYP -2 43 Human 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 -2 43 Human 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 -2 43 Human 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 -2 43 Human 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 -2 43 Human 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 -2 43 Human 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 -2 43 Human 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 -2 43 Human 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 -2 43 Human 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 -2 43 Human 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 -2 43 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
165193 3126 60 125I-ICYP -18 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 -18 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 -18 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 -18 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 -18 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 -18 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 -18 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 -18 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 -18 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 -18 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 -18 43 Rat 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
2405 658 71 125I-CYP -1 4 Human 7.7 pKi = 7.7 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 -1 4 Human 7.7 pKi = 7.7 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 -1 4 Human 7.7 pKi = 7.7 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 -1 4 Human 7.7 pKi = 7.7 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 -1 4 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 325 12 2 5 2.4 OC(COc1ccc(cc1)COCCOC(C)C)CNC(C)C None
2464 3570 52 125I-ICYP -37 6 Rat 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 125I-ICYP -37 6 Rat 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 125I-ICYP -37 6 Rat 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 125I-ICYP -37 6 Rat 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 125I-ICYP -37 6 Rat 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
1499 2052 43 125I-CYP -46 17 Human 6.7 pKi = 6.7 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 -46 17 Human 6.7 pKi = 6.7 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 -46 17 Human 6.7 pKi = 6.7 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 -46 17 Human 6.7 pKi = 6.7 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 -46 17 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
7153 97557 74 125I-Pindolol -123 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 125I-Pindolol -123 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
None 214400 0 125I-ICYP -8 2 Guinea pig 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 363 5 3 6 2.7 COC1=CC(=CC(=C1OC)OC)CC2C3=CC(=C(C(=C3CCN2)F)O)O None
105 3392 84 125I-CYP 1 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 125I-CYP 1 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 125I-CYP 1 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 125I-CYP 1 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 125I-CYP 1 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
3486 3096 51 125I-ICYP -1 11 Rat 6.6 pKi = 6.6 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 -1 11 Rat 6.6 pKi = 6.6 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 -1 11 Rat 6.6 pKi = 6.6 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 -1 11 Rat 6.6 pKi = 6.6 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 -1 11 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C None
2865 4064 67 125I-ICYP -1071 54 Human 5.6 pKi = 5.6 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 -1071 54 Human 5.6 pKi = 5.6 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 -1071 54 Human 5.6 pKi = 5.6 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 -1071 54 Human 5.6 pKi = 5.6 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 -1071 54 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
219050 3309 21 3H-CGP-12177 -16595 21 Human 5.6 pKi = 5.6 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 -16595 21 Human 5.6 pKi = 5.6 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 -16595 21 Human 5.6 pKi = 5.6 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 Human 5.5 pKi = 5.5 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
484 2804 45 125I-CYP -19 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 125I-CYP -19 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 125I-CYP -19 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
128658 33738 7 125I-ICYP -4 5 Human 7.4 pKi = 7.4 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 -4 5 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 363 5 3 6 2.7 COc1cc(CC2NCCc3cc(O)c(O)c(F)c32)cc(OC)c1OC None
688390 214733 0 125I-ICYP -7 3 Rat 5.4 pKi = 5.4 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 5.4 pKi = 5.4 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
2249 509 106 125I-CYP -5 12 Human 6.4 pKi = 6.4 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 -5 12 Human 6.4 pKi = 6.4 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 -5 12 Human 6.4 pKi = 6.4 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 -5 12 Human 6.4 pKi = 6.4 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 -5 12 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C None
1028 287 69 125I-CYP -64 30 Human 5.4 pKi = 5.4 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 -64 30 Human 5.4 pKi = 5.4 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 -64 30 Human 5.4 pKi = 5.4 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 -64 30 Human 5.4 pKi = 5.4 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 -64 30 Human 5.4 pKi = 5.4 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 -64 30 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
137 367 47 125I-ICYP -3 12 Rat 8.4 pKi = 8.4 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 8.4 pKi = 8.4 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 8.4 pKi = 8.4 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 8.4 pKi = 8.4 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 8.4 pKi = 8.4 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 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
123707 214732 0 125I-ICYP 3 3 Rat 8.4 pKi = 8.4 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
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
135398737 942 89 None -144 92 Rat 8.3 pKi = 8.3 Binding
Binding affinity measured at the Beta-1 adrenergic receptor by the inhibition of [3H]DHA binding to rat cortex using unlabeled isoprenalin for nonspecific binding.Binding affinity measured at the Beta-1 adrenergic receptor by the inhibition of [3H]DHA binding to rat cortex using unlabeled isoprenalin for nonspecific binding.
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 942 89 None -144 92 Rat 8.3 pKi = 8.3 Binding
Binding affinity measured at the Beta-1 adrenergic receptor by the inhibition of [3H]DHA binding to rat cortex using unlabeled isoprenalin for nonspecific binding.Binding affinity measured at the Beta-1 adrenergic receptor by the inhibition of [3H]DHA binding to rat cortex using unlabeled isoprenalin for nonspecific binding.
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 942 89 None -144 92 Rat 8.3 pKi = 8.3 Binding
Binding affinity measured at the Beta-1 adrenergic receptor by the inhibition of [3H]DHA binding to rat cortex using unlabeled isoprenalin for nonspecific binding.Binding affinity measured at the Beta-1 adrenergic receptor by the inhibition of [3H]DHA binding to rat cortex using unlabeled isoprenalin for nonspecific binding.
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 942 89 None -144 92 Rat 8.3 pKi = 8.3 Binding
Binding affinity measured at the Beta-1 adrenergic receptor by the inhibition of [3H]DHA binding to rat cortex using unlabeled isoprenalin for nonspecific binding.Binding affinity measured at the Beta-1 adrenergic receptor by the inhibition of [3H]DHA binding to rat cortex using unlabeled isoprenalin for nonspecific binding.
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 942 89 None -144 92 Rat 8.3 pKi = 8.3 Binding
Binding affinity measured at the Beta-1 adrenergic receptor by the inhibition of [3H]DHA binding to rat cortex using unlabeled isoprenalin for nonspecific binding.Binding affinity measured at the Beta-1 adrenergic receptor by the inhibition of [3H]DHA binding to rat cortex using unlabeled isoprenalin for nonspecific binding.
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
2389 3267 114 None -1023 68 Rat 8.3 pKi = 8.3 Binding
Binding affinity measured at the Beta-1 adrenergic receptor by the inhibition of [3H]DHA binding to rat cortex using unlabeled isoprenalin for nonspecific binding.Binding affinity measured at the Beta-1 adrenergic receptor by the inhibition of [3H]DHA binding to rat cortex using unlabeled isoprenalin for nonspecific binding.
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3267 114 None -1023 68 Rat 8.3 pKi = 8.3 Binding
Binding affinity measured at the Beta-1 adrenergic receptor by the inhibition of [3H]DHA binding to rat cortex using unlabeled isoprenalin for nonspecific binding.Binding affinity measured at the Beta-1 adrenergic receptor by the inhibition of [3H]DHA binding to rat cortex using unlabeled isoprenalin for nonspecific binding.
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3267 114 None -1023 68 Rat 8.3 pKi = 8.3 Binding
Binding affinity measured at the Beta-1 adrenergic receptor by the inhibition of [3H]DHA binding to rat cortex using unlabeled isoprenalin for nonspecific binding.Binding affinity measured at the Beta-1 adrenergic receptor by the inhibition of [3H]DHA binding to rat cortex using unlabeled isoprenalin for nonspecific binding.
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3267 114 None -1023 68 Rat 8.3 pKi = 8.3 Binding
Binding affinity measured at the Beta-1 adrenergic receptor by the inhibition of [3H]DHA binding to rat cortex using unlabeled isoprenalin for nonspecific binding.Binding affinity measured at the Beta-1 adrenergic receptor by the inhibition of [3H]DHA binding to rat cortex using unlabeled isoprenalin for nonspecific binding.
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3267 114 None -1023 68 Rat 8.3 pKi = 8.3 Binding
Binding affinity measured at the Beta-1 adrenergic receptor by the inhibition of [3H]DHA binding to rat cortex using unlabeled isoprenalin for nonspecific binding.Binding affinity measured at the Beta-1 adrenergic receptor by the inhibition of [3H]DHA binding to rat cortex using unlabeled isoprenalin for nonspecific binding.
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
2685 875 15 125I-CYP -1 7 Human 8.3 pKi = 8.3 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 -1 7 Human 8.3 pKi = 8.3 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 -1 7 Human 8.3 pKi = 8.3 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
448537 159691 86 None -50 25 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 None
CHEMBL411 159691 86 None -50 25 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 None
2146 3039 63 None -36 8 Rat 8.3 pKi = 8.3 Binding
Displacement of [3H]dihydroalprenolol from adrenergic beta 1 receptor of rat cerebral cortical membranesDisplacement of [3H]dihydroalprenolol from adrenergic beta 1 receptor of rat cerebral cortical membranes
Drug Central 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O None
485 3039 63 None -36 8 Rat 8.3 pKi = 8.3 Binding
Displacement of [3H]dihydroalprenolol from adrenergic beta 1 receptor of rat cerebral cortical membranesDisplacement of [3H]dihydroalprenolol from adrenergic beta 1 receptor of rat cerebral cortical membranes
Drug Central 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O None
6041 3039 63 None -36 8 Rat 8.3 pKi = 8.3 Binding
Displacement of [3H]dihydroalprenolol from adrenergic beta 1 receptor of rat cerebral cortical membranesDisplacement of [3H]dihydroalprenolol from adrenergic beta 1 receptor of rat cerebral cortical membranes
Drug Central 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O None
CHEMBL1215 3039 63 None -36 8 Rat 8.3 pKi = 8.3 Binding
Displacement of [3H]dihydroalprenolol from adrenergic beta 1 receptor of rat cerebral cortical membranesDisplacement of [3H]dihydroalprenolol from adrenergic beta 1 receptor of rat cerebral cortical membranes
Drug Central 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O None
DB00388 3039 63 None -36 8 Rat 8.3 pKi = 8.3 Binding
Displacement of [3H]dihydroalprenolol from adrenergic beta 1 receptor of rat cerebral cortical membranesDisplacement of [3H]dihydroalprenolol from adrenergic beta 1 receptor of rat cerebral cortical membranes
Drug Central 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O None
103 4074 56 125I-ICYP -501 54 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2875 4074 56 125I-ICYP -501 54 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5736 4074 56 125I-ICYP -501 54 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL285802 4074 56 125I-ICYP -501 54 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
DB09225 4074 56 125I-ICYP -501 54 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
1155 1592 45 125I-ICYP -23 5 Guinea pig 5.4 pKi = 5.4 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 -23 5 Guinea pig 5.4 pKi = 5.4 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 -23 5 Guinea pig 5.4 pKi = 5.4 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 -23 5 Guinea pig 5.4 pKi = 5.4 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 -23 5 Guinea pig 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O None
3663 99492 79 125I-Pindolol -125 29 Rat 5.4 pKi = 5.4 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 -125 29 Rat 5.4 pKi = 5.4 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
1499 2052 43 125I-ICYP -67 17 Guinea pig 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-ICYP -67 17 Guinea pig 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-ICYP -67 17 Guinea pig 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-ICYP -67 17 Guinea pig 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-ICYP -67 17 Guinea pig 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
1786 2474 79 125I-CYP -1 11 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O None
4171 2474 79 125I-CYP -1 11 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O None
553 2474 79 125I-CYP -1 11 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O None
CHEMBL13 2474 79 125I-CYP -1 11 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O None
DB00264 2474 79 125I-CYP -1 11 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O None
3682 188837 7 125I-CYP -229 8 Human 7.3 pKi = 7.3 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 -229 8 Human 7.3 pKi = 7.3 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 -229 8 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 277 6 2 3 2.6 Cc1ccc(OCC(O)C(C)NC(C)C)c2c1CCC2 None
681 1432 65 None -44 39 Rat 8.3 pKi = 8.3 Binding
Binding of [3H]dihydroalprenolol to beta-1 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-1 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 -44 39 Rat 8.3 pKi = 8.3 Binding
Binding of [3H]dihydroalprenolol to beta-1 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-1 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 -44 39 Rat 8.3 pKi = 8.3 Binding
Binding of [3H]dihydroalprenolol to beta-1 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-1 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 -44 39 Rat 8.3 pKi = 8.3 Binding
Binding of [3H]dihydroalprenolol to beta-1 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-1 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 -44 39 Rat 8.3 pKi = 8.3 Binding
Binding of [3H]dihydroalprenolol to beta-1 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-1 adrenergic receptor of rat cerebral cortical membranes
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
2247 502 77 None -128 42 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
249 502 77 None -128 42 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
2603 502 77 None -128 42 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
CHEMBL296419 502 77 None -128 42 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
DB00637 502 77 None -128 42 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
1016 3678 75 None -43 35 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
2561 3678 75 None -43 35 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
2733526 3678 75 None -43 35 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
5384 3678 75 None -43 35 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
CHEMBL83 3678 75 None -43 35 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
DB00675 3678 75 None -43 35 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
681 1432 65 None 1 39 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
940 1432 65 None 1 39 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
947 1432 65 None 1 39 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
CHEMBL59 1432 65 None 1 39 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
DB00988 1432 65 None 1 39 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
43815 186327 58 None 1 25 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 None
CHEMBL1708 186327 58 None 1 25 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 None
CHEMBL490 186327 58 None 1 25 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 None
3198 203792 73 None -38 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
CHEMBL1201049 203792 73 None -38 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
CHEMBL808 203792 73 None -38 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
4189 205185 91 None -38 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
CHEMBL1559 205185 91 None -38 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
CHEMBL91 205185 91 None -38 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
2812 4696 96 None -38 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 None
CHEMBL104 4696 96 None -38 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 None
165193 3126 60 125I-ICYP -5 43 Guinea pig 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
2303 3126 60 125I-ICYP -5 43 Guinea pig 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
4946 3126 60 125I-ICYP -5 43 Guinea pig 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
564 3126 60 125I-ICYP -5 43 Guinea pig 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
62882 3126 60 125I-ICYP -5 43 Guinea pig 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
63 3126 60 125I-ICYP -5 43 Guinea pig 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
66366 3126 60 125I-ICYP -5 43 Guinea pig 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
91536 3126 60 125I-ICYP -5 43 Guinea pig 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
CHEMBL27 3126 60 125I-ICYP -5 43 Guinea pig 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
CHEMBL452861 3126 60 125I-ICYP -5 43 Guinea pig 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
DB00571 3126 60 125I-ICYP -5 43 Guinea pig 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
1209 1620 69 None 1 32 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
203 1620 69 None 1 32 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
3386 1620 69 None 1 32 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
CHEMBL41 1620 69 None 1 32 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
DB00472 1620 69 None 1 32 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
5581 101175 10 125I-ICYP -1 7 Human 8.3 pKi = 8.3 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 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 345 5 3 6 2.6 COc1cc(CC2NCCc3cc(O)c(O)cc32)cc(OC)c1OC None
103 4074 56 None -501 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 -501 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 -501 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 -501 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 -501 54 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
105 3392 84 125I-ICYP 1 6 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O None
2083 3392 84 125I-ICYP 1 6 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O None
558 3392 84 125I-ICYP 1 6 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O None
CHEMBL714 3392 84 125I-ICYP 1 6 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O None
DB01001 3392 84 125I-ICYP 1 6 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O None
1028 287 69 None -23 30 Guinea pig 8.3 pKi = 8.3 Binding
Binding affinity against beta-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of Dihydro-[3H]-alprenololBinding affinity against beta-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of Dihydro-[3H]-alprenolol
Drug Central 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
139148732 287 69 None -23 30 Guinea pig 8.3 pKi = 8.3 Binding
Binding affinity against beta-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of Dihydro-[3H]-alprenololBinding affinity against beta-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of Dihydro-[3H]-alprenolol
Drug Central 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
479 287 69 None -23 30 Guinea pig 8.3 pKi = 8.3 Binding
Binding affinity against beta-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of Dihydro-[3H]-alprenololBinding affinity against beta-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of Dihydro-[3H]-alprenolol
Drug Central 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
5816 287 69 None -23 30 Guinea pig 8.3 pKi = 8.3 Binding
Binding affinity against beta-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of Dihydro-[3H]-alprenololBinding affinity against beta-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of Dihydro-[3H]-alprenolol
Drug Central 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
CHEMBL679 287 69 None -23 30 Guinea pig 8.3 pKi = 8.3 Binding
Binding affinity against beta-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of Dihydro-[3H]-alprenololBinding affinity against beta-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of Dihydro-[3H]-alprenolol
Drug Central 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
DB00668 287 69 None -23 30 Guinea pig 8.3 pKi = 8.3 Binding
Binding affinity against beta-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of Dihydro-[3H]-alprenololBinding affinity against beta-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of Dihydro-[3H]-alprenolol
Drug Central 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
2865 4064 67 None -1071 54 Human 8.3 pKi = 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 -1071 54 Human 8.3 pKi = 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 -1071 54 Human 8.3 pKi = 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 -1071 54 Human 8.3 pKi = 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 -1071 54 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
105 3392 84 None 1 6 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O None
2083 3392 84 None 1 6 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O None
558 3392 84 None 1 6 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O None
CHEMBL714 3392 84 None 1 6 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O None
DB01001 3392 84 None 1 6 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O None
11954224 214164 0 None -3388 60 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
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
5311064 1334 41 None - 1 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 317 8 3 5 2.3 COc1cc(CCNC[C@@H](c2ccc(cc2)O)O)ccc1OC None
534 1334 41 None - 1 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 317 8 3 5 2.3 COc1cc(CCNC[C@@H](c2ccc(cc2)O)O)ccc1OC None
806 1334 41 None - 1 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 317 8 3 5 2.3 COc1cc(CCNC[C@@H](c2ccc(cc2)O)O)ccc1OC None
CHEMBL493682 1334 41 None - 1 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 317 8 3 5 2.3 COc1cc(CCNC[C@@H](c2ccc(cc2)O)O)ccc1OC None
137 367 47 125I-CYP -19 12 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
2119 367 47 125I-CYP -19 12 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
563 367 47 125I-CYP -19 12 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
66368 367 47 125I-CYP -19 12 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
CHEMBL266195 367 47 125I-CYP -19 12 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
DB00866 367 47 125I-CYP -19 12 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
2810 67245 50 None -1 2 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
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 beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 213 4 2 2 2.4 CC(C)NCC(O)c1ccccc1Cl None
31101 719 39 None -245 36 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
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 -245 36 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
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 -245 36 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
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 -245 36 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
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 -245 36 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
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
1028 287 69 None -66 30 Rat 8.2 pKi = 8.2 Binding
Binding of [3H]dihydroalprenolol to beta-1 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-1 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 -66 30 Rat 8.2 pKi = 8.2 Binding
Binding of [3H]dihydroalprenolol to beta-1 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-1 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 -66 30 Rat 8.2 pKi = 8.2 Binding
Binding of [3H]dihydroalprenolol to beta-1 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-1 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 -66 30 Rat 8.2 pKi = 8.2 Binding
Binding of [3H]dihydroalprenolol to beta-1 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-1 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 -66 30 Rat 8.2 pKi = 8.2 Binding
Binding of [3H]dihydroalprenolol to beta-1 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-1 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 -66 30 Rat 8.2 pKi = 8.2 Binding
Binding of [3H]dihydroalprenolol to beta-1 adrenergic receptor of rat cerebral cortical membranesBinding of [3H]dihydroalprenolol to beta-1 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
135398737 942 89 125I-ICYP -269 92 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 942 89 125I-ICYP -269 92 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 942 89 125I-ICYP -269 92 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 942 89 125I-ICYP -269 92 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 942 89 125I-ICYP -269 92 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 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
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
31101 719 39 3H-CGP-12177 -245 36 Human 6.2 pKi = 6.2 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 -245 36 Human 6.2 pKi = 6.2 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 -245 36 Human 6.2 pKi = 6.2 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 -245 36 Human 6.2 pKi = 6.2 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 -245 36 Human 6.2 pKi = 6.2 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
1222 1626 44 125I-ICYP -100 33 Human 6.2 pKi = 6.2 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 -100 33 Human 6.2 pKi = 6.2 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 -100 33 Human 6.2 pKi = 6.2 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 -100 33 Human 6.2 pKi = 6.2 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 -100 33 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
1960 2805 64 None -20 26 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O None
439260 2805 64 None -20 26 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O None
505 2805 64 None -20 26 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O None
CHEMBL1437 2805 64 None -20 26 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O None
DB00368 2805 64 None -20 26 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O None
66265 93566 12 None -1 19 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 231 4 1 1 3.2 CCN[C@@H](C)Cc1cccc(C(F)(F)F)c1 None
CHEMBL248702 93566 12 None -1 19 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 231 4 1 1 3.2 CCN[C@@H](C)Cc1cccc(C(F)(F)F)c1 None
2419 3394 80 None -162 6 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 adrenoceptor
Drug Central 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O None
5152 3394 80 None -162 6 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 adrenoceptor
Drug Central 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O None
559 3394 80 None -162 6 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 adrenoceptor
Drug Central 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O None
CHEMBL1263 3394 80 None -162 6 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 adrenoceptor
Drug Central 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O None
DB00938 3394 80 None -162 6 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 adrenoceptor
Drug Central 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O None
2464 3570 52 None -2 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 -2 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 -2 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 -2 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 -2 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
2419 3394 80 125I-ICYP -162 6 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O None
5152 3394 80 125I-ICYP -162 6 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O None
559 3394 80 125I-ICYP -162 6 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O None
CHEMBL1263 3394 80 125I-ICYP -162 6 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O None
DB00938 3394 80 125I-ICYP -162 6 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O None
3083544 462 46 125I-ICYP -8 5 Human 8.2 pKi = 8.2 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 -8 5 Human 8.2 pKi = 8.2 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 -8 5 Human 8.2 pKi = 8.2 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 -8 5 Human 8.2 pKi = 8.2 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 -8 5 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O None
1222 1626 44 None -100 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 -100 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 -100 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 -100 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 -100 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
2419 3394 80 None -16 6 Mouse 8.2 pKi = 8.2 Binding
Displacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T cells after 60 mins by radioligand competition binding assay
Drug Central 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O None
5152 3394 80 None -16 6 Mouse 8.2 pKi = 8.2 Binding
Displacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T cells after 60 mins by radioligand competition binding assay
Drug Central 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O None
559 3394 80 None -16 6 Mouse 8.2 pKi = 8.2 Binding
Displacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T cells after 60 mins by radioligand competition binding assay
Drug Central 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O None
CHEMBL1263 3394 80 None -16 6 Mouse 8.2 pKi = 8.2 Binding
Displacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T cells after 60 mins by radioligand competition binding assay
Drug Central 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O None
DB00938 3394 80 None -16 6 Mouse 8.2 pKi = 8.2 Binding
Displacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T cells after 60 mins by radioligand competition binding assay
Drug Central 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O None
1960 2805 64 None -10 26 Guinea pig 8.2 pKi = 8.2 Binding
Binding affinity against beta-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of Dihydro-[3H]-alprenololBinding affinity against beta-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of Dihydro-[3H]-alprenolol
Drug Central 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O None
439260 2805 64 None -10 26 Guinea pig 8.2 pKi = 8.2 Binding
Binding affinity against beta-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of Dihydro-[3H]-alprenololBinding affinity against beta-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of Dihydro-[3H]-alprenolol
Drug Central 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O None
505 2805 64 None -10 26 Guinea pig 8.2 pKi = 8.2 Binding
Binding affinity against beta-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of Dihydro-[3H]-alprenololBinding affinity against beta-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of Dihydro-[3H]-alprenolol
Drug Central 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O None
CHEMBL1437 2805 64 None -10 26 Guinea pig 8.2 pKi = 8.2 Binding
Binding affinity against beta-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of Dihydro-[3H]-alprenololBinding affinity against beta-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of Dihydro-[3H]-alprenolol
Drug Central 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O None
DB00368 2805 64 None -10 26 Guinea pig 8.2 pKi = 8.2 Binding
Binding affinity against beta-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of Dihydro-[3H]-alprenololBinding affinity against beta-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of Dihydro-[3H]-alprenolol
Drug Central 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O None
1588 2284 24 None -218 44 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
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 -218 44 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
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 -218 44 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
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 -218 44 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
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 -218 44 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
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
3083544 462 46 None -8 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 adrenoceptor
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 -8 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 adrenoceptor
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 -8 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 adrenoceptor
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 -8 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 adrenoceptor
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 -8 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 adrenoceptor
Drug Central 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O None
2258 3104 36 None 1 2 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 225 6 3 4 1.1 O[C@H](COc1ccc(cc1)O)CNC(C)C None
42396 3104 36 None 1 2 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 225 6 3 4 1.1 O[C@H](COc1ccc(cc1)O)CNC(C)C None
537 3104 36 None 1 2 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 225 6 3 4 1.1 O[C@H](COc1ccc(cc1)O)CNC(C)C None
CHEMBL1160714 3104 36 None 1 2 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 225 6 3 4 1.1 O[C@H](COc1ccc(cc1)O)CNC(C)C None
DB13777 3104 36 None 1 2 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 225 6 3 4 1.1 O[C@H](COc1ccc(cc1)O)CNC(C)C None
68770 44384 49 None 1 2 Human 8.2 pKi = 8.2 Binding
Binding affinity to beta1 adrenergic receptor (unknown origin) by radioligand binding assayBinding affinity to beta1 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 beta1 adrenergic receptor (unknown origin) by radioligand binding assayBinding affinity to beta1 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
443372 10123 23 None -1 3 Mouse 8.2 pKi = 8.2 Binding
Displacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T cells after 60 mins by radioligand competition binding assay
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 Mouse 8.2 pKi = 8.2 Binding
Displacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T cells after 60 mins by radioligand competition binding assay
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 Mouse 8.2 pKi = 8.2 Binding
Displacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T cells after 60 mins by radioligand competition binding assayDisplacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T cells after 60 mins by radioligand competition binding assay
Drug Central 211 4 4 4 1.1 CC(C)NC[C@H](O)c1ccc(O)c(O)c1 None
1499 2052 43 None -5 17 Mouse 8.2 pKi = 8.2 Binding
Displacement of [3H]CGP12177 from mouse beta1 receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from mouse beta1 receptor expressed in HEK293 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 Mouse 8.2 pKi = 8.2 Binding
Displacement of [3H]CGP12177 from mouse beta1 receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from mouse beta1 receptor expressed in HEK293 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 Mouse 8.2 pKi = 8.2 Binding
Displacement of [3H]CGP12177 from mouse beta1 receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from mouse beta1 receptor expressed in HEK293 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 Mouse 8.2 pKi = 8.2 Binding
Displacement of [3H]CGP12177 from mouse beta1 receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from mouse beta1 receptor expressed in HEK293 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 Mouse 8.2 pKi = 8.2 Binding
Displacement of [3H]CGP12177 from mouse beta1 receptor expressed in HEK293 cellsDisplacement of [3H]CGP12177 from mouse beta1 receptor expressed in HEK293 cells
Drug Central 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
2291 3123 52 None -11 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O None
2561 3123 52 None -11 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O None
4932 3123 52 None -11 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O None
CHEMBL631 3123 52 None -11 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O None
DB01182 3123 52 None -11 12 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O None
3486 3096 51 None 1 11 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C None
4883 3096 51 None 1 11 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C None
555 3096 51 None 1 11 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C None
CHEMBL6995 3096 51 None 1 11 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C None
DB01297 3096 51 None 1 11 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C None
175540 118737 45 None -1 5 Human 8.2 pKi = 8.2 Binding
Binding affinity to human adrenergic beta1 receptor by radioligand displacement assayBinding affinity to human adrenergic beta1 receptor by radioligand displacement assay
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 8.2 pKi = 8.2 Binding
Binding affinity to human adrenergic beta1 receptor by radioligand displacement assayBinding affinity to human adrenergic beta1 receptor by radioligand displacement assay
Drug Central 266 8 3 4 0.5 CC(C)NC[C@H](O)COc1ccc(CC(N)=O)cc1 None
1621 2386 16 None -102 45 Human 8.2 pKi = 8.2 Binding
Binding affinity towards Beta-1 adrenergic receptorBinding affinity towards Beta-1 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 -102 45 Human 8.2 pKi = 8.2 Binding
Binding affinity towards Beta-1 adrenergic receptorBinding affinity towards Beta-1 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 -102 45 Human 8.2 pKi = 8.2 Binding
Binding affinity towards Beta-1 adrenergic receptorBinding affinity towards Beta-1 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 -102 45 Human 8.2 pKi = 8.2 Binding
Binding affinity towards Beta-1 adrenergic receptorBinding affinity towards Beta-1 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 -102 45 Human 8.2 pKi = 8.2 Binding
Binding affinity towards Beta-1 adrenergic receptorBinding affinity towards Beta-1 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
242 467 117 None -22 52 Human 8.2 pKi = 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 -22 52 Human 8.2 pKi = 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 -22 52 Human 8.2 pKi = 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 -22 52 Human 8.2 pKi = 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 -22 52 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
1054 1549 49 None -1 3 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 295 9 2 5 1.5 COC(=O)CCc1ccc(cc1)OCC(CNC(C)C)O None
59768 1549 49 None -1 3 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 295 9 2 5 1.5 COC(=O)CCc1ccc(cc1)OCC(CNC(C)C)O None
7178 1549 49 None -1 3 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 295 9 2 5 1.5 COC(=O)CCc1ccc(cc1)OCC(CNC(C)C)O None
CHEMBL768 1549 49 None -1 3 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 295 9 2 5 1.5 COC(=O)CCc1ccc(cc1)OCC(CNC(C)C)O None
DB00187 1549 49 None -1 3 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 295 9 2 5 1.5 COC(=O)CCc1ccc(cc1)OCC(CNC(C)C)O None
11823027 192006 33 None -1 3 Human 8.2 pKi = 8.2 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 8.2 pKi = 8.2 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 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 309 5 4 5 0.6 CC(C)(C)NCC(O)COc1cccc2c1CC(O)C(O)C2 None
1960 2805 64 None -144 26 Rat 8.2 pKi = 8.2 Binding
Tested for binding affinity against beta-1 adrenergic receptor in rat brain using [3H]-CGP- 26505 as radioligandTested for binding affinity against beta-1 adrenergic receptor in rat brain using [3H]-CGP- 26505 as radioligand
Drug Central 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O None
439260 2805 64 None -144 26 Rat 8.2 pKi = 8.2 Binding
Tested for binding affinity against beta-1 adrenergic receptor in rat brain using [3H]-CGP- 26505 as radioligandTested for binding affinity against beta-1 adrenergic receptor in rat brain using [3H]-CGP- 26505 as radioligand
Drug Central 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O None
505 2805 64 None -144 26 Rat 8.2 pKi = 8.2 Binding
Tested for binding affinity against beta-1 adrenergic receptor in rat brain using [3H]-CGP- 26505 as radioligandTested for binding affinity against beta-1 adrenergic receptor in rat brain using [3H]-CGP- 26505 as radioligand
Drug Central 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O None
CHEMBL1437 2805 64 None -144 26 Rat 8.2 pKi = 8.2 Binding
Tested for binding affinity against beta-1 adrenergic receptor in rat brain using [3H]-CGP- 26505 as radioligandTested for binding affinity against beta-1 adrenergic receptor in rat brain using [3H]-CGP- 26505 as radioligand
Drug Central 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O None
DB00368 2805 64 None -144 26 Rat 8.2 pKi = 8.2 Binding
Tested for binding affinity against beta-1 adrenergic receptor in rat brain using [3H]-CGP- 26505 as radioligandTested for binding affinity against beta-1 adrenergic receptor in rat brain using [3H]-CGP- 26505 as radioligand
Drug Central 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O None
135409468 1996 63 125I-Pindolol -2238 40 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
333 1996 63 125I-Pindolol -2238 40 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
CHEMBL845 1996 63 125I-Pindolol -2238 40 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
1786 2474 79 125I-ICYP -21 11 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O None
4171 2474 79 125I-ICYP -21 11 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O None
553 2474 79 125I-ICYP -21 11 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O None
CHEMBL13 2474 79 125I-ICYP -21 11 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O None
DB00264 2474 79 125I-ICYP -21 11 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O None
2601 3709 30 3H-CGP-12177 -72 21 Human 6.2 pKi = 6.2 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 -72 21 Human 6.2 pKi = 6.2 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 -72 21 Human 6.2 pKi = 6.2 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 -72 21 Human 6.2 pKi = 6.2 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 -72 21 Human 6.2 pKi = 6.2 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
1588 2284 24 3H-CGP-12177 -218 44 Human 7.2 pKi = 7.2 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 -218 44 Human 7.2 pKi = 7.2 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 -218 44 Human 7.2 pKi = 7.2 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 -218 44 Human 7.2 pKi = 7.2 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 -218 44 Human 7.2 pKi = 7.2 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
4183 1986 62 None -2 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 adrenoceptor
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 8.2 pKi = 8.2 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 adrenoceptor
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 8.2 pKi = 8.2 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 adrenoceptor
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 8.2 pKi = 8.2 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 adrenoceptor
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 8.2 pKi = 8.2 Binding
Displacement of [3H]CGP12177 from human beta-1 adrenoceptorDisplacement of [3H]CGP12177 from human beta-1 adrenoceptor
Drug Central 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O None
12582 935 40 None -3 5 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
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 -3 5 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
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 -3 5 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
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 -3 5 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 276 3 3 3 3.0 CC(C)(C)NCC(C1=CC(=C(C(=C1)Cl)N)Cl)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
2176 3065 66 125I-ICYP -22 27 Guinea pig 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
4828 3065 66 125I-ICYP -22 27 Guinea pig 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
91 3065 66 125I-ICYP -22 27 Guinea pig 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
CHEMBL500 3065 66 125I-ICYP -22 27 Guinea pig 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
DB00960 3065 66 125I-ICYP -22 27 Guinea pig 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
1978 248 54 None -16 6 Human 8.1 pKi = 8.1 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 8.1 pKi = 8.1 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 8.1 pKi = 8.1 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 8.1 pKi = 8.1 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 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 336 10 3 5 3.0 CCCC(=Nc1ccc(c(c1)C(=O)C)OCC(CNC(C)C)O)O None
2249 509 106 None -5 12 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C None
255 509 106 None -5 12 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C None
548 509 106 None -5 12 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C None
CHEMBL24 509 106 None -5 12 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C None
DB00335 509 106 None -5 12 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C None
1786 2474 79 None 1 11 Mouse 8.1 pKi = 8.1 Binding
Displacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranes
Drug Central 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O None
4171 2474 79 None 1 11 Mouse 8.1 pKi = 8.1 Binding
Displacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranes
Drug Central 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O None
553 2474 79 None 1 11 Mouse 8.1 pKi = 8.1 Binding
Displacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranes
Drug Central 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O None
CHEMBL13 2474 79 None 1 11 Mouse 8.1 pKi = 8.1 Binding
Displacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranes
Drug Central 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O None
DB00264 2474 79 None 1 11 Mouse 8.1 pKi = 8.1 Binding
Displacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranes
Drug Central 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O None
11504295 2867 40 None -1 3 Human 8.1 pKi = 8.1 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 8.1 pKi = 8.1 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 8.1 pKi = 8.1 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 8.1 pKi = 8.1 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 8.1 pKi = 8.1 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
4806 3933 85 None -2 13 Human 8.1 pKi = 8.1 Binding
Binding affinity to human beta 1 adrenergic receptorBinding affinity to human beta 1 adrenergic receptor
Drug Central 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 None
7351 3933 85 None -2 13 Human 8.1 pKi = 8.1 Binding
Binding affinity to human beta 1 adrenergic receptorBinding affinity to human beta 1 adrenergic receptor
Drug Central 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 None
9966051 3933 85 None -2 13 Human 8.1 pKi = 8.1 Binding
Binding affinity to human beta 1 adrenergic receptorBinding affinity to human beta 1 adrenergic receptor
Drug Central 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 None
CHEMBL2104993 3933 85 None -2 13 Human 8.1 pKi = 8.1 Binding
Binding affinity to human beta 1 adrenergic receptorBinding affinity to human beta 1 adrenergic receptor
Drug Central 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 None
DB09068 3933 85 None -2 13 Human 8.1 pKi = 8.1 Binding
Binding affinity to human beta 1 adrenergic receptorBinding affinity to human beta 1 adrenergic receptor
Drug Central 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 None
1786 2474 79 None -1 11 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O None
4171 2474 79 None -1 11 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O None
553 2474 79 None -1 11 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O None
CHEMBL13 2474 79 None -1 11 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O None
DB00264 2474 79 None -1 11 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O None
2405 658 71 None -1 4 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 325 12 2 5 2.4 OC(COc1ccc(cc1)COCCOC(C)C)CNC(C)C None
380 658 71 None -1 4 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 325 12 2 5 2.4 OC(COc1ccc(cc1)COCCOC(C)C)CNC(C)C None
7129 658 71 None -1 4 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 325 12 2 5 2.4 OC(COc1ccc(cc1)COCCOC(C)C)CNC(C)C None
CHEMBL645 658 71 None -1 4 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 325 12 2 5 2.4 OC(COc1ccc(cc1)COCCOC(C)C)CNC(C)C None
DB00612 658 71 None -1 4 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 325 12 2 5 2.4 OC(COc1ccc(cc1)COCCOC(C)C)CNC(C)C None
4631 193292 25 125I-ICYP 1 7 Rat 8.1 pKi = 8.1 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 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 265 9 2 4 2.0 C=CCOc1ccccc1OCC(O)CNC(C)C None
21268191 89203 0 UNDEFINED -1 3 Human 8.1 pKi = 8.1 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 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 340 6 3 3 3.5 OC(CNC12CC3CC(CC(C3)C1)C2)COc1cccc2[nH]ccc12 None
105 3392 84 125I-ICYP -181 6 Guinea pig 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O None
2083 3392 84 125I-ICYP -181 6 Guinea pig 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O None
558 3392 84 125I-ICYP -181 6 Guinea pig 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O None
CHEMBL714 3392 84 125I-ICYP -181 6 Guinea pig 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O None
DB01001 3392 84 125I-ICYP -181 6 Guinea pig 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O None
119376 1803 41 3H-CGP-26505 -43651 27 Rat 5.1 pKi = 5.1 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 3H-CGP-26505 -43651 27 Rat 5.1 pKi = 5.1 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 3H-CGP-26505 -43651 27 Rat 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C None
146294 913 0 None 6 2 Human 8.1 pKi = 8.1 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 8.1 pKi = 8.1 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 8.1 pKi = 8.1 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 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 323 12 2 5 2.2 OC(COc1ccc(cc1)OCCOCC1CC1)CNC(C)C None
2663 98294 30 None -1 3 Human 8.1 pKi = 8.1 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 8.1 pKi = 8.1 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
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
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
1531 2226 64 None -1 15 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
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 beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
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 beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
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 beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
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 beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O None
2405 658 71 None 1 4 Mouse 8.1 pKi = 8.1 Binding
Displacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranes
Drug Central 325 12 2 5 2.4 OC(COc1ccc(cc1)COCCOC(C)C)CNC(C)C None
380 658 71 None 1 4 Mouse 8.1 pKi = 8.1 Binding
Displacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranes
Drug Central 325 12 2 5 2.4 OC(COc1ccc(cc1)COCCOC(C)C)CNC(C)C None
7129 658 71 None 1 4 Mouse 8.1 pKi = 8.1 Binding
Displacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranes
Drug Central 325 12 2 5 2.4 OC(COc1ccc(cc1)COCCOC(C)C)CNC(C)C None
CHEMBL645 658 71 None 1 4 Mouse 8.1 pKi = 8.1 Binding
Displacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranes
Drug Central 325 12 2 5 2.4 OC(COc1ccc(cc1)COCCOC(C)C)CNC(C)C None
DB00612 658 71 None 1 4 Mouse 8.1 pKi = 8.1 Binding
Displacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranes
Drug Central 325 12 2 5 2.4 OC(COc1ccc(cc1)COCCOC(C)C)CNC(C)C None
39468 2270 33 None -3 7 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
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 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
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 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
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 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
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 8.1 pKi = 8.1 Binding
DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 291 5 2 4 2.3 O[C@H](COc1cccc2c1CCCC2=O)CNC(C)(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
165193 3126 60 None -18 43 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]CGP12177 from beta1 adrenoreceptor in Rattus norvegicus (rat) cerebral cortex by liquid scintillation countingDisplacement of [3H]CGP12177 from beta1 adrenoreceptor in Rattus norvegicus (rat) cerebral cortex by liquid scintillation counting
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
2303 3126 60 None -18 43 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]CGP12177 from beta1 adrenoreceptor in Rattus norvegicus (rat) cerebral cortex by liquid scintillation countingDisplacement of [3H]CGP12177 from beta1 adrenoreceptor in Rattus norvegicus (rat) cerebral cortex by liquid scintillation counting
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
4946 3126 60 None -18 43 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]CGP12177 from beta1 adrenoreceptor in Rattus norvegicus (rat) cerebral cortex by liquid scintillation countingDisplacement of [3H]CGP12177 from beta1 adrenoreceptor in Rattus norvegicus (rat) cerebral cortex by liquid scintillation counting
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
564 3126 60 None -18 43 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]CGP12177 from beta1 adrenoreceptor in Rattus norvegicus (rat) cerebral cortex by liquid scintillation countingDisplacement of [3H]CGP12177 from beta1 adrenoreceptor in Rattus norvegicus (rat) cerebral cortex by liquid scintillation counting
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
62882 3126 60 None -18 43 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]CGP12177 from beta1 adrenoreceptor in Rattus norvegicus (rat) cerebral cortex by liquid scintillation countingDisplacement of [3H]CGP12177 from beta1 adrenoreceptor in Rattus norvegicus (rat) cerebral cortex by liquid scintillation counting
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
63 3126 60 None -18 43 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]CGP12177 from beta1 adrenoreceptor in Rattus norvegicus (rat) cerebral cortex by liquid scintillation countingDisplacement of [3H]CGP12177 from beta1 adrenoreceptor in Rattus norvegicus (rat) cerebral cortex by liquid scintillation counting
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
66366 3126 60 None -18 43 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]CGP12177 from beta1 adrenoreceptor in Rattus norvegicus (rat) cerebral cortex by liquid scintillation countingDisplacement of [3H]CGP12177 from beta1 adrenoreceptor in Rattus norvegicus (rat) cerebral cortex by liquid scintillation counting
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
91536 3126 60 None -18 43 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]CGP12177 from beta1 adrenoreceptor in Rattus norvegicus (rat) cerebral cortex by liquid scintillation countingDisplacement of [3H]CGP12177 from beta1 adrenoreceptor in Rattus norvegicus (rat) cerebral cortex by liquid scintillation counting
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
CHEMBL27 3126 60 None -18 43 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]CGP12177 from beta1 adrenoreceptor in Rattus norvegicus (rat) cerebral cortex by liquid scintillation countingDisplacement of [3H]CGP12177 from beta1 adrenoreceptor in Rattus norvegicus (rat) cerebral cortex by liquid scintillation counting
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
CHEMBL452861 3126 60 None -18 43 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]CGP12177 from beta1 adrenoreceptor in Rattus norvegicus (rat) cerebral cortex by liquid scintillation countingDisplacement of [3H]CGP12177 from beta1 adrenoreceptor in Rattus norvegicus (rat) cerebral cortex by liquid scintillation counting
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
DB00571 3126 60 None -18 43 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]CGP12177 from beta1 adrenoreceptor in Rattus norvegicus (rat) cerebral cortex by liquid scintillation countingDisplacement of [3H]CGP12177 from beta1 adrenoreceptor in Rattus norvegicus (rat) cerebral cortex by liquid scintillation counting
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
165193 3126 60 None -4 43 Mouse 8.1 pKi = 8.1 Binding
Displacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranes
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
2303 3126 60 None -4 43 Mouse 8.1 pKi = 8.1 Binding
Displacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranes
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
4946 3126 60 None -4 43 Mouse 8.1 pKi = 8.1 Binding
Displacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranes
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
564 3126 60 None -4 43 Mouse 8.1 pKi = 8.1 Binding
Displacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranes
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
62882 3126 60 None -4 43 Mouse 8.1 pKi = 8.1 Binding
Displacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranes
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
63 3126 60 None -4 43 Mouse 8.1 pKi = 8.1 Binding
Displacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranes
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
66366 3126 60 None -4 43 Mouse 8.1 pKi = 8.1 Binding
Displacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranes
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
91536 3126 60 None -4 43 Mouse 8.1 pKi = 8.1 Binding
Displacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranes
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
CHEMBL27 3126 60 None -4 43 Mouse 8.1 pKi = 8.1 Binding
Displacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranes
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
CHEMBL452861 3126 60 None -4 43 Mouse 8.1 pKi = 8.1 Binding
Displacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranes
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
DB00571 3126 60 None -4 43 Mouse 8.1 pKi = 8.1 Binding
Displacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranesDisplacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranes
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
165193 3126 60 None -2 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 -2 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 -2 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 -2 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 -2 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 -2 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 -2 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 -2 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 -2 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 -2 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 -2 43 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)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
21138 97986 34 125I-ICYP -1 7 Rat 7.1 pKi = 7.1 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 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NC[C@@H](O)COc1cccc2ccccc12 None
2475 728 0 None -1 3 Human 8.1 pKi = 8.1 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 8.1 pKi = 8.1 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 8.1 pKi = 8.1 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 8.1 pKi = 8.1 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 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 271 5 2 3 2.8 OC(COc1cc(C)ccc1Cl)CNC(C)(C)C None
33624 3749 29 None -7 9 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C None
4061 3749 29 None -7 9 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C None
565 3749 29 None -7 9 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C None
CHEMBL499 3749 29 None -7 9 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C None
DB00373 3749 29 None -7 9 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C None
2585 788 100 None -4 22 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation methodDisplacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation method
Drug Central 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
522 788 100 None -4 22 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation methodDisplacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation method
Drug Central 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
551 788 100 None -4 22 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation methodDisplacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation method
Drug Central 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
CHEMBL723 788 100 None -4 22 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation methodDisplacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation method
Drug Central 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
DB01136 788 100 None -4 22 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation methodDisplacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation method
Drug Central 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
4752 2269 29 None 1 3 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 307 11 2 4 2.4 O[C@H](COc1ccc(cc1)CCOCC1CC1)CNC(C)C None
60657 2269 29 None 1 3 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 307 11 2 4 2.4 O[C@H](COc1ccc(cc1)CCOCC1CC1)CNC(C)C None
8035 2269 29 None 1 3 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 307 11 2 4 2.4 O[C@H](COc1ccc(cc1)CCOCC1CC1)CNC(C)C None
CHEMBL1201274 2269 29 None 1 3 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 307 11 2 4 2.4 O[C@H](COc1ccc(cc1)CCOCC1CC1)CNC(C)C None
DB09351 2269 29 None 1 3 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 307 11 2 4 2.4 O[C@H](COc1ccc(cc1)CCOCC1CC1)CNC(C)C 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
2176 3065 66 None -4 27 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
4828 3065 66 None -4 27 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
91 3065 66 None -4 27 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
CHEMBL500 3065 66 None -4 27 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
DB00960 3065 66 None -4 27 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
2585 788 100 None -1 22 Human 8.0 pKi = 8.0 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 = 8.0 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 = 8.0 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 = 8.0 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 = 8.0 Binding
NoneNone
Drug Central 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
44112 120764 41 None -2 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 -2 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
2249 509 106 125I-ICYP -2 12 Rat 7.0 pKi = 7.0 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 -2 12 Rat 7.0 pKi = 7.0 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 -2 12 Rat 7.0 pKi = 7.0 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 -2 12 Rat 7.0 pKi = 7.0 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 -2 12 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C None
128658 33738 7 125I-ICYP -11 5 Guinea pig 7.0 pKi = 7.0 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 -11 5 Guinea pig 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 363 5 3 6 2.7 COc1cc(CC2NCCc3cc(O)c(O)c(F)c32)cc(OC)c1OC None
2249 509 106 125I-ICYP -2 12 Rat 7.0 pKi = 7.0 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 -2 12 Rat 7.0 pKi = 7.0 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 -2 12 Rat 7.0 pKi = 7.0 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 -2 12 Rat 7.0 pKi = 7.0 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 -2 12 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C None
3337 214431 0 125I-Pindolol -58 41 Human 6.0 pKi = 6 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 -58 41 Human 6.0 pKi = 6 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 -58 41 Human 6.0 pKi = 6 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 -58 41 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
118422671 2706 0 None 3 4 Human 9.2 pKi = 9.2 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 20590599
118422671 2706 0 None 3 4 Human 9.2 pKi = 9.2 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 9.2 pKi = 9.2 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 20590599
1887 2706 0 None 3 4 Human 9.2 pKi = 9.2 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 9.2 pKi = 9.2 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 20590599
71301 2706 0 None 3 4 Human 9.2 pKi = 9.2 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 9.2 pKi = 9.2 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 20590599
7246 2706 0 None 3 4 Human 9.2 pKi = 9.2 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 9.2 pKi = 9.2 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 20590599
CHEMBL434394 2706 0 None 3 4 Human 9.2 pKi = 9.2 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 9.2 pKi = 9.2 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 20590599
DB04861 2706 0 None 3 4 Human 9.2 pKi = 9.2 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
36811 1421 34 None -93 7 Human 5.5 pKi = 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 301 7 4 4 3.0 CC(CCc1ccc(cc1)O)NCCc1ccc(c(c1)O)O 10531390
535 1421 34 None -93 7 Human 5.5 pKi = 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 301 7 4 4 3.0 CC(CCc1ccc(cc1)O)NCCc1ccc(c(c1)O)O 10531390
937 1421 34 None -93 7 Human 5.5 pKi = 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 301 7 4 4 3.0 CC(CCc1ccc(cc1)O)NCCc1ccc(c(c1)O)O 10531390
CHEMBL926 1421 34 None -93 7 Human 5.5 pKi = 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 301 7 4 4 3.0 CC(CCc1ccc(cc1)O)NCCc1ccc(c(c1)O)O 10531390
DB00841 1421 34 None -93 7 Human 5.5 pKi = 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 301 7 4 4 3.0 CC(CCc1ccc(cc1)O)NCCc1ccc(c(c1)O)O 10531390
1028 287 69 None -64 30 Human 5.7 pKi = 5.7 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 -64 30 Human 5.7 pKi = 5.7 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 -64 30 Human 5.7 pKi = 5.7 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 -64 30 Human 5.7 pKi = 5.7 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 -64 30 Human 5.7 pKi = 5.7 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 -64 30 Human 5.7 pKi = 5.7 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 -64 30 Human 5.7 pKi = 5.7 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 -64 30 Human 5.7 pKi = 5.7 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 -64 30 Human 5.7 pKi = 5.7 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 -64 30 Human 5.7 pKi = 5.7 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 -64 30 Human 5.7 pKi = 5.7 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 -64 30 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 2849109
1960 2805 64 None -20 26 Human 5.8 pKi = 5.8 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 -20 26 Human 5.8 pKi = 5.8 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 -20 26 Human 5.8 pKi = 5.8 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 -20 26 Human 5.8 pKi = 5.8 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 -20 26 Human 5.8 pKi = 5.8 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 -20 26 Human 5.8 pKi = 5.8 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 -20 26 Human 5.8 pKi = 5.8 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 -20 26 Human 5.8 pKi = 5.8 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 -20 26 Human 5.8 pKi = 5.8 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 -20 26 Human 5.8 pKi = 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 2849109
5311064 1334 41 None - 1 Human 5.8 pKi = 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 317 8 3 5 2.3 COc1cc(CCNC[C@@H](c2ccc(cc2)O)O)ccc1OC 10531390
5311064 1334 41 None - 1 Human 5.8 pKi = 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 317 8 3 5 2.3 COc1cc(CCNC[C@@H](c2ccc(cc2)O)O)ccc1OC 7902433
534 1334 41 None - 1 Human 5.8 pKi = 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 317 8 3 5 2.3 COc1cc(CCNC[C@@H](c2ccc(cc2)O)O)ccc1OC 10531390
534 1334 41 None - 1 Human 5.8 pKi = 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 317 8 3 5 2.3 COc1cc(CCNC[C@@H](c2ccc(cc2)O)O)ccc1OC 7902433
806 1334 41 None - 1 Human 5.8 pKi = 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 317 8 3 5 2.3 COc1cc(CCNC[C@@H](c2ccc(cc2)O)O)ccc1OC 10531390
806 1334 41 None - 1 Human 5.8 pKi = 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 317 8 3 5 2.3 COc1cc(CCNC[C@@H](c2ccc(cc2)O)O)ccc1OC 7902433
CHEMBL493682 1334 41 None - 1 Human 5.8 pKi = 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 317 8 3 5 2.3 COc1cc(CCNC[C@@H](c2ccc(cc2)O)O)ccc1OC 10531390
CHEMBL493682 1334 41 None - 1 Human 5.8 pKi = 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 317 8 3 5 2.3 COc1cc(CCNC[C@@H](c2ccc(cc2)O)O)ccc1OC 7902433
484 2804 45 None -19 36 Human 6.0 pKi = 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O 2849109
951 2804 45 None -19 36 Human 6.0 pKi = 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O 2849109
CHEMBL432 2804 45 None -19 36 Human 6.0 pKi = 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O 2849109
4508 3078 91 None -199 13 Human 6.0 pKi = 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNCC(c1ccc(c(c1)O)O)O 2849109
4866774 3078 91 None -199 13 Human 6.0 pKi = 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNCC(c1ccc(c(c1)O)O)O 2849109
509 3078 91 None -199 13 Human 6.0 pKi = 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNCC(c1ccc(c(c1)O)O)O 2849109
838 3078 91 None -199 13 Human 6.0 pKi = 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNCC(c1ccc(c(c1)O)O)O 2849109
CHEMBL1740 3078 91 None -199 13 Human 6.0 pKi = 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 3 4 4 0.4 CNCC(c1ccc(c(c1)O)O)O 2849109
2464 3570 52 None -2 6 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C None
5253 3570 52 None -2 6 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C None
7297 3570 52 None -2 6 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C None
CHEMBL471 3570 52 None -2 6 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C None
DB00489 3570 52 None -2 6 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C None
1978 248 54 None -16 6 Human 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 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 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 336 10 3 5 3.0 CCCC(=Nc1ccc(c(c1)C(=O)C)OCC(CNC(C)C)O)O None
3486 3096 51 None 1 11 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C 10079020
3486 3096 51 None 1 11 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C 15655528
4883 3096 51 None 1 11 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C 10079020
4883 3096 51 None 1 11 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C 15655528
555 3096 51 None 1 11 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C 10079020
555 3096 51 None 1 11 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C 15655528
CHEMBL6995 3096 51 None 1 11 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C 10079020
CHEMBL6995 3096 51 None 1 11 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C 15655528
DB01297 3096 51 None 1 11 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C 10079020
DB01297 3096 51 None 1 11 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C 15655528
3083544 462 46 None -8 5 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O 20655218
4943 462 46 None -8 5 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O 20655218
7479 462 46 None -8 5 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O 20655218
CHEMBL1363 462 46 None -8 5 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O 20655218
DB01274 462 46 None -8 5 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 344 9 4 5 2.2 O=CNc1cc(ccc1O)[C@H](CN[C@@H](Cc1ccc(cc1)OC)C)O 20655218
4183 1986 62 None -2 3 Human 6.7 pKi = 6.7 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 6.7 pKi = 6.7 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 6.7 pKi = 6.7 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 6.7 pKi = 6.7 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 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O 22932315
2291 3123 52 None -11 12 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O None
2561 3123 52 None -11 12 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O None
4932 3123 52 None -11 12 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O None
CHEMBL631 3123 52 None -11 12 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O None
DB01182 3123 52 None -11 12 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O None
1499 2052 43 None -46 17 Human 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 2849109
1499 2052 43 None -46 17 Human 6.8 pKi = 6.8 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 -46 17 Human 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 2849109
3779 2052 43 None -46 17 Human 6.8 pKi = 6.8 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 -46 17 Human 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 2849109
536 2052 43 None -46 17 Human 6.8 pKi = 6.8 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 -46 17 Human 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 2849109
CHEMBL434 2052 43 None -46 17 Human 6.8 pKi = 6.8 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 -46 17 Human 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 2849109
DB01064 2052 43 None -46 17 Human 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 8982677
1054 1549 49 None -1 3 Human 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 9 2 5 1.5 COC(=O)CCc1ccc(cc1)OCC(CNC(C)C)O 27451411
59768 1549 49 None -1 3 Human 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 9 2 5 1.5 COC(=O)CCc1ccc(cc1)OCC(CNC(C)C)O 27451411
7178 1549 49 None -1 3 Human 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 9 2 5 1.5 COC(=O)CCc1ccc(cc1)OCC(CNC(C)C)O 27451411
CHEMBL768 1549 49 None -1 3 Human 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 9 2 5 1.5 COC(=O)CCc1ccc(cc1)OCC(CNC(C)C)O 27451411
DB00187 1549 49 None -1 3 Human 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 9 2 5 1.5 COC(=O)CCc1ccc(cc1)OCC(CNC(C)C)O 27451411
39147 2662 0 None -7 3 Human 6.9 pKi = 6.9 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 6.9 pKi = 6.9 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 6.9 pKi = 6.9 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 6.9 pKi = 6.9 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
155774 4021 33 None 5 3 Human 7.0 pKi = 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 339 8 4 6 -0.2 OC(COc1ccc(cc1)O)CNCCNC(=O)N1CCOCC1 10531390
2848 4021 33 None 5 3 Human 7.0 pKi = 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 339 8 4 6 -0.2 OC(COc1ccc(cc1)O)CNCCNC(=O)N1CCOCC1 10531390
538 4021 33 None 5 3 Human 7.0 pKi = 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 339 8 4 6 -0.2 OC(COc1ccc(cc1)O)CNCCNC(=O)N1CCOCC1 10531390
CHEMBL75753 4021 33 None 5 3 Human 7.0 pKi = 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 339 8 4 6 -0.2 OC(COc1ccc(cc1)O)CNCCNC(=O)N1CCOCC1 10531390
DB13781 4021 33 None 5 3 Human 7.0 pKi = 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 339 8 4 6 -0.2 OC(COc1ccc(cc1)O)CNCCNC(=O)N1CCOCC1 10531390
2249 509 106 None -5 12 Human 7.2 pKi = 7.2 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 -5 12 Human 7.2 pKi = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 15060759
2249 509 106 None -5 12 Human 7.2 pKi = 7.2 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 -5 12 Human 7.2 pKi = 7.2 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 -5 12 Human 7.2 pKi = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 15060759
255 509 106 None -5 12 Human 7.2 pKi = 7.2 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 -5 12 Human 7.2 pKi = 7.2 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 -5 12 Human 7.2 pKi = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 15060759
548 509 106 None -5 12 Human 7.2 pKi = 7.2 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 -5 12 Human 7.2 pKi = 7.2 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 -5 12 Human 7.2 pKi = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 15060759
CHEMBL24 509 106 None -5 12 Human 7.2 pKi = 7.2 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 -5 12 Human 7.2 pKi = 7.2 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 -5 12 Human 7.2 pKi = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 15060759
DB00335 509 106 None -5 12 Human 7.2 pKi = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C 15655528
1786 2474 79 None -1 11 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10079020
1786 2474 79 None -1 11 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10411574
1786 2474 79 None -1 11 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 14645666
1786 2474 79 None -1 11 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 14730417
1786 2474 79 None -1 11 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 15655528
4171 2474 79 None -1 11 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10079020
4171 2474 79 None -1 11 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10411574
4171 2474 79 None -1 11 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 14645666
4171 2474 79 None -1 11 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 14730417
4171 2474 79 None -1 11 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 15655528
553 2474 79 None -1 11 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10079020
553 2474 79 None -1 11 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10411574
553 2474 79 None -1 11 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 14645666
553 2474 79 None -1 11 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 14730417
553 2474 79 None -1 11 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 15655528
CHEMBL13 2474 79 None -1 11 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10079020
CHEMBL13 2474 79 None -1 11 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10411574
CHEMBL13 2474 79 None -1 11 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 14645666
CHEMBL13 2474 79 None -1 11 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 14730417
CHEMBL13 2474 79 None -1 11 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 15655528
DB00264 2474 79 None -1 11 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10079020
DB00264 2474 79 None -1 11 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 10411574
DB00264 2474 79 None -1 11 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 14645666
DB00264 2474 79 None -1 11 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 14730417
DB00264 2474 79 None -1 11 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O 15655528
1531 2226 64 None -1 15 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O 14645666
1531 2226 64 None -1 15 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O 15655528
3869 2226 64 None -1 15 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O 14645666
3869 2226 64 None -1 15 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O 15655528
7207 2226 64 None -1 15 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O 14645666
7207 2226 64 None -1 15 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O 15655528
CHEMBL429 2226 64 None -1 15 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O 14645666
CHEMBL429 2226 64 None -1 15 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O 15655528
DB00598 2226 64 None -1 15 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O 14645666
DB00598 2226 64 None -1 15 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O 15655528
2405 658 71 None -1 4 Human 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 325 12 2 5 2.4 OC(COc1ccc(cc1)COCCOC(C)C)CNC(C)C 28400472
380 658 71 None -1 4 Human 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 325 12 2 5 2.4 OC(COc1ccc(cc1)COCCOC(C)C)CNC(C)C 28400472
7129 658 71 None -1 4 Human 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 325 12 2 5 2.4 OC(COc1ccc(cc1)COCCOC(C)C)CNC(C)C 28400472
CHEMBL645 658 71 None -1 4 Human 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 325 12 2 5 2.4 OC(COc1ccc(cc1)COCCOC(C)C)CNC(C)C 28400472
DB00612 658 71 None -1 4 Human 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 325 12 2 5 2.4 OC(COc1ccc(cc1)COCCOC(C)C)CNC(C)C 28400472
156297 3286 0 None - 1 Human 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 363 10 4 7 1.7 COc1cc(CCNCC(COc2ccc(c(c2)O)O)O)ccc1OC 9117106
5571 3286 0 None - 1 Human 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 363 10 4 7 1.7 COc1cc(CCNCC(COc2ccc(c(c2)O)O)O)ccc1OC 9117106
5311452 3601 8 None -7 3 Human 8.1 pKi = 8.1 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 8.1 pKi = 8.1 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 8.1 pKi = 8.1 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 8.1 pKi = 8.1 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 8.1 pKi = 8.1 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 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 325 7 2 3 3.7 CCc1ccccc1OC[C@H](CN[C@H]1CCCc2c1cccc2)O 15655528
2475 728 0 None -1 3 Human 8.2 pKi = 8.2 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 8.2 pKi = 8.2 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 8.2 pKi = 8.2 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 8.2 pKi = 8.2 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 8.2 pKi = 8.2 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 8.2 pKi = 8.2 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 8.2 pKi = 8.2 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 8.2 pKi = 8.2 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 8.2 pKi = 8.2 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 8.2 pKi = 8.2 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 8.2 pKi = 8.2 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 8.2 pKi = 8.2 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 8.2 pKi = 8.2 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 8.2 pKi = 8.2 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 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 271 5 2 3 2.8 OC(COc1cc(C)ccc1Cl)CNC(C)(C)C 15655528
12579 2701 0 None - 1 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 470 14 4 7 3.7 O[C@@H](CNCCOC1=CC=C(C=C1)C(O)=N)COC2=CC3=C(O[C@H](CCCC4CC4)CO3)C=C2 28400472
165193 3126 60 None -2 43 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10079020
165193 3126 60 None -2 43 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 15060759
165193 3126 60 None -2 43 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 15655528
165193 3126 60 None -2 43 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 27588207
2303 3126 60 None -2 43 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10079020
2303 3126 60 None -2 43 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 15060759
2303 3126 60 None -2 43 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 15655528
2303 3126 60 None -2 43 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 27588207
4946 3126 60 None -2 43 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10079020
4946 3126 60 None -2 43 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 15060759
4946 3126 60 None -2 43 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 15655528
4946 3126 60 None -2 43 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 27588207
564 3126 60 None -2 43 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10079020
564 3126 60 None -2 43 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 15060759
564 3126 60 None -2 43 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 15655528
564 3126 60 None -2 43 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 27588207
62882 3126 60 None -2 43 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10079020
62882 3126 60 None -2 43 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 15060759
62882 3126 60 None -2 43 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 15655528
62882 3126 60 None -2 43 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 27588207
63 3126 60 None -2 43 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10079020
63 3126 60 None -2 43 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 15060759
63 3126 60 None -2 43 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 15655528
63 3126 60 None -2 43 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 27588207
66366 3126 60 None -2 43 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10079020
66366 3126 60 None -2 43 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 15060759
66366 3126 60 None -2 43 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 15655528
66366 3126 60 None -2 43 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 27588207
91536 3126 60 None -2 43 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10079020
91536 3126 60 None -2 43 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 15060759
91536 3126 60 None -2 43 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 15655528
91536 3126 60 None -2 43 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 27588207
CHEMBL27 3126 60 None -2 43 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10079020
CHEMBL27 3126 60 None -2 43 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 15060759
CHEMBL27 3126 60 None -2 43 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 15655528
CHEMBL27 3126 60 None -2 43 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 27588207
CHEMBL452861 3126 60 None -2 43 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10079020
CHEMBL452861 3126 60 None -2 43 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 15060759
CHEMBL452861 3126 60 None -2 43 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 15655528
CHEMBL452861 3126 60 None -2 43 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 27588207
DB00571 3126 60 None -2 43 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10079020
DB00571 3126 60 None -2 43 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 15060759
DB00571 3126 60 None -2 43 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 15655528
DB00571 3126 60 None -2 43 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 27588207
39468 2270 33 None -3 7 Human 8.4 pKi = 8.4 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 8.4 pKi = 8.4 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 8.4 pKi = 8.4 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 8.4 pKi = 8.4 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 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 291 5 2 4 2.3 O[C@H](COc1cccc2c1CCCC2=O)CNC(C)(C)C None
2685 875 15 None -1 7 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 494 11 4 8 2.3 OC(COc1ccc(cc1)c1nc(cn1C)C(F)(F)F)CNCCOc1ccc(c(c1)C(=O)N)O 10079020
2685 875 15 None -1 7 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 494 11 4 8 2.3 OC(COc1ccc(cc1)c1nc(cn1C)C(F)(F)F)CNCCOc1ccc(c(c1)C(=O)N)O 10411574
2685 875 15 None -1 7 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 494 11 4 8 2.3 OC(COc1ccc(cc1)c1nc(cn1C)C(F)(F)F)CNCCOc1ccc(c(c1)C(=O)N)O 15655528
2685 875 15 None -1 7 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 494 11 4 8 2.3 OC(COc1ccc(cc1)c1nc(cn1C)C(F)(F)F)CNCCOc1ccc(c(c1)C(=O)N)O 26385885
2685 875 15 None -1 7 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 494 11 4 8 2.3 OC(COc1ccc(cc1)c1nc(cn1C)C(F)(F)F)CNCCOc1ccc(c(c1)C(=O)N)O 27588207
541 875 15 None -1 7 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 494 11 4 8 2.3 OC(COc1ccc(cc1)c1nc(cn1C)C(F)(F)F)CNCCOc1ccc(c(c1)C(=O)N)O 10079020
541 875 15 None -1 7 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 494 11 4 8 2.3 OC(COc1ccc(cc1)c1nc(cn1C)C(F)(F)F)CNCCOc1ccc(c(c1)C(=O)N)O 10411574
541 875 15 None -1 7 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 494 11 4 8 2.3 OC(COc1ccc(cc1)c1nc(cn1C)C(F)(F)F)CNCCOc1ccc(c(c1)C(=O)N)O 15655528
541 875 15 None -1 7 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 494 11 4 8 2.3 OC(COc1ccc(cc1)c1nc(cn1C)C(F)(F)F)CNCCOc1ccc(c(c1)C(=O)N)O 26385885
541 875 15 None -1 7 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 494 11 4 8 2.3 OC(COc1ccc(cc1)c1nc(cn1C)C(F)(F)F)CNCCOc1ccc(c(c1)C(=O)N)O 27588207
CHEMBL280822 875 15 None -1 7 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 494 11 4 8 2.3 OC(COc1ccc(cc1)c1nc(cn1C)C(F)(F)F)CNCCOc1ccc(c(c1)C(=O)N)O 10079020
CHEMBL280822 875 15 None -1 7 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 494 11 4 8 2.3 OC(COc1ccc(cc1)c1nc(cn1C)C(F)(F)F)CNCCOc1ccc(c(c1)C(=O)N)O 10411574
CHEMBL280822 875 15 None -1 7 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 494 11 4 8 2.3 OC(COc1ccc(cc1)c1nc(cn1C)C(F)(F)F)CNCCOc1ccc(c(c1)C(=O)N)O 15655528
CHEMBL280822 875 15 None -1 7 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 494 11 4 8 2.3 OC(COc1ccc(cc1)c1nc(cn1C)C(F)(F)F)CNCCOc1ccc(c(c1)C(=O)N)O 26385885
CHEMBL280822 875 15 None -1 7 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 494 11 4 8 2.3 OC(COc1ccc(cc1)c1nc(cn1C)C(F)(F)F)CNCCOc1ccc(c(c1)C(=O)N)O 27588207
12580 2702 0 None - 1 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 482 13 3 7 3.1 O[C@@H](CNCCOC1=CC=C2C(=O)NCC2=C1)COC3=CC4=C(O[C@H](CCCC5CC5)CO4)C=C3 28400472
4752 2269 29 None 1 3 Human 8.7 pKi = 8.7 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 1 3 Human 8.7 pKi = 8.7 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 1 3 Human 8.7 pKi = 8.7 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 1 3 Human 8.7 pKi = 8.7 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 1 3 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 307 11 2 4 2.4 O[C@H](COc1ccc(cc1)CCOCC1CC1)CNC(C)C 11572462
2369 615 75 None 5 8 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C 10079020
356 615 75 None 5 8 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C 10079020
549 615 75 None 5 8 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C 10079020
CHEMBL423 615 75 None 5 8 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C 10079020
DB00195 615 75 None 5 8 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C 10079020
123686 1942 44 None -1 9 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 9 4 5 1.7 C1=CC=C(C=C1)NC(=O)NCCNCC(COC2=CC=CC=C2C#N)O 23614528
12581 1942 44 None -1 9 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 9 4 5 1.7 C1=CC=C(C=C1)NC(=O)NCCNCC(COC2=CC=CC=C2C#N)O 23614528
CHEMBL11268 1942 44 None -1 9 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 9 4 5 1.7 C1=CC=C(C=C1)NC(=O)NCCNCC(COC2=CC=CC=C2C#N)O 23614528
2585 788 100 None -1 22 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10411574
2585 788 100 None -1 22 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 15655528
522 788 100 None -1 22 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10411574
522 788 100 None -1 22 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 15655528
551 788 100 None -1 22 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10411574
551 788 100 None -1 22 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 15655528
CHEMBL723 788 100 None -1 22 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10411574
CHEMBL723 788 100 None -1 22 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 15655528
DB01136 788 100 None -1 22 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10411574
DB01136 788 100 None -1 22 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 15655528
2176 3065 66 None -4 27 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C 17804228
4828 3065 66 None -4 27 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C 17804228
91 3065 66 None -4 27 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C 17804228
CHEMBL500 3065 66 None -4 27 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C 17804228
DB00960 3065 66 None -4 27 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C 17804228
135398737 942 89 None -269 92 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 942 89 None -269 92 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 942 89 None -269 92 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 942 89 None -269 92 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 942 89 None -269 92 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 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
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
1028 287 69 None -64 30 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
139148732 287 69 None -64 30 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
479 287 69 None -64 30 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
5816 287 69 None -64 30 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
CHEMBL679 287 69 None -64 30 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
DB00668 287 69 None -64 30 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
3337 214431 0 None -58 41 Human 8.2 pKi None 8.2 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 -58 41 Human 8.2 pKi None 8.2 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 -58 41 Human 8.2 pKi None 8.2 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 -58 41 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
2601 3709 30 None -72 21 Human 8.2 pKi None 8.2 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 -72 21 Human 8.2 pKi None 8.2 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 -72 21 Human 8.2 pKi None 8.2 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 -72 21 Human 8.2 pKi None 8.2 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 -72 21 Human 8.2 pKi None 8.2 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
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
2258 3104 36 None 1 2 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 225 6 3 4 1.1 O[C@H](COc1ccc(cc1)O)CNC(C)C 10531390
2258 3104 36 None 1 2 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 225 6 3 4 1.1 O[C@H](COc1ccc(cc1)O)CNC(C)C 2564629
42396 3104 36 None 1 2 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 225 6 3 4 1.1 O[C@H](COc1ccc(cc1)O)CNC(C)C 10531390
42396 3104 36 None 1 2 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 225 6 3 4 1.1 O[C@H](COc1ccc(cc1)O)CNC(C)C 2564629
537 3104 36 None 1 2 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 225 6 3 4 1.1 O[C@H](COc1ccc(cc1)O)CNC(C)C 10531390
537 3104 36 None 1 2 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 225 6 3 4 1.1 O[C@H](COc1ccc(cc1)O)CNC(C)C 2564629
CHEMBL1160714 3104 36 None 1 2 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 225 6 3 4 1.1 O[C@H](COc1ccc(cc1)O)CNC(C)C 10531390
CHEMBL1160714 3104 36 None 1 2 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 225 6 3 4 1.1 O[C@H](COc1ccc(cc1)O)CNC(C)C 2564629
DB13777 3104 36 None 1 2 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 225 6 3 4 1.1 O[C@H](COc1ccc(cc1)O)CNC(C)C 10531390
DB13777 3104 36 None 1 2 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 225 6 3 4 1.1 O[C@H](COc1ccc(cc1)O)CNC(C)C 2564629
173382 3648 0 None - 1 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 333 8 4 6 2.0 COc1cc(CCNCC(c2ccc(c(c2)O)O)O)ccc1OC 8982677
533 3648 0 None - 1 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 333 8 4 6 2.0 COc1cc(CCNCC(c2ccc(c(c2)O)O)O)ccc1OC 8982677
193122 1871 6 None 3 2 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 283 10 2 5 1.5 COCCOc1ccc(cc1)OCC(CNC(C)C)O 10079020
542 1871 6 None 3 2 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 283 10 2 5 1.5 COCCOc1ccc(cc1)OCC(CNC(C)C)O 10079020
CHEMBL142773 1871 6 None 3 2 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 283 10 2 5 1.5 COCCOc1ccc(cc1)OCC(CNC(C)C)O 10079020
10587912 2772 0 None 12 2 Human 7.1 pKi None 7.1 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 7.1 pKi None 7.1 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 8.0 pKi None 8 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 8.0 pKi None 8 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 8.0 pKi None 8 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 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 323 12 2 5 2.2 OC(COc1ccc(cc1)OCCOCC1CC1)CNC(C)C 10079020
3123920 2774 79 None -2 6 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 209 6 2 3 1.4 OC(COc1ccccc1)CNC(C)C 10079020
546 2774 79 None -2 6 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 209 6 2 3 1.4 OC(COc1ccccc1)CNC(C)C 10079020
CHEMBL7154 2774 79 None -2 6 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 209 6 2 3 1.4 OC(COc1ccccc1)CNC(C)C 10079020
5311116 2293 6 None 54 3 Human 8.5 pKi None 8.5 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 54 3 Human 8.5 pKi None 8.5 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 54 3 Human 8.5 pKi None 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 484 15 5 8 2.2 N#Cc1cc(OCCOCC2CC2)ccc1OCC(CNCCNC(=O)Nc1ccc(cc1)O)O 10079020
2687 874 15 None -1 5 Human 9.1 pKi None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 279 5 4 4 1.0 OC(COc1cccc2c1[nH]c(=O)[nH]2)CNC(C)(C)C 15060759
2687 874 15 None -1 5 Human 9.1 pKi None 9.1 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 9.1 pKi None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 279 5 4 4 1.0 OC(COc1cccc2c1[nH]c(=O)[nH]2)CNC(C)(C)C 15060759
532 874 15 None -1 5 Human 9.1 pKi None 9.1 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 9.1 pKi None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 279 5 4 4 1.0 OC(COc1cccc2c1[nH]c(=O)[nH]2)CNC(C)(C)C 15060759
5387 874 15 None -1 5 Human 9.1 pKi None 9.1 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 9.1 pKi None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 279 5 4 4 1.0 OC(COc1cccc2c1[nH]c(=O)[nH]2)CNC(C)(C)C 15060759
CHEMBL420746 874 15 None -1 5 Human 9.1 pKi None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 279 5 4 4 1.0 OC(COc1cccc2c1[nH]c(=O)[nH]2)CNC(C)(C)C 15655528
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
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
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
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